Page last updated: 2024-11-04

risperidone

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Description

Risperidone is an atypical antipsychotic medication primarily used to treat schizophrenia and bipolar disorder. It is a dopamine and serotonin antagonist, meaning it blocks the action of these neurotransmitters in the brain. Risperidone is effective in reducing the positive symptoms of schizophrenia, such as hallucinations and delusions, and is also effective in treating negative symptoms, such as social withdrawal and apathy. It is also used to treat agitation and aggression in people with dementia, autism, and intellectual disability. Risperidone is synthesized in a multi-step process involving several organic reactions, starting with the precursor 2-(4-fluorophenyl)-1-(4-piperidyl)-ethanone. The compound was first synthesized in the 1980s and has since become one of the most widely prescribed antipsychotic medications. Risperidone is studied extensively to understand its mechanisms of action, optimize its use in various psychiatric disorders, and explore its potential for treating other conditions like Alzheimer's disease and Parkinson's disease.'

Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5073
CHEMBL ID85
CHEBI ID8871
SCHEMBL ID27911
MeSH IDM0028338

Synonyms (222)

Synonym
BIDD:GT0262
AC-1306
AKOS005577302
HMS3393H07
AB00514010-12
AB00514010-11
BRD-K53857191-001-04-5
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[2,1-b]pyrimidin-4-one
gtpl96
okedi
risperidone
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)-1-piperidyl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
106266-06-2
3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperi-dino]ethyl]-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]-pyrimidin-4-one
4h-pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benz-isoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-
r-64766
risperidone-ism
belivon
risperdal m-tab
cp-018 ,
relday
EU-0101074
risperdal consta
rispolept
risperidal
risperidal m-tab
risperin
risperidona [spanish]
3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
r 64766
sequinan
rispolin
brn 4891881
risperidonum [latin]
risperdal
4h-pyrido(1,2-a)pyrimidin-4-one, 6,7,8,9-tetrahydro-3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-2-methyl-
4h-pyrido(1,2-a)pyrimidin-4-one, 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-
c23h27fn4o2
3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino)ethyl)-6,7,8,9-tetrahydro-2-methyl-4h-pyrido(1,2-a)pyrimidin-4-one
NCGC00015883-02
NCGC00015883-01
cas-106266-06-2
lopac-r-118
NCGC00179257-01
MLS001424081
AB00514010
MLS000759429
smr000466323
DB00734
risperdal (tn)
risperidone (jp17/usp/inn)
D00426
NCGC00094352-03
PRESTWICK0_001029
PRESTWICK1_001029
SPBIO_003078
NCGC00094352-02
NCGC00094352-01
r-64,766
r 64,766
MLS001165758
risperidona
3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-6,7,8,9-tetrahydro-4h-pyrido[1,2-a]pyrimidin-4-one
risperidonum
CHEBI:8871 ,
NCGC00015883-03
r 62 766
R-118 ,
HMS2051H07
HMS2089C22
L000510
rcn3028
nsc-759895
CHEMBL85 ,
perseris
ly03004
r 64 766
n05ax08
rcn-3028
ly-03004
r-64-766
HMS1571M19
5-[2-(4-benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-6-methyl-1,3-dihydro-indol-2-one(norastemizole)
3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one (risperidone)
us8802672, risperidone
3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one
(risperidone)3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one
bdbm50001885
3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one (resperidone)
3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one(risperidone)
2-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-6,7,8,8a-tetrahydro-5h-naphthalen-1-one
3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
2-(2-(4-(benzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-7,8,9,9a-tetrahydro-1h-pyrido[1,2-a]pyrimidin-4(6h)-one
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
STK646402
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-6,7,8,9-tetrahydro-4h-pyrido[1,2-a]pyrimidin-4-one
NCGC00015883-05
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)-1-piperidyl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one;risperidone
A801409
HMS2098M19
4h-pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-
R0087
nsc759895
pharmakon1600-01506038
dtxcid6025193
tox21_110253
dtxsid8045193 ,
3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
HMS2233O11
CCG-100930
NCGC00015883-06
NCGC00015883-08
NCGC00015883-04
NCGC00015883-07
zophrenal
psychodal
unii-l6uh7zf8hc
nsc 759895
risperidone [usan:usp:inn:ban]
spiron
l6uh7zf8hc ,
hsdb 7580
apexidone
FT-0631037
PB26023
S1615
HMS3373M18
3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-4h-pyrido(1,2-a)pyrimidin-4-one
risperidone [vandf]
risperidone [mi]
risperidone [usan]
risperidone [jan]
rykindo
risperidone [usp monograph]
risperidone [ep monograph]
risperidone [inn]
uzedy
risperidone [orange book]
risperidone [who-dd]
risperidone [ep impurity]
risperidone [mart.]
risperidone [usp-rs]
risperidone [usp impurity]
risperidone [hsdb]
AB00514010-09
CS-1619
HY-11018
3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimid-in-4-one
3-[2-[4(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl4h-pyrido[1,2-a]pyrimidin-4-one
3-{2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-4h-pyrido[1,2-a]pyrimidin-4-one
3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
3-[2-[4-(6 fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-ethyl]-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4h-pyrido[1,2-a]pyrimidin-4-one
3-[2-[4(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidiny]ethyl]-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
3-[2-[4-(6-fluoro- 1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl4h-pyrido[1,2-a]pyrimidin-4-one
NC00180
SCHEMBL27911
NCGC00015883-11
tox21_110253_1
KS-1106 ,
1026102-43-1
risperidone, british pharmacopoeia (bp) reference standard
HB1740
3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-me thyl-4h-pyrido[1,2-a]pyrimidin-4-one
3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido[1,2-a]pyrimidin-4-one
AB00514010_13
AB00514010_14
mfcd00274576
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4h,6h,7h,8h,9h-pyrido[1,2-a]pyrimidin-4-one
J-001555
risperidone, united states pharmacopeia (usp) reference standard
HMS3657G13
rispen
risperidone, pharmaceutical secondary standard; certified reference material
risperidone, >=98% (hplc), powder
risperidone for system suitability, european pharmacopoeia (ep) reference standard
risperidone, european pharmacopoeia (ep) reference standard
risperidone; 4h-pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl- (9ci); 1,2-benzisoxazole, 4h-pyrido[1,2-a]pyrimidin-4-one deriv.; r 64766; risperdal; spiron
risperidone 1.0 mg/ml in methanol
SR-01000075399-2
SR-01000075399-8
sr-01000075399
HMS3715M19
risperidone(r 64 766)
SW197348-4
3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]ethyl}-6,7,8,9-tetrahydro-2-methylpyrido[1,2-a]pyrimidin-4-one
FT-0674432
BCP08161
Q412443
106266-06-2 (free base)
Z1501480428
risperidone (risperdal)
3-[2-[4-(6-fluoranyl-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
BRD-K53857191-001-10-2
HMS3887G15
3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-ethyl}- 6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
risperidone impurity k
risperidone???
nsc801188
nsc-786035
nsc786035
nsc-801188
EN300-117259
risperidone- bio-x
BR164349
risperidone (usp impurity)
risperidone (ep monograph)
risperidone (usp monograph)
risperidone (usp-rs)
3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido(1,2-a)pyrimidin-4-one
risperidone m-tab
rykindoextended-release microspheres
perseris kit
risperidone (usan:usp:inn:ban)
risperidone (mart.)
risperidonum (latin)
risperidone (ep impurity)
3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino)ethyl)- 6,7,8,9-tetrahydro-2-methyl-4h-pyrido(1,2-a)pyrimidin-4-one
4h-pyrido(1,2-a)pyrimidin-4-one, 6,7,8,9-tetrahydro-3-(2-(4- (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-2- methyl-
risperidone, 1mg/ml in methanol

Research Excerpts

Overview

Risperidone is an effective drug used for the treatment of irritability in children with autism spectrum disorder (ASD) It is a second-generation antipsychotic agent used in psychiatric management, acutely and chronically.

ExcerptReferenceRelevance
"Risperidone ISM® is an effective, safe, and well-tolerated long-term treatment of schizophrenia in adults, regardless of the initial disease severity or whether patients were previously treated with Risperidone ISM® during an acute exacerbation or switched from stable doses of oral risperidone."( Long-term efficacy and safety of once-monthly Risperidone ISM® in the treatment of schizophrenia: Results from a 12-month open-label extension study.
Anta, L; Correll, CU; Filts, Y; Litman, RE; Martínez, J; Naber, D, 2022
)
2.42
"Risperidone is an atypical antipsychotic drug used for the pharmacotherapy of psychiatric disorders. "( Risperidone Toxicity on Human Blood Lymphocytes in Nano molar Concentrations.
Imani, F; Pourahmad, J; Ramezani, M; Salimi, A; Seydi, E; Shirani, K; Yousefsani, BS, 2022
)
3.61
"Risperidone is an effective drug used for the treatment of irritability in children with autism spectrum disorder (ASD). "( A Case of Priapism in a Child With Autism Spectrum Disorder, Possibly Due to Risperidone Treatment With Addition of Atomoxetine.
Bulut, ÖF; Tanir, Y,
)
1.8
"Risperidone is a second-generation antipsychotic agent used in psychiatric management, acutely and chronically. "( Risperidone induced hypotension: A case report and literature review.
Nkemjika, S; Oforeh, K; Saha, A; Singh, S; Wayne, K, 2022
)
3.61
"Risperidone is an antipsychotic medication used in the treatment of conditions like autism and schizophrenia. "( Assessment of Risperidone Toxicity in Zebrafish (
Bailone, RL; Borra, RC; Fukushima, HCS, 2023
)
2.71
"Risperidone is an atypical antipsychotic drug, which is used in schizophrenia and also to treat excitation and aggression in patients with delirium. "( Risperidone-induced anaemia.
Badiger, S; Chaukimath, SP; Chawath, S; Ramdurg, S,
)
3.02
"Risperidone is a second-generation antipsychotic drug metabolized to an active metabolite, 9-hydroxyrisperidone, primarily by cytochrome P450 (CYP) 2D6 and to a lesser extent by CYP3A4. "( CYP2D6 Genetic Polymorphisms and Risperidone Pharmacokinetics: A Systematic Review and Meta-analysis.
Allen, JD; Bishop, JR; Brown, SJ; de Leon, J; Eum, S; Lee, AM; Shan, Y; Zhang, L, 2020
)
2.28
"Risperidone is an atypical antipsychotic drug used increasingly in children to manage symptoms of ADHD and conduct disorder. "( Chronic risperidone administration leads to greater amphetamine-induced conditioned place preference.
Baltes Thompson, EC; Bardgett, ME; Crane, C; Downnen, T; Muncie, B; Pauly, JR; Steffen, SA; Yates, JR, 2020
)
2.44
"Risperidone (RSP) is an atypical antipsychotic drug widely used to treat schizophrenia and bipolar disorder. "( Proteinoid Nanocapsules as Drug Delivery System for Improving Antipsychotic Activity of Risperidone.
Einat, H; Grinberg, I; Lugasi, L; Madar, R; Margel, S; Sabag, R, 2020
)
2.22
"Risperidone is an antagonist, and the charge transfer process is different from dopamine."( Interaction of graphene with antipsychotic drugs: Is there any charge transfer process?
Del Castillo, RM; Martínez, A; Ramos, E, 2021
)
1.34
"Risperidone (RSP) is a commonly used atypical antipsychotic medication, and was therefore selected for encapsulation by proteinoid NPs."( Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity.
Einat, H; Grinberg, I; Lugasi, L; Margel, S; Okun, E; Rudnick-Glick, S, 2020
)
1.52
"Risperidone is a neuroleptic with a potent dopamine D2 and serotonin 5-HT2 receptor-blocking activity as well as a high affinity for adrenergic and histamine H1 receptors."( The Opioid Interactions of the Antipsychotic Medications Risperidone and Amisulpride in Mice and Their Potential Use in the Treatment of Other Non-Psychotic Medical Conditions.
Pick, CG; Schreiber, S, 2021
)
1.59
"Risperidone (RSP) is an atypical antipsychotic drug which acts as a potent antagonist of serotonin-2 (5TH2) and dopamine-2 (D2) receptors in the brain; it is used to treat schizophrenia, behavioral and psychological symptoms of dementia and irritability associated with autism. "( Encapsulation of Risperidone by Methylated β-Cyclodextrins: Physicochemical and Molecular Modeling Studies.
Barvinschi, P; Cîrcioban, D; Ledeți, A; Ledeți, I; Miclău, M; Sbârcea, L; Tănase, IM; Trandafirescu, C; Văruţ, RM; Vlase, G, 2020
)
2.34
"Risperidone is a potent psychotropic agent has been approved for symptomatic treatment of irritability in children and adolescents with autism spectrum disorders. "( Novel risperidone orally disintegrating minitablets for pediatric use: patient acceptance and dose adjustment.
Abdallaha, OY; Bebawy, G; Sokar, M, 2021
)
2.54
"Risperidone is a second-generation atypical antipsychotic and there have been case reports of risperidone-associated deep vein thrombosis, most of them reporting the complication from 2 weeks to a few months of initiation of therapy."( Deep vein thrombosis on the fourth day of risperidone therapy.
George, M; Konnakkaparambil Ramakrishnan, K, 2021
)
1.61
"Risperidone (RSP) is an atypical antipsychotic drug used in treating schizophrenia, behavioral, and psychological symptoms of dementia and irritability associated with autism. "( Risperidone/Randomly Methylated β-Cyclodextrin Inclusion Complex-Compatibility Study with Pharmaceutical Excipients.
Barvinschi, P; Cîrcioban, D; Ledeți, A; Ledeți, I; Miclău, M; Sbârcea, L; Suciu, O; Tănase, IM; Văruţ, RM; Vlase, G, 2021
)
3.51
"Risperidone is an atypical antipsychotic agent clinically used to treat schizophrenia, bipolar diseases, and autism. "( Determining the release kinetics of risperidone controlled release matrices to treat schizophrenia.
Akhtar, H; Ali, MM; Ali, SI; Arif, H; Inayat, S; Iqbal, MS; Kashif, SS; Naz, A; Nisa, Z; Perveen, S; Rizvi, M; Shahnaz, S; Sheikh, S; Swaleh, MM; Zehra, A, 2021
)
2.34
"Risperidone is a weak basic drug sparingly soluble in water frequently used to treat patients suffering of schizophrenia."( A method to slow down the ionization-dependent release of risperidone loaded in a thermoresponsive poly(N-acryloyl glycinamide) hydrogel.
Boustta, M; Vert, M, 2017
)
1.42
"Risperidone is an antipsychotic drug. "( Influence of Antipsychotic Drug Risperidone on Human Serum Albumin Affinity to Organic Anions.
Dobretsov, G; Kondratyuk, V; Smolina, N; Syrejshchikova, T; Uzbekov, M, 2018
)
2.21
"Risperidone is a widely accessible antipsychotic that can be used to manage psychosis-induced aggression or agitation."( Risperidone for psychosis-induced aggression or agitation (rapid tranquillisation).
Adams, CE; Ahmed, U; Hussein, M; Miramontes, K; Ostinelli, EG; Rehman, FU, 2018
)
2.64
"Risperidone is a promising drug to manage children with choreoathetoid cerebral palsy and is well tolerated in children."( Effect of Risperidone on the Motor and Functional Disability in Children With Choreoathetoid Cerebral Palsy.
Kamate, M; Metgud, D; Mittal, N, 2018
)
2.33
"Risperidone is an antipsychotic drug approved for use in children, but little is known about the long-term effects of early-life risperidone treatment. "( Adult rats treated with risperidone during development are hyperactive.
Bardgett, ME; Colemire, KR; Franks-Henry, JM; Griffith, MS; Juneau, KR; Marczinski, CA; Stevens, RM, 2013
)
2.14
"Risperidone is an antipsychotic medication suspected of causing QT prolongation and several cases are reported in this regard. "( Risperidone and corrected QT-interval prolongation in surface electrocardiogram.
Abbasnejhad, M; Ahmadi, NM; Akbarzadeh, F; Ranjbar, F, 2012
)
3.26
"Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. "( Optimization and in vivo toxicity evaluation of G4.5 PAMAM dendrimer-risperidone complexes.
Arévalo Arévalo, R; Carreño Gutierrez, H; Chiaramoni, NS; del Rio Zabala, NE; del Valle Alonso, S; Marotta, CH; Prieto, MJ, 2014
)
2.08
"Risperidone (RIS) is a frequently used efficacious psychotropic drug. "( Effect of risperidone metabolism and P-glycoprotein gene polymorphism on QT interval in patients with schizophrenia.
Fukui, N; Inoue, Y; Ono, S; Saito, M; Someya, T; Sugai, T; Suzuki, Y; Tsuneyama, N; Watanabe, J, 2014
)
2.25
"Risperidone is a poorly water soluble atypical antipsychotic drug. "( Effervescent tablet formulation for enhanced patient compliance and the therapeutic effect of risperidone.
Ghorab, MM; Ibrahim, HK; Mohammed, KA, 2016
)
2.1
"Risperidone is an antipsychotic drug that is approved for use in childhood psychiatric disorders such as autism. "( Early-life risperidone administration alters maternal-offspring interactions and juvenile play fighting.
Bardgett, ME; Brown, CJ; Gannon, MA; Griffith, MS; Marczinski, CA; Stevens, RM, 2015
)
2.25
"Risperidone is a common psychopharmacological treatment for irritability in autism spectrum disorder (ASD). "( Initial severity and efficacy of risperidone in autism: Results from the RUPP trial.
Furukawa, TA; Goldberg, Y; Kodesh, A; Kolevzon, A; Leucht, S; Levine, SZ; Reichenberg, A, 2016
)
2.16
"Risperidone is a second-generation antipsychotic that causes weight gain. "( Risperidone-induced weight gain is mediated through shifts in the gut microbiome and suppression of energy expenditure.
Bahr, SM; Burnett, CM; Castro, AN; deLeon, O; Grobe, JL; Kirby, JR; Murry, DJ; Pearson, NA; Walsh, JW; Weidemann, BJ, 2015
)
3.3
"Risperidone is a second-generation antipsychotic agent commonly used in the treatment of ~ 31.1% of schizophrenia patients in China, it is the most commonly-prescribed antipsychotic agent. "( Population pharmacokinetic-pharmacodynamic (PopPK/PD) modeling of risperidone and its active metabolite in Chinese schizophrenia patients.
Deng, C; Ji, S; Li, A; Li, L; Li, X; Lu, W; Shang, D; Wang, C; Wu, K; Zhou, T, 2016
)
2.11
"Risperidone is an atypical antipsychotic widely prescribed for the treatment of behavior problems in children with autism spectrum disorder."( Risperidone-induced priapism in an autistic child: a case report.
Aabbassi, B; Asri, F; Benali, A, 2016
)
2.6
"Risperidone (RIS) is a widely used atypical antipsychotic drug. "( Development and Validation of Liquid Chromatography/Tandem Mass Spectrometry Analysis for Therapeutic Drug Monitoring of Risperidone and 9-Hydroxyrisperidone in Pediatric Patients with Autism Spectrum Disorders.
Hongkaew, Y; Limsila, P; Nakorn, CN; Ngamsamut, N; Nuntamool, N; Prommas, S; Puangpetch, A; Sukasem, C; Vanwong, N, 2016
)
2.08
"Risperidone (Ris) is a second-generation antipsychotic (SGA) used to treat patients with schizophrenia. "( Effect of risperidone on plasma d-serine concentration in rats post-administered with d-serine.
Fukushima, T; Hakariya, H; Ichiba, H; Iizuka, H; Ishimaru, K; Nagashima, C; Nakazawa, H; Onozato, M; Sakamoto, T; Shishikura, M, 2016
)
2.28
"Risperidone is an atypical antipsychotic used in the treatment of schizophrenia and of symptoms of irritability associated with autism spectrum disorder (ASD). "( Two Binding Geometries for Risperidone in Dopamine D3 Receptors: Insights on the Fast-Off Mechanism through Docking, Quantum Biochemistry, and Molecular Dynamics Simulations.
Bezerra, EM; Caetano, EW; da Costa, RF; Della Flora Nunes, G; Freire, VN; Gottfried, C; Martins, A; Zanatta, G, 2016
)
2.17
"Risperidone is a widely used, second-generation antipsychotic approved for treating schizophrenia as well as for treating aggression in children and adolescents with mental retardation. "( Mild Hypothermia in a Child with Low-Dose Risperidone.
Denzer, C; Freudenmann, RW; Gahr, M; Grau, K; Plener, PL, 2017
)
2.16
"Risperidone is a relatively well-tolerated compound when it is prescribed at doses lower than 4 mg/d."( [Atypical antipsychotics in first-episode psychosis: a review].
Aouizerate, B; Rotgé, JY; Tignol, J, 2008
)
1.07
"Risperidone is a commonly prescribed antipsychotic drug. "( Simultaneous determination of risperidone and 9-hydroxyrisperidone enantiomers in human blood plasma by liquid chromatography with electrochemical detection.
Grabnar, I; Locatelli, I; Mrhar, A, 2009
)
2.08
"Risperidone (RSP) is a second generation anti-psychotic drug used for the treatment of schizophrenia and anxiety disorders. "( Time resolved analysis of risperidone and 9-hydroxy-risperidone in hair using LC/MS-MS.
Mühe, A; Neels, H; Schneider, S; Sibille, E; Wennig, R; Yegles, M, 2009
)
2.1
"Risperidone is proven to be an efficient product."( [Complex therapy of schizophrenia].
Gaszner, P, 2009
)
1.07
"Risperidone is a widely used antipsychotic drug for people with schizophrenia. "( Risperidone dose for schizophrenia.
Li, C; Wang, J; Xia, J, 2009
)
3.24
"Risperidone is an atypical antipsychotic drug that is widely prescribed to young patients with different psychotic disorders. "( Effects of repeated risperidone exposure on serotonin receptor subtypes in developing rats.
Choi, YK; Gardner, MP; Moran-Gates, T; Tarazi, FI, 2010
)
2.13
"Risperidone is an established cause of priapism."( Priapism and risperidone.
Koirala, S; Lippmann, S; Penagaluri, P; Smith, C, 2009
)
1.44
"Risperidone is a widely used atypical antipsychotic agent that produces considerable interindividual differences in patient response. "( Genetic variants in the BDNF gene and therapeutic response to risperidone in schizophrenia patients: a pharmacogenetic study.
Feng, G; Gao, R; He, L; Li, S; Lin, Z; St Clair, D; Xing, Q; Xu, M, 2010
)
2.04
"Risperidone is an effective short-term pharmacologic agent for controlling steroid-related psychiatric adverse effects when cessation or dose reduction of steroid therapy is not an option."( Concurrent treatment of steroid-related mood and psychotic symptoms with risperidone.
Dahl, G; Shaw, RJ; Tzuang, D; Ularntinon, S, 2010
)
1.31
"Risperidone is an antipsychotic commonly used during pregnancy. "( Risperidone inhibits contractions induced by serotonin and histamine and reduces K+ currents in smooth muscle of human umbilical artery.
Enrique, N; Iveli, MF; Martín, P; Milesi, V; Rebolledo, A; Rimorini, L; Roldán Palomo, AR; Salemme, S, 2010
)
3.25
"Risperidone is a widely prescribed drug in psychiatric practice and has a-blocking actions as well as strong affinity for serotonin 2A receptors. "( Intraoperative floppy iris syndrome associated with risperidone intake.
Ford, RL; Sallam, A; Towler, HM,
)
1.82
"Risperidone is a promising agent for the treatment of schizophrenia, Tourette's disorder, mood disorders, and disruptive behavior disorders in young populations. "( Six months of treatment with risperidone may be associated with nonsignificant abnormalities of liver function tests in children and adolescents: a longitudinal, observational study from Turkey.
Erdogan, A; Karaman, MG; Kurcer, MA; Ozdemir, E; Tufan, AE; Yurteri, N, 2010
)
2.09
"Risperidone (RSP) is a benzisoxazole antipsychotic agent used to treat schizophrenia and other psychiatric illnesses in adults and children (including those with autism). "( Relative bioavailability of two oral formulations of risperidone 2 mg: A single-dose, randomized-sequence, open-label, two-period crossover comparison in healthy Brazilian volunteers.
Belotto, KC; Ferreira, AS; Gattaz, WF; Raposo, NR, 2010
)
2.05
"Risperidone is an atypical antipsychotic that displays antidepressant properties due to its activity at various serotonergic and dopaminergic receptors. "( Use of risperidone as augmentation treatment for major depressive disorder.
Brown, JN; Brown, LT; Owenby, RK, 2011
)
2.27
"Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. "( Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer-risperidone complexes.
Alonso, Sdel V; del Río Zabala, NE; Marotta, CH; Prieto, MJ; Temprana, CF, 2011
)
2.05
"Risperidone (RIS) is a benzisoxazole derivative, an atypical neuroleptic used in the treatment of schizophrenia and other psychoses. "( [The review of acute risperidone poisoning].
Ciszowski, K; Szpak, D; Wilimowska, J, 2010
)
2.12
"Risperidone is an atypical antipsychotic agent used for the treatment of schizophrenia. "( Effect of cytochrome P450 3A4 inhibitor ketoconazole on risperidone pharmacokinetics in healthy volunteers.
Boonleang, J; Mahatthanatrakul, W; Pipatrattanaseree, W; Ridtitid, W; Rujimamahasan, N; Sriwiriyajan, S; Wongnawa, M, 2012
)
2.07
"Risperidone is an atypical antipsychotic drug with potent serotonin and moderate dopamine antagonistic properties. "( Comparative pharmacokinetics and bioequivalence of two tablet formulations of 2 mg risperidone in healthy Thai male volunteers.
Khorana, N; Lohitnavy, O; Maphanta, S; Sayasathid, J; Srichaiya, A, 2011
)
2.04
"Risperidone is an atypical antipsychotic drug used to treat many psychiatric disorders."( Risperidone interacts with serum albumin forming complex.
Cortez, CM; Cruz, FA; Fragoso, VM; Silva, D, 2012
)
2.54
"Risperidone is a second generation antipsychotic agent, with potent serotonin 5-HT2A and dopamine D2 receptor blocking effects. "( Risperidone in the treatment of schizophrenia.
Bravo-Mehmedbasic, A, 2011
)
3.25
"Risperidone is an atypical antipsychotic drug that may increase the risk of stroke."( Risperidone enhances the vulnerability to stroke in hypertensive rats.
Godfraind, T; Liu, C; Song, SW; Su, BL; Su, DF; Sun, Y; Yang, C, 2012
)
2.54
"Risperidone is a potent antagonist of both dopamine and serotonin receptors. "( Functional analysis of gene expression in risperidone treated cells provide new insights in molecular mechanism and new candidate genes for pharmacogenetic studies.
Bernardo, M; Gassó, P; Lafuente, A; Mas, S, 2013
)
2.1
"Risperidone is a benzisoxazole derivate and is effective in the treatment of schizophrenia and other psychiatric illnesses in adults and children. "( Bioequivalence and pharmacokinetic evaluation of two formulations of risperidone 2 mg : an open-label, single-dose, fasting, randomized-sequence, two-way crossover study in healthy male Chinese volunteers.
Jia, JY; Li, SJ; Liu, GY; Liu, Y; Liu, YM; Wang, W; Weng, LP; Yu, C; Zhang, MQ, 2013
)
2.07
"Risperidone appears to be an adequately tolerated and effective treatment in children with subaverage IQs and severe disruptive behaviors such as aggression and destructive behavior."( Effects of risperidone on conduct and disruptive behavior disorders in children with subaverage IQs.
Aman, M; Binder, C; Carroll, A; Fisman, S; Snyder, R; Turgay, A, 2002
)
2.15
"Risperidone is a novel and atypical agent with a dual antagonistic effect on 5-HT and D receptors. "( Risperidone-induced obsessive-compulsive symptoms: a series of six cases.
Alevizos, B; Christodoulou, GN; Lykouras, L; Zervas, IM, 2002
)
3.2
"1. Risperidone is an atypical antipsychotic drug that possesses 5-hydroxytryptamine 5-HT2 receptor antagonism combined with milder dopamine D2 receptor antagonism. "( Peripheral injection of risperidone, an atypical antipsychotic, alters the bodyweight gain of rats.
Fujiwara, K; Itoh, M; Kaneko, YS; Mori, K; Nagasaka, A; Nakashima, A; Ota, A; Ota, M, 2002
)
1.24
"Risperidone is a cytochrome P450 (CYP2D6) enzyme substrate and weak inhibitor and a CYP3A4 substrate."( Reversible coma caused by risperidone-ritonavir interaction.
Andreu, L; Cuadrado, JM; Jover, F; Merino, J,
)
1.15
"Risperidone (RIS) is a novel antipsychotic agent whose pharmacokinetics have yet to be fully determined. "( Sequential changes in the plasma concentration of risperidone following intentional overdose.
Nakanishi, T; Nishikage, H; Takamitsu, Y; Yamamoto, J,
)
1.83
"Risperidone is an atypical anti-psychotic medication with both 5HT2 receptor and D2 dopamine receptor antagonism. "( Risperidone and megacolon.
Lim, DK; Mahendran, R, 2002
)
3.2
"Risperidone is an atypical neuroleptic which has been incriminated as a cause of respiratory symptoms. "( [Respiratory effects of risperidone? A prospective study].
Antonini, MT; Bonnaud, F; Bourlot, D; Dalmay, F; Lombertie, E; Touraine, F; Trarieux, AM, 2003
)
2.07
"Risperidone is a widely used atypical antipsychotic with certain advantages over typical antipsychotics. "( Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone.
Ikeda, M; Iwata, N; Kitajima, T; Ozaki, N; Suzuki, T; Yamanouchi, Y, 2003
)
2
"Risperidone is a widely used agent as first-line treatment in schizophrenia with a favorable side-effect profile. "( Reduced short-term obsessive-compulsive symptoms in schizophrenic patients treated with risperidone: a single-blind prospective study.
Bayraktar, E; Ercan, ES; Kayahan, B; Varan, A; Veznedaroglu, B, 2003
)
1.98
"Risperidone appeared to be a very weak inhibitor of 3-N-demethylation and 8-hydroxylation (Ki = 202.5 microM) and had no effect on 1-N- and 7-N-demethylation of caffeine."( Influence of classic and atypical neuroleptics on caffeine oxidation in rat liver microsomes.
Daniel, WA; Kot, M; Wójcikowski, J,
)
0.85
"Risperidone is an atypical antipsychotic agent with efficacy for both positive and negative symptoms of schizophrenia. "( Effects of dopamine D2 receptor Ser311Cys polymorphism and clinical factors on risperidone efficacy for positive and negative symptoms and social function.
Chang, WH; Chang, YC; Huang, CH; Lane, HY; Lee, CC; Lu, CT, 2004
)
1.99
"Risperidone is an atypical antipsychotic agent with efficacy for both positive and negative symptoms of schizophrenia. "( Dopamine D3 receptor Ser9Gly polymorphism and risperidone response.
Chang, WH; Chang, YC; Hsu, SK; Huang, CH; Lane, HY; Liu, YC, 2005
)
2.03
"Risperidone is an atypical antipsychotic commonly used for treatment of schizophrenia and other psychotic disorders. "( Interpreting serum risperidone concentrations.
Boerth, JM; Caley, CF; Goethe, JW, 2005
)
2.1
"Risperidone is a frequently used member of a new class of atypical antipsychotics-the serotonin-dopamine antagonists (SDAs)-due to its comparatively high efficacy and low D2/5HT2 binding ratio, which results in a low incidence of extrapyramidal side effects including tardive dyskinesia (TD). "( Risperidone withdrawal-related respiratory dyskinesia: a case diagnosed by spirography and fibroscopy.
Arai, H; Inoue, Y; Kirino, E; Komatsu, S,
)
3.02
"Risperidone (Risperdal) is an atypical antipsychotic with high affinity for 5-hydroxytryptamine (5-HT)2A, dopamine D2 and alpha1- and alpha2-adrenergic receptors. "( Risperidone: a review of its use in the treatment of bipolar mania.
Fenton, C; Scott, LJ, 2005
)
3.21
"LA risperidone is a dominant strategy compared with both olanzapine and haloperidol depot."( [Cost-effectiveness analysis of schizophrenic patient care settings: impact of an atypical antipsychotic under long-acting injection formulation].
Casadebaig, F; Chicoye, A; Durand-Zaleski, I; Guillon, P; Jasso Mosqueda, G; Lançon, C; Llorca, PM; Mehnert, A; Miadi-Fargier, H; Omnès, LF; Philippe, A,
)
0.65
"Risperidone is an effective and well-tolerated treatment for BPSD in routine clinical practice."( Effects of risperidone on behavioral and psychological symptoms associated with dementia in clinical practice.
Kurz, A; Schmitt, A; Schwalen S, S, 2005
)
2.16
"Risperidone is an atypical neuroleptic drug widely used due to the lower incidence and severity of hepatic adverse effects in comparison to phenothiazines. "( Acute cholestatic hepatitis probably associated with risperidone.
Bosacoma Ros, N; Climent Grana, E; Hernández Prats, C; Llinares Tello, F; Navarro Polo, JN; Ordovás Baines, JP; Pérez Martínez, E, 2005
)
2.02
"Risperidone is an atypical antipsychotic drug used for the treatment of schizophrenia. "( Delayed respiratory depression after risperidone overdose.
Akyol, A; Erciyes, N; Karip, F; Senel, AC; Ulusoy, H, 2005
)
2.04
"Risperidone is a second-generation antipsychotic that lacks acute motor side effects at low doses (<6 mg/day), but above this level is associated with parkinsonism and akathesia. "( Multidose risperidone treatment evaluated in a rodent model of tardive dyskinesia.
Cooper, T; Gao, XM; Suckow, RF; Tamminga, CA, 2006
)
2.18
"Risperidone appears to be a safer antipsychotic drug in the long term, with regard to the risk of alterations in glucose and lipid metabolism."( [Therapy with antipsychotic drugs as a risk factor for diabetes in schizophrenia: a case-control study].
Burón, JA; Gómez-de-la-Cámara, A; Ledesma, F; Martínez-Junquera, G; Rodríguez-Morales, A; Rubio, G, 2006
)
1.06
"Risperidone is an atypical anti-psychotic, available in various formulations."( Lack of bioequivalence between generic risperidone oral solution and originator risperidone tablets.
Piniella, PM; Relleke, M; van Os, S, 2007
)
2.05
"Risperidone is a second-generation antipsychotic agent widely used in the treatment of schizophrenia and other psychotic disorders in adults. "( Plasma pharmacokinetic characteristics of risperidone and their relationship to saliva concentrations in children with psychiatric or neurodevelopmental disorders.
Aman, MG; Lindsay, RL; Malone, K; Mannaert, E; Masty, J; Ramadan, Y; Remmerie, B; Vinks, AA, 2007
)
2.05
"Risperidone is a widely used atypical antipsychotic medication and there is currently considerable interest in individual differences in patient response to it. "( Dopamine transporter polymorphisms and risperidone response in Chinese schizophrenia patients: an association study.
Du, J; Feng, G; He, L; Li, X; Lin, Z; Wang, L; Xing, Q; Yu, L; Zhang, A, 2007
)
2.05
"Risperidone is an atypical antipsychotic drug with combined dopamine-2/serotonin-2 (D(2)/5-HT(2)) antagonist activity that has been effective in reducing cocaine use in some animal studies."( A randomized, double-blind, placebo-controlled trial of long-acting risperidone in cocaine-dependent men.
Angarita, GA; Culhane, MA; Evins, AE; Huang, KL; Lee, SH; Loebl, T; Logvinenko, T; Nino, J; Pachas, GN, 2008
)
1.3
"Risperidone (Risperdal) is a novel antipsychotic drug, with beneficial effects on both positive and negative symptoms of schizophrenia, and with a low incidence of extrapyramidal side effects (EPS). "( Occupancy of central neurotransmitter receptors by risperidone, clozapine and haloperidol, measured ex vivo by quantitative autoradiography.
Janssen, PF; Leysen, JE; Megens, AA; Schotte, A, 1993
)
1.98
"Risperidone is a safe antipsychotic that is effective against both the positive and negative symptoms of schizophrenia."( Risperidone in the treatment of schizophrenia.
Marder, SR; Meibach, RC, 1994
)
3.17
"Risperidone is a serotonin/dopamine antipsychotic which differs in important ways from established antipsychotics. "( Risperidone: integrating research and practice.
Addington, D,
)
3.02
"Risperidone is a new benzisoxazole antipsychotic. "( Regional brain distribution of risperidone and its active metabolite 9-hydroxy-risperidone in the rat.
Geerts, RJ; Heykants, JJ; Leysen, JE; Megens, AA; Meuldermans, WE; van Beijsterveldt, LE; Van den Eynde, HM, 1994
)
2.02
"Risperidone is a new antipsychotic drug with high affinity in vitro for both central 5-HT2 and D2 receptors."( Positron emission tomography studies on D2 and 5-HT2 receptor binding in risperidone-treated schizophrenic patients.
Ericsson, B; Farde, L; Halldin, C; Nakashima, Y; Nyberg, S; Oxenstierna, G, 1995
)
1.24
"Risperidone is an effective antipsychotic with a good safety profile."( Antipsychotic medication in the treatment of schizophrenia.
Kane, JM, 1995
)
1.01
"Risperidone is a benzisoxazole derivative with antipsychotic activity that is chemically unrelated to other currently available antipsychotic agents. "( A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5-HT2 and dopamine D2 receptors.
He, H; Richardson, JS, 1995
)
1.98
"Risperidone is a recently introduced neuroleptic distinguished by a decreased incidence of extrapyramidal side effects (EPS). "( The D2 dopamine receptor occupancy of risperidone and its relationship to extrapyramidal symptoms: a PET study.
Houle, S; Kapur, S; Remington, G; Wilson, AA; Zipursky, RB, 1995
)
2
"Risperidone is an effective treatment for positive symptoms of schizophrenia and may be effective for negative symptoms. "( Risperidone: review and assessment of its role in the treatment of schizophrenia.
Cardoni, AA, 1995
)
3.18
"Risperidone is a useful addition to the antipsychotic drug armamentarium, but it should be viewed as an atypical antipsychotic agent. "( Risperidone: review and assessment of its role in the treatment of schizophrenia.
Cardoni, AA, 1995
)
3.18
"Risperidone is an effective antipsychotic for the treatment of chronic schizophrenia; doses of 4 and 8 mg seem to be optimal and have a lower incidence of side-effects than haloperidol."( Risperidone in the treatment of patients with chronic schizophrenia: a multi-national, multi-centre, double-blind, parallel-group study versus haloperidol. Risperidone Study Group.
Peuskens, J, 1995
)
3.18
"Risperidone is a new-generation atypical antipsychotic agent with potent dopaminergic and serotonergic antagonist activity. "( Risperidone in the treatment of affective illness and obsessive-compulsive disorder.
Jacobsen, FM, 1995
)
3.18
"Risperidone is a highly potent and selective serotonin2 and dopamine2 receptor antagonist with a side effect profile that appears to be much more tolerable and safer than that of typical neuroleptics."( Risperidone addition in fluvoxamine-refractory obsessive-compulsive disorder: three cases.
Epperson, CN; Fleischmann, RL; Leckman, JF; McDougle, CJ; Price, LH; Wasylink, S, 1995
)
2.46
"Risperidone is an investigational antipsychotic agent currently being tested in an international multicenter drug trial. "( Overdose of risperidone.
Brenner, C; Brown, K; Hamburg, EL; Leffler, S; Levy, H, 1993
)
2.11
"Risperidone appears to be an effective and well tolerated antipsychotic for elderly patients with chronic psychosis."( Outcome of risperidone therapy in elderly patients with chronic psychosis.
Brescan, D; Jurjus, G; Ramirez, LF; Sajatovic, M; Simon, M; Vernon, L, 1996
)
2.13
"Risperidone is a recently approved atypical antipsychotic that offers the advantages over existing typical antipsychotics of improved efficacy against negative symptoms and a decreased incidence of extrapyramidal side effects. "( Development and implementation of drug use evaluation (DUE) criteria for risperidone in an outpatient psychiatric setting.
Gross, LS; Gutierrez, MA; Shepski, JC; Wincor, MZ, 1996
)
1.97
"Risperidone (Risperdal) is a recently released novel antipsychotic medication. "( Acute risperidone overdose.
Catalano, G; Catalano, MC; Taylor, W, 1997
)
2.22
"Risperidone is a novel and clinically effective atypical antipsychotic medication with a unique biochemical profile. "( Adverse effects of risperidone on eye movement activity: a comparison of risperidone and haloperidol in antipsychotic-naive schizophrenic patients.
Bauer, KS; Haas, GL; Keshavan, MS; Kroboth, PD; Schooler, NR; Sweeney, JA, 1997
)
2.07
"Risperidone is a novel atypical neuroleptic with a favorable profile of side effects due to its unique pharmacological activity: it exhibits both potent dopamine D2 and 5-HT2 receptor blocking activity, as well as high affinity for alpha1 and alpha2 adrenergic receptors and histamine H1 receptor. "( Augmentation of opioid induced antinociception by the atypical antipsychotic drug risperidone in mice.
Backer, MM; Pick, CG; Schreiber, S; Weizman, R, 1997
)
1.97
"Risperidone is a newly available atypical antipsychotic agent that has been reported to be associated with fewer extrapyramidal side effects (EPS) than conventional neuroleptics in adults with schizophrenia. "( Risperidone in the treatment of children and adolescents with schizophrenia: a retrospective study.
Findling, RL; Friedman, L; Grcevich, SJ; Rowane, WA; Schulz, SC, 1996
)
3.18
"Risperidone may prove to be an effective alternative to haloperidol in delirious patients, especially the elderly and the severely medically ill, who are more prone to adverse effects."( Use of risperidone in delirium: case reports.
Masand, PS; Sipahimalani, A, 1997
)
1.47
"Risperidone is an antipsychotic drug with high affinity at dopamine D2 and serotonin 5-HT2 receptors. "( Extrapyramidal side effects with risperidone and haloperidol at comparable D2 receptor occupancy levels.
Heinz, A; Knable, MB; Raedler, T; Weinberger, DR, 1997
)
2.02
"Risperidone is an antipsychotic drug used for the treatment of schizophrenia. "( Risperidone-induced neuroleptic malignant syndrome.
Bajjoka, I; O'Sullivan, T; Patel, T, 1997
)
3.18
"Risperidone is a novel serotonin-dopamine antagonist antipsychotic in a class of benzisoxazole derivative which has been shown to be effective in reducing psychotic symptoms in schizophrenia. "( Efficacy and tolerability of risperidone in chronic schizophrenic Thai patients.
Bunditchate, A; Chaisirikul, S; Charisilp, C; Chrujiporn, W; Kessawai, D; Ratanachata, N; Sanichwannakul, K; Ukranand, P; Visanuyothin, T; Wangdee, P; Werapongset, W, 1998
)
2.03
"Risperidone is a relatively new antipsychotic drug that has been reported to improve both the positive and the negative symptoms of schizophrenia and produces relatively few extrapyramidal side effects at low doses. "( Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4.
Baker, GB; Bourin, M; Fang, J, 1999
)
2.11
"Risperidone is an atypical antipsychotic drug that has been used in the treatment of numerous psychiatric disorders in children and adolescents. "( Risperidone-induced hepatotoxicity in children and adolescents? A chart review study.
Branicky, LA; Findling, RL; Maxwell, K; Szigethy, E; Wiznitzer, M, 1999
)
3.19
"Risperidone is a dopaminergic as well as a 5-HT2 antagonist. "( Some behavioural effects of risperidone in rats: comparison with haloperidol.
Chodera, A; Kus, K; Nowakowska, E; Rybakowski, J, 1999
)
2.04
"Risperidone is an atypical antipsychotic that has been investigated as a treatment for several severe psychiatric disorders in children and adults. "( Separation anxiety in children and adolescents treated with risperidone.
Fischer, DJ; Fluent, TE; Hanna, GL, 1999
)
1.99
"Risperidone is a relatively new antipsychotic available world-wide since the early 1990s. "( Focus on risperidone.
Green, B, 2000
)
2.17
"Risperidone is a heterocyclic neuroleptic with prominent antiserotoninergic (5HT2) as well as antidopaminergic (D2) activity. "( Risperidone in idiopathic and symptomatic dystonia: preliminary experience.
Grassi, E; Latorraca, S; Marini, P; Piacentini, S; Sorbi, S, 2000
)
3.19
"Risperidone is a benzisoxazole derivative which has proven efficacy against the positive and negative symptoms of schizophrenia. "( Risperidone: a review of its use in the management of the behavioural and psychological symptoms of dementia.
Bhana, N; Spencer, CM, 2000
)
3.19
"Risperidone is a potent inducer of hyperprolactinemia in outpatients with schizophrenia in a community population. "( Risperidone-associated hyperprolactinemia.
Daniels, GH; Goff, DC; Hayden, DL; Kearns, AE,
)
3.02
"Risperidone is a novel antipsychotic agent that blocks both dopaminergic and serotonergic receptors. "( Use of the dopamine agonists bromocriptine and cabergoline in the management of risperidone-induced hyperprolactinemia in patients with psychotic disorders.
Tollin, SR, 2000
)
1.98
"Risperidone is an "atypical" antipsychotic with strong binding affinity for dopamine-2 and serotonin-2 receptors. "( Safety and tolerability of a rapidly escalating dose-loading regimen for risperidone.
Feifel, D; Moutier, CY; Perry, W, 2000
)
1.98
"Risperidone is a new efficacious antipsychotic with a low propensity for extrapyramidal side effects."( Risperidone versus pimozide in Tourette's disorder: a comparative double-blind parallel-group study.
Bruggeman, R; Buitelaar, JK; Gericke, GS; Hawkridge, SM; Temlett, JA; van der Linden, C, 2001
)
2.47
"Risperidone is an atypical antipsychotic drug that blocks dopamine as well as serotonin receptor systems. "( A randomized controlled trial of risperidone in the treatment of aggression in hospitalized adolescents with subaverage cognitive abilities.
Buitelaar, JK; Cohen-Kettenis, P; Melman, CT; van der Gaag, RJ, 2001
)
2.03
"Risperidone is an atypical antipsychotic agent with dopamine and serotonin antagonistic effects. "( Risperidone for controlling aggressive behavior in a mentally retarded child: a case report.
Intaprasert, S; Maneeton, N; Srisurapanont, M, 2001
)
3.2
"Risperidone is an antipsychotic drug with a combined effect as a dopamine antagonist and a 5-HT2A receptor antagonist."( [Risperidone as a tool to control hard aggression].
Heitun, OG, 2001
)
1.94
"Risperidone is an atypical antipsychotic with a low prevalence of extrapyramidal side-effects. "( [Mania, parkinson disease and risperidone. Case report].
Monreal, JA; Staner, L,
)
1.86
"Risperidone appears to be a more effective and better tolerated antipsychotic drug in treatment-refractory Chinese schizophrenia than haloperidol."( Risperidone versus haloperidol in the treatment of acute exacerbations of chronic inpatients with schizophrenia: a randomized double-blind study.
Cao, LY; Shen, YC; Wu, GY; Zhang, PY; Zhang, XY; Zhou, DF, 2001
)
2.47
"Risperidone is an atypical antipsychotic drug which has been suggested to be beneficial for the treatment of elderly patients with psychotic symptoms. "( The efficacy and safety of risperidone for the treatment of geriatric psychosis.
Chang, JW; Cheng, CY; Hwang, JP; Tsai, SJ; Yang, CH; Yu, HC, 2001
)
2.05
"Risperidone is an atypical antipsychotic medication commonly used to treat psychotic illnesses in adults. "( Atypical antipsychotic overdose in the pediatric population.
Catalano, G; Catalano, MC; Nunez, CY; Walker, SC, 2001
)
1.75
"Risperidone appears to be an effective therapy, but several authors report cases of TD during treatment."( Tardive dyskinesias and antipsychotics: a review.
Bayle, FJ; Chereau, I; Lancon, C; Llorca, PM, 2002
)
1.04
"Risperidone is an atypical antipsychotic drug that increases plasma norepinephrine (NE) levels, but the mechanism behind this effect is unclear. "( Effects of risperidone on the peripheral noradrenegic system in patients with schizophrenia: a comparison with clozapine and placebo.
Breier, A; Eisenhofer, G; Elman, I; Folio, CJ; Goldstein, DS; Green, AI; Holmes, CS; Pickar, D, 2002
)
2.15
"Risperidone is an atypical antipsychotic used in the treatment of several psychiatric disorders in both children and adults. "( Side-effects of risperidone therapy mimicking cerebrospinal fluid shunt malfunction: implications for clinical monitoring and management.
Edwards, RJ; Pople, IK, 2002
)
2.1
"Risperidone is a new benzisoxazole derivative displaying a very potent serotonin antagonism and a potent dopamine antagonism in pharmacological studies. "( Efficacy and tolerability of a new antipsychotic compound (risperidone): results of a pilot study.
Kissling, W; Möller, HJ; Pelzer, E; Riehl, T; Wernicke, T, 1991
)
1.97

Effects

Risperidone has a high affinity for 5-HT2 and D2 dopamine receptors in vitro. It has a low risk of haematotoxicity because of its different chemical and pharmacological profile compared to clozapine.

Risperidone has been approved by the Food and Drug Administration for the treatment of schizophrenia in the adolescent population. It has a relatively higher affinity for the D(2) receptor in comparison with other atypical antipsychotics, which may explain why it is associated with a higher incidence of hyperprolactinemia.

ExcerptReferenceRelevance
"Risperidone has a low risk of haematotoxicity because of its different chemical and pharmacological profile compared to other drugs such as clozapine."( Risperidone-induced anaemia.
Badiger, S; Chaukimath, SP; Chawath, S; Ramdurg, S,
)
2.3
"Risperidone has a hyperbolic mixed-type inhibition, designated as 'partial uncompetitive inhibition effect', with K(i) value of 41 microM on human DAO."( The effect of risperidone on D-amino acid oxidase activity as a hypothesis for a novel mechanism of action in the treatment of schizophrenia.
Abou El-Magd, RM; Chung, SP; Fukui, K; Iwana, S; Kawazoe, T; Miyano, M; Ono, K; Park, HK; Sakai, T; Yorita, K, 2010
)
1.44
"Risperidone has a relatively higher affinity for the D(2) receptor in comparison with other atypical antipsychotics, which may explain why it is associated with a higher incidence of hyperprolactinemia."( Resolution of risperidone-induced hyperprolactinemia with substitution of quetiapine.
Kunwar, AR; Megna, JL, 2003
)
1.4
"Risperidone has a relatively low risk of causing obesity and diabetes mellitus and is a first-line treatment for schizophrenia. "( Glucose and lipid metabolism of long-term risperidone monotherapy in patients with schizophrenia.
Hosoda, H; Inoue, T; Itoh, K; Izumi, T; Kangawa, K; Koyama, T; Kusumi, I; Murashita, M; Nakagawa, S; Tanaka, T, 2007
)
2.05
"Risperidone has a rapid onset of action and a favourable side-effect profile."( Clinical review of risperidone.
Arnott, W; Chouinard, G, 1993
)
1.34
"Risperidone, which has a high affinity for 5-HT2 and D2 dopamine receptors in vitro, is a new antipsychotic drug that has been developed according to this hypothesis."( 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone.
Eriksson, B; Eriksson, L; Farde, L; Halldin, C; Nyberg, S, 1993
)
1.23
"Risperidone has a relatively mild side effect profile when compared with conventional antipsychotics."( Clinical experience with risperidone.
Marder, SR, 1996
)
1.32
"Risperidone has a wider use in this population and has a favourable clinical profile (at low doses)."( The treatment of psychotic disorders in late life.
Thorpe, L, 1997
)
1.02
"Risperidone has a substantial cost advantage over olanzapine, and was preferred by psychiatrists for more indications."( Comparison of cost, dosage and clinical preference for risperidone and olanzapine.
Kaplan, Z; Lichtenberg, P; Rabinowitz, J, 2000
)
2
"Risperidone has an atypical property, but its effect on limbic-cortical regions has not been evaluated."( Dose relationship of limbic-cortical D2-dopamine receptor occupancy with risperidone.
Ichimiya, T; Inoue, M; Okubo, Y; Sudo, Y; Suhara, T; Tanada, S; Yasuno, F, 2001
)
1.26
"Risperidone's ranking has more implications supported by CINeMA."( Prolactin levels influenced by antipsychotic drugs in schizophrenia: A systematic review and network meta-analysis.
Jiang, K; Leucht, S; Li, C; Liu, D; Siafis, S; Wang, J; Wu, H; Zhang, C; Zhu, D; Zhu, Y; Zhuo, K, 2021
)
1.34
"Risperidone has been significant correlated with a direct effect of interleukin-6 (IL-6) levels in patients with schizophrenia. "( Effect of risperidone on serum IL-6 levels in individuals with schizophrenia: a systematic review and meta-analysis.
Castillo-Avila, RG; Genis-Mendoza, AD; González-Castro, TB; Juárez-Rojop, IE; López-Narváez, ML; Martínez-Magaña, JJ; Ramos-Méndez, MA; Tovilla-Zárate, CA; Villar-Juárez, GE; Villar-Soto, M, 2023
)
2.76
"Risperidone has been shown in several trials to have a statistically significant benefit when used in a therapeutic context."( Neuropharmacological effect of risperidone: From chemistry to medicine.
Afzal, O; Al-Abbasi, FA; Alfawaz Altamimi, AS; Almalki, WH; Alzarea, SI; Bhat, AA; Dua, K; Gupta, G; Kazmi, I; Singh, SK, 2023
)
1.92
"Risperidone has a low risk of haematotoxicity because of its different chemical and pharmacological profile compared to other drugs such as clozapine."( Risperidone-induced anaemia.
Badiger, S; Chaukimath, SP; Chawath, S; Ramdurg, S,
)
2.3
"Risperidone has weight-based dosing and a liquid dosage form available, making it a good option for use in the NICU."( Delirium in the NICU: Risk or Reality?
Liviskie, C; McPherson, C, 2021
)
1.34
"Risperidone has shown promise in the management of chorea and has been found to be safe in children less than five years."( Effect of Risperidone on the Motor and Functional Disability in Children With Choreoathetoid Cerebral Palsy.
Kamate, M; Metgud, D; Mittal, N, 2018
)
1.6
"Risperidone has been shown to be effective in reducing or eliminating hot flushes on women with hormonal variations."( Combination treatment of tamoxifen with risperidone in breast cancer.
Chen, DR; Lin, HY; Wu, HM; Yeh, WL, 2014
)
1.39
"Risperidone also has multiple receptor targets in which only a subset may be procognitive and others induce cognitive impairment."( Risperidone and the 5-HT2A receptor antagonist M100907 improve probabilistic reversal learning in BTBR T + tf/J mice.
Amodeo, DA; Jones, JH; Ragozzino, ME; Sweeney, JA, 2014
)
2.57
"Risperidone has significantly enhanced the expression of phosphorylated Akt and phosphorylated GSK3β (P< 0.05), but did not alter the mRNA expression of DRD2. "( [Regulation of PI3K-Akt-GSK3β signaling pathway in U251 cells by risperidone].
Gu, X; Li, T; Liang, L; Ma, X; Wang, Y; Wei, J; Xiang, B, 2014
)
2.08
"Risperidone has demonstrated efficacy for acute (8 week) and intermediate length (6 month) management of severe irritability and aggression in children and adolescents with autism. "( Tolerability, Safety, and Benefits of Risperidone in Children and Adolescents with Autism: 21-Month Follow-up After 8-Week Placebo-Controlled Trial.
Aman, M; Arnold, LE; Ghuman, J; Grados, M; Hellings, J; Hollway, JA; McCracken, J; McDougle, CJ; Nagaraja, HN; Posey, DJ; Rettiganti, M; Scahill, L; Shah, B; Swiezy, NB; Tierney, E; Vitiello, B, 2015
)
2.13
"risperidone) has been found to improve social functioning more than standard antipsychotic treatment."( Different mechanisms of risperidone result in improved interpersonal trust, social engagement and cooperative behavior in patients with schizophrenia compared to trifluoperazine.
Bond, AJ; Chan, CK; Chan, F; Pang, AH; Tse, WS; Wong, AS, 2016
)
1.46
"Risperidone has been shown to be clinically effective for the treatment of aggressive behavior in children, yet until recently no information was available regarding whether risperidone exhibits aggression-specific suppression in preclinical studies employing validated developmentally immature animal models of escalated aggression. "( Repeated risperidone administration during puberty prevents the generation of the aggressive phenotype in a developmentally immature animal model of escalated aggression.
Connor, DF; Melloni, RH; Morrison, RL; Ricci, LA; Schwartzer, JJ, 2008
)
2.21
"Risperidone has demonstrated therapeutic advantages over conventional neuroleptics and offers a valuable emerging option for the treatment of social behavior associated with autistic disorder. "( Atypical neuroleptic risperidone modulates glial functions in C6 astroglial cells.
Bobermin, LD; Gonçalves, CA; Gottfried, C; Kleinkauf-Rocha, J; Quincozes-Santos, A; Riesgo, R; Souza, DO, 2009
)
2.11
"Risperidone has been suggested to be superior to olanzapine for glucose tolerance in whites, but there is little information on these drugs in Asian populations, even though Asians have a higher risk of type 2 diabetes compared to whites."( Glucose metabolism in Japanese schizophrenia patients treated with risperidone or olanzapine.
Furukori, H; Kaneko, S; Nakagami, T; Saito, M; Sato, Y; Yasui-Furukori, N, 2009
)
1.31
"Risperidone has proved helpful in treating children and adolescents with autism spectrum, conduct and bipolar disorders, Tourette's syndrome, and schizophrenia."( [Risperidone use in child and adolescent psychiatric patients].
Bentué-Ferrer, D; Chevreuil, C; Frémaux, T; Polard, E; Reymann, JM; Séveno, T,
)
1.76
"Risperidone has been approved by the Food and Drug Administration for the treatment of schizophrenia in the adolescent population. "( Risperidone: a review of efficacy studies in adolescents with schizophrenia.
Madaan, V, 2009
)
3.24
"Risperidone has a hyperbolic mixed-type inhibition, designated as 'partial uncompetitive inhibition effect', with K(i) value of 41 microM on human DAO."( The effect of risperidone on D-amino acid oxidase activity as a hypothesis for a novel mechanism of action in the treatment of schizophrenia.
Abou El-Magd, RM; Chung, SP; Fukui, K; Iwana, S; Kawazoe, T; Miyano, M; Ono, K; Park, HK; Sakai, T; Yorita, K, 2010
)
1.44
"Risperidone has been used to treat ADHD in people with ID, although the evidence for its effectiveness is unclear."( Risperidone for attention-deficit hyperactivity disorder in people with intellectual disabilities.
Maltezos, S; Paliokosta, E; Thomson, A; Xenitidis, K, 2009
)
2.52
"Risperidone has been reported as a well-tolerated antipsychotic in children. "( An unreported side effect of risperidone in children: sinus arrest with long pauses causing syncope.
Ceviz, N; Karacan, M; Olgun, H; Sepetcigil, O, 2009
)
2.09
"Risperidone has lower affinity for alpha2-adrenoceptors than clozapine but higher than most other APDs."( Adjunctive alpha2-adrenoceptor blockade enhances the antipsychotic-like effect of risperidone and facilitates cortical dopaminergic and glutamatergic, NMDA receptor-mediated transmission.
Frånberg, O; Jardemark, K; Konradsson-Geuken, A; Langlois, X; Marcus, MM; Svensson, TH; Wiker, C, 2010
)
1.31
"Risperidone (RIS) has the highest propensity to elevate plasma prolactin (PRL) levels. "( Gender differences in the relationship between the risperidone metabolism and the plasma prolactin levels in psychiatric patients.
Fukui, N; Inoue, Y; Ono, S; Someya, T; Sugai, T; Suzuki, Y; Tsuneyama, N; Watanabe, J, 2010
)
2.06
"Risperidone has been used to treat behavioral symptoms, such as delusions and agitation, in people with Alzheimer's disease. "( Association of 9-hydroxy risperidone concentrations with risk of switching or discontinuation in the clinical antipsychotic trial of intervention effectiveness-Alzheimer's disease trial.
Anyama, NG; Bies, RR; Lieberman, JA; Marder, SR; Pollock, BG; Schneider, LS; Wessels, AM, 2010
)
2.11
"Risperidone has been used in some stress disorders and may be potentially protective against stress-induced gastric lesions. "( Gastroprotective potential of risperidone, an atypical antipsychotic, against stress and pyloric ligation induced gastric lesions.
Krishnamurthy, S; Saxena, B; Singh, S, 2011
)
2.1
"Risperidone have been reported to commonly lead to asymptomatic elevation of liver enzymes in adult population, and recently in children and adolescents. "( Risperidone rechallenge for marked liver function test abnormalities in an autistic child.
Copur, M; Erdogan, A, 2011
)
3.25
"Risperidone has been shown to improve serious behavioral problems in children with autism. "( Risperidone-related improvement of irritability in children with autism is not associated with changes in serum of epidermal growth factor and interleukin-13.
Aman, MG; Arnold, LE; Bothwell, AL; Chae, W; Hoekstra, PJ; Katsovich, L; Kawikova, I; Leckman, JF; McCracken, JT; McDougle, CJ; Scahill, L; Tierney, E; Tobiasova, Z; van der Lingen, KH; Vitiello, B; Volkmar, F; Zhang, Y, 2011
)
3.25
"Risperidone has been shown to improve verbal working memory, executive functioning, attention, reaction time, and verbal learning, which, in turn, have been associated with improved functional outcomes. "( Impact of risperidone versus haloperidol on activities of daily living in the treatment of refractory schizophrenia.
Green, M; Gutkind, D; Hayden, J; Liberman, RP; Marshall, BD; Mintz, J; Robertson, MJ,
)
1.98
"Risperidone has a relatively higher affinity for the D(2) receptor in comparison with other atypical antipsychotics, which may explain why it is associated with a higher incidence of hyperprolactinemia."( Resolution of risperidone-induced hyperprolactinemia with substitution of quetiapine.
Kunwar, AR; Megna, JL, 2003
)
1.4
"Risperidone has been reported to alleviate the severity of tardive dyskinesia, but without placebo control, the possibility of spontaneous tardive dyskinesia remission after discontinuing original conventional antipsychotics cannot be excluded. "( Risperidone for severe tardive dyskinesia: a 12-week randomized, double-blind, placebo-controlled study.
Bai, YM; Lin, CC; Yu, SC, 2003
)
3.2
"Risperidone has more affinity for serotonin type 2 (5-HT(2)) than for D(2) receptors."( A case of risperidone-induced hypothermia.
Razaq, M; Samma, M,
)
1.26
"Risperidone has been used in Singapore for schizophrenia since 1996. "( Drug utilization review of risperidone for outpatients in a tertiary referral hospital in Singapore.
Koh, Y; Kua, EH; Li, SC; Luo, N; Tan, CH, 2004
)
2.06
"Risperidone has been shown to inhibit the delayed rectifier leading to lengthening of cardiac repolarization."( QTc interval, CYP2D6 and CYP2C9 genotypes and risperidone plasma concentrations.
Berecz, R; de la Rubia, A; Dorado, P; Llerena, A, 2004
)
1.3
"Risperidone has also been reported to be useful in the longer-term treatment of bipolar disorder."( Risperidone for bipolar disorders.
Aulakh, L; Fuller, MA; Keaton, DB; Madhusoodanan, S; Sajatovic, M, 2005
)
2.49
"Risperidone has been found efficacious for decreasing severe tantrums, aggression, and self-injurious behavior in children and adolescents with autistic disorder (autism). "( Risperidone for the core symptom domains of autism: results from the study by the autism network of the research units on pediatric psychopharmacology.
Aman, MG; Arnold, LE; Chuang, SZ; Davies, M; Ghuman, JK; Gonzalez, NM; Hollway, J; Koenig, K; Martin, A; McCracken, JT; McDougle, CJ; McGough, JJ; Posey, DJ; Ritz, L; Scahill, L; Shah, B; Swiezy, NB; Tierney, E; Vitiello, B, 2005
)
3.21
"Risperidone has been the best studied among these medications."( Systematic review of randomized controlled trials of atypical antipsychotics and selective serotonin reuptake inhibitors for behavioural problems associated with pervasive developmental disorders.
Dinca, O; Paul, M; Spencer, NJ, 2005
)
1.05
"Risperidone has been reported to have neuroleptic activity. "( An efficient synthesis of risperidone via stille reaction: antipsychotic, 5-HT2, and dopamine-D2-antagonist.
Jeong, JH; Kang, MS; Kim, DM; Kim, JS, 2005
)
2.07
"Risperidone has shown safety and efficacy for aggressive and destructive behaviors in short-term studies. "( A crossover study of risperidone in children, adolescents and adults with mental retardation.
Fleming, KK; Hellings, JA; Marquis, JG; Reese, RM; Schroeder, SR; Valdovinos, MG; Zarcone, JR, 2006
)
2.1
"Risperidone has primarily serotonergic, dopaminergic, and alpha-adrenergic antagonist properties."( Priapism associated with the switch from oral to injectable risperidone.
Davis, RR; Kirshner, A, 2006
)
1.3
"Risperidone has a relatively low risk of causing obesity and diabetes mellitus and is a first-line treatment for schizophrenia. "( Glucose and lipid metabolism of long-term risperidone monotherapy in patients with schizophrenia.
Hosoda, H; Inoue, T; Itoh, K; Izumi, T; Kangawa, K; Koyama, T; Kusumi, I; Murashita, M; Nakagawa, S; Tanaka, T, 2007
)
2.05
"Risperidone has been shown to be clinically effective for the treatment of aggressive behavior in children, yet no information is available regarding whether risperidone exhibits aggression-specific suppression in preclinical studies that use validated developmentally immature animal models of escalated aggression. "( Risperidone exerts potent anti-aggressive effects in a developmentally immature animal model of escalated aggression.
Connor, DF; Melloni, RH; Morrison, R; Ricci, LA, 2007
)
3.23
"Risperidone has been used in the treatment of self-abuse, aggression toward others, and violent behaviors."( Risperidone for the treatment of fecal smearing in a developmentally disabled adult.
Brahm, NC; Brown, RC; Farmer, KC, 2007
)
2.5
"Risperidone has been reported to decrease the reduction of MRI volume during the clinical course of schizophrenia."( Risperidone significantly inhibits interferon-gamma-induced microglial activation in vitro.
Hashioka, S; Kanba, S; Kato, T; Monji, A, 2007
)
2.5
"Risperidone has been shown to be a safe and effective atypical antipsychotic agent. "( Novel uses for risperidone: focus on depressive, anxiety and behavioral disorders.
Bradbury, C; da Silva, TL; McKay, M; Ravindran, AV, 2007
)
2.14
"Risperidone has better extrapyramidal tolerability a"( Short-term treatment with risperidone or haloperidol in first-episode schizophrenia: 8-week results of a randomized controlled trial within the German Research Network on Schizophrenia.
Braus, DF; Buchkremer, G; Gaebel, W; Gastpar, M; Heuser, I; Jäger, M; Klosterkötter, J; Kühn, KU; Maier, W; Möller, HJ; Ohmann, C; Riedel, M; Riesbeck, M; Schlösser, R; Schneider, F; Wickelmaier, F, 2008
)
1.37
"Risperidone has a rapid onset of action and a favourable side-effect profile."( Clinical review of risperidone.
Arnott, W; Chouinard, G, 1993
)
1.34
"Risperidone has these pharmacologic properties."( Extrapyramidal side effects and tolerability of risperidone: a review.
Owens, DG, 1994
)
1.27
"Risperidone, which has a high affinity for 5-HT2 and D2 dopamine receptors in vitro, is a new antipsychotic drug that has been developed according to this hypothesis."( 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone.
Eriksson, B; Eriksson, L; Farde, L; Halldin, C; Nyberg, S, 1993
)
1.23
"Risperidone has excellent oral activity, a rapid onset, and a 24-h duration of action."( Survey on the pharmacodynamics of the new antipsychotic risperidone.
Awouters, FH; Dugovic, C; Leysen, JE; Meert, TF; Megens, AA; Niemegeers, CJ; Schotte, A, 1994
)
1.26
"Both risperidone and clozapine have been shown to be effective against negative symptoms."( New pharmacotherapeutic modalities for negative symptoms in psychosis.
Lindenmayer, JP, 1995
)
0.75
"Risperidone has antiserotonergic and antidopaminergic properties that may make it more effective than conventional antipsychotic agents in the treatment of the negative symptoms of schizophrenia. "( Risperidone in the treatment of negative symptoms of schizophrenia: a meta-analysis.
Carman, J; Peuskens, J; Vangeneugden, A, 1995
)
3.18
"Risperidone has not yet been extensively studied in treatment-resistant patients, but may also be a useful alternative."( Treatment-resistant schizophrenic patients.
Kane, JM, 1996
)
1.02
"Risperidone has a relatively mild side effect profile when compared with conventional antipsychotics."( Clinical experience with risperidone.
Marder, SR, 1996
)
1.32
"Risperidone has been described as having salutary effects as an adjunctive pharmacotherapy in adult and pediatric patients with AD."( An open clinical trial of risperidone monotherapy in young children with autistic disorder.
Findling, RL; Maxwell, K; Wiznitzer, M, 1997
)
1.32
"Risperidone appears to have been effective and well tolerated in this sample of adolescents with schizophrenia."( Risperidone in adolescents with schizophrenia: an open pilot study.
Armenteros, JL; Gorman, J; Stedge, DJ; Welikson, M; Whitaker, AH, 1997
)
3.18
"Risperidone has proven to be effective as an antipsychotic drug and has fewer extrapyramidal side-effects than classic neuroleptics. "( Effects of risperidone, clozapine and haloperidol on extracellular recordings of substantia nigra reticulata neurons of the rat brain.
Bruggeman, R; Timmerman, W; Westerink, BH, 1997
)
2.13
"Risperidone has a wider use in this population and has a favourable clinical profile (at low doses)."( The treatment of psychotic disorders in late life.
Thorpe, L, 1997
)
1.02
"Risperidone has proven efficacy with reduced likelihood of causing extrapyramidal symptoms in the treatment of schizophrenia. "( Risperidone for aggression and self-injurious behavior in adults with mental retardation.
Cohen, SA; Ihrig, K; Kerrick, JM; Lott, RS, 1998
)
3.19
"Risperidone has relatively consistent positive effects on working memory, executive functioning, and attention, whereas improvement in verbal learning and memory was inconsistent."( The effects of clozapine, risperidone, and olanzapine on cognitive function in schizophrenia.
McGurk, SR; Meltzer, HY, 1999
)
1.32
"Risperidone has been suggested as representative of the newer 'atypical' neuroleptics and is claimed to be only minimally sedative."( Electroencephalographic and psychomotor effects of chlorpromazine and risperidone relative to placebo in normal healthy volunteers.
Ervine, CM; Hughes, AM; Lynch, P; Rhodes, J; Yates, RA, 1999
)
1.26
"As risperidone use has risen each year since its introduction, mean doses in both inpatients and discharged patients have steadily declined. "( A dose-outcome analysis of risperidone.
Bartko, JJ; Conley, RR; Kelly, DL; Love, RC, 1999
)
1.22
"Risperidone has potent effects on 5-HT and DA neuronal systems, both of which have been implicated in the pathophysiology of autism."( Research Units on Pediatric Psychopharmacology (RUPP) Autism Network. Background and rationale for an initial controlled study of risperidone.
Aman, MG; Arnold, LE; Cronin, P; Freeman, BJ; Martin, A; McCracken, JT; McDougle, CJ; McGough, JJ; Posey, DJ; Riddle, MA; Ritz, L; Scahill, L; Swiezy, NB; Tierney, E; Vitiello, B; Volkmar, FR; Votolato, NA; Walson, P, 2000
)
1.23
"Risperidone has pharmacological properties resembling those of the atypical antipsychotic clozapine and an improved tolerability profile compared with the conventional antipsychotic haloperidol."( Risperidone: a review of its use in the management of the behavioural and psychological symptoms of dementia.
Bhana, N; Spencer, CM, 2000
)
2.47
"Risperidone has a substantial cost advantage over olanzapine, and was preferred by psychiatrists for more indications."( Comparison of cost, dosage and clinical preference for risperidone and olanzapine.
Kaplan, Z; Lichtenberg, P; Rabinowitz, J, 2000
)
2
"Risperidone use has been associated with substantial weight gain in children and adolescents. "( Risperidone-associated weight gain in children and adolescents: a retrospective chart review.
Cicchetti, D; Landau, J; Leckman, JF; Leebens, P; Martin, A; Scahill, L; Ulizio, K, 2000
)
3.19
"Risperidone has an atypical property, but its effect on limbic-cortical regions has not been evaluated."( Dose relationship of limbic-cortical D2-dopamine receptor occupancy with risperidone.
Ichimiya, T; Inoue, M; Okubo, Y; Sudo, Y; Suhara, T; Tanada, S; Yasuno, F, 2001
)
1.26
"Risperidone has been primarily marketed for the treatment of schizophrenia. "( Risperidone in the treatment of psychotic depression.
Lerner, V; Miodownik, C,
)
3.02
"Risperidone has been proved on efficacy for tic disorders but EPS still remain, even though it was claimed to be less."( Quetiapine for tic disorder: a case report.
Boonyanaruthee, V; Chan-Ob, T; Kuntawongse, N, 2001
)
1.03

Actions

Risperidone is known to increase prolactin secretion in treating mental illness patients. The drug can activate the Akt-GSK3β signaling pathway in the U251 cells. Ris peridone did not increase obsessive-compulsive symptoms.

ExcerptReferenceRelevance
"Risperidone led to a lower LDL level in only young adult IR rats in day 56 than undrugged rats."( Effects of Early Risperidone Treatment on Metabolic Parameters in Socially Isolated Rats-Implication of Antipsychotic Intervention across Developmental Stages of Schizophrenia.
Hsieh, PS; Lin, CC; Liu, YP; Tzeng, NS; Yang, YY, 2023
)
1.97
"Risperidone is known to increase prolactin secretion in treating mental illness patients. "( The central mechanism of risperidone-induced hyperprolactinemia.
Huang, XF; Li, LY; Lin, S; Shi, YC; Song, ZY; Sun, WW; Yang, HQ, 2017
)
2.2
"Risperidone can activate the Akt-GSK3β signaling pathway in the U251 cells, and PI3K is a common regulatory site in Akt-GSK3β signaling and D2 receptor gene expression."( [Regulation of PI3K-Akt-GSK3β signaling pathway in U251 cells by risperidone].
Gu, X; Li, T; Liang, L; Ma, X; Wang, Y; Wei, J; Xiang, B, 2014
)
2.08
"Risperidone ameliorated increase in the activity of mitochondrial respiratory complex (I, II, IV, and V), decreases in the levels of mitochondrial membrane potential, cytochrome-C and caspase-9 in the hippocampus, hypothalamus, pre-frontal cortex, and amygdala."( Risperidone Attenuates Modified Stress-Re-stress Paradigm-Induced Mitochondrial Dysfunction and Apoptosis in Rats Exhibiting Post-traumatic Stress Disorder-Like Symptoms.
Ahmad, A; Garabadu, D; Krishnamurthy, S, 2015
)
2.58
"Risperidone failed to enhance recognition memory in this paradigm whereas donepezil was effective such that rats discriminated between the novel and familiar object in the retention trial following a 6h ITI."( Nicotinic α7 and α4β2 agonists enhance the formation and retrieval of recognition memory: Potential mechanisms for cognitive performance enhancement in neurological and psychiatric disorders.
Grayson, B; Harte, MK; Marsh, S; McLean, SL; Neill, JC; Zarroug, SH, 2016
)
1.16
"Risperidone has lower affinity for alpha2-adrenoceptors than clozapine but higher than most other APDs."( Adjunctive alpha2-adrenoceptor blockade enhances the antipsychotic-like effect of risperidone and facilitates cortical dopaminergic and glutamatergic, NMDA receptor-mediated transmission.
Frånberg, O; Jardemark, K; Konradsson-Geuken, A; Langlois, X; Marcus, MM; Svensson, TH; Wiker, C, 2010
)
1.31
"Risperidone seems to produce somewhat more extrapyramidal side effects and clearly more prolactin increase than most other SGAs. "( Risperidone versus other atypical antipsychotics for schizophrenia.
Hunger, H; Kissling, W; Komossa, K; Leucht, S; Rummel-Kluge, C; Schmid, F; Schwarz, S, 2011
)
3.25
"risperidone (RIS), produce more extensive blockade of brain serotonin (5-HT)(2A) than dopamine (DA) D(2) receptors."( Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.
Elkis, H; Hacksell, U; Meltzer, HY; Peters, P; van Kammen, DP; Vanover, K; Weiner, DM, 2012
)
1.32
"Risperidone may cause more sexual dysfunction than olanzapine (n=370, 2 RCTs, RR abnormal ejaculation 4.36 CI 1.38 to 13.76, NNH 20 CI 6 to 176; n=31, 1 RCT, RR impotence 2.43 CI 0.24 to 24.07)."( Risperidone versus olanzapine for schizophrenia.
Hosalli, P; Jayaram, MB, 2005
)
2.49
"Risperidone displays a novel mechanism of antagonism of the h5-HT7 receptor. "( Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptor.
Herrick-Davis, K; Mazurkiewicz, J; Rahman, T; Smith, C; Teitler, M; Toohey, N, 2006
)
3.22
"Risperidone doses that produce marked 5-HT2, but low dopamine D2, receptor blockade (1 and 0.1 mg/kg/day, SC, for 9 and 10 days, respectively) did not modify 8% ethanol preference."( 5-HT2 receptor antagonists do not reduce ethanol preference in Sardinian alcohol-preferring (sP) rats.
Ciccocioppo, R; Massi, M; Panocka, I; Pompei, P, 1993
)
1.01
"Risperidone displays similar activity at pre- and postsynaptic D2 receptors and at D2 receptors from various rat brain regions."( Survey on the pharmacodynamics of the new antipsychotic risperidone.
Awouters, FH; Dugovic, C; Leysen, JE; Meert, TF; Megens, AA; Niemegeers, CJ; Schotte, A, 1994
)
1.26
"Risperidone, at lower than recommended doses, shows promise in the treatment of late onset delusional disorders and behavior syndrome of dementia. "( Risperidone: treatment response in adult and geriatric patients.
Ancill, RJ; Gibson, RE; Holliday, SG; Kiraly, SJ, 1998
)
3.19
"Risperidone-associated increase in serum prolactin levels was not significantly correlated to the emergence of possible prolactin-related side effects."( Prolactin levels and adverse events in patients treated with risperidone.
Brecher, M; Davis, JM; de Coster, R; Kleinberg, DL; Van Baelen, B, 1999
)
1.27
"For risperidone, lower dosages were associated with higher hospital discharge rates, whereas no significant association was observed for olanzapine."( Comparison of discharge rates and drug costs for patients with schizophrenia treated with risperidone or olanzapine.
Conley, RR; Kelly, DL; Love, RC; Nelson, MW; Yu, Y, 2001
)
1.01
"Risperidone did not increase obsessive-compulsive symptoms."( Risperidone in the treatment of tourette syndrome: a double-blind, placebo-controlled trial.
Annable, L; Chouinard, G; Dion, Y; Sandor, P, 2002
)
2.48
"Risperidone's ability to increase prolactin release was unchanged after S-9 treatment, and 9-hydroxy-risperidone, identified as a major metabolite in the S-9 conditioned media, was equipotent to risperidone in modulating prolactin release in vitro.(ABSTRACT TRUNCATED AT 250 WORDS)"( Stimulation by risperidone of rat prolactin secretion in vivo and in cultured pituitary cells in vitro.
Bowden, CR; De Coster, R; Heykants, J; Voina, SJ; Woestenborghs, R, 1992
)
1.36

Treatment

Co-treatment with risperidone (0.01 mg/kg) and mirtazapine (2.5 or 5 mg/ kg) abolished the effect of MK-801. Treatment with ris peridone over 6 weeks led to increased prolactin levels, liver functions, metabolic measures, and weight/body mass index (BMI)

ExcerptReferenceRelevance
"Risperidone-treatment upregulated expression of ketogenic key enzyme, mitochondrial 3-hydroxy-3-methyl-glutaryl-CoA synthase 2 (HMGCS2) in the kidney rather than liver."( Kidney plays an important role in ketogenesis induced by risperidone and voluntary exercise in juvenile female rats.
Deng, C; Lian, J; Sylvester, E; Yi, W, 2021
)
1.59
"Risperidone treatment also led to a decrease in Akt and CREB phosphorylation in the prefrontal cortex."( Chronic oral treatment with risperidone impairs recognition memory and alters brain-derived neurotrophic factor and related signaling molecules in rats.
Bartlett, MG; Callahan, PM; Hernandez, CM; Pillai, A; Poddar, I; Terry, AV; Yang, X, 2020
)
1.57
"Risperidone treatment further attenuated cocaine-induced elevation of DA."( Risperidone and 5-HT2A Receptor Antagonists Attenuate and Reverse Cocaine-Induced Hyperthermia in Rats.
Makiguchi, A; Okada, T; Shioda, K; Suda, S, 2020
)
2.72
"Risperidone treatment of sedentary rats resulted in significantly increased white adipose tissue, fasting triglyceride and fasting insulin compared to vehicle-treated sedentary rats."( Exercise intervention for preventing risperidone-induced dyslipidemia and gluco-metabolic disorders in female juvenile rats.
Deng, C; Han, M; Sylvester, E; Yi, W, 2020
)
1.55
"Risperidone treatment was significantly associated with an increase in BMI (effect size of exposure=0.45 SD (SE=0.06), "( Body mass index increase in preschoolers with heterogeneous psychiatric diagnoses treated with risperidone.
Avrahami, M; Balan-Moshe, L; Barzilay, R; Drapisz, A; Levy, T; Moore, T; Peskin, M; Segal-Gavish, H; Shachar, I; Taylor, J; Weizman, A, 2021
)
2.28
"Risperidone-treated 5 to 17 year-old males underwent anthropometric and bone measurements, using dual-energy X-ray absorptiometry and peripheral quantitative computed tomography."( Bone Mass in Boys with Autism Spectrum Disorder.
Calarge, CA; Schlechte, JA, 2017
)
1.18
"Risperidone-treated children and adolescents were assessed for CHRNA7 copy number state using droplet digital PCR and genomic quantitative PCR. "( CHRNA7 Deletions are Enriched in Risperidone-Treated Children and Adolescents.
Calarge, CA; Gillentine, MA; Grochowski, CM; Lupski, JR; Schaaf, CP; White, JJ, 2017
)
2.18
"Risperidone treatment decreased serum testosterone and estradiol levels. "( Effects of Risperidone and Aripiprazole on Serum Levels of Prolactin, Testosterone and Estradiol in Female Patients with Schizophrenia.
Hu, JQ; Jiang, XJ; Lin, WC; Shang, DW; Shi, L; Wen, YG; Wu, FX; Xiao, B; Zhang, JP; Zhu, HZ, 2018
)
2.31
"Risperidone treatment causes significant changes in certain fecal bacteria, which are likely associated with antipsychotic medication induced metabolic changes."( Changes in metabolism and microbiota after 24-week risperidone treatment in drug naïve, normal weight patients with first episode schizophrenia.
Fan, X; Hei, G; Huang, XF; Kumar, BU; Li, X; Liu, Y; Lv, L; Song, X; Wang, Y; Yuan, X; Zhang, P, 2018
)
1.45
"Risperidone-treated boys (n = 267; age: 12.7 ± 2.7 years), 71% of whom had ever taken an SSRI, contributed to the analysis. "( Selective Serotonin Reuptake Inhibitors Reduce Longitudinal Growth in Risperidone-Treated Boys.
Calarge, CA; Garcia, JM; Karaviti, L; Mills, JA; Teixeira, AL; Zemel, BS, 2018
)
2.16
"In risperidone-treated boys, SSRI use is associated with reduced longitudinal growth, particularly in those undergoing puberty. "( Selective Serotonin Reuptake Inhibitors Reduce Longitudinal Growth in Risperidone-Treated Boys.
Calarge, CA; Garcia, JM; Karaviti, L; Mills, JA; Teixeira, AL; Zemel, BS, 2018
)
1.34
"Risperidone treatment in youth is associated with elevated appetite during an OGTT, with no differences in gut peptides or adipocytokines to explain risperidone's effect on appetite. "( Risperidone But Not Quetiapine Treatment Is Associated With Increased Appetite But Not Satiety Hormones in Children During An Oral Glucose Tolerance Test: A Pilot Study.
Devlin, AM; Ngai, YF; Panagiotopoulos, C, 2018
)
3.37
"Risperidone treatment was associated with trends of BMI-Z increase in children and decrease in adolescents."( Weight-Change Trajectories of Pediatric Outpatients Treated with Risperidone or Aripiprazole in a Naturalistic Setting.
Bernardini, R; Biganzoli, E; Bravaccio, C; Capuano, A; Carnovale, C; Clementi, E; Marano, G; Molteni, M; Nobile, M; Pisano, S; Pozzi, M; Radice, S; Rafaniello, C; Rizzo, R; Rossi, F, 2019
)
1.47
"Risperidone treatment did not affect performance on the open field, object recognition, or Morris Water maze."( Neurobehavioral effects of chronic low-dose risperidone administration in juvenile male rats.
Boman, L; De Butte, M, 2019
)
1.5
"1288 risperidone-treated patients and 1334 aripiprazole-treated patients were included in the study, of whom 725 (56%) risperidone-treated and 890 (67%) aripiprazole-treated patients were eligible for the pharmacokinetic analyses. "( Effect of CYP2D6 genotype on exposure and efficacy of risperidone and aripiprazole: a retrospective, cohort study.
Haslemo, T; Ingelman-Sundberg, M; Jukic, MM; Molden, E; Smith, RL, 2019
)
1.28
"Risperidone-treated mice had a higher resting energy expenditure (P = 0.001) and total energy expenditure (TEE) (P = 0.005) than the placebo group."( Effects of risperidone on energy balance in female C57BL/6J mice.
Allison, DB; Johnson, MS; Kesterson, RA; Li, X; Li, Y; Nagy, TR; Smith, DL, 2013
)
1.5
"Risperidone treatment is associated with changes in serum pro-inflammatory cytokines levels and weight. "( Changes in pro-inflammatory cytokines and body weight during 6-month risperidone treatment in drug naïve, first-episode schizophrenia.
Fan, X; Gao, J; Harrington, A; Li, X; Lv, L; Song, X; Zhang, W; Zhao, J; Ziedonis, D, 2014
)
2.08
"Risperidone treatment increased methamphetamine choice, whereas bupropion treatment did not alter methamphetamine choice up to doses that decreased rates of operant behavior."( Effects of Environmental Manipulations and Treatment with Bupropion and Risperidone on Choice between Methamphetamine and Food in Rhesus Monkeys.
Banks, ML; Blough, BE, 2015
)
1.37
"Risperidone treatment significantly increased PON1 activity and decreased LOOH levels."( Oxidative stress in drug naïve first episode psychosis and antioxidant effects of risperidone.
Barbosa, DS; Belangero, SI; Bonifácio, KL; Bressan, RA; Brietzke, E; Cordeiro, Q; Gadelha, A; Maes, M; Noto, C; Noto, MN; Nunes, SO; Ota, VK, 2015
)
1.36
"Risperidone treatment was associated with elevated levels of serum prolactin (67.16% risperidone versus 52.31% blonanserin) and cardiac-related abnormalities (22.39% risperidone versus 12.31% blonanserin), and blonanserin patients were more prone to extrapyramidal side effects (48.46% blonanserin versus 29.10% risperidone)."( Comparative study of the efficacy and safety between blonanserin and risperidone for the treatment of schizophrenia in Chinese patients: A double-blind, parallel-group multicenter randomized trial.
Gu, N; Li, H; Li, J; Li, K; Li, L; Liu, C; Luo, X; Qi, S; Shi, J; Wang, C; Wang, L; Wang, Q; Yang, F; Yao, C; Zhang, H, 2015
)
1.37
"Risperidone-treated patients reported significantly greater METH craving reductions (p<0.001)."( Aripiprazole and Risperidone for Treatment of Methamphetamine-Associated Psychosis in Chinese Patients.
Chawarski, MC; Chen, H; Hao, W; Schottenfeld, RS; Wang, G; Xu, Z; Zhang, S; Zhang, Y, 2016
)
1.5
"The risperidone maintenance treatment in schizophrenia study was designed to identify the duration of maintenance treatment required with an initial therapeutic dose in contrast to reducing the dose over time. "( Extrapyramidal Symptoms During Risperidone Maintenance Treatment in Schizophrenia: A Prospective, Multicenter Study.
Bo, QJ; Li, AN; Li, XB; Ma, X; Wang, CY; Wang, ZM, 2016
)
1.28
"Risperidone treatment disturbed glucose homeostasis and endocrine regulation (particularly leptin) in children and adolescents with ASDs, in a dose- and duration-dependent manner, being suggestive of leptin and insulin resistance mechanisms. "( Impact of risperidone on leptin and insulin in children and adolescents with autistic spectrum disorders.
Hongkaew, Y; Intachak, B; Kroll, MH; Limsila, P; Ngamsamut, N; Puangpetch, A; Srisawasdi, P; Sukasem, C; Vanavanan, S; Vanwong, N, 2017
)
2.3
"The risperidone treated group had more patients with mixed states and lifetime panic disorder at randomization than the placebo group. "( Randomized, placebo-controlled trial of risperidone for acute treatment of bipolar anxiety.
Gonzalez, R; Harnett-Sheehan, K; Janavs, J; Keck, PE; McElroy, SL; Rogers, J; Sheehan, DV; Shivakumar, G; Suppes, T, 2009
)
1.18
"Risperidone-treated mice consumed more food (p=0.050) and gained more weight (p=0.0001) than PLA-treated mice after 3 weeks."( Risperidone alters food intake, core body temperature, and locomotor activity in mice.
Allison, DB; Cope, MB; DiCostanzo, CA; Jamison, WG; Jumbo-Lucioni, P; Kesterson, RA; Li, X; Nagy, TR, 2009
)
2.52
"More risperidone-treated patients completed the study (41.6%) than ziprasidone-treated patients (33.9%), but the difference was not statistically significant."( A comparison of ziprasidone and risperidone in the long-term treatment of schizophrenia: a 44-week, double-blind, continuation study.
Addington, DE; Johnson, G; Kulkarni, J; Labelle, A; Loebel, A; Mandel, FS, 2009
)
1.09
"Risperidone treatment can improve disgust recognition deficits in patients with schizophrenia."( Effect of risperidone on emotion recognition deficits in antipsychotic-naïve schizophrenia: a short-term follow-up study.
Arasappa, R; Behere, RV; Gangadhar, BN; Reddy, N; Venkatasubramanian, G, 2009
)
2.2
"Risperidone-treated participants exhibited lower movement velocities during production of simple loops compared to unmedicated patients."( Handwriting movement analyses for monitoring drug-induced motor side effects in schizophrenia patients treated with risperidone.
Caligiuri, MP; Dean, CE; Lohr, J; Niculescu, AB; Teulings, HL, 2009
)
1.28
"On risperidone treatment, the adjusted mean prolactin level at the 3rd month of treatment was significantly higher than at the 1st month; at the 12th month it was significantly lower than at the 1st month; the 1st and 6th months were not significantly different."( Short- and long-term effects on prolactin of risperidone and olanzapine treatments in children and adolescents.
D'Arrigo, C; de Leon, J; Diaz, FJ; Gagliano, A; Germanò, E; Migliardi, G; Siracusano, R; Spina, E, 2009
)
1.13
"Risperidone treatment increased CB(1) receptor binding in the arcuate nucleus (40%), hippocampus (25-30%) and amygdala (35%) without concurrent alterations in the CB(1) receptor mRNA."( Risperidone treatment increases CB1 receptor binding in rat brain.
Egerod, KL; Holst, B; Husum, H; Mellerup, E; Secher, A, 2010
)
2.52
"Risperidone treatment resulted in no decline in cognitive function among children and adolescents. "( Cognitive function with long-term risperidone in children and adolescents with disruptive behavior disorder.
Cornblatt, B; Pandina, GJ; Zhu, Y, 2009
)
2.07
"Risperidone pretreatment significantly attenuated increases in the levels of DA, 5-HT, glutamate, and NOx."( Effect of risperidone on acute methamphetamine-induced hyperthermia in rats.
Kato, S; Nisijima, K; Shioda, K; Yoshino, T, 2010
)
1.48
"Risperidone pretreatment (0.050 mg kg⁻¹) blocked the expression but not the development of nicotine-induced locomotor sensitization in rats."( Effects of risperidone on development and expression of nicotine-induced locomotor sensitization in rats.
Akdag, E; Kayir, H; Uzbay, TI, 2011
)
1.48
"Risperidone treatment induced a decrement of plasma DA levels and increments of plasma DOPAC and DA TR in the total group of schizophrenic patients."( Abnormal plasma monoamine metabolism in schizophrenia and its correlation with clinical responses to risperidone treatment.
Cai, HL; Fang, PF; Hu, L; Li, HD; Yang, W; Ye, HS; Zhang, XH, 2011
)
1.31
"Risperidone (n=63) treated patients had higher AUDIT scores and prolactin levels than those on other atypical antipsychotics (n = 113)."( Alcohol Use Disorders Identification Test (AUDIT) scores are elevated in antipsychotic-induced hyperprolactinaemia.
Barnes, M; Connor, JP; Heslop, K; Lawford, BR; Nyst, P; Young, RM, 2012
)
1.1
"Risperidone pretreatment reverses the stress induced alteration in hexosamine, PGE(2) and microvascular permeability."( Gastroprotective potential of risperidone, an atypical antipsychotic, against stress and pyloric ligation induced gastric lesions.
Krishnamurthy, S; Saxena, B; Singh, S, 2011
)
1.38
"risperidone-treated patients."( Olanzapine and risperidone effects on appetite and ghrelin in chronic schizophrenic patients.
Davis, JM; Dwivedi, S; Rachakonda, S; Smith, RC, 2012
)
1.45
"Risperidone treatment was associated with reduction of symptom severity and moderate improvement of formal thought disorder and some aspects of executive functions. "( Cognition and communication dysfunctions in early-onset schizophrenia: effect of risperidone.
Namysłowska, I; Remberk, B; Rybakowski, F, 2012
)
2.05
"Risperidone treatment was begun (1mg/d and 1.5mg/d after 24 hours), associated with oral clonazepam (0.05 mg/kg/d)."( [Follow-up of a 16-year-old adolescent with early-onset schizophrenia and catatonic symptoms].
Askenazy, F; Drici, M; Lavrut, T; Menard, ML; Yagoubi, F, 2013
)
1.11
"Risperidone treatment restored increased DARPP-32 phosphorylation in the striatum and CA1 regions of NVH-lesioned rats but did not rescue CaMKII and PKCα autophosphorylation."( Decreased CaMKII and PKC activities in specific brain regions are associated with cognitive impairment in neonatal ventral hippocampus-lesioned rats.
Fukunaga, K; Moriguchi, S; Nakagawasai, O; Onogi, H; Shioda, N; Tadano, T; Tan-No, K; Yabuki, Y, 2013
)
1.11
"2198 risperidone-treated patients were identified versus 3259 treated with other antipsychotics. "( A naturalistic study of risperidone treatment outcome using prognosis-adjusted discharge rates in New York State inpatients.
Allingham, BH; Cienfuegos, A; Javitt, DC; Levine, J; Miniati, M; Robinson, J; Silipo, G, 2002
)
1.14
"Risperidone treatment causes a greater increase in the body mass of patients than treatment with conventional antipsychotics, such as haloperidol."( Peripheral injection of risperidone, an atypical antipsychotic, alters the bodyweight gain of rats.
Fujiwara, K; Itoh, M; Kaneko, YS; Mori, K; Nagasaka, A; Nakashima, A; Ota, A; Ota, M, 2002
)
1.34
"Risperidone treatment significantly decreased the initially high blood SOD levels in schizophrenia."( The effect of risperidone treatment on superoxide dismutase in schizophrenia.
Cao, LY; Shen, YC; Wu, GY; Zhang, PY; Zhang, XY; Zhou, DF, 2003
)
1.4
"Risperidone pretreatment significantly attenuated the discriminative-stimulus effects of d-amphetamine, and some of the self-reported drug effects."( Risperidone attenuates the discriminative-stimulus effects of d-amphetamine in humans.
Glaser, PE; Hays, LR; Hays, LS; Rush, CR; Stoops, WW, 2003
)
2.48
"Risperidone-treated patients stayed a mean of 9 fewer days in the hospital compared with olanzapine-treated patients (49 vs."( Risperidone compared with olanzapine in a naturalistic clinical study: a cost analysis.
Libretto, SE; Taylor, DM; Wright, T, 2003
)
2.48
"Risperidone treatment, as opposed to olanzapine, for female premenopausal schizophrenia results in hyperprolactinemia and clinically relevant decrease in bone mineral density. "( Risperidone, but not olanzapine, decreases bone mineral density in female premenopausal schizophrenia patients.
Becker, D; Liver, O; Mester, R; Rapoport, M; Weiss, M; Weizman, A, 2003
)
3.2
"Risperidone treatment in children and adolescents (n = 51) with severe behavioural disturbances was assessed retrospectively to determine clinical response and adverse events. "( Use of risperidone in a paediatric population: an observational study.
Dossetor, D; King, B; Longworth, J; Nunn, K; Zwi, K,
)
2.03
"Risperidone treatment was generally well tolerated, although extrapyramidal symptoms were noted in a dose-dependent manner."( Risperidone use in Korean patients with Alzheimer's disease: optimal dosage and effect on behavioural and psychological symptoms, cognitive function and activities of daily living.
Choi, SK; Kim, JM; Lee, H; Shin, IS; Yoon, JS, 2003
)
2.48
"Risperidone treatment for 52 weeks commenced at 2 mg/d, with the option to titrate to 6 mg/d."( Treatment outcome in patients with chronic schizophrenia during long-term administration with risperidone.
Libretto, SE; Reveley, MA, 2004
)
1.26
"Risperidone-treated children had a mean increase in height 1.2 cm greater than the reference population, and they experienced no delay in progression through Tanner staging. "( Growth and sexual maturation during long-term treatment with risperidone.
Daneman, D; Dunbar, F; Kusumakar, V; Schulz, M, 2004
)
2.01
"Risperidone-treated patients had clinically and statistically significant reductions in both disruptive behavior and hyperactivity subscale scores, compared to placebo, regardless of concomitant stimulant use."( Risperidone effects in the presence/absence of psychostimulant medicine in children with ADHD, other disruptive behavior disorders, and subaverage IQ.
Aman, MG; Binder, C; Turgay, A, 2004
)
2.49
"Risperidone treatment was associated with an early and sustained reduction in nursing staff burden as measured using the M-NCAS compared with placebo treatment for older nursing home residents with dementia."( The effect of risperidone on nursing burden associated with caring for patients with dementia.
Brodaty, H; Ciesla, G; Frank, L; Kleinman, L; Rupnow, MF, 2004
)
2.13
"Risperidone-treated subjects also exhibited significantly greater decreases on the other 4 subscales of the ABC; on the conduct problem, insecure/anxious, hyperactive, and overly sensitive subscales of the Nisonger Child Behavior Rating Form (parent version); and on the Visual Analog Scale of the most troublesome symptom."( Risperidone in the treatment of disruptive behavioral symptoms in children with autistic and other pervasive developmental disorders.
Carroll, A; Dunbar, F; Orlik, H; Schulz, M; Shea, S; Smith, I; Turgay, A, 2004
)
2.49
"Risperidone-treated patients had a significantly greater reduction in total score on the CAPS-2 (z = -2.44, p = .015). "( A preliminary study of risperidone in the treatment of posttraumatic stress disorder related to childhood abuse in women.
Hennen, J; Reich, DB; Stanculescu, C; Watts, T; Winternitz, S, 2004
)
2.08
"Risperidone treatment reduced this deficit, suggesting a facilitation of attentional function, but haloperidol treatment did not."( Abnormalities in visually guided saccades suggest corticofugal dysregulation in never-treated schizophrenia.
Harris, MS; Keshavan, MS; Reilly, JL; Sweeney, JA, 2005
)
1.05
"Risperidone treatment, however, was more effective in the reduction of negative symptoms."( The effect of neuroleptic treatments on executive function and symptomatology in schizophrenia: a 1-year follow up study.
Cohen, H; Pourcher, E; Rémillard, S, 2005
)
1.05
"Risperidone treatment was well tolerated and resulted in further improvement during the 9-week extension, beyond the 3 weeks of ac"( An open-label extension trial of risperidone monotherapy in the treatment of bipolar I disorder.
Canuso, CM; Eerdekens, M; Hirschfeld, RM; Kalali, AH; Karcher, K; Khan, AA; Palumbo, JM, 2006
)
1.34
"The risperidone-treated subjects demonstrated changes in grey matter and white matter in several brain regions, including superior temporal gyrus."( Risperidone in first-episode psychosis: a longitudinal, exploratory voxel-based morphometric study.
Diwadkar, VA; Girgis, RR; Hardan, AY; Keshavan, MS; Nutche, JJ; Sweeney, JA, 2006
)
2.26
"Risperidone treatment significantly elevated serum PRL level (range: 26.9 ng/ml-320.0 ng/ml)."( The relationship between prolactin response and clinical efficacy of risperidone in acute psychotic inpatients.
Kim, YK; Lee, BH, 2006
)
1.29
"Risperidone-treated animals showed a catalepsy-like phenotype, which differed to that of haloperidol-treated rats, indicating that processes other than the anticipated dopaminergic mechanisms are underlying this phenomenon."( Behavioural effects of chronic haloperidol and risperidone treatment in rats.
Dedova, I; Duffy, L; Karl, T; Matsumoto, I; O'brien, E, 2006
)
1.31
"Risperidone treatment was associated with significant increases in relative metabolic rate in the striatum, cingulate gyrus, the prefrontal cortex, especially in the orbital region, and the thalamus."( Positron emission tomography imaging of risperidone augmentation in serotonin reuptake inhibitor-refractory patients.
Baldini Rossi, N; Bloom, R; Buchsbaum, MS; Hollander, E; Newmark, R; Pallanti, S; Platholi, J; Sood, E, 2006
)
1.32
"Risperidone treatment was associated with two- to four-fold mean increases in serum prolactin in children with autism. "( Effects of short- and long-term risperidone treatment on prolactin levels in children with autism.
Aman, MG; Anderson, GM; Arnold, LE; Katsovich, L; Martin, A; McCracken, JT; McDougle, CJ; Posey, DJ; Scahill, L; Shah, B; Tierney, E; Vitiello, B, 2007
)
2.07
"Only risperidone-treated patients exhibited significant decreases in uncontrolled hostility/excitement and anxiety and depression."( Efficacy of risperidone versus olanzapine in patients with schizophrenia previously on chronic conventional antipsychotic therapy: a switch study.
Borisov, A; Feldman, J; May, R; Miller, AH; Nemeroff, CB; Rosenberg, J; Savage, R; Tucker, M; Wang, X; Woolwine, B, 2006
)
1.17
"Risperidone treatment did not change P3 amplitudes and latencies."( Effects of risperidone on auditory information processing in neuroleptic-naive patients with schizophrenia spectrum disorders.
Dapsys, K; Kähkönen, S; Korostenskaja, M; Maciulis, V; Ruksenas, O; Siurkute, A, 2006
)
1.45
"Risperidone-treated patients had a significantly (p = .03) greater improvement in PANSS positive subscale score among all patients, but not among completers."( Comparison of quetiapine and risperidone in the treatment of schizophrenia: A randomized, double-blind, flexible-dose, 8-week study.
Hamer, RM; Lieberman, JA; Sweitzer, DE; Zhong, KX, 2006
)
1.35
"Risperidone treatment was well tolerated and significantly improved behavioral problems associated with autism."( Risperidone improves behavioral symptoms in children with autism in a randomized, double-blind, placebo-controlled trial.
Bossie, CA; Dunbar, F; Pandina, GJ; Youssef, E; Zhu, Y, 2007
)
2.5
"Risperidone treatment exacerbated these deficits, perhaps by impairing the encoding of information into working memory."( Adverse effects of risperidone on spatial working memory in first-episode schizophrenia.
Harris, MS; Keshavan, MS; Reilly, JL; Sweeney, JA, 2006
)
1.38
"Risperidone treatment reduced anxiety but increased heart rate."( Blood pressure, heart rate, and anxiety in schizophrenia.
Baier, MB; Becker, JE; Ritchie, MA; Townsend, MH, 2007
)
1.06
"Risperidone treatment appears to be well tolerated and modestly effective when used in combination with psychostimulants for treatment-resistant aggression in children with ADHD."( Risperidone augmentation for treatment-resistant aggression in attention-deficit/hyperactivity disorder: a placebo-controlled pilot study.
Armenteros, JL; Davalos, M; Lewis, JE, 2007
)
3.23
"Risperidone monotherapy treatment was associated with hyperprolactinaemia in 69% of patients ( n = 35) and in 100% of female patients (n = 16) and amisulpride monotherapy in 100% (n = 7)."( Prevalence of hyperprolactinaemia in a naturalistic cohort of schizophrenia and bipolar outpatients during treatment with typical and atypical antipsychotics.
Bushe, C; Shaw, M, 2007
)
1.06
"Risperidone treatment significantly increased serum prolactin levels."( Serum prolactin levels, plasma risperidone levels, polymorphism of cytochrome P450 2D6 and clinical response in patients with schizophrenia.
Du, J; Fang, C; Feng, GY; Gu, NF; He, L; Li, XW; Qin, SY; Wang, L; Xing, QH; Yu, L; Zhang, AP, 2007
)
1.35
"Oral risperidone treatment was better than placebo treatment in reducing irritability and other behavioral symptoms associated with autistic disorder in children and adolescents in two well designed short-term trials, with these benefits maintained in those receiving risperidone for up to 6 months."( Risperidone: a review of its use in the treatment of irritability associated with autistic disorder in children and adolescents.
Dhillon, S; Scott, LJ, 2007
)
2.24
"Risperidone treatment may be associated with alterations in glucose-regulating mechanisms in patients with schizophrenia."( Effects of risperidone on glucose metabolism in Chinese patients with schizophrenia: a prospective study.
Cai, ZJ; Chen, Q; Mao, PX; Mitchell, PB; Tang, YL; Zhai, YM, 2008
)
2.18
"Risperidone (6 to 16 mg)-treated patients showed significantly (p < 0.05) lower dyskinetic scores than those receiving placebo, whereas in haloperidol- and placebo-treated patients, no significant differences for dyskinetic symptoms were noted."( Effects of risperidone in tardive dyskinesia: an analysis of the Canadian multicenter risperidone study.
Chouinard, G, 1995
)
1.4
"With risperidone treatment, the vocalizations diminished to less than 20% of baseline ratings. "( The use of risperidone in severely demented patients with persistent vocalizations.
Honer, WG; Kopala, LC, 1997
)
1.2
"Risperidone treatment had a greater beneficial effect on verbal working memory than haloperidol treatment across testing conditions (with and without distraction) and study phases (fixed and flexible dose). "( Does risperidone improve verbal working memory in treatment-resistant schizophrenia?
Ames, D; Green, MF; Kern, RS; Marder, SR; Marshall, BD; McGurk, S; Mintz, J; Wirshing, WC, 1997
)
2.25
"Risperidone treatment produced a greater effect on patients' ability to perceive emotion compared with haloperidol treatment."( Risperidone versus haloperidol for perception of emotion in treatment-resistant schizophrenia: preliminary findings.
Green, MF; Kee, KS; Kern, RS; Marshall, BD, 1998
)
2.46
"Risperidone treatment was associated with a significant functional in-vivo 5-HT antagonism similar to clozapine."( Risperidone is associated with blunting of D-fenfluramine evoked serotonergic responses in schizophrenia.
Curtis, VA; Jones, H; Lucey, JV; Wright, PA, 1998
)
2.46
"Risperidone treatment produced significant improvements over baseline in the incidence and severity of extrapyramidal symptoms (EPS)."( Phase-IV multicentre clinical study of risperidone in the treatment of outpatients with schizophrenia. The RIS-CAN-3 Study Group.
Beauclair, L; Chouinard, G; Johnson, SV; Kopala, L; Labelle, A; Singh, KI, 1998
)
1.29
"Risperidone-treated patients showed greater improvement than haloperidol-treated patients in general verbal learning ability, a finding characterized by significant treatment effects on CVLT measures of learning acquisition, recall consistency, and recognition memory."( Risperidone versus haloperidol on secondary memory: can newer medications aid learning?
Green, MF; Kern, RS; Marder, SR; Marshall, BD; McGurk, SR; Mintz, J; Wirshing, D; Wirshing, WC, 1999
)
2.47
"Risperidone-treated subjects with a greater degree of acute mood change were both 3.58 times more likely to relapse than their risperidone counterparts who had experienced less mood improvement (p = .008) and 8.55 times more likely than olanzapine-treated subjects who had had similar mood improvements (p = .001)."( The course of depressive symptoms in predicting relapse in schizophrenia: a double-blind, randomized comparison of olanzapine and risperidone.
Andersen, SW; Tollefson, GD; Tran, PV, 1999
)
1.23
"Risperidone-treated subjects were significantly less likely than haloperidol-treated subjects to require concomitant anticholinergic medication after 4 weeks (20% versus 63%); they also had significantly les observable akathisia (24% versus 53%) and significantly less severe tardive dyskinesia."( Risperidone in treatment-refractory schizophrenia.
Green, MF; Marder, SR; Marshall, BD; Mintz, J; Wirshing, DA; Wirshing, WC, 1999
)
2.47
"Risperidone treatment did not adversely affect symptoms specific to Parkinson's disease, as assessed by the Unified Parkinson's Disease Rating Scale (UPDRS)."( Risperidone in the treatment of dopamine-induced psychosis in Parkinson's disease: an open pilot trial.
De Deyn, PP; Hildebrand, K; Mendis, T; Mohr, E, 2000
)
2.47
"Risperidone-treated children and adolescents experienced significant weight gain between baseline and endpoint (paired t test, p < 0.001) that was first evident within 2 months of starting treatment, progressed steadily at an average rate of 1.2 kg/month, and did not reach a clear plateau during 6 months of observation."( Risperidone-associated weight gain in children and adolescents: a retrospective chart review.
Cicchetti, D; Landau, J; Leckman, JF; Leebens, P; Martin, A; Scahill, L; Ulizio, K, 2000
)
2.47
"Risperidone pre-treatment reduced the self-rated 'high' produced by cocaine."( Risperidone pre-treatment reduces the euphoric effects of experimentally administered cocaine.
Kalechstein, AD; Ling, W; Newton, TF; Tervo, K; Uslaner, J, 2001
)
2.47
"Risperidone treatment was given for 8 weeks; the permitted dosage range was 4 mg to 10 mg daily."( Risperidone treatment of outpatients with schizophrenia: no evidence of sex differences in treatment response.
Dunbar, F; Labelle, A; Light, M, 2001
)
2.47
"Risperidone-treated patients showed a significantly greater decrease in the positive (P < 0.01), negative (P < 0.05) and general psychopathology (P < 0.001) scores than patients receiving other antipsychotics or haloperidol."( Treatment of the symptoms of schizophrenia: a combined analysis of double-blind studies comparing risperidone with haloperidol and other antipsychotic agents.
Glick, ID; Lemmens, P; Vester-Blokland, E, 2001
)
1.25
"Risperidone treatment improved symptoms, disability of the included patients with a significant reduction in the mean total scores of BPRS, CGI and DDS-SV observed from the first month of treatment onwards. "( [Risperidone in the treatment of psychotic patients with opiate abuse and dependence].
Bobes, J; Casas, M; Gibert, J; Gutiérrez, M; Octavio, I; Roncero, C,
)
2.48
"Risperidone treatment was well tolerated, and no clinically relevant changes in EPS."( Effect of risperidone on behavioral and psychological symptoms and cognitive function in dementia.
Ertl, MG; Haushofer, M; Kraxberger, E; Masching, AJ; Rainer, MK, 2001
)
1.43
"Risperidone-treated patients had a significantly higher DAI-10 score compared to haloperidol-treated patients."( Subjective response to antipsychotic treatment and compliance in schizophrenia. A naturalistic study comparing olanzapine, risperidone and haloperidol (EFESO Study).
Edgell, E; García-Cabeza, I; Gómez, JC; González de Chavez, M; Sacristán, JA, 2001
)
1.24
"Risperidone-treated patients did not differ from healthy subjects for PPI with any prepulse trials."( Prepulse inhibition of the startle response in risperidone-treated patients: comparison with typical antipsychotics.
Kumari, V; Sharma, T; Soni, W, 2002
)
1.29
"Risperidone treatment significantly increased the serum PRL levels of schizophrenic patients."( Risperidone-induced increase in serum prolactin is correlated with positive symptom improvement in chronic schizophrenia.
Shen, YC; Wu, GY; Yuan, CL; Zhang, PY; Zhang, XY; Zhou, DF, 2002
)
2.48
"Risperidone treatment was statistically superior to placebo, with a trend toward superiority to haloperidol."( Risperidone: clinical safety and efficacy in schizophrenia.
Borison, RL; Diamond, BI; Meibach, RC; Pathiraja, AP, 1992
)
2.45
"Co-treatment with risperidone and escitalopram (5mg/kg) or mirtazapine (10mg/kg) more efficiently increased the release of 5-HT but not DA in the rat frontal cortex, as compared to drugs given alone."( The effect of chronic co-treatment with risperidone and novel antidepressant drugs on the dopamine and serotonin levels in the rats frontal cortex.
Górska, A; Gołembiowska, K; Kamińska, K; Noworyta-Sokołowska, K; Rogóż, Z; Wojtas, A, 2018
)
1.07
"Treatment with risperidone significantly suppressed the IRS and CIRS."( Activation of the immune-inflammatory response system and the compensatory immune-regulatory system in antipsychotic naive first episode psychosis.
Belangero, SI; Bressan, RA; Cordeiro, Q; Gadelha, A; Maes, M; Noto, C; Noto, MN; Nunes, SOV; Ota, VK; Rossaneis, AC; Verri, WA, 2019
)
0.85
"The treatment with risperidone and aripiprazole in children with psychiatric disorders is not associated with clinically relevant modifications of QT interval."( ECG parameters in children and adolescents treated with aripiprazole and risperidone.
Calabrò, MP; D'Amico, G; Gagliano, A; Germanò, E; Guerriero, L; Ingrassia, M; Italiano, D; Lamberti, M; Privitera, C; Siracusano, R; Spina, E, 2014
)
0.95
"Co-treatment with risperidone (0.01 mg/kg) and mirtazapine (2.5 or 5 mg/kg) abolished the effect of MK-801, whereas those drugs given separately did not change the action of MK-801."( Effect of combined treatment with mirtazapine and risperidone on the MK-801-induced changes in the object recognition test in mice.
Rogóż, Z, 2013
)
0.97
"Treatment with risperidone was immediately discontinued."( Liver enzyme abnormalities during antipsychotic treatment: a case report of risperidone-associated hepatotoxicity.
Berecz, R; Doña, A; Dorado, P; LLerena, A; López-Torres, E; Peñas-LLedó, EM; Süveges, A, 2014
)
0.97
"Treatment with risperidone over 6 weeks led to increased prolactin levels, liver functions, metabolic measures, and weight/body mass index (BMI)."( Placebo-controlled trial of valproic Acid versus risperidone in children 3-7 years of age with bipolar I disorder.
Altaye, M; Delgado, S; Kowatch, RA; Lagory, D; Monroe, E; Scheffer, RE, 2015
)
1.01
"The treatment of risperidone significantly up-regulated the expressions of BDNF and TrkB in prefrontal cortex, temporal cortex and hippocampus, while the expression of P75NTR was not significantly changed."( [Effect of Risperidone on BDNF-TrkB Signaling Pathway in Rat Brain].
Li, T; Liang, LH; Ma, XH; Ni, PY; Wang, X; Wang, YC; Wei, JX; Yu, B; Zhao, LS, 2015
)
1.15
"Treatment with risperidone normalized topological parameters in the limbic system, and the enhancement positively correlated with the reduction in PANSS-positive symptoms."( Risperidone-induced topological alterations of anatomical brain network in first-episode drug-naive schizophrenia patients: a longitudinal diffusion tensor imaging study.
Chen, H; Chen, X; He, Y; Hu, M; Li, Y; Li, Z; Liao, Y; Lv, L; Mann, JJ; Pantazatos, SP; Sang, D; Tang, J; Zhao, H; Zheng, J; Zhou, J; Zong, X, 2016
)
2.22
"Pretreatment with risperidone largely attenuated ketamine-induced changes in FC."( Ketamine-induced changes in connectivity of functional brain networks in awake female nonhuman primates: a translational functional imaging model.
Gopinath, K; Howell, L; Kempf, D; Maltbie, E; Urushino, N, 2016
)
0.76
"Treatment with risperidone significantly increased the plasma NO(x) levels by 8 weeks (before; 1.85 +/- 0.70 microM, after; 2.25 +/- 1.00 microM, p = 0.0491)."( Association between plasma nitric oxide metabolites levels and negative symptoms of schizophrenia: a pilot study.
Hori, H; Ikenouchi-Sugita, A; Nakamura, J; Nakano, H; Nakano, Y; Ueda, N; Umene-Nakano, W; Yoshimura, R, 2010
)
0.7
"Treatment with risperidone for eight weeks (dose range, 0.5 to 3.5 mg per day) resulted in a 56.9 percent reduction in the Irritability score, as compared with a 14.1 percent decrease in the placebo group (P<0.001)."( Risperidone in children with autism and serious behavioral problems.
Aman, MG; Arnold, LE; Carroll, D; Cronin, P; Davies, M; Ghuman, J; Gonzalez, NM; Grados, M; Hollway, J; Hong, D; Koenig, K; Kohn, A; Lancor, A; Lindsay, R; Martin, A; McCracken, JT; McDougle, CJ; McGough, J; McMahon, D; Nash, P; Posey, D; Ritz, L; Robinson, J; Scahill, L; Shah, B; Swiezy, N; Tierney, E; Vitiello, B; Volkmar, F, 2002
)
2.1
"Treatment with risperidone resulted in a significant decrease in the intensity of schizophrenic symptoms and in an improvement in all neuropsychological tests applied."( Risperidone treatment of schizophrenia: improvement in psychopathology and neuropsychological tests.
Araszkiewicz, A; Borkowska, A; Rajewski, A; Rybakowski, JK, 2002
)
2.1
"Treatment with risperidone 0.25-0.5 mg per day was associated with clinically meaningful decreases in problem behaviors including hyperactivity, irritability, and aggressiveness."( Risperidone in the treatment of autistic Thai children under 4 years of age.
Boon-Yasidhi, V; Soising, L; Suwanwattana, C; Tarugsa, J, 2002
)
2.1
"Treatment with risperidone was in most cases effective (72% and 74%, respectively), but effectiveness was established sooner in the adult patients than in the elderly patients (7 versus 14 days)."( Outcomes and costs of treatment with risperidone in adult and elderly patients: the Delta patient using risperidone study.
Loonen, AJ; Loos, JC; Van Zonneveld, TH, 2002
)
0.93
"Treatment with risperidone improves symptoms."( [Autism of unknown aetiology].
Holguín, JA,
)
0.47
"Pretreatment with risperidone (0.5 mg/kg) and ketanserin (5 mg/kg) prevented the development of hyperthermia and the increase in the NA level."( Memantine, an NMDA antagonist, prevents the development of hyperthermia in an animal model for serotonin syndrome.
Kato, S; Nisijima, K; Shioda, K; Takano, K; Yoshino, T, 2004
)
0.65
"Treatment with risperidone was offered to acutely psychotic schizophrenic patients with the requirement of a minimum score of > or =4 on 2 items of the PANSS positive symptoms subscale. "( Risperidone in the treatment of acute schizophrenia.
Naber, D; Raedler, TJ; Schreiner, A; Wiedemann, K, 2004
)
2.12
"Treatment with risperidone reduced the mean CGI score from 5.9 to 4.8 (P < 0.001)."( Risperidone in the treatment of acute schizophrenia.
Naber, D; Raedler, TJ; Schreiner, A; Wiedemann, K, 2004
)
2.11
"Treatment with risperidone is associated with prolactin (PRL) elevation, and PRL elevations are associated with erectile dysfunction (ED). "( Prolactin levels and erectile function in patients treated with risperidone.
Bartztokis, G; Cargile, C; Spollen, JJ; Wooten, RG, 2004
)
0.92
"Treatment with risperidone was frequently associated with hyperprolactinemia and related symptoms, whereas the occurrence of PRL elevation and related symptoms was modest in patients receiving olanzapine and nonexistent in those receiving clozapine. "( Differences in prolactin elevation and related symptoms of atypical antipsychotics in schizophrenic patients.
Melkersson, K, 2005
)
0.68
"Treatment with risperidone for either 3 or 6 weeks in an open trial significantly reduced total and subscales scores on the PANSS and on the PTSD-I and CGI-S when compared to baseline scores in patients with psychotic PTSD."( Risperidone in psychotic combat-related posttraumatic stress disorder: an open trial.
Kozarić-Kovacić, D; Mück-Seler, D; Pivac, N; Rothbaum, BO, 2005
)
2.12
"Treatment with risperidone long-acting injectable was well tolerated, and no significant weight gain occurred during the study."( Sustained improvement of clinical outcome with risperidone long-acting injectable in psychotic patients previously treated with olanzapine.
Frazzingaro, S; Gastpar, M; Latif, MA; Lombertie, ER; Masiak, M; Medori, R, 2005
)
0.93
"Treatment with risperidone at the time of the first episode of schizophrenia is associated with wide-ranging improvements in cognitive functioning. "( Treatment of cognitive impairment in early psychosis: a comparison of risperidone and haloperidol in a large long-term trial.
Davidson, M; Eerdekens, M; Harvey, PD; Rabinowitz, J, 2005
)
0.92
"The treatment with risperidone was well tolerated."( [Changeover to risperidone after treatment with conventional low potency neuroleptics in dementia patients. An observation study during usage].
Schmitt, AB; Schreiner, A; Stoppe, G, 2006
)
1.01
"Treatment with risperidone or quetiapine was associated with the lowest overall costs when compared with olanzapine or clozapine."( Resource utilization in a Canadian national study of people with schizophrenia and related psychotic disorders.
Balshaw, R; Kopala, L; Love, L; Malla, A; Smith, G; Talling, D; Williams, R, 2006
)
0.69
"Treatment with risperidone for 8 weeks, but not 2 or 4 weeks, significantly improved working memory performance. "( Propranolol blocks chronic risperidone treatment-induced enhancement of spatial working memory performance of rats in a delayed matching-to-place water maze task.
Dawe, GS; Lim, EP; Nagarajah, R; Verma, V, 2007
)
0.99
"Treatment with risperidone was correlated with resolution of her psychosis and improvement in neuropsychiatric symptoms."( Hashimoto encephalopathy responding to risperidone.
Bismilla, Z; Donner, E; Sell, E, 2007
)
0.95
"Treatment with risperidone for 4 weeks did not increase daily cigarette consumption or plasma levels of cotinine and caffeine."( Acute risperidone treatment did not increase daily cigarette consumption or plasma levels of cotinine and caffeine: a pilot study.
Hori, H; Kakihara, S; Nakamura, J; Sugita, A; Ueda, N; Umene-Nakano, W; Yoshimura, R, 2008
)
1.17
"Treatment with risperidone solution orally or parenteral haloperidol until the day after admission, followed by olanzapine, successfully improved the clinical condition of the patients. "( Three cases of schizophrenia for which olanzapine was effective after early acute phase.
Inada, T; Oda, T; Yamamoto, N, 2008
)
0.7
"Treatment with risperidone appears to exert a more favorable effect on verbal working memory than treatment with a conventional neuroleptic. "( Does risperidone improve verbal working memory in treatment-resistant schizophrenia?
Ames, D; Green, MF; Kern, RS; Marder, SR; Marshall, BD; McGurk, S; Mintz, J; Wirshing, WC, 1997
)
1.16
"When treated with risperidone 2 mg/day, both his sleep and the delusional thoughts improved markedly and his daytime alertness increased."( Beneficial effect of risperidone on sleep disturbance and psychosis following traumatic brain injury.
Gross, Y; Klag, E; Pick, CG; Schreiber, S; Segman, RH, 1998
)
0.94
"Treatment with risperidone, 6 mg/day, is likely to induce unnecessarily high D2 receptor occupancy, with a consequent risk of extrapyramidal side effects. "( Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients.
Eriksson, B; Farde, L; Halldin, C; Nyberg, S; Oxenstierna, G, 1999
)
0.93
"Oral treatment with risperidone and lorazepam appears to be a tolerable and comparable alternative to intramuscular haloperidol and lorazepam for short-term treatment of agitated psychosis in patients who accept oral medications."( Risperidone liquid concentrate and oral lorazepam versus intramuscular haloperidol and intramuscular lorazepam for treatment of psychotic agitation.
Currier, GW; Simpson, GM, 2001
)
2.08
"Treatment with risperidone, though, results in considerably elevated plasma prolactin (PRL) levels which are not observed with other atypical neuroleptics, such as clozapine, indicating a differentiated action on receptors that are involved in PRL release, mainly dopaminergic and serotonergic."( Neuroendocrine serotonergic and dopaminergic responsivity in male schizophrenic patients during treatment with neuroleptics and after switch to risperidone.
Hatzimanolis, J; Lykouras, L; Markianos, M, 2001
)
0.85
"Treatment with risperidone was initiated at a dosage of 2 mg daily, increased to the target dosage of 6 mg daily by day 3, and maintained at 6 mg daily until day 14."( Risperidone treatment of outpatients with schizophrenia: no evidence of sex differences in treatment response.
Dunbar, F; Labelle, A; Light, M, 2001
)
2.09
"Treatment on risperidone also resulted in significant reduction in the PANSS score."( The effect of risperidone on cognitive functioning in a sample of Asian patients with schizophrenia in Singapore.
Chan, YH; Chong, SA; Chua, L; Ng, VP; Pang, E, 2001
)
1.02
"Treatment with risperidone was accompanied by an improvement in global functioning in patients with average to above-average impairment at baseline as measured by the Global Assessment of Functioning scale."( Risperidone in the treatment of tourette syndrome: a double-blind, placebo-controlled trial.
Annable, L; Chouinard, G; Dion, Y; Sandor, P, 2002
)
2.1
"Treatment with risperidone was associated with improvement in antisaccade errors."( Improved antisaccade performance with risperidone in schizophrenia.
Burke, JG; Reveley, MA, 2002
)
0.94

Toxicity

The Liverpool University Neuroleptic Side Effect Rating Scale (LUNSERS) was completed by 66 patients aged between 6 and 18 years. Young persons seemed to tolerate risperidone well, but longer exposure to the medication was associated with higher side effect levels.

ExcerptReferenceRelevance
" There were no major adverse reactions associated with risperidone use, but it was noted to reduce the signs of tardive dyskinesia."( Risperidone: clinical safety and efficacy in schizophrenia.
Borison, RL; Diamond, BI; Meibach, RC; Pathiraja, AP, 1992
)
1.97
"Compared to traditional neuroleptics, most of the new antipsychotics are characterized by a low extrapyramidal side effect (EPS) liability and varying antipsychotic efficacy."( New antipsychotics: classification, efficacy, and adverse effects.
Gerlach, J, 1991
)
0.28
" Other adverse effects were assessed using the UKU Side Effects Scale."( Extrapyramidal side effects and tolerability of risperidone: a review.
Owens, DG, 1994
)
0.54
"The purpose of this study was to compare the side effect +profiles of clozapine and risperidone."( Different side effect profiles of risperidone and clozapine in 20 outpatients with schizophrenia or schizoaffective disorder: a pilot study.
Daniel, DG; Goldberg, TE; Kleinman, JE; Lubick, LJ; Pickar, D; Weinberger, DR; Williams, TS, 1996
)
0.8
"In this exploratory study, the side effect profiles of clozapine and risperidone were consistent with the different pharmacodynamic profiles of the two drugs."( Different side effect profiles of risperidone and clozapine in 20 outpatients with schizophrenia or schizoaffective disorder: a pilot study.
Daniel, DG; Goldberg, TE; Kleinman, JE; Lubick, LJ; Pickar, D; Weinberger, DR; Williams, TS, 1996
)
0.81
" Considerable progress has been made in improving the motor side effect profile with the advent of clozapine and risperidone."( Side effect profiles of new antipsychotic agents.
Casey, DE, 1996
)
0.5
" The proportion of patients failing to reach at least 20% improvement on the positive and negative syndrome scale (PANSS) or brief psychiatric rating scale (BPRS), the proportion of patients discontinuing treatment because of adverse effects and the number of patients who needed antiparkinsonian medication were abstracted for use as outcome measures."( Risperidone versus haloperidol in the treatment of schizophrenia: a meta-analysis comparing their efficacy and safety.
Bacaltchuk, J; de Castro-e-Silva, E; de Oliveira, IR; de Sena, EP; Miranda-Scippa, AM; Pereira, EL; Ribeiro, MG, 1996
)
1.74
"The purpose of this case study is to document hepatic adverse effects associated with long-term risperidone use in pediatric populations."( Case study: risperidone-induced hepatotoxicity in pediatric patients.
Briguglia, C; Grothe, D; Herion, D; Jacobsen, LK; Kumra, S, 1997
)
0.89
" The adverse effects of risperidone may be due to the lack of development of acute tolerance to its powerful serotonergic (5-HT2A) antagonism, which could be responsible for the disruption of brainstem physiology in regions controlling saccadic eye movements."( Adverse effects of risperidone on eye movement activity: a comparison of risperidone and haloperidol in antipsychotic-naive schizophrenic patients.
Bauer, KS; Haas, GL; Keshavan, MS; Kroboth, PD; Schooler, NR; Sweeney, JA, 1997
)
0.93
" One general rule that may reduce the risks of toxic drug interactions is to add medication to the patient's current regimen in modest doses and increase the dose slowly."( Mood stabilizer combinations: a review of safety and efficacy.
Freeman, MP; Stoll, AL, 1998
)
0.3
" No correlation between the serum concentration of the active moiety and the side effects evaluated by the UKU Side Effect Scale was found."( Serum concentrations and side effects in psychiatric patients during risperidone therapy.
Bruun, T; Licht, RW; Linnet, K; Olesen, OV; Thomsen, E; Viftrup, JE, 1998
)
0.53
" Thus, clinicians should address patients' concerns about adverse effects and attempt to choose medications that will improve their patients' quality of life as well as overall health."( Adverse effects of the atypical antipsychotics. Collaborative Working Group on Clinical Trial Evaluations.
, 1998
)
0.3
" The two largest studies (the North American and multinational trials) included 841 patients (259 women, 582 men) with paired prolactin level data and 1,884 patients (554 women, 1,330 men) with data on six adverse events possibly associated with increased prolactin levels (amenorrhea, galactorrhea, and decreased libido in women; erectile dysfunction, ejaculatory dysfunction, gynecomastia, and decreased libido in men)."( Prolactin levels and adverse events in patients treated with risperidone.
Brecher, M; Davis, JM; de Coster, R; Kleinberg, DL; Van Baelen, B, 1999
)
0.54
"To compare the side effect profile of risperidone with that of oral haloperidol in patients with no previous exposure to antipsychotic drugs (APDs)."( Neurologic side effects in neuroleptic-naive patients treated with haloperidol or risperidone.
Mazurek, MF; Rosebush, PI, 1999
)
0.8
"Early studies suggested that the APD risperidone may have a side effect profile comparable with that of placebo."( Neurologic side effects in neuroleptic-naive patients treated with haloperidol or risperidone.
Mazurek, MF; Rosebush, PI, 1999
)
0.8
"The neurologic side effect profile of low-dose risperidone is comparable with that of haloperidol in patients receiving APDs for the first time."( Neurologic side effects in neuroleptic-naive patients treated with haloperidol or risperidone.
Mazurek, MF; Rosebush, PI, 1999
)
0.79
" To prove whether weight gain is a relevant side effect of atypical neuroleptics, the charts of all patients admitted with DSM-III-R diagnoses of schizophrenia, schizoaffective disorder, or delusional disorder in the years 1991 to 1995 were evaluated."( Weight gain: side effect of atypical neuroleptics?
Müssigbrodt, HE; Wetterling, T, 1999
)
0.3
" The side effects associated with traditional antipsychotic treatment are generally minimal in patients who take risperidone, a combined 5-HT2/D2 antagonist, but the literature is sparse on adverse events among the newer atypical antipsychotics."( Risperidone side effects.
Conley, RR, 2000
)
1.96
" Compared with traditional agents, olanzapine shows only a few adverse events such as dry mouth, sedation, and increase in appetite."( Adverse events related to olanzapine.
Conley, RR; Meltzer, HY, 2000
)
0.31
" Their adverse effects, which include extrapyramidal side effects, tardive dyskinesia, weight gain, sedation, and sexual dysfunction, often lead to non-compliance; their use may have a negative impact on the overall course of illness; and they may not be as effective as lithium in treating the core manic symptoms over the long term."( Antipsychotic drug side effect issues in bipolar manic patients.
Zarate, CA, 2000
)
0.31
" Safety was monitored by open adverse event reporting, the Simpson-Angus Scale, the Barnes Akathisia Scale and the Abnormal Involuntary Movement scale."( Safety profile of amisulpride in short- and long-term use.
Coulouvrat, C; Dondey-Nouvel, L; Rein, W, 2000
)
0.31
" Olanzapine seems to be safe in this patient, since no major decreases of haematological parameters were observed."( Olanzapine appears haematologically safe in patients who developed blood dyscrasia on clozapine and risperidone.
Dernovsek, MZ; Tavcar, R, 2000
)
0.52
" No patient experienced serious extrapyramidal side effects, sedation, or any other adverse event during the rapid titration, and in no case did risperidone have to be discontinued."( Safety and tolerability of a rapidly escalating dose-loading regimen for risperidone.
Feifel, D; Moutier, CY; Perry, W, 2000
)
0.74
" Assessments included the YMRS, the Positive and Negative Syndrome Scale (PANSS), the Hamilton Rating Scale for Depression (HAM-D), the 4-item Clinical Global Impressions (CGI) scale, and the UKU Side Effect Rating Scale subscale for neurologic side effects."( Efficacy and safety of risperidone in the treatment of schizoaffective disorder: initial results from a large, multicenter surveillance study. Group for the Study of Risperidone in Affective Disorders (GSRAD).
Benabarre, A; Colom, F; Fernández, A; Gastó, C; Herraiz, M; Martínez-Arán, A; Reinares, M; Vieta, E, 2001
)
0.62
" Despite the limitations of the open-label design, the results indicate that risperidone is a safe and effective therapy in combination with mood-stabilizers for the treatment of patients with manic, hypomanic, and depressive symptoms of mixed episodes in schizoaffective disorder, bipolar type."( Efficacy and safety of risperidone in the treatment of schizoaffective disorder: initial results from a large, multicenter surveillance study. Group for the Study of Risperidone in Affective Disorders (GSRAD).
Benabarre, A; Colom, F; Fernández, A; Gastó, C; Herraiz, M; Martínez-Arán, A; Reinares, M; Vieta, E, 2001
)
0.85
" The design of the most comprehensive of these, the Extrapyramidal Symptom Rating Scale (ESRS), is exhaustive, and it successfully quantifies EPS and distinguishes toxic from nontoxic medications."( Scales to assess efficacy and safety of pharmacologic agents in the treatment of behavioral and psychological symptoms of dementia.
De Deyn, PP; Wirshing, WC, 2001
)
0.31
"In 2 pivotal trials comparing risperidone with placebo, the risk of adverse events was similar in both treatment groups when risperidone was given at the optimal clinical dose (1 mg/day)."( Long-term safety of risperidone.
Davidson, M, 2001
)
0.92
" We conducted a survey of Spanish psychiatrists in mental health centers and outpatient treatment units to assess the severity scores that they would assign to a list of the most common adverse events (AEs) that usually occur with antipsychotic treatment."( Global index of safety (GIS): a new instrument to assess drug safety.
Badía, X; Gómez, JC; Kind, P; Sacristán, JA, 2001
)
0.31
" Adverse effects were monitored in all 110 patients."( The efficacy and safety of risperidone for the treatment of geriatric psychosis.
Chang, JW; Cheng, CY; Hwang, JP; Tsai, SJ; Yang, CH; Yu, HC, 2001
)
0.61
" Doses were adjusted to maximize efficacy and to minimize adverse events."( A comparison of the relative safety, efficacy, and tolerability of quetiapine and risperidone in outpatients with schizophrenia and other psychotic disorders: the quetiapine experience with safety and tolerability (QUEST) study.
Jibson, MD; Mullen, J; Sweitzer, D, 2001
)
0.54
" The most common adverse events in the quetiapine and risperidone groups were somnolence (31."( A comparison of the relative safety, efficacy, and tolerability of quetiapine and risperidone in outpatients with schizophrenia and other psychotic disorders: the quetiapine experience with safety and tolerability (QUEST) study.
Jibson, MD; Mullen, J; Sweitzer, D, 2001
)
0.78
" These preliminary results suggest that crossover from haloperidol to risperidone is generally safe and effective and may produce favorable moods in agitated dementia patients."( Shifting from haloperidol to risperidone for behavioral disturbances in dementia: safety, response predictors, and mood effects.
Chang, WH; Chang, YC; Chiu, CC; Huang, MC; Lane, HY; Su, MH, 2002
)
0.84
" Extrapyramidal symptoms (EPS) were assessed using the UKU Side Effect Rating Scale."( Risperidone safety and efficacy in the treatment of bipolar and schizoaffective disorders: results from a 6-month, multicenter, open study.
Benabarre, A; Colom, F; Corbella, B; Fernández, A; Goikolea, JM; Martínez, G; Martínez-Arán, A; Reinares, M; Torrent, C; Vieta, E, 2001
)
1.75
" Adverse events were few and mostly mild."( Risperidone safety and efficacy in the treatment of bipolar and schizoaffective disorders: results from a 6-month, multicenter, open study.
Benabarre, A; Colom, F; Corbella, B; Fernández, A; Goikolea, JM; Martínez, G; Martínez-Arán, A; Reinares, M; Torrent, C; Vieta, E, 2001
)
1.75
"Converging evidence indicates that, in controlled drug trials, individuals receiving novel antipsychotic medications have fewer adverse effects than those receiving conventional antipsychotic medications."( Short report: comparison of patient satisfaction and burden of adverse effects with novel and conventional neuroleptics: a naturalistic study.
Bromet, EJ; Davidson, M; Rabinowitz, J, 2001
)
0.31
"Psychopharmacology research aims to expand the therapeutic ratio between efficacy, on the one hand, and adverse events and safety, on the other."( Psychotropic drugs and adverse events in the treatment of bipolar disorders revisited.
McIntyre, RS, 2002
)
0.31
"The effects of haloperidol, risperidone, and thioridazine on the pharmacokinetics and side-effect profile of quetiapine were investigated in 36 patients with schizophrenia, schizoaffective disorder, or bipolar disorder in a single-center, two-period, multiple-dose, open-label, randomized trial."( The safety and pharmacokinetics of quetiapine when coadministered with haloperidol, risperidone, or thioridazine.
Alva, G; Arvanitis, LA; Bera, R; Potkin, SG; Thyrum, PT; Yeh, C, 2002
)
0.83
" The severity and incidence of extrapyramidal symptoms and adverse events did not significantly increase when fluoxetine was added."( The effect of fluoxetine on the pharmacokinetics and safety of risperidone in psychotic patients.
Baumann, P; Bertschy, G; Bondolfi, G; Eap, CB; Vermeulen, A; Zullino, D, 2002
)
0.55
" Adverse events caused by co-administration were assessed."( A pilot, randomized, open-label trial assessing safety and pharmakokinetic parameters of co-administration of rivastigmine with risperidone in dementia patients with behavioral disturbances.
Anand, R; Cicin-Sain, A; Hartman, R; Korczyn, AD; Rotmensch, HH; Weiser, M, 2002
)
0.52
"No clinically relevant adverse interactions were observed."( A pilot, randomized, open-label trial assessing safety and pharmakokinetic parameters of co-administration of rivastigmine with risperidone in dementia patients with behavioral disturbances.
Anand, R; Cicin-Sain, A; Hartman, R; Korczyn, AD; Rotmensch, HH; Weiser, M, 2002
)
0.52
"The novel antipsychotic medications offer a more favorable extrapyramidal side effect profile than conventional agents."( Sexual side effects of novel antipsychotic medications.
Marder, SR; Pierre, JM; Saunders, CS; Wirshing, DA; Wirshing, WC, 2002
)
0.31
"Sexual side effects are common clinically pertinent adverse effects associated with both novel and conventional antipsychotic medications."( Sexual side effects of novel antipsychotic medications.
Marder, SR; Pierre, JM; Saunders, CS; Wirshing, DA; Wirshing, WC, 2002
)
0.31
"This open study provides further evidence that risperidone is safe and effective in combination with mood stabilisers in the manic phase of bipolar disorder."( Risperidone in the treatment of mania: efficacy and safety results from a large, multicentre, open study in Spain.
Benabarre, A; Fernández, A; Goikolea, JM; Herraiz, M; Parramon, G; Vieta, E, 2002
)
2.01
" Galantamine and risperidone were both safe and well tolerated administered either alone or together."( Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs are administered alone and together.
Huang, F; Janssens, L; Lasseter, KC; Lau, H; Verhaeghe, T; Zhao, Q, 2002
)
0.9
" Adverse events (predominantly headache, nervousness, and somnolence) were minor and comparable for all treatment groups."( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil.
Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003
)
0.55
" This is because of their efficacy in the treatment of several psychiatric disorders, ease of administration, and absence of the well-known extrapyramidal adverse effects long-attributed to the standard dopamine blocking anti-psychotic medications."( Atypical psychotropic medications and their adverse effects: a review for the African-American primary care physician.
Bailey, RK, 2003
)
0.32
" Adverse events related to extrapyramidal symptoms were spontaneously reported by 13% of patients receiving placebo and 10% of patients in the 25-mg risperidone group, with higher rates in the 50-mg and 75-mg groups."( Long-acting injectable risperidone: efficacy and safety of the first long-acting atypical antipsychotic.
Eerdekens, M; Kane, JM; Karcher, K; Keith, SJ; Lesem, M; Lindenmayer, JP, 2003
)
0.83
"To assess the adverse events associated with the appropriate use of oral risperidone and oral olanzapine in long-term care patients with behavioral and psychotic disturbances associated with dementia."( Safety profile assessment of risperidone and olanzapine in long-term care patients with dementia.
Cornacchione, MJ; Deymann, S; Martin, H; Slyk, MP,
)
0.65
" Adverse events of particular significance in the elderly population, including agitation/anxiety, laxative use, dry eyes, and falls, were collected from audited medical records."( Safety profile assessment of risperidone and olanzapine in long-term care patients with dementia.
Cornacchione, MJ; Deymann, S; Martin, H; Slyk, MP,
)
0.42
"Among long-term care residents with dementia who received low doses of risperidone or olanzapine, the incidence of adverse events was low."( Safety profile assessment of risperidone and olanzapine in long-term care patients with dementia.
Cornacchione, MJ; Deymann, S; Martin, H; Slyk, MP,
)
0.66
" Side effects were monitored using the Abnormal Involuntary Movement Scale, the Simpson-Angus Scale, the Barnes Akathisia Rating Scale, and the Udvalg for Kliniske Undersogelser Side Effect Rating Scale."( Effectiveness, safety, and tolerability of risperidone in adolescents with schizophrenia: an open-label study.
Bensason, D; Carmon, E; Martin, A; Tyano, S; Weizman, A; Zalsman, G, 2003
)
0.58
" The aim of this study is to explore the adverse effects of conventional and atypical antipsychotic drugs and their associated factors."( Adverse effects of risperidone and haloperidol treatment in schizophrenia.
Chong, MY; Lung, FW; Yen, YC, 2004
)
0.65
" The safety and tolerability were assessed with the Extrapyramidal Symptom Rating Scale, the UKU Side-Effect Rating Scale and clinical laboratory assessments."( Adverse effects of risperidone and haloperidol treatment in schizophrenia.
Chong, MY; Lung, FW; Yen, YC, 2004
)
0.65
" The most frequent adverse effects for both groups were tremor and rigidity."( Adverse effects of risperidone and haloperidol treatment in schizophrenia.
Chong, MY; Lung, FW; Yen, YC, 2004
)
0.65
" The aim of this paper is to review literature about newer antipsychotics, focusing on their advantages in terms of efficacy and side effect profiles when compared to classical and older atypical antipsychotics, and to evaluate the efficacy of the different new antipsychotics when compared to one another."( New antipsychotics and schizophrenia: a review on efficacy and side effects.
Berardi, D; De Ronchi, D; Lorenzi, C; Serretti, A, 2004
)
0.32
" While typical antipsychotics are often switched to atypical agents when adverse effects become limiting, there is little preclinical information to support this strategy, both in terms of efficacy and side effects."( Combined treatment of quetiapine with haloperidol in animal models of antipsychotic effect and extrapyramidal side effects: comparison with risperidone and chlorpromazine.
Matsuoka, N; Mutoh, S; Shirakawa, K; Tada, M, 2004
)
0.53
" Adverse events related to movement disorders were reported in 3%."( Long-acting injectable risperidone: safety and efficacy in stable patients switched from conventional depot antipsychotics.
Eerdekens, E; Eerdekens, M; Jacko, M; Turner, M, 2004
)
0.63
" Of the 141 patients who participated in the study, the most frequently reported adverse events were insomnia (16%), headache (15%), psychosis (11%), and agitation (11%)."( Safety and efficacy of long-acting risperidone in schizophrenia: a 12-week, multicenter, open-label study in stable patients switched from typical and atypical oral antipsychotics.
Berry, SA; Eerdekens, E; Eerdekens, M; Lindenmayer, JP, 2004
)
0.6
"Switching treatment from oral antipsychotics to long-acting risperidone without an intervening period of oral risperidone was safe and well tolerated."( Safety and efficacy of long-acting risperidone in schizophrenia: a 12-week, multicenter, open-label study in stable patients switched from typical and atypical oral antipsychotics.
Berry, SA; Eerdekens, E; Eerdekens, M; Lindenmayer, JP, 2004
)
0.84
" Adverse events reported in >10% of patients were insomnia (14%), constipation (12%), and bronchitis (12%)."( Efficacy and safety of long-acting risperidone in elderly patients with schizophrenia and schizoaffective disorder.
Bossie, CA; Davidson, M; Eerdekens, M; Gharabawi, G; Lasser, RA; Zhu, Y, 2004
)
0.6
" Safety measures included the recording of spontaneous adverse events and extrapyramidal symptoms (EPS)."( Safety and tolerability of olanzapine compared with other antipsychotics in the treatment of elderly patients with schizophrenia: a naturalistic study.
Ciudad, A; Gómez, JC; Montes, JM; Olivares, JM, 2004
)
0.32
"The incidence of overall adverse events and EPS was non-significantly lower in patients treated with olanzapine than in patients treated with other antipsychotics."( Safety and tolerability of olanzapine compared with other antipsychotics in the treatment of elderly patients with schizophrenia: a naturalistic study.
Ciudad, A; Gómez, JC; Montes, JM; Olivares, JM, 2004
)
0.32
"Results from this naturalistic study showed that olanzapine was as safe and effective as other antipsychotic drugs in the treatment of elderly patients with schizophrenia."( Safety and tolerability of olanzapine compared with other antipsychotics in the treatment of elderly patients with schizophrenia: a naturalistic study.
Ciudad, A; Gómez, JC; Montes, JM; Olivares, JM, 2004
)
0.32
" The most common adverse event in both treatment groups was diarrhoea (6/16 risperidone + donepezil HCl patients and 9/16 donepezil HCl only subjects)."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.81
"Five new antipsychotic drugs introduced in the United States in the last decade offer physicians the ability to treat patients with schizophrenia and bipolar mania without the adverse effects of the first-generation antipsychotics."( The promise of atypical antipsychotics: fewer side effects mean enhanced compliance and improved functioning.
Citrome, L; Volavka, J, 2004
)
0.32
" No unexpected adverse events were recorded."( Comparative efficacy and safety of long-acting risperidone and risperidone oral tablets.
Augustyns, I; Chue, P; David, AS; Eerdekens, M; Eriksson, L; Lachaux, B; Molcan, P; Pretorius, H, 2005
)
0.59
" The only side effect significantly more severe in risperidone-treated compared to placebo-treated patients was sedation."( A double-blind controlled study of adjunctive treatment with risperidone in schizophrenic patients partially responsive to clozapine: efficacy and safety.
Alptekin, K; Anil Yağcioğlu, AE; Ertuğrul, A; Göğüş, A; Jayathilake, K; Kivircik Akdede, BB; Meltzer, HY; Tümüklü, M; Tunca, Z; Turgut, TI; Yazici, MK, 2005
)
0.82
" However, there are still significant adverse effects and toxicities with this class of medications."( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer?
Dubois, D, 2005
)
0.33
"Continued research to evaluate adverse effects and tolerability of atypical antipsychotics compared with first-generation antipsychotics and each other is reviewed."( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer?
Dubois, D, 2005
)
0.33
"While new atypical antipsychotic medications may have a safer therapeutic and overdose profile than first-generation antipsychotic medications, many adverse and toxic effects still need to be considered in therapeutic monitoring and overdose management."( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer?
Dubois, D, 2005
)
0.33
" Side effects were carefully monitored using adverse event evaluation charts."( Effectiveness and safety of risperidone for children and adolescents with chronic tic or tourette disorders in Korea.
Cho, SC; Hwang, JW; Kim, BN; Lee, CB; Shin, MS, 2005
)
0.62
" Psychotic symptoms were assessed by the Positive and Negative Syndrome Scale (PANSS); movement disorders by the Extrapyramidal Symptom Rating Scale (ESRS); adverse events (AEs) were reported spontaneously."( Lack of impact of race on the efficacy and safety of long-acting risperidone versus placebo in patients with schizophrenia or schizoaffective disorder.
Bossie, CA; Ciliberto, N; Lasser, RA; Urioste, R, 2005
)
0.57
"Treatment-emergent adverse events (AEs) were monitored during an 8-week, double-blind, placebo-controlled trial of risperidone (0."( Acute and long-term safety and tolerability of risperidone in children with autism.
Aman, MG; Arnold, LE; Chuang, S; Davies, M; Ghuman, JK; Gonzalez, NM; Koenig, K; Lindsay, RL; Martin, A; McCracken, JT; McDougle, CJ; McGough, J; Nash, PL; Posey, DJ; Ritz, L; Scahill, L; Shah, B; Swiezy, NB; Tierney, E; Vitiello, B, 2005
)
0.8
"Both drugs were well tolerated and their use was associated with fewer symptoms of schizophrenia and less adverse effects than were seen when the patients were taking a typical antipsychotic at baseline."( A comparison of the efficacy and safety of olanzapine and risperidone in the treatment of elderly patients with schizophrenia: an open study of six months duration.
Ames, D; Chiu, E; Hall, K; Halliday, G; Harrigan, S; Hassett, A; Hustig, H; MacFarlane, S; Mastwyk, M; Nagalingam, V; O'Connor, DW; Opie, J; Ritchie, CW; Snowdon, J, 2006
)
0.58
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Safety was assessed using the Extrapyramidal Symptom Rating Scale (ESRS), clinical laboratory tests, electrocardiograms, and the recording of adverse events, vital signs, Tanner score, and changes in body mass index (BMI)."( Long-term safety and efficacy of risperidone in children with disruptive behaviour disorders. Results of a 2-year extension study.
Augustyns, I; Csaba, K; Eerdekens, M; Olah, R; Reyes, M, 2006
)
0.62
" Most adverse events were mild or moderate in severity, and none of them were considered probably or very likely related to risperidone."( Long-term safety and efficacy of risperidone in children with disruptive behaviour disorders. Results of a 2-year extension study.
Augustyns, I; Csaba, K; Eerdekens, M; Olah, R; Reyes, M, 2006
)
0.82
"Continuing low-dose risperidone for up to 3 years appears to be safe and effective in children with disruptive behaviour disorders."( Long-term safety and efficacy of risperidone in children with disruptive behaviour disorders. Results of a 2-year extension study.
Augustyns, I; Csaba, K; Eerdekens, M; Olah, R; Reyes, M, 2006
)
0.94
" Safety and tolerability were good overall, with the number of adverse events (AEs) decreasing in the extension trial, compared to the original trial."( Long-term use of risperidone in children with disruptive behavior disorders and subaverage intelligence: efficacy, safety, and tolerability.
Augustyns, I; Croonenberghs, J; Eerdekens, M; Reyes, M, 2006
)
0.67
"Risperidone is safe and effective in treating DBDs in children over a cumulative period of 2 years."( Long-term use of risperidone in children with disruptive behavior disorders and subaverage intelligence: efficacy, safety, and tolerability.
Augustyns, I; Croonenberghs, J; Eerdekens, M; Reyes, M, 2006
)
2.12
" When patients were switched directly or indirectly from another antipsychotic agent, LAR was generally well tolerated, with a low incidence of withdrawals due to adverse events (1%-16%)."( Long-acting risperidone: focus on safety.
Möller, HJ, 2006
)
0.71
" When patients were switched from other antipsychotics, use of LAR was not associated with an increased risk of adverse events compared with placebo."( Long-acting risperidone: focus on safety.
Möller, HJ, 2006
)
0.71
" Most frequent adverse events were psychosis, headache, insomnia, agitation, and rhinitis."( Long-term safety and tolerability of long-acting injectable risperidone in patients with schizophrenia or schizoaffective disorder.
Eerdekens, M; Khan, A; Kushner, S; Lindenmayer, JP; Van Hove, I, 2007
)
0.58
"Preschool children tolerated low-dose risperidone well with no serious adverse effects observed over a 6-month treatment period."( Risperidone in preschool children with autistic spectrum disorders: an investigation of safety and efficacy.
Belden, A; Heffelfinger, A; Luby, J; Mrakotsky, C; Spitznagel, E; Stalets, MM; Williams, M, 2006
)
2.05
" This occurred in the absence of any generalized adverse effect on oculomotor systems or significant extrapyramidal adverse effects."( Adverse effects of risperidone on spatial working memory in first-episode schizophrenia.
Harris, MS; Keshavan, MS; Reilly, JL; Sweeney, JA, 2006
)
0.66
" Studies with nonhuman primates performing oculomotor delayed response tasks suggest that the apparent adverse effect of risperidone might result from treatment-related changes in modulatory functions of prefrontal D1 receptor systems."( Adverse effects of risperidone on spatial working memory in first-episode schizophrenia.
Harris, MS; Keshavan, MS; Reilly, JL; Sweeney, JA, 2006
)
0.87
" Extrapyramidal symptoms (EPS), weight gain, serum prolactin level, QTc interval, and self-reported adverse events were assessed as measures of safety and tolerability."( Efficacy and safety of aripiprazole in the acute treatment of schizophrenia in Chinese patients with risperidone as an active control: a randomized trial.
Chan, HY; Chiang, SC; Hwang, TJ; Hwu, HG; Lin, SK; Lin, WW; Su, TP, 2007
)
0.56
" Most people did not have any adverse effects; 5 patients (15."( Behavioral and psychological symptoms of dementia (BPSD) in elderly demented subjects: is the long lasting use of atypical antipsychotic drugs useful and safe?
Angelini, A; Bendini, C; Neri, M; Neviani, F, 2007
)
0.34
" Safety was evaluated by recording treatment-emergent adverse events, vital signs, body weight and, when available, laboratory parameters."( [Safety and tolerability of olanzapine versus risperidone: a one-year randomized study in outpatients with schizophrenia with prominent negative symptoms].
Alvarez, E; Bousoño, M; Ciudad, A; Gómez, JC; Olivares, JM,
)
0.39
"0292) and risperidone patients reported significantly more sexual adverse events (21."( [Safety and tolerability of olanzapine versus risperidone: a one-year randomized study in outpatients with schizophrenia with prominent negative symptoms].
Alvarez, E; Bousoño, M; Ciudad, A; Gómez, JC; Olivares, JM,
)
0.79
"Significantly less treatment-emergent extrapyramidal and sexual adverse events were observed in patients treated with olanzapine compared to those treated with risperidone."( [Safety and tolerability of olanzapine versus risperidone: a one-year randomized study in outpatients with schizophrenia with prominent negative symptoms].
Alvarez, E; Bousoño, M; Ciudad, A; Gómez, JC; Olivares, JM,
)
0.59
" Cerebrovascular adverse events and all-cause mortality were observed more frequently, although not statistically significantly, with risperidone versus placebo."( The efficacy and safety of risperidone in the treatment of psychosis of Alzheimer's disease and mixed dementia: a meta-analysis of 4 placebo-controlled clinical trials.
Brodaty, H; de Deyn, PP; Greenspan, A; Katz, I; Mintzer, J; Zhu, Y, 2007
)
0.84
"The aim of this study was to determine the risk of adverse events for risperidone and haloperidol in delirium patients."( Comparison of the risk of adverse events between risperidone and haloperidol in delirium patients.
Hoshino, S; Miyaji, S; Miyaoka, H; Sakai, Y; Yamamoto, H; Yamamoto, K, 2007
)
0.83
" Safety evaluations included the incidence of extrapyramidal symptoms (EPS) and adverse events (AEs)."( Quetiapine versus risperidone in elderly patients with behavioural and psychological symptoms of dementia: efficacy, safety and cognitive function.
Haushofer, M; Pfolz, H; Rainer, M; Struhal, C; Wick, W, 2007
)
0.67
" Safety outcome measures were all new clinical adverse events between the start of treatment (which could be before April 2003) and 30 November 2004."( Safety and usage of atypical antipsychotic medicines in children: a nationwide prospective cohort study.
Ashton, J; Garcia-Quiroga, J; Harrison-Woolrych, M; Herbison, P, 2007
)
0.34
" A total of 131 (31%) children experienced an adverse event."( Safety and usage of atypical antipsychotic medicines in children: a nationwide prospective cohort study.
Ashton, J; Garcia-Quiroga, J; Harrison-Woolrych, M; Herbison, P, 2007
)
0.34
" Study outcomes included adverse events, movement disorder severity, psychiatric symptoms, functional ability, quality of life and patient satisfaction."( Long-term safety and efficacy of long-acting risperidone in elderly psychotic patients.
Glue, P; Kissling, W; Medori, R; Simpson, S, 2007
)
0.6
" In addition, adverse events were also evaluated."( [A naturalistic, observational study of outpatients with schizophrenia: efficacy and safety results after 6 months. The International Schizophrenia Outpatient Health Outcomes study, IC-SOHO].
Agoston, T; István, S; Tamás, T; Zoltán, J, 2007
)
0.34
" Based on recent criteria for pediatric populations, patients were considered "at risk for adverse health outcome" if they met at least 1 of the following criteria: (1) > or = 85th BMI percentile plus presence of 1 or more negative weight-related clinical outcomes, or (2) > or = 95th BMI percentile."( Metabolic and hormonal side effects in children and adolescents treated with second-generation antipsychotics.
Arango, C; Cifuentes, A; Fraguas, D; Giráldez, M; Laita, P; Merchán-Naranjo, J; Moreno, D; Parellada, M; Ruiz-Sancho, A, 2008
)
0.35
" The number of patients at risk for adverse health outcome increased from 11 (16."( Metabolic and hormonal side effects in children and adolescents treated with second-generation antipsychotics.
Arango, C; Cifuentes, A; Fraguas, D; Giráldez, M; Laita, P; Merchán-Naranjo, J; Moreno, D; Parellada, M; Ruiz-Sancho, A, 2008
)
0.35
" Safety and tolerability were assessed by monitoring adverse events, extrapyramidal symptoms (EPS), laboratory values, electrocardiograms, prolactin levels, and weight."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.35
" The most common treatment-emergent adverse events (TEAEs) noted with bifeprunox were gastrointestinal; no clear dose-related trend in the incidence of any TEAE was observed in the bifeprunox groups."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.35
" Bifeprunox appeared to be safe and well tolerated by patients in this 6-week study."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.35
" During the assessment periods Positive and Negative Syndrome Scale (PANSS) was administered to monitor the progress in psychopathology and Udvalg for Kliniske Undersogelser (UKU) side effects rating scale was applied to rate the treatment emergent adverse effects."( An open, randomized, comparative study of efficacy and safety of risperidone and haloperidol in schizophrenia.
Adhikari, SR; Gurung, CK; Koirala, NR; Nepal, MK; Sharma, VD; Tamrakar, SM,
)
0.37
" Adverse events (AEs) and clinical laboratory test results were recorded."( Treating disruptive behavior disorders with risperidone: a 1-year, open-label safety study in children and adolescents.
Haas, M; Karcher, K; Pandina, GJ, 2008
)
0.61
"Risperidone reinitiated for DBD in children with normal intelligence quotients (IQ) was safe and well tolerated over an additional year of treatment."( Treating disruptive behavior disorders with risperidone: a 1-year, open-label safety study in children and adolescents.
Haas, M; Karcher, K; Pandina, GJ, 2008
)
2.05
" Safety assessment involved adverse event reporting, physical examination, blood pressure, heart rate and ECG monitoring, and laboratory tests."( A pilot study of the safety and efficacy of amisulpride and risperidone in elderly psychotic patients.
Eich, FX; Möller, HJ; Riedel, M, 2009
)
0.6
" A total of 26 adverse events were experienced by 10 patients in the amisulpride group and five patients in the risperidone group."( A pilot study of the safety and efficacy of amisulpride and risperidone in elderly psychotic patients.
Eich, FX; Möller, HJ; Riedel, M, 2009
)
0.81
" Treatment-emergent adverse events occurred in 74% (regimen A) and 65% (regimen B) of patients; 4% of patients overall discontinued for adverse events."( Efficacy, safety and tolerability of two dosing regimens in adolescent schizophrenia: double-blind study.
Augustyns, I; Eerdekens, M; Haas, M; Kushner, S; Kusumakar, V; Pandina, G; Quiroz, J; Singer, J, 2009
)
0.35
" Primary endpoint was rate of discontinuation due to adverse events (AEs) during the 12-week study."( Switching to aripiprazole in outpatients with schizophrenia experiencing insufficient efficacy and/or safety/tolerability issues with risperidone: a randomized, multicentre, open-label study.
Kahn, JP; Kerselaers, W; Lissens, J; McQuade, RD; Modell, S; Ryckmans, V; Sanchez, R; Werner, C, 2009
)
0.56
"Numerous publications have provided evidence for clinically important metabolic adverse effects of antipsychotics, but there is no systematic evaluation as to whether weight gain and other metabolic changes are dose dependent."( Are weight gain and metabolic side effects of atypical antipsychotics dose dependent? A literature review.
De Hert, M; Simon, V; van Winkel, R, 2009
)
0.35
" Assessments included the Positive and Negative Syndrome Scale (PANSS), clinical response (> or =20% reduction in PANSS total score), adverse event (AE) monitoring, and extrapyramidal symptom (EPS) scale ratings."( A 6-week, randomized, double-blind, placebo-controlled study of the efficacy and safety of risperidone in adolescents with schizophrenia.
Armenteros, J; Copenhaver, MD; Haas, M; Kushner, SF; Quiroz, JA; Unis, AS, 2009
)
0.57
" Sixty-nine per cent of patients completed the trial; 8% discontinued due to adverse events (AEs)."( Switching stable patients with schizophrenia from depot and oral antipsychotics to long-acting injectable risperidone: reasons for switching and safety.
Curtis, V; Hawley, C; Latif, MA; Saleem, PT; Turner, M; Wilton, K, 2010
)
0.57
"The Liverpool University Neuroleptic Side Effect Rating Scale (LUNSERS) was completed by 66 patients aged between 6 and 18 years who had been taking low-dose risperidone (alone or in conjunction with other medications) for up to 13 years."( Self-reported side effects in children and adolescents taking risperidone.
Byrne, S; Cleary, M; Concannon, P; Crawford, G; Duffy, P; Hunt, G; Krabman, P; Malhi, G; Soh, N; Walter, G, 2010
)
0.8
"Young persons, overall, seemed to tolerate risperidone well, but longer exposure to the medication was associated with higher side effect levels, particularly for the psychic (pertaining to mind and emotion) and extrapyramidal subscales."( Self-reported side effects in children and adolescents taking risperidone.
Byrne, S; Cleary, M; Concannon, P; Crawford, G; Duffy, P; Hunt, G; Krabman, P; Malhi, G; Soh, N; Walter, G, 2010
)
0.86
" Safety was evaluated by recording treatment-emergent adverse events (AE)."( Safety and efficacy of long-acting injectable risperidone in daily practice: an open-label, noninterventional, prospective study in schizophrenia and related disorders.
Don, L; Kouniakis, F; Parellada, E; Schreiner, A; Siurkute, A, 2010
)
0.62
" In this work we will present a 14-year old girl adolescent with psychotic symptoms, in which case the course of treatment and discontinuance of therapy was caused by a side effect - an oculogyric crisis."( The influence of side effect of antipsychotic on the course of treatment in adolescent.
Dadić-Hero, E; Francisković, T; Graovac, M; Rebić, J; Ruzić, K, 2010
)
0.36
" Bipolar disorder treatment was started with carbamazepine, but later it was discontinued due to adverse events and extreme increase of liver transaminases."( Galactorrhea - side effect of risperidone in combination with depakine chrono in a patient with bipolar disorder.
Grahovac, T; Pavlović, E; Peitl, MV; Peitl, V, 2010
)
0.65
" Adverse effects (n = 15), inadequate efficacy (n = 14), or study nonadherence (n = 8) were the most common reasons for discontinuation."( Double-blind maintenance safety and effectiveness findings from the Treatment of Early-Onset Schizophrenia Spectrum (TEOSS) study.
Findling, RL; Frazier, JA; Hamer, RM; Hlastala, S; Johnson, JL; Kaufman, EM; Lieberman, JA; Lingler, J; Maloney, AE; McClellan, J; McNamara, NK; Noyes, N; Pierson, L; Puglia, M; Ritz, L; Sikich, L; Vitiello, B, 2010
)
0.36
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" However, despite increasing use of psychotropic medication in children and adolescents, their endocrine and metabolic side-effects (weight gain, obesity, and related metabolic abnormalities such as hyperglycaemia and dyslipidemia) are of particular concern, especially within this paediatric population that appears to be at greater risk as compared with adults for antipsychotic-induced metabolic adverse effects."( [Metabolic side effects of risperidone in early onset schizophrenia].
Bordet, R; Delion, P; Duhamel, A; Goeb, JL; Jardri, R; Kechid, G; Marco, S; Thomas, P, 2010
)
0.66
" However, some at risk states requiring action are proposed in literature: more than 5% increase in weight within a three-month period; more than half a point increase in BMI Z score; between 85th and 95th BMI percentile plus one adverse health consequence (i."( [Metabolic side effects of risperidone in early onset schizophrenia].
Bordet, R; Delion, P; Duhamel, A; Goeb, JL; Jardri, R; Kechid, G; Marco, S; Thomas, P, 2010
)
0.66
" Clinicians and caregivers need to be aware of the potential endocrine and metabolic adverse effects of atypical antipsychotics, and systematically ask for family history of metabolic disorder, life style, diet and habits."( [Metabolic side effects of risperidone in early onset schizophrenia].
Bordet, R; Delion, P; Duhamel, A; Goeb, JL; Jardri, R; Kechid, G; Marco, S; Thomas, P, 2010
)
0.66
" Patients reported similar levels of adverse events and treatment-emergent adverse events (TEAEs), except for extrapyramidal syndrome-related TEAEs, which were more common in the risperidone-treated group."( A double-blind, randomized study comparing the efficacy and safety of sertindole and risperidone in patients with treatment-resistant schizophrenia.
Buckley, PF; Daniel, DG; Kane, JM; Potkin, SG, 2011
)
0.79
"RLAI and OP show good short- and long-term safety when treating patients with schizophrenia, with uncommon discontinuation due to adverse effects."( Long-acting atypical injectable antipsychotics in the treatment of schizophrenia: safety and tolerability review.
Cañas, F; Möller, HJ, 2010
)
0.36
"To compare the efficacy and adverse effect profiles of 2 widely used atypical antipsychotics in the short-term phase of first-episode schizophrenia in patients who were treatment-naive."( Esquire trial: efficacy and adverse effects of quetiapine versus risperidone in first-episode schizophrenia.
Craig, TK; Elanjithara, T; Gafoor, R; Landau, S; McGuire, P; Power, P, 2010
)
0.6
" Psychopathologic diagnoses and adverse effects were assessed by blinded raters at 4 weekly intervals."( Esquire trial: efficacy and adverse effects of quetiapine versus risperidone in first-episode schizophrenia.
Craig, TK; Elanjithara, T; Gafoor, R; Landau, S; McGuire, P; Power, P, 2010
)
0.6
"Both quetiapine and risperidone were associated with a reduction in immediate symptoms and relatively few adverse effects other than weight gain."( Esquire trial: efficacy and adverse effects of quetiapine versus risperidone in first-episode schizophrenia.
Craig, TK; Elanjithara, T; Gafoor, R; Landau, S; McGuire, P; Power, P, 2010
)
0.92
"Quetiapine and risperidone are both effective treatments in first-episode schizophrenia at doses lower than those used in patients with long-term schizophrenia and are similar in efficacy and the incidence of adverse effects."( Esquire trial: efficacy and adverse effects of quetiapine versus risperidone in first-episode schizophrenia.
Craig, TK; Elanjithara, T; Gafoor, R; Landau, S; McGuire, P; Power, P, 2010
)
0.95
"Long-acting injectable (LAI) formulations of antipsychotics are valuable treatment alternatives for patients with psychotic disorders, and understanding their safe use is critical."( Are the long-acting intramuscular formulations of risperidone or paliperidone palmitate associated with post-injection delirium/sedation syndrome? An assessment of safety databases.
Alphs, L; Gopal, S; Karcher, K; Kent, J; Kushner, S; Nuamah, I; Singh, J; Sliwa, JK, 2011
)
0.62
"Thermodysregulation, including hypothermia, is recognized as a potential adverse effect secondary to atypical antipsychotics."( Possible long-acting risperidone-induced hypothermia precipitating phenytoin toxicity in an elderly patient.
Brandon Bookstaver, P; Miller, AD, 2011
)
0.69
" Hypothermia should be recognized as a potential adverse event with the long-acting injectable formulation of risperidone."( Possible long-acting risperidone-induced hypothermia precipitating phenytoin toxicity in an elderly patient.
Brandon Bookstaver, P; Miller, AD, 2011
)
0.9
" There was no statistical significance among treatment arms in remission rates, secondary outcome measures, and adverse events."( A pilot study of the efficacy and safety of paroxetine augmented with risperidone, valproate, buspirone, trazodone, or thyroid hormone in adult Chinese patients with treatment-resistant major depression.
Calabrese, JR; Cao, L; Chen, J; Cui, X; Fang, Y; Gao, K; Hong, W; Jiang, K; Wang, Y; Wu, Z; Xu, Y; Yi, Z; Yuan, C, 2011
)
0.6
" Thus, the aim of this study was to investigate the putative association of genetic markers with the occurrence of four frequently observed adverse events secondary to risperidone treatment: sleepiness, weight gain, extrapyramidal symptoms and sexual adverse events."( Association of common genetic variants with risperidone adverse events in a Spanish schizophrenic population.
Abad-Santos, F; Almoguera, B; Ayuso, C; Baca-García, E; Dal-Ré, R; Dorado, P; Fernandez-Piqueras, J; Llerena, A; Lopez-Castroman, J; Riveiro-Alvarez, R; Vaquero-Lorenzo, C, 2013
)
0.85
" Outcome measures included adverse events (AEs), vital signs, ECG, and laboratory tests."( Long-term safety and tolerability of lurasidone in schizophrenia: a 12-month, double-blind, active-controlled study.
Citrome, L; Cucchiaro, J; Loebel, A; Phillips, D; Sarma, K; Silva, R; Tsuchiya, S, 2012
)
0.38
" Higher doses may provide additional benefit as well as dose-related increases in some adverse reactions."( Oral paliperidone extended-release: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability.
Citrome, L, 2012
)
0.38
"This cross-sectional study aimed to compare the effects of treatment with an atypical antipsychotic drug (olanzapine or risperidone) on quality of life (QoL) and to document adverse effects in 115 patients diagnosed with schizophrenia who attended the ambulatory service of Hospital Dr."( Quality of life and adverse effects of olanzapine versus risperidone therapy in patients with schizophrenia.
Chaves, KM; de Araújo Júnior, RF; de Araújo, AA; de Paula Soares Rachetti, V; do Socorro Costa Feitosa Alves, M; Filgueira Júnior, A; Guerra, GC; Ribeiro, SB; Serrano-Blanco, A; Soares, LA, 2013
)
0.84
" It is well-tolerated and rather safe for elderly patients."( [Efficasy and safety of the use of risperidone (rispoluxe) in demented patients with psychotic and behavioural disorders].
Bocharov, AV; Kondakova, VE; Tuleninov, ES, 2012
)
0.66
"Atypical antipsychotic agents have been associated with cerebrovascular adverse events, particularly in elderly dementia patients."( Comparative risk of cerebrovascular adverse events in community-dwelling older adults using risperidone, olanzapine and quetiapine: a multiple propensity score-adjusted retrospective cohort study.
Aparasu, RR; Chatterjee, S; Chen, H; Johnson, ML, 2012
)
0.6
"16) was associated with a decrease in the risk of cerebrovascular adverse events compared with olanzapine."( Comparative risk of cerebrovascular adverse events in community-dwelling older adults using risperidone, olanzapine and quetiapine: a multiple propensity score-adjusted retrospective cohort study.
Aparasu, RR; Chatterjee, S; Chen, H; Johnson, ML, 2012
)
0.6
" Prescribers should closely monitor the patients treated with atypical agents for the incidence of cerebrovascular adverse events."( Comparative risk of cerebrovascular adverse events in community-dwelling older adults using risperidone, olanzapine and quetiapine: a multiple propensity score-adjusted retrospective cohort study.
Aparasu, RR; Chatterjee, S; Chen, H; Johnson, ML, 2012
)
0.6
"Primary metabolic markers (body mass index, blood pressure, fasting blood glucose, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and triglycerides), percentage of patients who stay on the randomly assigned atypical antipsychotic for at least 6 months, psychopathology, percentage of patients who develop metabolic syndrome, and percentage of patients who develop serious and nonserious adverse events."( Comparison of longer-term safety and effectiveness of 4 atypical antipsychotics in patients over age 40: a trial using equipoise-stratified randomization.
Arndt, S; Glorioso, DK; Golshan, S; Henry, R; Jeste, DV; Jin, H; Kraemer, HC; Mudaliar, S; Shih, PA, 2013
)
0.39
"Because of a high incidence of serious adverse events, quetiapine was discontinued midway through the trial."( Comparison of longer-term safety and effectiveness of 4 atypical antipsychotics in patients over age 40: a trial using equipoise-stratified randomization.
Arndt, S; Glorioso, DK; Golshan, S; Henry, R; Jeste, DV; Jin, H; Kraemer, HC; Mudaliar, S; Shih, PA, 2013
)
0.39
"Hyperprolactinemia is a common side effect in young males treated over the long term with risperidone."( Risk of hyperprolactinemia and sexual side effects in males 10-20 years old diagnosed with autism spectrum disorders or disruptive behavior disorder and treated with risperidone.
Boot, AM; Buitelaar, JK; Roke, Y; Tenback, D; van Harten, PN, 2012
)
0.8
" However, researchers lack a standardised method to compare different drugs for common adverse effects on the nervous system."( Assessment of adverse effects of neurotropic drugs in monkeys with the "drug effects on the nervous system" (DENS) scale.
Menniti, FS; Papa, SM; Schmidt, CJ; Shaffer, CL; Uthayathas, S, 2013
)
0.39
" Double-blind, randomized, controlled trials investigating the metabolic adverse effects (weight gain, lipid, glucose, and prolactin level abnormalities) associated with atypical antipsychotic use in children and adolescents aged ≤ 18 years were included, irrespective of whether the investigation of adverse effects was a primary or secondary endpoint."( Weight gain and other metabolic adverse effects associated with atypical antipsychotic treatment of children and adolescents: a systematic review and meta-analysis.
Aitchison, KJ; Almandil, NB; Besag, FM; Liu, Y; Murray, ML; Wong, IC, 2013
)
0.39
"5%) in the SOC group discontinued due to adverse events (physician and subject decision combined, P = ."( A long-term, phase 2, multicenter, randomized, open-label, comparative safety study of pomaglumetad methionil (LY2140023 monohydrate) versus atypical antipsychotic standard of care in patients with schizophrenia.
Adams, DH; Baygani, S; Kinon, BJ; Kollack-Walker, S; Millen, BA; Velona, I; Walling, DP, 2013
)
0.39
"These data provide further evidence that the potential antipsychotic LY2140023 monohydrate, with a glutamatergic mechanism of action, may have a unique tolerability profile characterized by a low association with some adverse events such as extrapyramidal symptoms and weight gain that may characterize currently available dopaminergic antipsychotics."( A long-term, phase 2, multicenter, randomized, open-label, comparative safety study of pomaglumetad methionil (LY2140023 monohydrate) versus atypical antipsychotic standard of care in patients with schizophrenia.
Adams, DH; Baygani, S; Kinon, BJ; Kollack-Walker, S; Millen, BA; Velona, I; Walling, DP, 2013
)
0.39
" Adverse events were assessed."( A head-to-head comparison of aripiprazole and risperidone for safety and treating autistic disorders, a randomized double blind clinical trial.
Berk, M; Ghanizadeh, A; Sahraeizadeh, A, 2014
)
0.66
" The objective of this analysis was to report the results of a population pharmacokinetic analysis and to describe the relationship between risperidone and 9-hydroxyrisperidone levels with dopamine (DA) D2-receptor occupancy, prolactin levels, and adverse events using data collected in 45 clinically stable schizophrenic patients receiving RBP-7000 in single ascending doses (risperidone) of 60, 90, and 120 mg."( A model-based approach to characterize the population pharmacokinetics and the relationship between the pharmacokinetic and safety profiles of RBP-7000, a new, long-acting, sustained-released formulation of risperidone.
Fudala, PJ; Gomeni, R; Heidbreder, C; Nasser, AF, 2013
)
0.78
" At the end of recovery phase, the above changes mostly recovered to normal, and on administering 3 mg/kg dose level once in 2 weeks on Beagle dogs showed no observed adverse effect."( A 12-week intramuscular toxicity study of risperidone-loaded microspheres in Beagle dogs.
Cen, X; Du, G; Guan, X; Li, Y; Liu, W; Tian, J; Wang, W; Ye, L; Yu, P; Zhang, J, 2014
)
0.67
" The safety was evaluated by the Udvalg Kliniske Undersogelser side effect rating scale."( Efficacy and safety of haloperidol versus atypical antipsychotic medications in the treatment of delirium.
Choi, SH; Choi, WJ; Kim, JJ; Park, JY; Park, KM; Seok, JH; Yoon, HJ, 2013
)
0.39
" Fifteen subjects experienced a few adverse events, but there were no significant differences in adverse event profiles among the four groups."( Efficacy and safety of haloperidol versus atypical antipsychotic medications in the treatment of delirium.
Choi, SH; Choi, WJ; Kim, JJ; Park, JY; Park, KM; Seok, JH; Yoon, HJ, 2013
)
0.39
"Haloperidol, risperidone, olanzapine, and quetiapine were equally efficacious and safe in the treatment of delirium."( Efficacy and safety of haloperidol versus atypical antipsychotic medications in the treatment of delirium.
Choi, SH; Choi, WJ; Kim, JJ; Park, JY; Park, KM; Seok, JH; Yoon, HJ, 2013
)
0.76
"Fifty-six (71%) out of 79 enrolled patients completed the OLE; the most common discontinuations were for insufficient response (7 [9%]) or adverse events (AE) (5 [6%])."( An open-label extension study of the safety and efficacy of risperidone in children and adolescents with autistic disorder.
Hough, D; Karcher, K; Kent, JM; Pandina, G; Singh, J, 2013
)
0.63
" The five-dimension EuroQoL (EQ-5D) was used to evaluate QoL, and side effects were assessed using the Udvalg for Kliniske Undersøgelser (UKU) Side Effect Rating Scale and the Simpson-Angus Scale."( Quality of life in patients with schizophrenia: the impact of socio-economic factors and adverse effects of atypical antipsychotics drugs.
Chaves, KM; de Araújo Dantas, D; de Araújo, AA; de Araújo, RF; de Lima Silva, V; de Medeiros, CA; de Souza, DL; do Nascimento, GG; Ribeiro, SB, 2014
)
0.4
" Extrapyramidal symptoms (EPS), weight gain, serum prolactin level, QTc interval, and self-reported adverse events were also assessed as measures of safety and tolerability."( Efficacy and safety of aripiprazole in Chinese Han schizophrenia subjects: a randomized, double-blind, active parallel-controlled, multicenter clinical trial.
Gu, N; Kane, JM; Li, H; Luo, J; Wang, C; Wang, X; Xie, S; Xu, X; Yu, W, 2014
)
0.4
"To identify genetic markers capable of predicting the pharmacokinetics, pharmacodynamics, and adverse effects of risperidone."( Effect of polymorphisms on the pharmacokinetics, pharmacodynamics, and safety of risperidone in healthy volunteers.
Abad-Santos, F; Ayuso, C; Cabaleiro, T; López-Rodríguez, R; Novalbos, J; Ochoa, D; Román, M, 2014
)
0.84
" Differences in adverse reactions can be explained by gender and polymorphisms in CYP2C19, AGTR1, and NAT2."( Effect of polymorphisms on the pharmacokinetics, pharmacodynamics, and safety of risperidone in healthy volunteers.
Abad-Santos, F; Ayuso, C; Cabaleiro, T; López-Rodríguez, R; Novalbos, J; Ochoa, D; Román, M, 2014
)
0.63
"The aim of this study was to compare the efficacy and side-effect profile of the typical antipsychotic haloperidol with that of the atypical antipsychotics risperidone, olanzapine, and aripiprazole in the management of delirium."( Haloperidol, risperidone, olanzapine and aripiprazole in the management of delirium: A comparison of efficacy, safety, and side effects.
Boettger, S; Breitbart, W; Jenewein, J, 2015
)
0.98
"The Memorial Delirium Assessment Scale (MDAS), the Karnofsky Performance Status (KPS) scale, and a side-effect rating were recorded at baseline (T1), after 2-3 days (T2), and after 4-7 days (T3)."( Haloperidol, risperidone, olanzapine and aripiprazole in the management of delirium: A comparison of efficacy, safety, and side effects.
Boettger, S; Breitbart, W; Jenewein, J, 2015
)
0.79
"Haloperidol, risperidone, aripiprazole, and olanzapine were equally effective in the management of delirium; however, they differed in terms of their side-effect profile."( Haloperidol, risperidone, olanzapine and aripiprazole in the management of delirium: A comparison of efficacy, safety, and side effects.
Boettger, S; Breitbart, W; Jenewein, J, 2015
)
1.16
"Atypical antipsychotics are considered safe for treating schizophrenia and are rarely reported to induce rhabdomyolysis."( Multidrug overdose-induced myoclonus complicated by rhabdomyolysis: possible role and mechanism of muscle toxicity of risperidone.
Hsu, YC; Yeh, YW, 2014
)
0.61
" Risk assessment for the potential use of a drug, such as aripiprazole (Abilify), should not focus on any particular adverse effect, but rather should consider risk assessment in a broader context."( Atypical antipsychotics are not all alike: side effects and risk assessment.
Howland, RH, 2014
)
0.4
" Safety measures included body mass index, serum prolactin, extrapyramidal adverse effects, and electrocardiogram."( Efficacy and Safety of Risperidone and Quetiapine in Adolescents With Bipolar II Disorder Comorbid With Conduct Disorder.
Masi, G; Milone, A; Pisano, S; Stawinoga, A; Veltri, S, 2015
)
0.73
" They were assessed at baseline and at follow-up on safety and tolerability measures (blood, urinalysis, electrocardiogram [ECG], medical history, vital signs, neurological symptoms, other adverse events), developmental measures (adaptive behavior, intelligence quotient [IQ]), and standardized rating instruments."( Tolerability, Safety, and Benefits of Risperidone in Children and Adolescents with Autism: 21-Month Follow-up After 8-Week Placebo-Controlled Trial.
Aman, M; Arnold, LE; Ghuman, J; Grados, M; Hellings, J; Hollway, JA; McCracken, J; McDougle, CJ; Nagaraja, HN; Posey, DJ; Rettiganti, M; Scahill, L; Shah, B; Swiezy, NB; Tierney, E; Vitiello, B, 2015
)
0.69
" At follow-up, risperidone was associated with more enuresis, more excessive appetite, and more weight gain, but not more adverse neurological effects."( Tolerability, Safety, and Benefits of Risperidone in Children and Adolescents with Autism: 21-Month Follow-up After 8-Week Placebo-Controlled Trial.
Aman, M; Arnold, LE; Ghuman, J; Grados, M; Hellings, J; Hollway, JA; McCracken, J; McDougle, CJ; Nagaraja, HN; Posey, DJ; Rettiganti, M; Scahill, L; Shah, B; Swiezy, NB; Tierney, E; Vitiello, B, 2015
)
1.04
" EPS were assessed at baseline and 4, 8, and 12 weeks after naturalistic SGA initiation for schizophrenia, mood, disruptive behavior, and autism spectrum disorders using the Simpson-Angus Scale (SAS), Barnes Akathisia Scale, Abnormal Involuntary Movement Scale (AIMS), and Treatment Emergent Side Effect Scale."( Neuromotor Adverse Effects in 342 Youth During 12 Weeks of Naturalistic Treatment With 5 Second-Generation Antipsychotics.
Al-Jadiri, A; Azzo, S; Carbon, M; Correll, CU; Kane, JM; Kapoor, S; Saito, E; Sarkaria, T; Sheridan, E, 2015
)
0.42
"The aim of this study was to evaluate demographic, clinical, and treatment factors that may impact on neurological adverse effects in naive and quasi-naive children and adolescents treated with antipsychotics."( Neurological Adverse Effects of Antipsychotics in Children and Adolescents.
Alda, JA; Andrés Nestares, P; Arango, C; Baeza, I; Cantarero, CM; Castro-Fornieles, J; de la Serna, E; Garcia-Amador, M; Merchán-Naranjo, J; Moreno, C; Muñoz, D; Tapia, C, 2015
)
0.42
" Total dyskinesia score (DyskinesiaS) and total Parkinson score (ParkinsonS) were calculated from the Maryland Psychiatric Research Center Involuntary Movement Scale, total UKU-Cognition score was calculated from the UKU Side Effect Rating Scale."( Neurological Adverse Effects of Antipsychotics in Children and Adolescents.
Alda, JA; Andrés Nestares, P; Arango, C; Baeza, I; Cantarero, CM; Castro-Fornieles, J; de la Serna, E; Garcia-Amador, M; Merchán-Naranjo, J; Moreno, C; Muñoz, D; Tapia, C, 2015
)
0.42
"Antipsychotics increased neurological adverse effects in a naive and quasi-naive pediatric population and should be carefully monitored."( Neurological Adverse Effects of Antipsychotics in Children and Adolescents.
Alda, JA; Andrés Nestares, P; Arango, C; Baeza, I; Cantarero, CM; Castro-Fornieles, J; de la Serna, E; Garcia-Amador, M; Merchán-Naranjo, J; Moreno, C; Muñoz, D; Tapia, C, 2015
)
0.42
" The most frequently reported treatment-emergent adverse events in RBP-7000 groups compared with placebo were somnolence, weight gain, and akathisia."( Efficacy, Safety, and Tolerability of RBP-7000 Once-Monthly Risperidone for the Treatment of Acute Schizophrenia: An 8-Week, Randomized, Double-Blind, Placebo-Controlled, Multicenter Phase 3 Study.
Fava, M; Fudala, PJ; Heidbreder, C; Henderson, DC; Kouassi, A; Nasser, AF; Twumasi-Ankrah, P, 2016
)
0.68
" Generally, the antipsychotics significantly enhanced NRG1/ErbB signaling with increased expression of NRG1 and phosphorylation of ErbB4 and ErbB2 in the brain and myocardium, except that clozapine partly blocked the cardiac NRG1/ErbB2 activation, which could be associated with its more severe cardiac adverse actions."( Effects of prolonged antipsychotic administration on neuregulin-1/ErbB signaling in rat prefrontal cortex and myocardium: implications for the therapeutic action and cardiac adverse effect.
Cai, H; Dang, R; Guo, Y; Jiang, P; Liang, D; Lv, C; Yang, R, 2016
)
0.43
" Case reports, case series, and prospective or cross-sectional studies including relevant data such as relative infant dose (RID), milk-to-plasma ratio (M/P ratio), infant drug plasma levels, and adverse events were identified."( Second-Generation Antipsychotics During the Lactation Period: A Comparative Systematic Review on Infant Safety.
Uguz, F, 2016
)
0.43
" Other than clozapine, adverse events were rarely reported in infants exposed to SGAs."( Second-Generation Antipsychotics During the Lactation Period: A Comparative Systematic Review on Infant Safety.
Uguz, F, 2016
)
0.43
"The current data suggest that SGAs seem to be relatively safe in the exposed breastfed infants for short-term usage."( Second-Generation Antipsychotics During the Lactation Period: A Comparative Systematic Review on Infant Safety.
Uguz, F, 2016
)
0.43
"Antipsychotic drugs can induce various undesirable adverse motor reactions, such as extrapyramidal side effects (EPS)."( Risperidone-induced extrapyramidal side effects: is the need for anticholinergics the consequence of high plasma concentrations?
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B; Veselinovic, T, 2016
)
1.88
" Overall, 34 patients experienced at least one treatment-emergent adverse event (TEAE)."( Phase I, open-label, randomized, parallel study to evaluate the pharmacokinetics, safety, and tolerability of one intramuscular injection of risperidone ISM at different dose strengths in patients with schizophrenia or schizoaffective disorder (PRISMA-1).
Anta, L; Ayani, I; Gutierro, I; Ivanov, M; Llaudó, J; Martínez, J; Morozova, M; Schronen, J, 2016
)
0.64
" Outcomes included the positive and negative syndrome scale (PANSS) scores, the curative rate of senile dementia, and prevalence of adverse effects (somnolence, headache, loss of weight, extrapyramidal system response, irritation and insomnia)."( Tiapride is more effective and causes fewer adverse effects than risperidone in the treatment of senile dementia.
Huang, YJ; Lei, LF; Li, LH; Yuan, Y, 2016
)
0.67
" Prevalence of adverse reactions was significantly lower in the latter group (9."( Tiapride is more effective and causes fewer adverse effects than risperidone in the treatment of senile dementia.
Huang, YJ; Lei, LF; Li, LH; Yuan, Y, 2016
)
0.67
"Tiapride is more effective in improving clinical symptoms of senile dementia and causes fewer adverse effects."( Tiapride is more effective and causes fewer adverse effects than risperidone in the treatment of senile dementia.
Huang, YJ; Lei, LF; Li, LH; Yuan, Y, 2016
)
0.67
" Rare reports concern severe adverse drug reaction in multiple organic systems with their combined use."( Neurotoxicity and nephrotoxicity caused by combined use of lithium and risperidone: a case report and literature review.
Hsu, CW; Lee, CY; Lee, Y; Lin, PY, 2016
)
0.67
" These adverse effects resolved soon after discontinuing these medications and adequate hydration."( Neurotoxicity and nephrotoxicity caused by combined use of lithium and risperidone: a case report and literature review.
Hsu, CW; Lee, CY; Lee, Y; Lin, PY, 2016
)
0.67
" No serious adverse event was reported."( A Randomized, Double-Blind Placebo-Controlled Trial on Effectiveness and Safety of Celecoxib Adjunctive Therapy in Adolescents with Acute Bipolar Mania.
Akhondzadeh, S; Gholamian, F; Karkhaneh-Yousefi, MA; Khezri, R; Mohammadi, MR; Mohammadinejad, P; Mousavi, SY; Zeinoddini, A, 2017
)
0.46
" The aims of this study were to investigate the effectiveness and adverse effects of LAIR in children and adolescents with conduct disorder, bipolar disorder, and schizophrenia."( Effectiveness, Adverse Effects and Drug Compliance of Long-Acting Injectable Risperidone in Children and Adolescents.
Ceylan, MF; Cop, E; Erdogan, B; Tural Hesapcioglu, S, 2017
)
0.68
" The effectiveness and adverse effects of the treatment were examined."( Effectiveness, Adverse Effects and Drug Compliance of Long-Acting Injectable Risperidone in Children and Adolescents.
Ceylan, MF; Cop, E; Erdogan, B; Tural Hesapcioglu, S, 2017
)
0.68
" Weight-gain, dystonia, and galactorrhea were the adverse effects that were responsible for LAIR treatment cessation."( Effectiveness, Adverse Effects and Drug Compliance of Long-Acting Injectable Risperidone in Children and Adolescents.
Ceylan, MF; Cop, E; Erdogan, B; Tural Hesapcioglu, S, 2017
)
0.68
" Antipsychotics have important adverse effects, and systematic monitoring of drug safety is infrequently performed."( Feasibility and Relevance of Antipsychotic Safety Monitoring in Children With Tourette Syndrome: A Prospective Longitudinal Study.
Hammer, T; Ho, J; Patten, S; Pringsheim, T; Sarna, JR, 2017
)
0.46
" Children were monitored for extrapyramidal, metabolic, and hormonal adverse effects using the Canadian Alliance for Monitoring Effectiveness and Safety of Antipsychotic Medications guidelines."( Feasibility and Relevance of Antipsychotic Safety Monitoring in Children With Tourette Syndrome: A Prospective Longitudinal Study.
Hammer, T; Ho, J; Patten, S; Pringsheim, T; Sarna, JR, 2017
)
0.46
"This study suggests that oral risperidone may be a safe option for acute agitation in patients presenting to the ED with alcohol intoxication."( Safety of Risperidone for Acute Agitation and Alcohol Intoxication in Emergency Department Patients.
Huynh, HE; Lee, KC; Pepa, PA; Wilson, MP, 2017
)
1.15
" Overall, 63 (94%) patients experienced at least one treatment-emergent adverse event (TEAE)."( A phase II study to evaluate the pharmacokinetics, safety, and tolerability of Risperidone ISM multiple intramuscular injections once every 4 weeks in patients with schizophrenia.
Anta, L; Ayani, I; Gutierro, I; Litman, RE; Llaudó, J; Martínez, J, 2018
)
0.71
" The use of antipsychotics is associated with a number of adverse effects for which routine monitoring is recommended."( Antipsychotic Prescribing and Safety Monitoring Practices in Children and Youth: A Population-Based Study in Alberta, Canada.
Cepoiu-Martin, M; Chen, W; Cooke, L; Duncan, D; Pringsheim, T; Stang, A; Symonds, C, 2018
)
0.48
" The association between a drug and a rare but potentially serious side effect in an individual patient can be difficult to determine with precision, and the decision to press ahead and try to work around the reaction, versus stopping the likely offender and finding a substitute, is a matter for seasoned clinical judgment."( Commentary on 2 Cases of Rare but Serious Side Effects of Commonly Used Medications: Dilemmas in Clinical Decision-making.
Kahn, DA, 2018
)
0.48
"There are few and conflicting data on the role of cytochrome P450 2D6 (CYP2D6) polymorphisms in relation to risperidone adverse events (AEs) in children."( CYP2D6 genotype and adverse events to risperidone in children and adolescents.
Aka, IT; Carroll, RJ; Maxwell-Horn, AC; Neely, KM; Oshikoya, KA; Roden, DM; Van Driest, SL, 2019
)
1
"The aim of the study is to find a relationship between the individual intervariability of CYP2D6 and the incidence of hyperprolactinemia as side effect of atypical antipsychotics."( Impact of the CYP2D6 phenotype on hyperprolactinemia development as an adverse event of treatment with atypical antipsychotic agents in pediatric patients.
Andreescu, N; Grădinaru, R; Nussbaum, L; Puiu, M; Suciu, L, 2019
)
0.51
"For the slow and intermediate metabolizers, atypical antipsychotics determined a significant increase of prolactinemia with high risk of adverse events."( Impact of the CYP2D6 phenotype on hyperprolactinemia development as an adverse event of treatment with atypical antipsychotic agents in pediatric patients.
Andreescu, N; Grădinaru, R; Nussbaum, L; Puiu, M; Suciu, L, 2019
)
0.51
"Despite frequent use of antipsychotic medications to target severe behavioral problems among children with intellectual disabilities (ID), there is little information as to the extent to which adverse effect monitoring is in place for this population."( Adherence to Antipsychotic Adverse Effect Monitoring Among a Referred Sample of Children with Intellectual Disabilities.
Javaheri, KR; McLennan, JD, 2019
)
0.51
" Charts of all those on antipsychotic medications were reviewed for a 12-week period to determine the extent to which adverse effect monitoring was documented using the parameters stipulated by the Canadian Alliance for Monitoring Effectiveness and Safety of Antipsychotics in Children (CAMESA), including laboratory, anthropometric, and neurological measures."( Adherence to Antipsychotic Adverse Effect Monitoring Among a Referred Sample of Children with Intellectual Disabilities.
Javaheri, KR; McLennan, JD, 2019
)
0.51
"There were significant gaps in adverse effect monitoring in this cohort."( Adherence to Antipsychotic Adverse Effect Monitoring Among a Referred Sample of Children with Intellectual Disabilities.
Javaheri, KR; McLennan, JD, 2019
)
0.51
" The current report presents adverse events in an infant exposed to a combination of risperidone and haloperidol through breast milk."( Adverse Events in a Breastfed Infant Exposed to Risperidone and Haloperidol.
Uguz, F, 2019
)
0.99
"With the second-generation antipsychotics (SGAs) widely applied to treat patients with schizophrenia, adverse effects, especially the metabolic syndrome (MetS), were paid more attention following by the efficacy of SGAs."( Efficacy and safety of electroacupuncture on metabolic syndrome due to olanzapine and risperidone: Study protocol for a randomized controlled pilot trial.
Chen, P; Jia, H; Ning, Y; Yin, D; Zhu, H, 2019
)
0.74
" The effect size, remission/response rate, and risk for discontinuation due to adverse events (AEs), weight gain (WG), nervous systems and gastrointestinal AEs were assessed and compared between two regions with Cohen's d or number needed to treat/harm."( Do Asian and North American patients with bipolar disorder have similar efficacy, tolerability, and safety profile during clinical trials with atypical antipsychotics?
Bai, Y; Chen, G; Gao, K; Yang, H, 2020
)
0.56
"Risperidone (RIS), a commonly used drug during a lifetime for the treatment of schizophrenia, causes some adverse effects in the male reproductive system; however, there is no comprehensive reproductive toxicity study of RIS."( Risperidone induced reproductive toxicity in male rats targeting leydig cells and hypothalamic-pituitary-gonadal axis by inducing oxidative stress.
Atlı-Eklioğlu, Ö; Aydoğan-Kılıç, G; Baysal, M; Görmüş, G; Ilgın, S; Karaduman, AB; Karagöz, O; Kılıç, V, 2021
)
3.51
" We Propose a text mining approach to detect adverse events and medication episodes from the clinical text to enhance our understanding of adverse effects related to Clozapine, the most effective antipsychotic drug for the management of treatment-resistant schizophrenia, but underutilised due to concerns over its side effects."( The side effect profile of Clozapine in real world data of three large mental health hospitals.
Broadbent, M; Dobson, RJB; Dzahini, O; Govind, R; Ibrahim, ZM; Iqbal, E; Kim, CH; MacCabe, JH; Romero, A; Smith, T; Stewart, R; Werbeloff, N, 2020
)
0.56
" We explored the prevalence of 33 adverse effects by age, gender, ethnicity, smoking status and admission type three months before and after the patients started Clozapine treatment."( The side effect profile of Clozapine in real world data of three large mental health hospitals.
Broadbent, M; Dobson, RJB; Dzahini, O; Govind, R; Ibrahim, ZM; Iqbal, E; Kim, CH; MacCabe, JH; Romero, A; Smith, T; Stewart, R; Werbeloff, N, 2020
)
0.56
"Sedation, fatigue, agitation, dizziness, hypersalivation, weight gain, tachycardia, headache, constipation and confusion were amongst the highest recorded Clozapine adverse effect in the three months following the start of treatment."( The side effect profile of Clozapine in real world data of three large mental health hospitals.
Broadbent, M; Dobson, RJB; Dzahini, O; Govind, R; Ibrahim, ZM; Iqbal, E; Kim, CH; MacCabe, JH; Romero, A; Smith, T; Stewart, R; Werbeloff, N, 2020
)
0.56
"To investigate the relationship between -759C/T, functional polymorphism of the HTR2C gene and metabolic adverse effects in Thai psychiatric patients treated with risperidone monotherapy."( Effect of 5-HT2C receptor gene polymorphism (HTR2C-759C/T) on metabolic adverse effects in Thai psychiatric patients treated with risperidone.
Hongkaew, Y; Jiratjintana, N; Na Nakorn, C; Puangpetch, A; Sukasem, C; Unaharassamee, W; Vanwong, N, 2021
)
1.02
" These findings highlighted that APP with RIS and CLZ might increase the plasma concentrations of RIS and 9-hydroxy-RIS beyond the safety ranges and cause toxic side effects."( Clozapine affects the pharmacokinetics of risperidone and inhibits its metabolism and P-glycoprotein-mediated transport in vivo and in vitro: A safety attention to antipsychotic polypharmacy with clozapine and risperidone.
Liu, W; Liu, X; Sun, H; Sun, Y; Wang, W; Xu, L; Zhang, Y, 2021
)
0.89
" SGAs used for approved indications are associated with significant metabolic adverse effects, including weight gain."( Metabolic adverse effects of off-label use of second-generation antipsychotics in the adult population: a systematic review and meta-analysis.
Agarwal, SM; Asgariroozbehani, R; Bowden, S; Hahn, MK; McIntyre, WB; Remington, G; Siskind, D; Smith, E; Stogios, N; Tran, V, 2022
)
0.72
"In this systematic literature review (SLR), we qualitatively synthesized evidence on the comparative efficacy (based on neuropsychiatric inventory), tolerability (weight gain), and safety (cerebrovascular adverse events [CVAE], cardiovascular events, mortality, somnolence, extrapyramidal symptoms [EPS]) of AAPs used to treat DRP."( Comparative Efficacy, Safety, Tolerability, and Effectiveness of Antipsychotics in The Treatment of Dementia-Related Psychosis (DRP): A Systematic Literature Review.
Abler, V; Rajagopalan, K; Rashid, N; Yunusa, I, 2021
)
0.62
" Safety evaluation included treatment-emergent adverse events (TEAEs), injection site reactions (ISR), laboratory tests and several safety scales."( Long-term efficacy and safety of once-monthly Risperidone ISM® in the treatment of schizophrenia: Results from a 12-month open-label extension study.
Anta, L; Correll, CU; Filts, Y; Litman, RE; Martínez, J; Naber, D, 2022
)
0.98
" The study used the Delirium Rating Scale (DRS) Revised-98 to measure effectiveness and the CTCAE (Common Terminology Criteria for Adverse Events) version 4 to assess safety."( Safety and Effectiveness of Perospirone in Comparison to Risperidone for Treatment of Delirium in Patients with Advanced Cancer: A Multicenter Prospective Observational Study in Real-World Psycho-Oncology Settings.
Inoue, S; Maeda, I; Ogawa, A; Terada, S; Yamada, N; Yoshiuchi, K, 2022
)
0.97
" Secondary outcomes included psychopathology, remission, all-cause-discontinuation, inefficacy-related discontinuation, and adverse events."( Efficacy and safety/tolerability of antipsychotics in the treatment of adult patients with major depressive disorder: a systematic review and meta-analysis.
Correll, CU; Hagi, K; Kane, JM; Kishimoto, T; Kurokawa, S, 2023
)
0.91
" Some reports indicate that risperidone is toxic to various systems of the body, including the immune system."( Risperidone Toxicity on Human Blood Lymphocytes in Nano molar Concentrations.
Imani, F; Pourahmad, J; Ramezani, M; Salimi, A; Seydi, E; Shirani, K; Yousefsani, BS, 2022
)
2.46
"Retrospective studies using spontaneous reporting system databases have provided a great understanding of adverse drug reactions (ADRs) in the real world, complementing the data obtained from randomized controlled trials."( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019.
Byeon, SJ; Chung, SJ; Oh, S, 2022
)
0.72
"Data were collected from the Korea Adverse Event Reporting System database between 2010 and 2019."( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019.
Byeon, SJ; Chung, SJ; Oh, S, 2022
)
0.72
"In total, 5067 adverse events associated with antipsychotic drugs were reported."( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019.
Byeon, SJ; Chung, SJ; Oh, S, 2022
)
0.72
" The most common adverse events with Lu AF35700 were increased weight and headache."( Efficacy and safety of Lu AF35700 in treatment-resistant schizophrenia: A randomized, active-controlled trial with open-label extension.
Forray, C; Hertel, P; Howes, OD; Kane, JM; Kinon, BJ; Lemming, OM; Mittoux, A; Such, P, 2022
)
0.72
"Current methods are not designed to relate the incidence of individual adverse events reported in clinical trials to the plurality of adverse events accumulated in spontaneous reporting databases during real-world use."( Depicting Risperidone Safety Profiles in Clinical Trials Across Different Diagnoses Using a Dopamine D
Hopkins, SC; Koblan, KS; Ogirala, A; Worden, M; Zeni, C, 2022
)
1.12
"Patient-level adverse event data (n = 4400) from controlled clinical trials of the antipsychotic risperidone in schizophrenia, bipolar disorder, Alzheimer's disease psychosis, and autism were obtained through the Yale University Open Data Access (YODA) project."( Depicting Risperidone Safety Profiles in Clinical Trials Across Different Diagnoses Using a Dopamine D
Hopkins, SC; Koblan, KS; Ogirala, A; Worden, M; Zeni, C, 2022
)
1.34
"In pooled data from seven trials of adult schizophrenia, class-specific adverse events were identified in 49% of patients treated with risperidone; in 49% of risperidone-treated patients in two trials in adolescent schizophrenia; in 65% of risperidone-treated patients in four trials in adult bipolar disorder; in 50% of risperidone-treated patients in two trials in adolescent schizophrenia; in 36% of risperidone-treated patients in one trial in Alzheimer's disease; and in 94% of risperidone-treated patients in one trial in autism."( Depicting Risperidone Safety Profiles in Clinical Trials Across Different Diagnoses Using a Dopamine D
Hopkins, SC; Koblan, KS; Ogirala, A; Worden, M; Zeni, C, 2022
)
1.33
"The cumulative curves of class-specific adverse events in risperidone clinical trials of schizophrenia were similar to those first reported for other atypical antipsychotic drugs."( Depicting Risperidone Safety Profiles in Clinical Trials Across Different Diagnoses Using a Dopamine D
Hopkins, SC; Koblan, KS; Ogirala, A; Worden, M; Zeni, C, 2022
)
1.37
" Although there are some reports in literature, the side effect profile in this population remains poorly defined and there is a need to raise awareness among clinicians across specialties."( Recognising side effects of antipsychotics in children with intellectual disabilities.
Anand, G; Lee, J; Shepperd, R; Smith, M, 2023
)
0.91
"This study indicated that fingolimod is a safe and effective adjuvant agent for schizophrenia treatment."( Efficacy and safety of adjunctive therapy with fingolimod in patients with schizophrenia: A randomized, double-blind, placebo-controlled clinical trial.
Akhondzadeh, S; Amanollahi, M; Ardakani, MK; Basti, FA; Jameie, M; Karbalaee, M; Mokhtari, S; Moradi, K; Parsaei, M; TaghaviZanjani, F, 2023
)
0.91
"To compare the risk for in-hospital adverse events associated with oral haloperidol, olanzapine, quetiapine, and risperidone in older patients after major surgery."( Comparative Safety Analysis of Oral Antipsychotics for In-Hospital Adverse Clinical Events in Older Adults After Major Surgery : A Nationwide Cohort Study.
Bateman, BT; Ely, EW; Inouye, SK; Jones, RN; Kim, DH; Lee, SB; Levin, R; Marcantonio, ER; Metzger, E; Pandharipande, PP; Park, CM; Pisani, MA, 2023
)
1.12
"These results suggest that atypical antipsychotics and haloperidol have similar rates of in-hospital adverse clinical events in older patients with postoperative delirium who receive an oral low-to-moderate dose antipsychotic drug."( Comparative Safety Analysis of Oral Antipsychotics for In-Hospital Adverse Clinical Events in Older Adults After Major Surgery : A Nationwide Cohort Study.
Bateman, BT; Ely, EW; Inouye, SK; Jones, RN; Kim, DH; Lee, SB; Levin, R; Marcantonio, ER; Metzger, E; Pandharipande, PP; Park, CM; Pisani, MA, 2023
)
0.91
" Most frequently reported treatment-related adverse events (ie, ≥5% of patients in either TV-46000 group) that occurred more often in patients receiving TV-46000 (once monthly or once every 2 months) versus placebo were injection site nodules (7% for TV-46000 once monthly, 7% for TV-46000 once every 2 months, 3% for placebo), weight increased (4%, 6%, 2%, respectively), and extrapyramidal disorder (5%, 3%, 0% respectively)."( Efficacy and safety of TV-46000, a long-acting, subcutaneous, injectable formulation of risperidone, for schizophrenia: a randomised clinical trial in the USA and Bulgaria.
Correll, CU; Davis, GL; Eshet, R; Franzenburg, KR; Harary, E; Kane, JM; Leucht, S; Merenlender-Wagner, A; Sharon, N; Suett, M; Tohami, O; Weiser, M, 2023
)
1.13

Pharmacokinetics

There are a few reports in the literature regarding the pharmacokinetic characteristics of risperidone, but insufficient data on its pharmacokinetics in a Chinese population. An open-label study evaluated the effect of steady-state venlafaxine on the single-dose Pharmacokinetic profile of ris peridone.

ExcerptReferenceRelevance
" Following are the mean pharmacokinetics of risperidone and risperidone + 9-OH-risperidone: area under the plasma concentration curve (AUC) from 0 to 96 hours; 278."( Pharmacokinetics of risperidone in chronic schizophrenic patients.
Borison, RL; Diamond, B; Meibach, RC; Pathiraja, A, 1994
)
0.87
" Risperidone can be characterized as a potent D2 antagonist with predominant 5HT2 antagonistic activity and optimal pharmacokinetic properties."( Survey on the pharmacodynamics of the new antipsychotic risperidone.
Awouters, FH; Dugovic, C; Leysen, JE; Meert, TF; Megens, AA; Niemegeers, CJ; Schotte, A, 1994
)
1.45
" Most traditional antipsychotic drugs have similar pharmacokinetic profiles that differ from the newer agents in several key respects."( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs.
DeVane, CL, 1995
)
0.29
" Risperidone half-life was about 3 hours in extensive metabolizers and 22 hours in poor metabolizers."( Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects.
De Coster, R; Heykants, J; Huang, ML; Jansen, AA; Jonkman, JH; Van Peer, A; Visscher, HW; Woestenborghs, R; Zylicz, Z, 1993
)
1.45
" The current clinical pharmacokinetic database for these atypical antipsychotics suggests that much can be learned with additional study that would be of value in individualizing their dosage regimens."( Pharmacokinetics of clozapine and risperidone: a review of recent literature.
Byerly, MJ; DeVane, CL, 1996
)
0.57
" Pharmacokinetic interactions with other drugs have been described but, in some cases, their mechanism is unknown."( Pharmacokinetic interactions involving clozapine.
Taylor, D, 1997
)
0.3
"Published trials and case reports relevant to the human metabolism of clozapine and to suspected pharmacokinetic interactions were reviewed."( Pharmacokinetic interactions involving clozapine.
Taylor, D, 1997
)
0.3
"An open-label study evaluated the effect of steady-state venlafaxine on the single-dose pharmacokinetic profile of risperidone, a CYP2D6 substrate; its active metabolite, 9-hydroxyrisperidone; and the total active moiety (risperidone plus 9-hydroxyrisperidone)."( Effect of venlafaxine on the pharmacokinetics of risperidone.
Albano, D; Amchin, J; Klockowski, PM; Taylor, KP; Zarycranski, W, 1999
)
0.77
"Following an oral dose of risperidone (RSP), concentrations of its major metabolite 9-hydroxyrisperidone (9-OHRSP) were high in plasma and tissues but disproportionately lower in the brain compared to RSP, indicating that 9-OHRSP may have different pharmacokinetic properties."( Brain, plasma and tissue pharmacokinetics of risperidone and 9-hydroxyrisperidone after separate oral administration to rats.
Aravagiri, M; Marder, SR, 2002
)
0.87
" The terminal elimination half-life (t(1/2) ) of RSP after the RSP dose was longest in the liver (17."( Brain, plasma and tissue pharmacokinetics of risperidone and 9-hydroxyrisperidone after separate oral administration to rats.
Aravagiri, M; Marder, SR, 2002
)
0.57
" A full pharmacokinetic time profile of lithium was obtained."( Bayesian pharmacokinetics of lithium after an acute self-intoxication and subsequent haemodialysis: a case report.
Beijnen, JH; Kerbusch, T; Mathôt, RA; Meesters, EW; Otten, HM; Schellens, JH; van Kan, HJ, 2002
)
0.31
"To explore the steady-state pharmacokinetic profile after coadministration of galantamine and risperidone, an open-label, randomized, single-center, two-way crossover drug-drug interaction study was conducted in 16 healthy elderly subjects, ages 60 years and older."( Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs are administered alone and together.
Huang, F; Janssens, L; Lasseter, KC; Lau, H; Verhaeghe, T; Zhao, Q, 2002
)
0.78
" The treatment ratios of Cmax and associated 90% CIs for risperidone active moiety (ratio = 114."( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil.
Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003
)
0.8
" Blood samples for pharmacokinetic analysis of the active moiety (risperidone + 9-hydroxy-risperidone), risperidone, and its active metabolite 9-hydroxy-risperidone were obtained during a 96-hour period after dosing."( Pharmacokinetic comparison of fast-disintegrating and conventional tablet formulations of risperidone in healthy volunteers.
Ko, G; Lasseter, KC; Lechat, P; Mannaert, E; Remmerie, BM; van Schaick, EA, 2003
)
0.78
"The bioequivalence assessment was based on pharmacokinetic and statistical analysis of data from 37 subjects who completed both treatment periods."( Pharmacokinetic comparison of fast-disintegrating and conventional tablet formulations of risperidone in healthy volunteers.
Ko, G; Lasseter, KC; Lechat, P; Mannaert, E; Remmerie, BM; van Schaick, EA, 2003
)
0.54
" Mean half-life of dopamine D2 receptor occupancy of risperidone was 80."( Estimation of the time-course of dopamine D2 receptor occupancy in living human brain from plasma pharmacokinetics of antipsychotics.
Ichimiya, T; Ikoma, Y; Inoue, M; Maeda, J; Okubo, Y; Sudo, Y; Suhara, T; Takano, A; Yasuno, F, 2004
)
0.57
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" Although overall bioequivalence of the two formulations was established, the differences in pharmacokinetic profiles between the two formulations indicate potential benefits for long-acting risperidone."( Pharmacokinetics and tolerability of long-acting risperidone in schizophrenia.
Eerdekens, M; Mannaert, E; Remmerie, B; Van Hove, I, 2004
)
0.77
"On analysis, steady-state pharmacokinetic parameters (peak plasma concentrations [C(max)], time to C(max,) area under the concentration-time curve) of valproate were of the same order of magnitude on day 14 (monotherapy) and day 28 (valproate plus risperidone or placebo), with no period effect."( Risperidone does not affect steady-state pharmacokinetics of divalproex sodium in patients with bipolar disorder.
Alexander, J; Lacroix, D; Ravindran, A; Silverstone, P; van Schaick, E; Vermeulen, A, 2004
)
1.95
" Pharmacokinetic parameters (C(max), t(max) and AUC) were assessed from plasma drug concentrations measured in blood collected before, during and after administration (for 12 h after risperidone on days 0 and 7, and for 24 h after donepezil HCl on day 7)."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.77
" Pharmacokinetic parameters for risperidone and 9-OH risperidone were not altered in patients with schizophrenia after 7 days of donepezil HCl administration (AUC(0-12 h) standardized by dose: risperidone = 59."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.86
" Combining the attributes of the atypical antipsychotic class with the pharmacokinetic profile and compliance advantages of a long-acting formulation could potentially be an important advance in the management of patients requiring continuous anti- psychotic therapy."( Pharmacokinetic profile and clinical efficacy of long-acting risperidone: potential benefits of combining an atypical antipsychotic and a new delivery system.
Ereshefsky, L; Mannaert, E, 2005
)
0.57
" The AUC from 0 to 24 hours of 9-hydroxyrisperidone, but not other pharmacokinetic parameters, was significantly increased during verapamil treatment."( Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition.
Kaneo, S; Nakagami, T; Saito, M; Tateishi, T; Yasui-Furukori, N, 2005
)
0.83
"Population pharmacokinetic modeling was used to assess the consistency of risperidone exposure in Alzheimer's disease patients with agitation."( Population pharmacokinetics as a method to detect variable risperidone exposure in patients suffering from dementia with behavioral disturbances.
Bies, RR; Huber, KA; Kirshner, MA; Mulsant, BH; Pollock, BG; Rosen, J; Wilson, NL, 2005
)
0.8
" A pharmacokinetic analysis was performed using both traditional compartmental modeling and a population pharmacokinetic approach."( Population pharmacokinetic analysis of drug-drug interactions among risperidone, bupropion, and sertraline in CF1 mice.
DeVane, CL; Donovan, JL; Gibson, BB; Markowitz, JS; Wang, JS; Zhu, HJ, 2006
)
0.57
" It increased the plasma AUC and elimination half-life (T1/2e) of desmethyl-SERT 12."( Population pharmacokinetic analysis of drug-drug interactions among risperidone, bupropion, and sertraline in CF1 mice.
DeVane, CL; Donovan, JL; Gibson, BB; Markowitz, JS; Wang, JS; Zhu, HJ, 2006
)
0.57
"These results suggest that pharmacokinetic interactions exist among these three psychoactive drugs involving inhibition of drug metabolizing enzymes and/or P-gp and other drug transporters present in the BBB."( Population pharmacokinetic analysis of drug-drug interactions among risperidone, bupropion, and sertraline in CF1 mice.
DeVane, CL; Donovan, JL; Gibson, BB; Markowitz, JS; Wang, JS; Zhu, HJ, 2006
)
0.57
"The single dose pharmacokinetic profiles of long-acting injectable (LAI) risperidone and oral risperidone were extrapolated to steady-state."( Pharmacokinetic profile of long-acting injectable risperidone at steady-state: comparison with oral administration.
Bouhours, P; Levron, JC; Mannaert, E; Remmerie, B; Vermeulen, A,
)
0.62
"A population model was developed with the aim to simultaneously describe risperidone and 9-hydroxyrisperidone pharmacokinetics; to obtain estimates for pharmacokinetic parameters and associated inter- and intra-individual variability of risperidone and 9-hydroxyrisperidone; and to evaluate the influence of patient demographic characteristics and other factors on risperidone, 9-hydroxyrisperidone, and active moiety pharmacokinetics."( Population pharmacokinetics of risperidone and 9-hydroxyrisperidone in patients with acute episodes associated with bipolar I disorder.
Ludwig, EA; Piotrovsky, V; Vermeulen, A, 2007
)
0.86
" This article reports results from 3 studies examining the potential for cytochrome P450-dependent pharmacokinetic interactions between STS and 3 psychotropic medications that might be coadministered."( Selegiline transdermal system: an examination of the potential for CYP450-dependent pharmacokinetic interactions with 3 psychotropic medications.
Azzaro, AJ; Campbell, BJ; Kemper, E; VanDenBerg, C; Ziemniak, J, 2007
)
0.34
"To develop a parent-metabolite pharmacokinetic model for risperidone (RIP) and its major active metabolite (9-hydroxyrisperidone) and investigate their pharmacokinetics characteristics in healthy male volunteers, twenty-two healthy volunteers were orally given a single dose of 2 mg RIP."( [Development and identifiability analysis of parent-metabolite pharmacokinetic model for risperidone and its main active metabolite 9-hydroxyrisperidone].
Ding, JJ; Jiao, Z; Shi, XJ; Yu, YQ, 2007
)
0.81
"The goals of this study were to estimate the pharmacokinetic parameters of risperidone and its enantiomers in a pediatric population and explore relationships between saliva and plasma concentrations."( Plasma pharmacokinetic characteristics of risperidone and their relationship to saliva concentrations in children with psychiatric or neurodevelopmental disorders.
Aman, MG; Lindsay, RL; Malone, K; Mannaert, E; Masty, J; Ramadan, Y; Remmerie, B; Vinks, AA, 2007
)
0.83
" Standard pharmacokinetic parameters were calculated."( Plasma pharmacokinetic characteristics of risperidone and their relationship to saliva concentrations in children with psychiatric or neurodevelopmental disorders.
Aman, MG; Lindsay, RL; Malone, K; Mannaert, E; Masty, J; Ramadan, Y; Remmerie, B; Vinks, AA, 2007
)
0.6
"In this preliminary pharmacokinetic study of parameters for risperidone and the enantiomers of 9-OH-risperidone in a pediatric population, mean C(max) and t(1/2) of risperidone were generally similar to those previously described in adults."( Plasma pharmacokinetic characteristics of risperidone and their relationship to saliva concentrations in children with psychiatric or neurodevelopmental disorders.
Aman, MG; Lindsay, RL; Malone, K; Mannaert, E; Masty, J; Ramadan, Y; Remmerie, B; Vinks, AA, 2007
)
0.85
"3 mg/kg haloperidol, however, exhibited similar pharmacodynamic effects in both genotypes."( Pharmacodynamic consequences of P-glycoprotein-dependent pharmacokinetics of risperidone and haloperidol in mice.
Henken, S; Hiemke, C; Kirschbaum, KM; Schmitt, U, 2008
)
0.57
" The linear range corresponds well with the serum concentrations of the analytes obtained in clinical pharmacokinetic studies."( Determination of risperidone in human plasma by HPLC-MS/MS and its application to a pharmacokinetic study in Chinese volunteers.
Chen, JC; Huang, MZ; Liu, J; Shentu, JZ; Zhou, HL, 2008
)
0.69
"At equivalent daily doses and typical patterns of compliance, fortnightly intramuscular depot administrations of risperidone provide better pharmacokinetic coverage than once-daily oral dosing."( Estimation of the impact of noncompliance on pharmacokinetics: an analysis of the influence of dosing regimens.
Hughes, DA, 2008
)
0.56
"At therapeutic concentrations and with typical patterns of noncompliance, intramuscular injections of risperidone resulted in a 41% (SD 12%) greater pharmacokinetic coverage than the oral dose, 76% (SD 10%) vs."( Estimation of the impact of noncompliance on pharmacokinetics: an analysis of the influence of dosing regimens.
Hughes, DA, 2008
)
0.56
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" These long-term effects would not be captured by a standard 5-day pharmacokinetic TDM developmental testing model for antipsychotics, and a new model for characterizing variation in C/D by time course is therefore proposed."( Long-term therapeutic drug monitoring of risperidone and olanzapine identifies altered steady-state pharmacokinetics: a clinical, two-group, naturalistic study.
Darby, JK; Herbert, J; Pasta, DJ; Wilson, MG, 2008
)
0.61
"To characterize pharmacokinetic (PK) variability of risperidone and 9-OH risperidone using sparse sampling and to evaluate the effect of covariates on PK parameters."( Population pharmacokinetic analysis for risperidone using highly sparse sampling measurements from the CATIE study.
Aravagiri, M; Bies, RR; Coley, K; Feng, Y; Kirshner, M; Marder, S; Miller, D; Pollock, BG; Schneider, L, 2008
)
0.86
" The limited available paliperidone pharmacokinetic information suggests that there are four minor metabolic pathways."( The pharmacokinetics of paliperidone versus risperidone.
de Leon, J; Sandson, NB; Wynn, G,
)
0.39
" The pharmacokinetic profile of risperidone is well documented in adults."( Population pharmacokinetics of oral risperidone in children, adolescents and adults with psychiatric disorders.
Fabre, MA; Fuseau, E; Mannaert, E; Thyssen, A; Vermeulen, A, 2010
)
0.92
"The pharmacokinetics of oral risperidone in children and adolescents were investigated through non-compartmental analysis (paediatric phase I study; n = 24) and population pharmacokinetic analysis using nonlinear mixed-effects modelling software (NONMEM) on a pooled database including both paediatric (n = 304) and adult (n = 476) data."( Population pharmacokinetics of oral risperidone in children, adolescents and adults with psychiatric disorders.
Fabre, MA; Fuseau, E; Mannaert, E; Thyssen, A; Vermeulen, A, 2010
)
0.93
"Non-compartmental pharmacokinetic analysis showed that, after correcting doses for bodyweight, plasma exposure was comparable between children and adolescents and in line with historical adult data."( Population pharmacokinetics of oral risperidone in children, adolescents and adults with psychiatric disorders.
Fabre, MA; Fuseau, E; Mannaert, E; Thyssen, A; Vermeulen, A, 2010
)
0.64
" A population pharmacokinetic modeling approach was used to estimate the interindividual variability of the pharmacokinetic parameters in 50 hospitalized patients with acute episode of schizophrenia."( A population pharmacokinetic evaluation of the influence of CYP2D6 genotype on risperidone metabolism in patients with acute episode of schizophrenia.
Dolzan, V; Grabnar, I; Kastelic, M; Koprivsek, J; Kores-Plesnicar, B; Locatelli, I; Mrhar, A, 2010
)
0.59
" There was a clear relationship between the number of active alleles and the pharmacokinetic parameters for risperidone and 9-hydroxyrisperidone, but there were no differences for total active moiety."( Effects of CYP2D6 genotype on the pharmacokinetics, pharmacodynamics, and safety of risperidone in healthy volunteers.
Abad-Santos, F; Gallego-Sandín, S; López-Rodríguez, R; Novalbos, J; Ochoa, D; Román, M, 2010
)
0.8
"Data regarding the pharmacokinetic properties of risperidone in the Thai population are limited."( Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in Thailand.
Boonleang, J; Mahatthanatrakul, W; Pipatrattanaseree, W; Tanthana, C, 2010
)
0.85
"The aim of this study was to evaluate and compare the pharmacokinetic properties of risperidone and its active metabolite, 9-hydroxyrisperidone (which reportedly contributes to the drug's pharmacodynamic effects), in a newly developed generic tablet formulation (test) and a branded formulation (reference) in healthy, fasting, male Thai volunteers."( Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in Thailand.
Boonleang, J; Mahatthanatrakul, W; Pipatrattanaseree, W; Tanthana, C, 2010
)
0.82
" The effects of formulation, period, sequence, and subject (within sequence) on pharmacokinetic parameters were analyzed using ANOVA."( Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in Thailand.
Boonleang, J; Mahatthanatrakul, W; Pipatrattanaseree, W; Tanthana, C, 2010
)
0.6
" The ANOVA suggested no statistically significant effect of formulation, period, or sequence on the studied pharmacokinetic parameters of the active moiety, risperidone, or 9-hydroxyrisperidone."( Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in Thailand.
Boonleang, J; Mahatthanatrakul, W; Pipatrattanaseree, W; Tanthana, C, 2010
)
0.79
"The single-dose pharmacokinetic data in this small, all-male, selected sample of fasting, healthy volunteers met Thailand's regulatory criteria for assuming bioequivalence of the tested generic and reference 2-mg risperidone tablets."( Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in Thailand.
Boonleang, J; Mahatthanatrakul, W; Pipatrattanaseree, W; Tanthana, C, 2010
)
0.78
"Significant differences were observed between the ABCB1 3435C>T genotypes for the pharmacokinetic parameters (peak serum concentration) of risperidone and the active moiety (risperidone and its main metabolite, 9-hydroxyrisperidone)."( Influence of ABCB1 genetic polymorphisms on the pharmacokinetics of risperidone in healthy subjects with CYP2D6*10/*10.
Cho, HY; Kang, HA; Lee, IK; Lee, SN; Lee, YB; Yoo, HD, 2011
)
0.81
" Pharmacokinetic parameters of Test and Reference were obtained by noncompartmental analysis."( Comparative pharmacokinetics and bioequivalence of two tablet formulations of 2 mg risperidone in healthy Thai male volunteers.
Khorana, N; Lohitnavy, O; Maphanta, S; Sayasathid, J; Srichaiya, A, 2011
)
0.59
"The 90% confidence intervals for Test/Reference ratios of the pharmacokinetic parameters (Cmax, AUC0-t and AUC0-∞) of both risperidone and its active metabolite (9-hydroxyrisperidone) fell within the acceptable bioequivalence range (80 - 125%) according to ASEAN guideline."( Comparative pharmacokinetics and bioequivalence of two tablet formulations of 2 mg risperidone in healthy Thai male volunteers.
Khorana, N; Lohitnavy, O; Maphanta, S; Sayasathid, J; Srichaiya, A, 2011
)
0.8
" In this study, fexofenadine, verapamil, risperidone, ondansetron, and imipramine were used as model compounds to investigate the effectiveness of MIM in pharmacokinetic studies."( Development of a novel high-throughput analytical methodology, multiple injection method, for quantitative analysis in drug metabolism and pharmacokinetic studies using liquid chromatography with tandem mass spectrometry.
Ohkawa, T; Tanaka, Y; Yasui, H, 2011
)
0.64
"Due to high interindividual variability in peripheral pharmacokinetic parameters, dosing of antipsychotics relies on clinical trial and error."( Predicting plasma concentration of risperidone associated with dosage change: a population pharmacokinetic study.
Bies, RR; Mamo, DC; Mimura, M; Pollock, BG; Suzuki, T; Tsunoda, K; Uchida, H; Watanabe, K, 2012
)
0.66
" We conducted the population pharmacokinetic analysis of risperidone and 9-hydroxyrisperidone using a nonlinear mixed effects modeling (NONMEM) method and explored the possible influence of genetic polymorphisms in CYP2D6 alleles and ABCB1 (2677G>T/A and 3435C>T) on the population pharmacokinetics of risperidone and 9-hydroxyrisperidone."( Population pharmacokinetic analysis of risperidone and 9-hydroxyrisperidone with genetic polymorphisms of CYP2D6 and ABCB1.
Cho, HY; Lee, SN; Lee, YB; Yoo, HD; Yoon, H, 2012
)
0.89
"The purpose of this review is to describe the pharmacokinetic profile of paliperidone and its clinical implications in the treatment of schizophrenia and schizoaffective disorder."( Oral paliperidone extended-release: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability.
Citrome, L, 2012
)
0.38
" Genetic polymorphisms that manifest as highly variable pharmacodynamic and pharmacokinetic measures are its expected causes."( Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
Cremers, TI; Flik, G; Hofland, C; Stratford, RE, 2012
)
0.38
"The study aims were to characterize risperidone and (±)-9-hydroxyrisperidone pharmacokinetic (PK) variability in children and adolescents and to evaluate covariate effects on PK parameters."( Population pharmacokinetic modeling of risperidone and 9-hydroxyrisperidone to estimate CYP2D6 subpopulations in children and adolescents.
Aman, MG; Bies, RR; Saldaña, SN; Sherwin, CM; Vinks, AA, 2012
)
0.92
"05), while the other pharmacokinetic parameters did not show any significant differences."( Effects of single or repeated silymarin administration on pharmacokinetics of risperidone and its major metabolite, 9-hydroxyrisperidone in rats.
Chae, SW; Choi, JM; Lee, HJ; Lee, KS; Park, JH; Rhie, SJ, 2013
)
0.62
" Although there are a few reports in the literature regarding the pharmacokinetic characteristics of risperidone, insufficient data on its pharmacokinetic properties in a Chinese population are available."( Bioequivalence and pharmacokinetic evaluation of two formulations of risperidone 2 mg : an open-label, single-dose, fasting, randomized-sequence, two-way crossover study in healthy male Chinese volunteers.
Jia, JY; Li, SJ; Liu, GY; Liu, Y; Liu, YM; Wang, W; Weng, LP; Yu, C; Zhang, MQ, 2013
)
0.84
"To meet the requirements for marketing a new generic product, this study was designed to compare the pharmacokinetic properties and bioequivalence of two 2 mg tablet formulations of risperidone: a newly developed generic formulation (test) and a branded formulation (reference) in healthy adult male Chinese volunteers."( Bioequivalence and pharmacokinetic evaluation of two formulations of risperidone 2 mg : an open-label, single-dose, fasting, randomized-sequence, two-way crossover study in healthy male Chinese volunteers.
Jia, JY; Li, SJ; Liu, GY; Liu, Y; Liu, YM; Wang, W; Weng, LP; Yu, C; Zhang, MQ, 2013
)
0.82
" The present study aims to improve our understanding of antipsychotic-related adverse reactions (ARs) and their possible association with common genetic variants of pharmacodynamic proteins such as neurotransmitter receptors/transporters."( Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers.
Abad-Santos, F; Ayuso, C; Borobia, AM; Cabaleiro, T; Carcas, AJ; López-Rodríguez, R; Novalbos, J; Ochoa, D; Román, M, 2013
)
0.39
"Genetic variants in pharmacodynamic genes could represent valuable markers of AR risk and antipsychotic safety."( Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers.
Abad-Santos, F; Ayuso, C; Borobia, AM; Cabaleiro, T; Carcas, AJ; López-Rodríguez, R; Novalbos, J; Ochoa, D; Román, M, 2013
)
0.39
" The objective of this analysis was to report the results of a population pharmacokinetic analysis and to describe the relationship between risperidone and 9-hydroxyrisperidone levels with dopamine (DA) D2-receptor occupancy, prolactin levels, and adverse events using data collected in 45 clinically stable schizophrenic patients receiving RBP-7000 in single ascending doses (risperidone) of 60, 90, and 120 mg."( A model-based approach to characterize the population pharmacokinetics and the relationship between the pharmacokinetic and safety profiles of RBP-7000, a new, long-acting, sustained-released formulation of risperidone.
Fudala, PJ; Gomeni, R; Heidbreder, C; Nasser, AF, 2013
)
0.78
" Moreover, its ability to predict actigraphy records is similar to the predictive power of pharmacokinetic parameters (24%)."( Effect of CYP2D6 on risperidone pharmacokinetics and extrapyramidal symptoms in healthy volunteers: results from a pharmacogenetic clinical trial.
Arnaiz, JA; Bernardo, M; Bioque, M; de Bobadilla, RF; Ferrando, E; Gassó, P; Lafuente, A; Mas, S; Papagianni, K, 2014
)
0.73
" The pharmacokinetic profiles of RIS-EOP were evaluated compared with immediate release tablets in beagle dogs."( Preparation, release and pharmacokinetics of a risperidone elementary osmotic pump system.
Gong, W; Liu, Y; Mei, DY; Mei, XG; Yang, M, 2015
)
0.67
" An integrated population pharmacokinetic model describing simultaneously risperidone and 9-hydroxyrisperidone after risperidone oral intake and RBP-7000 administration was developed in NON-MEM using 5,232 quantifiable plasma concentrations."( Population pharmacokinetics and prediction of dopamine D2 receptor occupancy after multiple doses of RBP-7000, a new sustained-release formulation of risperidone, in schizophrenia patients on stable oral risperidone treatment.
Fudala, PJ; Gomeni, R; Heidbreder, C; Laffont, CM; Nasser, AF; Zheng, B, 2014
)
0.83
" The objective of this study was to use pharmacokinetic and pharmacodynamic modeling tools to relate CAT with D2RO in rats and to compare that with the relationship between D2RO and EPS in humans."( Dopamine D2 receptor occupancy as a predictor of catalepsy in rats: a pharmacokinetic-pharmacodynamic modeling approach.
Barton, HA; Danhof, M; de Greef, R; Grimwood, S; Groothuis, GM; Johnson, M; Kozielska, M; Pilla Reddy, V; Proost, JH; Vermeulen, A, 2014
)
0.4
" Two single-dose, two-period crossover studies of risperidone (n = 70) were reanalysed to calculate CVw for AUCt and Cmax ."( Polymorphisms in CYP2D6 have a greater effect on variability of risperidone pharmacokinetics than gender.
Abad-Santos, F; Cabaleiro, T; López-Rodríguez, R; Moreno, I; Novalbos, J; Ochoa, D; Román, M, 2015
)
0.91
" They also showed lower Cmax and AUC and higher t1/2 for hydroxyrisperidone."( Effect of polymorphisms on the pharmacokinetics, pharmacodynamics, and safety of risperidone in healthy volunteers.
Abad-Santos, F; Ayuso, C; Cabaleiro, T; López-Rodríguez, R; Novalbos, J; Ochoa, D; Román, M, 2014
)
0.87
" A population pharmacokinetic model of RBP-7000 was developed in 90 clinically stable schizophrenic patients having received single/repeated doses of 60, 90, or 120 mg."( Population pharmacokinetic modeling and simulation to guide dose selection for RBP-7000, a new sustained-release formulation of risperidone.
Fudala, PJ; Gomeni, R; Heidbreder, C; Laffont, CM; Nasser, AF; Zheng, B, 2015
)
0.62
"This article gives an overview of the pharmacokinetic profile of risperidone and a comprehensive review of treatment studies regarding the use of risperidone in ASD."( Clinical and pharmacokinetic evaluation of risperidone for the management of autism spectrum disorder.
Dietrich, A; Dinnissen, M; Hoekstra, PJ; van den Hoofdakker, BJ, 2015
)
0.92
" The validated UPLC method was successfully applied to the pharmacokinetic study of RIS and 9-OHRIS in human plasma."( Concurrent determination of olanzapine, risperidone and 9-hydroxyrisperidone in human plasma by ultra performance liquid chromatography with diode array detection method: application to pharmacokinetic study.
Ramanathan, M; Siva Selva Kumar, M, 2016
)
0.7
"Using a population pharmacokinetic approach, we aimed to characterize the genetic and non-genetic sources of variability affecting risperidone and 9-hydroxyrisperidone pharmacokinetics, and relate them to common side effects."( Genetics-Based Population Pharmacokinetics and Pharmacodynamics of Risperidone in a Psychiatric Cohort.
Choong, E; Conus, P; Csajka, C; Eap, CB; Guidi, M; Vandenberghe, F; von Gunten, A, 2015
)
0.86
" Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer)."( Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation.
Cekić, ND; Daniels, R; Isailović, TM; Marković, BD; Ranđelović, DV; Savić, MM; Savić, SD; Savić, SR; Timić Stamenić, T; Đorđević, SM, 2015
)
0.89
" Pharmacokinetic parameters were derived from plasma concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone (formed via CYP2D6 and CYP3A4), collected before and over 4 days after risperidone administration, and from steady-state plasma concentrations of armodafinil and its circulating metabolites, R-modafinil acid and modafinil sulfone."( Evaluation of potential pharmacokinetic drug-drug interaction between armodafinil and risperidone in healthy adults.
Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015
)
0.87
"Our data show a potential pharmacokinetic interaction, most likely via CYP3A4 between amlodipine and RIS, reflected in significantly different C/Ds for RIS, 9-OH-RIS and AM."( Pharmacokinetic considerations in the treatment of hypertension in risperidone-medicated patients - thinking of clinically relevant CYP2D6 interactions.
Gründer, G; Haen, E; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B; Walther, S, 2016
)
0.67
" The pharmacokinetic of the active moiety was biphasic for all three dose groups, and the mean plasma concentration was 21."( Phase I, open-label, randomized, parallel study to evaluate the pharmacokinetics, safety, and tolerability of one intramuscular injection of risperidone ISM at different dose strengths in patients with schizophrenia or schizoaffective disorder (PRISMA-1).
Anta, L; Ayani, I; Gutierro, I; Ivanov, M; Llaudó, J; Martínez, J; Morozova, M; Schronen, J, 2016
)
0.64
" The objective of the study was to identify pharmacokinetic interactions of different mood stabilizers on the metabolism of risperidone (RIS) under natural conditions."( Pharmacokinetic Drug-Drug Interactions of Mood Stabilizers and Risperidone in Patients Under Combined Treatment.
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B, 2016
)
0.88
"The data give evidence for pharmacokinetic interactions between RIS and different anticonvulsant mood stabilizers."( Pharmacokinetic Drug-Drug Interactions of Mood Stabilizers and Risperidone in Patients Under Combined Treatment.
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B, 2016
)
0.67
"To disentangle an association between tobacco smoking, smoking habits and pharmacokinetic patterns such as plasma concentrations of risperidone (RIS), its active metabolite 9-hydroxyrisperidone (9-OH-RIS) and the active moiety, AM, (RIS+9-OH-RIS) in a naturalistic sample."( Effect of smoking on risperidone pharmacokinetics - A multifactorial approach to better predict the influence on drug metabolism.
Gründer, G; Haen, E; Hiemke, C; Paulzen, M; Schoretsanitis, G; Stegmann, B, 2017
)
0.98
"011) for the group of moderate smokers while other pharmacokinetic parameters did not differ."( Effect of smoking on risperidone pharmacokinetics - A multifactorial approach to better predict the influence on drug metabolism.
Gründer, G; Haen, E; Hiemke, C; Paulzen, M; Schoretsanitis, G; Stegmann, B, 2017
)
0.77
"Alterations of risperidone metabolism suggest pharmacokinetic interactions for levomepromazine and melperone."( Pharmacokinetic considerations in antipsychotic augmentation strategies: How to combine risperidone with low-potency antipsychotics.
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KRJ; Stegmann, B; Walther, S, 2017
)
1.03
" The mean Cmax of the active moiety was achieved 24-48 h (tmax) after each administration, regardless of injection site."( A phase II study to evaluate the pharmacokinetics, safety, and tolerability of Risperidone ISM multiple intramuscular injections once every 4 weeks in patients with schizophrenia.
Anta, L; Ayani, I; Gutierro, I; Litman, RE; Llaudó, J; Martínez, J, 2018
)
0.71
" Various pharmacokinetic parameters were determined in both studies."( Pharmacokinetics and Safety of Risperidone Subcutaneous Implants in Stable Patients With Schizophrenia.
Adera, M; Dammerman, R; Kim, S; Schwarz, A, 2018
)
0.77
"We assessed the dosage strengths of paliperidone palmitate 1-month (PP1M) long-acting injectable resulting in similar steady-state (SS) exposures to the dosage strengths of oral risperidone using pharmacokinetic (PK) simulations."( Maintenance dose conversion between oral risperidone and paliperidone palmitate 1 month: Practical guidance based on pharmacokinetic simulations.
Gopal, S; Kern Sliwa, J; Kim, E; Mathews, M; Ravenstijn, P; Russu, A; Singh, A, 2018
)
0.94
" The goal of this study was to develop a physiologically based pharmacokinetic (PBPK) model considering the CYP2D6 genetic polymorphism for risperidone and 9-hydroxyrisperidone (9-OH-RIS) taking CYP3A4 into account."( Physiologically Based Pharmacokinetic Modelling to Describe the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone According to Cytochrome P450 2D6 Phenotypes.
Abad-Santos, F; Hempel, G; Kneller, LA, 2020
)
0.98
" The goal of the study was to develop physiologically based pharmacokinetic (PBPK) models for the elderly aged 65+ years."( Modelling Age-Related Changes in the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone in Different CYP2D6 Phenotypes Using a Physiologically Based Pharmacokinetic Approach.
Hempel, G; Kneller, LA, 2020
)
0.8
" Overall, age-related changes of the pharmacokinetics in the elderly were mainly observed in Cmax and AUC."( Modelling Age-Related Changes in the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone in Different CYP2D6 Phenotypes Using a Physiologically Based Pharmacokinetic Approach.
Hempel, G; Kneller, LA, 2020
)
0.8
"A comprehensive electronic database search identified studies reporting relationships between genetically determined CYP2D6 metabolism and risperidone pharmacokinetic properties."( CYP2D6 Genetic Polymorphisms and Risperidone Pharmacokinetics: A Systematic Review and Meta-analysis.
Allen, JD; Bishop, JR; Brown, SJ; de Leon, J; Eum, S; Lee, AM; Shan, Y; Zhang, L, 2020
)
1.04
"The purpose of this study was to investigate the impacts of the formulation parameters on the pharmacokinetics and bioequivalence of risperidone orodispersible film (ODF) using physiologically based pharmacokinetic model."( Evaluation of the Impacts of Formulation Parameters on the Pharmacokinetics and Bioequivalence of Risperidone Orodispersible Film: a Physiologically Based Pharmacokinetic Modeling Approach.
Chen, F; Chen, Y; Jiao, Z; Lin, HS; Liu, H; Quan, Y; Wang, B; Wang, H; Xiang, X; Yang, L; Yang, Z, 2020
)
0.98
" With this review, we aim to provide an overview of the pharmacodynamic interactions between ketamine and mood stabilizers, benzodiazepines, monoamine oxidase-inhibitors, antipsychotics, and psychostimulants."( Pharmacodynamic Interactions Between Ketamine and Psychiatric Medications Used in the Treatment of Depression: A Systematic Review.
Bakker, IM; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Touw, DJ; Veraart, JKE; Visser, BAE, 2021
)
0.62
" More studies are needed to provide insight into pharmacodynamic interactions with ketamine."( Pharmacodynamic Interactions Between Ketamine and Psychiatric Medications Used in the Treatment of Depression: A Systematic Review.
Bakker, IM; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Touw, DJ; Veraart, JKE; Visser, BAE, 2021
)
0.62
" The rate of removal of LAIs is regulated by the slow rate of absorption in the site of injection and the phenomenon of their increased half-life is called flip-flop pharmacokinetics."( [Clinical pharmacokinetics and pharmaceutical forms of long-acting injectable antipsychotics].
Kyziridis, TC, 2022
)
0.72
" A population pharmacokinetic (PPK) modeling and simulation approach was implemented to identify TV-46000 doses and dosing schedules for clinical development that would provide the best balance between clinical efficacy and safety."( Population Pharmacokinetic Modeling and Simulation of TV-46000: A Long-Acting Injectable Formulation of Risperidone.
Elgart, A; Gomeni, R; Harary, E; Kalmanczhelyi, A; Lamson, M; Levi, M; Loupe, P; Merenlender Wagner, A; Perlstein, I; Spiegelstein, O; Tiver, R, 2022
)
0.94
"As outlined in changes to the US prescribing information for all methylphenidate and risperidone products, health care professionals should be aware that changes to this combination may be associated with a pharmacodynamic drug-drug interaction resulting in acute hyperkinetic movement disorder."( Acute Hyperkinetic Movement Disorders as a Multifactorial Pharmacodynamic Drug Interaction Between Methylphenidate and Risperidone in Children and Adolescents.
Burkhart, K; Chen, Q; Cheng, C; Croteau, D; Demczar, D; Kortepeter, C; Mohamoud, M; Stone, M; Volpe, DA,
)
0.56
"This study aimed to determine the effects of pregnancy and ontogeny on risperidone and paliperidone pharmacokinetics by assessing their serum concentrations in two subjects and constructing a customized physiologically-based pharmacokinetic (PBPK) model."( Physiologically-based pharmacokinetic model to investigate the effect of pregnancy on risperidone and paliperidone pharmacokinetics: Application to a pregnant woman and her neonate.
Fujioka, K; Fujiwara, N; Horai, T; Iijima, K; Imafuku, H; Ito, T; Mahdy, WYB; Omura, T; Otsuka, I; Yamamoto, K; Yano, I, 2023
)
1.37

Compound-Compound Interactions

The potential interaction of risperidone (RISP), which is metabolized by 2D6 and transported across the blood brain barrier (BBB) by P-gp, was studied in combination with bupropion (BUP) and also with sertraline (SERT)

ExcerptReferenceRelevance
" A number of patient-related variables also affect the clinical significance of a drug-drug interaction."( Drug interactions and antipsychotic therapy.
DeVane, CL,
)
0.13
" This study examined the effect of electroconvulsive therapy (ECT) in combination with risperidone in an open trial in 10 male schizophrenic patients with significant aggressive behaviors."( Effectiveness of ECT combined with risperidone against aggression in schizophrenia.
Ashby, CR; Hirose, S; Mills, MJ, 2001
)
0.81
" One concern raised by the widespread use of multiple concurrent pharmacotherapies is the potential for drug-drug interactions to adversely affect patient outcome."( An evaluation of risperidone drug interactions.
DeVane, CL; Nemeroff, CB, 2001
)
0.65
"This study examined the short-term efficacy of electroconvulsive therapy (ECT) combined with antipsychotic medication in treatment-resistant schizophrenia (TRS)."( Efficacy of electroconvulsive therapy combined with antipsychotic medication in treatment-resistant schizophrenia: a prospective, open trial.
Tang, WK; Ungvari, GS, 2002
)
0.31
" Treatment with divalproex in combination with an atypical antipsychotic agent resulted in earlier improvements in a range of psychotic symptoms among acutely hospitalized patients with schizophrenia."( Effect of divalproex combined with olanzapine or risperidone in patients with an acute exacerbation of schizophrenia.
Casey, DE; Daniel, DG; Sommerville, KW; Tracy, KA; Wassef, AA; Wozniak, P, 2003
)
0.57
" The aim of this study was to compare the effectiveness and tolerability of topiramate and divalproex in combination with risperidone for treating acute mania patients in a naturalistic treatment setting."( Topiramate and divalproex in combination with risperidone for acute mania: a randomized open-label study.
Bahk, WM; Choi, SK; Chung, SK; Jon, DI; Lee, JS; Pae, CU; Paik, IH; Shin, YC; Woo, JM; Yoon, BH, 2005
)
0.79
" As ciproxifan and thioperamide are inhibitors of cytochrome P450 enzymes, responsible for metabolizing risperidone and haloperidol, the possibility that the augmentation of antipsychotics by imidazoles resulted from drug-drug interactions was tested."( Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs.
Ballard, ME; Cowart, M; Decker, MW; Esbenshade, TA; Faghih, R; Fox, GB; Hancock, AA; Pan, L; Roberts, S; Rueter, LE; Zhang, M, 2005
)
0.54
"Accumulating evidence indicates that modulation of the activity of cytochrome P450 (CYP) enzymes and the multidrug resistance transporter P-glycoprotein (P-gp) is responsible for many drug-drug interactions."( Population pharmacokinetic analysis of drug-drug interactions among risperidone, bupropion, and sertraline in CF1 mice.
DeVane, CL; Donovan, JL; Gibson, BB; Markowitz, JS; Wang, JS; Zhu, HJ, 2006
)
0.57
"The potential interaction of risperidone (RISP), which is metabolized by 2D6 and transported across the blood brain barrier (BBB) by P-gp, was studied in combination with bupropion (BUP) and also with sertraline (SERT)."( Population pharmacokinetic analysis of drug-drug interactions among risperidone, bupropion, and sertraline in CF1 mice.
DeVane, CL; Donovan, JL; Gibson, BB; Markowitz, JS; Wang, JS; Zhu, HJ, 2006
)
0.86
"To compare oral risperidone and intramuscular (IM) haloperidol, both in combination with IM lorazepam, in the management of acute agitation and psychosis in the medical emergency department."( Risperidone versus haloperidol, in combination with lorazepam, in the treatment of acute agitation and psychosis: a pilot, randomized, double-blind, placebo-controlled trial.
Currier, GW; McMullan, JT; Veser, BD; Veser, FH; Zealberg, J, 2006
)
2.12
" These results further support the previous suggestion that the cortical dopamine system plays an important role in the effects of antipsychotic drugs administered in combination with fluvoxamine."( Lack of enhanced effect of antipsychotics combined with fluvoxamine on acetylcholine release in rat prefrontal cortex.
Ago, Y; Baba, A; Matsuda, T; Nakamura, S; Sato, M, 2006
)
0.33
"The treatment of DD combined with low dosage of risperidone is effective on chronic schizophrenia and shows less adverse reaction."( [Clinical observation on effect of modified Daotan Decoction combined with small dose risperidone in treating chronic schizophrenia].
Liu, JL; Ma, L; Wang, Y, 2007
)
0.82
"Any attempt to develop personalized dosing needs to be anchored in our understanding of the pharmacological response of each drug in each person's environment, particularly drug-drug interactions (DDIs) and how genetic make-up influences drug response."( A preliminary attempt to personalize risperidone dosing using drug-drug interactions and genetics: part I.
Cozza, KL; de Leon, J; Sandson, NB,
)
0.4
"The objective of this study was to evaluate the efficacy and safety of divalproex sodium extended release (divalproex ER) vs placebo in combination with olanzapine or risperidone for the treatment of acute exacerbations of schizophrenia."( Divalproex ER combined with olanzapine or risperidone for treatment of acute exacerbations of schizophrenia.
Abi-Saab, W; Baker, J; Casey, DE; Daniel, DG; Greco, N; Kane, JM; Redden, L; Saltarelli, M; Tamminga, C; Tran-Johnson, T; Wozniak, P, 2009
)
0.81
" The need to provide effective therapeutic interventions to patients who do not have an optimal response to clozapine is the most common reason for simultaneously prescribing a second antipsychotic drug in combination with clozapine."( Clozapine combined with different antipsychotic drugs for treatment resistant schizophrenia.
Barbui, C; Boso, M; Cipriani, A, 2009
)
0.35
"In a randomized trial, we recently obtained evidence for comparable efficacy and differential side effects of clozapine in combination with ziprasidone (CZ, N=12) versus risperidone (CR, N=12)."( Long-term efficacy and tolerability of clozapine combined with ziprasidone or risperidone.
Dressing, H; Englisch, S; Krumm, B; Kuwilsky, A; Zink, M, 2010
)
0.78
"The aim of this paper was to explore the efficacy of modified electroconvulsive therapy (MECT) combined with risperidone oral solution in the treatment of agitation in the acute stage of epilepsy, and the effects of insulin-like growth factor-1 mRNA and protein expression."( Study of modified electroconvulsive therapy combined with risperidone oral solution in the treatment of agitation in the acute stage of epilepsy and expression level changes of insulin-like growth factor-1.
Li, C; Li, J, 2016
)
0.89
" The patients in the experimental group were treated with MECT combined with risperidone oral solution."( Study of modified electroconvulsive therapy combined with risperidone oral solution in the treatment of agitation in the acute stage of epilepsy and expression level changes of insulin-like growth factor-1.
Li, C; Li, J, 2016
)
0.91
" If the ar/mod-antipsychotic drug combination is necessary, for whatever reason, then the dose of the atypical antipsychotic drug may need to be appropriately raised."( Delayed drug interactions in psychiatry: armodafinil and risperidone as a potential case in point.
Andrade, C, 2015
)
0.66
"The combination of anticonvulsant mood stabilizers with antipsychotic drugs may lead to clinically relevant drug-drug interactions."( Pharmacokinetic Drug-Drug Interactions of Mood Stabilizers and Risperidone in Patients Under Combined Treatment.
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B, 2016
)
0.67
" For these people, a number of treatment strategies have emerged, including the prescription of a second anti-psychotic drug in combination with clozapine."( Clozapine combined with different antipsychotic drugs for treatment-resistant schizophrenia.
Barber, S; Cipriani, A; Corsi, M; Olotu, U, 2017
)
0.46
"To assess whether a "drugome-wide" screen with case-crossover design is a feasible approach for identifying candidate drugs and drug-drug interactions."( Screening approach for identifying candidate drugs and drug-drug interactions related to hip fracture risk in persons with Alzheimer disease.
Hartikainen, S; Koponen, M; Lavikainen, P; Paananen, J; Taipale, H; Tanskanen, A; Tiihonen, J; Tolppanen, AM, 2017
)
0.46
"Case-crossover analysis is a potential approach for identifying candidate drugs and drug-drug interactions associated with adverse events as it implicitly controls for fixed confounders."( Screening approach for identifying candidate drugs and drug-drug interactions related to hip fracture risk in persons with Alzheimer disease.
Hartikainen, S; Koponen, M; Lavikainen, P; Paananen, J; Taipale, H; Tanskanen, A; Tiihonen, J; Tolppanen, AM, 2017
)
0.46
" Food and Drug Administration to treat "irritability" in children and adolescents with autism spectrum disorder, in combination with another drug with respect to experimental design, assessment techniques, drug co-administered, reported effects, and participant characteristics."( Risperidone in combination with other drugs: Experimental research in individuals with autism spectrum disorder.
Curiel, H; Li, A; MacNeill, B; Poling, A, 2017
)
1.9
"As outlined in changes to the US prescribing information for all methylphenidate and risperidone products, health care professionals should be aware that changes to this combination may be associated with a pharmacodynamic drug-drug interaction resulting in acute hyperkinetic movement disorder."( Acute Hyperkinetic Movement Disorders as a Multifactorial Pharmacodynamic Drug Interaction Between Methylphenidate and Risperidone in Children and Adolescents.
Burkhart, K; Chen, Q; Cheng, C; Croteau, D; Demczar, D; Kortepeter, C; Mohamoud, M; Stone, M; Volpe, DA,
)
0.56
" We hypothesized that a low dose of risperidone in combination with sertraline would reduce serious adverse effects without decreasing treatment response."( Efficacy of low-dose risperidone in combination with sertraline in first-episode drug-naïve patients with schizophrenia: a randomized controlled open-label study.
Lang, X; Wu, F; Xiu, M; Xue, M; Zang, X; Zhang, X, 2023
)
1.5
"A total of 230 patients with FEMN SZ were randomly assigned to receive low-dose risperidone in combination with sertraline (RS group) or regular-dose risperidone (control group)."( Efficacy of low-dose risperidone in combination with sertraline in first-episode drug-naïve patients with schizophrenia: a randomized controlled open-label study.
Lang, X; Wu, F; Xiu, M; Xue, M; Zang, X; Zhang, X, 2023
)
1.46
"Our study suggests that low-dose risperidone in combination with sertraline was more effective for psychotic symptoms and psychosocial functioning, with significantly fewer adverse effects in patients with FEMN SZ."( Efficacy of low-dose risperidone in combination with sertraline in first-episode drug-naïve patients with schizophrenia: a randomized controlled open-label study.
Lang, X; Wu, F; Xiu, M; Xue, M; Zang, X; Zhang, X, 2023
)
1.51
" However, the effects of the low frequency of rTMS combined with antipsychotics on the gut microbiome in chronic SCH have been poorly investigated."( Effects of low-frequency rTMS combined with risperidone on the gut microbiome in hospitalized patients with chronic schizophrenia.
Bai, J; Chen, YH; Cui, ZQ; Fu, R; Guo, L; Li, R; Peng, ZW; Tan, QR; Yang, JB, 2023
)
1.17

Bioavailability

The absolute oral bioavailability of risperidone is nearly 70%, and after oral administration, it is rapidly absorbed. The plasma level reaching a peak at about 1 h. It was hypothesized that cytochrome P450 (CYP)3A inhibition of the small intestine by voriconazole and P-glycoprotein (P-gp) inhibition by risperids exerted a synergistic effect on tacrolimus.

ExcerptReferenceRelevance
" bioavailability and a relatively long duration of action."( Pharmacology of risperidone (R 64 766), a new antipsychotic with serotonin-S2 and dopamine-D2 antagonistic properties.
Awouters, F; Janssen, PA; Meert, TF; Megens, AA; Niemegeers, CJ; Schellekens, KH, 1988
)
0.62
" The newer antipsychotic agents clozapine and risperidone are also well absorbed and undergo extensive presystemic elimination."( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs.
DeVane, CL, 1995
)
0.55
" Risperidone absolute oral bioavailability was 66%."( Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects.
De Coster, R; Heykants, J; Huang, ML; Jansen, AA; Jonkman, JH; Van Peer, A; Visscher, HW; Woestenborghs, R; Zylicz, Z, 1993
)
1.45
" These drugs are well absorbed when taken orally but are poorly bioavailable because of presystemic elimination."( Pharmacokinetics of clozapine and risperidone: a review of recent literature.
Byerly, MJ; DeVane, CL, 1996
)
0.57
"The bioavailability of risperidone was evaluated in an open-label, randomized, two-way, crossover study comparing a 1-mg tablet with a 1-mg/ml oral solution."( Risperidone: effects of formulations on oral bioavailability.
Gutierrez, R; Huang, ML; Lee, PI; Woestenborghs, R,
)
1.88
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" It may be less well absorbed and/or less effective than Clozaril, although evidence is conflicting."( Advances in atypical antipsychotics for the treatment of schizophrenia: new formulations and new agents.
Albert, MJ; Baldessarini, RJ; Centorrino, F; Kelleher, JP, 2002
)
0.31
" The results showed that risperidone, when administered with galantamine, did not change the bioavailability of galantamine at steady state."( Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs are administered alone and together.
Huang, F; Janssens, L; Lasseter, KC; Lau, H; Verhaeghe, T; Zhao, Q, 2002
)
0.86
" Therefore, studies of comparative bioavailability of different formulations of a same drug are worthwhile."( [Comparative bioavailability study of two formulations of risperidone available in the Chilean market].
Carrillo, MJ; Gaete, LE; Saavedra, I; Schatloff, O; Solís, J; Venegas, P, 2003
)
0.56
"To compare the bioavailability of two risperidone formulations available in the Chilean market."( [Comparative bioavailability study of two formulations of risperidone available in the Chilean market].
Carrillo, MJ; Gaete, LE; Saavedra, I; Schatloff, O; Solís, J; Venegas, P, 2003
)
0.83
"The bioavailability of a local risperidone formulation (Spiron) was compared with the original formulation of the drug (Risperdal) in 12 healthy volunteers, aged 19 +/- 1 years."( [Comparative bioavailability study of two formulations of risperidone available in the Chilean market].
Carrillo, MJ; Gaete, LE; Saavedra, I; Schatloff, O; Solís, J; Venegas, P, 2003
)
0.85
"This study demonstrated that the bioavailability of risperidone was increased by verapamil, suggesting in vivo involvement of P-glycoprotein in the pharmacokinetics of risperidone."( Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition.
Kaneo, S; Nakagami, T; Saito, M; Tateishi, T; Yasui-Furukori, N, 2005
)
0.82
" The oral bioavailability of the polymer was 40%."( Intestinal uptake and biodistribution of novel polymeric micelles after oral administration.
Ariën, A; Brewster, M; Mathot, F; Préat, V; van Beijsterveldt, L, 2006
)
0.33
" Based on the results, one candidate was selected for advancement that showed moderate in vitro solubility, but had the highest in vitro permeability and ratio of colonic to duodenal bioavailability (0."( Preclinical assessment of the feasibility of applying controlled release oral drug delivery to a lead series of atypical antipsychotics.
Ashton, D; Borghys, H; Chen, J; Dai, W; Dong, L; Eichenbaum, G; Evans, J; Kennis, L; Li, S; Mackie, C; Megens, A; Nguyen, J; Pollock-Dove, C; Scicinski, J; van Osdol, W; Xu, Y, 2006
)
0.33
" The absorption rate constant was lower in the verapamil group."( P-glycoprotein and cytochrome P450 3A4 involvement in risperidone transport using an in vitro Caco-2/TC7 model and an in vivo model.
Barthélémy, C; Brossard, D; Clavey, V; Cousein, E; Crauste-Manciet, S; Danel, C; Joiris, E; Lestavel, S; Odou, P; Poullain, S; Robert, H; Simon, N; Vaccher, C; Williame, V, 2007
)
0.59
"The objective of the study was to compare the bioavailability of a generic oral solution of risperidone (Test formulation) and Risperdal tablets (Reference formulation)."( Lack of bioequivalence between generic risperidone oral solution and originator risperidone tablets.
Piniella, PM; Relleke, M; van Os, S, 2007
)
0.83
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" Thus, rifampin reduced the exposure to risperidone, probably because of a decrease in its bioavailability through the induction of CYP3A and probably P-glycoprotein."( Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone.
Kim, KA; Kim, KB; Lee, HJ; Liu, KH; Park, JY; Park, PW; Shin, JG, 2008
)
0.84
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" The pharmacokinetics following deltoid injection and bioequivalence between deltoid and gluteal administration were assessed in an open-label, single-dose, crossover, fully powered bioavailability study."( Risperidone long-acting injection: pharmacokinetics following administration in deltoid versus gluteal muscle in schizophrenic patients.
Herben, V; Mannaert, E; Quiroz, J; Rusch, S; Thyssen, A, 2010
)
1.8
"To compare the bioavailability of two risperidone orodispersible tablet products, Risperidone 1 mg Mouth dissolving tablet, Ranbaxy (Malaysia) Sdn."( Comparative bioavailability of two risperidone orodispersible tablet products after single dose administration.
Gaysonsiri, D; Jain, R; Kaewkamson, T; Kanjanawart, S; Khuroo, A; Kumar, S; Monif, T; Phunikhom, K; Rao Thudi, N; Reyar, S; Tangsucharit, P; Tassaneeyakul, W; Vannaprasaht, S, 2010
)
0.91
" Many excellent active compounds are confined because of general low oral bioavailability due to poor solubility."( [Advances in the study of polymeric micelles used in oral administration].
Chen, D; Deng, YH; Ding, PT; Wang, SL, 2010
)
0.36
"The aims of this study were to compare the relative bioavailability of a pharmaceutical-equivalent (test) formulation with a reference formulation of oral RSP 2 mg, both available commercially on the Brazilian pharmaceutical market, and to generate data regarding the oral bioavailability of the tested drug in healthy Brazilian volunteers."( Relative bioavailability of two oral formulations of risperidone 2 mg: A single-dose, randomized-sequence, open-label, two-period crossover comparison in healthy Brazilian volunteers.
Belotto, KC; Ferreira, AS; Gattaz, WF; Raposo, NR, 2010
)
0.61
" This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%)."( Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer-risperidone complexes.
Alonso, Sdel V; del Río Zabala, NE; Marotta, CH; Prieto, MJ; Temprana, CF, 2011
)
0.6
" It possesses good bioavailability following oral administration."( Comparative pharmacokinetics and bioequivalence of two tablet formulations of 2 mg risperidone in healthy Thai male volunteers.
Khorana, N; Lohitnavy, O; Maphanta, S; Sayasathid, J; Srichaiya, A, 2011
)
0.59
" The calculated relative bioavailability of risperidone transdermal patch was 115."( Formulation, in vitro and in vivo evaluation of transdermal patches containing risperidone.
Aggarwal, G; Dhawan, S; Hari Kumar, SL, 2013
)
0.88
" Preliminary tests for oral bioavailability also revealed promising results for this new class of potential antipsychotic compounds."( Molecular combination of the dopamine and serotonin scaffolds yield in novel antipsychotic drug candidates - characterization by in vivo experiments.
Enzensperger, C; Fleck, C; Lehmann, J; Mueller, FK; Robaa, D; Schulze, M; Siol, O, 2012
)
0.38
"This study was designed to compare the pharmacokinetic (PK) properties and bioavailability of 2 RIS formulations-the dispersible formulation (test) and a branded formulation (reference) in healthy male Chinese volunteers."( Comparative fasting bioavailability of dispersible and conventional tablets of risperidone: a single-dose, randomized-sequence, open-label, two-period crossover study in healthy male Chinese volunteers.
Chen, J; Hu, X; Huang, M; Liu, J; Shen-Tu, J; Wu, L, 2012
)
0.61
" There was significant difference in the absorption rate constant (k ( a )) of risperidone among the CYP2D6*10 genotype groups."( Population pharmacokinetic analysis of risperidone and 9-hydroxyrisperidone with genetic polymorphisms of CYP2D6 and ABCB1.
Cho, HY; Lee, SN; Lee, YB; Yoo, HD; Yoon, H, 2012
)
0.85
" The repeated exposures of silymarin, compared to single administration of silymarin, increased oral bioavailability and affected the pharmacokinetics of risperidone and 9-hydroxyrisperidone, by inhibiting P-gp."( Effects of single or repeated silymarin administration on pharmacokinetics of risperidone and its major metabolite, 9-hydroxyrisperidone in rats.
Chae, SW; Choi, JM; Lee, HJ; Lee, KS; Park, JH; Rhie, SJ, 2013
)
0.82
" This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%)."( Optimization and in vivo toxicity evaluation of G4.5 PAMAM dendrimer-risperidone complexes.
Arévalo Arévalo, R; Carreño Gutierrez, H; Chiaramoni, NS; del Rio Zabala, NE; del Valle Alonso, S; Marotta, CH; Prieto, MJ, 2014
)
0.64
" The relative bioavailability (RB) of risperidone from this formula was 161."( Effervescent tablet formulation for enhanced patient compliance and the therapeutic effect of risperidone.
Ghorab, MM; Ibrahim, HK; Mohammed, KA, 2016
)
0.92
" RISP has low solubility in aqueous medium and poor bioavailability because of its metabolism and high protein binding."( Development of Nutraceutical Emulsions as Risperidone Delivery Systems: Characterization and Toxicological Studies.
Calienni, MN; Chiaramoni, NS; Del Valle Alonso, S; Feas, DA; Igartúa, DE; Prieto, MJ, 2015
)
0.68
" Optimized formula showed significant improved bioavailability compared with marketed tablets."( The use of experimental design in the optimization of risperidone biodegradable nanoparticles: in vitro and in vivo study.
Ahmed, OA; Ahmed, TA; Alzubaidi, AF; El-Helw, AM, 2017
)
0.7
"To improve the solubility, dissolution and intestinal permeation thereby bioavailability of risperidone through a novel self-nanoemulsifying powder (SNEP) formulations."( Enhanced oral delivery of risperidone through a novel self-nanoemulsifying powder (SNEP) formulations: in-vitro and ex-vivo assessment.
Bakshi, V; Bandi, S; Sanka, K, 2016
)
0.95
"The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats."( Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone.
Gu, F; Ma, W; Meng, G; Wang, Y; Wu, C, 2016
)
0.91
" Risperidone bioavailability is 66% in extensive metabolizers and 82% in slow metabolizers."( Response surface optimization, Ex vivo and In vivo investigation of nasal spanlastics for bioavailability enhancement and brain targeting of risperidone.
Abdelrahman, FE; Elsayed, I; Elshafeey, AH; Gad, MK; Mohamed, MI, 2017
)
1.57
" It was hypothesized that cytochrome P450 (CYP)3A inhibition of the small intestine by voriconazole and P-glycoprotein (P-gp) inhibition of the small intestine by risperidone exerted a synergistic effect on the bioavailability of tacrolimus."( The possible clinical impact of risperidone on P-glycoprotein-mediated transport of tacrolimus: A case report and in vitro study.
Adachi, Y; Higashi, H; Nakamura, S; Nomura, K; Taguchi, M; Watanabe, N, 2018
)
0.96
" A combination of 6% menthol and 6% PG exhibited highest RIS in vitro penetration rate and showed a high efficiency in vivo, with a relative bioavailability of 131."( Delivery of risperidone from gels across porcine skin in vitro and in vivo in rabbits.
Chen, X; Li, F; Liang, W; Ning, Y; Yu, Z, 2018
)
0.86
" Presence of drug in the olfactory bulb, in turn, increases the drug bioavailability in the brain and reduces the drug degradation as well as wastage of the drug through` systemic clearance."( Nose-to-brain drug delivery: An update on clinical challenges and progress towards approval of anti-Alzheimer drugs.
Agrawal, M; Alexander, A; Antimisiaris, SG; Chougule, MB; Saraf, S; Shoyele, SA, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" The supramolecular adduct of RSP with RM-β-CD represents a valuable candidate for further research in developing new formulations with enhanced bioavailability and stability, and the results of this study allow a pertinent selection of three excipients that can be incorporated in solid dosage forms."( Risperidone/Randomly Methylated β-Cyclodextrin Inclusion Complex-Compatibility Study with Pharmaceutical Excipients.
Barvinschi, P; Cîrcioban, D; Ledeți, A; Ledeți, I; Miclău, M; Sbârcea, L; Suciu, O; Tănase, IM; Văruţ, RM; Vlase, G, 2021
)
2.06
" The rate of removal of LAIs is regulated by the slow rate of absorption in the site of injection and the phenomenon of their increased half-life is called flip-flop pharmacokinetics."( [Clinical pharmacokinetics and pharmaceutical forms of long-acting injectable antipsychotics].
Kyziridis, TC, 2022
)
0.72

Dosage Studied

The present study evaluated associations between risperidone metabolism and QT interval in 61 psychiatric patients. Patients entered the study on a stable SRI dosage and were randomized to EX/RP (N = 40), ris peridone, or placebo.

ExcerptRelevanceReference
" The dose-response curve of haloperidol remained virtually unchanged, apparently because of the potent dopamine-D2 antagonism associated with these doses which may block the potentiating effect of apomorphine."( Functional interaction between serotonin-S2 and dopamine-D2 neurotransmission as revealed by selective antagonism of hyper-reactivity to tryptamine and apomorphine.
Awouters, F; Janssen, PA; Megens, AA; Niemegeers, CJ, 1990
)
0.28
" This article discusses the relevant clinical considerations in switching neuroleptics and proposes practical guidelines on issues such as dosing and course of therapy with risperidone."( Clinical considerations in the use of risperidone.
Remington, GJ, 1993
)
0.75
" Dose-response analysis of receptor occupancy revealed risperidone demonstrated higher binding affinity for 5-HT2 than for D2, while the reverse was observed with haloperidol."( In vivo dopamine-D2 and serotonin-5-HT2 receptor binding study of risperidone and haloperidol.
Kido, H; Mori, H; Sakamoto, H; Shiba, K; Sumiyoshi, T; Suzuki, K; Urasaki, K; Yamaguchi, N; Yokogawa, K, 1994
)
0.77
" Risperidone was found to have a curvilinear dose-response curve with an optimum effect of 4 mg day on the negative, anxious/depressive and cognitive factors and with an optimum effect of 8 mg day on the positive and excited factors."( Changes in single symptoms and separate factors of the schizophrenic syndrome after treatment with risperidone or haloperidol.
Lindström, E; von Knorring, L, 1994
)
1.42
" Risperidone is 4-10 times less potent than haloperidol as a central D2 antagonist in rats and it differs from haloperidol by the following characteristics: predominant 5-HT2 antagonism; LSD antagonism; effects on sleep; smooth dose-response curves for D2 antagonism; synergism of combined 5-HT2/D2 antagonism; pronounced effects on amphetamine-induced oxygen consumption; increased social interaction; and pronounced effects on dopamine (DA) turnover."( Survey on the pharmacodynamics of the new antipsychotic risperidone.
Awouters, FH; Dugovic, C; Leysen, JE; Meert, TF; Megens, AA; Niemegeers, CJ; Schotte, A, 1994
)
1.45
" At a dosage of 4 to 8 mg/day, risperidone is comparable to 10 mg/day of haloperidol."( A risk-benefit assessment of risperidone in schizophrenia.
Curtis, VA; Kerwin, RW, 1995
)
0.87
" Recent research has underscored the need for optimum dosing strategies."( Antipsychotic medication in the treatment of schizophrenia.
Kane, JM, 1995
)
0.29
" In patients in whom low-to-moderate dosage is effective, there should be fewer and less severe adverse effects with risperidone than with haloperidol."( Risperidone: review and assessment of its role in the treatment of schizophrenia.
Cardoni, AA, 1995
)
1.94
" However, risperidone induced a U-shaped dose-response curve."( Differential effects of repeated administration of novel antipsychotic drugs on the activity of midbrain dopamine neurons in the rat.
Skarsfeldt, T, 1995
)
0.69
" Antipsychotic use in the elderly should be accompanied by careful conservative dosing and close patient monitoring."( Management of late-life psychosis.
Eastham, JH; Field, MG; Gierz, M; Harris, MJ; Jeste, DV; Lacro, JP, 1996
)
0.29
" The current clinical pharmacokinetic database for these atypical antipsychotics suggests that much can be learned with additional study that would be of value in individualizing their dosage regimens."( Pharmacokinetics of clozapine and risperidone: a review of recent literature.
Byerly, MJ; DeVane, CL, 1996
)
0.57
" In most cases, interactions are of clinical significance only when drug therapy is initiated or discontinued, or when major changes in dosage are made."( Drug interactions and antipsychotic therapy.
DeVane, CL,
)
0.13
" In vivo, risperidone showed the highest potency for 5-HT2A-receptor occupancy; To obtain the same extent of D2-receptor occupancy, a 19-times higher dosage was required."( In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used.
Bonaventure, P; Janssen, PF; Leysen, JE; Schotte, A, 1995
)
0.92
" Therapeutic gains can be accomplished with minimal dosing strategies, targeted drug therapy for medication-refusing patients, psychosocial interventions, and new drugs."( Maintenance therapy of persons with schizophrenia.
Carpenter, WT, 1996
)
0.29
"), all reduced the freezing behavior with U-shaped dose-response curves."( Evaluation of perospirone (SM-9018), a novel serotonin-2 and dopamine-2 receptor antagonist, and other antipsychotics in the conditioned fear stress-induced freezing behavior model in rats.
Ishibashi, T; Ishida-Tokuda, K; Morita, T; Nakamura, M; Ohno, Y; Sakamoto, H; Tojima, R; Wakabayashi, J, 1996
)
0.29
" In particular, they have the distinction of having achieved separation between the effective dosage and the dosage that causes extrapyramidal symptoms, which has significant implications for patient care."( Use of novel antipsychotic drugs.
Raleigh, F,
)
0.13
"Risperidone had a bell-shaped dose-response curve, with optimal therapeutic responses occurring at a daily dose of 8 mg."( [Risperidone in the treatment of chronic schizophrenia: multicenter study comparative to haloperidol].
Ayuso, JL; Chinchilla, A; Eguiluz, I; Fernández, A; González Pinto, A; Guimon, J; Gutiérrez, M; Herraiz, ML; López Ibor, JJ,
)
2.48
" Side-effects can be minimized by optimization of clinical strategies, including choice of appropriate drug, slow titration and dosage reduction."( Minimizing the non-extrapyramidal side-effects of antipsychotics.
Keks, NA, 1996
)
0.29
" Patients were treated with risperidone in two different dosage groups (3 mg and 8 mg) and haloperidol (10-20 mg) and compared with eight healthy control subjects."( Striatal dopamine-2 receptor occupancy in psychotic patients treated with risperidone.
Asenbaum, S; Brücke, T; Gössler, R; Kasper, S; Küfferle, B; Podreka, I; Tauscher, J; Topitz-Schratzberger, A; Vesely, C, 1996
)
0.82
" The patient developed postural hypotension and the risperidone dosage was held at 2 mg bid."( Fatal cardiac event following initiation of risperidone therapy.
Levenson, JW; Ravin, DS,
)
0.64
" On the maximum dose of risperidone (5-8 mg), 32% of the total sample developed mild akathisia or parkinsonism, both of which diminished with dosage reduction."( Extrapyramidal signs and clinical symptoms in first-episode schizophrenia: response to low-dose risperidone.
Good, KP; Honer, WG; Kopala, LC, 1997
)
0.82
" The results suggest the value of risperidone blood levels, consideration of reduction of initial recommended starting dosages, and a need to optimize risperidone dosage approaches individually to patients."( Risperidone dose and blood level variability: accumulation effects and interindividual and intraindividual variability in the nonresponder patient in the clinical practice setting.
Clark, L; Dabiri, L; Darby, JK; Elfand, L; Herbert, J; Pasta, DJ, 1997
)
2.02
" Gradual dosage titration over the first 3 days of treatment was well-tolerated in both groups."( Therapeutic equivalence of risperidone given once daily and twice daily in patients with schizophrenia. The Risperidone Study Group.
Nair, NP, 1998
)
0.6
" The aim of this study was to evaluate the degree of dopamine D2 receptor occupancy in relation to the neuroleptic dosage and to correlate the findings with the presence of extrapyramidal symptoms (EPS)."( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients.
Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998
)
0.3
" The degree of occupancy displayed an exponential dose-response relationship (r = -0."( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients.
Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998
)
0.3
"The findings suggest an exponential dose-response relationship between the daily dosage of risperidone and the dopamine D2 receptor occupancy."( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients.
Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998
)
0.52
" Proper dosing has emerged as a vital factor in the effective use of these newer drugs."( Risperidone and olanzapine: optimal dosing for efficacy and tolerability in patients with schizophrenia.
Kasper, S, 1998
)
1.74
" Dosing requirements for elderly patients tend to be much lower than those for younger adults."( Conventional vs. newer antipsychotics in elderly patients.
Harris, MJ; Jeste, DV; Lacro, J; Lohr, JB; Rockwell, E, 1999
)
0.3
" Thirty healthy subjects received a 1 mg oral dose of risperidone before and after venlafaxine dosing to steady state."( Effect of venlafaxine on the pharmacokinetics of risperidone.
Albano, D; Amchin, J; Klockowski, PM; Taylor, KP; Zarycranski, W, 1999
)
0.81
" The atypical properties of first-line atypical antipsychotics as well as clozapine are reviewed here, with clinical pearls and dosing tips for each based upon a consensus of information from both clinical trials and clinical practice."( Selecting an atypical antipsychotic by combining clinical experience with guidelines from clinical trials.
Stahl, SM, 1999
)
0.3
" The study objectives were to asses: 1) risperidone efficiency in psychotic and affective symptomatology and behavioral disturbances; 2) risperidone influence in the patient's performance, 3) dosage range at which efficiency is observed; and 4) safety in this group of patients."( [Risperidone in the treatment of psychotic, affective and behavioral symptoms associated to Alzheimer's disease].
Barcia, D; Giles, E; Herraiz, M; Moríñigo, A; Roca, M; Rodríguez, A,
)
1.31
" The decreased D(2)/D(3) receptor availability revealed an exponential dose-response relationship (r=-0."( In vivo effects of olanzapine on striatal dopamine D(2)/D(3) receptor binding in schizophrenic patients: an iodine-123 iodobenzamide single-photon emission tomography study.
Dresel, S; Hahn, K; Mager, T; Meisenzahl, E; Möller, HJ; Rossmüller, B; Tatsch, K, 1999
)
0.3
" Volunteers were dosed on 3 separate days with a minimum of 7 days interval between trial days."( Electroencephalographic and psychomotor effects of chlorpromazine and risperidone relative to placebo in normal healthy volunteers.
Ervine, CM; Hughes, AM; Lynch, P; Rhodes, J; Yates, RA, 1999
)
0.54
" However, 7 of the 12 volunteers dosed with risperidone 2 mg also reported drowsiness/lethargy which was of greater severity and duration than 5 of the 12 volunteers who reported somnolence following dosing with chlorpromazine 50 mg."( Electroencephalographic and psychomotor effects of chlorpromazine and risperidone relative to placebo in normal healthy volunteers.
Ervine, CM; Hughes, AM; Lynch, P; Rhodes, J; Yates, RA, 1999
)
0.8
" It also appears that rapid dosage increases for antimanic treatment can cause potentially severe side effects."( Tiagabine appears not to be efficacious in the treatment of acute mania.
Amann, B; Erfurth, A; Grunze, H; Marcuse, A; Normann, C; Walden, J, 1999
)
0.3
"Although the establishment of appropriate dosage ranges for antipsychotics has important ramifications for both short-term treatment and long-term therapeutic outcomes, difficulties in dosing persist."( A dose-outcome analysis of risperidone.
Bartko, JJ; Conley, RR; Kelly, DL; Love, RC, 1999
)
0.6
"Patients treated with doses less than the 6-mg/day initial dosing recommendations have better outcomes in terms of discharge."( A dose-outcome analysis of risperidone.
Bartko, JJ; Conley, RR; Kelly, DL; Love, RC, 1999
)
0.6
" Risperidone at a low dosage has been shown to be effective in controlling alterations of conduct and neuropsychology."( [Behavioral and neuropsychological phenotype of the 48XXYY syndrome: a longitudinal study of a case].
Blánquez-Rodríguez, MP; Díaz-Atienza, J,
)
1.04
" Adding risperidone to mirtazapine probably does not necessitate a change of the dosage of either drug, but more extensive investigations are needed."( Lack of drug interactions between mirtazapine and risperidone in psychiatric patients: a pilot study.
Doorschot, CH; Loonen, AJ; Oostelbos, MC; Sitsen, JM, 1999
)
0.99
" Surprisingly, there has been little relationship between the pivotal trials designed for FDA approval and current dosing strategies in broader clinical settings."( New antipsychotic medications: more than old wine and new bottles.
Schulz, SC, 2000
)
0.31
"The optimal risperidone dosing strategy for acute schizophrenia requires elucidation."( Risperidone in acutely exacerbated schizophrenia: dosing strategies and plasma levels.
Chang, WH; Chiu, WC; Chou, JC; Lane, HY; Su, MH; Wu, ST, 2000
)
2.13
" Cases admitted in the first semester received a significantly higher daily dosage of antipsychotic drugs and more frequently received anticholinergics."( Second-generation antipsychotics in the emergency care setting. A prospective naturalistic study.
Azzoni, A; Raja, M,
)
0.13
" Longitudinal study is required because this relationship may have implications for dosing strategies."( Subjective experience and striatal dopamine D(2) receptor occupancy in patients with schizophrenia stabilized by olanzapine or risperidone.
Booij, J; de Haan, L; Dingemans, PM; Lavalaye, J; Linszen, D, 2000
)
0.51
" A low initial dosage that is gradually adjusted upward is recommended."( Risperidone for control of agitation in dementia patients.
Falsetti, AE, 2000
)
1.75
" After 6 months of therapy, two patients developed facial dystonia: this disappeared after reducing dosage in one case, after drug discontinuation in the other."( Long-term risperidone for pervasive developmental disorder: efficacy, tolerability, and discontinuation.
Cianchetti, C; Di Martino, A; Muglia, P; Zuddas, A, 2000
)
0.71
" Risperidone, administered at a low dosage of 1 mg/day was associated with fewer extrapyramidal symptoms compared with haloperidol in elderly patients."( Risperidone: a review of its use in the management of the behavioural and psychological symptoms of dementia.
Bhana, N; Spencer, CM, 2000
)
2.66
" Therefore, risperidone was added and the dosage titrated up to the mean dose of 3 mg/day over 8 weeks."( Risperidone augmentation in refractory obsessive-compulsive disorder: an open-label study.
Cassano, GB; Dell'Osso, L; Gemignani, A; Marazziti, D; Milanfranchi, A; Pfanner, C; Presta, S, 2000
)
2.13
" Risperidone (4 mg/day) was added to her drug regimen and after increasing the dosage to 6 mg/day, she began to exhibit retrocollis."( Tardive dystonia provoked by concomitantly administered risperidone.
Hori, M; Hori, T; Kawanishi, Y; Shiraishi, H; Suzuki, T; Tachikawa, H, 2000
)
1.46
" A dose-response relationship was not consistently confirmed with any of the drug treatments."( The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.
Breier, A; David, SR; Kinon, BJ; Taylor, CC, 2000
)
0.6
" No consistent dose-response relationship was observed, and the time course and sex-dependency of the response differed between the 3 agents."( The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.
Breier, A; David, SR; Kinon, BJ; Taylor, CC, 2000
)
0.6
" In addition, psychiatrists' clinical preference of antipsychotic medication and dosage for patient subtypes were examined by the national survey."( Comparison of cost, dosage and clinical preference for risperidone and olanzapine.
Kaplan, Z; Lichtenberg, P; Rabinowitz, J, 2000
)
0.55
" Taking into account drug costs and dosage requirements, the average daily retail price was US $6."( Comparison of cost, dosage and clinical preference for risperidone and olanzapine.
Kaplan, Z; Lichtenberg, P; Rabinowitz, J, 2000
)
0.55
"In this open case series, the dose-response relationship of atypical antipsychotic augmentation in the treatment of obsessive compulsive disorder (OCD), and the dose-severity relationship in atypical anti psychotic-induced OC symptoms were examined."( Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.
Lapierre, Y; Ramasubbu, R; Ravindran, A, 2000
)
0.31
"Case 1: A linear dose-response relationship between increasing doses of olanzapine and improvement in OC symptoms was observed in an OCD patient resistant to 5-HT reuptake inhibitors."( Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.
Lapierre, Y; Ramasubbu, R; Ravindran, A, 2000
)
0.31
"Controlled studies are needed to investigate the dose-response or dose-severity relationships between OCD and atypical antipsychotics."( Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.
Lapierre, Y; Ramasubbu, R; Ravindran, A, 2000
)
0.31
"Evaluation of relationships between serum antipsychotic drug concentrations and clinical response may provide valuable information for rational dosage adjustments."( Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia.
Ancione, M; Avenoso, A; Facciolà, G; Madia, AG; Perucca, E; Salemi, M; Scordo, MG; Spina, E, 2001
)
0.6
" The design of the study was open and risperidone dosage could be adjusted individually according to clinical response."( Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia.
Ancione, M; Avenoso, A; Facciolà, G; Madia, AG; Perucca, E; Salemi, M; Scordo, MG; Spina, E, 2001
)
0.88
"These results suggest that aggressive dosing of risperidone is well tolerated in most psychiatric inpatients."( Safety and tolerability of a rapidly escalating dose-loading regimen for risperidone.
Feifel, D; Moutier, CY; Perry, W, 2000
)
0.79
" We performed this study to determine whether repeated dosing with risperidone reduced the subjective effects of experimentally administered cocaine."( Risperidone pre-treatment reduces the euphoric effects of experimentally administered cocaine.
Kalechstein, AD; Ling, W; Newton, TF; Tervo, K; Uslaner, J, 2001
)
1.99
" Adherence to a few guidelines for the design of dosage regimens should limit the effect of drug-drug interactions on patient status and contribute to optimal pharmacotherapy with risperidone."( An evaluation of risperidone drug interactions.
DeVane, CL; Nemeroff, CB, 2001
)
0.84
" Treatment with risperidone was initiated at a dosage of 2 mg daily, increased to the target dosage of 6 mg daily by day 3, and maintained at 6 mg daily until day 14."( Risperidone treatment of outpatients with schizophrenia: no evidence of sex differences in treatment response.
Dunbar, F; Labelle, A; Light, M, 2001
)
2.1
" The absence of sex differences in response to risperidone treatment may obviate the need for a sex-based differential dosing in schizophrenia management."( Risperidone treatment of outpatients with schizophrenia: no evidence of sex differences in treatment response.
Dunbar, F; Labelle, A; Light, M, 2001
)
2.01
" Fortunately, inpatient treatment was not necessary due to an increase of topiramate dosage and addition of risperidone and clonazepam."( Topiramate as a mood stabilizer.
Kasper, S; Letmaier, M; Schreinzer, D; Wolf, R, 2001
)
0.52
"We investigated the relationships between extrapyramidal symptoms (EPS) induced by risperidone, the dosage of risperidone and the combined plasma concentrations of risperidone plus its active metabolite, 9-hydroxyrisperidone, in 20 schizophrenic patients."( Possible relationship between combined plasma concentrations of risperidone plus 9-hydroxyrisperidone and extrapyramidal symptoms. Preliminary study.
Nakamura, J; Ueda, N; Yoshimura, R, 2001
)
0.77
" The trial was divided into two periods: eight weeks during which the dosage was escalated and then fixed, and six weeks during which variable dosages were used."( Effects of clozapine, olanzapine, risperidone, and haloperidol on hostility among patients with schizophrenia.
Chakos, M; Citrome, L; Cooper, TB; Czobor, P; Lieberman, JA; Lindenmayer, JP; McEvoy, J; Sheitman, B; Volavka, J, 2001
)
0.59
" The dosage of medication was increased in fixed increments during the first week of double-blind treatment and thereafter in a flexible dose regimen according to clinical response."( Risperidone in the treatment of tourette syndrome: a double-blind, placebo-controlled trial.
Annable, L; Chouinard, G; Dion, Y; Sandor, P, 2002
)
1.76
" Subjective impairment, as assessed with the subscale 'mental functioning', was significantly correlated with greater conventional neuroleptic dosage after controlling for psychopathology (P<0."( Relationship between neuroleptic dosage and subjective cognitive dysfunction in schizophrenic patients treated with either conventional or atypical neuroleptic medication.
Krausz, M; Moritz, S; Naber, D; Woodward, TS, 2002
)
0.31
" Among the group receiving novel antipsychotics, dosage was not related to satisfaction or burden of adverse effects."( Short report: comparison of patient satisfaction and burden of adverse effects with novel and conventional neuroleptics: a naturalistic study.
Bromet, EJ; Davidson, M; Rabinowitz, J, 2001
)
0.31
" Key assessments included the pharmacokinetics of quetiapine at steady state (area under the curve within a dosing interval [AUCtSS], maximum [CmaxSS], and minimum [CminSS] observed plasma concentrations, and oral clearance [Cl/f]), as well as the UKU Side Effect Rating Scale scores and safety evaluations."( The safety and pharmacokinetics of quetiapine when coadministered with haloperidol, risperidone, or thioridazine.
Alva, G; Arvanitis, LA; Bera, R; Potkin, SG; Thyrum, PT; Yeh, C, 2002
)
0.54
" This series covers four main areas of concern when treating the elderly: low-maintenance dosing minimising the likelihood of adverse events; successful treatment of patients previously uncontrolled and experiencing side effects with other antipsychotics; the possibility of intermittent rather than continuous treatment; and the benefits to patients, carers and the health services."( Risperidone in the treatment of psychoses in the elderly: a case report series.
Bullock, R; Libretto, S, 2002
)
1.76
" On the same day, the patient increased the risperidone dosage to 3 mg twice daily."( Extrapyramidal symptoms with ritonavir/indinavir plus risperidone.
Béïque, LC; Bowmer, MI; Kelly, DV, 2002
)
0.82
" The authors assessed eight patients on CBZ monotherapy (CBZ extended-release capsules) at a mean dosage of 625 +/- 253 mg/day (range, 400-1,200 mg/day) for at least 1 year."( Carbamazepine-risperidone interactions in patients with epilepsy.
Monaco, F; Mula, M,
)
0.49
" Twenty geriatric inpatients were evaluated in a naturalistic setting with regard to total daily risperidone dose and dosing interval."( Risperidone and 9-hydroxyrisperidone concentrations are not dependent on age or creatinine clearance among elderly subjects.
Kastango, KB; Kirshner, MA; Maxwell, RA; Mulsant, BH; Pollock, BG; Rosen, J; Sweet, RA, 2002
)
1.97
" Clinicians should attempt to treat patients with the lowest effective dosage of medication for the briefest therapeutic period to minimize the risks of adverse reactions."( Metoclopramide-induced supersensitivity psychosis.
Lu, ML; Pan, JJ; Shen, WW; Su, KP; Teng, HW, 2002
)
0.31
" Since the estimated risk of the extrapyramidal side effects varied with the dose, the present method of predicting the extrapyramidal side effects of risperidone may provide a basis for developing a rational dosing regimen for the drug."( Prediction and assessment of extrapyramidal side effects induced by risperidone based on dopamine D(2) receptor occupancy.
Fukuda, M; Iga, T; Nakashima, Y; Ohno, Y; Sato, H; Sawada, Y; Takayanagi, R; Tsuchiya, F; Yamada, Y, 2002
)
0.75
" D2 receptor blockade, a dose-response study was employed to determine whether low doses of these atypical antipsychotics would also upregulate hippocampal BDNF mRNA in the absence of significant D2 receptor blockade."( Differential regulation of hippocampal BDNF mRNA by typical and atypical antipsychotic administration.
Ashe, P; Chlan-Fourney, J; Juorio, AV; Li, XM; Nylen, K, 2002
)
0.31
"049) and a linear dose-response relation (P=0."( Cardiac arrest and ventricular arrhythmia in patients taking antipsychotic drugs: cohort study using administrative data.
Bilker, WB; Glasser, DB; Hennessy, S; Kimmel, SE; Knauss, JS; Margolis, DJ; Morrison, MF; Reynolds, RF; Strom, BL, 2002
)
0.31
") yielded an inverse dose-response relationship regarding LI."( Effects of fencamfamine on latent inhibition.
Alves, CR; Delucia, R; Silva, MT, 2002
)
0.31
" Divalproex was initiated at 15 mg/kg/day and titrated over 12 days to a maximum dosage of 30 mg/kg/day."( Effect of divalproex combined with olanzapine or risperidone in patients with an acute exacerbation of schizophrenia.
Casey, DE; Daniel, DG; Sommerville, KW; Tracy, KA; Wassef, AA; Wozniak, P, 2003
)
0.57
" Exposure to any previous antipsychotic and the longest maintained final dosage of risperidone were significantly different in the two groups."( A naturalistic study of risperidone treatment in seven affiliated university hospitals in Korea.
Bahk, WM; Chae, JH; Choi, BM; Go, HJ; Han, JH; Han, SI; Jun, TY; Kim, DJ; Kim, KS; Lee, C; Lee, CT; Pae, CU; Tsoh, J, 2003
)
0.85
" In this pilot study, 10 Hispanic and 8 non-Hispanic patients with schizophrenia were enrolled in a double-blind, parallel-group, inpatient risperidone dosing (daily versus twice daily) trial with the novel antipsychotic risperidone."( Risperidone in the treatment of Hispanic inpatients with schizophrenia: a pilot study.
Collazo, Y; Frackiewicz, EJ; Herrera, JM; Lawson, WB; Sramek, JJ, 2002
)
1.96
" ChAT staining in the caudate-putamen and hippocampus was also decreased after 90 days of RISP exposure, raising the possibility of deleterious cognitive effects after exposure to this dosage for longer periods of time."( Differential effects of haloperidol, risperidone, and clozapine exposure on cholinergic markers and spatial learning performance in rats.
Evans, DR; Hill, WD; Mahadik, SP; Parikh, V; Terry, AV; Waller, JL, 2003
)
0.59
" The results indicate that no clinically meaningful drug interactions occurred between risperidone 1 mg daily and donepezil 5 mg daily at steady state, and therefore no dosage adjustment is required when both drugs are combined with the dosage regimen studied."( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil.
Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003
)
0.77
" Forty-one inpatients with diagnosed schizophrenia (DSM-III-R) were assigned to 12 weeks of treatment with risperidone at a fixed dosage of 6 mg/d after a 2-week washout period."( The effect of risperidone treatment on superoxide dismutase in schizophrenia.
Cao, LY; Shen, YC; Wu, GY; Zhang, PY; Zhang, XY; Zhou, DF, 2003
)
0.89
" The patients were treated with conventional antipsychotics for seven days after admission and were then randomised to the treatment arms with risperidone (4 mg/day) or with olanzapine (10 mg/day) at a fixed dosage in the first week and thereafter in flexible dosages for the remaining seven weeks."( Measurement of simple reaction time in antipsychotic treatment of patients with schizophrenia.
Kores Plesnicar, B; Krajnc, I; Tomori, M; Zalar, B, 2003
)
0.52
" At a higher dosage (0."( The atypical antipsychotics risperidone, clozapine and olanzapine differ regarding their sedative potency in rats.
Ahnaou, A; Drinkenburg, WH; Megens, AA, 2003
)
0.61
" However, no correlation between prolactin levels and dosage could be found."( [Plasma prolactin level and incidence of adverse endocrinologic effects during therapy with atypical neuroleptics].
Fric, M; Laux, G, 2003
)
0.32
" The diagnosis of rhabdomyolysis was confirmed by myoglobinemia dosage and ortholuidine test."( [Rhabdomyolysis associated with respiratory infection in chronic psychiatric patients during neuroleptic treatment].
Busiello, L; Cascella, M; De Robertis, E; Di Domenico, MG; Palmese, S; Pezza, M, 2003
)
0.32
"We tested a hypothesis that fine-tuning risperidone dosage to relieve side effects still yields efficacy."( Fine-tuning risperidone dosage for acutely exacerbated schizophrenia: clinical determinants.
Chang, WH; Chang, YC; Chiu, CC; Lane, HY; Lee, SH; Lin, CY, 2004
)
0.97
"These findings suggest that dosage adjustment to diminish side effects does not compromise risperidone response and that disorganized patients and perhaps patients with longer illness duration are prone to receive larger doses."( Fine-tuning risperidone dosage for acutely exacerbated schizophrenia: clinical determinants.
Chang, WH; Chang, YC; Chiu, CC; Lane, HY; Lee, SH; Lin, CY, 2004
)
0.92
" Atypical antipsychotics offer better safety and efficacy, while depot formulations of conventional antipsychotics provide more reliable drug delivery, reduced differences in peak and trough plasma levels of drug, and greater dosing precision."( Comparison of the effects of different routes of antipsychotic administration on pharmacokinetics and pharmacodynamics.
Ereshefsky, L; Mascarenas, CA, 2003
)
0.32
"Although the kinetic profile of antipsychotics at dopamine D2 receptor sites has been suggested to be important for antipsychotic action and dosing schedule, the kinetic profiles of the respective antipsychotic drugs in the brain have not yet been clearly defined."( Estimation of the time-course of dopamine D2 receptor occupancy in living human brain from plasma pharmacokinetics of antipsychotics.
Ichimiya, T; Ikoma, Y; Inoue, M; Maeda, J; Okubo, Y; Sudo, Y; Suhara, T; Takano, A; Yasuno, F, 2004
)
0.32
" Unfortunately, this type of drugs cannot block the D2 receptors only in the mesolimbic dopaminergic pathway (which mediates their therapeutic effects), because of their non-selective D2 receptor blockage in both the mesolimbic and striatal regions, and the consequent appearance of side effects related to striatal interaction in the same dosage range as is needed for the therapeutical effects."( New antipsychotics and schizophrenia: a review on efficacy and side effects.
Berardi, D; De Ronchi, D; Lorenzi, C; Serretti, A, 2004
)
0.32
" This may provide valuable information for rational dosage titration."( Correlation between scores on Continuous Performance Test and plasma concentration for schizophrenic patients on risperidone.
Chang, JW; Chen, PS; Liao, YC; Su, SF; Yang, YK; Yeh, TL, 2004
)
0.53
"These data indicate that the dosage of these medications, found to be effective in the treatment of schizophrenia, reduces DA stimulation of D2 receptors to levels slightly lower than those found in unmedicated healthy subjects."( Occupancy of dopamine D2 receptors by the atypical antipsychotic drugs risperidone and olanzapine: theoretical implications.
Abi-Dargham, A; Cangiano, C; Frankle, WG; Gil, R; Gorman, JM; Hackett, E; Kochan, LD; Laruelle, M; Mawlawi, O; Slifstein, M; Zea-Ponce, Y; Zhu, Z, 2004
)
0.56
" The most common dosage was 6 mg/d."( Treatment outcome in patients with chronic schizophrenia during long-term administration with risperidone.
Libretto, SE; Reveley, MA, 2004
)
0.54
" The failure to improve without an adequate dosage of LT4 suggests that hypothyroidism was probably an aggravating factor."( Coexistent hypothyroidism, psychosis, and severe obsessions in an adolescent: a 10-year follow-up.
Alshari, MG; Bhatara, A; Bhatara, V; McMillin, JM; Warhol, P, 2004
)
0.32
" The two major degradation products in the dosage forms were also characterized as 9-hydroxy risperidone and N-oxide of risperidone, after enrichment through preparative LC, by LC-MS/MS and HPLC."( Identification and characterization of major degradation products of risperidone in bulk drug and pharmaceutical dosage forms.
Joseph, TJ; Krishna Reddy, KV; Murthy, AS; Subbaiah, G; Tomar, RS; Yadav, DV, 2004
)
0.78
" However, the results suggest that quetiapine, when given within the recommended dosage range, has a benign EPS profile, with potentially greater tolerability and comparable efficacy to risperidone in older outpatients with psychotic disorders."( A comparison of extrapyramidal symptoms in older outpatients treated with quetiapine or risperidone.
Mintzer, JE; Mullen, JA; Sweitzer, DE, 2004
)
0.74
"The pharmacology, pharmaceutics, clinical efficacy, adverse effects, cost, and dosage and administration of long-acting risperidone injection are reviewed."( Long-acting risperidone injection.
Conley, RJ; Love, RC, 2004
)
0.91
"These results suggest that once-daily dosing of 5 mg donepezil HCl does not alter the PK of risperidone in patients with schizophrenia."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.8
" It is dosed at 25-50 mg every 2 weeks."( Long-acting injectable risperidone.
Ehret, MJ; Fuller, MA, 2004
)
0.63
"Ten patients stable for at least 10 days on monotherapy with oral risperidone 2 mg to 4 mg taken once daily were switched for 7 days to an equivalent dosage of orally disintegrating risperidone."( Acceptability and disintegration rates of orally disintegrating risperidone tablets in patients with schizophrenia or schizoaffective disorder.
Binder, C; Chue, P; Welch, R, 2004
)
0.8
" The failure to confirm previous claims of greater improvement on either risperidone or olanzapine in patients with a first episode of psychosis may be the result of methodological bias introduced by unequal dosing between the two drugs or the use of chronically ill and treatment-refractory patients in previous studies."( A comparison of two novel antipsychotics in first episode non-affective psychosis: one-year outcome on symptoms, motor side effects and cognition.
Haricharan, R; Malla, A; Manchanda, R; Norman, R; Scholten, D; Takhar, J; Townsend, L, 2004
)
0.56
" The duration and dosage of previous clozapine monotherapy was adequate for 16 patients."( Case studies of adjunctive agents in clozapine-resistant schizophrenic patients.
Christodoulou, GN; Ferentinos, PP; Havaki-Kontaxaki, BJ; Kontaxakis, VP; Paplos, KG; Roukas, DK,
)
0.13
" These results suggest that a low dosage of levomepromazine, use as a sedative adjuvant to risperidone treatment, have no statistically significant effect on the trough plasma concentrations of risperidone."( Little effects of low dosage of levomepromazine on plasma risperidone levels.
Goto, M; Kaji, K; Kakihara, S; Nakamura, J; Shinkai, K; Ueda, N; Yamada, Y; Yoshimura, R, 2005
)
0.79
" Initially, active moiety risperidone concentrations increased linearly with prescribed dosage increases."( Interpreting serum risperidone concentrations.
Boerth, JM; Caley, CF; Goethe, JW, 2005
)
0.96
" Mice were acclimated to individual housing, given ad libitum access to chow and water, dosed with placebo peanut butter pills for 1 week, and then dosed daily with AAPD-laced peanut butter pills for 4 weeks."( Antipsychotic drug-induced weight gain: development of an animal model.
Allison, DB; Casey, DE; Cope, MB; Fernández, JR; Geary, N; Nagy, TR, 2005
)
0.33
" For most patients, the initial dosage should be 25 mg every 2 weeks, and oral administration should continue for the first 3 weeks after initial injection."( Clinical review of a long-acting, injectable formulation of risperidone.
Knox, ED; Stimmel, GL, 2004
)
0.57
"OXC, at a dosage of 900-1,200 mg/day, was administered for 5 consecutive weeks to 25 outpatients, 10 men and 15 women, aged 25 to 64 years, with bipolar or schizoaffective disorder."( Plasma concentrations of risperidone and olanzapine during coadministration with oxcarbazepine.
Cacciola, M; D'Arrigo, C; La Torre, D; Migliardi, G; Pacetti, M; Rosaria Muscatello, M; Spina, E; Zoccali, R, 2005
)
0.63
"In treating patients with psychosis, practicing clinicians use various dosing strategies of antipsychotic medications, including risperidone."( Risperidone dosing pattern and clinical outcome in psychosis: an analysis of 1713 cases.
Choi, SK; Hong, JP; Joo, YH; Kim, CY; Lee, GH; Shin, YW, 2005
)
1.98
" Cluster analysis was performed to identify homogeneous dosing patterns among the heterogeneous total population."( Risperidone dosing pattern and clinical outcome in psychosis: an analysis of 1713 cases.
Choi, SK; Hong, JP; Joo, YH; Kim, CY; Lee, GH; Shin, YW, 2005
)
1.77
"Our results indicate that the current consensus regarding risperidone dosing is appropriate for clinical practice, whereas a slower titration schedule does not guarantee a better clinical outcome, thus emphasizing the need for appropriate early titration."( Risperidone dosing pattern and clinical outcome in psychosis: an analysis of 1713 cases.
Choi, SK; Hong, JP; Joo, YH; Kim, CY; Lee, GH; Shin, YW, 2005
)
2.02
" When OCSs appear with clozapine, dosage can be reduced and a serotonin reuptake inhibitor treatment added."( [Obsessive-compulsive symptoms treatment in: schizophrenia].
Dardennes, R; Faucher, S; Ghaëm, O; Guelfi, JD, 2005
)
0.33
" It is dosed at 25-50 mg every 2 weeks."( [The first long-acting atypical antipsychotic: new milestone in the treatment of schizophrenia].
Faludi, G, 2005
)
0.33
"For many antipsychotics, dose-response relationships remain poorly understood."( Establishing a dose-response relationship for oral risperidone in relapsed schizophrenia.
Ezewuzie, N; Taylor, D, 2006
)
0.59
" Patients were initiated with quetiapine to 400 mg/day over 7 days, and then flexibly dosed (300-750 mg/day) for 11 weeks."( Efficacy and tolerability of quetiapine in patients with schizophrenia who switched from haloperidol, olanzapine or risperidone.
Altman, C; de Nayer, A; Jones, AM; Larmo, I; Lindenbauer, B; Platz, T; Rittmannsberger, H; Windhager, E, 2005
)
0.54
" Clozapine dosage and laboratory results were recorded at 12-month intervals."( Clozapine, diabetes mellitus, hyperlipidemia, and cardiovascular risks and mortality: results of a 10-year naturalistic study.
Borba, CP; Cather, C; Copeland, PM; Evins, AE; Freudenreich, O; Goff, DC; Hayden, DL; Henderson, DC; Louie, PM; Nguyen, DD, 2005
)
0.33
" Among parameters analyzed were chlorpromazine equivalent dosage of antipsychotic, metabolic parameters, body mass index (BMI), level of concurrent medications, and concomitant dietary restrictions."( Metabolic effects associated with atypical antipsychotic treatment in the developmentally disabled.
Ball, MP; Bodfish, JW; Heeth, WL; Mahorney, SL; McKee, JR, 2005
)
0.33
" Ninety-four outpatients who had been on a stable drug dosage were evaluated (clozapine group: n=57, mean dose=254."( Subjective response to clozapine and risperidone treatment in outpatients with schizophrenia.
Ahn, YM; Kim, JH; Kim, SY; Kim, YS, 2006
)
0.61
" The psychiatrists agreed with the patients in deciding to continue treatment with peroral liquid risperidone (83%) because of better tolerability in 88% patients, better cooperation in 82% and more precise dosage in 80% patients."( Risperidone liquid in psychotic disorders--efficacy and attitudes.
Damjanović, A; Jasović-Gasić, M; Marić, N, 2005
)
1.99
" Treatment was naturalistic, and dosing was based on the discretion of the treating physician."( Olanzapine versus risperidone in newly admitted acutely ill psychotic patients.
Cook, A; Kraus, JE; Lieberman, JA; Reviere, R; Sheitman, BB, 2005
)
0.66
" Results of the sensitivity analysis confirmed that the results were robust to a wide variation of different input variables (effectiveness, dosing distribution, patient status according to healthcare system)."( Long-acting risperidone compared with oral olanzapine and haloperidol depot in schizophrenia: a Belgian cost-effectiveness analysis.
Caleo, S; De Graeve, D; Lecompte, D; Mehnert, A; Miadi-Fargier, H; Mosqueda, GJ; Peuskens, J; Smet, A, 2005
)
0.71
"6%) with a higher mean daily dosage in the public care setting."( [Neuroleptic drug utilization among schizophrenic outpatients].
Blin, P; Cialdella, P; Gérard, A; Hanssens, L; Olié, JP; Petitjean, F; Sechter, D; Westerloppe, J, 2005
)
0.33
"Clinical studies have consistently demonstrated that long-acting risperidone, available in dosage strengths of 25, 37."( Clinical experience and management considerations with long-acting risperidone.
Parellada, E, 2006
)
0.81
" Larger studies regarding the PK/PD relationship may be required to develop a reasonable clinical dosage regimen for Chinese female patients."( Multiple dose pharmacokinetics of risperidone and 9-hydroxyrisperidone in Chinese female patients with schizophrenia.
Deng, CY; Li, HD; Li, WB; Li, X; Lin, QX; Lin, SG; Peng, HY; Su, FL; Wang, CY; Wang, F; Yang, M; Yu, XY; Zhou, ZL; Zhu, RH, 2006
)
0.61
"Thirty patients with a primary diagnosis of an anxiety disorder-panic disorder (PD), social anxiety disorder (SAD), or generalized anxiety disorder (GAD)-refractory to initial pharmacotherapy with an adequate (or maximally tolerated) antidepressant and/or benzodiazepine trial of at least 8 weeks' duration prior to study initiation received open-label augmentation with flexibly dosed risperidone for 8 weeks."( An open-label trial of risperidone augmentation for refractory anxiety disorders.
Christian, KM; Fischmann, D; Hoge, EA; Kinrys, G; Pollack, MH; Simon, NM; Worthington, JJ, 2006
)
0.81
" We used the Dosage Record Treatment Emergent Symptom Scale (DOTES) in a supplemented version to measure the presence and severity of side effects."( Clinical drug monitoring in child and adolescent psychiatry: side effects of atypical neuroleptics.
Fleischhaker, C; Heiser, P; Hennighausen, K; Herpertz-Dahlmann, B; Holtkamp, K; Mehler-Wex, C; Rauh, R; Remschmidt, H; Schulz, E; Warnke, A, 2006
)
0.33
" Dosage could be modified during the study according to clinical criteria."( Improvement in social functioning in outpatients with schizophrenia with prominent negative symptoms treated with olanzapine or risperidone in a 1 year randomized, open-label trial.
Alvarez, E; Bousoño, M; Ciudad, A; Gómez, JC; Olivares, JM, 2006
)
0.54
" Mean CLZ dosage during the combined treatment was 474."( Risperidone augmentation of clozapine: a critical review.
Christodoulou, GN; Ferentinos, PP; Havaki-Kontaxaki, BJ; Kontaxakis, VP; Paplos, KG; Pappa, DA, 2006
)
1.78
" Lamotrigine was titrated up to a final dosage of 200 mg/day over 8 weeks, and pharmacokinetic assessments were made at baseline and during treatment weeks 6 and 10, at lamotrigine dosages of 100 and 200 mg/day respectively."( Effect of adjunctive lamotrigine treatment on the plasma concentrations of clozapine, risperidone and olanzapine in patients with schizophrenia or bipolar disorder.
D'Amico, G; D'Arrigo, C; Micò, U; Migliardi, G; Muscatello, MR; Perucca, E; Santoro, V; Spina, E, 2006
)
0.56
" Dosing was determined by clinical judgment."( Switching to olanzapine after unsuccessful treatment with risperidone during the first episode of schizophrenia: an open-label trial.
Higuchi, H; Ishigooka, J; Kamata, M; Takahashi, H; Yoshida, K, 2006
)
0.58
" The mean dosage of olanzapine was 15."( Switching to olanzapine after unsuccessful treatment with risperidone during the first episode of schizophrenia: an open-label trial.
Higuchi, H; Ishigooka, J; Kamata, M; Takahashi, H; Yoshida, K, 2006
)
0.58
" Failure in switching to monotherapy was associated with higher dosage of antipsychotics at baseline."( Effects of switching from conventional antipsychotics to risperidone in Japanese patients with chronic schizophrenia.
Kunugi, H; Murray, RM; Nakanishi, S; Nojima, S; Ogawa, T; Takahashi, T, 2006
)
0.58
" Therefore, if flupentixol's efficacy on negative symptoms is based on its interaction with 5-HT(2A) and/or D(1) receptors, it should be highly dependent on serum concentration and thus on dosage and metabolism."( Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol.
Bares, R; Bartels, M; Beneke, M; Glaser, T; Machulla, HJ; Noda, S; Reimold, M; Schaefer, JE; Solbach, C; Wormstall, H, 2007
)
0.54
" Data were obtained from 407 patients enrolled in four Phase 1 (serial blood sampling) and three Phase 3 trials (sparse sampling), representing dosage regimens ranging from 4 mg single dose to flexible 1-6 mg once daily."( Population pharmacokinetics of risperidone and 9-hydroxyrisperidone in patients with acute episodes associated with bipolar I disorder.
Ludwig, EA; Piotrovsky, V; Vermeulen, A, 2007
)
0.63
", dosage adjustments, behavioral or psychosocial interventions) before switching medications."( Effectiveness of switching antipsychotic medications.
Covell, NH; Davis, SM; Essock, SM; Lieberman, JA; Rosenheck, RA; Stroup, TS, 2006
)
0.33
" While the mechanism is unclear, treatment of steroid psychosis involves dosage reduction or discontinuation of prednisone."( Steroid-induced psychosis in an adolescent: treatment and prophylaxis with risperidone.
Bilge, I; Hergüner, S; Tüzün, DU; Yavuz Yilmaz, A,
)
0.36
" In total, 568 patients (60% men, mean age 36-40 years) were included and grouped according to pre-trial oral risperidone dosage (56% < or =4 mg; 30% >4 to < or =6 mg; 14% >6 mg)."( Efficacy and safety of risperidone long-acting injectable in stable psychotic patients previously treated with oral risperidone.
Kahn, JP; Medori, R; Sacchetti, E; Schmauss, M, 2007
)
0.86
" During the course of treatment, the risperidone dosage was increased to a total daily dose of 4 mg."( Risperidone for the treatment of fecal smearing in a developmentally disabled adult.
Brahm, NC; Brown, RC; Farmer, KC, 2007
)
2.06
" Most clinicians (89-100%) found the guidebook useful, and were adherent to key aspects of appropriate treatment use including concomitant oral risperidone use and injection and dosing parameters for long-acting risperidone."( Evaluation of a treatment manual for risperidone long-acting injectable.
Docherty, JP; Jones, R; Kujawa, M; Lasser, RA; Turkoz, I, 2007
)
0.81
"Thirty-eight outpatients on long-term treatment with clozapine (250-500 mg/d, n = 10), olanzapine (10-20 mg/d, n = 12), risperidone (3-6 mg/d, n = 9), or quetiapine (200-600 mg/d, n = 7) received adjunctive topiramate, gradually titrated up to a final dosage of 200 mg/d for 6 weeks."( Effect of topiramate on plasma concentrations of clozapine, olanzapine, risperidone, and quetiapine in patients with psychotic disorders.
Bruno, A; Cacciola, M; Campolo, D; Cortese, L; D'Arrigo, C; Migliardi, G; Santoro, V; Spina, E,
)
0.57
"To evaluate the clinical efficacy of modified Daotan Decoction (DD) combining low dosage of risperidone in treating chronic schizophrenia patients of phlegm-dampness blockage type, and compare with patients treated with risperidone alone."( [Clinical observation on effect of modified Daotan Decoction combined with small dose risperidone in treating chronic schizophrenia].
Liu, JL; Ma, L; Wang, Y, 2007
)
0.78
"The treatment of DD combined with low dosage of risperidone is effective on chronic schizophrenia and shows less adverse reaction."( [Clinical observation on effect of modified Daotan Decoction combined with small dose risperidone in treating chronic schizophrenia].
Liu, JL; Ma, L; Wang, Y, 2007
)
0.82
"There is no evidence that haloperidol in low dosage has different efficacy in comparison with the atypical antipsychotics olanzapine and risperidone in the management of delirium or has a greater frequency of adverse drug effects than these drugs."( Antipsychotics for delirium.
Britton, AM; Lonergan, E; Luxenberg, J; Wyller, T, 2007
)
0.54
" Patients were switched from their previous dosage of compressed tablets (0."( Do formulation switches exacerbate existing medical illness? Results of an open-label transition to orally disintegrating risperidone tablets.
Binder, CE; Chue, P; Prinzo, RS, 2007
)
0.55
" Both formulations contained 1 mg risperidone per dosing unit."( Lack of bioequivalence between generic risperidone oral solution and originator risperidone tablets.
Piniella, PM; Relleke, M; van Os, S, 2007
)
0.89
" The most common dosage of RLAI used at endpoint was 25 mg every 14 days (60%)."( Long-term safety and efficacy of long-acting risperidone in elderly psychotic patients.
Glue, P; Kissling, W; Medori, R; Simpson, S, 2007
)
0.6
" During the subsequent week, rates of problem behavior typically decreased without reinstating the prior dosage of medication."( Temporary increases in problem behavior and sleep disruption following decreases in medication: a descriptive analysis of conditional rates.
Dornbusch, K; Rapp, JT; Swanson, G, 2007
)
0.34
" After 4 weeks, the dosage of risperidone was increased to 2 mg/d in some cases."( Risperidone for treatment-refractory major depressive disorder: a randomized trial.
Canuso, CM; Gharabawi-Garibaldi, GM; Kosik-Gonzalez, C; Kujawa, MJ; Mahmoud, RA; Pandina, GJ; Turkoz, I, 2007
)
2.07
" Future prospective studies are necessary to clarify whether the prescribed dosage should be different in young and older patients."( Age and gender effects on olanzapine and risperidone plasma concentrations in children and adolescents.
Aichhorn, W; Hinterhuber, H; Kemmler, G; Marksteiner, J; Stuppaeck, C; Walch, T; Zernig, G, 2007
)
0.61
"The trial was a prospective, open-label, single-center one with a flexible dosing of SGAs."( Differences in the effect of second-generation antipsychotics on prolactinaemia: six weeks open-label trial in female in-patients.
Cejpková, A; Rodáková, I; Svestka, J; Synek, O; Tomanová, J, 2007
)
0.34
" We treated catatonic symptoms with drugs within the upper limit of dosage and electroconvulsive therapy (ECT) to determine the maximal response."( Maximal response to electroconvulsive therapy for the treatment of catatonic symptoms.
Arai, H; Hatta, K; Miyakawa, K; Nakamura, H; Ota, T; Usui, C, 2007
)
0.34
" In treated patients, no correlation was found between NSS and daily dosage or duration of exposure of neuroleptic treatment, extrapyramidal symptoms and level of CGI-improvement."( [Neuroleptic treatment and neurological soft signs in schizophrenic patients].
Chebel, S; Gaha, L; Mandhouj, O; Mechri, A; Slama, H,
)
0.13
" Dosage adjustments were performed as clinically necessary."( Long-term remission in schizophrenia and related psychoses with long-acting risperidone: results obtained in an open-label study with an observation period of 18 months.
Kissling, W; Llorca, PM; Lloyd, K; Medori, R; Sacchetti, E, 2008
)
0.58
" Paliperidone's advanced-generation osmotic release delivery system allows for the avoidance of dosage adjustment when initiating therapy and may decrease the frequency of antido-paminergic effects that would occur with an immediate-release formulation."( Paliperidone for schizophrenia.
Deyo, Z; Dolder, C; Nelson, M, 2008
)
0.35
" Haloperidol (mean dosage 4,1 mg daily) was administered to 17 patients and trifluoperazine (mean dosage 7,1 mg daily) to 14 patients."( [Prescription of traditional neuroleptics in the remission period for schizophrenic patients with excess of body mass caused by atypical antipsychotics].
Danilov, DS; Tiul'pin, IuG, 2007
)
0.34
"Patient compliance is better with formulations that require less frequent dosing than with formulations that require more frequent dosing."( Estimation of the impact of noncompliance on pharmacokinetics: an analysis of the influence of dosing regimens.
Hughes, DA, 2008
)
0.35
" Once-daily dosing of oxybutynin is no better at maintaining pharmacokinetic exposure than twice-daily dosing at half strength."( Estimation of the impact of noncompliance on pharmacokinetics: an analysis of the influence of dosing regimens.
Hughes, DA, 2008
)
0.35
"To determine whether, for oxybutynin and risperidone, drug exposure is better with less frequent dosing regimens than with regimens that require more frequent dosing."( Estimation of the impact of noncompliance on pharmacokinetics: an analysis of the influence of dosing regimens.
Hughes, DA, 2008
)
0.61
" Neuroleptic drugs can produce severe side effects and need careful dosage and monitoring."( [Delusion in the critical patient].
Palencia-Herrejón, E; Romera, MA; Silva, JA, 2008
)
0.35
"Personalized prescription is described even in lay journals, but there has been no attempt to propose personalizing dosing for any specific psychiatric drug."( A preliminary attempt to personalize risperidone dosing using drug-drug interactions and genetics: part I.
Cozza, KL; de Leon, J; Sandson, NB,
)
0.4
"Any attempt to develop personalized dosing needs to be anchored in our understanding of the pharmacological response of each drug in each person's environment, particularly drug-drug interactions (DDIs) and how genetic make-up influences drug response."( A preliminary attempt to personalize risperidone dosing using drug-drug interactions and genetics: part I.
Cozza, KL; de Leon, J; Sandson, NB,
)
0.4
"Age, body mass index (BMI), illness duration, drug type and dosage were considered as covariates when analysing association with genetic variants as they were associated with baseline or final BPRS and CGI scores and/or extrapyramidal side effects."( Acute antipyschotic efficacy and side effects in schizophrenia: association with serotonin transporter promoter genotypes.
Dolzan, V; Kastelic, M; Koprivsek, J; Mandelli, L; Plesnicar, BK; Serretti, A, 2008
)
0.35
" However, dosing of long-acting antipsychotics is frequently extended in clinical practice, and a recent clinical trial has lent support to monthly dosing of long-acting risperidone."( Monthly administration of long-acting injectable risperidone and striatal dopamine D2 receptor occupancy for the management of schizophrenia.
Kapur, S; Labelle, A; Mamo, DC; Mann, SW; Mannaert, EJ; Remington, G; Shammi, C; Uchida, H, 2008
)
0.79
" This work suggests a possibility that sustained D(2) occupancy at or above the accepted threshold with acute clinical response may not be necessary to maintain response, a hypothesis with important clinical implications as we consider antipsychotic dosing and future antipsychotic development."( Monthly administration of long-acting injectable risperidone and striatal dopamine D2 receptor occupancy for the management of schizophrenia.
Kapur, S; Labelle, A; Mamo, DC; Mann, SW; Mannaert, EJ; Remington, G; Shammi, C; Uchida, H, 2008
)
0.6
"Three rapid, simple, reproducible and sensitive extractive colorimetric methods (A--C) for assaying dothiepin hydrochloride (I) and risperidone (II) in bulk sample and in dosage forms were investigated."( Extractive colorimetric method for the determination of dothiepin hydrochloride and risperidone in pure and in dosage forms.
Hassan, Wel-S, 2008
)
0.77
" Deficits were unrelated to drug dosage and clinical ratings."( Effects of second-generation antipsychotic medication on smooth pursuit performance in antipsychotic-naive schizophrenia.
Harris, MS; Keshavan, MS; Lencer, R; Reilly, JL; Sprenger, A; Sweeney, JA, 2008
)
0.35
" Treatment was at the psychiatrist's discretion, including flexible dosing and use of concomitant therapies and medications, with assessments at 0, 3, 6, 12, 18, 24, 30, and 36 months."( Long-term antipsychotic monotherapy for schizophrenia: disease burden and comparative outcomes for patients treated with olanzapine, quetiapine, risperidone, or haloperidol monotherapy in a pan-continental observational study.
Anders, M; Dossenbach, M; Irimia, V; Kotler, M; Logozar-Perkovic, D; Lowry, AJ; Pecenak, J; Peciukaitiene, D; Smulevich, AB; Szulc, A; Treuer, T; West, TM, 2008
)
0.55
" Divalproex ER was initiated on day 1 at 20 mg/kg per day q AM and was titrated to clinical effect on days 3, 7, and 10, not to exceed a maximum dosage of 35 mg/kg per day."( Divalproex ER combined with olanzapine or risperidone for treatment of acute exacerbations of schizophrenia.
Abi-Saab, W; Baker, J; Casey, DE; Daniel, DG; Greco, N; Kane, JM; Redden, L; Saltarelli, M; Tamminga, C; Tran-Johnson, T; Wozniak, P, 2009
)
0.62
"To compare efficacy and safety of two dosing regimens of risperidone."( Efficacy, safety and tolerability of two dosing regimens in adolescent schizophrenia: double-blind study.
Augustyns, I; Eerdekens, M; Haas, M; Kushner, S; Kusumakar, V; Pandina, G; Quiroz, J; Singer, J, 2009
)
0.6
" This finding has important implications for dosing of antipsychotics in older patients with schizophrenia."( Sensitivity of older patients to antipsychotic motor side effects: a PET study examining potential mechanisms.
Graff-Guerrero, A; Kapur, S; Mamo, DC; Mulsant, BH; Pollock, BG; Uchida, H, 2009
)
0.35
" The preferred switch strategy was immediate discontinuation, and the preferred dosing regimen was 120 mg/day."( Efficacy and tolerability of switching to ziprasidone from olanzapine, risperidone or haloperidol: an international, multicenter study.
Akkaya, C; Alptekin, K; Brook, S; Danaci, AE; El Tallawy, H; Hafez, J; Karayal, ON; Lowe, W; Tzebelikos, E; Ucok, A, 2009
)
0.59
"Although clozapine has been shown to be the treatment of choice in people with schizophrenia that are resistant to treatment, one third to two thirds of people still have persistent positive symptoms despite clozapine monotherapy of adequate dosage and duration."( Clozapine combined with different antipsychotic drugs for treatment resistant schizophrenia.
Barbui, C; Boso, M; Cipriani, A, 2009
)
0.35
" Following oral dosing of antipsychotics, peaks and troughs in plasma drug concentrations may be mirrored by fluctuations in D(2)-receptor occupancy."( A comparison of continuous subcutaneous paliperidone infusion and repeated subcutaneous injection of risperidone free-base in rats.
Casu, G; Deriu, A; Lazzari, P; Marchese, G; Pani, L; Peddio, G; Pira, M; Pisu, C; Pittau, B; Portesani, F; Spada, GP, 2010
)
0.58
"This review of the available literature aimed to explore a possible relationship between dosage of second-generation antipsychotics (SGAs) and the degree of metabolic side effects."( Are weight gain and metabolic side effects of atypical antipsychotics dose dependent? A literature review.
De Hert, M; Simon, V; van Winkel, R, 2009
)
0.35
"Preliminary evidence suggests a dose-response relationship between clozapine and olanzapine serum concentrations and metabolic outcomes, although the association between administered daily dose and metabolic outcomes is not clear."( Are weight gain and metabolic side effects of atypical antipsychotics dose dependent? A literature review.
De Hert, M; Simon, V; van Winkel, R, 2009
)
0.35
"3 times higher after controlling for dosing potency)."( Short- and long-term effects on prolactin of risperidone and olanzapine treatments in children and adolescents.
D'Arrigo, C; de Leon, J; Diaz, FJ; Gagliano, A; Germanò, E; Migliardi, G; Siracusano, R; Spina, E, 2009
)
0.61
"The existence of such resin complex may provide taste-masking properties to the dosage forms."( Complexation between risperidone and amberlite resin by various methods of preparation and binding study.
Khan, MA; Sayeed, VA; Shah, RB; Tawakkul, MA, 2009
)
0.67
" Analysis of the ways in which the test results were reportedly utilized revealed that they generally played a supporting role with regard to dosing decisions, rather than being the main influence on clinician behaviour."( Clinician experiences of employing the AmpliChip® CYP450 test in routine psychiatric practice.
Butler, R; Dunbar, L; Miles, W; Pulford, J; Sheridan, J; Wheeler, A, 2012
)
0.38
"Patients 5-17 years old with DBDs and an intelligence quotient (IQ) > or =54 were randomized to flexibly dosed risperidone or placebo in a 6-month recurrence prevention trial."( Cognitive function with long-term risperidone in children and adolescents with disruptive behavior disorder.
Cornblatt, B; Pandina, GJ; Zhu, Y, 2009
)
0.84
" Plasma samples were collected before the medications were given and 12h after the bedtime dosing each week."( Gender-specific prolactin response to antipsychotic treatments with risperidone and olanzapine and its relationship to drug concentrations in patients with acutely exacerbated schizophrenia.
Furukori, H; Kaneko, S; Nakagami, T; Saito, M; Sato, Y; Sugawara, N; Tsuchimine, S; Yasui-Furukori, N, 2010
)
0.6
" "Instead of the medicament prescribed, a GP doctor is allowed to prescribe an alternative medicament of the same efficacy in the dosage of an adequate strength" (taken from the specialist medical report form)."( Side-effects of generic.
Dadić-Hero, E; Graovac, M; Grzeta, IR; Medved, P; Ruzić, K; Tatalović-Vorkapić, S, 2010
)
0.36
" Prolactin concentrations before dosing during risperidone treatment were significantly higher than during treatment with olanzapine and perospirone in females."( Prolactin fluctuation over the course of a day during treatments with three atypical antipsychotics in schizophrenic patients.
Fujii, A; Furukori, H; Inoue, Y; Kaneko, S; Sugawara, N; Tsuchimine, S; Yasui-Furukori, N, 2010
)
0.62
" Risperidone can be individually titrated to optimal dosage for excellent response in the majority of children."( Moderators, mediators, and other predictors of risperidone response in children with autistic disorder and irritability.
Aman, MG; Arnold, LE; Chuang, S; Davies, M; DiSilvestro, R; Farmer, C; Kraemer, HC; McCracken, J; McDougle, CJ; Posey, DJ; Scahill, L; Swiezy, NB; Vitiello, B; Witwer, A, 2010
)
1.53
" Further investigations are warranted to identify patient characteristics and antipsychotic dosage regimens that are not associated with a greater risk of mortality in elderly patients with dementia."( Are all commonly prescribed antipsychotics associated with greater mortality in elderly male veterans with dementia?
Dysken, MW; Lederle, FA; Rector, TS; Rossom, RC, 2010
)
0.36
"In the male patients, there was no correlation between the RIS dosage and plasma PRL levels, between plasma RIS levels and PRL levels, or between the plasma 9-OH-RIS levels and PRL levels."( Gender differences in the relationship between the risperidone metabolism and the plasma prolactin levels in psychiatric patients.
Fukui, N; Inoue, Y; Ono, S; Someya, T; Sugai, T; Suzuki, Y; Tsuneyama, N; Watanabe, J, 2010
)
0.61
" Medication was administered by a specialized clinical team following dosing guidelines."( Esquire trial: efficacy and adverse effects of quetiapine versus risperidone in first-episode schizophrenia.
Craig, TK; Elanjithara, T; Gafoor, R; Landau, S; McGuire, P; Power, P, 2010
)
0.6
" The effect occurs even when a low dosage (3 mg/d) of aripiprazole was used and achieves a plateau at dosages beyond 6 mg/d."( Dose-dependent effects of adjunctive treatment with aripiprazole on hyperprolactinemia induced by risperidone in female patients with schizophrenia.
Fujii, A; Furukori, H; Kaneko, S; Sugawara, N; Yasui-Furukori, N, 2010
)
0.58
"Individuals in the extended dosing group were not at greater risk of symptom exacerbation, relapse, or rehospitalization; indeed, more rehospitalizations occurred in those receiving regular dosing."( "Extended" antipsychotic dosing in the maintenance treatment of schizophrenia: a double-blind, placebo-controlled trial.
Feingold, A; Kapur, S; Mann, S; Remington, G; Seeman, P; Shammi, C, 2011
)
0.37
" After the OGTT, the medication was switched to another by decreasing the previous dosage gradually over 2 to 8 months after the initiation of the second medicine."( A crossover study on the glucose metabolism between treatment with olanzapine and risperidone in schizophrenic patients.
Furukori, H; Kaneko, S; Nakagami, T; Saito, M; Sato, Y; Yasui-Furukori, N, 2010
)
0.59
" Early discontinuation was less likely when the recommendations in the manufacturer's prescribing information regarding dosage and supplementation with oral antipsychotics were followed."( Risperidone long-acting therapy prescribing patterns and their impact on early discontinuation of treatment in a large Medicaid population.
Becker, MA; Boaz, TL; Constantine, RJ; Howe, AM; Robst, J, 2011
)
1.81
"), and once-monthly flexible dosing as deltoid or gluteal injections on day 36 (50 mg eq."( A double-blind study of paliperidone palmitate and risperidone long-acting injectable in adults with schizophrenia.
Gassmann-Mayer, C; Gopal, S; Hough, D; Lane, R; Pandina, G; Remmerie, B; Simpson, G, 2011
)
0.62
" Side effects were assessed with Dosage Record and Treatment Emergent Symptoms Scale, other symptom-specific scales, laboratory and instrumental tests."( Olanzapine vs. risperidone in treating aggressive behaviours in adults with intellectual disability: a single blind study.
Amore, M; Bertelli, M; Rossi, M; Tamborini, S; Villani, D, 2011
)
0.72
" We find that, despite not knowing patients' metabolic status, clinicians modify risperidone dosage in order to obtain the best therapeutic option."( Intuitive pharmacogenetics: spontaneous risperidone dosage is related to CYP2D6, CYP3A5 and ABCB1 genotypes.
Alvarez, S; Bernardo, M; Gassò, P; Lafuente, A; Mas, S; Parellada, E, 2012
)
0.87
"025 mg/kg of risperidone daily for 4 months, then the dosage was doubled for another 4 months."( Post-drug consequences of chronic atypical antipsychotic drug administration on the ability to adjust behavior based on feedback in young monkeys.
Mandell, DJ; Sackett, GP; Unis, A, 2011
)
0.74
" The dosage range of paliperidone ER (6-12 mg/day) was compared with 2 risperidone dosage ranges: 2-4 and 4-6 mg/day."( Paliperidone ER and oral risperidone in patients with schizophrenia: a comparative database analysis.
Bossie, CA; Canuso, CM; Lindenmayer, JP; Schooler, N; Turkoz, I, 2011
)
0.91
"]; then once-monthly deltoid or gluteal injections, flexibly dosed [50, 100, or 150 mg eq."( A comparative study of paliperidone palmitate and risperidone long-acting injectable therapy in schizophrenia.
Gu, N; Li, H; Ning, X; Rui, Q; Xu, H, 2011
)
0.62
"The aim of this study was to assess human striatal dopamine receptor 2 (D(2)) and cortical 5-hydroxytryptamine receptor 2A (5-HT(2A)) occupancy of SB-773812 to demonstrate brain penetration and binding to the target receptors and assess the pharmacokinetics-receptor occupancy relationship over time to aid dose selection and dosage regimen, in preparation for the phase II trials."( Contribution of SPECT measurements of D2 and 5-HT2A occupancy to the clinical development of the antipsychotic SB-773812.
Bullich, S; Burgess, C; Catafau, AM; Gray, F; Merlo-Pich, E; Nucci, G, 2011
)
0.37
" In patients with schizophrenia, D(2) occupancy levels induced by a single dose were maintained over time, indicating that once-daily dosing regimens are appropriate."( Contribution of SPECT measurements of D2 and 5-HT2A occupancy to the clinical development of the antipsychotic SB-773812.
Bullich, S; Burgess, C; Catafau, AM; Gray, F; Merlo-Pich, E; Nucci, G, 2011
)
0.37
" During the 3 months preceding admission, phenytoin dosing was stable and consecutive therapeutic concentrations were documented."( Possible long-acting risperidone-induced hypothermia precipitating phenytoin toxicity in an elderly patient.
Brandon Bookstaver, P; Miller, AD, 2011
)
0.69
"Patients with schizophrenia or schizoaffective disorder with a body mass index ≥ 27 and non-high-density lipoprotein (non-HDL) cholesterol ≥ 130 mg/dl who were on a stable treatment dosage of olanzapine, quetiapine, or risperidone were randomly assigned to switch to ari-piprazole (N=109) for 24 weeks or stay on their current medication (N=106)."( A randomized trial examining the effectiveness of switching from olanzapine, quetiapine, or risperidone to aripiprazole to reduce metabolic risk: comparison of antipsychotics for metabolic problems (CAMP).
Hamer, RH; LaVange, LM; Lieberman, JA; McEvoy, JP; Nussbaum, AM; Perkins, DO; Ring, KD; Rosenheck, RA; Stroup, TS; Swartz, MS, 2011
)
0.77
" on days 1 and 8, and flexible dosing [25-100 mg eq."( A randomized trial of paliperidone palmitate and risperidone long-acting injectable in schizophrenia.
Eerdekens, M; Fleischhacker, WW; Gassmann-Mayer, C; Gopal, S; Hough, D; Lane, R; Lim, P; Remmerie, B, 2012
)
0.63
" Sarsasapogenin at a dosage of 200 mg per day added to a flexible dosage of risperidone at 2-4 mg per day is safe and well tolerated by patients with negative symptoms dominated schizophrenia."( A double-blind, placebo-controlled study of traditional Chinese medicine sarsasapogenin added to risperidone in patients with negative symptoms dominated schizophrenia.
Chen, C; Li, GJ; Li, X; Xiao, SF; Xue, HB; Yuan, CM; Zhang, MY, 2011
)
0.82
" Administration and dosage of Trihexiphenidil (THF) was recorded."( First generation antipsychotics switch with Risperidone in the treatment of chronic schizophrenic patients.
Popović, I; Popović, V; Ravanić, D; Stanojević, A; Stojanović, M; Vladejić, S, 2011
)
0.63
" The FGA group demonstrated that extrapyramidal syndrome (EPS) worsened under an increased dosage of anti-EPS drugs."( Risperidone and olanzapine versus another first generation antipsychotic in patients with schizophrenia inadequately responsive to first generation antipsychotics.
Chan, HY; Chen, CH; Chen, JJ; Gau, SS; Hwu, HG, 2012
)
1.82
" In the patient with laryngeal dystonia these symptoms appeared after restarting risperidone treatment, in the other patient after diminishing the dosage of risperidone and adding sertindole, and in the third patient the syndrome appeared after beginning ziprasidone."( Pisa syndrome and laryngeal dystonia induced by novel antipsychotics.
Lerner, V; Miodownik, C; Witztum, E, 2011
)
0.6
"There was no correlation between risperidone dosage and QTc or plasma risperidone levels and QTc."( QT prolongation of the antipsychotic risperidone is predominantly related to its 9-hydroxy metabolite paliperidone.
Fukui, N; Inoue, Y; Ono, S; Saito, M; Someya, T; Sugai, T; Suzuki, Y; Tsuneyama, N; Watanabe, J, 2012
)
0.93
" Iloperidone 4-8, 10-16, and 20-24 mg/day (all dosed twice daily) were compared with placebo."( Efficacy of iloperidone in the short-term treatment of schizophrenia: a post hoc analysis of pooled patient data from four phase III, placebo- and active-controlled trials.
Citrome, L; Hochfeld, M; Meng, X; Stahl, SM, 2012
)
0.38
" Propensity-stratified and propensity-weighted models as well as analyses controlling for site of care and medication dosage revealed similar patterns."( Risk of mortality among individual antipsychotics in patients with dementia.
Blow, FC; Chiang, C; Cunningham, F; Kales, HC; Kim, HM; Schneider, LS; Seyfried, LS; Valenstein, M; Zivin, K, 2012
)
0.38
" A dose-response effect on impairment of balance was observed that followed the expected time course of the drug pharmacokinetics."( Influence of risperidone on balance control in young healthy individuals.
Cohen, H; Corbeil, P; Pourcher, E; Rodrigue, J; Simoneau, M, 2012
)
0.75
" There was a dose-response relation for all drugs except quetiapine."( Differential risk of death in older residents in nursing homes prescribed specific antipsychotic drugs: population based cohort study.
Avorn, J; Crystal, S; Gerhard, T; Huybrechts, KF; Levin, R; Lucas, JA; Olfson, M; Schneeweiss, S, 2012
)
0.38
"Due to high interindividual variability in peripheral pharmacokinetic parameters, dosing of antipsychotics relies on clinical trial and error."( Predicting plasma concentration of risperidone associated with dosage change: a population pharmacokinetic study.
Bies, RR; Mamo, DC; Mimura, M; Pollock, BG; Suzuki, T; Tsunoda, K; Uchida, H; Watanabe, K, 2012
)
0.66
" In light of the known relationship between plasma drug concentration, dopamine D2 receptor occupancy, and clinical effects, our results confirm that individualized dosing with the measurement of antipsychotic plasma concentrations has the potential for bedside clinical application."( Predicting plasma concentration of risperidone associated with dosage change: a population pharmacokinetic study.
Bies, RR; Mamo, DC; Mimura, M; Pollock, BG; Suzuki, T; Tsunoda, K; Uchida, H; Watanabe, K, 2012
)
0.66
" During the double-blind period, dosing was fixed at patients' final open-label dose (25 mg, 66% of patients; 37."( A randomized, double-blind, placebo-controlled trial to assess prevention of mood episodes with risperidone long-acting injectable in patients with bipolar I disorder.
Cordoba, R; Huberlant, B; Martinez, L; Montgomery, S; Schreiner, A; Sulaiman, AH; Vieta, E, 2012
)
0.6
" Multiple linear regression analysis (95 samples) revealed that sex, smoking habit, and dose explained 21% of the variation in plasma total risperidone after oral dosage (dose alone only explained 11% of the variation)."( Risperidone and total 9-hydroxyrisperidone in relation to prescribed dose and other factors: data from a therapeutic drug monitoring service, 2002-2010.
Bowskill, SV; Fisher, DS; Flanagan, RJ; Handley, SA; Patel, MX, 2012
)
2.02
"Risperidone therapeutic drug monitoring can help assess adherence and guide dosage even after RLAI."( Risperidone and total 9-hydroxyrisperidone in relation to prescribed dose and other factors: data from a therapeutic drug monitoring service, 2002-2010.
Bowskill, SV; Fisher, DS; Flanagan, RJ; Handley, SA; Patel, MX, 2012
)
3.26
" The aim of the present study was to analyze on a single case basis the relationship between a sudden increase in suicidality, anxiety symptoms, medication dosing and clinician- and patient-rated akathisia."( The relationship of Akathisia with treatment emergent suicidality among patients with first-episode schizophrenia treated with haloperidol or risperidone.
Bauer, M; Doucette, S; Lewitzka, U; Meyer, S; Möller, HJ; Musil, R; Riedel, M; Schennach, R; Seemüller, F, 2012
)
0.58
" Although paliperidone is the active metabolite of risperidone, paliperidone's route of metabolism and elimination is quite different from that for risperidone and paliperidone ER may be preferred over risperidone when liver disease, drug-drug interactions or other alterations in metabolism render the appropriate dosing of risperidone difficult to determine for an individual patient."( Oral paliperidone extended-release: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability.
Citrome, L, 2012
)
0.63
" When flexibly dosed with a mean doses of approximately 70 to 110 mg every four weeks, paliperidone palmitate appears comparable in efficacy and tolerability to risperidone long-acting injection flexibly dosed with mean doses of approximately 35 mg every two weeks."( Paliperidone palmitate for schizophrenia.
Nussbaum, AM; Stroup, TS, 2012
)
0.58
" This model may aid the development of individualized risperidone dosing regimens in children and adolescents."( Population pharmacokinetic modeling of risperidone and 9-hydroxyrisperidone to estimate CYP2D6 subpopulations in children and adolescents.
Aman, MG; Bies, RR; Saldaña, SN; Sherwin, CM; Vinks, AA, 2012
)
0.9
" No study addressed the issue of pre-existing/concurrent psychosocial interventions, and comorbid stimulant medication and its dosage was only partially addressed."( Atypical antipsychotics for disruptive behaviour disorders in children and youths.
Hetrick, SE; Loy, JH; Merry, SN; Stasiak, K, 2012
)
0.38
" Results of the own study on the efficacy of risperidone (rispolux) in dosage 102 mg daily in patients with dementia with psychotic and behavioral disorders are presented."( [Efficasy and safety of the use of risperidone (rispoluxe) in demented patients with psychotic and behavioural disorders].
Bocharov, AV; Kondakova, VE; Tuleninov, ES, 2012
)
0.92
" The RLAI group needed a lower dosage of biperiden compared with the control group, even though they had similar risperidone-equivalent daily dosages."( The influence of switching from haloperidol decanoate depot to risperidone long-acting injection on the clinical symptoms and cognitive function in schizophrenia.
Gen, K; Suzuki, H, 2012
)
0.83
"All trials were industry supported, with some variability in dosage of haloperidol."( Lower rate of depressive switch following antimanic treatment with second-generation antipsychotics versus haloperidol.
Capapey, J; Colom, F; Goikolea, JM; Grande, I; Sanchez-Moreno, J; Torres, I; Undurraga, J; Valentí, M; Vieta, E, 2013
)
0.39
" Risperidone accelerates the hydrolytic degradation of PLGA, presumably within the microenvironment of the drug-loaded particles, and this phenomenon must be taken into consideration in designing PLGA dosage forms of tertiary amine drugs."( Accelerated polymer biodegradation of risperidone poly(D, L-lactide-co-glycolide) microspheres.
Blasi, P; DeLuca, PP; Selmin, F, 2012
)
1.56
" They responded well to the reduction in dosage or to withdrawal of the apparent causing agent."( [Medication-related oculogyric crises: a description of four cases and a review of the literature].
Campistol, J; Darling, A; Perez-Duenas, B; Poo, P, 2013
)
0.39
"The results of this study suggest that switching elderly patients from risperidone to PAL may result in superior safety and patient satisfaction, and may also make it possible to reduce the dosage of biperiden."( Study of the efficacy and safety of switching from risperidone to paliperidone in elderly patients with schizophrenia.
Gen, K; Hibino, H; Inoue, Y; Matsumoto, H; Mikami, A; Mikami, K; Otomo, M; Suzuki, H, 2013
)
0.87
" Subjects received either: 1) paliperidone palmitate (PP; 234 mg day 1 and 156 mg day 8 [corresponding to 150 and 100 milligram equivalents of paliperidone, respectively], both administered in deltoid muscle, followed by once-monthly flexible dosing in deltoid or gluteal muscle) and risperidone long-acting injection (RLAI)-matched placebo injections; or, 2) RLAI (25 mg, days 8 and 22; followed by biweekly flexible dosing) and PP-matched placebo injections."( Paliperidone palmitate versus risperidone long-acting injection in markedly-to-severely ill schizophrenia subjects: onset of efficacy with recommended initiation regimens.
Alphs, L; Bossie, CA; Fu, DJ; Kern Sliwa, J; Ma, YW, 2014
)
0.87
"Using the recommended dosing regimens for PP and RLAI, both PP and oral risperidone (used during RLAI initiation) improved symptoms of schizophrenia in markedly-to-severely ill subjects at days 4-22."( Paliperidone palmitate versus risperidone long-acting injection in markedly-to-severely ill schizophrenia subjects: onset of efficacy with recommended initiation regimens.
Alphs, L; Bossie, CA; Fu, DJ; Kern Sliwa, J; Ma, YW, 2014
)
0.92
" Data were derived from an earlier study, designed to compare efficacy and tolerability of fixed dosage of extended-release venlafaxine, mitazapine, paroxetine, and risperidone, sodium valproate, buspirone, trazodone or thyroid hormone augmenting to paroxetine in those patients."( Difference in remission in a Chinese population with anxious versus nonanxious treatment-resistant depression: a report of OPERATION study.
Cao, L; Chen, J; Fang, Y; Hong, W; Peng, D; Wu, Z; Yuan, C; Zhang, C, 2013
)
0.59
" A biweekly simulation of multiple dosing revealed that Formulation C, the selected formulation, with a high load and large particle size would provide adequate initial and maintenance levels of the active moiety (Risperidone and its metabolite, 9-hydroxyrisperidone)."( Microsphere delivery of Risperidone as an alternative to combination therapy.
D'Souza, S; DeLuca, P; Faraj, J, 2013
)
0.88
" All values were more than 30 ng/mL after 11-16 h from dosing to sample collection, and the mean value was 47."( The possibility that requiring high-dose olanzapine cannot be explained by pharmacokinetics in the treatment of acute-phase schizophrenia.
Hatta, K; Hirata, T; Ito, S; Kasuya, M; Katayama, S; Kuga, H; Morikawa, F; Nakamura, H; Nakamura, M; Nakase, R; Ohnuma, T; Sawa, Y; Shirai, Y; Sudo, Y; Takebayashi, H; Usui, C, 2013
)
0.39
" We conducted an 8-week, rater-blinded, randomized trial, administering flexibly dosed risperidone, yokukansan, or fluvoxamine."( Efficacy and tolerability of risperidone, yokukansan, and fluvoxamine for the treatment of behavioral and psychological symptoms of dementia: a blinded, randomized trial.
Kurita, M; Nishino, S; Numata, Y; Okubo, Y; Sato, T; Takeyoshi, K; Tateno, A; Teranishi, M, 2013
)
0.9
" One-third of children and adolescents had abnormal serum triglycerides and cholesterol; however, a dose-response was not demonstrated."( Metabolic changes in first-episode early-onset schizophrenia with second-generation antipsychotics.
Amminger, GP; Becker, J; O'Donoghue, B; Papageorgiou, K; Schäfer, MR, 2014
)
0.4
"This was a 6-week, multicenter, randomized, open-label, parallel-group, flexible dosing study."( An open-label, randomized, controlled trial of zotepine and risperidone for acutely ill, hospitalized, schizophrenic patients with symptoms of agitation.
Chan, HY; Chen, KP; Chen, YY; Cheng, JS; Lin, AS; Tsai, CJ, 2013
)
0.63
" In the USA, dosing tends to be expressed in mg] or oral risperidone [during initiation of risperidone long-acting injection (RLAI) days 1-28] and biweekly flexible-dose RLAI (n=173; initial injection day 8)."( Paliperidone palmitate versus oral risperidone and risperidone long-acting injection in patients with recently diagnosed schizophrenia: a tolerability and efficacy comparison.
Alphs, L; Bossie, CA; Fu, DJ; Ma, YW; Sliwa, JK, 2014
)
0.92
" The time to development of Pisa syndrome, patient demographics, dosing and titration of causative medications, approach to treatment, and resolution of Pisa syndrome varied widely in these reports."( Risperidone-induced Pisa syndrome in MS: resolution with lurasidone and recurrence with Chlorpromazine.
Diefenderfer, LA; Iuppa, CA, 2013
)
1.83
"The purpose of this prospective study was to evaluate the effects of switching from oral risperidone to flexibly dosed oral paliperidone extended-release (ER) in Brazilian adults with schizophrenia because of lack of efficacy, intolerability, or nonadherence after a minimum trial of 30 days on adequate (labeled) doses of oral risperidone, according to individual clinical judgment."( Switching from oral risperidone to flexibly dosed oral paliperidone extended-release: core symptoms, satisfaction, and quality of life in patients with stable but symptomatic schizophrenia: the RISPALI study.
Appolinário, JC; Bressan, RA; Campos, JA; de Oliveira, IR; Elkis, H; Gattaz, WF; Grabowski, HM; Henna, E; Lacerda, AL; Lawson, FL; Louzã, MR; Périco, Cde A; Quevedo, J; Rocha, FL; Ruschel, SI; Sacomani, E; Zorzetto Filho, D, 2014
)
0.95
"In this 6 month (26 week) open-label extension (OLE) study, patients (5-17 years of age, who completed the previous fixed-dose, 6 week, double-blind [DB] phase) were flexibly dosed with risperidone based on body weight."( An open-label extension study of the safety and efficacy of risperidone in children and adolescents with autistic disorder.
Hough, D; Karcher, K; Kent, JM; Pandina, G; Singh, J, 2013
)
0.82
" All patients were titrated on iloperidone to 6mg BID by Day 4, then flexibly dosing between 6 and 12mg BID, as needed."( A trial evaluating gradual- or immediate-switch strategies from risperidone, olanzapine, or aripiprazole to iloperidone in patients with schizophrenia.
Alva, G; Brams, M; Citrome, L; Glick, ID; Hochfeld, M; Jackson, R; Kianifard, F; Mattingly, G; Meng, X; Pestreich, L; Weiden, PJ; Winseck, A, 2014
)
0.64
" Initial and maintenance dosage of RLAI were adjusted according to clinical judgment."( A prospective, open-label study to evaluate symptomatic remission in schizophrenia with risperidone long-acting injectable in Korea.
Ahn, YM; Cho, SJ; Chung, YC; Jung, IK; Kim, CY; Kim, DH; Kim, SH; Kim, YS; Lee, DG; Lee, NY; Lee, YH; Lim, WJ; Na, YS; Shin, SE; Woo, JM; Yoon, BH; Yoon, JS, 2014
)
0.62
" The results indicated that the dosage of 10-90 mg/kg of RM for 2 weeks did not cause treatment-related mortality."( A 12-week subchronic intramuscular toxicity study of risperidone-loaded microspheres in rats.
Cen, X; Dong, Q; Du, G; Fu, F; Guan, X; Tian, J; Wang, W; Ye, L; Yu, X; Zhang, J; Zhu, X, 2015
)
0.67
" No correlation was found between risperidone dosage and either risperidone or drug metabolite plasma levels."( CYP2D6 genotyping in paediatric patients with autism treated with risperidone: a preliminary cohort study.
Bar-Chaim, A; Benveniste-Levkovitz, P; Berkovitch, M; Britzi, M; Gabis, LV; Soback, S; Youngster, I; Zachor, DA; Ziv-Baran, T, 2014
)
0.92
" The compound exhibited high peripheral and adequate brain levels upon oral dosing in rodents."( Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
Avhad, VB; Bajpai, M; Bhateja, DK; Das, S; Gandhi, MN; Gudi, GS; Gullapalli, S; Gupta, PK; Harde, RL; Jadhav, SB; Joshi, AA; Khairatkar-Joshi, N; Mahat, MY; Marathe, MY; Shelke, DE; Thomas, A, 2014
)
0.4
" However, a higher dosage of risperidone was used for treating the disorder in those taking concomitant lovastatin compared to placebo."( Lovastatin for the adjunctive treatment of schizophrenia: a preliminary randomized double-blind placebo-controlled trial.
Akhondzadeh, S; Berk, M; Dehbozorgi, S; Ghanizadeh, A; Rezaee, Z, 2014
)
0.69
"Retrospective data were gathered including age, sex, IQ, birth weight, dosage of risperidone, urinary density, as well as existence of urinary and fecal incontinence."( Risperidone-associated urinary incontinence in patients with autistic disorder with mental retardation.
Imasaka, Y; Iwata, K; Kumazaki, H; Mimura, M; Tomoda, A; Watanabe, K, 2014
)
2.07
" To address this question we have investigated the cytological and functional effects of four APs: chlorpromazine (CLP), haloperidol (HAL), risperidone (RIS) and clozapine (CLZ), at concentrations typical of high therapeutic dosage on a human brain microvascular endothelial cell (HBMEC) model of the BBB."( Adverse effects of antipsychotics on micro-vascular endothelial cells of the human blood-brain barrier.
Elmorsy, E; Elsheikha, HM; Elzalabany, LM; Smith, PA, 2014
)
0.6
" On day 8, the amisulpride dosage was increased to 800 mg orally daily and his manic symptoms worsened."( Amisulpride-associated mania in a young adult with schizophrenia and cerebral disease.
Chen, CY; Chen, TY; Chuang, WC; Kuo, SC; Yeh, YW, 2014
)
0.4
"In this prospective multicentre, open-label, 6-month study (Paliperidone Palmitate Flexible Dosing in Schizophrenia [PALMFlexS]), tolerability, safety and treatment response with paliperidone palmitate (PP) were explored in patients with acute symptoms of schizophrenia following switching from previously unsuccessful treatment with oral antipsychotics."( Intramuscular long-acting paliperidone palmitate in acute patients with schizophrenia unsuccessfully treated with oral antipsychotics.
Bergmans, P; Bez, Y; Carpiniello, B; Cherubin, P; Hargarter, L; Keim, S; Parellada, E; Rancans, E; Schreiner, A; Vidailhet, P, 2015
)
0.42
" The mean serum PRL was higher in females in the pubertal/postpubertal stage and for risperidone dosage up 1 mg/day."( Prolactin variations during risperidone therapy in a sample of drug-naive children and adolescents.
Lamanna, AL; Margari, F; Margari, L; Matera, E; Palmieri, VO; Pastore, A; Petruzzelli, MG; Simone, M, 2015
)
0.93
"The objective of this study was to evaluate the effectiveness and impact of once- versus twice-daily dosing of risperidone and olanzapine on clinical outcomes in patients with schizophrenia."( Effectiveness of different dosing regimens of risperidone and olanzapine in schizophrenia.
Agid, O; Fervaha, G; Lee, J; Remington, G; Takeuchi, H, 2015
)
0.89
" Although our study suggests the prescription dosage and duration of antipsychotic treatment decreased significantly after FDA warning in 2005, the duration of treatment was still long."( Dosage and duration of antipsychotic treatment in demented outpatients with agitation or psychosis.
Chiang, HL; Hwang, TJ; Hwu, HG; Lin, YT; Shan, JC; Sheu, YH, 2015
)
0.42
" The incremental dosage of olanzapine from 5 to 20 mg/day was given but failed to control her psychotic symptoms during the first week, and was therefore switched to risperidone."( Chemotherapy-induced acute psychosis in a patient with malignant germ cell tumour.
Pongpirul, K; Puangthong, U, 2015
)
0.61
" However, the ideal dosing regimen for this purpose is unknown."( Adjunctive aripiprazole in the treatment of risperidone-induced hyperprolactinemia: A randomized, double-blind, placebo-controlled, dose-response study.
Bian, QT; Chen, JX; Correll, C; Liu, YH; Soares, JC; Su, YA; Wang, SL; Wei, LH; Yang, FD; Zhang, RZ; Zhang, XY, 2015
)
0.68
"PALMFlexS, a prospective multicentre, open-label, 6-month, phase IIIb interventional study, explored tolerability, safety and treatment response in adults (n = 231) with non-acute but symptomatic schizophrenia switching to flexibly dosed paliperidone palmitate (PP) after unsuccessful treatment with risperidone long-acting injectable therapy (RLAT) or conventional depot antipsychotics (APs)."( Paliperidone palmitate in non-acute patients with schizophrenia previously unsuccessfully treated with risperidone long-acting therapy or frequently used conventional depot antipsychotics.
Bergmans, P; Cherubin, P; Corrivetti, G; Cosar, B; Hargarter, L; Keim, S; Llorca, PM; Petralia, A; Schreiner, A, 2015
)
0.81
" Patients entered the study on a stable SRI dosage and were randomized to EX/RP (N = 40), risperidone (N = 40), or placebo (N = 20)."( Augmenting serotonin reuptake inhibitors in obsessive-compulsive disorder: What moderates improvement?
Foa, EB; Rosenfield, D; Simpson, HB; Wheaton, MG, 2015
)
0.64
" These results highlight the importance of a personalized dosage adjustment during risperidone treatment."( Genetics-Based Population Pharmacokinetics and Pharmacodynamics of Risperidone in a Psychiatric Cohort.
Choong, E; Conus, P; Csajka, C; Eap, CB; Guidi, M; Vandenberghe, F; von Gunten, A, 2015
)
0.88
" After the dosage was titrated to 6 mg/d, she experienced generalized seizure attacks."( High-Dose Risperidone Induced Latent Syndrome of Inappropriate Antidiuretic Hormone Secretion With Seizure Presentation.
Lee, YF; Liang, CS; Tsai, CK,
)
0.53
"Population pharmacokinetics can predict antipsychotic blood concentrations at a given time point prior to a dosage change."( Dopamine D2/3 Receptor Occupancy Following Dose Reduction Is Predictable With Minimal Plasma Antipsychotic Concentrations: An Open-Label Clinical Trial.
Bies, RR; Caravaggio, F; Gerretsen, P; Graff-Guerrero, A; Mamo, DC; Mar, W; Mulsant, BH; Nakajima, S; Plitman, E; Pollock, BG; Suzuki, T; Uchida, H, 2016
)
0.43
"D2/3R occupancy levels can be predicted from blood drug concentrations collected prior to dosage change."( Dopamine D2/3 Receptor Occupancy Following Dose Reduction Is Predictable With Minimal Plasma Antipsychotic Concentrations: An Open-Label Clinical Trial.
Bies, RR; Caravaggio, F; Gerretsen, P; Graff-Guerrero, A; Mamo, DC; Mar, W; Mulsant, BH; Nakajima, S; Plitman, E; Pollock, BG; Suzuki, T; Uchida, H, 2016
)
0.43
" Concomitant armodafinil and risperidone use may necessitate risperidone dosage adjustment, particularly when starting or stopping coadministration of the two drugs."( Evaluation of potential pharmacokinetic drug-drug interaction between armodafinil and risperidone in healthy adults.
Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015
)
0.93
" The problem of low exposure of 18b was effectively addressed by its conversion to an acetate prodrug 25b, which upon oral dosing resulted in an improved pharmacokinetic profile (Cmax = 359 ng."( Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
Bajpai, M; Dahale, DH; Gudi, GS; Gullapalli, S; Gupta, PK; Jadhav, SB; Khairatkar-Joshi, N; Kummari, S; Lingam, VS; Mindhe, AS; Pattem, R; Rathi, VE; Sapalya, RS; Shah, DM; Shingote, YB; Thakur, RR; Thomas, A, 2015
)
0.42
" Thus, antipsychotic dose and dosing interval should be optimized for each patient."( [Optimal Antipsychotic Dose and Dosing Interval in the Treatment of Schizophrenia].
Takeuchi, H, 2015
)
0.42
" Moreover, available tools that guide dosing in neuropsychiatric pediatric patients are scant, leading to the possibility of reduced efficacy and/or increased risks of toxicity."( Therapeutic drug monitoring of second-generation antipsychotics in pediatric patients: an observational study in real-life settings.
Auricchio, F; Baldelli, S; Bernardini, R; Bertella, S; Bravaccio, C; Capuano, A; Carnovale, C; Cattaneo, D; Clementi, E; Ferrajolo, C; Fucile, S; Guastella, G; Mani, E; Molteni, M; Pascotto, A; Pisano, S; Pozzi, M; Radice, S; Rafaniello, C; Riccio, MP; Rizzo, R; Rossi, F; Scuderi, MG; Sperandeo, S; Sportiello, L; Villa, L, 2016
)
0.43
" The design was employed to understand the influence of the critical excipient combinations on the production of OD-mini-tablets and thus guarantee the feasibility of obtaining products with dosage form uniformity."( Risperidone oral disintegrating mini-tablets: A robust-product for pediatrics.
Abdelbary, MF; Ahmed, TA; Ali, BE; Aljaeid, BM; El-Say, KM; Zidan, AS, 2015
)
1.86
" Analyses were conducted assuming pooled dosing from randomised clinical trials included in the MTCs."( Cost-effectiveness Analysis of Aripiprazole Once-Monthly for the Treatment of Schizophrenia in the UK.
Beillat, M; Robinson, P; Sapin, C; Tempest, M; Treur, M, 2015
)
0.42
" Age, gender, years of education, total intracranial volume, apolipoprotein E genotype, dosage of risperidone, the baseline scores on the Korean version of the Mini-Mental State Examination, and the baseline psychotic and nonpsychotic symptoms scores on the K-NPI were measured as covariates of no interest."( Gray matter volumes and treatment response of psychotic symptoms to risperidone in antipsychotic-naïve Alzheimer's disease patients.
Chung, YI; Jeong, HJ; Kim, HJ; Kim, JH; Kim, TH; Kim, YH; Lee, BD; Lee, YM; Moon, E; Mun, CW; Park, JM, 2016
)
0.89
" The dosage of risperidone and paliperidone were maintained; and aripiprazole was maintained at 5mg/day during the 8-week study period."( Add-on effects of a low-dose aripiprazole in resolving hyperprolactinemia induced by risperidone or paliperidone.
Guo, Q; Li, C; Ouyang, Q; Qiao, Y; Shen, W; Sheng, J; Wen, H; Yang, F; Zhu, S, 2016
)
1.01
" NMS occurs most often during the first week of treatment or after increasing the dosage of the neuroleptic medication."( [Case report: Neuroleptic malignant syndrome and diagnostic difficulties].
Khouri, C; Logerot, S; Mallaret, M; Planès, S; Villier, C, 2016
)
0.43
" The daily dosage of RIS did not differ between groups."( Risperidone-induced extrapyramidal side effects: is the need for anticholinergics the consequence of high plasma concentrations?
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B; Veselinovic, T, 2016
)
1.88
"The median daily dosage of RIS did not differ between the groups (p=0."( Pharmacokinetic considerations in the treatment of hypertension in risperidone-medicated patients - thinking of clinically relevant CYP2D6 interactions.
Gründer, G; Haen, E; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B; Walther, S, 2016
)
0.67
" Higher RIS dosage has a tendency to produce higher RIS plasma levels."( Development and Validation of Liquid Chromatography/Tandem Mass Spectrometry Analysis for Therapeutic Drug Monitoring of Risperidone and 9-Hydroxyrisperidone in Pediatric Patients with Autism Spectrum Disorders.
Hongkaew, Y; Limsila, P; Nakorn, CN; Ngamsamut, N; Nuntamool, N; Prommas, S; Puangpetch, A; Sukasem, C; Vanwong, N, 2016
)
0.64
" This open-label, parallel-group study was performed to compare finger-stick-based capillary with corresponding venous plasma concentrations for risperidone, paliperidone, quetiapine, olanzapine, and aripiprazole and their major metabolites after repeated dosing in patients with schizophrenia or related illnesses."( Comparison of Capillary and Venous Plasma Drug Concentrations After Repeated Administration of Risperidone, Paliperidone, Quetiapine, Olanzapine, or Aripiprazole.
Ariyawansa, J; De Meulder, M; Remmerie, B; Savitz, A, 2016
)
0.85
" Daily dosage of risperidone did not differ between responders and non-responders."( Clinical response in a risperidone-medicated naturalistic sample: patients' characteristics and dose-dependent pharmacokinetic patterns.
Gründer, G; Haen, E; Hiemke, C; Paulzen, M; Schoretsanitis, G; Stegmann, B; Unterecker, S, 2017
)
1.11
" Then we re-administered decreased dosage of lithium 600 mg/day and risperidone 3 mg/day, and the similar episode occurred again 3 days later."( Neurotoxicity and nephrotoxicity caused by combined use of lithium and risperidone: a case report and literature review.
Hsu, CW; Lee, CY; Lee, Y; Lin, PY, 2016
)
0.9
"Daily dosage of risperidone differed significantly with smokers receiving higher doses than patients in the control group (p=0."( Effect of smoking on risperidone pharmacokinetics - A multifactorial approach to better predict the influence on drug metabolism.
Gründer, G; Haen, E; Hiemke, C; Paulzen, M; Schoretsanitis, G; Stegmann, B, 2017
)
1.12
" Prolactin levels could assist in the determination of appropriate antipsychotic dosing to minimize adverse effects."( Threshold of Dopamine D2/3 Receptor Occupancy for Hyperprolactinemia in Older Patients With Schizophrenia.
Caravaggio, F; Chung, JK; Gerretsen, P; Graff-Guerrero, A; Iwata, Y; Mamo, DC; Mar, W; Mulsant, BH; Nakajima, S; Plitman, E; Pollock, BG; Rajji, TK; Suzuki, T; Uchida, H, 2016
)
0.43
" Groups were matched for demographic characteristics and daily dosage of RIS."( Cytochrome P450-mediated interaction between perazine and risperidone: implications for antipsychotic polypharmacy.
Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Stegmann, B, 2017
)
0.7
"The mean concentrations of glucose, insulin, prolactin and leptin and HOMA-IR significantly rose with risperidone dosage (all P<0."( Impact of risperidone on leptin and insulin in children and adolescents with autistic spectrum disorders.
Hongkaew, Y; Intachak, B; Kroll, MH; Limsila, P; Ngamsamut, N; Puangpetch, A; Srisawasdi, P; Sukasem, C; Vanavanan, S; Vanwong, N, 2017
)
1.07
" inverted U) association between changes in dentate gyrus/CA4 volume and cumulative antipsychotic dosage between the scans."( Hippocampal subregion volume changes associated with antipsychotic treatment in first-episode psychosis.
Gallego, JA; Malhotra, AK; Rhindress, K; Robinson, DG; Szeszko, PR; Wellington, R, 2017
)
0.46
" The finding of a non-linear relationship between changes in dentate gyrus/CA4 subregion volume and antipsychotic exposure may provide new avenues into understanding dosing strategies for therapeutic interventions relevant to neurobiological models of hippocampal dysfunction in psychosis."( Hippocampal subregion volume changes associated with antipsychotic treatment in first-episode psychosis.
Gallego, JA; Malhotra, AK; Rhindress, K; Robinson, DG; Szeszko, PR; Wellington, R, 2017
)
0.46
" In a naturalistic cohort of chronic psychiatric inpatients, we demonstrated that clinicians adjust R dosage by CYP2D6 activity, despite being blinded to the genotype, which we described as an "intuitive pharmacogenetic" process."( Intuitive pharmacogenetic dosing of risperidone according to CYP2D6 phenotype extrapolated from genotype in a cohort of first episode psychosis patients.
Bernardo, M; Bioque, M; Bobes, J; Castro-Fornieles, J; Corripio, I; Gassó, P; González-Pinto, A; Lafuente, A; Llerena, A; Lobo, A; Mas, S; Olmeda, MS; Rodriguez-Jimenez, R; Saiz-Ruiz, J; Torra, M; Usall, J; Vieta, E, 2017
)
0.73
"Second-generation long-acting injectable therapies (SGA-LAIs) may reduce health care resource utilization (HRU) and health care costs compared with daily oral atypical antipsychotics (OAAs) in patients with schizophrenia due to reduced dosing frequency, delivery/monitoring by a health care provider, and improved adherence."( Treatment Patterns, Health Care Resource Utilization, and Spending in Medicaid Beneficiaries Initiating Second-generation Long-acting Injectable Agents Versus Oral Atypical Antipsychotics.
Emond, B; Joshi, K; Kamstra, R; Lafeuille, MH; Lefebvre, P; Pilon, D; Tandon, N, 2017
)
0.46
"Clinicians tend to be more cautious with dosing of risperidone to geriatric patients in the ED."( Risperidone in the Emergency Setting is Associated with More Hypotension in Elderly Patients.
Castillo, EM; Hopper, A; Nordstrom, K; Porter, A; Vilke, GM; Wilson, MP, 2017
)
2.15
" Based upon the patient's history and the dosing time line of the medications, we propose that an interaction between the clozapine and residual risperidone was responsible for the development of the acute buccal dystonia."( An Unexpected Circumstance: Acute Dystonic Reaction in the Setting of Clozapine Administration.
Ahmed, I; Kaplan, AM; Pitts, WB, 2019
)
0.71
" Active moiety achieved therapeutic levels by 2 h after dose, and the levels were maintained throughout the 4-week dosing period."( A phase II study to evaluate the pharmacokinetics, safety, and tolerability of Risperidone ISM multiple intramuscular injections once every 4 weeks in patients with schizophrenia.
Anta, L; Ayani, I; Gutierro, I; Litman, RE; Llaudó, J; Martínez, J, 2018
)
0.71
" We sought to determine the change in cognitive function and symptomatology after reducing risperidone or olanzapine dosage in stable schizophrenic patients."( Dose reduction of risperidone and olanzapine can improve cognitive function and negative symptoms in stable schizophrenic patients: A single-blinded, 52-week, randomized controlled study.
Cui, H; Li, D; Li, G; Ning, Y; Zhou, Y, 2018
)
1.04
" The duration of each adequate antipsychotic treatment at an optimal dosage was 4 weeks or more."( Predictors of remission during acute treatment of first-episode schizophrenia patients involuntarily hospitalized and treated with algorithm-based pharmacotherapy: Secondary analysis of an observational study.
Sakamoto, S; Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019
)
0.51
" There were no differences in first-line antipsychotics, dosage of antipsychotics at time of response and adherence rates to algorithm-based pharmacotherapy between remitters and non-remitters."( Predictors of remission during acute treatment of first-episode schizophrenia patients involuntarily hospitalized and treated with algorithm-based pharmacotherapy: Secondary analysis of an observational study.
Sakamoto, S; Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019
)
0.51
" We report a boy with autism-spectrum disorder, who developed frequent penile erections after an increase in risperidone dosage for a month."( Frequent Penile Erection in a Boy With Autism-spectrum Disorder: Case Report.
Bejrananda, T; Thongseiratch, T, 2018
)
0.69
"We assessed the dosage strengths of paliperidone palmitate 1-month (PP1M) long-acting injectable resulting in similar steady-state (SS) exposures to the dosage strengths of oral risperidone using pharmacokinetic (PK) simulations."( Maintenance dose conversion between oral risperidone and paliperidone palmitate 1 month: Practical guidance based on pharmacokinetic simulations.
Gopal, S; Kern Sliwa, J; Kim, E; Mathews, M; Ravenstijn, P; Russu, A; Singh, A, 2018
)
0.94
" However, it is not known whether intermittent dosing would produce similar deleterious effects."( Spontaneous recovery after controlled cortical impact injury is not impeded by intermittent administration of the antipsychotic drug risperidone.
Bao, GC; Besagar, S; Bondi, CO; Carlson, LJ; Kline, AE; Leary, JB; Radabaugh, HL, 2018
)
0.68
"Risperidone is applied in oral dosage formulations in the treatment of mental diseases."( Formulation of delivery systems with risperidone based on biodegradable terpolymers.
Borecka, A; Janeczek, H; Kasperczyk, J; Sobota, M; Turek, A, 2018
)
2.2
"5% of the baseline dosage every 2 weeks."( Changes in Health-Related Quality of Life in People With Intellectual Disabilities Who Discontinue Long-Term Used Antipsychotic Drugs for Challenging Behaviors.
de Kuijper, G; Hoekstra, PJ; Ramerman, L, 2019
)
0.51
" Hence, a different dosing strategy is required among smoking and nonsmoking patients."( Analysis of smoking behavior on the pharmacokinetics of antidepressants and antipsychotics: evidence for the role of alternative pathways apart from CYP1A2.
Deckert, J; Hommers, LG; Menke, A; Samanski, L; Scherf-Clavel, M; Unterecker, S, 2019
)
0.51
" Upon decreasing the dosage of risperidone, the cystoid macular edema resolved and visual acuity markedly improved."( Risperidone-related bilateral cystoid macular edema: a case report.
Gelman, R; Kozlova, A; McCanna, CD, 2019
)
2.24
"During a period of inflammation in patients taking quetiapine, according to our results, attention in dosing strategies is required to prevent toxic plasma concentrations."( Pathological Concentration of C-reactive Protein is Correlated to Increased Concentrations of Quetiapine, But Not of Risperidone, Olanzapine and Aripiprazole in a Naturalistic Setting.
Deckert, J; Menke, A; Scherf-Clavel, M; Unterecker, S; Weidner, A, 2020
)
0.77
" Pre-emptive CYP2D6 genotyping would be valuable for individualising risperidone and aripiprazole dosing and treatment optimisation."( Effect of CYP2D6 genotype on exposure and efficacy of risperidone and aripiprazole: a retrospective, cohort study.
Haslemo, T; Ingelman-Sundberg, M; Jukic, MM; Molden, E; Smith, RL, 2019
)
1
" We report that low-dose risperidone treatment results in global immunosuppression in mice, observed following 5 days of dosing and exacerbated with longer term drug treatment (4 weeks)."( The antipsychotic medication, risperidone, causes global immunosuppression in healthy mice.
Barlow, D; Beauchemin, M; Houseknecht, KL; May, M; Vary, C, 2019
)
1.11
"Modeling dose-response relationships of drugs is essential to understanding their safety effects on patients under realistic circumstances."( Bayesian Meta-analysis of Multiple Continuous Treatments with Individual Participant-Level Data: An Application to Antipsychotic Drugs.
Horvitz-Lennon, M; Normand, ST; Spertus, J, 2019
)
0.51
" Resveratrol dosage was 250 mg twice per day from the beginning of the study."( Resveratrol as adjunctive therapy in treatment of irritability in children with autism: A double-blind and placebo-controlled randomized trial.
Akhondzadeh, S; Hendouei, F; Mohammadi, MR; Rezaei, F; Sanjari Moghaddam, H; Taslimi, N, 2020
)
0.56
" Particularly, impact associated with dosage has been barely studied."( Effects of long-term antipsychotics treatment on body weight: A population-based cohort study.
Bazo-Alvarez, JC; Carpenter, JR; Hayes, JF; Morris, TP; Petersen, I, 2020
)
0.56
"The dose-response relationships of antipsychotic drugs for schizophrenia are not well defined, but such information would be important for decision making by clinicians."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" Dose-response curves were constructed with random-effects dose-response meta-analyses and a spline model."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" For some drugs, higher than currently licensed doses might be tested in further trials, because their dose-response curves did not plateau."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
"This short report provides guidance for antipsychotic medication dosing to improve early intervention outcomes."( Early behavioral and developmental interventions in ADNP-syndrome: A case report of SWI/SNF-related neurodevelopmental syndrome.
Hopkin, R; Pedapati, E; Shillington, A; Suhrie, K, 2020
)
0.56
" We used the Generalized Propensity Score method to evaluate the dose-response risk of Parkinsonism associated with SGAs."( Comparative risk of Parkinsonism associated with olanzapine, risperidone and quetiapine in older adults-a propensity score matched cohort study.
Chyou, TY; Nishtala, PS; Nishtala, R, 2020
)
0.8
" Effect sizes between groups were pooled and stratified by single or multiple dosing regimens."( CYP2D6 Genetic Polymorphisms and Risperidone Pharmacokinetics: A Systematic Review and Meta-analysis.
Allen, JD; Bishop, JR; Brown, SJ; de Leon, J; Eum, S; Lee, AM; Shan, Y; Zhang, L, 2020
)
0.84
" The results from the literature underline the necessity of caution and patient monitoring when risperidone dosing is modified during methylphenidate therapy."( Movement disorders and use of risperidone and methylphenidate: a review of case reports and an analysis of the WHO database in pharmacovigilance.
Burden, AM; Stämpfli, D; Weiler, S, 2021
)
1.13
" Regression and dose-response models were utilized to identify the threshold dose (maximum daily dose)."( Discontinuation of antipsychotics treatment for elderly patients within a specialized behavioural unit: a retrospective review.
Gao, RL; Lim, KS; Luthra, AS, 2021
)
0.62
"Lithium was given for mood stabilization and decreased dosage of prior antidepressant medication."( Manic episode in patient with bipolar disorder and recent multiple sclerosis diagnosis: A case report.
Wichser, L; Yang, S, 2020
)
0.56
"Proteinoid NPs enhance RSP delivery and may potentially increase drug efficiency by reducing dosage and side effects."( Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity.
Einat, H; Grinberg, I; Lugasi, L; Margel, S; Okun, E; Rudnick-Glick, S, 2020
)
0.8
"In Iran, the most important challenges these patients faced with are as follows: the absence of a specific referral center, patients resort to self-treatment or traditional methods, and lack of a certain duration and dosage of antipsychotic for these cases."( A comprehensive entomological survey and evaluation of the efficacy of different therapies on a suspected delusional parasitosis case.
Soltan-Alinejad, P; Soltani, A; Turki, H; Vahedi, M, 2021
)
0.62
"25 mg/day (85 years, MMSE of 5), to 1 mg/day (75 years, MMSE of 15), with alternate day dosing required for those with slower drug clearance."( Towards safer risperidone prescribing in Alzheimer's disease.
Bertrand, J; Bies, R; Bramon, E; Howard, R; Liu, KY; Otani, Y; Ozer, M; Pollock, BG; Reeves, S; Uchida, H; Yoshida, K, 2021
)
0.98
" Additional prospective studies with accurate dosage information are needed to validate our findings."( Occurrence of metabolic diseases associated with antipsychotic use among Korean patients with schizophrenia.
Kim, BH; Kim, E; Kim, S; Kuk, S; Lee, W; Park, SI, 2021
)
0.62
" Dosing strategies, discontinuation considerations, and side effects are discussed."( The Psychopharmacology Algorithm Project at the Harvard South Shore Program: An update on management of behavioral and psychological symptoms in dementia.
Chen, A; Cloutier, A; Copeli, F; Metzger, E; Osser, DN, 2021
)
0.62
" Avoiding amisulpride and warning against increasing the dosage in renal failure is the only recommendation by drug manufacturers and clinical guidelines."( Antipsychotics and hemodialysis: A systematic review.
Atlani, MK; Chaudhary, P; Sutar, R, 2021
)
0.62
"Findings of the review reveals modest evidence favoring multiple dosing regimens of oral aripiprazole, ziprasidone, olanzapine, and risperidone."( Antipsychotics and hemodialysis: A systematic review.
Atlani, MK; Chaudhary, P; Sutar, R, 2021
)
0.83
" However, its bitter taste and dose adjustment of liquid dosage forms are a main hurdle for patient acceptance."( Novel risperidone orally disintegrating minitablets for pediatric use: patient acceptance and dose adjustment.
Abdallaha, OY; Bebawy, G; Sokar, M, 2021
)
1.1
" Atypical antipsychotic dosages were standardized using a defined daily dose, and the cumulative dosage was calculated."( Atypical Antipsychotics Augmentation in Patients with Depressive Disorder and Risk of Subsequent Dementia: A Nationwide Population-Based Cohort Study.
Ha, TH; Kim, DK; Kim, H; Kim, J; Kim, K; Lee, EM; Lee, H; Lewis, M; Myung, W; Won, HH, 2021
)
0.62
" A cumulative dose-response relationship was observed (test for trend, p < 0."( Atypical Antipsychotics Augmentation in Patients with Depressive Disorder and Risk of Subsequent Dementia: A Nationwide Population-Based Cohort Study.
Ha, TH; Kim, DK; Kim, H; Kim, J; Kim, K; Lee, EM; Lee, H; Lewis, M; Myung, W; Won, HH, 2021
)
0.62
"The data of 161 women were obtained from the Risperidone Maintenance Treatment in Schizophrenia study, including patients' characteristics, menstrual conditions, and duration and dosage of risperidone."( Menstrual Dysfunction in Women With Schizophrenia During Risperidone Maintenance Treatment.
Bo, Q; Li, T; Mao, Z; Wang, C; Xing, X; Zhou, F,
)
0.64
" The participants had drug dosage adjustment based on body weight/dose (mg/kg)."( Methylphenidate decreases the EEG mu power in the right primary motor cortex in healthy adults during motor imagery and execution.
Aprigio, D; Basile, LF; Bastos, VH; Bittencourt, J; Budde, H; Cagy, M; Gongora, M; Marinho, V; Ribeiro, P; Teixeira, S; Velasques, B, 2021
)
0.62
" Risperidone has weight-based dosing and a liquid dosage form available, making it a good option for use in the NICU."( Delirium in the NICU: Risk or Reality?
Liviskie, C; McPherson, C, 2021
)
1.53
" The supramolecular adduct of RSP with RM-β-CD represents a valuable candidate for further research in developing new formulations with enhanced bioavailability and stability, and the results of this study allow a pertinent selection of three excipients that can be incorporated in solid dosage forms."( Risperidone/Randomly Methylated β-Cyclodextrin Inclusion Complex-Compatibility Study with Pharmaceutical Excipients.
Barvinschi, P; Cîrcioban, D; Ledeți, A; Ledeți, I; Miclău, M; Sbârcea, L; Suciu, O; Tănase, IM; Văruţ, RM; Vlase, G, 2021
)
2.06
"Antipsychotic (AP) dosing is well established in nonelderly patients with acute exacerbations of schizophrenia, but not in special populations."( Dosing antipsychotics in special populations of patients with schizophrenia: severe psychotic agitation, first psychotic episode and elderly patients.
Baloche, E; Blin, O; Bourgin-Duchesnay, J; Corruble, E; Ferreri, F; Garay, RP; Llorca, PM; Mouaffak, F; Vandel, P; Vidailhet, P, 2021
)
0.62
"To investigate the relationship between patient age and the selection and dosage of antipsychotic drugs (APDs) for treatment of schizophrenia."( Antipsychotic drug treatment of schizophrenia in later life: Results from the European cross-sectional AMSP study.
Bleich, S; Dahling, V; Greiner, T; Grohmann, R; Heinze, M; Ramin, T; Schneider, M; Seifert, J; Toto, S; Zindler, T; Zolk, O, 2022
)
0.72
" APD selection and dosage were related to patient age with sex as an influencing variable."( Antipsychotic drug treatment of schizophrenia in later life: Results from the European cross-sectional AMSP study.
Bleich, S; Dahling, V; Greiner, T; Grohmann, R; Heinze, M; Ramin, T; Schneider, M; Seifert, J; Toto, S; Zindler, T; Zolk, O, 2022
)
0.72
" The dosage of APDs increased with age until about age 40 years, then decreased slowly at first and more steeply beyond age 55 years."( Antipsychotic drug treatment of schizophrenia in later life: Results from the European cross-sectional AMSP study.
Bleich, S; Dahling, V; Greiner, T; Grohmann, R; Heinze, M; Ramin, T; Schneider, M; Seifert, J; Toto, S; Zindler, T; Zolk, O, 2022
)
0.72
"In clinical routine, age has a significant impact on selection and dosing of APDs."( Antipsychotic drug treatment of schizophrenia in later life: Results from the European cross-sectional AMSP study.
Bleich, S; Dahling, V; Greiner, T; Grohmann, R; Heinze, M; Ramin, T; Schneider, M; Seifert, J; Toto, S; Zindler, T; Zolk, O, 2022
)
0.72
" Previous studies have related more frequent dosing to poor medication adherence."( Time to Rehospitalization for Different Oral Risperidone Dosing Frequencies in Patients With Schizophrenia: A 17-Year Retrospective Cohort Study.
Chan, HY; Lin, CH; Wang, XY,
)
0.39
"There were 1504 patients grouped by daily dosing frequency of oral risperidone."( Time to Rehospitalization for Different Oral Risperidone Dosing Frequencies in Patients With Schizophrenia: A 17-Year Retrospective Cohort Study.
Chan, HY; Lin, CH; Wang, XY,
)
0.63
"Risperidone and aripiprazole with no dosage restrictions."( Risperidone and aripiprazole for autism spectrum disorder in children: an overview of systematic reviews.
Chen, MH; Escobar Liquitay, CM; Fieiras, C; Franco, JVA; Madrid, E; Meza, N; Rojas, V, 2023
)
3.8
" A population pharmacokinetic (PPK) modeling and simulation approach was implemented to identify TV-46000 doses and dosing schedules for clinical development that would provide the best balance between clinical efficacy and safety."( Population Pharmacokinetic Modeling and Simulation of TV-46000: A Long-Acting Injectable Formulation of Risperidone.
Elgart, A; Gomeni, R; Harary, E; Kalmanczhelyi, A; Lamson, M; Levi, M; Loupe, P; Merenlender Wagner, A; Perlstein, I; Spiegelstein, O; Tiver, R, 2022
)
0.94
" For 25 years, this author has focused on a circumscribed type of precision medicine: personalized dosing using pharmacokinetic mechanisms to stratified patients."( Precision psychiatry: The complexity of personalizing antipsychotic dosing.
de Leon, J, 2022
)
0.72
"Twenty-eight patients were consecutively recruited and treated with SRI (drug(s) and doses previously administered), SGA (risperidone median dosage 1 mg/day in 14 cases, aripiprazole median dosage 3 mg/day in 14 cases) and CBT/ERP (median hours 32."( Serotonin reuptake inhibitor-cognitive behavioural therapy-second generation antipsychotic combination for severe treatment-resistant obsessive-compulsive disorder. A prospective observational study.
Balestrini, V; Cieri, L; Di Spigno, D; Iommi, M; Necci, R; Orazi, F; Salvati, L; Tundo, A, 2022
)
0.93
" Despite no statistically significant differences between groups regarding clinical efficacy, aripiprazole required higher chlorpromazine equivalent dosage (χ 2 = 2."( Aripiprazole vs Risperidone Head-to-Head Effectiveness in First-Episode Non-Affective-Psychosis: A 3-Month Randomized, Flexible-Dose, Open-Label Clinical Trial.
Ayesa-Arriola, R; Crespo-Facorro, B; Garrido-Sánchez, L; Gómez-Revuelta, M; Juncal-Ruiz, M; Mayoral-Van Son, J; Ortiz-García de la Foz, V; Pelayo-Terán, JM; Ruiz-Veguilla, M; Vázquez-Bourgon, J, 2022
)
1.07
"The effects of antipsychotic drugs are dose-dependent, which is particularly true for their efficacy, each antipsychotic having a specific dose-response curve."( Comorbidities and the right dose: antipsychotics.
Azorin, JM; Simon, N; Torrents, R,
)
0.13
"Factors liable to impact antipsychotic dosage are numerous and their subsequent effects often hard to predict, due to multilevel interactions and compensatory phenomena."( Comorbidities and the right dose: antipsychotics.
Azorin, JM; Simon, N; Torrents, R,
)
0.13
" ISM® technology applied to risperidone allows therapeutic levels of the active moiety to be achieved within 2 h of intramuscular administration without the need for loading doses or oral supplementation, leading to a constant release over the whole dosing period."( Risperidone ISM as a New Option in the Clinical Management of Schizophrenia: A Narrative Review.
Álamo, C, 2022
)
2.46
" In the TDM group, physicians will receive dosing advice based on plasma levels of risperidone and aripiprazole and its metabolites at 4 and 10 weeks."( The effect of therapeutic drug monitoring of risperidone and aripiprazole on weight gain in children and adolescents: the SPACe 2: STAR (trial) protocol of an international multicentre randomised controlled trial.
de Winter, BCM; Dierckx, B; Hermans, RA; Hillegers, MHJ; Kloosterboer, SM; Koch, BCP; Liang, K; Ringeling, LT, 2022
)
1.21
" Our constructed PBPK model can predict risperidone and paliperidone pharmacokinetics in pregnant and neonatal populations, which could help with precision dosing using the PBPK model-informed approach in special populations."( Physiologically-based pharmacokinetic model to investigate the effect of pregnancy on risperidone and paliperidone pharmacokinetics: Application to a pregnant woman and her neonate.
Fujioka, K; Fujiwara, N; Horai, T; Iijima, K; Imafuku, H; Ito, T; Mahdy, WYB; Omura, T; Otsuka, I; Yamamoto, K; Yano, I, 2023
)
1.4
" In the two studies, estimated increased risks of breast cancer were disconcertingly high (up to 62%), but a third recent study found only a weak dose-response association."( Association between long-term use of prolactin-elevating antipsychotics in women and the risk of breast cancer: What are the clinical implications?
Copolov, DL; Hope, JD; Keks, NA, 2023
)
0.91
"The study design included 3 phases of treatment: an oral run-in to establish tolerability to risperidone (1 week), lead-in treatment with flexibly dosed PP1M to identify a stable dose (17 weeks) and maintenance treatment with PP3M (24 weeks)."( Feasibility study to evaluate capabilities for conducting psychiatric clinical research within the Rwandan mental healthcare system.
Abraham, E; Alphs, L; Bizoza, R; Damascene Iyamuremye, J; Hooker, E; Kayiteshonga, Y; Keenan, A; Mancevski, B; Schotte, A; Smith-Swintosky, V; Turkoz, I, 2023
)
1.13
" We applied one-stage random-effects dose-response meta-analyses using restricted cubic splines to model the dose-response relationships."( Antipsychotic-induced akathisia in adults with acute schizophrenia: A systematic review and dose-response meta-analysis.
Burschinski, A; Davis, JM; Leucht, S; Priller, J; Schneider-Thoma, J; Siafis, S; Wang, D; Wu, H, 2023
)
0.91
"The LAI landscape has evolved significantly in the last decade with more formulations available, longer dosing intervals, and extended indications."( Switching to long-acting injectable antipsychotics: pharmacological considerations and practical approaches.
Correll, CU; Højlund, M,
)
0.13
" However, only the max dosage (4 mg) of risperidone showed meaningful improvement in increasing mechanical allodynia."( The effect of risperidone on behavioral reactions and gene expression of pro- and anti-inflammatory cytokines in neuropathic pain model induced by chronic constriction injury of the sciatic nerve in rat.
Banafshe, HR; Haddad Kashani, H; Haghighat Lari, MM; Seyed Hosseini, E, 2023
)
1.54
" This is the first reported case where 1 mg/day dosage of risperidone in nursing mother was associated with acute adverse effects such as respiratory depression in her neonate."( Risperidone-induced respiratory depression in a neonate through breast milk.
Appikatla, MB; Babu, TA; Pasi, R,
)
1.82
" We extracted the following data: author, year, country, diagnostic criteria, sample size, course of treatment, dosage and outcomes."( Efficacy and safety of blonanserin versus risperidone in the treatment of schizophrenia: a systematic review and meta-analysis of randomized controlled trials.
Deng, SW; Hong, B; Jiang, WL; Li, BH; Sun, DW; Xu, Q; Yang, HB, 2023
)
1.17
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (7)

RoleDescription
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
alpha-adrenergic antagonistAn agent that binds to but does not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous alpha-adrenergic agonists. alpha-Adrenergic antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
H1-receptor antagonistH1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
second generation antipsychoticAntipsychotic drugs which can have different modes of action but which tend to be less likely than first generation antipsychotics to cause extrapyramidal motor control disabilities such as body rigidity or Parkinson's disease-type movements.
dopaminergic antagonistA drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists.
psychotropic drugA loosely defined grouping of drugs that have effects on psychological function.
EC 3.4.21.26 (prolyl oligopeptidase) inhibitorAny EC 3.4.21.* (serine endopeptidase) inhibitor that interferes with the action of prolyl oligopeptidase (EC 3.4.21.26).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
pyridopyrimidineAny organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
heteroarylpiperidine
1,2-benzoxazolesCompounds based on a fused 1,2-oxazole and benzene bicyclic ring skeleton, with the O atom positioned adjacent to one of the positions of ring fusion.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (96)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.12510.631035.7641100.0000AID504339
acetylcholinesteraseHomo sapiens (human)Potency12.09800.002541.796015,848.9004AID1347395; AID1347398
thioredoxin reductaseRattus norvegicus (Norway rat)Potency15.00300.100020.879379.4328AID588453
TDP1 proteinHomo sapiens (human)Potency24.80330.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency30.04740.000221.22318,912.5098AID1259243; AID1259247
Smad3Homo sapiens (human)Potency15.84890.00527.809829.0929AID588855
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.94330.001318.074339.8107AID926
EWS/FLI fusion proteinHomo sapiens (human)Potency33.17340.001310.157742.8575AID1259252
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency14.25050.001530.607315,848.9004AID1224848; AID1224849; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.52070.000229.305416,493.5996AID1259244; AID1259248; AID743080; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency2.75400.00108.379861.1304AID1645840
thyroid stimulating hormone receptorHomo sapiens (human)Potency29.84930.001628.015177.1139AID1259385
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency5.55280.00207.533739.8107AID891
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency75.686323.934123.934123.9341AID1967
cytochrome P450 2C19 precursorHomo sapiens (human)Potency1.58490.00255.840031.6228AID899
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.81460.01789.637444.6684AID588834
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency3.98110.794321.275750.1187AID624246
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency26.60110.000627.21521,122.0200AID743202; AID743219
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency32.19680.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency1.25890.125912.234435.4813AID1458
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency15.18610.00106.000935.4813AID943; AID944
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency21.13170.001557.789015,848.9004AID1259244
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency21.13170.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)11.00000.40003.10009.7000AID721751
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)34.20000.00032.63119.0000AID1207767
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.01500.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.04940.00000.887110.0000AID5836; AID625218
Bile salt export pumpHomo sapiens (human)IC50 (µMol)92.75000.11007.190310.0000AID1443980; AID1449628; AID1473738
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki5.00000.00000.690210.0000AID141100
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki5.00000.00000.79519.1201AID141100
Cytochrome P450 3A4Homo sapiens (human)Ki0.22400.00011.41629.9000AID599884
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.31840.00010.532610.0000AID1169862; AID1393366; AID1724108; AID1762056; AID298481; AID342783; AID3657; AID4442
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)0.00270.00040.629810.0000AID4782; AID4803; AID4812; AID5061
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.01900.00020.667710.0000AID1335641; AID1409483; AID1704720; AID5246
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki5.00000.00000.72926.9183AID141100
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00970.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.01020.00010.807410.0000AID1724111; AID238989; AID36197; AID36199; AID625201
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)5.27340.00002.015110.0000AID625249
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki4.26670.00000.59729.1201AID141100; AID141174; AID342774
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)4.19010.00001.612910.0000AID625171
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki3.43280.00042.03378.6606AID625171
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.01670.00000.74728.0000AID1462313; AID61049; AID625253
D(2) dopamine receptorHomo sapiens (human)Ki0.00380.00000.651810.0000AID1062948; AID1169860; AID1393368; AID1691230; AID1724107; AID1762054; AID239052; AID298478; AID342777; AID439064; AID625253; AID63060; AID63070; AID63971; AID64327; AID714109
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)0.09910.00040.908610.0000AID4782; AID4803; AID4812; AID5061; AID5479; AID750648
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00030.00010.601710.0000AID1335644; AID1409481; AID1704718; AID410335; AID5246; AID5324; AID5328; AID5337; AID5504; AID5522
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.01870.00010.949010.0000AID1335646; AID1409484; AID1704719; AID238991; AID298478; AID36016; AID3657; AID37455
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.02600.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.00710.00020.725710.0000AID36197; AID36199; AID625202
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki22.00000.00000.667310.0000AID40406
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00960.00001.47257.8980AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.00350.00030.483410.0000AID238990; AID36197; AID36199; AID625203
DRattus norvegicus (Norway rat)Ki0.06030.00010.610010.0000AID238855; AID410331; AID61499
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.03190.00010.25675.8000AID1409486
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.79900.00031.38338.4000AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.36900.00010.739610.0000AID1335643; AID1409480; AID1704717; AID3992; AID4357; AID625190
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00370.00000.929610.0000AID750653
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50 (µMol)55.00000.00011.01049.9280AID1403798; AID1659273
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki5.00000.00000.54057.7600AID141100
D(1A) dopamine receptorHomo sapiens (human)IC50 (µMol)0.47900.00031.84739.2250AID625252
D(1A) dopamine receptorHomo sapiens (human)Ki0.32180.00010.836310.0000AID342775; AID439068; AID625252; AID63345; AID63347
D(4) dopamine receptorHomo sapiens (human)Ki0.01060.00000.436210.0000AID298480; AID342779; AID61808; AID63524; AID63537; AID65954
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.00370.00000.970810.0000AID750653
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01440.00000.937510.0000AID35637; AID750653
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.01870.00000.575110.0000AID1335646; AID1409484; AID1704719; AID238991; AID298478; AID36016; AID3657; AID37455
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.03100.00030.37088.1600AID64984
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)1.48300.02202.298710.0000AID625270
Histamine H2 receptorHomo sapiens (human)Ki1.45800.00062.197310.0000AID625270
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01000.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.00530.00000.360910.0000AID1682829; AID1724114; AID36113; AID36116; AID36122; AID625200
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.00160.00010.88018.8500AID1462315; AID1570293; AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.00040.00000.385510.0000AID1062949; AID1152668; AID1169863; AID1393364; AID1570286; AID1691231; AID1724109; AID1762057; AID239010; AID298482; AID308685; AID342784; AID439066; AID5197; AID5199; AID5363; AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.00570.00011.03029.0000AID1301294; AID1373837; AID1403795; AID1462318; AID1659274; AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.02710.00010.954910.0000AID1169864; AID1724113; AID1762058; AID239069; AID298485; AID308686; AID342781; AID439070; AID5614; AID5616; AID5831; AID5835; AID5836; AID5951; AID599883; AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.79900.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.45700.00031.29679.2440AID625190
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)0.00270.00040.615610.0000AID4782; AID4803; AID4812; AID5061
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.00020.00020.590910.0000AID5246
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.03760.00261.783210.0000AID1335645; AID1704721
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.40000.00000.70488.1930AID342787
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.02100.00000.14803.1800AID1704722; AID6648
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)IC50 (µMol)0.00150.00150.01480.0280AID5020
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.00190.00030.380610.0000AID1393367; AID239149; AID298487
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01050.00020.56145.4000AID1301292; AID1373835; AID1403797; AID1462316; AID1659265
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00500.00000.272610.0000AID1682829; AID1724114; AID1762060; AID36113; AID36116; AID36122
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC50 (µMol)0.00150.00150.01480.0280AID5020
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)0.45150.00000.44365.1768AID1301293; AID1373836; AID1403796; AID1462317; AID1659275; AID625269
Histamine H1 receptorHomo sapiens (human)Ki0.03090.00000.511010.0000AID1682828; AID1724112; AID1762061; AID239091; AID342782; AID625269; AID87242; AID87244
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.00530.00000.471310.0000AID1682829; AID1724114; AID36113; AID36116; AID36122
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)0.02400.00011.01788.7960AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.01320.00000.602010.0000AID1169861; AID1762055; AID239150; AID298479; AID342778; AID410333; AID439069; AID625254; AID64984; AID65121; AID65785
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.02300.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.01750.00030.769310.0000AID298483; AID625217
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01750.00000.965010.0000AID1335646; AID1409484; AID1704719; AID238991; AID298478; AID36016; AID3657; AID36890; AID37455
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.21240.00020.522910.0000AID1335640; AID1393365; AID1409485; AID1704723; AID1724110; AID1762059; AID342773; AID599884
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.03300.00100.01630.0330AID599883
D(2) dopamine receptorMus musculus (house mouse)IC50 (µMol)0.02300.00090.47332.4310AID61049
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01540.00010.54948.4000AID61388; AID64264; AID64296
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00480.00000.437510.0000AID1335642; AID1704716; AID239086; AID410332; AID63804; AID63811; AID63822; AID65243; AID65402; AID65713; AID750653
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)34.20000.00032.59559.0000AID1207767
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC50 (µMol)0.00150.00150.01480.0280AID5020
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.63030.00091.901410.0000AID1207230; AID1301295; AID1403799; AID1409487; AID1462319; AID161281; AID1659272; AID1704724; AID1762063; AID222148; AID240820; AID243188; AID397743; AID408340; AID420668; AID576612; AID625171; AID750648
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki2.17640.00211.840710.0000AID410338; AID625171
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)34.20000.00032.63119.0000AID1207767
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)79.60000.00032.25459.6000AID1207698; AID1207767
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)102.00000.00033.64849.2000AID1207171
TransporterRattus norvegicus (Norway rat)Ki28.00000.00010.76295.5000AID342786
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC50 (µMol)0.43000.00210.35812.0000AID3960
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC50 (µMol)4.19010.10482.83988.3173AID625171
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki3.43280.08582.95428.6606AID625171
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50 (µMol)291.00000.16003.95718.6000AID721752
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)1.60000.01002.765610.0000AID721754
TransporterRattus norvegicus (Norway rat)Ki5.45400.00010.866710.0000AID238962
Histamine H3 receptorHomo sapiens (human)Ki1.10550.00010.33998.5110AID1762062
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AlbuminRattus norvegicus (Norway rat)Kd43.80001.47006.53179.3100AID1215123
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC50 (µMol)10.00000.00010.25718.0000AID1462314
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.39810.00010.95285.0119AID438555
Glycine receptor subunit alpha-1Homo sapiens (human)EC50 (µMol)0.32000.32001.45774.2000AID1203550
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent translocase ABCB1Homo sapiens (human)Km12.40000.01403.717210.0000AID681619
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (524)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
startle responseGlycine receptor subunit alpha-1Homo sapiens (human)
regulation of membrane potentialGlycine receptor subunit alpha-1Homo sapiens (human)
startle responseGlycine receptor subunit alpha-1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processGlycine receptor subunit alpha-1Homo sapiens (human)
monoatomic ion transportGlycine receptor subunit alpha-1Homo sapiens (human)
chloride transportGlycine receptor subunit alpha-1Homo sapiens (human)
muscle contractionGlycine receptor subunit alpha-1Homo sapiens (human)
neuropeptide signaling pathwayGlycine receptor subunit alpha-1Homo sapiens (human)
acrosome reactionGlycine receptor subunit alpha-1Homo sapiens (human)
visual perceptionGlycine receptor subunit alpha-1Homo sapiens (human)
adult walking behaviorGlycine receptor subunit alpha-1Homo sapiens (human)
neuronal action potentialGlycine receptor subunit alpha-1Homo sapiens (human)
neuromuscular process controlling postureGlycine receptor subunit alpha-1Homo sapiens (human)
negative regulation of transmission of nerve impulseGlycine receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, glycinergicGlycine receptor subunit alpha-1Homo sapiens (human)
righting reflexGlycine receptor subunit alpha-1Homo sapiens (human)
excitatory postsynaptic potentialGlycine receptor subunit alpha-1Homo sapiens (human)
inhibitory postsynaptic potentialGlycine receptor subunit alpha-1Homo sapiens (human)
cellular response to amino acid stimulusGlycine receptor subunit alpha-1Homo sapiens (human)
cellular response to zinc ionGlycine receptor subunit alpha-1Homo sapiens (human)
cellular response to ethanolGlycine receptor subunit alpha-1Homo sapiens (human)
response to alcoholGlycine receptor subunit alpha-1Homo sapiens (human)
regulation of presynaptic membrane potentialGlycine receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGlycine receptor subunit alpha-1Homo sapiens (human)
positive regulation of acrosome reactionGlycine receptor subunit alpha-1Homo sapiens (human)
chemical synaptic transmissionGlycine receptor subunit alpha-1Homo sapiens (human)
regulation of membrane potentialGlycine receptor subunit alpha-1Homo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (156)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
transmembrane signaling receptor activityGlycine receptor subunit alpha-1Homo sapiens (human)
protein bindingGlycine receptor subunit alpha-1Homo sapiens (human)
zinc ion bindingGlycine receptor subunit alpha-1Homo sapiens (human)
glycine bindingGlycine receptor subunit alpha-1Homo sapiens (human)
extracellularly glycine-gated chloride channel activityGlycine receptor subunit alpha-1Homo sapiens (human)
taurine bindingGlycine receptor subunit alpha-1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlycine receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlycine receptor subunit alpha-1Homo sapiens (human)
neurotransmitter receptor activityGlycine receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGlycine receptor subunit alpha-1Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activityGlycine receptor subunit alpha-1Homo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (91)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membraneGlycine receptor subunit alpha-1Homo sapiens (human)
external side of plasma membraneGlycine receptor subunit alpha-1Homo sapiens (human)
membraneGlycine receptor subunit alpha-1Homo sapiens (human)
dendriteGlycine receptor subunit alpha-1Homo sapiens (human)
neuron projectionGlycine receptor subunit alpha-1Homo sapiens (human)
neuronal cell bodyGlycine receptor subunit alpha-1Homo sapiens (human)
perikaryonGlycine receptor subunit alpha-1Homo sapiens (human)
intracellular membrane-bounded organelleGlycine receptor subunit alpha-1Homo sapiens (human)
synapseGlycine receptor subunit alpha-1Homo sapiens (human)
postsynaptic membraneGlycine receptor subunit alpha-1Homo sapiens (human)
inhibitory synapseGlycine receptor subunit alpha-1Homo sapiens (human)
glycinergic synapseGlycine receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGlycine receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGlycine receptor subunit alpha-1Homo sapiens (human)
synapseGlycine receptor subunit alpha-1Homo sapiens (human)
neuron projectionGlycine receptor subunit alpha-1Homo sapiens (human)
plasma membraneGlycine receptor subunit alpha-1Homo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (788)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID63366In vitro affinity against Dopamine receptor D1; No data2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID1393367Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
AID298491Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID141153Binding affinity measured at the Muscarinic acetylcholine receptor by the inhibition of [3H]-pyrilamine binding to guinea pig cerebellum using unlabeled Triprolidine for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1462315Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID5485Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1332853Toxicity in Sprague-Dawley rat assessed as cataleptogenic effect by measuring time spent in cataleptic position at 1 to 10 mg/kg, po measured after 0.5 to 2 hrs2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.
AID177887Inhibition of apomorphine-induced stereotypy in rats.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID4782Binding affinity towards serotonin 5-HT2 receptor was determined in rat cortex using [3H]spiperone as ligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1256663Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1071727Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID238991Inhibition of [3H]prazosin binding to rat Alpha-1 adrenergic receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1462319Inhibition of human ERG2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID420787Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors.
AID1762059Binding affinity to 5-HT6 receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID298480Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID63822In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID1301294Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID239010Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1393368Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
AID176734Dose (administered orally) inhibiting apomorphine-induced stereotypy in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1762072Toxicity in mouse assessed as effect on serum prolactin level at 0.05 to 1.35 mg/kg administered for 28 days2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1301295Inhibition of human ERG after 10 mins2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID1335641Displacement of [3H]mesulergine from 5-HT2C receptor in Sprague-Dawley rat cerebral cortex incubated for 15 mins in presence of spiperone by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID3730Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1724111Binding affinity to alpha2 adrenergic receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1762071Chronic toxicity in mouse assessed as change in body weight at 0.05 to 1.35 mg/kg administered for 28 days2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1210227Total brain to plasma partition coefficient of the compound in wild type Sprague-Dawley rat expressing Abcb1a at 5 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID410135Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg measured on 20 mins2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID1335651Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed Chinese Kun Ming mouse to ED50 for inhibition of apomorphine-induced climbing behavior in po dosed Chinese Kun Ming mouse2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID36122The compound was tested against Alpha-1 adrenergic receptor for percent displacement of radioligand at 10e-6 M1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID5836In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID1209294AUC(0 to 1 hr) in cynomolgus monkey brain at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1704750Toxicity in po dosed Kunming mouse assessed as catalepsy
AID239069Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID298490Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1677164In vivo receptor occupancy at human dopamine D2 receptor in schizophrenia patient brain at 10 mCi, iv by PET scanning
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1462314Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID5197Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID705400Antipsychotic activity in sc dosed rat by conditioned avoidance response test2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID308686Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1462321Metabolic stability in human liver microsomes assessed as parent compound remaining at 2 uM after 60 mins in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID750655Displacement of [3H]prazosin from alpha-1 adrenergic receptor in rat cerebral cortex after 60 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1335646Displacement of [3H]prazosin from adrenergic alpha1 receptor in Sprague-Dawley rat cerebral cortex incubated for 60 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID36199Binding affinity towards human alpha-2 adrenergic receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID176251Intracranial self stimulation in rat was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1210170Unbound brain to plasma partition coefficient of the compound in wild type Sprague-Dawley rat expressing Abcb1a at 5 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID342777Binding affinity to human cloned dopamine D2 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID410136Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg measured on 30 mins2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID1211445Equilibration rate constant in Wistar rat brain extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1211430Uptake clearance in Wistar rat brain extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID61623Binding affinity to the dopamine receptor D2L in rat brain membranes1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID1210226Total drug level in wild type Sprague-Dawley rat brain expressing Abcb1a at 5 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1403799Inhibition of human ERG by auomated patch clamp assay
AID301868Selectivity ratio of pKi for rat brain 5HT2A receptor to pKi for rat brain dopamine D2 receptor2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID176735Dose (administered orally) inhibiting spontaneous locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1256676Toxicity in po dosed Chinese Kun Ming mouse assessed as induction of catalepsy by measuring immobility score of 30 seconds administered 30 mins before first assessment2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1335648Inhibition of MK-801 induced hyperactivity in po dosed Chinese Kun Ming mouse administered for 60 mins followed by MK-801 challenge and measured for 90 mins2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1211409Cmax in Wistar rat extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1256670Displacement of [3H]mesulergine from 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1704747Antipsychotic activity in Kunming mouse assessed as inhibition of apomorphine-induced climbing behavior administered orally 30 mins prior to apomorphine challenge and measured for 10 to 30 mins
AID593483Displacement of [3H]-Spiperone from human dopamine D2L receptor expressed in CHO cells at 4 times IC50 for 5 mins measured after 60 mins by topcount scintillation counting2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Molecular properties affecting fast dissociation from the D2 receptor.
AID1691231Antagonist activity at 5HT2A receptor (unknown origin)2020European journal of medicinal chemistry, May-01, Volume: 193Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.
AID750624Antipsychotic activity in po dosed mouse assessed as reduction in apomorphine-induced climbing behavior administered for 30 mins prior to apomorphine-challenge measured at 10 to 30 mins post-dose2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID180343The compound was measured at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat via oral administration.1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1071729Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1211460Unbound Tmax in Wistar rat plasma at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID343685Ratio of drug level in brain to blood in Wistar rat2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Toward prediction of alkane/water partition coefficients.
AID87242Binding affinity towards human histamine H1 receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1409509Antipsychotic activity in po dosed Kunming mouse assessed as reduction in apomorphine-induced climbing pretreated for 30 mins followed by apomorphine injection measured at 10 to 30 mins post dose2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1203550Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
AID1203552Modulation of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as effect on acetylcholine-induced currents at 10 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
AID1570294Competitive antagonist activity at human D2S receptor expressed in CHOK1 cells assessed as quinpirole mediated inhibition of forskolin induced cAMP accumulation by measuring parallel rightward shifts of quinpirole concentration-response curves incubated f
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID176733Dose (administered orally) inhibiting amphetamine-induced locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1704716Displacement of [3H]spiperone from D2 receptor in rat striatum measured after 15 mins by liquid scintillation counting method
AID36730Its affinity towards alpha-1 receptor using [3H]WB-4101 as radioligand in whole brain minus cerebellum1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID229631Selectivity ratio for serotonin 5-HT2C to that of serotonin 5-HT2A receptors2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID1335650Induction of catalepsy in po dosed Chinese Kun Ming mouse assessed as increase in unwanted extrapyramidal motor disturbances measured for 60 seconds2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1210175Unbound brain to plasma partition coefficient of the compound in mdr1a-deficient rat at 5 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID229447Selectivity ratio between serotonin 5-HT2A and dopamine D2 receptors was determined; nd=Not determined2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID298492Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1204337Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as total radioligand binding at 1 uM incubated for 60 mins by microbeta plate reader based method2015European journal of medicinal chemistry, Jun-05, Volume: 97Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.
AID1659265Antagonist activity at alpha-1a adrenergic receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID176802In vivo activity administered intraperitoneally was determined by induction of catalepsy in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1209293AUC(0 to 2 hrs) in Beagle dog brain at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID5053Compound was tested for the inhibition of quipazine induced head twitches in rats1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID5504Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID5328Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1403795Antagonist activity at 5-HT2C receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1570293Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
AID1462322Antipsychotic activity in PCP-induced hyperactivity ICR mouse model assessed as inhibition of hyper-locomotion administered ig incubated for 10 mins followed by PCP challenge measured after 10 mins for 75 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID1704719Displacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptor measured after 60 mins by liquid scintillation counting method
AID113872Intraperitoneal effective dose required for inhibition of apomorphine-induced climbing in mice1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1764402Unbound brain-to-plasma concentration ratio in P-gp knock out Sprague-Dawley rat2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID1211427Unbound volume of distribution in Wistar rat brain at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID374353Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport.
AID1393369Selectivity index, ratio of pKi for 5-HT2AR to pKi for human D2LR
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1393364Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method
AID439067Ratio of pKi for human cloned dopamine D2 receptor to pKi for human cloned 5HT2A receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1071726Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID750628Toxicity in mouse assessed as weight gain at 0.06 to 0.16 mg/kg, po for 28 days2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1207697Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID65121Binding affinity towards human dopamine receptor D32001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID1724115Antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing behaviour2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID439070Displacement of [3H]mesulergine from human 5HT2C receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID1062949Displacement of [3H]ketanserin from human 5-HT2A receptor2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.
AID1409480Displacement of [3H]-8-OH-DPAT from serotonin 5-HT1A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID5479In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1211795Dissociation constant, pKa of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID231369Ratio representing inhibitory activity against catalepsy to inhibitory activity against amphetamine-induced locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID4803Compound was measured for affinity at 5-hydroxytryptamine 2 receptor in rat cortical by [3H]spiroperidol displacement.1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID330561Displacement of [3H]mepyramine from H1R in rat brain2007Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
AID1762064Antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing behaviour2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1210218Percentage unbound in Crl:NMRI(Han) mouse plasma at 1 uM after 5 hrs by equilibrium dialysis method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID395329Dissociation constant, pKa by mass spectrometry2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID750649Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID182841Activity administered intraperitoneally was determined by social interaction of rat at 0.5 uM1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID65402Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID63537Binding affinity towards human dopamine receptor D42001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID298486Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID239149Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1211439Ratio of unbound AUC in extracellular fluid to unbound AUC in plasma of Wistar rat at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID5835Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1207171Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID714109Displacement of [3H]methylspiperone from human low affinity Dopamine D2S receptor by competition binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1209374Unbound fraction in Beagle dog brain at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1207261Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID113690Inhibition of p-chloroamphetamine-induced hyperactivity in mice.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID168345Social interaction of rats was determined after 1 hr of intraperitoneal administration at 0.5 mg/kg1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1462318Antagonist activity at 5-HT2C receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID63345Binding affinity against dopamine receptor D12001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID439064Displacement of [3H]spiperone from human cloned dopamine D2 receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID197397compound was tested for antipsychotic activity by conditioned avoidance response(CAR) assay in rats with a pretreatment period of 30 min upon intra peritoneal administration at a concentration of 5 mg/kg.1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID1211451Fraction unbound in Wistar rat plasma at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1704720Displacement of [3H]mesulergine from rat cerebral cortex 5HT2C receptor measured after 15 mins by liquid scintillation counting method
AID65713Displacement of [3H]NPA from rat brain Dopamine receptor D21996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID141100Binding affinity towards human muscarinic receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID247009In vivo effective dose to inhibit apomorphine induced agitation in rats upon subcutaneous administration2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1724110Binding affinity to 5HT6 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID230009Ratio of Ki value towards dopamine D2L receptor to that of D-4 receptor.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID1169864Binding affinity to 5HT2C receptor (unknown origin)2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID64264Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D21992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID5020Inhibitory activity against serotonin 5-hydroxytryptamine 2 receptor from mice.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID681118TP_TRANSPORTER: transepithelial transport in Caco-2 cells2003International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2
Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.
AID1335643Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in Sprague-Dawley rat cerebral cortex incubated for 30 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID176457Pole climb avoiding activity in rats was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1724121Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID61536Binding affinity towards Dopamine receptor D2 was determined in rat striatum using [3H]- spiperone as radioligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1209320Ratio of unbound drug level in brain to plasma in Beagle dog at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID227557In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID61388Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1724108Binding affinity to 5HT1A receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1071723Antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK801-induced hyperactivity compound administered 30 mins prior to MK801 challenge measured for 90 mins post challenge2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1209389AUC(0 to infinity) in Sprague-Dawley rat plasma at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID750651Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID410332Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID5331Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.
AID230011Ratio of Ki value towards dopamine D2L receptor to that of serotonin S-2A receptor.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID65087Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID298493Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral cortex2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID750652Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID65785Binding affinity towards human Dopamine receptor D32004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID36890Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID176805In vivo activity administered intraperitoneally was determined by pole climb escape failures in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1255777Antipsychotic activity in Sprague Dawley rat psychosis model assessed as inhibition of 0.2 mg/kg dizocilpine-induced hyperlocomotion at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured every 5 mins for 1 hr starting from the 15th m2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
AID246918In vivo effective dose to inhibit tryptamine-induced bilateral convulsions in rats2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID231370Ratio representing inhibitory activity against spontaneous locomotor behavior to inhibitory activity against amphetamine-induced stereotypy in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID230492Relative receptor binding affinities for dopamine D2 and serotonin 5-HT21996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID298482Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID5246Affinity for 5-hydroxytryptamine 2 receptor1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID1336516Anti-psychotic activity in C57Bl/6J mouse assessed as inhibition of PCP-induced hyperlocomotion at 0.056 mg/kg, sc pretreated for 30 mins followed by PCP challenge measured for 2 hrs
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID87244Binding affinity towards human H1 receptor2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID1659267Cytotoxicity against human HEK293 cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1211797Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1393474Toxicity in ip dosed Sprague-Dawley rat assessed as induction of catalepsy measured every 30 mins up to 240 mins by bar test
AID1210190Total brain to plasma partition coefficient of the compound in wild type Crl:CF1 mouse expressing Abcb1a mutant at 4 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1210188Total plasma concentration in wild type Crl:CF1 mouse expressing Abcb1a mutant at 4 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1211296Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID178872Compound was tested for the inhibition of quipazine-induced head twitches 24 hours after subcutaneous administration1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID1409485Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1211295Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1210165Unbound brain to plasma partition coefficient of the compound in mdr1a-deficient mouse at 4 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID180551The compound was tested in vivo for induction of catalepsy in rat after ip administration1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1704717Displacement of [3H](+)8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 30 mins by liquid scintillation counting method
AID225180Dose required to induce 50% maximum catalepsy in rat1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID1169863Binding affinity to 5HT2A receptor (unknown origin)2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1209328AUC(0 to 1 hr) in cynomolgus monkey plasma at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID222148K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID1256665Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID714108Displacement of [3H]7-OH-DPAT from human high affinity Dopamine D2S receptor by competition binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID1762062Binding affinity to histamine H3 receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID3699The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1409510Antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK-801-induced hyperactivity pretreated for 60 mins followed by MK-801 challenge measured for 90 mins2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID5199Binding affinity for human 5-hydroxytryptamine 2A receptor2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID298032Acid dissociation constant, pKa of the compound2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID61046Compound was tested in vivo for methyl phenidate-induced gnawing behavior antagonistic activity against dopamine receptor D2 in mice1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID3743Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID397743Inhibition of human ERG channel2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.
AID5061Affinity for 5-hydroxytryptamine 2 receptor binding sites by its ability to displace [3H]spiperone from rat frontal cortex.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1393366Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID246985Effective dose for antagonistic activity against m-chlorophenyl-piperazine induced anxiety in rats2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID4442Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID63060Binding affinity towards human Dopamine receptor D22004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1704718Displacement of [3H]ketanserin from rat cerebral cortex 5HT2A receptor measured after 15 mins by liquid scintillation counting method
AID714094Reduction in spontaneous locomotor activity in Sprague-Dawley rat at 2.4 umol/kg, sc measured after 15 to 60 mins relative to saline-treated control2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID1409481Displacement of [3H]-ketanserine from serotonin 5-HT2A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1373837Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.
AID238962Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID177715In vivo suppression of the conditioned avoidance response (CAR) in rats after po administration of the compound2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID1210225Total plasma concentration in wild type Sprague-Dawley rat expressing Abcb1a at 5 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID705395Antipsychotic activity in sc dosed rat assessed as reversal of MK801-induced prepulse inhibition deficit2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1209373Unbound fraction in Beagle dog plasma at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1409482Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1409528Cognitive enhancing effect in Sprague-Dawley rat assessed as effect on total exploration time for familiar objects in acquisition trial at 0.2 mg/kg, po administered 1 hr measured for 3 mins by novel object recognition test2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID342781Binding affinity to human cloned 5HT2C receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID342787Binding affinity to human SERT2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID410142Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID1578090Unbound brain-to-plasma concentration ratio in rat2019European journal of medicinal chemistry, Nov-15, Volume: 182Practical approaches to evaluating and optimizing brain exposure in early drug discovery.
AID1762067Antipsychotic activity in po dosed rat assessed as suppression in conditioned avoidance response by CAR test2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID238855Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D12005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1762056Binding affinity to 5-HT1A receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID36116Binding affinity towards human alpha-1 adrenergic receptor2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID141174Binding affinity towards human M1 receptor.2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID239091Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor 2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1393481Effect on failure incidence during conditioned avoidance response test in Sprague-Dawley rat at 0.3 mg/kg, ip administered 60 mins prior to testing
AID227559Relative binding affinity for dopamine D2 and alpha receptors1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID110213Ability to inhibit apomorphine-induced climbing behavior in mice.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID177506In vivo inhibition of apomorphine induced stereotypy in rat by the compound administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1677163In vivo receptor occupancy at human dopamine D1 receptor in schizophrenia patient brain at 10 mCi, iv by PET scanning
AID750646Toxicity in rat assessed as QT interval prolongation at 30 mg/kg, po by electrophysiology assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1210189Total drug level in wild type Crl:CF1 mouse brain expressing Abcb1a mutant at 4 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID750619Therapeutic Index, ratio of ED50 for catalepsy in mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperactivity2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1373836Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.
AID225491Compound was tested for antagonist activity against apomorphine-induced mouse climbing(intraperitoneally - ip). using in vivo method1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID439068Displacement of [3H]SCH23390 from human dopamine D1 receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID298489Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID298479Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID187172ED50 value for catalepsy indicates the dose required to produce a 50% of maximum catalepsy score1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1762058Binding affinity to 5-HT2C receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1682828Binding affinity to H1 histamine receptor (unknown origin)
AID1393472Antipsychotic activity in ip dosed Sprague-Dawley rat assessed as suppression of avoidance behavior by avoiding foot shock administered 60 mins prior to test by conditioned avoidance response test
AID1211406AUC (0 to infinity) in Wistar rat extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID342783Binding affinity to human cloned 5HT1A receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID246931In vivo effective dose for reversal of tryptamine-induced backward locomotion in rats2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1256669Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID308688Ratio of pKi for human 5HT2A receptor to pKi for human D2 receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID410338Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID114064Oral effective dose required for inhibition of apomorphine-induced climbing in mice1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1209305Ratio of drug level in cerebrospinal fluid to unbound plasma concentration in cynomolgus monkey at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID246894In vivo effective dose for reversal of RO-4-1284 induced hypothermia in mouse2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID177959Antagonistic activity administered intraperitoneally on head twitches induced by 5- HTP; NT = not tested1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1207698Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1210178Percentage unbound in Crl:NMRI(Han) mouse brain at 1 uM after 5 hrs by equilibrium dialysis method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1211433Efflux clearance in Wistar rat brain extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1704724Inhibition of human ERG expressed in HEK293 cells by whole-cell patch clamp method
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID232560Ratio of ED50 for induction of catalepsy to ED50 for antagonism of apomorphine-induced climbing.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID1211792Hepatic clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID5324In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID298031Lipophilicity, log D at pH7.42007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID1462317Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID36016Displacement of [3H]prazosin from rat brain Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1762054Binding affinity to dopamine D2 receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1207767Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID65954Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID1210240Total plasma concentration in mdr1a-deficient rat at 5 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID5337In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID298488Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID204461Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID5363Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID1724116Antipsychotic activity in po dosed mouse assessed as suppression in DOI-induced head twitching response2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID113687Inhibition of head twitches-induced by 2,5-dimethoxy-4-iodoamphetamine in mice.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1659266Cytotoxicity against human Chang cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID1207230Inhibition of hERG K channel2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1169861Binding affinity to dopamine D3 receptor (unknown origin)2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID705396Antipsychotic activity in sc dosed rat prepulse inhibition model2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID750648Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1393365Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
AID1211298Dissociation constant, pKa of the compound2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1724113Binding affinity to 5HT2C receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1256668Displacement of [3H]-rauwolscine from adrenergic alpha2 receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1724107Binding affinity to D2 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1211294Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID439066Displacement of [3H]ketanserin from human cloned 5HT2A receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID1071722Toxicity in po dosed Kunming mouse assessed as induction of catalepsy2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID298483Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1210182Unbound brain to plasma partition coefficient of the compound in wild type Crl:CF1 mouse expressing Abcb1a mutant at 4 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1764401Ratio of drug concentration in brain to plasma of P-gp knock out Sprague-Dawley rat2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID750621Antipsychotic activity in po dosed rat assessed as reduction in conditioned avoidance response after 60 mins2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID342778Binding affinity to human cloned dopamine D3 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1762066Induction of catalepsy in po dosed mouse by Horizontal grid and elevated bar test2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1764398Substrate activity at P-gp (unknown origin) assessed as net efflux ratio2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID177133In vivo antipsychotic activity measured by the induction of catalepsy in rats after po administration.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1207696Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID714105Displacement of [3H]Ro 41-1049 from MAO-A in rat cerebral cortex by competition binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID1210206Total plasma concentration in mdr1a-deficient mouse at 4 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID113351In vivo effective dose for inhibition of apomorphine-induced climbing in mice after intraperitoneal administration at a dose 20 mg/kg1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1255782Antipsychotic activity in Sprague Dawley rat assessed as inhibition of 1 mg/kg quipazine-induced head twitches at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured for 30 mins2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1659272Inhibition of human ERG2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID1071724Antipsychotic activity in po dosed Kunming mouse assessed as reversal of apomorphine-induced cage climbing response compound administered 30 mins prior to apomorphine challenge measured for 30 mins post challenge2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID218904In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID342774Binding affinity to human cloned muscarinic M1 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1462324Induction of catalepsy in ig dosed ICR mouse assessed as incidence of unwanted extrapyramidal motor disturbances2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID1409483Displacement of [3H]-mesulergine from serotonin 5-HT2C receptor in rat brain cerebral cortex homogenates incubated for 15 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1301291Therapeutic index, ratio of ED50 for toxicity in orally dosed mouse by catalepsy test to ED50 for antipsychotic activity in mouse2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID1409484Displacement of [3H]-prazosin from alpha-1 adrenergic receptor in rat cerebral cortex homogenates incubated for 60 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1209313Ratio of unbound brain concentration to drug level in cerebrospinal fluid in Beagle dog at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1335644Displacement of [3H] ketanserin from 5-HT2A receptor in Sprague-Dawley rat cerebral cortex incubated for 30 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1210208Total brain to plasma partition coefficient of the compound in mdr1a-deficient mouse at 4 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID750622Toxicity in po dosed mouse assessed as induction of catalepsy2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1209367Unbound fraction in cynomolgus monkey plasma at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1659262Agonist activity at D2 receptor (unknown origin) relative to 10 uM dopamine2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID176744Dose inhibiting conditioned avoidance response in rats after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID714104Increase in DOPAC level in sc dosed Sprague-Dawley rat striatum by HPLC analysis2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID1058778Antipsychotic activity in Sprague-Dawley rat psychosis model assessed as inhibition of MK-801-induced hyperlocomotion at 1 mg/kg, ip administered 5 mins prior to MK-801-challenge measured after 15 mins up to 1 hr2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors.
AID1409487Inhibition of human ERG expressed in HEK293 cells at -50 mV holding potential by patch clamp assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID239150Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D32005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1211457Unbound Cmax in Wistar rat plasma at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID113189In vivo antipsychotic activity measured by the inhibition of apomorphine-induced climbing behavior in mice after 30 min po administration.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1409486Displacement of [3H] 7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle homogenates after 60 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID37475Compound was evaluated for its binding affinity with Alpha-1 adrenergic receptor using membranes prepared from rat cerebral cortex1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID1762102Cognitive enhancement effect in rat assessed as effect on total exploration time at 0.05 to 0.3 mg/kg, po administered 1 hr prior to acquisition trial and by novel object recognition test2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1209337Ratio of drug level in brain to plasma in Sprague-Dawley rat at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1211791Fraction unbound in human hepatocytes2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1403797Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
AID1762061Binding affinity to histamine H1 receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID298494Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1462320Metabolic stability in human liver microsomes assessed as parent compound remaining at 2 uM after 30 mins in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID1209327AUC(0 to 2 hrs) in Beagle dog plasma at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1210242Total brain to plasma partition coefficient of the compound in mdr1a-deficient Sprague-Dawley rat at 5 mg/kg/day administered through continuous minipump treatment for 3 days2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1209332AUC(0 to 2 hrs) in Beagle dog cerebrospinal fluid at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID113686Inhibition of grooming-induced by SKF 38393 in mice.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1207200Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID5831In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID61236Compound was tested in vivo for induction of catalepsy against dopamine receptor D2 in rats1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1256674Antipsychotic activity in po dosed Chinese Kun Ming mouse assessed as inhibition of apomorphine-induced climbing administered 30 mins before apomorphine challenge measured up to 30 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID177499In vivo inhibition of amphetamine induced stereotypy in rat by the compound administered intraperitoneally; nt=Not tested1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1209311Ratio of unbound brain concentration to drug level in cerebrospinal fluid in cynomolgus monkey at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1704751Therapeutic index, ratio of ED50 for toxicity in po dosed Kunming mouse assessed as catalepsy to ED50 for antipsychotic activity in Kunming mouse assessed as inhibition of apomorphine-induced climbing behavior
AID1255778Antipsychotic activity in Sprague Dawley rat psychosis model assessed as inhibition of 0.2 mg/kg dizocilpine-induced stereotypy at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured every 5 mins for 1 hr starting from the 15th min of2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
AID1210207Total drug level in mdr1a-deficient mouse brain at 4 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1691230Antagonist activity at D2 receptor (unknown origin)2020European journal of medicinal chemistry, May-01, Volume: 193Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.
AID61375Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID130881Inhibition of apomorphine induced mouse climbing, administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1704722Displacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting method
AID410334Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID750650Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1724114Binding affinity to alpha1 adrenergic receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID330537Increase in phospho-AMPK levels in H1RKO mouse hyphalamic slices at 500 nM after 30 mins by Western blotting2007Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
AID63811Displacement of [3H]NPA from rat brain Dopamine receptor D21996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1403798Antagonist activity at M3 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
AID5303The binding affinity was measured on 5-hydroxytryptamine 2 receptor in rat brain tissue1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1724119Induction of catalepsy in po dosed mouse by vertical grid and elevated bar test2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID714107Displacement of [3H]imipramine from human SERT expressed in CHO cells by competition binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID374351Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport.
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID184416The compound was measured at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1256677Ratio of ED50 for Chinese Kun Ming mouse assessed as induction of catalepsy to ED50 for Chinese Kun Ming mouse assessed as inhibition of apomorphine-induced climbing behaviour2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID225497Compound was tested for induction of catalepsy in mouse.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID177809Compound was evaluated in vivo for its antipsychotic activity for inhibition of apomorphine-induced stereotypy in rat1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1071728Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID61049Inhibition of mouse Dopamine receptor D21996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID1724120Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1613972Solubility of the compound in DMSO2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID342782Binding affinity to human cloned histamine H1 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1215124Binding affinity to Wistar rat brain lipid assessed as percentage unbound by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID35637Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1704786Toxicity in Kunming mouse assessed as change in body weight at 0.1 to 0.3 mg/kg, po administered for 28 days measured daily during compound dosing
AID1762069Cognitive enhancement effect in rat assessed as increase in time spent in exploring novel object at 0.3 mg/kg, po administered 1 hr prior to acquisition trial by novel object recognition test2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID298485Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID3992Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID238990Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID5804Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor; No data2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID714084Decrease in 5-HIAA level in Sprague-Dawley rat striatum at 2.4 umol/kg, sc by HPLC analysis relative to saline-treated control2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID65243Affinity for Dopamine receptor D21998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID1762060Binding affinity to alpha1 adrenoceptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1211422Absorption rate constant in Wistar rat extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID721751Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1762070Cognitive enhancement effect in rat assessed as increase in novelty discrimination index at 0.3 mg/kg, po administered 1 hr prior to acquisition trial by novel object recognition test2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1301292Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID1409514Therapeutic index, ratio of ED50 for catalepsy in Kunming mouse to ED50 for MK-801-induced hyperactivity in Kunming mouse2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1209307Ratio of drug level in cerebrospinal fluid to unbound plasma concentration in Beagle dog at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID750654Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID132469The compound was tested for antagonistic activity against apomorphine induced climbing in the mouse, percentages are for reduction in climbing after peroral administration1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID5951Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID750653Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID750620Therapeutic Index, ratio of ED50 for catalepsy in mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in apomorphine-induced climbing behavior2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1211796Intrinsic clearance in cryopreserved human HepaRG cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID176254Intraperitoneal effective dose required for inhibition of apomorphine-induced stereotypy in rat1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1209301Ratio of drug level in brain to plasma in Beagle dog at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID63804Affinity against Dopamine receptor D22000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1210215Percentage unbound in Sprague-Dawley rat plasma at 1 uM after 5 hrs by equilibrium dialysis method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1215120Binding affinity to Wistar rat brain lipid by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1704752Therapeutic index, ratio of ED50 for toxicity in po dosed Kunming mouse assessed as catalepsy to ED50 for antipsychotic activity in Kunming mouse assessed as inhibition of MK801-induced locomotor activity
AID1071720Therapeutic index, ratio of ED50 for induction of catalepsy to ED50 for antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK801-induced hyperactivity2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1462325Therapeutic index, ratio of ED50 for induction of catalepsy in ig dosed ICR mouse to ED50 for inhibition of PCP-induced hyper-locomotion in ig dosed ICR mouse2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID35277Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID705397Antipsychotic activity in sc dosed rat assessed as decrease in amphetamine-induced spontaneous locomotor activity2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1393475Reversal of ketamine-induced cognitive flexibility in ip dosed Sprague-Dawley rat administered 30 mins prior to ketamine administration by attentional set-shifting test
AID315816Antagonist activity at human recombinant 5HT2B receptor expressed in CHO cells assessed as increase in calcium levels2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID246883In vivo effective dose for reversal of tryptamine-induced cyanosis in rats2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1682829Binding affinity to adrenergic alpha1 receptor (unknown origin)
AID5616Binding affinity towards human 5-hydroxytryptamine 2C receptor2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID1210216Percentage unbound in Sprague-Dawley rat brain at 1 uM after 5 hrs by equilibrium dialysis method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID1181679Antipsychotic activity in Sprague-Dawley rat prepulse inhibition deficit model assessed as reversal of MK-801-induced effect at 1 mg/kg, ip administered 20 mins prior to MK-801 challenge relative to vehicle-treated control2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID1209381AUC(0 to 2 hrs) in Sprague-Dawley rat plasma at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1071730Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID178920Effective dose required for antipsychotic activity was evaluated by rat CAR assay1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID342786Binding affinity to rat NET2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1209353Ratio of unbound brain concentration to drug level in cerebrospinal fluid in Sprague-Dawley rat at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID37455Affinity for alpha-1 adrenergic receptor1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID410331Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID1462313Antagonist activity at dopamine D2 receptor (unknown origin) after 60 mins by Ultra lance cAMP assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID1762055Binding affinity to dopamine D3 receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID239086Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
AID40406Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1409512Antipsychotic activity in po dosed Sprague-Dawley rat assessed as reduction in conditioned avoidance response measured at 90 mins post single dose2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID410336Displacement of [3H]mesulergine from 5HT2C receptor in CRL:(HA) BR albino guinea pig cortex by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID1570286Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cell membranes measured after 30 mins
AID3657Binding affinity towards human 5-hydroxytryptamine 1 receptor2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID176804In vivo activity administered intraperitoneally was determined by pole climb avoidance in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID239249Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1724112Binding affinity to H1 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID176458Pole climb escape failures of rats was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID342779Binding affinity to human cloned dopamine D4 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1409511Induction of catalepsy in po dosed Kunming mouse measured after 60 secs2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1373835Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.
AID35427The binding affinity was measured on adrenergic alpha-1 receptor in rat brain tissue1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1211454Unbound AUC (0 to infinity) in Wistar rat plasma at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID176743Dose inducing catalepsy in rats after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID410333Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1659273Antagonist activity at muscarinic M3 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID63971Binding affinity for dopamine receptor D2 determined using [3H]spiperone2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID750656Displacement of [3H]rauwolscine from alpha-2 adrenergic receptor in rat cerebral cortex after 60 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID342775Binding affinity to human cloned dopamine D1 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1209345Ratio of drug level in cerebrospinal fluid to unbound plasma concentration in Sprague-Dawley rat at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1301293Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID1762086Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID64327Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID1209421AUC(0 to infinity) in Sprague-Dawley rat brain at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID63347Binding affinity towards human Dopamine receptor D12004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID61808Binding affinity towards human dopamine-4.2 receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID503306Antiproliferative activity against human PC3 cells at 2 uM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID1393473Reversal of ketamine-induced working social withdrawal in ip dosed Sprague-Dawley rat pretreated for 60 mins followed by ketamine administration
AID4357The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID1659274Antagonist activity at 5-HT2C receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID1256667Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID410335Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID1462316Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
AID63524Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID63070Binding affinity towards human D2 dopamine receptor.2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID1209317Ratio of unbound drug level in brain to plasma in cynomolgus monkey at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1823847Anti-antidepressant like activity in Wistar rat assessed as reduction in locomotor activity by measuring total immobility time by Forced swim test
AID410141Toxic cataleptic effect against Swiss albino mouse2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID177555Ability to block apomorphine-induced stereotypy in rats.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID342773Binding affinity to human cloned 5HT6 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID301866Displacement of [3H]spiperone from dopamine D2 receptor in rat brain2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID1659275Antagonist activity at H1 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID1409479Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum homogenates after 30 mins by liquid scintillation counting2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID750623Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperactivity administered for 30 mins prior to MK-801-challenge measured after 90 mins2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID180925The percentage production of catalepsy in rat at a dose of 4 mg/kg ip.1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID177721Induction of catalepsy in rats was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID225495Compound was tested for antagonist activity against apomorphine-induced mouse stereotypy(per orally - po). using in vivo method1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID65902The binding affinity was measured on dopamine receptor D2 in rat brain tissue1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1335652Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed Chinese Kun Ming mouse to ED50 for inhibition of MK-801 induced hyperactivity in po dosed Chinese Kun Ming mouse2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1211442Ratio of steady state drug level in extracellular fluid to unbound drug level in plasma of Wistar rat at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1704721Displacement of [3H]pyrilamine from guinea pig cerebellum histamine H1 receptor measured after 60 mins by liquid scintillation counting method
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID3656In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1211448Equilibration half life in Wistar rat brain extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID439069Displacement of [3H]spiperone from human dopamine D3 receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID1211798Intrinsic clearance in human using well stirred liver model by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1209413AUC(0 to 2 hrs) in Sprague-Dawley rat brain at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1724123Memory enhancement effect in rat assessed as increase in total exploratory time for novel objects at 0.1 mg/kg, po administered 1 hr prior to acquisition trial and measured after 24 hrs by novel object recognition test2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1762057Binding affinity to 5-HT2A receptor (unknown origin)2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1071721Therapeutic index, ratio of ED50 for induction of catalepsy to ED50 for antipsychotic activity in po dosed Kunming mouse assessed as reversal of apomorphine-induced cage climbing response2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1062948Displacement of [3H]spiperone from human D2 receptor2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.
AID1209298Ratio of drug level in brain to plasma in cynomolgus monkey at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1764400Unbound brain concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID3960Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID61562Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1704753Therapeutic index, ratio of ED50 for toxicity in po dosed Kunming mouse assessed as catalepsy to ED50 for antipsychotic activity in Kunming mouse assessed as inhibition of DOI-induced head twitch
AID721752Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1215126Ratio of fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID63996Binding affinity towards dopamine D2 receptor was determined; nd=Not determined2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID1823851Sedative activity in ip dosed Wistar rat assessed as effect on spontaneous locomotor activity measured for 10 mins by social interaction test
AID1335640Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1211794Fraction unbound in blood (not specified)2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID729702Antipsychotic activity in Sprague-Dawley rat schizophrenia model assessed as inhibition of PCP-induced prepulse inhibition at 0.5 mg/kg, ip administered 10 mins prior testing monitored for 5 mins2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID599884Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells2010Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
AID1256666Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1704748Antipsychotic activity in Kunming mouse assessed as inhibition of MK801-induced locomotor activity administered orally 30 mins prior to MK801 challenge and measured for 90 mins
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID410138Inhibition of 5HT2A receptor-mediated quipazine-induced head twitches in Swiss albino mouse at 10 mg/kg2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID1169862Binding affinity to 5HT1A receptor (unknown origin)2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID1724117Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1409518Induction of serum prolactin levels in Kunming mouse at 0.03 to 0.27 mg/kg, po administered for 28 days measured at 180 mins post last dose by EIA2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1764399Unbound plasma concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID1255779Antipsychotic activity in Sprague Dawley rat psychosis model assessed as inhibition of 0.2 mg/kg dizocilpine-induced ataxia at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured every 5 mins for 1 hr starting from the 15th min of pos2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
AID1256675Antipsychotic activity in po dosed Chinese Kun Ming mouse assessed as inhibition of DOI-induced head twitch administered 60 mins before DOI challenge measured up to 15 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1211416Central volume of distribution in Wistar rat extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1301290Toxicity in ig dosed mouse assessed as induction of catalepsy by horizontal bar method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID298478Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1209368Unbound fraction in cynomolgus monkey brain at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1209405AUC(0 to infinity) in Sprague-Dawley rat cerebrospinal fluid at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID301867Displacement of [3H]ketanserin from 5HT2A receptor in rat brain2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID239052Inhibition of [3H]-spiperone binding to human Dopamine receptor D22005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID342784Binding affinity to human cloned 5HT2A receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1762063Inhibition of human ERG by automated patch method relative to control2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID298481Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1704749Antipsychotic activity in Kunming mouse assessed as inhibition of DOI-induced head twitch administered orally 60 mins prior to DOI challenge incubated for 5 mins and measured for 15 mins
AID1762087Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID4812Inhibition of [3H]ketanserin binding to dopamine 5-hydroxytryptamine 2 receptor1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID223306Effective dose administered in catalepsy test in mice(in vivo) value in parentheses represents 95% confidence limit2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1215123Binding affinity to Wistar rat serum albumin2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1724109Binding affinity to 5HT2A receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID315817Antagonist activity at human recombinant 5HT2C receptor expressed in CHO cells assessed as increase in calcium levels2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.
AID238989Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID315815Antagonist activity at human recombinant 5HT2A receptor expressed in mouse NIH3T3 cells assessed as increase in calcium levels2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.
AID112509In vivo Antipsychotic activity was quantified by inhibition of apomorphine-induced climbing(CL 95%) by mice1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID1776498Antidepressant activity in ICR mouse aassessed as inhibition of apomorphine-induced climbing behaviour at 10 mg/kg, ip administered prior to APO challenge and measured after 30 mins2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of Novel and Potent
AID1409513Therapeutic index, ratio of ED50 for catalepsy in Kunming mouse to ED50 for apomorphine-induced climbing in Kunming mouse2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1211297Drug recovery in plasma (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID410143Ratio of inhibition of quipazine-induced head twitches to inhibition of apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID1169860Binding affinity to dopamine D2 receptor (unknown origin)2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID1211436Ratio of uptake clearance to efflux clearance in Wistar rat brain extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1211412Tmax in Wistar rat extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID705399Antipsychotic activity in sc dosed rat assessed as decrease in spontaneous locomotor activity2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID130711In vivo inhibition of the apomorphine-induced climbing behavior in mice2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID235066The binding affinity was measured on alpha-1 adrenergic receptor in rat brain tissue1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID225492Compound was tested for antagonist activity against apomorphine-induced mouse climbing(per orally - po). using in vivo method1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID4061Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID1203551Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents at 10 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
AID298487Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1204338Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as total radioligand binding at 1.66 x 10'-7 M incubated for 60 mins by microbeta plate reader based method2015European journal of medicinal chemistry, Jun-05, Volume: 97Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.
AID36197Binding affinity towards human alpha-2 adrenergic receptor2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Current and novel approaches to the drug treatment of schizophrenia.
AID410134Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg measured on 10 mins2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID599883Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells2010Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
AID5573Relative binding affinity for D2 receptor and 5-hydroxytryptamine 2A receptor, ratio of Ki1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1659261Agonist activity at D2 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.
AID1704723Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
AID1403796Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
AID61499Affinity for Dopamine receptor D11998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID1209397AUC(0 to 2 hrs) in Sprague-Dawley rat cerebrospinal fluid at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1724118Antipsychotic activity in po dosed rat assessed as suppression in conditioned avoidance response measured after 90 mins by CAR test2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID6648Binding affinity towards rat 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID1578087Brain to plasma partition coefficient, Kp of the compound in rat2019European journal of medicinal chemistry, Nov-15, Volume: 182Practical approaches to evaluating and optimizing brain exposure in early drug discovery.
AID714089Increase in DOPAC level in Sprague-Dawley rat striatum at 2.4 umol/kg, sc by HPLC analysis relative to saline-treated control2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID232554Ratio of ED50 for antagonism of apomorphine-induced stereotypy to ED50 for antagonism of apomorphine-induced climbing.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1210241Total drug level in mdr1a-deficient rat brain at 5 mg/kg/day administered through continuous minipump treatment for 3 days by UPLC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Species comparison of in vivo P-glycoprotein-mediated brain efflux using mdr1a-deficient rats and mice.
AID64296Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D21998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1409516Induction of weight gain in Kunming mouse at 0.03 to 0.27 mg/kg, po administered for 28 days measured every day during compound dosing2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1211419Systemic clearance in Wistar rat extracellular fluid at 3 mg/kg, sc by HPLC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
AID1335645Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum incubated for 60 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1301289Antipsychotic activity in ig dosed mouse assessed as inhibition of PCP-induced hyperactivity2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
AID308685Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID410140Toxic cataleptic effect in Swiss albino mouse assessed as maximum average cataleptic time2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID1211293Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1209361Ratio of unbound drug level in brain to plasma in Sprague-Dawley rat at 1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID410139Inhibition of 5HT2A receptor-mediated quipazine-induced head twitches in Swiss albino mouse at 0.6 mg/kg, ip2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID225182Inhibition of apomorphine-induced climbing behavior in mice, after peroral administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID1203549Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents at 1 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
AID64984Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID419436Lipophilicity, log P of the compound2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Synthesis and evaluation of 1-(quinoliloxypropyl)-4-aryl piperazines for atypical antipsychotic effect.
AID1570292Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as maximal inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay relative to control
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1570291Agonist activity at human 5HT1A receptor expressed in HEK293 cell membranes assessed as maximal inhibition of forskolin induced cAMP production incubated for 24 hrs followed by forskolin addition by HTRF assay relative to control
AID1335649Inhibition of apomorphine-induced climbing behavior in po dosed Chinese Kun Ming mouse administered for 30 mins followed by apomorphine challenge and measured for 10 to 30 mins2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1256678Ratio of ED50 for Chinese Kun Ming mouse assessed as induction of catalepsy to ED50 for Chinese Kun Ming mouse assessed as inhibition of DOI-induced head twitch2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID705398Antipsychotic activity in sc dosed rat assessed as decrease in phencyclidine-induced locomotor activity2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1704774Effect on total exploration time in Sprague-Dawley rat at 0.2 mg/kg, po measured after 1 hr by novel object recognition test
AID681619TP_TRANSPORTER: ATP hydrolysis in membranes from MDR1-expressing insect cells2002Life sciences, May-31, Volume: 71, Issue:2
In vitro P-glycoprotein affinity for atypical and conventional antipsychotics.
AID750625Toxicity in mouse assessed as effect on serum prolactin level at 0.02 to 0.16 mg/kg, po for 28 days measured 180 mins after last treatment by enzyme immunoassay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID65920In vitro affinity against Dopamine receptor D4; No data2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1823849Antipsychotic activity in ip dosed Wistar rat assessed as induction of MK801-induced hyperlocomotor activity by measuring minimum effective dose measured for 15 mins
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1062947Selectivity ratio of pKi for human 5-HT2A receptor to pKi for human D2 receptor2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.
AID225181Inhibition of apomorphine-induced climbing behavior in mice, after Intraperitoneal administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID229516Ratio of IC50 value against dopamine receptor D2 to that of 5-hydroxytryptamine 3 receptor.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1256664Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID3688Affinity for 5-hydroxytryptamine 1 receptor1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID5614Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID36113Binding affinity towards human alpha-1 adrenergic receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1762065Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID176803In vivo activity administered intraperitoneally was determined by intracranial self stimulation in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID112508In vivo Antipsychotic activity was quantified by induction of catalepsy in mice1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID197749Inhibition of apomorphine-induced stereotypy in Rat, after peroral administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID233511Ratio of pKi of 5-HT2A receptor to that of D2 receptor2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1152668Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.
AID1335642Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum incubated for 30 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID1209288AUC(0 to 1 hr) in cynomolgus monkey cerebrospinal fluid at 0.1 mg/kg, sc by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
AID5522Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID223305Effective dose administered in apomorphine induced climbing test in mice (in vivo)value in parentheses represents 95% confidence limit2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID624231Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1D1996Molecular pharmacology, Dec, Volume: 50, Issue:6
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamin
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)2009Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1
Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1996Molecular pharmacology, Dec, Volume: 50, Issue:6
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamin
AID1346919Rat 5-HT2A receptor (5-Hydroxytryptamine receptors)1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2000The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.
AID624232Antagonists at Human 5-Hydroxytryptamine receptor 5-ht1e1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346037Human H1 receptor (Histamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID624222Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs.
AID1345971Human alpha1D-adrenoceptor (Adrenoceptors)2001Japanese journal of pharmacology, Jun, Volume: 86, Issue:2
Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1996European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3
Iloperidone binding to human and rat dopamine and 5-HT receptors.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1998British journal of pharmacology, Apr, Volume: 123, Issue:8
Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines.
AID1346000Human alpha1B-adrenoceptor (Adrenoceptors)2001Japanese journal of pharmacology, Jun, Volume: 86, Issue:2
Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624226Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1F1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1998British journal of pharmacology, Jul, Volume: 124, Issue:6
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2002European journal of pharmacology, Aug-16, Volume: 450, Issue:1
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.
AID624217Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT1A1996European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3
Iloperidone binding to human and rat dopamine and 5-HT receptors.
AID1345602Rat 5-HT1A receptor (5-Hydroxytryptamine receptors)1996European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3
Iloperidone binding to human and rat dopamine and 5-HT receptors.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)2001Japanese journal of pharmacology, Jun, Volume: 86, Issue:2
Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Jan, Volume: 66, Issue:1
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
AID1346037Human H1 receptor (Histamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)2005Psychopharmacology, May, Volume: 179, Issue:2
Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
AID1345788Human D2 receptor (Dopamine receptors)1998Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Feb, Volume: 18, Issue:2
Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2002European journal of pharmacology, Aug-16, Volume: 450, Issue:1
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1996European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3
Iloperidone binding to human and rat dopamine and 5-HT receptors.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624231Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1D1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345833Human D3 receptor (Dopamine receptors)1995The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2
Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID493017Wombat Data for BeliefDocking1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,447)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (0.12)18.7374
1990's903 (14.01)18.2507
2000's2754 (42.72)29.6817
2010's2258 (35.02)24.3611
2020's524 (8.13)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 124.68

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index124.68 (24.57)
Research Supply Index9.04 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index232.87 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (124.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,505 (21.74%)5.53%
Reviews825 (11.92%)6.00%
Case Studies1,376 (19.87%)4.05%
Observational58 (0.84%)0.25%
Other3,160 (45.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (451)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Post Marketing Study of Escitalopram Versus Risperidone for the Treatment of Behavioral and Psychological Symptoms Amongst Alzheimer's Disease Patients [NCT01119638]Phase 440 participants (Actual)Interventional2008-04-30Completed
Effects of NMDA Receptor Antagonism on Cognitive Processes in Healthy Volunteers and Its Reversal by a Dopamine Antagonist: Comparison to Patients With Schizophrenia [NCT01140620]Phase 487 participants (Actual)Interventional2010-06-30Completed
Risperidone Effects On Frontal And Temporal Cortical Function In Schizophrenia Patients Undergoing FMRI Cognitive Task Performance [NCT01234454]34 participants (Actual)Interventional2002-01-31Completed
Optimizing Response in Psychosis Study [NCT00314327]Phase 41 participants (Actual)Interventional2006-04-30Terminated(stopped due to Recruitment for the study was limited.)
Research and Evaluation of Antipsychotic Treatment in Community Behavioral Health Organizations [NCT01181960]1,066 participants (Actual)Observational2010-08-31Completed
A 6-month, Randomised, Double-blind, Parallel-group, Risperidone-controlled, Fixed-dose Study Evaluating the Safety and Efficacy of Zicronapine in Patients With Schizophrenia [NCT01295372]Phase 3160 participants (Actual)Interventional2011-04-30Completed
Open Flexible-dose Randomized Study of the Effectiveness of Second Generation Antipsychotics in First Episode Psychosis Patients: A 1-year Follow-up [NCT02532491]Phase 4200 participants (Anticipated)Interventional2014-05-31Enrolling by invitation
Pragmatic Randomized Trial of Risperdal Consta Versus Oral Atypical Antipsychotics in Poorly Adherent Subjects With Schizophrenia in a Routine Care Setting [NCT00256997]Phase 4167 participants (Actual)Interventional2006-01-31Terminated(stopped due to Inability to recruit number of planned patients)
Clinical Study to Assess the Treatment of Schizophrenia With Paliperidone Palmitate in Rwandan Healthcare Settings [NCT04940039]Phase 493 participants (Actual)Interventional2021-07-22Active, not recruiting
Therapeutic Issues for Autism Spectrum Disorders: a Clinical Trial [NCT03887754]Phase 280 participants (Actual)Interventional2016-01-31Completed
A Double Blind Pilot Trial to Evaluate Efficacy Trends and Safety of Risperidone and Olanzapine as add-on Therapy to Serotonin Type Antidepressants in Subjects With Treatment Resistant Depression (TRD) [NCT01282632]Phase 1/Phase 242 participants (Actual)Interventional2002-08-31Completed
A Twelve-Month, Prospective, Randomized, Active-Controlled, Open-Label, Flexible-Dose Study of Paliperidone Palmitate Compared With Oral Antipsychotic Treatment in Adults With Schizophrenia Who Have Been Recently Discharged From an Inpatient Psychiatric H [NCT01193166]Phase 40 participants (Actual)Interventional2010-08-31Withdrawn(stopped due to This study was stopped due to an internal reconsideration of priorities of the product portfolio.)
A Multicentre, 8-week, Single-arm, Open-label, Pragmatic Trial to Explore Acceptance and Performance of Using a Digital Medicine System With Healthcare Professionals and Adult Subjects With Schizophrenia, Schizoaffective Disorder, or First Episode Psychos [NCT03568500]Phase 444 participants (Actual)Interventional2018-05-21Completed
Single Dose Two-way Crossover Fed Bioequivalence Study of Risperidone 1 mg ODT Tablets in Healthy Volunteers [NCT01222923]40 participants (Actual)Interventional2004-10-31Completed
Phase I Clinical Trial. Study of the Impact of Pharmacogenetic Markers in Predicting the Appearance of Extrapyramidal Symptomatology After the Treatment With Typical vs. Atypical Antipsychotics, in Healthy Volunteers [NCT01259973]Phase 124 participants (Anticipated)Interventional2011-02-28Enrolling by invitation
Comparative, Randomized, Single-Dose, 2-way Crossover Bioavailability Study of Dr.Reddy's Laboratories Ltd. and Janssen Pharmaceutica Products, LP. (Risperdal M-TABTM)1 mg Risperidone Orally Disintegrating Tablets in Healthy Adult Male Volunteers Under Fa [NCT01155921]Phase 136 participants (Actual)Interventional2004-08-31Completed
Multicenter, Randomized, Double-Blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of Intramuscular Injections of Risperidone ISM® in Patients With Acute Exacerbation of Schizophrenia [NCT03160521]Phase 3438 participants (Actual)Interventional2017-06-02Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy, Safety, and Tolerability of Risperidone Extended-Release Injectable Suspension (TV-46000) for Subcutaneous Use as Maintenance Treatment in Adult and Adolescent Pat [NCT03503318]Phase 3544 participants (Actual)Interventional2018-04-27Completed
Evaluation of the Effects of Sequential Multiple-Dose Regimens of Cariprazine on Cardiac Repolarization in Patients With Schizophrenia [NCT01376076]Phase 1129 participants (Actual)Interventional2011-06-30Completed
Comparison of Aripiprazole Versus Risperidone on Brain Morphology Using MRI [NCT02334904]60 participants (Anticipated)Observational2014-07-31Recruiting
A Phase IIa, Randomized, Double-Blind, Placebo-Controlled Clinical Trial of the Efficacy and Safety of MK-8189 Using Risperidone as an Active Control in Subjects Experiencing an Acute Episode of Schizophrenia [NCT03055338]Phase 2224 participants (Actual)Interventional2017-03-08Completed
An Open-Label, One-Sequence Study to Evaluate the Steady- State Comparative Bioavailability of Intramuscular Risperidone ISM® and EU Risperdal® (Sourced From Germany) [NCT05179525]Phase 180 participants (Actual)Interventional2021-03-09Completed
An Observational Drug Utilization Study of SYCREST^® (Asenapine) in the United Kingdom [NCT01498770]42 participants (Actual)Observational2013-04-01Completed
A Pilot-Study in Rwandan Health Care Settings to Examine the Feasibility of a Large Pragmatic Clinical Study to Assess the Value of Paliperidone Palmitate in Rwanda [NCT03713658]Phase 434 participants (Actual)Interventional2018-10-18Completed
Biomarkers in Autism of Aripiprazole and Risperidone Treatment [NCT01333072]Phase 480 participants (Actual)Interventional2011-07-31Completed
A Randomized, Open-Label, Parallel-Group Study to Assess the Relative Bioavailability of LY03004 and Risperdal® Consta® at 25 mg Following Multiple Intramuscular Injections in Stable Patients With Schizophrenia or Schizoaffective Disorder [NCT02091388]Phase 1108 participants (Actual)Interventional2014-09-30Completed
Interventional, Randomized, Double-blind, Active-controlled Study of the Efficacy of Lu AF35700 in Patients With Early-in-disease or Late-in-disease Treatment-resistant Schizophrenia [NCT03230864]Phase 3119 participants (Actual)Interventional2017-07-20Terminated(stopped due to New data; the study was terminated based on new efficacy data from another study)
Efficacy and Safety of Risperidone and Trazodone Monotherapy and Combination Therapy in Critically Ill Patients With Delirium: A Four-arm Prospective, Randomized, Double-blind, Placebo-controlled Pilot Study [NCT02118688]Phase 40 participants (Actual)Interventional2011-03-31Withdrawn(stopped due to Lack of enrollment)
Liquid Risperidone in the Treatment of Acute Agitation in Psychiatrically Hospitalized Children [NCT00790075]Phase 424 participants (Actual)Interventional2003-01-31Completed
Effectiveness of Antipsychotic Drugs to Treat Psychosis Syndrome: an Open Label, Controlled Study [NCT02137616]300 participants (Anticipated)Interventional2012-06-30Recruiting
Repetitive Transcranial Magnetic Stimulation (rTMS) for First-episode Schizophrenia Patients:A Double-blinded , Randomized and Functional Magnetic Resonance Imaging (fMRI)Study [NCT01370291]Phase 360 participants (Anticipated)Interventional2011-06-30Recruiting
Comparative, Randomized, Single-Dose, 2-way Crossover Bioavailability Study of Dr.Reddy's Laboratories Ltd. and Janssen Pharmaceutica Products, LP. (Risperdal M-TABTM)1 mg Risperidone Orally Disintegrating Tablets in Healthy Adult Male Volunteers Under Fe [NCT01155934]Phase 136 participants (Actual)Interventional2004-08-31Completed
Neurocognitive Effectiveness in Treatment of First-episode Non-affective Psychosis: a Randomized Comparison of Aripiprazole and Risperidone Over 3 Years [NCT03883204]Phase 4115 participants (Anticipated)Interventional2015-01-01Enrolling by invitation
Evaluation of Negative Symptoms and Cognitive Function After Administration of Antipsychotics in Healthy Volunteer: a Double-blind, Randomized Trial of a Single Dose of Placebo, Haloperidol, Amisulpride, Risperidone and Aripiprazole [NCT01185418]80 participants (Actual)Observational2009-03-31Completed
A Randomized, Double-blind, Placebo-controlled Study to Explore the Efficacy and Safety of Risperidone Long-acting Intramuscular Injectable in the Prevention of Mood Episodes in Bipolar 1 Disorder, With Open-label Extension [NCT00132678]Phase 3559 participants (Actual)Interventional2005-02-28Completed
A Double-blind, Placebo Controlled Trial of Risperidone for the Treatment of Anorexia Nervosa [NCT00140426]Phase 441 participants (Actual)Interventional2004-08-31Completed
CSP #555 - Long-Acting Injectable Risperidone in the Treatment of Schizophrenia [NCT00132314]Phase 3382 participants (Actual)Interventional2006-09-30Completed
The Effect of MS14 in Association With Risperidone in Treatment of Schizophrenia: A Double Blind Randomized Control Trial [NCT01083381]Phase 250 participants (Anticipated)Interventional2010-02-28Recruiting
EFFECT OF RISPERIDONE vs ARIPIPRAZOLE ON OXIDATIVE STRESS IN PATIENTS WITH AUTISM SPECTRUM DISORDER: A RANDOMIZED CONTROLLED TRIAL [NCT05868720]42 participants (Anticipated)Interventional2023-07-01Not yet recruiting
A Randomized, Open-Label Pharmacokinetic Study of LY03004 Compared to Risperdal® Consta® Following a Single Intramuscular Injection at 25 mg or 50 mg in Stable Patients With Schizophrenia and/or Schizoaffective Disorder [NCT02186769]Phase 116 participants (Actual)Interventional2014-07-31Completed
A Study to Evaluate the Efficacy of Repetitive Transcranial Magnetic Stimulation in the Prevention of Relapse of the Symptoms of Schizoaffective Disorder [NCT02221635]540 participants (Anticipated)Observational2013-03-31Recruiting
Evaluation of the Safety and Efficacy of RGH-188 in the Acute Exacerbation of Schizophrenia [NCT00694707]Phase 2732 participants (Actual)Interventional2008-06-30Completed
Comparative Single-Dose Pharmacokinetics and Safety of Gluteal and Deltoid Intramuscular Injection of Long-Acting Injectable Risperidone in Subjects With Chronic Stable Schizophrenia [NCT00843687]Phase 3188 participants (Actual)Interventional2005-09-30Completed
A Randomized, Multi-site, Parallel-group, Rater-blind Study Comparing Response With Aripiprazole Once Monthly and Standard of Care Oral Antipsychotics in Non-adherent Outpatients With Schizophrenia Identified Using the Brief Adherence Rating Scale [NCT02282085]Phase 4200 participants (Anticipated)Interventional2014-12-31Recruiting
Neuroendocrine, Metabolite Substrates, Clinical Symptoms and Cognitive Function in Schizophrenia [NCT02423096]200 participants (Anticipated)Observational [Patient Registry]2013-12-31Recruiting
A Multicenter, Randomized, Double-blind, Parallel-group Fixed-dose Study of the Effect on Weight of Bifeprunox Versus Risperidone in the Treatment of Outpatients With Schizophrenia. [NCT00366704]Phase 3400 participants (Anticipated)Interventional2006-11-30Terminated
The Relationship Between the Efficacy of Lumateperone and Central Glutamate and Dopaminergic Metabolism: A Comparison With Risperidone in First Episode Psychosis [NCT05890768]Phase 435 participants (Anticipated)Interventional2023-05-11Recruiting
An Open-Label, One-Sequence Study to Evaluate the Steady-State Comparative Bioavailability of Intramuscular Risperidone ISM® and Oral Risperidone [NCT03527186]Phase 181 participants (Actual)Interventional2018-07-09Completed
A Long-Term, Open-Label, Multicenter Study of LY2140023 Compared to Atypical Antipsychotic Standard of Care in Patients With DSM-IV-TR Schizophrenia [NCT01129674]Phase 2/Phase 31,210 participants (Anticipated)Interventional2010-06-30Terminated(stopped due to The decision to stop the trial was based on efficacy results in the overall schizophrenia participant population.)
Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics for the Prevention of Relapse in Long-term Stabilized Schizophrenic Patients: a Randomized, Single-blind, Longitudinal Trial [NCT02307396]Phase 421 participants (Actual)Interventional2015-02-01Completed
A Long-Term, Phase 2, Multicenter, Randomized, Open-Label Comparative Safety Study of LY2140023 Versus Atypical Antipsychotic Standard of Care in Patients With DSM-IV-TR Schizophrenia [NCT00845026]Phase 2261 participants (Actual)Interventional2009-03-31Completed
CSP #504 - Risperidone Treatment for Military Service Related Chronic Post-Traumatic Stress Disorder [NCT00099983]Phase 2296 participants (Actual)Interventional2006-10-31Completed
Risperidone ISM® Effectiveness in Schizophrenia Patients Hospitalised Due to A Relapse: a Prospective Non-interventional Evaluation (RESHAPE Study) [NCT05480046]1,200 participants (Anticipated)Observational2022-10-18Recruiting
Phase I, Open-Label, Randomized, Parallel Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of One Intramuscular Injection of Risperidone ISM® at Different Dose Strengths in Subjects With Schizophrenia or Schizoaffective Disorder [NCT01788774]Phase 136 participants (Actual)Interventional2013-04-30Completed
Single Dose Two-way Crossover Fasted Bioequivalence Study of Risperidone 1 mg ODT Tablets in Healthy Volunteers [NCT01222975]44 participants (Actual)Interventional2004-10-31Completed
The Characteristics of Treatment Resistant Schizophrenia From the Illness Onset [NCT06128408]300 participants (Anticipated)Observational2023-12-01Not yet recruiting
A Phase II Study to Assess the Efficacy, Safety and Tolerability of VAL401 in the Treatment of Patients With Locally Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC) After Failure of at Least One Prior Chemotherapeutic Regimen [NCT02875340]Phase 28 participants (Actual)Interventional2016-10-31Completed
A Prospective, Matched-Control, Randomized, Open-Label, Flexible-Dose, Study in Subjects With Recent-Onset Schizophrenia or Schizophreniform Disorder to Compare Disease Progression and Disease Modification Following Treatment With Paliperidone Palmitate L [NCT02431702]Phase 3337 participants (Actual)Interventional2015-07-08Completed
Efficacy of Treatment With Pramipexole or Risperidone in Patients With Refractory Obsessive-compulsive Disorder (OCD): Randomized Controlled Trial [NCT05401019]Phase 252 participants (Anticipated)Interventional2022-06-30Not yet recruiting
Mirror-image Study Exploring Relapse and Resource Utilization of Paliperidone Palmitate and Risperidone Long-acting Injection in Vitalité Health Network Patients [NCT03390712]328 participants (Anticipated)Observational2018-01-02Enrolling by invitation
Continuation Electroconvulsive Therapy Associated With Pharmacotherapy Versus Pharmacotherapy Alone for Relapse Prevention in Major Depression. A Clinical, Controlled, Prospective and Randomized Trial [NCT01305707]Phase 4104 participants (Actual)Interventional2009-07-31Terminated(stopped due to Difficulties in recruiting)
Identification of Multi-modal Bio-markers for Early Diagnosis and Treatment Prediction in Schizophrenia Individuals [NCT03790085]Early Phase 12,700 participants (Anticipated)Interventional2018-09-01Recruiting
Risperidone in the Treatment of Children and Adolescents With Autistic Disorder: A Double-Blind, Placebo-Controlled Study of Efficacy and Safety, Followed by an Open-Label Extension Study of Safety [NCT00576732]Phase 496 participants (Actual)Interventional2007-12-31Completed
Discontinuation of Antipsychotics and Antidepressants Among Patients With Dementia and BPSD Living in Nursing Homes - a 24 Weeks Double Blind RCT. [NCT00594269]Phase 4149 participants (Actual)Interventional2008-08-31Completed
A Randomized, Open-label, Active-controlled Study to Evaluate Social Functioning of Long Acting Injectable Risperidone and Oral Risperidone in the Treatment of Subjects With Schizophrenia or Schizoaffective Disorder [NCT00992407]Phase 475 participants (Actual)Interventional2007-12-31Completed
Risperidone and Zotepine in the Treatment of Delirium [NCT00622011]Phase 45 participants (Actual)Interventional2008-01-31Terminated(stopped due to inadequate participant)
Comparative Study of Recommended Treatment for Schizophrenia Guideline Treatment vs Treatment as Usual in Child Psychiatric Hospital: Effect on Adherence, Efficacy on Symptoms, and Global Function [NCT02573701]91 participants (Actual)Interventional2011-10-31Completed
[NCT00629252]14 participants (Actual)Interventional2008-02-29Terminated(stopped due to Not enough subjects have been recruited in the expected period.)
Nicotinic Receptors and Schizophrenia [NCT02538081]Phase 1/Phase 20 participants (Actual)Interventional2015-08-31Withdrawn(stopped due to Withdrawn)
A Pilot Study of Three-Week, Randomised, Open Comparison in Schizophrenic In-patients Treated With Quetiapine Prolong or Oral Risperidone at Flexible Dose [NCT00660595]Phase 329 participants (Actual)Interventional2008-09-30Terminated(stopped due to To difficult to recruit patients in the acute setting)
Assessment of the Inter-patient Variability in Clinical Response and Correlated Genetic Variations in Substance Use Disorders [NCT05833399]200 participants (Anticipated)Observational2022-11-28Recruiting
A Randomized, Double-blind, Placebo-controlled, Multi-center Study to Assess the Antipsychotic Efficacy of ITI-007 in Patients With Schizophrenia [NCT01499563]Phase 2335 participants (Actual)Interventional2011-12-31Completed
Effectiveness of 6 Antipsychotic Drugs in the Treatment of Acute Exacerbations of Chronic Inpatients With Schizophrenia: a Randomized Double-blind Study [NCT02192723]550 participants (Actual)Interventional2012-06-30Completed
Cannabidiol as a Different Type of an Antipsychotic: Drug Delivery and Interaction Study With Approved Antipsychotics in Vivo [NCT02051387]Phase 174 participants (Actual)Interventional2013-01-31Completed
The Assessment of Efficacy and Tolerability of Methylphenidate vs. Risperidone in the Treatment of Children and Adolescents With ADHD and Disruptive Disorders [NCT02063945]Phase 45 participants (Actual)Interventional2017-02-01Terminated(stopped due to Major difficulties recruiting participants)
Open-Label Pharmacokinetic Study to Evaluate the Steady-State Venous and Capillary Plasma Concentrations of Five Antipsychotics: Aripiprazole, Olanzapine, Paliperidone, Quetiapine and Risperidone [NCT02087579]Phase 1305 participants (Actual)Interventional2014-02-28Completed
A Double-Blind, Randomized, Multiple Dose Study of Weight Associated Parameters: SEP-363856 vs Prior Antipsychotic (PA) Standard of Care in Subjects With Schizophrenia Suffering From Metabolic Dysregulation [NCT05542264]Phase 160 participants (Anticipated)Interventional2022-11-15Recruiting
Does Psilocybin Require Psychedelic Effects to Treat Depression? A 4-Week, Double-Blind, Proof-of-Concept Randomized Controlled Trial [NCT05710237]Phase 260 participants (Anticipated)Interventional2023-07-01Recruiting
The Effectiveness of Supplementing Supported Employment With Behavioral Skills Training [NCT00183625]Phase 4107 participants (Actual)Interventional2000-06-30Completed
Interventions to Test the Alpha7 Nicotinic Receptor Model in Schizophrenia [NCT00509067]Phase 243 participants (Actual)Interventional2007-11-30Completed
Bioequivalence Study of Risperidone 1 mg Tablets of Torrent Pharmaceuticals Limited., India and Risperdal® (Risperidone) 1 mg Tablets of Janssen Pharmaceutical Products, LP, USA, in Healthy Human Adult Subjects, Under Fed Conditions [NCT00939926]Phase 10 participants InterventionalCompleted
Tropisetron With Risperidone for Schizophrenia [NCT00435370]Phase 3179 participants (Actual)Interventional2006-11-30Completed
A Randomized Controlled Trial to Evaluate the Effectiveness of Clozapine Versus Olanzapine, Quetiapine or Risperidone in Treatment Resistant Bipolar Disorder [NCT02562287]Phase 454 participants (Anticipated)Interventional2015-10-31Recruiting
A Comparative Study of the Steady-state Pharmacokinetics of Risperidone and Topiramate on Monotherapy and During Combination Therapy in Patients With Bipolar or Schizoaffective Disorder [NCT00986336]Phase 156 participants (Actual)Interventional2001-02-28Completed
A Randomized, Double Blind, Placebo and Active Controlled Parallel Group Study to Evaluate the Efficacy and Safety of Risperidone Long-acting Injectable (LAI) for the Prevention of Mood Episodes in the Treatment of Subjects With Bipolar I Disorder [NCT00391222]Phase 3585 participants (Actual)Interventional2006-11-30Completed
Observational, Non-interventional Registry to Assess Medication Usage Patterns in Clinical Routine Practice, in Subjects Receiving Antipsychotic Treatment With Risperidone Long Acting Injectable (Gluteal or Deltoid) or Oral Antipsychotics [NCT01026285]1,085 participants (Actual)Observational2009-06-30Completed
Placebo Controlled Trial of Valproate and Risperidone in Young Children With Bipolar Disorders [NCT00221403]Phase 346 participants (Actual)Interventional2004-09-30Completed
A Multicenter, Open Label, Flexible-dose, Parallel-group Evaluation of the Cataractogenic Potential of Quetiapine Fumarate (Seroquel) and Risperidone (Risperdal) in the Long Term Treatment of Participants With Schizophrenia or Schizoaffective Disorder [NCT00206102]Phase 41,098 participants (Actual)Interventional2003-09-30Completed
A Prospective, Randomized, Active-controlled, Rater-blinded Study of the Prevention of Relapse Comparing Paliperidone Palmitate With Oral Risperidone in Adults With Recently-Diagnosed Schizophrenia Who Are at High Risk of Relapse [NCT00946985]Phase 4163 participants (Actual)Interventional2009-06-30Terminated(stopped due to The recruitment rate for the study was inadequate to achieve its enrollment goals.)
A Randomized, Open-Label, Parallel Group Comparative Study of Paliperidone Palmitate (50, 100, 150 mg eq) and Risperidone LAI (25, 37.5, or 50 mg) in Subjects With Schizophrenia [NCT00604279]Phase 3452 participants (Actual)Interventional2008-01-31Completed
Contrasting the Brain Effects of Risperidone and Invega With fMRI and PET Scanning [NCT00937261]Phase 496 participants (Anticipated)Interventional2009-07-31Recruiting
A Six Week, Multicenter, Double Blind, Double-Dummy, Parallel, Comparative Study To Compare The Efficacy, Safety And Tolerability Of Ziprasidone With Risperidone In The Treatment Of Chinese Subjects With Acute Exacerbation Of Schizophrenia [NCT00645372]Phase 3242 participants (Actual)Interventional2004-07-31Completed
A One-Year Randomized, Prospective, Parallel, Open Comparison of Subjective Well-being in Schizophrenic Out-patients Treated With Quetiapine XR (SEROQUEL XR™) or Oral Risperidone at Flexible Dose in a Naturalistic Setting [NCT00600756]Phase 3798 participants (Actual)Interventional2008-01-31Completed
A Randomized Controlled Trial of Risperidone and Olanzapine for the Schizophrenic Patients With Neuroleptic-Induced Tardive Dyskinesia [NCT00621998]Phase 460 participants (Actual)Interventional2000-07-31Completed
Multiple-dosing Study of Long Acting Injectable of Risperidone in Schizophrenic Patients [NCT00653406]Phase 1/Phase 229 participants (Actual)Interventional2002-11-30Completed
Effectiveness of Antipsychotic Combination With Psychosocial Intervention on Outcome of Patients With Schizophrenia:One-Year Follow up. [NCT00654576]Phase 41,400 participants (Anticipated)Interventional2005-02-28Completed
A Multicenter, Randomized, Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of RBP-7000 Using Poly (DL-lactide-co-glycolide) Polymer of Two Different Molecular Weights (Low and High Molecular Weights as Test Treatme [NCT02687984]Phase 144 participants (Actual)Interventional2016-02-29Completed
Sertraline Alone vs. in Combination With Risperidone in the Treatment of Attenuated Positive and Negative Symptoms [NCT00169988]8 participants (Actual)Interventional2004-03-31Completed
A Randomized, Multicenter Clinical Trial to Assess the Efficacy and Safety of Clozapine vs Treatment as Usual for Treatment-resistant Psychosis in Adolescents and Young Adults With Intellectual Disability. [NCT04529226]Phase 2114 participants (Anticipated)Interventional2020-11-26Recruiting
Interventional, Randomised, Double-blind, Parallel-group, Active-comparator, Flexible-dose Study to Compare the Effectiveness of Brexpiprazole to That of Risperidone in Adult Patients With Schizophrenia [NCT02758067]Phase 30 participants (Actual)Interventional2016-06-30Withdrawn(stopped due to This study was withdrawn for administrative reasons. There were no safety concerns.)
[NCT02535156]Phase 1/Phase 221 participants (Actual)Interventional2003-01-31Completed
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404]5,000 participants (Anticipated)Observational2020-03-05Recruiting
Bioequivalence Study of Risperidone 1.0 mg Tablets of Torrent Pharmaceuticals Limited., India and Risperdal® (Risperidone) 1.0 mg Tablets of Janssen Pharmaceutical Products, LP, USA, in Healthy Human Adult Subjects, Under Fasting Conditions [NCT00939497]Phase 10 participants InterventionalCompleted
Early Predictors of Poor Treatment Response in Patients With Schizophrenia Treated With Atypical Antipsychotics [NCT03730857]Phase 1111 participants (Actual)Interventional2008-01-31Completed
A Phase 2a, Randomized, Double-Blind, Placebo-Controlled, Parallel-group Study to Assess the Safety and Efficacy of ASP4345 as Add-on Treatment for Cognitive Impairment in Subjects With Schizophrenia on Stable Doses of Antipsychotic Medication [NCT03557931]Phase 2233 participants (Actual)Interventional2018-07-13Completed
Local Site Tolerability of Multiple Dose Treatment With Deltoid Intramuscular Injection of RISPERDAL CONSTA in Subjects With Chronic Schizophrenia. [NCT00828958]Phase 353 participants (Actual)Interventional2006-02-28Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Risperidone 1 mg Tablets and Risperdal® 1 mg Tablets Administered as a 1 x 1 mg Tablets in Subjects Under Fed Conditions [NCT00829894]Phase 124 participants (Actual)Interventional2001-06-30Completed
Randomized, Placebo-controlled, Double-blind, Parallel-group, Confirmatory Study of SM-13496 (Lurasidone HCl) in Patients With Schizophrenia [NCT00711269]Phase 3460 participants (Actual)Interventional2008-06-27Completed
Ziprasidone Versus Risperidone In The Treatment Of Chronic Schizophrenia: A Six Months, Double Blind Randomized, Parallel Group Study [NCT00645515]Phase 3240 participants (Anticipated)Interventional2003-06-30Terminated(stopped due to This study was terminated on November 20, 2003 because of poor recruitment. This study was not terminated due to safety/efficacy.)
Transcranial Direct Current Stimulation for Hallucinations in First-Episode Schizophrenia [NCT02661347]0 participants (Actual)Interventional2016-02-29Withdrawn(stopped due to Difficulty in recruiting patients who met the eligibility criteria.)
Joining Forces: Integrating Psychotropic Medication Into the Care of People With Mental Disorders in a Prayer Camp in Ghana [NCT02593734]Phase 4139 participants (Actual)Interventional2013-07-31Completed
Sertindole Versus Risperidone Safety Outcome Study: a Randomised, Partially-blinded, Parallel-group, Active-controlled, Post-marketing Study [NCT00856583]Phase 39,809 participants (Actual)Interventional2002-07-31Completed
Non-randomized Control Clinical Trial to Evaluate the Efficacy and Safety of Symptomatic Drug Therapy for Mild to Moderate Huntington's Disease Patients [NCT04071639]Phase 160 participants (Anticipated)Interventional2020-03-12Recruiting
Investigating Metabolic Side Effects of Antipsychotic Medications in Children [NCT00746252]5 participants (Actual)Interventional2008-06-30Terminated(stopped due to Due low rate of participation and lack of funding)
A Randomized, Double-Blind, Parallel-Group, Comparative Study of Flexible Doses of Paliperidone Palmitate and Flexible Doses of Risperidone Long-Acting Intramuscular Injection in Subjects With Schizophrenia [NCT00589914]Phase 31,221 participants (Actual)Interventional2007-03-31Completed
Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736]725,489 participants (Actual)Observational2012-04-30Completed
A Multi-center, Randomized, Open, Treatment-switching Study From Orally Administered Antipsychotic Monotherapy in the Treatment of Chronic Schizophrenic and Schizoaffective Patients [NCT00304616]Phase 4500 participants Interventional2004-10-31Completed
A 6-Week, Multicenter, Rater-blind, Randomized, Risperidone-controlled Study to Evaluate the Efficacy and Safety of Seroquel (Quetiapine Fumarate) in the Treatment of Chinese Han Patients With Schizophrenia [NCT00817648]Phase 4120 participants (Actual)Interventional2008-12-31Completed
Adjunctive Treatment With Divalproex or Risperidone for Aggression Refractory to Stimulant Monotherapy Among Children With ADHD [NCT00794625]Phase 4270 participants (Anticipated)Interventional2008-11-30Recruiting
The Consta Club: A Demonstration Project for Setting up a Consta Club in a Community Mental Health Center [NCT00845572]30 participants (Anticipated)Interventional2007-01-31Completed
Whole Blood and Plasma Sample Collection for the Development of Antipsychotic Immunoassays From Participants Taking Aripiprazole, Olanzapine, Paliperidone, or Risperidone [NCT02634463]Phase 181 participants (Actual)Interventional2015-11-30Completed
[NCT00633802]30 participants (Anticipated)Interventional2004-04-30Recruiting
Dopamine D2 and D3 Receptor Occupancy and Clinical Response in Older Patients With Schizophrenia [NCT00825045]14 participants (Anticipated)Interventional2008-12-31Active, not recruiting
An Open-label Study to Assess the Safety, Tolerability, Pharmacokinetics, and Efficacy of 180 mg Risperidone Subcutaneous Injection (PERSERIS) Following a Switch From 6 mg Oral Risperidone in Patients With Clinically Stable Schizophrenia [NCT03978832]Phase 469 participants (Actual)Interventional2019-06-28Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Risperidone 1 mg Tablets and Risperdal 1 mg Tablets Administered as a 1 x 1 mg Tablet in Healthy Subjects Under Fasting Conditions [NCT00830349]Phase 130 participants (Actual)Interventional2001-06-30Completed
A Phase IIa, Double-blind, Double-Dummy, Placebo-controlled, Active-controlled, Randomized, Parallel-Group Study to Assess the Efficacy, Safety, Tolerability, and Pharmacokinetics of AZD8529 in Adult Schizophrenia Patients [NCT00921804]Phase 2296 participants (Actual)Interventional2009-06-30Completed
Comparative Efficacy of Amisulpride vs Risperidone on Cognitive Functions in Patients With Chronic Schizophrenia [NCT00761670]Phase 437 participants (Actual)Interventional2008-09-30Completed
The Psychiatric and Cognitive Phenotypes in Velocardiofacial Syndrome (VCFS), Williams Syndrome (WS)and Fragile X Syndrome Characterization, Treatment and Examining the Connection to Developmental and Molecular Factors [NCT00768820]Phase 4400 participants (Anticipated)Interventional2001-05-31Recruiting
Metabolic Effects of Antipsychotics in Children [NCT00205699]Phase 4144 participants (Actual)Interventional2006-04-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Risperidone-Referenced, Parallel-Group, Adaptive-Design Study of the Efficacy, Safety, and Tolerability of Vabicaserin (SCA-136) in Subjects With Acute Exacerbations of Schizophrenia [NCT00563706]Phase 2199 participants (Actual)Interventional2007-12-31Completed
A Randomized, Double-Blind, Risperidone-Reference, Parallel-Group, Safety, and Tolerability Study of Vabicaserin (SCA-136) in Japanese Subjects With Acute Exacerbation of Schizophrenia [NCT00768612]Phase 20 participants (Actual)Interventional2008-11-30Withdrawn
Risperidone Pharmacokinetics in Children With Pervasive Developmental Disorder [NCT00147394]Phase 1100 participants Interventional2001-12-31Completed
Use, Effects and Side-effects of Second-generation Antipsychotics in a Naturalistic Setting. [NCT00932529]Phase 4226 participants (Actual)Interventional2003-02-28Completed
Does Risperidone Consta Reduce Relapse and Rehospitalization in Bipolar Disorder? [NCT00571688]Phase 450 participants (Actual)Interventional2007-11-30Completed
Sequenced Atypical Antipsychotics Therapy With Intensive or Basic Psychosocial Intervention for First-episode Schizophrenia: An Effectiveness Study [NCT01057849]600 participants (Anticipated)Interventional2008-09-30Recruiting
A Phase I, Open Label, Single Center, Single Ascending Dose Study of the Safety, Tolerability, and Pharmacokinetic Profile of RBP-7000 at Low, Medium, and High Doses [NCT02768649]Phase 145 participants (Actual)Interventional2011-04-30Completed
A Blinded-initiation Study of Medication Satisfaction in Subjects With Schizophrenia Treated With Paliperidone ER After Suboptimal Response to Oral Risperidone [NCT00535132]Phase 4201 participants (Actual)Interventional2007-10-31Completed
A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic [NCT02600741]296 participants (Actual)Observational2015-07-24Completed
A Phase 2B Randomized, Double-Blind, Placebo- and Active-Controlled Trial of the Efficacy and Safety of MK-8189 in Participants Experiencing an Acute Episode of Schizophrenia [NCT04624243]Phase 2500 participants (Anticipated)Interventional2020-12-15Recruiting
Pharmacological Treatment of Children and Adolescents With Severe Mood Dysregulation. An Open Trial With Risperidone. [NCT00825552]20 participants (Anticipated)Interventional2009-01-31Enrolling by invitation
A Randomized, Double-Blind, Comparison of the Efficacy and Safety of Risperidone Versus Risperidone Combined With Low Dose of Haloperidol in the Treatment of Schizophrenic Disorder [NCT00998608]Phase 488 participants (Actual)Interventional2007-08-31Terminated(stopped due to terminated)
Phase 4 Study of Efficacy and Safety of Tandospirone Combined With Atypical Antipsychotic Drugs to Improve Cognitive Function in Schizophrenia [NCT02040883]Phase 4100 participants (Anticipated)Interventional2014-02-28Not yet recruiting
Efficacy and Safety of Risperidone Oral Solution Combination Clonazepam Versus Haloperidol IM Injection for Treatment of Acute Psychotic Agitation in Schizophrenia [NCT00859872]Phase 4198 participants (Actual)Interventional2008-08-31Completed
Efficacy of Risperidone in the Management of Suicidality in Major Depressive Disorder [NCT00167154]Phase 330 participants (Actual)Interventional2004-06-30Completed
Prospective Double-Blind Randomized Comparison Study of Improvement in Negative Symptoms With Risperidone vs Risperidone +Citalopram Combination Therapy in Schizophrenia--a Clinical Study [NCT00893256]Phase 448 participants (Actual)Interventional2004-12-31Completed
Open-Label Comparative Study of Risperidone Versus Olanzapine for Mania in Preschool Children 4 to 6 Years of Age With Bipolar Spectrum Disorder [NCT00181935]Phase 440 participants Interventional2001-03-31Completed
[NCT00182013]Phase 4106 participants (Actual)Interventional2001-06-30Completed
Single-Dose, Open-Label Pilot Study to Explore the Pharmacokinetics, Safety and Tolerability of a Gluteal Intramuscular Injection of a 4-Week Long-Acting Injectable Formulation of Risperidone in Patients With Chronic Stable Schizophrenia [NCT00821600]Phase 124 participants (Actual)Interventional2008-12-31Completed
High Dose Risperidone Consta for Patients With Schizophrenia With Unsatisfactory Response to Standard Dose Risperidone or Long-Acting Injectable [NCT00539071]Phase 4160 participants (Actual)Interventional2008-03-31Completed
Paliperidone ER Versus Risperidone for Neurocognitive Function in Patients With Schizophrenia: a Randomized, Open-label, Controlled Trial [NCT00827840]Phase 458 participants (Actual)Interventional2008-11-30Completed
The Metabolic Syndrome in Patients With Schizophrenia [NCT00338949]Phase 477 participants (Actual)Interventional2006-06-30Completed
A Relative Bioavailability Study of Two Risperidone 1 mg Tablet Formulations Under Fed Conditions [NCT01064271]Phase 126 participants (Actual)Interventional2006-10-31Completed
Effect on Efficacy, Safety and Quality of Life by Long-Term Treatment of Long-Acting Risperidone Microspheres in Patients With Schizophrenia [NCT00269919]Phase 440 participants (Actual)Interventional2005-08-31Completed
Antipsychotic Discontinuation in Alzheimer's Disease [NCT00417482]Phase 4180 participants (Actual)Interventional2004-08-31Completed
Predicting Response to Risperidone Treatment Through Identification of Early-onset of Antipsychotic Drug Action in Schizophrenia. [NCT00337662]Phase 4628 participants (Actual)Interventional2006-05-31Completed
A 16-Week, Multicenter, Randomized, Open-label Study to Assess the Effects of Aripiprazole Versus Other Atypical Antipsychotics in the Treatment of Schizophrenic Patients With Metabolic Syndrome [NCT00508157]Phase 4125 participants (Actual)Interventional2007-11-30Terminated(stopped due to Slow Accrual)
A Relative Bioavailability Study of Two Risperidone 1 mg Tablet Formulations Under Fasting Conditions [NCT01064232]Phase 130 participants (Actual)Interventional2006-10-31Completed
A 2-year, Prospective, Blinded-rater, Open-label, Active-controlled, Multicenter, Randomized Study of Long-term Efficacy and Effectiveness Comparing Risperdal® Consta® and Abilify® (Aripiprazole) in Adults With Schizophrenia [NCT00299702]Phase 4355 participants (Actual)Interventional2006-02-28Completed
A Comparative Study of New Medications for Psychosis in Adolescents [NCT00222495]30 participants Interventional2002-08-31Completed
Prospective Cytochrome P450 Genotyping and Clinical Outcomes in Patients With Psychosis [NCT01878513]88 participants (Actual)Interventional2009-09-23Completed
Maintenance of Clinical Response With Risperidone Long Acting Injectable (R-LAI) in Patients With Schizophrenia or Schizoaffective Disorder [NCT01888107]Phase 3347 participants (Actual)Interventional2005-01-31Completed
An Exploratory Analysis of Immune and Inflammatory Response Associated With Clozapine Versus Non-Clozapine Antipsychotics in Individuals With Treatment-resistant Schizophrenia [NCT05741502]Phase 460 participants (Anticipated)Interventional2023-08-16Recruiting
Risperidone Monotherapy in the Treatment of PTSD in Women Survivors of Domestic Abuse and Rape Trauma: a Double-Blind, Placebo Controlled, Randomized Clinical Trial [NCT00208182]Phase 420 participants Interventional2001-07-31Completed
Divalproex ER vs. Risperidone for Bipolar Disorder With Comorbid Substance Use Disorder [NCT00203528]Phase 430 participants Interventional2004-01-31Completed
Effects of Classical and Atypical Antipsychotics on Dopamine Receptor Binding of 123I-epidepride, Cognition, Startle Response and Extrapyramidal Side-effects in Drug-naive First-episode Schizophrenic Patients [NCT00206960]56 participants (Actual)Interventional1998-01-31Completed
A Phase 2, Multicenter, Double-Blind, Placebo-Controlled Comparator Study of 2 Doses of LY2140023 Versus Placebo in Patients With DSM-IV-TR Schizophrenia [NCT01086748]Phase 2880 participants (Anticipated)Interventional2010-03-31Completed
A Parallel-Group Comparative Open-Label Study of Long-Acting Injectible Risperidone Versus Risperidone Tablets in Patients With Schizophrenia. [NCT00240708]Phase 3205 participants (Actual)Interventional2004-06-30Completed
A Multicenter, Open-Label Study to Evaluate Safety and Efficacy of Risperidone as Adjunctive Therapy to Mood Stabilizers in the Long-term Treatment of Bipolar Mania [NCT00216554]Phase 4118 participants (Actual)Interventional2004-09-30Completed
Treatment Success in Patients Requiring Treatment Change From Olanzapine to Risperidone Long Acting Injectable (TRESOR) [NCT00216632]Phase 499 participants (Actual)Interventional2005-03-31Completed
Risperidone Depot (Microspheres) in the Treatment of Subjects With Schizophrenia or Schizoaffective Disorder - an Open Label Follow up Trial of RIS-INT-57 and RIS-INT-61. [NCT00558298]Phase 3811 participants (Actual)Interventional2000-02-29Completed
A Randomized, Open-label Trial of RISPERDAL® CONSTA™ Versus Oral Antipsychotic Care in Subjects With Bipolar Disorder [NCT00246246]Phase 348 participants (Actual)Interventional2004-01-31Completed
The Efficacy And Safety Of Risperidone In The Treatment Of Adolescents With Schizophrenia: A Six-Month Open-Label Study. [NCT00246285]Phase 3381 participants (Actual)Interventional2001-04-30Completed
Evaluation of Efficacy and Safety of Long-acting Risperidone Microspheres in Patients With Schizophrenia or Other Psychotic Disorders When Switching From Typical Antipsychotic (Oral/Depot) or Atypical Oral Other Than Risperidone [NCT00563017]30 participants (Anticipated)Interventional2004-10-31Recruiting
A Randomized, Open-Label, Single Dose, Cross-over Study of Gastric Emptying Rate: SEP-363856 vs Prior Antipsychotic Standard of Care in Subjects With Schizophrenia [NCT05402111]Phase 131 participants (Actual)Interventional2022-06-13Completed
Atypical Antipsychotics for Continuation and Maintenance Treatment After an Acute Manic Episode [NCT01977300]Phase 3159 participants (Actual)Interventional2003-01-31Completed
Comparison of Oral Risperdal in Combination With Oral Lorazepam vs Standard Care Including Initial Conventional Neuroleptic IM Treatment, in Acute Schizophrenic Patients [NCT00249171]Phase 4226 participants (Actual)Interventional2001-06-30Completed
A Comparison of Risperidone and Haloperidol for Prevention of Relapse in Subjects With Schizophrenia and Schizoaffective Disorders [NCT00253110]Phase 4396 participants (Actual)Interventional1996-05-31Completed
Reducing the Abuse Liability of Prescription Opioids [NCT04587115]Early Phase 115 participants (Actual)Interventional2017-06-16Completed
Safety and Efficacy of Seroquel in First Episode Schizophrenia [NCT00254241]Phase 480 participants Interventional2002-05-31Completed
Clozapine-Augmentation With Ziprasidone or Risperidone, a Randomized, Prospective Trial [NCT00224315]Phase 424 participants Interventional2003-11-30Completed
Cannabidiol for Treatment of Non-affective Psychosis and Cannabis Use [NCT04105231]Phase 2130 participants (Anticipated)Interventional2021-06-01Recruiting
Assessment of Incidence of Adverse Events in a Naive Pediatric Population Treated With an (Typical and Atypical) Antipsychotic Drug Over 12 Months Follow-up [NCT02007928]200 participants (Actual)Interventional2013-04-30Completed
Bioequivalence Test for Risperdal OD Tab. 2mg of Janssen Korea [NCT02012049]Phase 136 participants (Actual)Interventional2009-08-31Completed
A SINGLE-CENTER, RANDOMIZED, INVESTIGATOR/SUBJECT-BLIND, MULTIPLE-DOSE, PLACEBO-CONTROLLED, PARALLEL STUDY TO INVESTIGATE THE SAFETY, TOLERABILITY AND PHARMACOKINETICS OF RO5545965 IN PATIENTS WITH SCHIZOPHRENIA ON RISPERIDONE. [NCT02019329]Phase 132 participants (Actual)Interventional2014-01-31Completed
Risperidone and Behavioral Therapy in Treatment of Children and Adolescents With Autistic Disorder [NCT00080145]124 participants (Actual)Interventional2004-02-29Completed
The Effect of Sertindole and Risperidone on Endophenotypic Markers of Schizophrenia, a Comparative Study [NCT02021201]Phase 41 participants (Actual)Interventional2008-07-31Terminated(stopped due to No suitable patients could be recruited in the available time period)
Glutamate, Brain Connectivity and Duration of Untreated Psychosis [NCT02034253]134 participants (Actual)Observational2014-01-31Completed
[NCT00006195]0 participants InterventionalRecruiting
Risperidone for the Treatment of Huntington's Disease Chorea [NCT04201834]Phase 212 participants (Anticipated)Interventional2020-08-13Suspended(stopped due to Temporarily on pause due to updating protocol and other study measurements and design)
A Six-week, Randomized, Double-blind, Placebo-controlled, Parallel Group, Multi-center, Phase II Study to Determine the Efficacy, Tolerability and Safety of Low and High Non-overlapping Dose Ranges of BL-1020 Compared to Placebo and Risperidone [NCT00567710]Phase 2360 participants (Anticipated)Interventional2008-07-31Completed
Insulin Sensitivity in Patients With Schizophrenia or Schizoaffective Disorder Treated With Olanzapine and Risperidone [NCT00190749]Phase 4130 participants (Actual)Interventional2003-10-31Completed
A Random Assignment,Parallel Group, Open Label Comparison of Clinical Outcomes and Resource Utilization Among Bipolar Disorder Patients Receiving Either Long Acting Injectable Risperidone Microspheres (Risperdal Consta® ) or Other Second Generation Oral A [NCT00177164]Phase 350 participants (Actual)Interventional2003-11-30Completed
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371]1,037,352 participants (Actual)Observational2016-09-30Completed
Comparison of Single-Dose Plasma and Blood Concentrations of Aripiprazole, Olanzapine, Quetiapine, Paliperidone and Risperidone After Capillary and Venous Blood Sample Collection [NCT01607762]Phase 131 participants (Actual)Interventional2012-02-29Completed
Comparison of Quetiapine Extended-Release (Seroquel XR™) and Risperidone in the Treatment of Depressive Symptoms, in Schizophrenic or Schizoaffective Patients: A Randomized, Open Label, Flexible-dose, Parallel Group, Non Inferiority, 12-week Study [NCT00640562]Phase 3216 participants (Actual)Interventional2008-02-29Completed
A Six-Week, Randomized, Double-Blind, Parallel Group Extension Study To Evaluate The Long-Term Safety, Tolerability, And Efficacy Of Low And High Doses Of Bl-1020 Compared To Risperidone [NCT00722176]Phase 2220 participants (Anticipated)Interventional2008-06-30Completed
Risperidone Long Acting: A Healthcare Resource Utilization Pilot Study [NCT00272597]Phase 430 participants (Actual)Interventional2005-09-30Completed
A Randomized Double-blind Trial of Aripiprazole and Risperidone in Schizophrenia: An Evaluation of Neuroimaging, Neuropsychological, and Pharmacogenomic Markers of Differential Treatment Response [NCT00712270]Phase 421 participants (Actual)Interventional2005-04-30Terminated(stopped due to Study terminated due to failure to meet sufficient enrollment for valid analysis)
A Phase 2, Multicenter, Double-blind, Randomized, Parallel Group, 4-week Inpatient Study To Evaluate The Safety And Efficacy Of Two Fixed Doses Of Pf-02545920 Compared To Placebo In The Treatment Of Acute Exacerbation Of Schizophrenia Using Risperidone As [NCT01175135]Phase 2259 participants (Actual)Interventional2010-10-31Completed
A Fifteen-month, Prospective, Randomized, Active-controlled, Open-label, Flexible Dose Study of Paliperidone Palmitate Compared With Oral Antipsychotic Treatment in Delaying Time to Treatment Failure in Adults With Schizophrenia Who Have Been Incarcerated [NCT01157351]Phase 4450 participants (Actual)Interventional2010-05-31Completed
A Bioequivalence Study Comparing a Single Oral Intake of a 4mg Orally-disintegrating Tablet With a 4mg Conventional Risperdal Tablet in Patients With Schizophrenia [NCT00645502]Phase 140 participants (Actual)Interventional2003-06-30Completed
The Role of miR-30 Family Dysregulation in Response to Antipsychotic Treatment [NCT02650102]Phase 1/Phase 2200 participants (Anticipated)Interventional2013-01-31Recruiting
Phase IV Study of General Clinical Research Center Of the Jinan Mental Hospital(TAIWAN) [NCT00626613]Phase 40 participants InterventionalActive, not recruiting
Pharmacogenetics of Risperidone in Children With Pervasive Developmental Disorder (PDD) [NCT00166595]Phase 1/Phase 2100 participants Interventional2003-02-28Completed
Treatment of Geriatric Bipolar Mood Disorders: A Pilot Study [NCT00177567]Phase 460 participants Interventional2001-07-31Completed
A Randomized, Double-Blind, Placebo-Controlled Clinical Study of the Efficacy and Safety of Risperidone for the Treatment of Schizophrenia in Adolescents [NCT00088075]Phase 3160 participants (Actual)Interventional2004-08-31Completed
Risperidone (Risperdal) Augmentation in Depressed Partial Responders to SRI Treatment [NCT00178854]Phase 40 participants (Actual)Interventional2004-05-31Withdrawn(stopped due to failed recruitment efforts)
A Double-Blind Study Comparing Adjunctive Risperidone Versus Placebo in Major Depressive Disorder That Is Not Responding to Standard Therapy [NCT00095134]Phase 3630 participants (Actual)Interventional2004-10-31Completed
A Randomized, Double-Blind, Crossover Add-On Study To Assess The Differential Sensitivity Of 2 Spatial Working Memory Tests (The Groton Maze Learning Test [GMLT] And The Motor Delayed Response Test [MDR]) In Non-Agitated, Antipsychotic Drug-Naive First-Ep [NCT00174200]20 participants Interventional2004-12-31Completed
Efficacy of Risperidone Versus Haloperidol in the Treatment of Aggression and Hostility in Psychotic Inmates [NCT00203775]0 participants Interventional2002-07-31Terminated
Risperidone Maintenance Treatment for Relapse Prevention in Schizophrenia [NCT00848432]Phase 4404 participants (Actual)Interventional2002-12-31Completed
Treatment of Major Depressive Disorder With Psychotic Features With Risperidone Monotherapy; Risperidone and Sertraline; or Haloperidol and Sertraline [NCT00174590]Phase 330 participants Interventional2001-09-30Terminated
A 16-Week, Randomized, Controlled Trial of the Effect of Aripiprazole Versus Standard of Care on Non-HDL Cholesterol Among Patients With Schizophrenia and Bipolar I Disorder Who Have Pre-existing Metabolic Syndrome [NCT00857818]Phase 364 participants (Actual)Interventional2009-04-30Terminated(stopped due to Slow Accrual)
The Treatment Efficacy of Combination Atypical Antipsychotics With Sertraline in Patients With Schizophrenia [NCT04076371]1,640 participants (Actual)Interventional2012-01-31Completed
Risperidone in the Treatment of Psychotic-like and Deficit Symptoms of Schizotypal Personality Disorder [NCT00158028]25 participants (Actual)Interventional1995-11-30Completed
A Prospective, Open-Label Study to Evaluate Symptomatic Remission in Schizophrenia With Long Acting Risperidone Microspheres (Risperdal Consta) [NCT00216528]Phase 4527 participants (Actual)Interventional2005-07-31Completed
Placebo-Controlled Trial of Risperidone Augmentation for SSRI-Resistant Civilian PTSD [NCT00215241]Phase 2/Phase 380 participants Interventional2004-04-30Completed
Evaluation of Efficacy and Safety of Long-acting Risperidone Microspheres in Patients With Schizophrenia or Schizoaffective Disorders, Who is Receiving Psychiatric Home-care Treatment, When Switching From Typical Depot or Oral Antipsychotics to Long-actin [NCT00526877]Phase 431 participants (Actual)Interventional2007-07-31Completed
Phase 1 Study of Insulin Sensitivity, Adjusted β-Cell Function and Adiponectin Among Lean Drug-naïve Schizophrenic Subjects Treated With Atypical Antipsychotic Drugs [NCT00528359]36 participants (Actual)Observational2005-10-31Completed
A Randomized, Double-Blind, Placebo- and Active-Controlled, Multi-Center Study to Assess the Antipsychotic Efficacy of ITI-007 After 6 Weeks of Treatment in Patients With Schizophrenia [NCT02469155]Phase 3696 participants (Actual)Interventional2015-06-30Completed
Glucose and Lipid Metabolism on Antipsychotic Medication [NCT00515723]96 participants (Actual)Interventional2001-09-30Completed
Early Versus Late Initiation of Treatment With Risperdal Consta in Subjects With Schizophrenia After an Acute Episode [NCT00216671]Phase 4220 participants (Actual)Interventional2005-11-30Completed
An Open-Label, Multiple Dose, Safety and Pharmacokinetic Trial With Injectable ZX003 (Risperidone-SABER®) Compared to Risperdal® Consta® in Patients With Chronic, Stable Schizophrenia or Schizoaffective Disorder [NCT02411526]Phase 160 participants (Actual)Interventional2015-02-28Completed
Risperidone for the Treatment of Cocaine Dependence [NCT00000342]Phase 20 participants Interventional1996-07-31Completed
CONSTATRE: Risperdal Consta Trial Of Relapse Prevention And Effectiveness [NCT00216476]Phase 3753 participants (Actual)Interventional2004-10-31Completed
A Biological Basis of Therapy for Negative Symptom Spectrum Disorders: Risperdal Effect on Frontal Metabolism in Asperger's Disorder [NCT00352196]Phase 423 participants (Actual)Interventional2001-11-30Completed
Risperdal Safety Protocol Evaluation Consta Treatment; A Post Authorization Safety Survey With RISPERDAL CONSTA TM [NCT00458367]5,296 participants (Actual)Observational2002-06-30Completed
Discontinuation of Antipsychotics and Antidepressants Among Patients With Dementia and BPSD Living in Nursing Homes - an Open Study. [NCT00433121]Phase 424 participants (Actual)Interventional2006-09-30Completed
Serotonin/Dopamine Antagonism of Cocaine Effect [NCT00000309]Phase 20 participants Interventional1994-08-31Terminated(stopped due to Unable to recruit adequate number of subjects)
Managing Acute Schizophrenia, a Double Blind Comparison Between Two Atypical Antipsychotics - Olanzapine and Risperidone [NCT00485498]Phase 4122 participants (Actual)Interventional2003-04-30Completed
BMI-2002 Study: Evaluation of Functionality and Evolution of Body Weight of Psychotic Patients With a High Body Mass Index [NCT00511628]1,717 participants (Actual)Observational2001-07-31Terminated(stopped due to Due to the achievement of minimum required sample size and new changes in local regulations.)
Aggressiveness and Agitation of Acute Psychotic Patients: Influence in Safety and Effectiveness of Risperidone Treatment [NCT00515489]1,882 participants (Actual)Observational2001-11-30Terminated(stopped due to Due to the achievement of minimum required sample size and new changes in local regulations.)
"Re-examining Maintenance Antipsychotic Treatment in Schizophrenia: Extended Antipsychotic Dosing" [NCT04478838]Phase 4120 participants (Anticipated)Interventional2022-06-06Recruiting
The Efficacy And Safety Of Flexible Dose Ranges Of Risperidone Versus Placebo Or Haloperidol In The Treatment Of Manic Episodes Associated With Bipolar I Disorder. [NCT00253162]Phase 3439 participants (Actual)Interventional2001-03-31Completed
Pediatric Trials Network Long-term Antipsychotic Pediatric Safety Trial (LAPS) NICHD-2016-LAP01 Phase 4 Trial [NCT03522168]509 participants (Actual)Observational2019-01-10Active, not recruiting
Metabolic Profile and Anthropometric Changes in Schizophrenia [NCT00534183]2,006 participants (Actual)Interventional2006-06-30Completed
The Optimal Treatment for Treatment-resistant Schizophrenia [NCT02926976]150 participants (Anticipated)Interventional2016-11-30Recruiting
"The Therapeutic Window of the Atypical Antipsychotic Paliperidone Extended Release (ER)-A Positron Emission Tomography Study With [18F]Fallypride as the Radiotracer" [NCT00934635]Phase 42 participants (Actual)Interventional2009-09-30Terminated
Risperidone Depot (Microspheres) vs. Placebo in the Treatment of Subjects With Schizophrenia [NCT00253136]Phase 3458 participants (Actual)Interventional1999-11-30Completed
Placebo-Controlled Study of Risperidone for the Treatment of Children and Adolescents With Autism and Negative Behavioral Symptoms [NCT00005014]Phase 3101 participants (Actual)Interventional1997-10-31Completed
Assessment and Treatment of Impulsivity and Thought Process Disorder in Patients With Active Suicidal Ideation and Depression. [NCT01770600]0 participants (Actual)Interventional2010-04-30Withdrawn(stopped due to never initiated, did different study)
Differences in Cognitive Function Due to Acute Sedative Effects of Risperidone and Quetiapine in Stable Bipolar I Out-Patients. [NCT00097032]Phase 330 participants (Actual)Interventional2004-10-31Completed
An Open-label Study of the Efficacy and Safety of RISPERDAL Long-acting Microspheres (RISPERDAL CONSTA) Administered Once Monthly in Adults With Schizophrenia or Schizoaffective Disorder [NCT00236353]Phase 386 participants (Actual)Interventional2002-05-31Completed
Risperidone in the Treatment of Children and Adolescents With Conduct and Other Disruptive Behavior Disorders - an Open Label Follow-up Trial of CR002020 [NCT00236470]Phase 3232 participants (Actual)Interventional2002-01-31Completed
An Open-label Evaluation of the Utility of the RISPERDAL CONSTA Treatment Guidebook During Transition of Adult Patients With Schizophrenia or Schizoaffective Disorder to RISPERDAL CONSTA (Risperidone) Treatment Over Three Months in the Community Mental He [NCT00236548]Phase 31 participants (Actual)InterventionalCompleted
An Open Label, Long Term Trial of Risperidone Long Acting Microspheres in the Treatment of Patients Diagnosed With Schizophrenia [NCT00236587]Phase 3100 participants (Actual)Interventional2001-11-30Completed
Severe Aberrant Behavior Among Persons With Mental Retardation. Project III: Behavioral Selectivity of Atypical Neuroleptic Drugs: Effects on Cognitive and Social Behaviors [NCT00065273]Phase 350 participants Interventional1998-07-31Completed
A Multicenter, Randomized, Naturalistic, Open-Label Study Between Aripiprazole and Standard of Care in the Management of Community-Treated Schizophrenic Patients (Schizophrenia Trial of Aripiprazole - STAR) [NCT00237913]Phase 3700 participants Interventional2004-07-31Completed
Metabolic Effects of Newer Antipsychotics in Older Patients [NCT00245206]Phase 4406 participants (Actual)Interventional2005-08-31Completed
Risperidone in the Treatment of Behavioral Disturbances in Demented Patients: an International, Multicenter, Placebo-controlled, Double-blind, Parallel-group Trial Using Haloperidol as Internal Reference [NCT00249145]Phase 3349 participants (Actual)Interventional1995-04-30Completed
Risperidone Depot (Microspheres) vs. Risperidone Tablets - a Non-inferiority, Efficacy Trial in Subjects With Schizophrenia [NCT00249223]Phase 3641 participants (Actual)Interventional2000-01-31Completed
The Safety And Efficacy Of Risperidone Versus Placebo In Conduct Disorder In Mild, Moderate And Borderline Mentally Retarded Children Aged 5 To 12 Years [NCT00250354]Phase 3110 participants (Actual)Interventional1997-09-30Completed
A Randomized, Double-Blind, Placebo-Controlled Study of Risperidone for Treatment of Behavioral Disturbances in Subjects With Dementia [NCT00253123]Phase 3626 participants (Actual)InterventionalCompleted
Efficacy And Safety Of Risperidone In The Treatment Of Children With Autistic Disorder And Other Pervasive Developmental Disorders: A Canadian, Multicenter, Double-Blind, Placebo-Controlled Study [NCT00261508]Phase 380 participants (Actual)Interventional1999-08-31Completed
Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Intramuscular Injections of Risperidone ISM® in Patients With Acute Exacerbation of Schizophrenia: Open Label Extension (PRISMA-3_OLE) [NCT03870880]Phase 3215 participants (Actual)Interventional2017-08-25Completed
Continuation Pharmacotherapy for Agitation of Dementia [NCT00073658]Phase 2137 participants Interventional2000-01-31Completed
A Parallel Study to Investigate Dopaminergic D2 and Serotoninergic 5HT2A Receptor Occupancy at Stable Plasma Concentrations of SB-773812 After Repeated Doses in Schizophrenic Patients. Relationship With Pharmacokinetics and Efficacy Readouts. [NCT00269035]Phase 195 participants (Actual)Interventional2005-06-21Completed
International Study of Improving Treatment for the Most Severely Ill With Schizophrenia [NCT00272584]Phase 4100 participants Interventional2001-06-30Completed
A Randomized, Double-Blind, Placebo-Controlled Study of Risperidone Monotherapy in Ambulatory Bipolar Disorder With Concurrent Moderately Severe Anxiety and Lifetime Panic or Generalized Anxiety Disorder [NCT00277654]Phase 3111 participants (Actual)Interventional2004-02-29Completed
Research on the Effectiveness of Risperidone in Bipolar Disorder in Adolescents and Children (REACH): A Double-Blind, Randomized, Placebo-Controlled Study of the Efficacy and Safety of Risperidone for the Treatment of Acute Mania in Bipolar I Disorder [NCT00076115]Phase 313 participants (Actual)Interventional2003-12-31Completed
An Open-Label Trial of Long-Acting Injectable Risperidone in the Treatment of Methamphetamine Dependence [NCT00284206]Phase 220 participants (Anticipated)Interventional2006-01-31Completed
Risperidone Augmentation in Patients With Schizophrenia Partially Responsive to Clozapine [NCT00289861]Phase 424 participants (Actual)Interventional2003-02-28Completed
A Double-blind, Randomized, Prospective Study to Evaluate Adjunctive Risperidone Versus Adjunctive Placebo in Generalized Anxiety Disorder Sub-optimally Responsive to Standard Psychotropic Therapy [NCT00086112]Phase 3301 participants (Actual)InterventionalCompleted
A Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Crossover, Bioequivalence Study of Risperidone Tablet 1 mg With Risperdal® 1 mg in Normal, Healthy, Adult, Human Subjects Under Fasting Condition [NCT01722201]Phase 148 participants (Actual)Interventional2012-06-30Completed
Effects of Risperidone on Cognitive-Motor Performance and Motor Movements in Chronically Medicated Children [NCT00399698]Phase 330 participants Interventional1999-05-31Completed
Efficacy of Quetiapine Compared to Risperidone on Negative Symptoms and Cognition With Regard to Underlying Neurobiological Mechanisms and Brain Activation. [NCT00305422]Phase 345 participants (Actual)Interventional2001-11-30Completed
A Multi-centre Comparative Study to Evaluate the Anti-aggression Effect and Safety of Zotepine Versus Risperidone in Aggressive Schizophrenic Patients of Acute Ward [NCT00418873]Phase 439 participants (Actual)Interventional2007-03-31Terminated(stopped due to Study was stopped due to difficulty in patient enrollment)
A 52-wk Prospective, Randomized, Double-blind, Multicenter Study of Relapse Following Transition From Oral Antipsychotic Medication to 2 Different Doses (25 or 50 mg Every 2 Wks) of Risperidone Long-acting Microspheres (Risperdal� CONSTA�) in Adults With [NCT00297388]Phase 340 participants (Actual)InterventionalCompleted
Risperidone Augmentation for Treatment-Resistant Aggression in ADHD [NCT00297739]Phase 425 participants Interventional2003-01-31Completed
A Prospective, Randomized, Double-blind, Placebo-controlled Study of the Effectiveness and Safety of RISPERDAL CONSTA Augmentation in Adult Patients With Frequently-relapsing Bipolar Disorder [NCT00094926]Phase 3275 participants (Actual)Interventional2004-05-31Completed
A Randomized Controlled Trial Study of Risperidone and Olanzapine for the Schizophrenic Patients With Neuroleptic-Induced Acute Dystonia or Parkinsonism [NCT00331825]Phase 470 participants Interventional2000-07-31Completed
A Multicenter, Open-Label, Parallel-Group, Randomized, Flexible Dose Study To Evaluate the Safety and Tolerability of Switching From Existing Atypical Antipsychotics to Bifeprunox in Subjects With Schizophrenia or Schizoaffective Disorder [NCT00347425]Phase 3286 participants (Actual)Interventional2006-12-31Completed
A Multicenter, Double-Blind, Double-Dummy, Placebo-Controlled, Randomized, Parallel Group Evaluation of the Efficacy and Safety of a Fixed-Dose of Talnetant Versus Placebo Versus Risperidone in Subjects With Schizophrenia [NCT00103727]Phase 2282 participants (Actual)Interventional2004-12-31Completed
The Cognitive Effects of Risperidone and Olanzapine [NCT00108368]Phase 40 participants Interventional2003-10-31Completed
Comparison of Cognitive Functions of Schizophrenic Patients Treated With Sertindole Versus Risperidone [NCT00480844]Phase 460 participants (Anticipated)Interventional2008-10-31Recruiting
Is Premorbid Functioning a Predictor of Outcome in Patients With Early Onset Psychosis Treated With Risperdal Consta? [NCT00369239]Phase 4303 participants (Actual)Interventional2006-03-31Completed
Risperidone Depot (Microspheres) in the Treatment of Subjects With Schizophrenia or Schizoaffective Disorder - an Open-label Follow-up Trial of RIS-INT-62 and RIS-INT-85. [NCT00495118]Phase 3314 participants (Actual)Interventional2001-10-31Completed
Randomized, Open Label, 8-Week Study of Quetiapine and Risperidone on Quality of Life in Female With Schizophrenia [NCT00498004]Phase 4100 participants (Anticipated)Interventional2007-08-31Terminated(stopped due to difficult to recruit subject)
One Year Maintenance Treatment With Low Dose Haloperidol vs. Risperidone in First-Episode Schizophrenia [NCT00159081]Phase 4159 participants (Actual)Interventional2000-11-30Completed
Efficacy of Risperidone Consta for Improving Ability to Benefit From Skills Training in Schizophrenia [NCT00148083]Phase 35 participants (Actual)Interventional2005-09-30Completed
Stimulant and Risperidone in Children With Severe Physical Aggression [NCT00796302]Phase 4168 participants (Actual)Interventional2008-08-31Completed
Evaluation of Growth, Sexual Maturation, and Prolactin-Related Adverse Events in the Pediatric Population Exposed to Atypical Antipsychotic Drugs [NCT01050582]Phase 4244 participants (Actual)Interventional2009-10-31Completed
Tolerability, Safety, And Efficacy Of Ziprasidone (80 - 160 Mg/D) Versus Olanzapine (10 - 20 Mg/D), Risperidone (4 - 8 Mg/D) Or Quetiapine (300 - 750 Mg/D) In Pretreated Patients With Schizophrenia, Schizoaffective Disorder Or Schizophreniform Disorders - [NCT00159770]Phase 3290 participants Interventional2001-11-30Completed
[NCT00161018]Phase 3150 participants Interventional2003-11-30Completed
Seroquel (Quetiapine) Therapy for Schizophrenia and Schizoaffective Disorders and Comorbid Cocaine and/or Amphetamine Abuse/Dependence: A Comparative Study With Risperidone [NCT00208143]Phase 420 participants Interventional2003-11-30Completed
A Comparison Study of Combined ECT and Risperidone Versus ECT Alone for Treatment Resistant Depression. [NCT00203723]Phase 445 participants Interventional2005-03-31Terminated
Effective Measurement of Risperidone Treatment Outcome for Persons With Borderline Personality Disorder: The UAB Borderline Rating Scale (BRS) [NCT00204347]Phase 420 participants Interventional2003-07-31Completed
A Single-blind Trial of Risperidone vs. Paroxetine for Treatment of Panic Attacks [NCT00206765]Phase 290 participants (Anticipated)Interventional2003-01-31Terminated
Effectiveness of Atypical Vs Conventional Antipsychotics [NCT00237861]Phase 40 participants InterventionalCompleted
[NCT00215579]Phase 464 participants (Actual)Interventional2004-04-30Completed
Risperidone Versus Haloperidol Versus Placebo in the Treatment of Chronic Schizophrenia [NCT00249132]Phase 3523 participants (Actual)InterventionalCompleted
The Safety And Efficacy Of Risperdal� (Risperidone) Versus Placebo Versus Haloperidol As Add-On Therapy To Mood Stabilizers In The Treatment Of The Manic Phase Of Bipolar Disorder [NCT00253149]Phase 3158 participants (Actual)InterventionalCompleted
Different Safety Profile of Risperidone and Paliperidone Extended-release: a Double-blind, Placebo-controlled Trial With Healthy Volunteers [NCT01284959]Phase 434 participants (Actual)Interventional2010-06-30Completed
A Single-Blind Trial of Risperidone vs. Paroxetine for Treatment of Panic Attacks [NCT00457106]90 participants (Anticipated)Interventional2002-06-30Completed
Antipsychotic Polypharmacy in Schizophrenia [NCT00493233]100 participants (Anticipated)Interventional2006-11-30Completed
A Pilot, Open-Label, Non-Randomized, Single Ascending Dose, Safety and Pharmacokinetic Trial With Injectable Risperidone-SABER and the DosePro Delivery System in Patients With Chronic, Stable Schizophrenia or Schizoaffective Disorder [NCT01592110]Phase 140 participants (Actual)Interventional2012-07-31Completed
Risperidone for Treatment of Cocaine Dependence in Outpatients [NCT00000347]Phase 20 participants Interventional1997-07-31Completed
Systematic Treatment Enhancement Program for Bipolar Disorder (STEP-BD) [NCT00012558]5,000 participants Interventional1998-09-30Completed
Comparative Effectiveness of Antipsychotic Medications in Patients With Schizophrenia (CATIE Schizophrenia Trial) [NCT00014001]Phase 41,600 participants Interventional2000-12-31Completed
Efficacy And Safety Of A Flexible Dose Of Risperidone Versus Placebo In The Treatment Of Psychosis Of Alzheimer's Disease. [NCT00034762]Phase 3473 participants (Actual)Interventional2000-12-31Completed
Specific Interventions for Agitation in Alzheimer's Disease [NCT00018291]0 participants Interventional2001-01-31Completed
Treatment and Outcome of Early Onset Bipolar Disorder [NCT00048802]Phase 440 participants Interventional2002-08-31Completed
A Study to Evaluate the Safety, Tolerability, and Effect of Risperidone Extended-Release Injectable Suspension (TV-46000) for Subcutaneous Use as Maintenance Treatment in Adult and Adolescent Patients With Schizophrenia [NCT03893825]Phase 3336 participants (Actual)Interventional2019-04-17Completed
Comparative Effectiveness of Antipsychotic Medications in Patients With Alzheimer's Disease (CATIE Alzheimer's Disease Trial) [NCT00015548]450 participants Interventional2001-03-31Completed
Measurement of Risperidone and 9-Hydroxyrisperidone in Plasma and Saliva [NCT00395499]19 participants Observational2001-05-31Completed
The Efficacy and Safety of Risperidone in Adolescents With Schizophrenia: a Comparison of Two Dose Ranges of Risperidone [NCT00034749]Phase 3279 participants (Actual)Interventional2001-04-30Completed
[NCT00034905]Phase 40 participants Interventional2001-07-31Completed
The Minimal Effective Dose of Antipsychotic Medication in Older Patients With Schizophrenia: a PET Study. [NCT00716755]45 participants (Actual)Interventional2009-10-31Completed
Antipsychotic Response to Clozapine in B-SNIP Biotype-1 (Clozapine) [NCT04580134]Phase 4524 participants (Anticipated)Interventional2022-03-01Recruiting
Psychopharmacologic Aspects of Motor Slowing in Schizophrenia [NCT00018668]Phase 40 participants Interventional2000-10-31Completed
Olanzapine Versus Active Comparator in the Treatment of Bipolar I Disorder, Manic or Mixed [NCT00034580]Phase 4326 participants Interventional2001-08-31Completed
Open-Label Trial Exploring A Switching Regimen From Oral Neuroleptics, Other Than Risperidone, To Risperidone Depot Microspheres [NCT00034775]Phase 3141 participants (Actual)Interventional2001-08-31Completed
Efficacy and Tolerability of Olanzapine, Quetiapine and Risperidone in the Treatment of First Episode Psychosis: A Randomized Double Blind 52-Week Comparison [NCT00034892]Phase 30 participants Interventional2002-03-31Completed
Developmental Processes in Schizophrenic Disorders: Improving and Predicting Work Outcome in Recent-Onset Schizophrenia [NCT00203788]Phase 487 participants (Actual)Interventional1999-05-31Completed
Glucose Regulation During Risperidone and Olanzapine Treatment [NCT00205738]120 participants (Actual)Interventional2000-07-31Completed
Maximizing Treatment Outcome in OCD [NCT00389493]100 participants (Actual)Interventional2006-10-31Completed
Randomized Comparison of Monotherapy (Risperidone, Quetiapine, or Olanzapine) Versus Combination Therapy (Risperidone, Quetiapine, or Olanzapine + Divalproex)in the Management of Dementia With Agitation: A Pilot Comparison of Two Standard Therapies [NCT00208819]Phase 450 participants (Anticipated)Interventional2003-09-30Completed
A Study of the Safety and Efficacy of Depakote ER Plus an Atypical Antipsychotic Vs. an Atypical Antipsychotic Alone in the Treatment of Schizophrenia [NCT00073164]Phase 2400 participants Interventional2003-07-31Completed
Risperidone Depot (Microspheres) in the Treatment of Subjects With Schizophrenia or Schizoaffective Disorder [NCT00210691]Phase 3273 participants (Actual)Interventional1999-12-31Completed
An Open-label Trial of Risperidone Long-acting Injectable in the Treatment of Subjects With Recent Onset Psychosis [NCT00216580]Phase 350 participants (Actual)Interventional2004-02-29Completed
A Study to Evaluate the Efficacy, Safety and Maintenance Effect of Risperidone Augmentation of SSRI Monotherapy in Young and Older Adult Patients With Unipolar Treatment-Resistant Depression [NCT00044681]Phase 3258 participants (Actual)Interventional2002-10-31Completed
Placebo-Controlled Trial of Risperidone Augmentation for SSRI-Resistant Civilian PTSD [NCT00133822]Phase 1/Phase 265 participants Interventional2004-04-30Completed
A Multicenter, Double-Blind, Double-Dummy, Placebo-Controlled, Randomized, Parallel Group Evaluation of the Efficacy and Safety of a Fixed-Dose of Talnetant Versus Placebo Versus Risperidone in Subjects With Schizophrenia [NCT00049946]Phase 2231 participants Interventional2002-10-31Completed
Optimization of Acute Treatment in First Episode Schizophrenic Patients by New Pharmacological Treatments [NCT00157378]Phase 4300 participants Interventional2000-11-30Active, not recruiting
A Randomized, Double-Blind, Placebo-Controlled Study of Risperidone Monotherapy in Ambulatory Bipolar Disorder With Current at Least Moderately Severe Anxiety and Lifetime Panic Disorder or Generalized Anxiety Disorder [NCT00167479]Phase 460 participants Interventional2003-09-30Completed
Risperidone Augmentation Therapy in Patients Who Have Failed or Only Partially Responded to an Adequate Trial of Antidepressant [NCT00174577]Phase 384 participants Interventional2003-02-28Active, not recruiting
Effects of Risperidone and Olanzapine on Weight Gain, Physical Health, and Outcome in a Community Sample of Severity and Persistently Ill Patients [NCT00179062]300 participants (Actual)Interventional2000-02-29Completed
A Randomized, Double Blind Study to Evaluate the Efficacy and Safety of Two Atypical Antipsychotics vs. Placebo in Patients With an Acute Exacerbation of Either Schizophrenia or Schizoaffective Disorder [NCT00061802]Phase 4225 participants (Actual)Interventional2003-06-30Completed
Preventing Relapse: Oral Antipsychotics Compared To Injectables: Evaluating Efficacy (PROACTIVE) [NCT00330863]Phase 4357 participants (Actual)Interventional2006-05-31Completed
Preventing Morbidity in First Episode Schizophrenia, Part II [NCT00320671]Phase 4198 participants (Actual)Interventional2005-12-31Completed
A Double-Blind, Placebo-Controlled Study of the Effects of Risperdal Consta on Brain Reward Circuitry, Craving and Cocaine Use in Active Cocaine Dependence [NCT00385801]Phase 231 participants (Actual)Interventional2005-09-30Completed
Pharmacogenomics in Autism Treatment [NCT00584701]Phase 2/Phase 349 participants (Actual)Interventional2008-01-31Completed
Clozapine Vs. Risperidone for People With First Episode Schizophrenia and Co-Occurring Substance Use Disorder [NCT00573287]14 participants (Actual)Interventional2006-06-30Completed
An Open-Label Randomized Trial Comparing Risperdal Consta With Oral Antipsychotic Care in the Treatment of Early Psychosis [NCT00246259]Phase 477 participants (Actual)Interventional2004-10-31Completed
Clozapine for Cannabis Use Disorder in Schizophrenia [NCT01639872]Phase 449 participants (Actual)Interventional2013-05-01Completed
Open-Label Study in Stable Schizophrenia Patients to Evaluate the Safety, Tolerability, and Pharmacokinetics of Switching From Oral Risperidone to Risperidone Implant (DLP-114) [NCT04418466]Phase 1/Phase 228 participants (Actual)Interventional2021-04-01Completed
A Multiple Dose Study to Assess the Safety, Tolerability and Pharmacokinetics of Risperidone Extended Release Capsules in Subjects With Schizophrenia, Schizoaffective Disorder [NCT04567524]Phase 234 participants (Actual)Interventional2020-08-13Completed
Neuroleptic Induced Movement Disorders in Older Patients [NCT00255879]Phase 1250 participants Interventional1999-01-31Completed
A Randomized Control Trial Comparing Quetiapine to Risperidone in Bipolar Disorder Outpatients With Current Stimulant Dependence [NCT00227123]96 participants (Actual)Interventional2002-10-31Completed
A Six-month, Double-blind, Randomized, International, Multicenter Trial to Evaluate the Glucoregulatory Effects of Risperidone and Olanzapine in Subjects With Schizophrenia or Schizoaffective Disorder [NCT00236379]Phase 459 participants (Actual)InterventionalCompleted
Randomized, Multi-center, Open Label Trial Comparing Risperidone Depot (Microspheres) and Olanzapine Tablets in Patients With Schizophrenia or Schizoaffective Disorder [NCT00236457]Phase 3629 participants (Actual)Interventional2000-11-30Completed
Risperidone in the Prevention of Relapse: a Randomized, Double-blind, Placebo-controlled Trial in Children and Adolescents With Conduct and Other Disruptive Behavior Disorders. [NCT00236444]Phase 3375 participants (Actual)Interventional2001-12-31Completed
Efficacy and Safety of Aripiprazole in the Treatment of Acutely Relapsed Patients With Schizophrenia or Schizoaffective Disorder With Risperidone as an Active Control [NCT00283179]Phase 383 participants (Actual)Interventional2004-03-31Completed
The SOURCE Study: Schizophrenia Outcomes-utilization, Relapse, and Clinical Evaluation: a Prospective 2-year Observational Study of Patients With Schizophrenia Who Initiate Treatment With Injectable Risperidone Long-acting Microspheres (RISPERDAL CONSTA) [NCT00246194]532 participants (Actual)Observational2004-09-30Completed
An Open-label Study Evaluating the Maintenance of Clinical Effect in Adults With Schizophrenia Switched From RISPERDAL® Tablets (Risperidone) to an Equivalent Dose of a Rapidly-dissolving Tablet Formulation of Risperdone [NCT00246272]Phase 382 participants (Actual)Interventional2004-10-31Completed
Risperidone in the Treatment of Chronic Schizophrenic Patients: an International Multicentre Double-blind Parallel-group Comparative Study Versus Haloperidol. [NCT00249119]Phase 31,579 participants (Actual)InterventionalCompleted
Risperidone in the Treatment of Behavioural and Psychological Signs and Symptoms in Dementia (BPSSD): a Multicentre, Double-blind, Placebo-controlled Parallel-group Trial [NCT00249158]Phase 3344 participants (Actual)Interventional1998-03-31Completed
The Efficacy And Safety Of Flexible Dosage Ranges Of Risperidone Versus Placebo In The Treatment Of Manic Or Mixed Episodes Associated With Bipolar I Disorder [NCT00249236]Phase 3291 participants (Actual)Interventional2001-03-31Completed
The Safety And Efficacy Of Risperdal� (Risperidone) Versus Placebo As Add-On Therapy To Mood Stabilizers In The Treatment Of The Manic Phase Of Bipolar Disorder [NCT00250367]Phase 3151 participants (Actual)Interventional1997-10-31Completed
Double-blind, Placebo-controlled Clinical Trial of JK6476 (Risperidone) in Patients With Hallucinations and Delusions Associated With Alzheimer's Disease [NCT00287742]Phase 333 participants (Actual)Interventional2002-03-31Terminated(stopped due to A decision was made to discontinue the study due to a change in the strategic direction of the company.)
Independent Investigator Grant Study-Comparative Effects of Chronic Treatment With Olanzapine and Risperidone on Glucose and Lipid Metabolism [NCT00287820]Phase 446 participants (Anticipated)Interventional2004-02-29Completed
Prospective Trial of Risperdal (Risperidone) Following Psychological Therapy for Challenging Behaviour in Learning Disabled Children [NCT00254930]Phase 319 participants (Actual)Interventional2003-09-30Completed
The Efficacy And Safety Of Flexible Dosage Ranges Of Risperidone Versus Placebo In The Treatment Of Manic Episodes Associated With Bipolar I Disorder. [NCT00257075]Phase 3267 participants (Actual)Interventional2000-12-31Completed
Risperidone Plus Mood Stabilizer in the Treatment of Mixed Mania [NCT00294255]Phase 445 participants (Actual)Interventional2003-03-31Completed
The Safety And Efficacy Of Risperidone Versus Placebo In Conduct Disorder and Other Disruptive Behavior Disorders In Mild, Moderate And Borderline Mentally Retarded Children Aged 5 To 12 Years [NCT00266552]Phase 3118 participants (Actual)InterventionalCompleted
Functional Brain Imaging and Employment in First-Episode Psychotic Patients Treated With Risperdal [NCT00314613]Phase 430 participants (Anticipated)Interventional2006-04-30Terminated
Electronic Schizophrenia Treatment Adherence Registry(e-STAR): An Observational, International Study to Evaluate Treatment Adherence in Schizophrenia With Long Acting Risperidone Microspheres [NCT00294008]230 participants (Actual)Observational2004-12-31Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled, 16 Week Study of Aripiprazole Used as Dual Therapy in the Treatment of Patients With Chronic Stable Schizophrenia or Schizoaffective Disorder Demonstrating an Inadequate Response to Quetiapine o [NCT00325689]Phase 4323 participants (Actual)Interventional2006-07-31Completed
Identification and Treatment of the Liability to Develop Schizophrenia [NCT00305474]Phase 4100 participants (Anticipated)Interventional2003-12-31Recruiting
Risperidone Alone Vs. Risperidone Plus Valproate in the Treatment of Patients With Schizophrenia and Hostility [NCT00308360]Phase 446 participants Interventional1999-09-30Completed
The Effects of Risperdal Consta on Health Care Utilization Costs in Chronically Ill Schizophrenic Patients [NCT00313391]Phase 40 participants Interventional2005-12-31Completed
Evaluation of the Effects of Psychological and Pharmacological Treatment of Psycho-stimulant and Cannabis-dependent Users in Kfar Izun in Israel [NCT01510015]100 participants (Anticipated)Interventional2012-01-31Not yet recruiting
A Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Crossover, Bioequivalence Study of Risperidone Tablet 1 mg With Risperdal® 1 mg in Normal, Healthy, Adult, Human Subjects Under Fed Condition [NCT01618760]Phase 148 participants (Actual)Interventional2012-05-31Completed
A Randomized, Double-Blind, Active-Controlled, Multicenter Study to Evaluate Efficacy and Safety Study of Iloperidone Virus Risperidone to Treat Schizophrenia [NCT01623713]Phase 2260 participants (Actual)Interventional2012-06-30Completed
A Double-blind, Placebo-controlled Study, Followed by an Open-label Extension Study Evaluating the Efficacy and Safety of Risperidone (R064766) in Children and Adolescents With Irritability Associated With Autistic Disorder [NCT01624675]Phase 339 participants (Actual)Interventional2012-09-30Completed
Evaluation of Efficacy and Safety of Risperidone in Long-acting Microspheres in Patients With Schizophrenia, Schizophreniform or Schizoaffective Disorders Diagnosed According to the DSM-IV Criteria, After Switching Treatment With Any Antipsychotic Therapy [NCT01855074]Phase 480 participants (Actual)Interventional2007-11-30Completed
[NCT03007303]30 participants (Anticipated)Observational [Patient Registry]2016-06-30Recruiting
Early Phase II Trials for Cocaine Medication Development [NCT00000317]Phase 231 participants (Actual)Interventional1996-08-31Completed
A Single-center, Randomized, Double-blind, Two-period Crossover Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of the Combination of Multiple Doses of RO5285119 With a Single Dose of Risperidone in Healthy Sub [NCT01708616]Phase 124 participants (Actual)Interventional2012-11-30Completed
A Longitudinal Comparison of Aripiprazole vs. Higher Metabolic Risk Antipsychotic Drugs on Adiposity Using MRI [NCT01739127]83 participants (Actual)Observational2012-11-30Completed
[NCT01742390]Phase 4120 participants (Anticipated)Interventional2013-02-28Recruiting
Randomized Multicentric Open-label Phase III Clinical Trial to Evaluate the Efficacy of Continual Treatment Versus Discontinuation Based in the Presence of Prodromes in a First Episode of Non-affective Psychosis. [NCT01765829]Phase 3104 participants (Anticipated)Interventional2012-11-30Recruiting
A Multiple-Center, Randomized, Double-Blind Study of Comparison of Risperidone and Aripiprazole for Treatment [NCT01813643]Phase 450 participants (Actual)Interventional2012-07-31Terminated(stopped due to Effects of aripiprazole was not obvious and showed adverse reaction obviously)
A Multiple-Center, Randomized, Double-Blind Study of Comparison of Paliperidone and Risperidone for Treatment of Patirnts With Methamphetamine-Associated Psychosis [NCT01822730]Phase 4120 participants (Actual)Interventional2013-02-28Completed
Atypical Antipsychotics Influence on the Safety of the Heart and Monitoring Indicators Model Building [NCT04446234]Phase 4350 participants (Anticipated)Interventional2021-05-31Not yet recruiting
A Randomized, Double-blinded, Double-dummy, Parallel-controlled and Multicenter Study to Investigate Blonanserin in Treatment of Schizophrenia When Compared With Risperidone [NCT01516424]Phase 3267 participants (Actual)Interventional2012-02-29Completed
Cost- Effectiveness and Quality of Life Assessment in Bipolar Disorder Depressive Episode [NCT02918097]Phase 478 participants (Actual)Interventional2010-05-31Completed
Correlation Between Cognitive Function and Relapse of Schizophrenia Regarding Dose Reduction in Patients Undergoing High-dose Antipsychotic Therapy [NCT03019887]139 participants (Actual)Interventional2011-04-30Completed
Reducing the Abuse Liability of Prescription Opioids in Recreational Drug Users: A Pilot Study [NCT03837860]Early Phase 13 participants (Actual)Interventional2019-04-01Terminated(stopped due to PI leaving institution)
A Randomized, Double-blind, Double-dummy, Parallel-group and Multicenter Study to Investigate Lurasidone in Treatment of Schizophrenia Compared With Risperidone [NCT02002832]Phase 3388 participants (Actual)Interventional2013-12-31Completed
Study in Stabilized Schizophrenic Patients to Evaluate the Pharmacokinetics of Risperidone and 9-Hydroxy (OH)-Risperidone When Risperidone is Administered From a Polyurethane Implant [NCT02658357]Phase 266 participants (Actual)Interventional2015-10-31Completed
A Randomized Open-Label, Rater Blinded Assessment of Optimal Treatment Change Strategy to Risperidone for Patients Intolerant of Olanzapine [NCT00378183]Phase 4120 participants (Actual)Interventional2001-02-28Completed
Risperidone Treatment in Dually-Diagnosed Individuals [NCT00000267]Phase 20 participants InterventionalCompleted
A Randomized, Double-Blind, Active-Controlled,Phase 2/3 Study to Determine the Short-Term (6-Week) and Long-Term (6 Month) Cognitive and Anti-Psychotic Efficacy, Safety and Tolerability of CYP-1020 Compared to Risperidone in Patients With Schizophrenia [NCT01363349]Phase 2/Phase 3269 participants (Actual)Interventional2011-05-31Terminated(stopped due to pre-planned interim analysis of the Phase II/III CLARITY trial of BL-1020 indicate that the trial would not meet the pre-specified primary efficacy endpoint.)
Infusion Laboratory: Protocol 3 (Risperidone) [NCT00000339]Phase 113 participants Interventional1996-06-30Active, not recruiting
Risk of Breakthrough Symptoms On Antipsychotic Maintenance Medication When Remitted Patients Are Treated With Long-Acting Injectable Medications [NCT05473741]180 participants (Anticipated)Observational2023-01-09Recruiting
Biomarkers of Conversion Risk and Treatment Response in Early-Stage Schizophrenia [NCT03323437]Phase 447 participants (Actual)Interventional2017-09-15Completed
Randomized Double Blind Comparison of Applied Behavioral Analysis Versus ABA and Risperidone [NCT00374764]60 participants Interventional2000-07-31Completed
A One Year, Open-label, Study to Evaluate the Safety and Tolerability of Risperidone Implants as a Maintenance Treatment in Patients With Schizophrenia [NCT02773576]Phase 3140 participants (Actual)Interventional2016-04-30Completed
Serotonin/Dopamine Antagonism of Cocaine Effect [NCT00000310]Phase 20 participants Interventional1996-01-31Terminated
Clozapine Treatment of Schizophrenic Patients [NCT00056498]Phase 465 participants (Actual)Interventional2001-12-31Completed
Efficacy of Interpersonal Psychotherapy in Treatment Resistant Depression [NCT01896349]74 participants (Anticipated)Interventional2013-04-30Recruiting
Treatment of Schizophrenia and Related Disorders in Children and Adolescents [NCT00053703]Phase 4116 participants (Actual)Interventional2002-02-28Completed
Detecting Which Patients With Schizophrenia Will Improve With Omega-3 Treatment [NCT01786239]50 participants (Actual)Interventional2013-05-31Completed
"Observational Study on the Effect of Switch to Lurasidone or Other Antipsychothics on Metabolic and Weight Changes in Subjects With Schizophrenia" [NCT04312503]95 participants (Actual)Observational2020-07-13Completed
An Open-label, Prospective, Randomized and Comparative Study of Patient Satisfaction Between Continued Administration of Previous Antipsychotics Versus Switched Administration to Paliperidone ER in Non-satisfied Patients With Previous Antipsychotic Drug [NCT01592201]Phase 413 participants (Actual)Interventional2012-07-31Terminated(stopped due to This study was early terminated due to insufficient enrollment required for hypothesis testing.)
Evaluation of Predictability of the Initial Response to a Low Dose of Risperidone on the Middle Term Efficiency in Anxious Subjects [NCT03227562]Phase 3120 participants (Actual)Interventional2017-09-01Terminated(stopped due to not enough patient)
Clinical and Cognitive Effects of Paliperidone Palmitate vs. Oral Risperidone in First-Episode Schizophrenia [NCT01451736]Phase 4146 participants (Actual)Interventional2011-10-31Completed
Controlled Trial of Risperidone and Divalproex Sodium With MRI Assessment of Affected Circuitry in Pre and Post Treatment in Pediatric Bipolar [NCT00176202]Phase 365 participants (Actual)Interventional2003-04-30Completed
Neurocognitive Effects of Ziprasidone: Relationship to Working Memory and Dopamine Blockade [NCT00225498]35 participants (Actual)Interventional2002-06-30Completed
Preventing Morbidity in First-Episode Schizophrenia [NCT00000374]Phase 4125 participants (Actual)Interventional1998-09-30Completed
A Sequential and Parallel Cohort Design to Test the Clinical Utility of Antipsychotic Medication Levels in Plasma as Determined by Liquid Chromatography-Tandem Mass Spectrometry [NCT02462473]Phase 29 participants (Actual)Interventional2015-05-31Terminated(stopped due to Due to poor enrollment sponsor terminated early after enrolling 9 in Cohort 1 and no enrollment in Cohorts 2 and 3.)
[NCT00004393]Phase 250 participants Interventional1997-07-31Completed
Clinical Observation of the Efficacy and Safety of Risperidone Long-Acting Injection (Risperdal Consta) in the Treatment of Schizophrenia in China [NCT01894984]640 participants (Actual)Observational2007-01-31Terminated(stopped due to The study was terminated because of high dropout rate.)
A Multi-Center, Randomized, Double-Blind Study, Comparing With Risperidone, to Evaluate the Efficacy and Safety of Aripiprazole in the Treatment of Patients With Schizophrenia [NCT00202007]Phase 2240 participants Interventional2005-02-28Completed
Investigation of the NMDA Receptor System in Man as a Potential Surrogate Marker for Deficit Syndrome in Schizophrenia: a [123]I-CNS 1261 Single Photon Emission Tomography (SPET) Study [NCT00364429]Phase 155 participants (Actual)Interventional2005-07-31Terminated(stopped due to terminated)
Developing a Single Patient Open-label Trial Tapering Algorithm for Antipsychotics in Long-Term Care - A Pilot Study [NCT02958800]20 participants (Anticipated)Interventional2016-12-31Recruiting
A Prospective Study of the Clinical Outcome Following Treatment Discontinuation After Remission in First-Episode Schizophrenia [NCT00378092]Phase 433 participants (Actual)Interventional2006-04-30Completed
Risperidone Long-Acting for Alcohol and Schizophrenia Treatment (R-LAST) [NCT00130923]Phase 495 participants (Actual)Interventional2005-09-30Completed
Developmental Processes in Schizophrenic Disorders: Cognitive Remediation, Medication Adherence, and Work Outcome in Recent-Onset Schizophrenia [NCT00333177]Phase 492 participants (Actual)Interventional2006-03-31Completed
A Single-Dose, Randomized, Open-Label, Two-Treatment, Two-Period, Two-Cohort, Crossover Study to Assess the Bioequivalence of Xian Risperdal Tablets Under Fasting and Fed Conditions in Chinese Healthy Subjects Compared With Gurabo Risperdal Tablets [NCT03220867]Phase 10 participants (Actual)Interventional2017-12-11Withdrawn(stopped due to CFDA announced Xi'An Risperdal as reference drug, no need for this BE trial from both scientific and ethical perspective.)
Study of add-on Ramelteon Therapy on Sleep and Circadian Rhythm Disruption in Patients With Schizophrenia [NCT03075657]Phase 4120 participants (Actual)Interventional2017-05-01Completed
Interventional, Randomised, Double-blind, Active-controlled, Fixed-dose Study of Lu AF35700 in Patients With Treatment-resistant Schizophrenia [NCT02717195]Phase 31,098 participants (Actual)Interventional2016-04-30Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Evaluate the Efficacy, Safety and Tolerability of RBP-7000 as a Treatment in Subjects With Acute Schizophrenia Over 8 Weeks (2 Subcutaneous Doses) [NCT02109562]Phase 3354 participants (Actual)Interventional2014-04-30Completed
Efficacy of Hydroxyzine Versus Treatment as Usual for Panic Disorder: An Eight-Week, Open Label, Pilot, Randomized Controlled Trial. [NCT05737511]Phase 480 participants (Anticipated)Interventional2023-12-30Not yet recruiting
A Phase 2A, Open-Label, Multiple Ascending Dose Study of the Safety, Tolerability, Pharmacokinetics, and Primary Pharmacodynamic Markers of Efficacy of 60mg, 90mg, and 120mg of Risperidone in RBP-7000 Subcutaneous Injections in Subjects With Clinically St [NCT01677377]Phase 245 participants (Actual)Interventional2012-08-31Completed
1/2-MC4R Genotype and Pediatric Antipsychotic Drug- Induced Weight Gain [NCT01844700]Phase 414 participants (Actual)Interventional2013-07-31Terminated(stopped due to very slow recruitment, no sufficient results)
Risperidone Treatment In Children With Autism Spectrum Disorder And High Levels of Repetitive Behavior [NCT01171937]Phase 241 participants (Actual)Interventional2008-09-30Completed
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
Open Flexible-dose Randomized Study of the Effectiveness of Second Generation Antipsychotics in First Episode Psychosis Patients: A 3-year Follow-up [NCT03090503]Phase 4200 participants (Anticipated)Interventional2014-06-30Enrolling by invitation
Long-Term Safety, Tolerability, and Effectiveness of Lurasidone in Subjects With Schizophrenia or Schizoaffective Disorder: A Randomized, Active Comparator-Controlled Trial [NCT00641745]Phase 3629 participants (Actual)Interventional2008-03-31Completed
Alcoholism and Schizophrenia: A Translational Approach to Treatment [NCT01411085]Phase 212 participants (Actual)Interventional2011-12-31Completed
An Open-Label Study of Oral Antipsychotics Replacement by Prolonged Release Risperidone (Risperdal Consta) in Schizophrenic Subjects With Bad Adhesion to the Treatment [NCT01726335]Phase 453 participants (Actual)Interventional2006-01-31Completed
Acute D2 Receptor Blockade Induced Neuronal Network Changes in Human Volunteers [NCT01931059]11 participants (Actual)Interventional2013-07-31Completed
Multicenter, Open-label, Two-arm, Parallel-design, Repeat-dose Clinical Trial to Evaluate the PK, Safety, and Tolerability of Four Intramuscular Injections of Risperidone ISM® 75 mg, at 28 Day Intervals in Patients With Schizophrenia [NCT02086786]Phase 270 participants (Actual)Interventional2014-03-31Completed
A Multi Dose, Open-Label, Parallel-Group Study to Evaluate the PK and Safety/Tolerability of Long-Acting Oral Risperidone (LYN-005) in Participants With Schizophrenia or Schizoaffective Disorder [NCT05779241]Phase 390 participants (Anticipated)Interventional2023-04-30Recruiting
Striatal Connectivity and Clinical Outcome in Psychosis [NCT02822092]170 participants (Anticipated)Observational2016-07-31Recruiting
Actigraphic Analysis of Treatment Response in a Six Year Old Girl With Kabuki Syndrome [NCT00723580]1 participants (Actual)Interventional2008-05-31Completed
Locus Coeruleus Neuroimaging of Antipsychotic/Modafinil Interactions on Cognition in Schizophrenia [NCT01913327]Phase 44 participants (Actual)Interventional2013-04-30Terminated(stopped due to Insufficient Funds and Inadequate Subject Recruitment)
Safety and Pharmacokinetics of Antipsychotics in Children 2: Studying TDM in an RCT [NCT05146245]Phase 4140 participants (Anticipated)Interventional2021-12-01Recruiting
Effects of Risperdal Consta Versus Oral Antipsychotic Medication on Clinical and Functional Outcome and Neurocognition in First-episode Schizophrenia [NCT00330551]Phase 4126 participants (Actual)Interventional2006-03-31Completed
Metabolic Signatures and Biomarkers in First Episode and Recurrent Patients With Schizophrenia in Comparison to Healthy Controls [NCT00466310]Phase 171 participants (Actual)Interventional2007-02-28Completed
Clinical Management of Metabolic Problems in Patients With Schizophrenia [NCT00423878]Phase 4215 participants (Actual)Interventional2007-01-31Completed
Improving Metabolic Parameters of Antipsychotic Child Treatment (IMPACT) [NCT00806234]Phase 4127 participants (Actual)Interventional2009-01-31Completed
Effects of Modulation of the Dopaminergic System Using Risperidone on Memory and Executive Processes in Individuals With 22q11.2 Deletion Syndrome [NCT04639960]16 participants (Actual)Interventional2017-09-29Terminated(stopped due to Difficulties in recruitment of participants and end of funding)
A Research in Pharmacogenomics and Accurate Medication of Risperidone [NCT03302364]800 participants (Anticipated)Observational [Patient Registry]2017-10-22Recruiting
Pragmatic Trial Comparing Weight Gain in Children With Autism Taking Risperidone Versus Aripiprazole [NCT04903353]Phase 4350 participants (Anticipated)Interventional2022-02-01Recruiting
A Phase II, Multi-Center, Randomized, Double-Blind, Parallel Group, Placebo-Controlled Trial of the Efficacy and the Safety of RO6889450 (Ralmitaront) vs Placebo in Patients With an Acute Exacerbation of Schizophrenia or Schizoaffective Disorder [NCT04512066]Phase 2287 participants (Actual)Interventional2020-09-08Completed
Placebo Controlled Trial of Valproate Versus Risperidone in Young Children With Bipolar Disorder [NCT02456454]Phase 346 participants (Actual)Interventional2006-01-31Completed
A Randomized, Open-Label, Study To Evaluate The Effect of Oral Paliperidone Extended-Release and Oral Risperidone Immediate-Release on Selected Cognitive Domains in Clinically Stable Subjects With Schizophrenia [NCT01670071]Phase 417 participants (Actual)Interventional2013-01-31Terminated(stopped due to The study was terminated due to insufficient sample size and protocol compliance issue.)
Clinical Psychopharmacology Division Institute of Mental Health, Peking University [NCT03148509]Phase 4300 participants (Anticipated)Interventional2017-06-01Not yet recruiting
Estimating the Optimal Dynamic Antipsychotic Treatment Regime: Sequential Multiple-assignment Randomized Clinical Antipsychotic Trials in Chinese Patients With First-episode Psychosis. [NCT03510325]Phase 41,260 participants (Anticipated)Interventional2018-10-01Not yet recruiting
Comparable Efficacy of Transcranial Direct Current Stimulation and Pharmacological Treatments in Children With Autism Spectrum Disorder [NCT05491720]Phase 145 participants (Actual)Interventional2020-08-15Completed
A 4-week, Double-blind, Placebo-controlled Study of the Efficacy and Safety of Mifepristone in the Prevention of Risperidone-induced Weight Gain in Healthy Male Volunteers [NCT00698022]Phase 176 participants (Actual)Interventional2008-11-30Completed
Long-Term Extension Study of MP-214 in Patients With Schizophrenia [NCT01626872]Phase 2/Phase 3254 participants (Actual)Interventional2012-09-30Completed
A Double-Blind, Placebo-Controlled Study of MP-214 in Patients With Schizophrenia [NCT01625000]Phase 2/Phase 3512 participants (Actual)Interventional2012-05-31Completed
A Long-term Study of MP-214 in Patients With Chronic Phase or Elderly Schizophrenia [NCT01625897]Phase 2/Phase 3125 participants (Actual)Interventional2012-05-31Completed
Double-blind,Double-simulation,Risperidone-controlled,Multicentre Clinical Trial of Iloperidone in Patients With Schizophrenia [NCT02453893]Phase 3288 participants (Anticipated)Interventional2013-11-30Recruiting
Treatment of Early Age Mania (TEAM) Study [NCT00057681]Phase 3379 participants (Actual)Interventional2003-02-28Completed
Effectiveness of Switching Antipsychotic Medications [NCT00044655]Phase 4219 participants (Actual)Interventional2001-07-31Completed
An Open-Label, Long-Term Safety and Tolerability Study of RBP-7000 in the Treatment of Subjects With Schizophrenia [NCT02203838]Phase 3500 participants (Actual)Interventional2014-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00044655 (1) [back to overview]Number Who Discontinued Medication Within First 6 Study Months
NCT00053703 (6) [back to overview]Change From Baseline in PANSS Positive Symptom Subscale Score at 8 Weeks.
NCT00053703 (6) [back to overview]Change From Baseline in PANSS Negative Symptom Subscale at Week 8
NCT00053703 (6) [back to overview]Change From Baseline in Body Mass Index Change, kg/m2, at Week 8
NCT00053703 (6) [back to overview]Change From Baseline in Barnes Akathisia Scale at Week 8
NCT00053703 (6) [back to overview]Change From Baseline in Weight at Week 8
NCT00053703 (6) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at 8 Weeks
NCT00056498 (3) [back to overview]Neuropsychological Testing - Overall Composite Z-score
NCT00056498 (3) [back to overview]Positive Symptom Item Scores by Week and Treatment Group
NCT00056498 (3) [back to overview]Negative Symptom Total Score by Week and Treatment Group
NCT00057681 (3) [back to overview]Modified Side Effects Form for Children and Adolescents
NCT00057681 (3) [back to overview]K-SADS Mania Rating Scale
NCT00057681 (3) [back to overview]Clinical Global Impressions-Bipolar Mania Improvement
NCT00099983 (1) [back to overview]Change in CAPS Score From Baseline to Week 24
NCT00130923 (6) [back to overview]Change Over Time in Frequency of Heavy Drinking Days (Used to Evaluate Treatment Efficacy)
NCT00130923 (6) [back to overview]Average Over Time of Positive and Negative Symptoms (Used to Evaluate Treatment Efficacy)
NCT00130923 (6) [back to overview]Average Over Time of Severity of Illness and Global Improvement (Used to Evaluate Treatment Efficacy)
NCT00130923 (6) [back to overview]Number of Participants With Medication Adherence
NCT00130923 (6) [back to overview]Average Over Time of Frequency of Drinking Days (Used to Evaluate Treatment Efficacy)
NCT00130923 (6) [back to overview]Average Over Time of Global Functioning (Used to Evaluate Treatment Efficacy)
NCT00132314 (2) [back to overview]Hazard Ratio for Hospitalization
NCT00132314 (2) [back to overview]Hospitalization-free Survival - Time to Event
NCT00132678 (3) [back to overview]Change in Montgomery-Åsberg Depression Rating Scale (MADRS)
NCT00132678 (3) [back to overview]Change in Young Mania Rating Scale (YMRS) Scores.
NCT00132678 (3) [back to overview]Number of Participants Who Had a Mood Relapse.
NCT00140426 (13) [back to overview]Time to Reach 90% Ideal Body Weight (IBW) and Maintain for 1 Month, Stratified by >=80% at Start of Study
NCT00140426 (13) [back to overview]Time to Reach 90% IBW and Maintain for 1 Month, Stratified by IBW <80% at Start of Study
NCT00140426 (13) [back to overview]Hazard Ratio for Time to Reaching Ease Of Eating Level 3 From Start of Study (Normal Eating Behavior)
NCT00140426 (13) [back to overview]Color A Person Test (CAPT)
NCT00140426 (13) [back to overview]Change in Ratings of Anxiety Symptoms on the Multidimensional Anxiety Scale for Children (MASC)
NCT00140426 (13) [back to overview]Change in Prolactin Levels
NCT00140426 (13) [back to overview]Change in Leptin Levels
NCT00140426 (13) [back to overview]Change in Eating Disorder Inventory-2 Drive for Thinness Subscale (DT)
NCT00140426 (13) [back to overview]Change in Eating Disorder Inventory (EDI)-2 Score for Body Dissatisfaction (BD)
NCT00140426 (13) [back to overview]Body Image Software (BIS) - Point of Subjective Equality (PSE)
NCT00140426 (13) [back to overview]Body Image Software (BIS): Average Desired Thinness
NCT00140426 (13) [back to overview]Body Image Software (BIS): Average Distortion
NCT00140426 (13) [back to overview]Body Image Software (BIS) - Difference Limen (DL)
NCT00176202 (4) [back to overview]Child Depression Rating Scale- Revised (CDRS-R)
NCT00176202 (4) [back to overview]Child Mania Rating Scale (CMRS)
NCT00176202 (4) [back to overview]Clinical Global Improvement in Bipolar Disorder Overall (CGI-BP Overall)
NCT00176202 (4) [back to overview]Young Mania Rating Scale (YMRS)
NCT00177164 (4) [back to overview]Number of Participants With Treatment Emergent Hyperlipidemia
NCT00177164 (4) [back to overview]Number of Participants With Treatment - Emergent Hyperglycemia
NCT00177164 (4) [back to overview]BMI
NCT00177164 (4) [back to overview]Evaluate the Number of Clinical Events (Pooled) Occurring Between 3-15 Months Following a Switch/Stabilization of the Antipsychotic Agents Among Patients Who Receive Either Risperidal Consta or One of the 4 Marketed 2nd Generation Antipsychotic Agents.
NCT00183625 (2) [back to overview]Total Weeks Worked
NCT00183625 (2) [back to overview]Body Mass Index
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Abnormal Involuntary Movement Scale Scores.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Body Mass Index (BMI)
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Brief Psychiatric Rating Scale Scores.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Clinical Global Impression - Severity of Illness Scale Scores.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Subcutaneous Fat Area.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Visceral Fat Area.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Waist Circumference.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Weight.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Ratio of Visceral Fat Area to the Subcutaneous Fat Area.
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Barnes Akathisia Rating Scale (BARS) Scores
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Body Mass Index
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Brief Psychiatric Rating Scale (BPRS) Scores
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Clinical Global Impression - Severity of Illness Scores
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Eating Behavior Assessment Scale Scores
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Direct Low Density Lipoprotein (LDL)
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including High Density Lipoprotein (HDL)
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Lipoprotein Subclasses
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Total Cholesterol
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Triglycerides
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Simpson Angus Scale Scores
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Subcutaneous Fat Area
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in the Ratio of the Visceral Fat Area to the Subcutaneous Fat Area
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Visceral Fat Area
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Waist Circumference
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Weight
NCT00190749 (30) [back to overview]Change in Baseline to Last Observation In Normalized Insulin Sensitivity Index at Low Insulin Phase Using Change in Weight as a Covariate
NCT00190749 (30) [back to overview]Pairwise Correlations Between Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Eating Behavior Assessment Scale Scores.
NCT00190749 (30) [back to overview]Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in the Simpson Angus Scale Scores.
NCT00190749 (30) [back to overview]Pairwise Correlation Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Barnes Akathisia Scale Scores.
NCT00190749 (30) [back to overview]Change From Baseline to 12 Week Endpoint in Abnormal Involuntary Movement Scale Scores
NCT00205699 (6) [back to overview]Change in MRI-measured Subcutaneous Abdominal Fat
NCT00205699 (6) [back to overview]Change in Insulin-stimulated Glucose Rate of Disappearance (Glucose Rd)
NCT00205699 (6) [back to overview]Change in Insulin-stimulated Glucose Rate of Appearance (Glucose Ra)
NCT00205699 (6) [back to overview]Change in DEXA % Body Fat
NCT00205699 (6) [back to overview]Change in Insulin-stimulated Glycerol Rate of Appearance (Glycerol Ra)
NCT00205699 (6) [back to overview]Change in MRI-measured Visceral Abdominal Fat
NCT00206102 (15) [back to overview]Change in the PANSS Psychopathology Subscale Score
NCT00206102 (15) [back to overview]Change in the Positive and Negative Syndrome Scale (PANSS) Total Score
NCT00206102 (15) [back to overview]Number of Participants With Potential Extrapyramidal Symptoms (EPS)
NCT00206102 (15) [back to overview]Number of Relapses of Schizophrenia or Schizoaffective Disorder
NCT00206102 (15) [back to overview]Presence of a Cortical (C) Type of Cataractogenic Potential Events in Participants as Assessed and Agreed by 2 Independent, Treatment-masked Ophthalmologists Using the Lens Opacities Classification System II (LOCS II ) Grading Scale
NCT00206102 (15) [back to overview]Change in Personal Evaluation of Transitions in Treatment (PETiT) Total Score
NCT00206102 (15) [back to overview]Presence of a Nuclear Opalescence (N) Type of Cataractogenic Potential Events in Participants as Assessed and Agreed by 2 Independent, Treatment-masked Ophthalmologists Using the LOCS II Grading Scale
NCT00206102 (15) [back to overview]Presence of a Posterior Subcapsular (P) Type Cataractogenic Potential Events in Participants as Assessed and Agreed by 2 Independent, Treatment-masked Ophthalmologists Using the LOCS II Grading Scale
NCT00206102 (15) [back to overview]Change in the Clinical Global Impression - Severity of Illness (CGI-S) Score
NCT00206102 (15) [back to overview]Change in Simpson-Angus Scale (SAS) Total Score
NCT00206102 (15) [back to overview]Change in the PANSS Negative Subscale Score
NCT00206102 (15) [back to overview]Change in the PANSS Positive Subscale Score
NCT00206102 (15) [back to overview]Change in Barnes Akathisia Rating Scale (BARS) Global Score
NCT00206102 (15) [back to overview]Change in Abnormal Involuntary Movement Scale (AIMS) Total Score
NCT00206102 (15) [back to overview]Change in Health-related Quality of Life as Measured by Quality of Life Enjoyment and Satisfaction Questionnaire - Short Form (Q-LES-Q SF) Total Score
NCT00216476 (5) [back to overview]Change From Baseline to Endpoint in Total Positive and Negative Syndrome Scale (PANSS) Score
NCT00216476 (5) [back to overview]Mean Relapse Free Period (Exploratory/Aripiprazole)
NCT00216476 (5) [back to overview]Mean Relapse Free Period(Risperidone LAI Versus Quetiapine)
NCT00216476 (5) [back to overview]Change From Baseline to Endpoint in Short-Form Health Survey 12 (SF-12) Scores
NCT00216476 (5) [back to overview]Change From Baseline to Endpoint in Clinical Global Impression Scale (CGI) Score
NCT00216671 (6) [back to overview]Change From Baseline in PANSS Total Score at Week 12
NCT00216671 (6) [back to overview]Change From Baseline in PANSS Total Score at Week 6
NCT00216671 (6) [back to overview]Change in Positive And Negative Syndrome Scale (PANSS) Total Score From Baseline to Endpoint
NCT00216671 (6) [back to overview]Change From Baseline to Endpoint in Global Assessment of Functioning (GAF)
NCT00216671 (6) [back to overview]Change From Baseline to Endpoint in Quality of Life Questionnaire SF-12
NCT00216671 (6) [back to overview]Change From Baseline to Endpoint in Clinical Global Impression - Severity (CGI-S)
NCT00221403 (1) [back to overview]YMRS
NCT00225498 (1) [back to overview]Working Memory
NCT00246259 (15) [back to overview]Abnormal Involuntary Movement Scale (AIMS)
NCT00246259 (15) [back to overview]Time to Relapse
NCT00246259 (15) [back to overview]Percentage of Participants With Relapse
NCT00246259 (15) [back to overview]Change From Baseline in Standardized Mental Component Scale Score in Short Form 36 (SF-36) at Week 104 or LRV
NCT00246259 (15) [back to overview]Change From Baseline in Drug Attitude Inventory (DAI-10) Score at Week 104 or LRV
NCT00246259 (15) [back to overview]Number of Participants With Cognitive Assessment Using Trail A
NCT00246259 (15) [back to overview]Total Words Score Over Time
NCT00246259 (15) [back to overview]Simpson Angus Scale (SAS)
NCT00246259 (15) [back to overview]Number of Participants With Cognitive Assessments Using Trail B
NCT00246259 (15) [back to overview]Change From Baseline in Young Mania Rating Scale (YMRS) at Week 104 or LRV
NCT00246259 (15) [back to overview]Change From Baseline in Social and Occupational Functioning Assessment Scale (SOFAS) at Week 104 or LRV
NCT00246259 (15) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 104 or Last Reported Visit (LRV)
NCT00246259 (15) [back to overview]Change From Baseline in Calgary Depression Symptom Scale (CDSS) Score at Week 104 or LRV
NCT00246259 (15) [back to overview]Change From Baseline Hamilton Anxiety Scale (HAM-A) Total Score at Week 104 or LRV
NCT00246259 (15) [back to overview]Barnes Akathisia Rating Scale (BARS) Global Clinical Assessment
NCT00256997 (9) [back to overview]Percentage of Participants Who Experienced a Clinical Exacerbation From Month 3 Post-Randomization
NCT00256997 (9) [back to overview]Time to First Clinical Exacerbation
NCT00256997 (9) [back to overview]Change From Baseline in Assessment of Quality of Life (AQoL) Score at Month 24
NCT00256997 (9) [back to overview]Change From Baseline in Personal and Social Performance Scale (PSP) Total Score at Month 24
NCT00256997 (9) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Total Score at Month 24
NCT00256997 (9) [back to overview]Number of Participants With Clinical Global Impression of Change (CGI-C)
NCT00256997 (9) [back to overview]Number of Participants With Clinical Global Impression of Severity (CGI-S)
NCT00256997 (9) [back to overview]Number of Participants With Response to Resource Utilization Questionnaire (RUQ)
NCT00256997 (9) [back to overview]Percentage of Participants Who Experienced a Clinical Exacerbation
NCT00269919 (14) [back to overview]Change From Baseline in Drug Attitude Inventory-10 (DAI-10) Item Scale Score at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in Global Assessment of Functioning (GAF) Score at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in NCFT: Controlled Oral Word Association Test at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in NCFT: Memory Quotient (MQ) at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in Clinical Global Impression-Severity (CGI-S) Score at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in World Health Organization (WHO)-Quality of Life (QOL) at Week 96
NCT00269919 (14) [back to overview]Total Drug Induced Extra-Pyramidal Symptoms Scale (DIEPSS) Score
NCT00269919 (14) [back to overview]Change From Baseline in NCFT: Trail Making Test (TMT)-Time at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in NCFT: TMT-Error at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in Neurocognitive Function Test (NCFT): General Intelligence (Korean-Wechsler Adults Intelligence Scale [K-WAIS]) at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in Total Positive and Negative Syndrome Scale (PANSS) Score at Week 96
NCT00269919 (14) [back to overview]Liverpool University Neuroleptic Side Effect Rating Scale (LUNSERS) Score
NCT00269919 (14) [back to overview]Change From Baseline in NCFT: Rey Kim Memory Test- Korean-Rey Complex Figure Test (K-RCFT) at Week 96
NCT00269919 (14) [back to overview]Change From Baseline in NCFT: Rey Kim Memory Test-Korean Auditory Verbal Learning Test (KAVLT) at Week 96
NCT00299702 (2) [back to overview]Time in Remission
NCT00299702 (2) [back to overview]Time to Relapse
NCT00320671 (1) [back to overview]Percentage of Participants That Responded to Treatment
NCT00330551 (8) [back to overview]Medication Adherence
NCT00330551 (8) [back to overview]Number of Participants Who Had an Exacerbation or Relapse of Psychotic Symptoms
NCT00330551 (8) [back to overview]Number of Participants Who Returned to Work or School (SAS Work Section)
NCT00330551 (8) [back to overview]Retention in Treatment
NCT00330551 (8) [back to overview]Number of Weeks Maintaining Work or School (SAS)
NCT00330551 (8) [back to overview]Awareness of Illness, as Assessed by the Scale to Assess Unawareness of Mental Disorder-Revised (SUMD-R)
NCT00330551 (8) [back to overview]Change in Global Functioning Scale: Role
NCT00330551 (8) [back to overview]MATRICS Consensus Cognitive Battery (MCCB) Overall Composite T Score
NCT00330863 (3) [back to overview]Number of Patients Discontinuing From the Study
NCT00330863 (3) [back to overview]Side Effects and Metabolic Measures
NCT00330863 (3) [back to overview]Substantial Clinical Deterioration Measured by Psychotic Symptoms
NCT00333177 (10) [back to overview]Work Behavior Inventory (WBI) Quality of Work/School Performance
NCT00333177 (10) [back to overview]Work/School Functioning (Global Functioning Scale: Role)
NCT00333177 (10) [back to overview]Work/School Functioning (Global Functioning Scale: Role)
NCT00333177 (10) [back to overview]Retention in Treatment
NCT00333177 (10) [back to overview]Maintenance of Work/School Attendance
NCT00333177 (10) [back to overview]Exacerbation or Relapse of Psychotic Symptoms
NCT00333177 (10) [back to overview]Change in Motivation for Work/School
NCT00333177 (10) [back to overview]Awareness of Illness, as Assessed by the Scale to Assess Unawareness of Mental Disorder, Revised Version (SUMD-R)
NCT00333177 (10) [back to overview]Average Medication Non-adherence
NCT00333177 (10) [back to overview]Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Consensus Cognitive Battery (MCCB)
NCT00337662 (18) [back to overview]Mean Change From Baseline to 10 Week Endpoint in Extrapyramidal Symptoms as Measured by the Abnormal Involuntary Movement Scale (AIMS)- Non-Global Total Score
NCT00337662 (18) [back to overview]Mean Change From Baseline to 10 Week Endpoint in Extrapyramidal Symptoms as Measured by the Barnes Akathisia Rating Scale - Total Score
NCT00337662 (18) [back to overview]Mean Change From Baseline to 10 Week Endpoint in Extrapyramidal Symptoms as Measured by the Modified Simpson-Angus Scale
NCT00337662 (18) [back to overview]Changes From Study Period II Baseline (Week 0) to Weeks 3, 4, 6, 8, and 12 in Positive and Negative Syndrome Scale (PANSS) Total Score in Early Onset Response and Not Early Onset Response-Risperidone Patients
NCT00337662 (18) [back to overview]Changes From Study Period III Baseline (Week 2) to Weeks 3, 4, 6, 8, and 12 in Positive and Negative Syndrome Scale Total Score in Not Early Onset Response-Risperidone and Not Early Onset Response-Olanzapine Patients
NCT00337662 (18) [back to overview]Number of Participants in the Not Early Onset-Risperidone and Not Early Onset-Olanzapine Groups Who Show a 50% or Greater Reduction in Positive and Negative Syndrome Scale Total Score From Baseline or Meet 'a Priori' Specified Criteria for Remission
NCT00337662 (18) [back to overview]Number of Participants With Psychiatric Hospitalizations in the Early Onset and Not Early Onset-Risperidone Groups
NCT00337662 (18) [back to overview]Number of Participants With Treatment-Emergent Abnormal Fasting Laboratory Analytes Reported in >=2% of All Participants
NCT00337662 (18) [back to overview]The Number of Participants in the Early Onset (EO) and Not Early Onset-Risperidone (NEO-RIS) Groups Who Show a 20% or Greater Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score
NCT00337662 (18) [back to overview]Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Body Mass Index
NCT00337662 (18) [back to overview]Vital Signs - Change From Baseline to 10 Week Endpoint in Standing Mean Arterial Pressure
NCT00337662 (18) [back to overview]Vital Signs - Change From Baseline to 10 Week Endpoint in Standing Diastolic Blood Pressure
NCT00337662 (18) [back to overview]The Number of Participants in the Not Early Onset-Risperidone (NEO-RIS) and Not Early Onset-Olanzapine (NEO-OLZ) Groups Who Show a 20% or Greater Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score
NCT00337662 (18) [back to overview]Number of Participants in the Early Onset and Not Early Onset-Risperidone Groups Who Show a 50% or Greater Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Baseline or Meet 'a Priori' Specified Criteria for Remission
NCT00337662 (18) [back to overview]Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Body Weight
NCT00337662 (18) [back to overview]Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Standing Systolic Blood Pressure
NCT00337662 (18) [back to overview]Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Standing Pulse Rate
NCT00337662 (18) [back to overview]Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Sitting Pulse Rate
NCT00338949 (2) [back to overview]Change in Visceral Fat Mass From Baseline to Week 26
NCT00338949 (2) [back to overview]Change in Insulin Sensitivity Index From Baseline to Week 26 ((1/mU/L) x 1/Min)
NCT00385801 (2) [back to overview]Cocaine Craving
NCT00385801 (2) [back to overview]Cocaine Use by Quantitative Urine Samples
NCT00389493 (5) [back to overview]Score on the Yale-Brown Obsessive Compulsive Scale (Y-BOCS)
NCT00389493 (5) [back to overview]Quality of Life Enjoyment and Satisfaction Questionnaire-Short Form
NCT00389493 (5) [back to overview]Social Adjustment Scale-SR
NCT00389493 (5) [back to overview]Brown Assessment of Beliefs (BABS)
NCT00389493 (5) [back to overview]Hamilton Depression Rating Scale (Ham-D)
NCT00391222 (7) [back to overview]Time to Early Study Discontinuation for Any Reason
NCT00391222 (7) [back to overview]Change From Double-blind Baseline to Endpoint in Young Mania Rating Scale (YMRS)
NCT00391222 (7) [back to overview]Change From Double-blind Baseline to Endpoint in Montgomery Åsberg Depression Rating Scale (MADRS)
NCT00391222 (7) [back to overview]Time to Recurrence of an Elevated Mood (Hypomanic, Manic, or Mixed) Episode
NCT00391222 (7) [back to overview]Time to Recurrence of a Mood Episode (Risperidone LAI Versus Placebo)
NCT00391222 (7) [back to overview]Time to Recurrence of a Mood Episode (Exploratory/Olanzapine)
NCT00391222 (7) [back to overview]Time to Recurrence of a Depressive Episode
NCT00417482 (8) [back to overview]AIMS
NCT00417482 (8) [back to overview]Mini Mental State Exam (MMSE)
NCT00417482 (8) [back to overview]Weight
NCT00417482 (8) [back to overview]Treatment Emergent Symptoms Scale (TESS)
NCT00417482 (8) [back to overview]Relapse by Study Week 48
NCT00417482 (8) [back to overview]Relapse by Study Week 32
NCT00417482 (8) [back to overview]Physical Self-Maintenance Scale (PSMS)
NCT00417482 (8) [back to overview]Extrapyramidal Signs (EPS)
NCT00423878 (2) [back to overview]Efficacy Failure, Defined as Psychiatric Hospitalization, a 25 Percent Increase From Baseline on the Positive and Negative Syndrome Scale or Substantial Clinical Deterioration on the Clinical Global Impressions-Change (CGI-C)
NCT00423878 (2) [back to overview]Change in Non-HDL Cholesterol Level for Patients Assigned to Stay and Patients Assigned to Switch Over 24 Weeks
NCT00435370 (1) [back to overview]Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Cognition Domains
NCT00466310 (1) [back to overview]Total Plasmalogen Levels in the Lipid Profile
NCT00508157 (2) [back to overview]Number of Participants Remaining on Metabolic Syndrome at Week 16
NCT00508157 (2) [back to overview]Mean Percent Change From Baseline in Fasting Non-high Density Lipoprotein (HDL) Cholesterol at Week 16
NCT00509067 (3) [back to overview]Negative Symptoms Measured on Positive and Negative Syndrome Scale (PANSS)
NCT00509067 (3) [back to overview]MATRICS Verbal Learning and Memory
NCT00509067 (3) [back to overview]Clinical Global Impression
NCT00515723 (2) [back to overview]Clamp Derived Insulin Sensitivity (mg/kg/Min)
NCT00515723 (2) [back to overview]DEXA Total Fat
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to the Week 6 Endpoint.
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to Week 2 (Observed).
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to Week 4 (Observed).
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to Week 6 (Observed).
NCT00535132 (15) [back to overview]Modified COVI Anxiety Scale (m-COVI) Change From Baseline to the Week 6 Endpoint
NCT00535132 (15) [back to overview]Pittsburgh Sleep Quality Index (PSQI) Change From Baseline to the Week 6 Endpoint
NCT00535132 (15) [back to overview]Positive and Negative Syndrome Scale (PANSS) Total Score Change From Baseline to Week 6 Endpoint
NCT00535132 (15) [back to overview]Short Form-36 Health Survey (SF-36) Mental Health Composite Score Change From Baseline to the Week 6 Endpoint
NCT00535132 (15) [back to overview]Short Form-36 Health Survey (SF-36) Physical Health Composite Score Change From Baseline to the Week 6 Endpoint
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 2 (Observed).
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 4 (Observed).
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 6 (Observed).
NCT00535132 (15) [back to overview]Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 6 LOCF.
NCT00535132 (15) [back to overview]Treatment Satisfaction Questionnaire for Medication (TSQM) Global Satisfaction Score Change From Baseline to the Week 6 Endpoint
NCT00535132 (15) [back to overview]Clinical Global Impression - Severity (CGI-S) Change From Baseline to Week 6 Endpoint
NCT00563706 (2) [back to overview]Positive and Negative Symptom Scale (PANSS) Total Score at Baseline
NCT00563706 (2) [back to overview]Change From Baseline in Positive and Negative Symptom Scale (PANSS) Total Score at Day 28
NCT00571688 (1) [back to overview]Number of Relapse-related Events Normalized to Unit Time
NCT00573287 (2) [back to overview]Number of Participants Demonstrating Improvement in Psychiatric Symptoms Using the BPRS, CGIS, and SANS at 24 Weeks
NCT00573287 (2) [back to overview]Number of Participants Demonstrating Improvement in Substance Use
NCT00576732 (8) [back to overview]Change in Clinical Global Impression Severity (CGI-S)
NCT00576732 (8) [back to overview]Change in Aberrant Behavior Checklist Irritability (ABC-I) Subscale
NCT00576732 (8) [back to overview]Change in Insulin Resistance (IR) at 6 Weeks
NCT00576732 (8) [back to overview]Change in Fasting Glucose (mg/dL) at 6 Weeks
NCT00576732 (8) [back to overview]Change in Fasting Glucose (mg/dL) at 6 Months
NCT00576732 (8) [back to overview]Change in Insulin Resistance (IR) at 6 Months
NCT00576732 (8) [back to overview]Number of Participants Who Had at Least 25% Improvement in ABC-I
NCT00576732 (8) [back to overview]Number of Participants Who Had Clinical Global Impression Change Ratings of Much or Very Much Improved.
NCT00584701 (2) [back to overview]Exon Expression Positively or Negatively Correlated With Percentage Improvement in ABC-I
NCT00584701 (2) [back to overview]Percent Change of ABC - Irritability Subscale Score
NCT00589914 (3) [back to overview]The Change From Baseline in the PSP Score
NCT00589914 (3) [back to overview]Change in the Positive and Negative Syndrome Scale (PANSS) Total Score for Schizophrenia
NCT00589914 (3) [back to overview]The Change From Baseline for the CGI-S Score
NCT00600756 (31) [back to overview]The Remission Rate in Both the Quetiapine XR Group and the Risperidone Group at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR vs Risperidone by Evaluating the Number of Participants at Month 12 in Safety Population With Individual Symptoms Assessed by the Modified Udvalg for Kliniske Undersogelser, Side Effect Rating Scale: Neurologic
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Time Between First Study Drug Intake and First Hospitalization for Patients With 1 Hospitalization in the ITT Population
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants With a Treatment-emergent Adverse Event (TEAEs) at Month 12 in the Safety Population
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Mean Number of Lost School/Work Days at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone by Evaluating the Relapse Rate at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population on Core Schizophrenic and Depressive Symptoms by Evaluating the Change From Baseline in the Calgary Depression Scale for Schizophrenia (CDSS) Total Score
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population on Core Schizophrenic and Depressive Symptoms by Evaluating the Change From Baseline in CGI-SCH Overall Severity Score (Improved).
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants Who Had at Least 1 Extra-pyramidal TEAE at Month 12 in the Safety Population
NCT00600756 (31) [back to overview]Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Mental Functioning at Month 12 in the ITT Population.
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population on Core Schizophrenic and Depressive Symptoms by Evaluating the Change From Baseline in CGI-SCH Overall Severity Score
NCT00600756 (31) [back to overview]The Compliance of Patients Taking Quetiapine XR Versus Risperidone at Month 12 by Evaluating the Number of Participants Who Returned Study Drug at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]Responder Rate at Month 6 in the Per Protocol Population Using the Subjective Well-being Under Neuroleptics Scale, Short Version (SWN-K) Total Score
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Participants With at Least 1 Hospitalization Due to Psychiatric Disorders at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]Number of Participants Using Antidepressants at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]Evaluation of Effect of Quetiapine XR Versus Risperidone on the Health-related Quality of Life of Patients With Schizophrenia by Evaluating the Change From Baseline in EQ-5D(Euro Quality of Life-5 Dimension) Index Score at Month 12 in the ITT Population.
NCT00600756 (31) [back to overview]Change From Baseline in Mean Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Total Score at Month 12 in the Per Protocol Population
NCT00600756 (31) [back to overview]To Evaluate the Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population Regarding Health Economics Outcomes by Evaluating the Functional Improvement Rate of the Modified Vocational Status Index/ Location Code Index: Stable State
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants Who Discontinued the Study Because of an TEAE at Month 12 in the Safety Population
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants at Month 12 in the Safety Population With Individual Symptoms Assessed by the Modified UKU: Sexual Dysfunction in Men
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants Who Had at Least 1 Cardiac TEAE at Month 12 in the Safety Population
NCT00600756 (31) [back to overview]Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Social Integration at Month 12 in the ITT Population.
NCT00600756 (31) [back to overview]Change From Baseline in Mean Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Total Score at Month 12 in the Intent-to-Treat (ITT) Population
NCT00600756 (31) [back to overview]Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Self-control at Month 12 in the ITT Population.
NCT00600756 (31) [back to overview]Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Physical Functioning at Month 12 in the ITT Population.
NCT00600756 (31) [back to overview]The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Number of Participants Using Other Psychotropic Medications at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Emotional Regulation at Month 12 in the ITT Population.
NCT00600756 (31) [back to overview]Number of Subjects Who Had an Unscheduled Visits Due to Worsening of Schizophrenia, Dose Change, or Adverse Event at Month 12 in the ITT Population
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants at Month 12 in the Safety Population With Individual Symptoms Assessed by the Modified UKU: Hyperprolactinaemia in Women
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Extra-pyramidal Events at Month 12 in the Safety Population
NCT00600756 (31) [back to overview]The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Mean Change From Baseline to Month 12 in Prolactin Levels in the Safety Population
NCT00604279 (5) [back to overview]Percentage of Participants Who Responded to PANSS Total Score at Day 92 or Early Withdrawal
NCT00604279 (5) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Day 92 or Early Withdrawal
NCT00604279 (5) [back to overview]Change From Baseline in Personal and Social Performance (PSP) Score at Day 92 or Early Withdrawal
NCT00604279 (5) [back to overview]Change From Baseline in Clinical Global Impression-Severity (CGI-S) Score at Day 92 or Early Withdrawal
NCT00604279 (5) [back to overview]Change From Baseline in the Sleep Visual Analog Scale (VAS) Score at Day 92 or Early Withdrawal
NCT00640562 (11) [back to overview]Change From Baseline to Week 12 of HAM-D Score
NCT00640562 (11) [back to overview]Change From Baseline to Week 12 of Drug Attitude Inventory 10 Item Scale (DAI 10) Score
NCT00640562 (11) [back to overview]Change From Baseline to Week 12 of Calgary Depression Scale for Schizophrenia (CDSS) Score.
NCT00640562 (11) [back to overview]Concomitant Use of Antidepressive Drugs From Baseline to Week 12
NCT00640562 (11) [back to overview]Change From Baseline in the Simpson Angus Scale (SAS) Total Score to Week 12 as an Indication of Neurological Side Effects Section
NCT00640562 (11) [back to overview]Concomitant Use of Antidepressive Drugs From Baseline to Week 12
NCT00640562 (11) [back to overview]Change From Screening Visit to Week 12 of Prolactin Live
NCT00640562 (11) [back to overview]CGI- Global Improvement Mean Score at Week 12
NCT00640562 (11) [back to overview]Body Mass Index (BMI) at Week 12
NCT00640562 (11) [back to overview]- Change From Baseline to Week 12 of Clinical Global Impression (CGI- Severity of Illness) Score
NCT00640562 (11) [back to overview]Change From Baseline to Week 12 of PANSS Score
NCT00641745 (1) [back to overview]Number of Participants With Adverse Events.
NCT00694707 (2) [back to overview]Change From Baseline to Week 6 in the PANSS Total Score
NCT00694707 (2) [back to overview]Change From Baseline to Week 6 in the CGI-S Score
NCT00698022 (4) [back to overview]Change From Baseline in Body Weight
NCT00698022 (4) [back to overview]Percentage of Participants With One or More Adverse Events
NCT00698022 (4) [back to overview]Percentage of Participants With <5% and <7% Increase From Baseline in Body Weight
NCT00698022 (4) [back to overview]Percentage of Participants Discontinued From the Study Due to an Adverse Event
NCT00711269 (7) [back to overview]Proportion of Participants With TEAEs Leading to Discontinuation
NCT00711269 (7) [back to overview]Change From Baseline in the PANSS Negative Subscales at Week 6
NCT00711269 (7) [back to overview]Change From Baseline in the PANSS General Psychopathology Subscales at Week 6 (LOCF)
NCT00711269 (7) [back to overview]Proportion of Participants With Treatment-emergent Serious Adverse Events (SAEs)
NCT00711269 (7) [back to overview]Change From Baseline in the PANSS Positive Subscales at Week 6 (LOCF)
NCT00711269 (7) [back to overview]Change From Baseline in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 6 (LOCF)
NCT00711269 (7) [back to overview]Proportion of Participants With Treatment-emergent Adverse Events (TEAEs)
NCT00712270 (1) [back to overview]QTc Measurement
NCT00723580 (1) [back to overview]Actigraphic Measurement of Treatment Conditions
NCT00746252 (1) [back to overview]Weight Gain
NCT00796302 (4) [back to overview]NCBRF-TIQ D-Total Score
NCT00796302 (4) [back to overview]Clinical Global Impressions Scale for Severity of Illness
NCT00796302 (4) [back to overview]Antisocial Behavior Scale - Reactive Aggression Subscale
NCT00796302 (4) [back to overview]Clinical Global Impressions Scale for Improvement
NCT00806234 (4) [back to overview]Body Mass Index (BMI) Z-score Change
NCT00806234 (4) [back to overview]Change in Low Density Lipoprotein (LDL) Cholesterol Level
NCT00806234 (4) [back to overview]Change in Whole Body Insulin Sensitivity Index
NCT00806234 (4) [back to overview]Triglyceride Levels
NCT00845026 (26) [back to overview]Change From Baseline in Pulse Rate at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Number of Participants With Potentially Clinically Significant Changes in QT Intervals Electrocardiograms (ECGs)
NCT00845026 (26) [back to overview]Percentage of Participants With Remission (Rate of Remission) at Week 24 Endpoint
NCT00845026 (26) [back to overview]Percentage of Participants With Response (Rate of Response) at 6 and 24 Weeks Endpoints
NCT00845026 (26) [back to overview]Number of Participants With Treatment-Emergent Change in Neurological Examination
NCT00845026 (26) [back to overview]Time to Discontinuation Due to Adverse Event (AE)
NCT00845026 (26) [back to overview]Number of Participants With Suicidal Behaviors and Ideations Baseline Through 52 Weeks
NCT00845026 (26) [back to overview]Number of Participants With Shift From Baseline to Maximum Post-Baseline Grading in Electroencephalograms (EEGs)
NCT00845026 (26) [back to overview]Change From Baseline in Measurement and Treatment Research to Improve Cognition in Schizophrenia Consensus Cognitive Battery (MCCB): Overall Composite T-Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in EuroQoL Questionnaire-5 Dimension (EQ-5D) at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Blood Pressure (BP) at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Clinical Global Impression Severity Scale (CGI-S) at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Number of Participants With Potentially Clinical Significant Change in Lipids Level
NCT00845026 (26) [back to overview]Change From Baseline in Barnes Akathisia Scale (BAS) Global Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in 16-Item Negative Symptoms Assessment (NSA-16) Total Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Weight at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in University of California-San Diego (UCSD) Performance-Based Skills Assessment-B (UPSA-B) Total Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Subjective Well-Being Under Neuroleptic Treatment-Short Form (SWN-S) Total Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Simpson-Angus Scale (SAS) Total Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Personal and Social Performance (PSP) at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Number of Psychiatric Visits at 24 Weeks Endpoint
NCT00845026 (26) [back to overview]Number of Participants With Potentially Clinical Significant Change in Fasting Glucose Level
NCT00845026 (26) [back to overview]Change From Baseline in Montgomery-Asberg Depression Rating Scale (MADRS) Total Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Change From Baseline in Abnormal Involuntary Movement Scale (AIMS) Total Score at 52 Weeks Endpoint
NCT00845026 (26) [back to overview]Percentage of Participants With Relapse (Rate of Relapse)
NCT00856583 (12) [back to overview]Number of Participants With Hospitalisations, Excluding Hospitalisations Related to the Primary Psychiatric Disease
NCT00856583 (12) [back to overview]Cause-specific Mortality: Number of Participants With Completed Suicides - MedDRA
NCT00856583 (12) [back to overview]Cause-specific Mortality: Number of Participants With Completed Suicides - ISC
NCT00856583 (12) [back to overview]Cause-specific Mortality: Number of Participants With Cardiac Deaths - ISC
NCT00856583 (12) [back to overview]Cause-specific Mortality: Number of Participants With Cardiac Deaths - MedDRA
NCT00856583 (12) [back to overview]Number of Participants With Suicide Attempts (Fatal and Non-fatal) - MedDRA
NCT00856583 (12) [back to overview]Number of Participants With All-cause Mortality
NCT00856583 (12) [back to overview]Second Primary Outcome: Number of Participants With Cardiac Events, Including Arrhythmias, Requiring Hospitalisation
NCT00856583 (12) [back to overview]Number of Participants With Suicide Attempts (Fatal and Non-fatal) - ISC
NCT00856583 (12) [back to overview]Number of Participants With Discontinuation of Treatment for Any Reason Other Than Study Closure
NCT00856583 (12) [back to overview]Cause-specific Mortality: Number of Participants With Other Than Cardiac Deaths and Completed Suicides - MedDRA
NCT00856583 (12) [back to overview]Cause-specific Mortality: Number of Participants With Other Than Cardiac Deaths and Completed Suicides - ISC
NCT00857818 (3) [back to overview]Number of Participants With Death, Serious Adverse Events (SAEs), Adverse Events (AEs) Leading to Discontinuation, and 1 or More AEs
NCT00857818 (3) [back to overview]Mean Percent Change From Baseline in Fasting Non-high Density Lipoprotein (Non-HDL) Cholesterol Levels
NCT00857818 (3) [back to overview]Mean Baseline Fasting Non-HDL Levels
NCT00934635 (1) [back to overview]Percentage of Paliperidone or Risperidone Dopamine D2 Receptor Occupancies
NCT00992407 (22) [back to overview]Change From Baseline in Abnormal Involuntary Movement Scale (AIMS) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Barnes Akathisia Rating Scale (BARS) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Clinical Global Impression-Severity Scale (CGI-S) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Continuous Performance Task (CPT) Based on Neurocognitive Function Test (NCFT) at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Personal and Social Performance (PSP) Scale Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Number of Outpatient Clinic Visits at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Trail Making Test Based on Neurocognitive Function Test (NCFT) at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Total Outpatients and Inpatients Hours at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Theory of Mind (TOM) Scale Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Social Functioning Scale (SFS) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Simpson and Angus Rating Scale (SAS) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Verbal Working Memory (VWM) Response Based on Neurocognitive Function Test (NCFT) at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Travelling Fee for Outpatients, Hospitalization Travelling Fee and Salary Paid a Participant Before Being Ill at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Global Assessment of Functioning (GAF) Test Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Working Memory Based on Neurocognitive Function Test (NCFT) at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Scale to Assess Unawareness of Mental Disorder (SUMD) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Psychosocial Well-being Index (PWI) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Members for Outpatients, Members Visiting Inpatients, Affected Members and Visiting Inpatients at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Emotional & Social Functioning Scale (SFS) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Drug Attitude Inventory-10 (DAI-10) Score at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Days of Hospitalization, Number of Days Affected by Participants and Family, at Week 52
NCT00992407 (22) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Score at Week 52
NCT01050582 (3) [back to overview]Height (cm) Z-score at Study Visit
NCT01050582 (3) [back to overview]Number of Participants With Retrospectively Reported Potentially Prolactin-Related Adverse Events
NCT01050582 (3) [back to overview]Age (Years) at Current Tanner Stage
NCT01157351 (6) [back to overview]Time to First Treatment Failure
NCT01157351 (6) [back to overview]Percentage of Participants in Each Event Category of First Treatment Failure
NCT01157351 (6) [back to overview]Change From Baseline in Clinical Global Impression - Severity (CGI-S) Score During Overall Treatment Duration
NCT01157351 (6) [back to overview]Change From Baseline in Personal and Social Performance (PSP) Total Score During Overall Treatment Duration
NCT01157351 (6) [back to overview]Time to First Psychiatric Hospitalization
NCT01157351 (6) [back to overview]Time to First Psychiatric Hospitalization or Arrest/Incarceration
NCT01175135 (19) [back to overview]Number of Participants With Response to Columbia-Suicide Severity Rating Scale (C-SSRS)
NCT01175135 (19) [back to overview]Number of Participants With Clinically Significant Findings in Vital Signs and Electrocardiogram (ECG)
NCT01175135 (19) [back to overview]Number of Participants With Clinically Significant Laboratory Test Abnormalities for Fasting Insulin, High Density Lipoprotein (HDL), Low Density Lipoprotein (LDL), Cholesterol, Triglycerides, Hemoglobin Type A1c (HbA1c) and Prolactin
NCT01175135 (19) [back to overview]Number of Participants With Laboratory Test Abnormalities
NCT01175135 (19) [back to overview]Proportion of Participants With Dystonia Adverse Events
NCT01175135 (19) [back to overview]Change From Baseline in Abdominal Girth at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Body Weight at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Global Assessment of Functioning (GAF) Score at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Clinical Global Impression - Severity (CGI-S) Score at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Extrapyramidal Symptom Rating Scale-Abbreviated (ESRS-A) Parameter Scores at Week 4
NCT01175135 (19) [back to overview]Number of Participants With Abnormal White Blood Cell (WBC) Count and Absolute Neutrophil Count (ANC)
NCT01175135 (19) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Positive, Negative, and General Subscales Score at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Marder Factors Score at Week 4
NCT01175135 (19) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Derived Brief Psychiatric Rating Scale (BPRS) Core Score at Week 4
NCT01175135 (19) [back to overview]Treatment Satisfaction Questionnaire for Medication (TSQM) Score
NCT01175135 (19) [back to overview]Number of Participants With Clinically Significant Changes in Physical Examinations
NCT01175135 (19) [back to overview]Clinical Global Impression - Improvement (CGI-I) Score
NCT01175135 (19) [back to overview]Change From Baseline in Movement Disorder Burden Score for Dystonia (MDBS-D) at Week 4
NCT01284959 (7) [back to overview]Assessment of Adverse Events by Objective Rating Scales and Self Report Scales
NCT01284959 (7) [back to overview]Assessment of Adverse Events by Objective Rating Scales and Self Report Scales
NCT01284959 (7) [back to overview]Assessment of Cognitive Functioning-1
NCT01284959 (7) [back to overview]Assessment of Cognitive Functioning-2
NCT01284959 (7) [back to overview]Assessment of Cognitive Functioning-3
NCT01284959 (7) [back to overview]Assessment of Negative Symptoms and Neuroleptic Induced Deficit Syndromes by Objective Rating Scales
NCT01284959 (7) [back to overview]Symptoms Assessment by Objective Rating Scales
NCT01333072 (1) [back to overview]Changes in the Irritability Subscale of the Larger ABC (Abberent Behavior Checklist) That Occur From Baseline to 10 Weeks
NCT01363349 (1) [back to overview]Cognition
NCT01411085 (1) [back to overview]Timeline Followback Assessing Number of Drinks Per Week
NCT01516424 (1) [back to overview]Change From Baseline in PANSS(Positive and Negative Syndrome Scale) Total Score at Week 8
NCT01625000 (2) [back to overview]Change in the Clinical Global Impression-Severity (CGI-S) Score at Week 6
NCT01625000 (2) [back to overview]Change in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 6
NCT01625897 (1) [back to overview]Number of Participants With Adverse Events as a Measure of Safety and Tolerability
NCT01626872 (1) [back to overview]Number of Participants With Adverse Events as a Measure of Safety and Tolerability
NCT01639872 (2) [back to overview]Average Over Time of Frequency of Cannabis Use
NCT01639872 (2) [back to overview]Average Over Time of Intensity of Cannabis Use (Used to Evaluate Treatment Efficacy)
NCT01677377 (64) [back to overview]Total Risperidone PK: Percent Fluctuation Over the Secondary Peak
NCT01677377 (64) [back to overview]Total Risperidone PK: Percent Fluctuation Over the PK Profile
NCT01677377 (64) [back to overview]Total Risperidone PK: Minimum Plasma Concentration (Cmin) Over the Secondary Peak
NCT01677377 (64) [back to overview]Total Risperidone PK: Minimum Plasma Concentration (Cmin) Over the PK Profile
NCT01677377 (64) [back to overview]Total Risperidone PK: Maximum Plasma Concentration Over the Secondary Peak (Cmax)
NCT01677377 (64) [back to overview]Risperidone PK: Maximum Plasma Concentration (Cmax) During Initial Peak
NCT01677377 (64) [back to overview]Total Risperidone PK: Average Plasma Concentration Over the Secondary Peak (Cavg, Day 2-29)
NCT01677377 (64) [back to overview]Total Risperidone PK: Average Plasma Concentration (Cavg) Over the PK Profile
NCT01677377 (64) [back to overview]Total Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to Time Tau (Where Tau=28 Days) (AUCtau)
NCT01677377 (64) [back to overview]Total Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24)
NCT01677377 (64) [back to overview]Total Risperidone PK: Area Under the Plasma Concentration-Time Curve From Day 2-29 Post Injection (AUC Day 2-29)
NCT01677377 (64) [back to overview]Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the Secondary Peak
NCT01677377 (64) [back to overview]Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the PK Profile
NCT01677377 (64) [back to overview]Risperidone PK: Time of Maximum Plasma Concentration (Tmax) During Initial Peak
NCT01677377 (64) [back to overview]Risperidone PK: Swing Over the Secondary Peak
NCT01677377 (64) [back to overview]Risperidone PK: Swing Over the PK Profile
NCT01677377 (64) [back to overview]Risperidone PK: Percent Fluctuation Over the Secondary Peak
NCT01677377 (64) [back to overview]Risperidone PK: Percent Fluctuation Over the PK Profile
NCT01677377 (64) [back to overview]Risperidone PK: Minimum Plasma Concentration (Cmin) Over the Secondary Peak
NCT01677377 (64) [back to overview]Risperidone PK: Minimum Plasma Concentration (Cmin) Over the PK Profile
NCT01677377 (64) [back to overview]Risperidone PK: Maximum Plasma Concentration Over the Secondary Peak (Cmax)
NCT01677377 (64) [back to overview]Risperidone PK: Maximum Plasma Concentration (Cmax) Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Average Plasma Concentration (Cavg) Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to Time Tau (Where Tau=28 Days) (AUCtau)
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24)
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Area Under the Plasma Concentration-Time Curve From Day 2-29 Post Injection (AUC Day 2-29)
NCT01677377 (64) [back to overview]Total Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Maximum Plasma Concentrations (Rac(Cmax))
NCT01677377 (64) [back to overview]Total Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Area Under the Plasma Concentration Curve (Rac(AUC))
NCT01677377 (64) [back to overview]Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Maximum Plasma Concentrations (Rac(Cmax))
NCT01677377 (64) [back to overview]Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Area Under the Plasma Concentration Curve (Rac(AUC))
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Maximum Plasma Concentrations (Rac(Cmax))
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Maximum Plasma Concentration (Cmax) During Initial Peak
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Maximum Plasma Concentration (Cmax) Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Maximum Plasma Concentration Over the Secondary Peak (Cmax)
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Minimum Plasma Concentration (Cmin) Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Minimum Plasma Concentration (Cmin) Over the Secondary Peak
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Percent Fluctuation Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Percent Fluctuation Over the Secondary Peak
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Swing Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Average Plasma Concentration Over the Secondary Peak (Cavg, Day 2-29)
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Swing Over the Secondary Peak
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Area Under the Plasma Concentration Curve (Rac(AUC))
NCT01677377 (64) [back to overview]Total Risperidone PK: Maximum Plasma Concentration (Cmax) During Initial Peak
NCT01677377 (64) [back to overview]Summary of Participants With Treatment-Emergent Adverse Events (TEAE)
NCT01677377 (64) [back to overview]Total Risperidone PK: Maximum Plasma Concentration (Cmax) Over the PK Profile
NCT01677377 (64) [back to overview]Total Simpson-Angus Scale (SAS) Score at Baseline and Days 28, 56, 84 and 106
NCT01677377 (64) [back to overview]Total Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the Secondary Peak
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Time of Maximum Plasma Concentration (Tmax) During Initial Peak
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the PK Profile
NCT01677377 (64) [back to overview]9-hydroxyrisperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the Secondary Peak
NCT01677377 (64) [back to overview]Clinical Global Impression (CGI) Scores (Severity of Illness and Global Improvement) at Baseline and Days 28, 56, 84 and 106
NCT01677377 (64) [back to overview]Global Assessment of the Abnormal Involuntary Movement Scale (AIMS) for Tardive Dyskinesia at Baseline and Days 28, 56, 84 and 106
NCT01677377 (64) [back to overview]Global Clinical Assessment of Akathisia Using the Barnes Akathisia Scale (BAS) at Baseline and Days 28, 56, 84 and 106
NCT01677377 (64) [back to overview]Participants With Suicidal Ideation or Behavior as Identified Using the Columbia-Suicide Severity Rating Scale (C-SSRS) Score at Baseline and Days 28, 56, 84 and 106
NCT01677377 (64) [back to overview]Positive and Negative Syndrome Scale (PANSS) Scores at Baseline and Days 28, 56, 84 and 106
NCT01677377 (64) [back to overview]Risperidone PK: Area Under the Plasma Concentration-Time Curve From Day 2-29 Post Injection (AUC Day 2-29)
NCT01677377 (64) [back to overview]Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24)
NCT01677377 (64) [back to overview]Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to Time Tau (Where Tau=28 Days) (AUCtau)
NCT01677377 (64) [back to overview]Risperidone PK: Average Plasma Concentration (Cavg) Over the PK Profile
NCT01677377 (64) [back to overview]Total Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the PK Profile
NCT01677377 (64) [back to overview]Total Risperidone PK: Time of Maximum Plasma Concentration (Tmax) During Initial Peak
NCT01677377 (64) [back to overview]Total Risperidone PK: Swing Over the Secondary Peak
NCT01677377 (64) [back to overview]Total Risperidone PK: Swing Over the PK Profile
NCT01677377 (64) [back to overview]Risperidone PK: Average Plasma Concentration Over the Secondary Peak (Cavg, Day 2-29)
NCT01726335 (13) [back to overview]Clinical Global Impressions (CGI) - Disease Severity Score
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 4
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 50
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 8
NCT01726335 (13) [back to overview]Drug Attitude Inventory (DAI-10)
NCT01726335 (13) [back to overview]Extrapyramidal Symptoms Rating Scale (ESRS) Total Score
NCT01726335 (13) [back to overview]Global Assessment of Functioning (GAF) Scale Score
NCT01726335 (13) [back to overview]Personal and Social Performance (PSP) Scale Score
NCT01726335 (13) [back to overview]Short Form-36 (SF-36) - Quality of Life
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 24
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 2
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 38
NCT01726335 (13) [back to overview]Positive and Negative Syndromes Scale (PANSS) Total Score at Week 16
NCT01786239 (1) [back to overview]Treatment Response
NCT01844700 (4) [back to overview]BMI Z-scores
NCT01844700 (4) [back to overview]Percent Weight Change Compared to Baseline Weight
NCT01844700 (4) [back to overview]Weight Change
NCT01844700 (4) [back to overview]BMI Percentile
NCT01855074 (6) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 26
NCT01855074 (6) [back to overview]Global Assessment of Functioning (GAF) Score
NCT01855074 (6) [back to overview]Extrapyramidal Symptom Rating Scale (ESRS) Score
NCT01855074 (6) [back to overview]Clinical Global Impressions (CGI) - Disease Severity Score
NCT01855074 (6) [back to overview]Patient Satisfaction With Treatment
NCT01855074 (6) [back to overview]Short Form-36 (SF-36) - Quality of Life Score
NCT01894984 (6) [back to overview]Total Personal and Social Performance (PSP) Score
NCT01894984 (6) [back to overview]Number of Participants With Reasons for Discontinuation From Study Treatment
NCT01894984 (6) [back to overview]Percentage of Participants With Relapse at Week 24
NCT01894984 (6) [back to overview]Percentage of Participants Attaining Remission Criteria
NCT01894984 (6) [back to overview]Clinical Global Impressions-Severity (CGI-S) Score
NCT01894984 (6) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 24
NCT01931059 (3) [back to overview]Feedback-based Probabilistic Classification Task
NCT01931059 (3) [back to overview]Repeatable Battery for the Assessment of Neuropsychological Status
NCT01931059 (3) [back to overview]Simpson-Angus Extrapyramidal Side Effects Scale
NCT02002832 (2) [back to overview]Mean Change From Baseline to Week 6 in Positive and Negative Syndrome Scale (PANSS) Total Scores.
NCT02002832 (2) [back to overview]Mean Clinical Global Impression Scale-Improvement (CGI-I) Score at Week 6.
NCT02086786 (10) [back to overview]Area Under the Curve Extrapolated to Infinity (AUC∞) for Active Moiety
NCT02086786 (10) [back to overview]Area Under the Curve to the Last Quantified Concentration (AUClast) for Active Moiety
NCT02086786 (10) [back to overview]PTF for Active Moiety
NCT02086786 (10) [back to overview]Accumulation Ratio (RA) for Active Moiety
NCT02086786 (10) [back to overview]Trough Plasma Concentration (Cmin) for Active Moiety
NCT02086786 (10) [back to overview]Positive and Negative Syndrome Scale (PANSS) Total Score
NCT02086786 (10) [back to overview]Time to Peak Concentration (Tmax) for Active Moiety
NCT02086786 (10) [back to overview]Peak Plasma Concentration (Cmax) for Active Moiety
NCT02086786 (10) [back to overview]AUCτ for Active Moiety
NCT02086786 (10) [back to overview]Terminal Half-life (t1/2) for Active Moiety
NCT02109562 (3) [back to overview]Mixed Model for Repeated Measures (MMRM) Analysis of Change From Baseline to End of Treatment in the Positive and Negative Syndrome Scale (PANSS) Total Score
NCT02109562 (3) [back to overview]Mixed Model for Repeated Measures (MMRM) Analysis of Change From Baseline to End of Treatment in Clinical Global Impression - Severity Scale (CGI-S)
NCT02109562 (3) [back to overview]Summary of Participants With Treatment-Emergent Adverse Events (TEAE)
NCT02203838 (6) [back to overview]Participants With Treatment-Emergent Adverse Events (TEAE)
NCT02203838 (6) [back to overview]Change From Baseline in Clinical Global Impression - Severity Scores (CGI-S) to Days 29, 169 and End of Study
NCT02203838 (6) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Subscale Scores to End of Study
NCT02203838 (6) [back to overview]Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score to Days 29, 169 and End of Study
NCT02203838 (6) [back to overview]Participants With Injection Site-Related Treatment-Emergent Adverse Events (TEAEs)
NCT02203838 (6) [back to overview]Participants With Markedly Abnormal Weight Gain Anytime During the Study as Compared to Baseline
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Visual Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Verbal Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Speed of Processing Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Social Cognition Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Reasoning and Problem Solving: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Total Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Attention/Vigilance Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Adjusted Intracortical Myelin (ICM) Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)
NCT02431702 (31) [back to overview]Part 3 (EDP): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by CRDPSS
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by Clinician-Rated Dimensions of Psychosis Symptom Severity Scale (CRDPSS)
NCT02431702 (31) [back to overview]Part-2 (Disease Progression): Time to First Treatment Failure
NCT02431702 (31) [back to overview]Part 3 (Extended Disease Progression [EDP]): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Time to First Treatment Failure
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Working Memory Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Visual Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Verbal Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Speed of Processing Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Social Cognition Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Reasoning and Problem Solving: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Attention/Vigilance Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Personal and Social Performance (PSP) Total Observed Score
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (SE MRI)
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Working Memory Score: MCCB Domain
NCT02462473 (8) [back to overview]Number of Participants With Medication Treatment Modifications (MTM)
NCT02462473 (8) [back to overview]Adherence to Antipsychotic Medication as Assessed by Brief Adherence Rating Scale (BARS) at Week 0 and 12
NCT02462473 (8) [back to overview]Clinician's Rating Scale of Adherence (CRS) Score at Week 0 and 12
NCT02462473 (8) [back to overview]Clinical Global Impression-Severity (CGI-S) Score at Week 0 and 12
NCT02462473 (8) [back to overview]Dimensions of Psychosis Symptom Severity Scale (DPSS) Total Score at Week 0 and 12
NCT02462473 (8) [back to overview]Antipsychotic Medication Plasma Levels (AMPL) During the Active Assessment Phase at Week 12
NCT02462473 (8) [back to overview]Number of Participants With Factors Considered in Clinical Decision as Assessed by Clinical Assessment of the Schizophrenia Patient (CASP)
NCT02462473 (8) [back to overview]Patient Satisfaction Survey (PSS) Total Score at Week 0 and 12
NCT02717195 (8) [back to overview]Response at Week 10, Defined as ≥50% Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Randomization
NCT02717195 (8) [back to overview]Change From Randomization to Week 10 in Positive and Negative Syndrome Scale (PANSS) Total Score
NCT02717195 (8) [back to overview]Response at Week 10, Defined as ≥40% Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Randomization
NCT02717195 (8) [back to overview]Response at Week 10, Defined as ≥30% Reduction in PANSS Total Score From Randomization
NCT02717195 (8) [back to overview]Response at Week 10, Defined as ≥20% Reduction in PANSS Total Score, PANSS (Positive and Negative Syndrome Scale) Total Score ≤70, CGI-S (Clinical Global Impression Scale - Severity of Illness) Score <4
NCT02717195 (8) [back to overview]Change From Randomization to Week 10 in PSP Total Personal and Social Performance (PSP) Total Score
NCT02717195 (8) [back to overview]Change From Randomization to Week 10 in Global Clinical Impression - Severity of Illness (CGI-S) Score
NCT02717195 (8) [back to overview]Response at Week 10, Defined as ≥20% Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Randomization
NCT02875340 (8) [back to overview]Overall Survival
NCT02875340 (8) [back to overview]Peak Plasma Concentration (Cmax)
NCT02875340 (8) [back to overview]Plasma VAL401 Half-life (t 1/2)
NCT02875340 (8) [back to overview]Progression-free Survival (PFS)
NCT02875340 (8) [back to overview]Trough Plasma Concentration (Cmin)
NCT02875340 (8) [back to overview]Number of Patients With Disease Control
NCT02875340 (8) [back to overview]Number of Participants Reporting Adverse Events and Serious Adverse Events
NCT02875340 (8) [back to overview]Patient Quality of Life During VAL401 Treatment
NCT02918097 (3) [back to overview]"Number of Participants With Response to Treatment"
NCT02918097 (3) [back to overview]Number of Participants With Remission to Treatment
NCT02918097 (3) [back to overview]Quality of Life Instrument Scores
NCT03019887 (1) [back to overview]Number of Participants With Relapse
NCT03055338 (4) [back to overview]Least Squares Mean (LSM) Change From Baseline in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 4
NCT03055338 (4) [back to overview]Percentage of Participants Experiencing an Adverse Event (AE)
NCT03055338 (4) [back to overview]Percentage of Participants Discontinuing Study Treatment Due to an Adverse Event
NCT03055338 (4) [back to overview]Least Squares Mean (LSM) Change From Baseline in the Clinical Global Impression-Severity of Illness (CGI-S) Score at Week 4
NCT03160521 (11) [back to overview]PSP Total Score From Baseline at Each Post-baseline Assessment Time Point
NCT03160521 (11) [back to overview]Plasma PK Parameters
NCT03160521 (11) [back to overview]PANSS Total Score Mean Change From Baseline to Endpoint
NCT03160521 (11) [back to overview]PANSS Response Rate at Endpoint
NCT03160521 (11) [back to overview]PANSS Positive Subscale Mean Change From Baseline to Endpoint
NCT03160521 (11) [back to overview]SWN-20 Total Score From Baseline at Each Post-baseline Assessment Time Point
NCT03160521 (11) [back to overview]PANSS General Psychopathology Subscale Mean Change From Baseline to Endpoint
NCT03160521 (11) [back to overview]Overall Response Rate at Endpoint
NCT03160521 (11) [back to overview]CGI-S Total Score Mean Change From Baseline to Endpoint
NCT03160521 (11) [back to overview]CGI-I Score Mean at Endpoint
NCT03160521 (11) [back to overview]PANSS Negative Subscale Mean Change From Baseline to Endpoint
NCT03230864 (5) [back to overview]Change From Randomization to Week 8 in Global Clinical Impression - Severity of Illness (CGI-S) Score
NCT03230864 (5) [back to overview]Change From Randomization to Week 8 in 16-item Negative Symptom Assessment (NSA-16 Total) Score
NCT03230864 (5) [back to overview]Response
NCT03230864 (5) [back to overview]Change From Randomization to Week 8 in Positive and Negative Syndrome Scale (PANSS) Total Score
NCT03230864 (5) [back to overview]Change From Randomization to Week 8 in PANSS Marder Negative Factor Score
NCT03503318 (17) [back to overview]Number of Participants Who Maintain Stability at the Endpoint
NCT03503318 (17) [back to overview]Number of Participants Achieving Remission at the Endpoint
NCT03503318 (17) [back to overview]Plasma Concentration of Risperidone, 9-OH-risperidone, and Total Active Moiety (Sum of Risperidone and 9-OH-risperidone)
NCT03503318 (17) [back to overview]Number of Participants Reporting Suicidal Behavior and Suicidal Ideation Using Columbia-Suicide Severity Rating Scale (C-SSRS) at Baseline and Post-Baseline
NCT03503318 (17) [back to overview]Change From Baseline in Total Barnes Akathisia Rating Scale (BARS) Score at the End of Treatment
NCT03503318 (17) [back to overview]Change From Baseline in Total Abnormal Involuntary Movement Scale (AIMS) Score at the End of Treatment
NCT03503318 (17) [back to overview]Change From Baseline in Simpson-Angus Scale (SAS) Mean Score at the End of Treatment
NCT03503318 (17) [back to overview]Change From Baseline in Schizophrenia Quality of Life Scale (SQLS) Total Score at the Endpoint and End of Treatment
NCT03503318 (17) [back to overview]Change From Baseline in Drug Attitudes Inventory 10-item Version (DAI-10) Total Score at the Endpoint and End of Treatment
NCT03503318 (17) [back to overview]Change From Baseline in Clinical Global Impression-Severity of Suicidality (CGI-SS) Score at the End of Treatment
NCT03503318 (17) [back to overview]Change From Baseline in Calgary Depression Scale for Schizophrenia (CDSS) Score at the End of Treatment
NCT03503318 (17) [back to overview]Time to Impending Relapse (Number of Participants With Impending Relapse) in the Adolescent Participants
NCT03503318 (17) [back to overview]Time to Impending Relapse (Number of Participants With Impending Relapse) for Intent-to-treat [ITT] Analysis Set
NCT03503318 (17) [back to overview]Time to Impending Relapse (Number of Participants With Impending Relapse) for Extended ITT [eITT] Analysis Set
NCT03503318 (17) [back to overview]Proportion of Participants With Impending Relapse
NCT03503318 (17) [back to overview]Observed Rate of Impending Relapse (Number of Participants With Impending Relapse) at the Endpoint
NCT03503318 (17) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT03557931 (8) [back to overview]Change From Baseline to Week 12/EoT in University of California San Diego Performance-based Skills Assessment-2 Extended Range (UPSA-2-ER) Total Score
NCT03557931 (8) [back to overview]Number of Participants With Clinically Significant Differences in Simpson Angus Scale (SAS) Values
NCT03557931 (8) [back to overview]Number of Participants With Clinically Significant Differences in Barnes Akathisia Rating Scale (BARS) Values
NCT03557931 (8) [back to overview]Number of Participants With Clinically Significant Differences in Abnormal Involuntary Movement Scale (AIMS) Values
NCT03557931 (8) [back to overview]Number of Participants With Adverse Event (AE)
NCT03557931 (8) [back to overview]Change From Baseline to Week 12/End of Treatment (EoT) in Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Consensus Cognitive Battery (MCCB) Neurocognitive Composite Score
NCT03557931 (8) [back to overview]Number of Participants With Clinically Significant Differences in Columbia-Suicide Severity Rating Scale (C-SSRS) Values
NCT03557931 (8) [back to overview]Concentration at Trough Level (Ctrough) for ASP4345
NCT03568500 (2) [back to overview]Percentage Of Days With Good Patch Coverage
NCT03568500 (2) [back to overview]Participant Adherence
NCT03870880 (11) [back to overview]PANSS Negative Subscale Mean Change From Baseline to Endpoint
NCT03870880 (11) [back to overview]PANSS General Psychopathology Subscale Mean Change From Baseline to Endpoint
NCT03870880 (11) [back to overview]Clinician Global Impression - Improvement (CGI-I) Score
NCT03870880 (11) [back to overview]TEAEs Leading to Study Drug Discontinuation
NCT03870880 (11) [back to overview]Overall Response Rate at Endpoint
NCT03870880 (11) [back to overview]Clinician Global Impression - Severity (CGI-S) Total Score Mean Change From Baseline to Endpoint
NCT03870880 (11) [back to overview]PANSS Positive Subscale Mean Change From Baseline to Endpoint
NCT03870880 (11) [back to overview]Patients With Treatment-related TEAEs
NCT03870880 (11) [back to overview]Patients With Treatment Emergent Adverse Events (TEAEs)
NCT03870880 (11) [back to overview]Relapse Rate
NCT03870880 (11) [back to overview]PANSS Total Score Mean Change From Baseline to Endpoint
NCT03893825 (3) [back to overview]Number of Participants With SAEs
NCT03893825 (3) [back to overview]Number of Participants With Adverse Events (AEs)
NCT03893825 (3) [back to overview]Number of Participants Who Were Withdrawn From the Treatment
NCT03978832 (19) [back to overview]Percent Fluctuation in Concentration Over the Dosing Interval
NCT03978832 (19) [back to overview]Maximum Plasma Concentration Over the Dosing Interval
NCT03978832 (19) [back to overview]Columbia-Suicide Severity Rating Scale (C-SSRS)-Change
NCT03978832 (19) [back to overview]Clinical Global Impression-Severity of Illness Scale (CGI-S)
NCT03978832 (19) [back to overview]Average Plasma Concentration (Cavg) Over the Dosing Interval of Risperidone, 9-OH and Total Active Moiety
NCT03978832 (19) [back to overview]Area Under the Plasma Concentration-time Curve Over the Dosing Interval
NCT03978832 (19) [back to overview]The Number of Participants With TEAEs as Assessed by Local Injection Site*
NCT03978832 (19) [back to overview]The Number of Participants With TEAEs as Assessed by Changes in ECG
NCT03978832 (19) [back to overview]The Number of Participants With TEAEs as Assessed by Changes in Body Weight
NCT03978832 (19) [back to overview]Positive and Negative Syndrome Scale (PANSS)
NCT03978832 (19) [back to overview]The Number of Participants With TEAEs as Assessed by Changes in Laboratory Testing
NCT03978832 (19) [back to overview]Trough Plasma Concentration
NCT03978832 (19) [back to overview]Minimum Plasma Concentration Over the Dosing Interval
NCT03978832 (19) [back to overview]Assessment of Local Injection Site Tolerability*
NCT03978832 (19) [back to overview]Safety as Measured by Columbia-Suicide Severity Rating Scale (C-SSRS) Scores
NCT03978832 (19) [back to overview]The Number of Participants With TEAEs as Assessed by Changes in Vital Signs
NCT03978832 (19) [back to overview]Time to Occurrence of Maximum Concentration
NCT03978832 (19) [back to overview]The Number of Participants With TEAEs as Assessed by Extrapyramidal Symptoms (EPS) of Anti-psychotic Drug Treatment
NCT03978832 (19) [back to overview]Steady-state Average Plasma Concentration (Cavg,ss) of Risperidone and Total Active Moiety
NCT04512066 (12) [back to overview]Mean Change From Baseline in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 4
NCT04512066 (12) [back to overview]PANSS Total Score at Week 12
NCT04512066 (12) [back to overview]Plasma Concentration of RO6889450
NCT04512066 (12) [back to overview]Plasma Concentration of RO6889450
NCT04512066 (12) [back to overview]Proportion of Participants With at Least 20% or 50% Improvement From Baseline in the PANSS Total Score
NCT04512066 (12) [back to overview]Proportion of Participants With at Least 20% or 50% Improvement in the PANSS Total Score up to Week 12
NCT04512066 (12) [back to overview]Participants Ready for Discharge From First Randomized Treatment Intake to Readiness for Discharge as Assessed by the Readiness for Discharge Questionnaire (RDQ) at 4-Week Treatment
NCT04512066 (12) [back to overview]CGI-I up to Week 12
NCT04512066 (12) [back to overview]Change From Baseline in PANSS Factor Scores at Week 4
NCT04512066 (12) [back to overview]CGI-S up to Week 12
NCT04512066 (12) [back to overview]Change From Baseline in Clinical Global Impression Severity (CGI-S) Scores
NCT04512066 (12) [back to overview]Clinical Global Impression - Improvement (CGI-I) Scores
NCT04567524 (12) [back to overview]PK of 9-Hydroxyrisperidone (Cmax).
NCT04567524 (12) [back to overview]PK of Risperidone (Cmax).
NCT04567524 (12) [back to overview]Active Moiety PK (AUC0-24, AUC0-168)
NCT04567524 (12) [back to overview]Active Moiety PK (AUC0-24, AUC0-168)
NCT04567524 (12) [back to overview]PK of 9-Hydroxyrisperidone (AUC0-24h, AUC0-168h).
NCT04567524 (12) [back to overview]Participants With at Least One Treatment Emergent Adverse Event (TEAE).
NCT04567524 (12) [back to overview]Active Moiety Tmax
NCT04567524 (12) [back to overview]PK of 9-Hydroxyrisperidone (AUC0-24h, AUC0-168h).
NCT04567524 (12) [back to overview]PK of Risperidone (AUC0-24h, AUC0-168).
NCT04567524 (12) [back to overview]PK of Risperidone (AUC0-24h, AUC0-168).
NCT04567524 (12) [back to overview]Total Number of Treatment Emergent Adverse Events (TEAEs).
NCT04567524 (12) [back to overview]Active Moiety PK (Cmax)

Number Who Discontinued Medication Within First 6 Study Months

(NCT00044655)
Timeframe: Measured at Six Months

Interventionparticipants (Number)
Stay11
Switch23

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Change From Baseline in PANSS Positive Symptom Subscale Score at 8 Weeks.

The PANSS (described above) includes 7 items that reflect positive psychotic symptoms such as hallucinations and delusions. As are all items within the PANSS, items are categorically rated by the clinician between 0 - no symptoms to 7 extreme symptoms. The minimal score is 0 reflecting no positive symptoms to 49 reflecting that all items were extreme. Higher scores reflect more severe symptoms. Scores above 18 are usually clinically significant. (NCT00053703)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Olanzapine-8.9
Risperidone-8.4
Molindone-8.8

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Change From Baseline in PANSS Negative Symptom Subscale at Week 8

The PANSS (described above) includes 7 items that reflect negative psychotic symptoms such as amotivation and social withdrawal. As are all items within the PANSS, items are categorically rated by the clinician between 0 - no symptoms to 7 extreme symptoms. The minimal score is 0 reflecting no positive symptoms to 49 reflecting that all items were extreme. Higher scores reflect more severe symptoms. Scores above 18 are usually clinically significant. (NCT00053703)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Olanzapine-5.3
Risperidone-5.1
Molindone-5.8

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Change From Baseline in Body Mass Index Change, kg/m2, at Week 8

Change from baseline in Body Mass Index Change, kg/m2, at week 8, last observation was carried forward for individuals who withdrew from treatment early. (NCT00053703)
Timeframe: 8 weeks

Interventionkg/m2 (Mean)
Olanzapine1.27
Risperidone2.20
Molindone0.15

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Change From Baseline in Barnes Akathisia Scale at Week 8

Barnes Akathisia Scale is a clinician rated scale which considers information based on observation of the participant as well as participant report. The scale includes 3 items rated between 0- none to 3 severe and 1 summary item rated between 0 none to 5 severe. All items are summed to obtain the total score. The minimal total score is 0 and the maximal score is 14 with higher scores reflecting more severe akathisia. A score of 4 or more is clinically significant. (NCT00053703)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Olanzapine0.19
Risperidone0.41
Molindone1.23

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Change From Baseline in Weight at Week 8

change in weight from baseline to week 8 in kg (NCT00053703)
Timeframe: 8 weeks

InterventionKg (Mean)
Olanzapine6.12
Risperidone3.64
Molindone0.34

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at 8 Weeks

Assessed with the Positive and Negative Syndrome Scale in which a clinician rates various psychotic symptoms on the basis of observation of the participant, interview with the participant, and review of all other available information including informant reports. The scale consists of 30 items which are rated categorically between 1 - no symptoms to 7 - extreme symptoms. The minimal score is 0 and the maximal score is 210, with higher scores reflecting more symptoms. Typically scores > that 60 are considered clinically significant. (NCT00053703)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Olanzapine-26.6
Risperidone-23.7
Molindone-27.0

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Neuropsychological Testing - Overall Composite Z-score

The neuropsychological testing measured attention, executive function/problem solving, motor speed, processing speed/response generation, and verbal, visual, and working memory. The individual test raw scores were converted to z-scores and an overall composite z-score was computed from the average of the individual test z-scores. Z-scores range from -3 standard deviations up to +3 standard deviations. Higher scores indicate better test performance. (NCT00056498)
Timeframe: Baseline and Week 16

,
Interventionz-score (Mean)
BaselineWeek 16
Placebo-0.030.07
Risperidone0.020.12

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Positive Symptom Item Scores by Week and Treatment Group

"The Brief Psychiatric Rating Scale (BPRS) positive symptom items are: conceptual disorganization, hallucinatory behavior, unusual thought content, and suspiciousness. The total score is calculated by adding the scores for each item. Each scale ranges from 1=Not Present to 7=Very Severe. The minimum score is 4 and the maximum score is 28. A higher score indicates a more severe positive symptom rating. A mixed model for unbalanced repeated measures analysis of covariance (ANCOVA), in which follow-up symptom score = baseline symptom score + treatment + week + treatment x week, and week is treated as a categorical, rather than a continuous measure. The treatment term estimates the average across weeks of the week-specific group differences, and is used as the main test for treatment effects on symptom change." (NCT00056498)
Timeframe: Baseline and every two weeks for 16 weeks.

,
Interventionunits on a scale (Mean)
Week 0Week 2Week 4Week 6Week 8Week 10Week 12Week 14Week 16Change Score
Placebo15.515.114.414.714.914.915.314.214.1-1.5
Risperidone15.514.613.313.913.513.913.813.413.2-2.6

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Negative Symptom Total Score by Week and Treatment Group

The Scale for the Assessment of Negative Symptoms (SANS) total score, minus the global items, inappropriate affect, poverty of content of speech, and attention items, used to measure negative symptoms. SANS total score range = 0-85. Higher scores indicate more severe negative symptoms. A mixed model for unbalanced repeated measures analysis of covariance (ANCOVA), in which follow-up symptom score = baseline symptom score + treatment + week + treatment x week, and week is treated as a categorical, rather than a continuous measure. The treatment term estimates the average across weeks of the week-specific group differences, and is used as the main test for treatment effects on symptom change. (NCT00056498)
Timeframe: Baseline and every two weeks for 16 weeks.

,
Interventionunits on a scale (Mean)
Week 0Week 2Week 4Week 6Week 8Week 10Week 12Week 14Week 16Change Score
Placebo33.034.032.933.034.033.132.434.434.41.1
Risperidone32.330.829.831.230.430.631.631.731.3-2.6

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Modified Side Effects Form for Children and Adolescents

The Modified Side Effects Form for Children and Adolescents includes 62 potential side effects, with measures of frequency and severity for each item. Frequencies are 0=not present, 1=1-2 days, 2=3-4 days, 3=5-7 days. Severity scores are 0=not present, 1=mild (does not interfere with functioning), 2=moderate (some interference with functioning), 3=severe (functioning is significantly impaired because of side effects). Items for cardiovascular, gastrointestinal, central nervous system, ocular, mouth and nose, genito urinary, dermatology, musculo-skeletal, and other side effects are included. For analyses, side effects that were reported at any frequency and a severity of 2 or greater were considered present. (NCT00057681)
Timeframe: Measured at Week 8

Interventionside effects at week 8 (Mean)
Randomized Medication - Lithium5.11
Randomized Medication - Divalproex Sodium4.95
Randomized Medication - Risperidone3.70

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K-SADS Mania Rating Scale

The K-SADS Mania Rating Scale (KMRS) is comprised of 15 items modified from WASH-U-KSADS items. The individual items are scored on a 1-6 severity scale and then these item scores are summed to create an overall KMRS score. Guidelines for interpretation are as follows: 0-11 = no or minimal mania, 12-17 = mild mania, 18-25 = moderate mania, 26+ = marked or worse mania. The maximum possible score is 64. (NCT00057681)
Timeframe: Measured at Week 8

Interventionunits on a scale (Mean)
Randomized Medication - Lithium24.06
Randomized Medication - Divalproex Sodium26.31
Randomized Medication - Risperidone14.58

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Clinical Global Impressions-Bipolar Mania Improvement

The Clinical Global Impressions-Bipolar (CGI-BP) assessment instrument measured improvement in mania, depression, and overall bipolar illness. The primary outcome measure was mania improvement, which measured the change in mania from baseline. Scores were 1=very much improved, 2=much improved, 3=minimally improved, 4=no change, 5=minimally worse, 6=much worse, 7=very much worse. (NCT00057681)
Timeframe: Measured at Week 8

Interventionunits on a scale (Mean)
Randomized Medication - Lithium2.49
Randomized Medication - Divalproex Sodium2.73
Randomized Medication - Risperidone1.70

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Change in CAPS Score From Baseline to Week 24

The primary outcome measure for this study was the total score on the 34-item Clinician-Administered PTSD Scale (CAPS). This study was the intent-to-treat analysis of the improvement in PTSD symptoms from baseline to week-24 follow-up as measured by the CAPS. Total score range for the CAPS is 0-136 with higher values representing a worse outcome. This study was powered initially to detect a 9-point difference between the treatment groups in the CAPS change score. (NCT00099983)
Timeframe: 24 Weeks

Interventionunits on a scale (Least Squares Mean)
Risperidone-16.3
Sugar Pill-12.5

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Change Over Time in Frequency of Heavy Drinking Days (Used to Evaluate Treatment Efficacy)

Frequency of heavy drinking days is obtained each week retrospectively as the number of heavy drinking days during the prior week (assessed by the Timeline Followback Scale). A heavy drinking day is defined as 4 or more drinks per day for a female and 5 or more drinks per day for a male. Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT00130923)
Timeframe: 6 months

Interventionheavy drinking days per week (Number)
Risperidone Long Acting Injectable (LAI)-.11
Oral Risperidone Aka Risperal.68

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Average Over Time of Positive and Negative Symptoms (Used to Evaluate Treatment Efficacy)

A rater assesses positive and negative symptoms of schizophrenia using a 30-item scale (Positive and Negative Symptom Score) Scores range from 30 to 210, where higher values represent a worse outcome. Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT00130923)
Timeframe: 6 months

Interventionordinal severity of symptoms (Number)
Risperidone Long Acting Injectable (LAI)78.2
Oral Risperidone Aka Risperdal75.5

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Average Over Time of Severity of Illness and Global Improvement (Used to Evaluate Treatment Efficacy)

A rater assesses the severity of illness and global impression using a scale from 1 to 7 (Clinical Global Impression), where higher values represent a worse outcome. Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT00130923)
Timeframe: 6 months

Interventionordinal unit of severity (Number)
Risperidone Long Acting Injectable (LAI)4.02
Oral Risperidone Aka Risperal3.96

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Number of Participants With Medication Adherence

Number of participants with medication adherence (defined as taking medication at least 75% of the days in the treatment period). (NCT00130923)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Risperidone Long Acting Injectable (LAI)43
Oral Risperidone Aka Risperdal28

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Average Over Time of Frequency of Drinking Days (Used to Evaluate Treatment Efficacy)

Frequency of drinking days is obtained each week retrospectively as the number of drinking days during the prior week (assessed using the Timeline Followback). Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT00130923)
Timeframe: 6 months

Interventiondrinking days per week (Number)
Risperidone Long Acting Injectable (LAI)2.84
Oral Risperidone Aka Risperdal3.46

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Average Over Time of Global Functioning (Used to Evaluate Treatment Efficacy)

A rater assesses social, occupational and psychological functioning on a hypothetical continuum of mental health - illness (using Global Assessment of Functioning); scores range from 100 to 1, where higher values represent a better outcome. Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT00130923)
Timeframe: 6 months

Interventionordinal severity of impairment (Number)
Risperidone Long Acting Injectable (LAI)50.8
Oral Risperidone Aka Risperdal49.9

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Hazard Ratio for Hospitalization

Hazard ratio of LAI versus Oral for psychiatric hospitalization (in both VA and non-VA hospitals), after randomization up to 24 months, obtained from a Cox proportional hazards model. (NCT00132314)
Timeframe: 24 months

,
Interventionparticipants (Number)
Patients with psychiatric hospitalizationPatients without psychiatric hospitalization
Injectable Risperidone72115
Oral Antipsychotic81101

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Hospitalization-free Survival - Time to Event

A hospitalization-free survival was defined as the time from the date of randomization to the time of a psychiatric hospitalization (in both VA and non-VA hospitals) or, in the case of patients who were hospitalized at randomization, the time from the date of discharge from the initial stay to subsequent hospitalization. Patients without an event were censored at 24 months after the date of randomization. (NCT00132314)
Timeframe: From randomization until date of first re-hospitalization, assessed up to 24 months

Interventionyears (Median)
Injectable RisperidoneNA
Oral Antipsychotic1.97

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Change in Montgomery-Åsberg Depression Rating Scale (MADRS)

Measure of depression; score range 0 to 60 (lower score = less severity) (NCT00132678)
Timeframe: Baseline and Endpoint (last observation carried forward) of 24 month Double-Blind Period IV

Interventionunits on a scale (Mean)
RISPERDAL CONSTA2.8
Placebo4.9

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Change in Young Mania Rating Scale (YMRS) Scores.

Measure of mania; score range 0 to 60 (lower score = less severity) (NCT00132678)
Timeframe: Baseline and Endpoint (last observation carried forward) of 24 month Double-Blind Period IV

Interventionunits on a scale (Mean)
RISPERDAL CONSTA2.9
Placebo9.1

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Number of Participants Who Had a Mood Relapse.

"Mood Relapse was defined as:~The subject met DSM-IV criteria for a manic, hypomanic, mixed, or depressive episode; or, the subject needed treatment intervention with any mood stabilizer, antipsychotic medication (other than study drug), benzodiazepine (beyond the dosage allowed), or antidepressant medication; or the subject required hospitalization for any bipolar mood episode; or the subject had a YMRS or MADRS score >12 or a CGI-S score >4; or a dose increase, or supplementation with oral risperidone or another antipsychotic or mood stabilizer, was needed in the opinion of the investigator." (NCT00132678)
Timeframe: 24 months

,
InterventionParticipants (Number)
RelapsedNot Relapsed
Placebo7659
RISPERDAL CONSTA4298

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Time to Reach 90% Ideal Body Weight (IBW) and Maintain for 1 Month, Stratified by >=80% at Start of Study

The mean survival time and its standard error were underestimated because the largest observation was censored and the estimation was restricted to the largest event time. These estimates were produced using Kaplan-Meier probabilities. This was measured weekly from 0-18 weeks. (NCT00140426)
Timeframe: weekly

Interventionweeks (Mean)
Placebo10.7
Risperidone8.1

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Time to Reach 90% IBW and Maintain for 1 Month, Stratified by IBW <80% at Start of Study

The mean survival time and its standard error were underestimated because the largest observation was censored and the estimation was restricted to the largest event time. These estimates were produced using Kaplan-Meier probabilities. (NCT00140426)
Timeframe: 0 - 18 weeks

Interventionweeks (Mean)
Placebo10.1
Risperidone12.9

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Hazard Ratio for Time to Reaching Ease Of Eating Level 3 From Start of Study (Normal Eating Behavior)

"The Ease of Eating Scale (EOES) is a 14 item scale which measures Food avoidance behaviors (FABs). The scale is rated by staff observing a subject eating a meal or snack. 0 = normal eating behavior, maximum score 28.~Higher scores indicate more food avoidance behaviors, such as taking small bites, taking > 30 seconds between bites (slow eating), etc.~EOE was completed for each meal a subject ate in the program and scores were averaged for each week in the study and entered in the data base.~Change in EOES score was calculated by evaluating change over time. This measure was only used in Phase 1 of the study, for days the subjects were in the treatment program." (NCT00140426)
Timeframe: weekly up to study endpoint: reaching target weight and maintaining for 1 month

Interventionhazard ratio (Number)
Placebo0.85
Risperidone1

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Color A Person Test (CAPT)

"Color A Person Test (CAPT) - Subjects color an outlined image of a body to indicate body dissatisfaction (red (5)= very dissatisfied, Yellow, dissatisfied, black, neutral, green satisfied, blue very satisfied (1). The outline is divided into16 sections for scoring. The CAPT was completed at baseline and monthly during study participation.~Total CAPT scores were calculated by adding the total score and dividing by 16. Score range is 1-5. Lower scores indicate less body dissatisfaction.~Change in the CAPT score during the study was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points." (NCT00140426)
Timeframe: monthly

Interventionunits on a scale (Mean)
Risperidone or Placebo0.03
Risperidone0.22

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Change in Ratings of Anxiety Symptoms on the Multidimensional Anxiety Scale for Children (MASC)

"The Multidimensional Anxiety Scale for Children (MASC) is a self report measure completed by the subject that measures anxiety symptoms.~Higher scores indicate greater anxiety. A score of over 50 is significant for anxiety~Change in MASC scores was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points." (NCT00140426)
Timeframe: monthly to study end point

Interventionunits on a scale (Mean)
Placebo7.41
Risperidone7.87

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Change in Prolactin Levels

Prolactin serum blood levels, measured in nanograms / ml (NCT00140426)
Timeframe: week 0 and week 7

Interventionng/ml (Mean)
Placebo-5.18
Risperidone38.27

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Change in Leptin Levels

Leptin levels were measured by serum blood draws, results reports in nanograms / ml (ng/ml). (NCT00140426)
Timeframe: Week 0 and week 7

Interventionng/ml (Mean)
Placebo0.88
Risperidone3.27

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Change in Eating Disorder Inventory-2 Drive for Thinness Subscale (DT)

"Eating Disorder Inventory -2 - Subscale : Drive for Thinness Subscale (DT). Lower scores are better on this scale and indicate less cognitive focus on drive for thinness.~The EDI 2 is a 91 item scale with 8 subscales - (Drive for thinness, Bulimia, body dissatisfaction, ineffectiveness, perfection, interpersonal distrust, interoceptive awareness and maturity fears.). The DT subscale was used for this outcome. Respondents rate each item as usually , often, sometimes, rarely or never. Subscale scores are computed by summing all item scores for each subscale. There are 7 items in the DT subscale (questions 1,7,11,16,25,32 and 49). the subscale score range is 0-21. The EDI-2 was completed by subjects at baseline and then monthly during study participation (range 0 -18 weeks). Change in the DT subscale score was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points." (NCT00140426)
Timeframe: month

Interventionunits on a scale (Mean)
Placebo1.36
Risperidone3.93

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Change in Eating Disorder Inventory (EDI)-2 Score for Body Dissatisfaction (BD)

"change in Eating Disorder Inventory (EDI) 2-score for Body Dissatisfaction (BD).~Lower scores are better on this scale. Higher scores indicate the subject has greater body dissatisfaction. BD is one of the 8 subscales of the EDI-2. 9 of the 91 questions in the EDI-2 scale constitute this subscale. The score range is 0-27. Subjects completed the EDI-2 at baseline and monthly during study participation (range 0 to 18 weeks). Change in the BD subscale score during the study was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points." (NCT00140426)
Timeframe: monthly

Interventionunits on a scale (Mean)
Placebo0.82
Risperidone2.67

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Body Image Software (BIS) - Point of Subjective Equality (PSE)

"Body Image Software (BIS) - the subject adjusts a digital image of themselves on the computer to their desired image, and also completes a task that determines their perception of their current image. Accuracy is measured by a smaller score between desired image and actual image.~Change in BIS -PSE was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points.~There are no identifiable minimum/maximum values as there would be in a questionnaire scale. Interpreting the PSE is how it compares to a PSE = 0, which is no distortion in body size." (NCT00140426)
Timeframe: monthly

Interventionunits on a scale (Mean)
Risperidone or Placebo-0.32
Risperidone-2.18

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Body Image Software (BIS): Average Desired Thinness

"Body Image Software (BIS) - the subject adjusts a digital image of themselves on the computer to their desired image. The BIS program calculates the difference between their actual image, and how much they have adjusted the image to represent their desired image. Accuracy is measured by a smaller score between desired image and actual image.~Change in BIS - Average Desired Thinness score was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points.~There are no identifiable minimum/maximum values as there would be in a questionnaire scale. . There are no subscales." (NCT00140426)
Timeframe: monthly

Interventionunits on a scale (Mean)
Risperidone or Placebo1.88
Risperidone-1.42

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Body Image Software (BIS): Average Distortion

"Body Image Software (BIS) - the subject adjusts a digital image of themselves on the computer using the direction to adjust their image to how they see themselves right now, this determines their perception of their current image. Accuracy is measured by a smaller score between desired image and actual image.~Change in the BIS Average Distortion score during the study was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points.~There are no identifiable minimum/maximum values as there would be in a questionnaire scale. There are no subscales. The BIS program calculates the difference between their actual image and the size of the image they have adjusted the digital image to based on their perception of how they see themselves right now" (NCT00140426)
Timeframe: monthly

Interventionunits on a scale (Mean)
Risperidone or Placebo-0.22
Risperidone1.40

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Body Image Software (BIS) - Difference Limen (DL)

"Body Image Software (BIS) - the subject adjusts a digital image of themselves on the computer to their desired image, and also completes a task that determines their perception of their current image. Accuracy is measured by a smaller score between desired image and actual image.~Change in BIS-DL was calculated using an estimate of change in score between week 0 and week 7 derived from the mixed effect model across all time points.~There are no identifiable minimum/maximum values as there would be in a questionnaire scale. There are no subscales. Interpreting the DL occurs by referencing it to DL= 0, which would reflect a total inability to detect size differences, which has never occurred in studies using the BIS program." (NCT00140426)
Timeframe: monthly

Interventionunits on a scale (Mean)
Risperidone or Placebo-0.19
Risperidone-1.16

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Child Depression Rating Scale- Revised (CDRS-R)

Response for depressive symptoms was defined as a score less than 40 on the CDRS-R. Range is 18 to 120. Score 18 is normal and higher score signifies depression. The Children's Depression Rating Scale (CDRS) is a 16-item measure used to determine the severity of depression in children 6-18 years of age. Items are measured on 3-, 4-, 5-, and 6-point scales. The mean and standard deviation are measured in this study to illustrate outcome at baseline and when the subject ended the study. (NCT00176202)
Timeframe: Six week study with assessment at baseline and end of the study (at the end of 6 weeks or earlier if they ended the study before 6 week end point).

,
Interventionunits on a scale (Mean)
BaselineLast Observation Carried Forward (p<.01)
Divalproex40.7635.76
Risperidone41.7225.88

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Child Mania Rating Scale (CMRS)

Child Mania rating scale is a parent rated measure to screen for symptoms of mania. It includes 21 items reflecting the DSM-IV criteria for a manic episode. Each item is answered on a four-point Likert type scale anchored by 0 (Never/Rare), 1 (Sometimes), 2 (Often), and 3 (Very Often). Maximum score possible is 63. Score higher than 20 is considered clinically significant, and this is a dimensional score of manic severity. (NCT00176202)
Timeframe: Six week study with assessment at baseline and end of the study (at the end of 6 weeks or earlier if they ended the study before 6 week end point).

,
Interventionunits on scale (Mean)
BaselineLOCF
Divalproex Sodium28.019.20
Risperidone30.8416.35

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Clinical Global Improvement in Bipolar Disorder Overall (CGI-BP Overall)

Severity of Illness and Global Improvement are rated on a 7-point scale by the clinician. In addition to rating the overall illness with the CGI-BP, severity and improvement are considered on various other dimensions such as mania, depression, attention deficit/hyperactivity, psychosis, aggression and sleep difficulties. Score of 1, 2 and 3 would mean there is clinically observed symptom improvement where 1 is the best outcome than 2 or 3. The point 4 is the point where the subject presents at baseline of that specific individual. If they become worse on clinical symptoms, they are rated as 5, 6 or 7 where 7 is worse than 5. (NCT00176202)
Timeframe: Six week study with assessment at baseline and end of the study (at the end of 6 weeks or earlier if they ended the study before 6 week end point).

,
Interventionunits on a scale (Mean)
BaselineLOCF
Divalproex Sodium4.372.97
Risperidone4.802.77

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Young Mania Rating Scale (YMRS)

This measure has 11 items. The purpose of each item is to rate the severity of that abnormality in the patient. A severity rating is assigned to each of the eleven items, based on the patient's subjective report of his or her condition over the previous forty-eight hours and the clinician's behavioral observations during the interview, with the emphasis on the latter. There are four items that are graded on a 0 to 8 scale (irritability, speech, thought content, and disruptive/aggressive behavior), while the remaining seven items are graded on a 0 to 4 scale. Total score of zero to 60 is possible, zero being normal and 60 being severe, 12 serving as a cut off point for illness if equal or above. There are several ways to show change in outcome. We show the mean and standard deviation at week 0 and 6. (NCT00176202)
Timeframe: Six week study with assessment at baseline and end of the study (at the end of 6 weeks or earlier if they ended the study before 6 week end point).

,
Interventionunits on a scale (Mean)
BaselineLast observation carried forward (LOCF)
Divalproex25.0915.24
Risperidone30.5910.22

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Number of Participants With Treatment Emergent Hyperlipidemia

Number of participants with Hyperlipidemia as determined by safety labs (NCT00177164)
Timeframe: from baseline to end of 15 months

Interventionparticipants (Number)
Risperidone LAI0
Oral AAP0

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Number of Participants With Treatment - Emergent Hyperglycemia

Number of participants with hyperglycemia based on safety labs (NCT00177164)
Timeframe: from baseline to end of 15 months

Interventionparticipants (Number)
Risperidone LAI0
Oral AAP0

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BMI

BMI at baseline and at end of 15 months for Risperidone LAI and oral AAP groups (NCT00177164)
Timeframe: baseline to end of 15 months

,
Interventionkg / m^2 (Mean)
BaselineFinal
Oral AAP29.8632.0
Risperidone LAI31.0532.27

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Evaluate the Number of Clinical Events (Pooled) Occurring Between 3-15 Months Following a Switch/Stabilization of the Antipsychotic Agents Among Patients Who Receive Either Risperidal Consta or One of the 4 Marketed 2nd Generation Antipsychotic Agents.

(NCT00177164)
Timeframe: Upto 15 months

InterventionNumber of clinical events (Mean)
Risperidone LAI0.86
Oral AAP1.61

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Total Weeks Worked

(NCT00183625)
Timeframe: 24 months

InterventionWeeks (Mean)
Individual Placement and Support (IPS)51.53
Individual Placement and Support With Workplace Fundamentals41.37

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Body Mass Index

Intent was to compare medication and not work group conditions. This was initially assessed at baseline and includes total time on either risperidone or olanzapine up to 18 months. (NCT00183625)
Timeframe: First 18 months of study

Interventionkg/m^2 (Least Squares Mean)
Risperidone Treatment29.21
Olanzapine Treatment30.4

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Abnormal Involuntary Movement Scale Scores.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in Abnormal Involuntary Movement Scale scores (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine0.001
Risperidone-0.134

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Body Mass Index (BMI)

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in BMI (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.182
Risperidone-0.195

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Brief Psychiatric Rating Scale Scores.

Normalized insulin senstivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in Brief Psychiatric Rating Scale scores (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine0.035
Risperidone0.066

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Clinical Global Impression - Severity of Illness Scale Scores.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in Clinical Global Impression-Severity of Illness scale scores (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine0.068
Risperidone0.234

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Subcutaneous Fat Area.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in subcutaneous fat area (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.043
Risperidone-0.085

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Visceral Fat Area.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in visceral fat area (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.048
Risperidone-0.057

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Waist Circumference.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in waist circumference (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.206
Risperidone-0.263

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Weight.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in weight (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.212
Risperidone-0.188

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Ratio of Visceral Fat Area to the Subcutaneous Fat Area.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in ratio of visceral far area to subcutaneous fat area (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.055
Risperidone0.101

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Change From Baseline to 12 Week Endpoint in Barnes Akathisia Rating Scale (BARS) Scores

The BARS is a 4-item instrument that evaluates akathisia associated with use of antipsychotic medications. Item 4 is the Global clinical assessment and is rated 0 to 5 (0 = absent, 5 = severe). The other 3 items (related to objective and subjective assessments) are not used for these analyses. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionunits on a scale (Mean)
BaselineChange to last observation
Olanzapine0.240.02
Risperidone0.36-0.02

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Change From Baseline to 12 Week Endpoint in Body Mass Index

Within-and Between-Treatment Group changes in Body Mass Index from baseline to last observation carried forward. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionkilograms per square meter (kg/m2) (Mean)
BaselineChange to Last Observation
Olanzapine28.961.02
Risperidone28.790.39

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Change From Baseline to 12 Week Endpoint in Brief Psychiatric Rating Scale (BPRS) Scores

Brief Psychiatric Rating Scale (BPRS) is an 18-item clinician-administered scale used to assess the degree of severity of a subject's general psychopathological symptoms. Item scores range from 0 (not present) to 6 (extremely severe). Total Scores range from 0 to 108; Positive Subscale Scores range from 0 to 24. Negative Subscale Scores range from 0 to 18. Anxiety-Depression Subscale Scores range from 0 to 24. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionunits on a scale (Mean)
Total Score BaselineTotal Score Change to Last ObservationPositive Subscale Score BaselinePositive Subscale Score Change to Last ObservationNegative Subscale Score BaselineNegative Subscale Score Change to Last ObservationAnxiety-Depression BaselineAnxiety-Depression Change to Last Observation
Olanzapine13.32-1.985.22-0.822.32-0.384.33-0.78
Risperidone13.96-1.485.27-1.201.88-0.023.73-0.32

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Change From Baseline to 12 Week Endpoint in Clinical Global Impression - Severity of Illness Scores

Measures severity of illness at the time of assessment. Scores range from 1 (normal, not at all ill) to 7 (among the most extremely ill patients. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionunits on a scale (Mean)
BaselineChange to last observation
Olanzapine3.65-0.22
Risperidone3.61-0.23

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Change From Baseline to 12 Week Endpoint in Eating Behavior Assessment Scale Scores

Eating Behavior Assessment Scale is a 9-item self-rated tool used to evaluate appetite and eating behaviors. Item scores range from 0 (never) to 4 (always). (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionunits on a scale (Mean)
Item 1 Baseline (How Hungry?)Item 1 Change to Last ObservationItem 2 Baseline (How Strong Appetite?)Item 2 Change to Last ObservationItem 3 Baseline (Craved Sweets or Other Carbos?)Item 3 Change to Last ObservationItem 4 Baseline (Craved Fatty Foods?)Item 4 Change to Last ObservationItem 5 Baseline (Felt Full After Meal?)Item 5 Change to Last ObservationItem 6 Baseline(Excessive Food to Feel Satisfied?)Item 6 Change to Last ObservationItem 7 Baseline (Thinking About Food?)Item 7 Change to Last ObservationItem 8 Baseline (Overeating?)Item 8 Change to Last ObservationItem 9 Baseline (Feel Eating is Out of Control?)Item 9 Change to Last Observation
Olanzapine1.420.251.540.171.000.190.800.312.59-0.170.860.170.900.120.420.170.100.25
Risperidone1.320.421.320.380.830.360.740.252.550.000.790.280.770.130.530.150.260.11

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Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Direct Low Density Lipoprotein (LDL)

Fasting lipid parameters including Direct LDL, change from baseline to last observation carried forward. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionmillimoles per Liter (mmol/L) (Mean)
BaselineChange to last observation
Olanzapine3.18-0.03
Risperidone3.11-0.02

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Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including High Density Lipoprotein (HDL)

Fasting lipid parameters including HDL change from baseline to last observation carried forward. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionmillimoles per Liter (mmol/L) (Mean)
BaselineChange to last observation
Olanzapine1.080.06
Risperidone1.180.05

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Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Lipoprotein Subclasses

Changes in lipid parameters and subclass lipoproteins last observation carried forward (LOCF) mean change from baseline. HDL=High Density Lipoprotein, IDL=Intermdiate Density Lipoprotein, LDL=Low Density Lipoprotein, VLDL=Very Low Density Lipoprotein. (NCT00190749)
Timeframe: baseline and 12 weeks.

,
Interventionnanomoles per Liter (nmol/L) (Mean)
HDL particles, total, baselineHDL particles, total, change to last observationIDL, baselineIDL, change to last observationMedium small LDL, baselineMedium small LDL, change to last observationSmall LDL, baselineSmall LDL, change to last observationVery small LDL, baselineVery small LDL, change to last observationVLDL mean particle size, baselineVLDL mean particle size, change to last observ.
Olanzapine28.391.7153.1821.40175.1535.70878.68128.55703.6392.7551.214.09
Risperidone29.81-1.0952.56-2.69197.00-11.47977.84-74.09780.78-62.5051.051.80

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Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Total Cholesterol

Fasting lipid parameters including total cholesterol, change from baseline to last observation carried forward. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionmillimoles per Liter (mmol/L) (Mean)
BaselineChange to Last Observation
Olanzapine4.910.18
Risperidone4.970.01

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Change From Baseline to 12 Week Endpoint in Fasting Lipid Parameters Including Triglycerides

Changes in fasting lipid parameters including triglycerides last observation carried forward (LOCF) mean change from baseline (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionmillimoles per Liter (mmol/L) (Mean)
BaselineChange to Last Observation
Olanzapine1.680.34
Risperidone1.55-0.10

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Change From Baseline to 12 Week Endpoint in Simpson Angus Scale Scores

Measures neuroleptic-induced parkinsonism. Total score of Simpson Angus Scale consists of the sum of 10 items rated on a 5-point severity scale where 0=normal and 4=extreme. The total score ranges from 0 to 40. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionunits on a scale (Mean)
BaselineChange to last observation
Olanzapine1.13-0.06
Risperidone0.940.30

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Change From Baseline to 12 Week Endpoint in Subcutaneous Fat Area

Subcutaneous fat area change from baseline to last observation carried forward, all randomized patients, double-blind treatment period (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionsquare centimeters (cm2) (Mean)
BaselineChange to last observation
Olanzapine281.074.94
Risperidone317.1635.15

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Change From Baseline to 12 Week Endpoint in the Ratio of the Visceral Fat Area to the Subcutaneous Fat Area

Ratio of the visceral fat area to the subcutaneous fat area change from baseline to last observation carried forward, all randomized patients, double-blind treatment period (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionratio in square centimeters (cm2) (Mean)
BaselineChange to last observation
Olanzapine0.410.01
Risperidone0.430.00

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Change From Baseline to 12 Week Endpoint in Visceral Fat Area

Visceral fat area change from baseline to last observation carried forward, all randomized patients, double-blind treatment period (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionsquare centimeters (cm2) (Mean)
BaselineChange to Last Observation
Olanzapine101.464.70
Risperidone102.178.70

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Change From Baseline to 12 Week Endpoint in Waist Circumference

Waist circumference change from baseline to last observation carried forward. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventioncentimeters (Mean)
BaselineChange to Last Observation
Olanzapine99.132.38
Risperidone98.490.17

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Change From Baseline to 12 Week Endpoint in Weight

Weight change from baseline to last visit (last observation carried forward) (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionkilograms (Mean)
BaselineChange to Last Observation
Olanzapine85.932.98
Risperidone86.551.23

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Change in Baseline to Last Observation In Normalized Insulin Sensitivity Index at Low Insulin Phase Using Change in Weight as a Covariate

Normalized insulin sensitivity index (Mffm/I) was defined as the ratio of whole body glucose disposal rate normalized to fat-free mass (Mffm) divided by the plasma insulin concentration (I) during steady-state conditions of the clamp procedure. Units:[(mg glucose)*min*mL] / [(kg fat free body mass)*(micro IU insulin)] (NCT00190749)
Timeframe: baseline and 12 weeks

,
InterventionMffm/I (Mean)
BaselineChange to Last Observation
Olanzapine0.1664-0.0149
Risperidone0.1937-0.0327

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Pairwise Correlations Between Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Eating Behavior Assessment Scale Scores.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in Eating Behavior Assessment Scale scores (NCT00190749)
Timeframe: 12 weeks

,
Interventioncorrelation (Number)
Item 1: How Hungry?Item 2: How Strong Appetite?Item 3: Craved Sweets or Other Carbohydrates?Item 4: Craved Fatty Foods?Item 5: Felt Full or Satisfied After Meal?Item 6:Excessive Amount of Food to Feel Satisfied?Item 7: Thinking About Food?Item 8: Overeating?Item 9: Feel Eating is Out of Control?
Olanzapine-0.137-0.137-0.009-0.068-0.1170.134-0.172-0.032-0.075
Risperidone-0.371-0.2690.035-0.184-0.0600.0670.045-0.165-0.354

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Pairwise Correlations Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in the Simpson Angus Scale Scores.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in the Simpson Angus Scale scores (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine0.184
Risperidone0.249

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Pairwise Correlation Between Changes in Normalized Insulin Sensitivity Index at Low Insulin Phase and Changes in Barnes Akathisia Scale Scores.

Normalized insulin sensitivity index (Mffm/I) at low insulin phase-pairwise correlations between changes in Mffm/I and changes in Barnes Akathisia scores (NCT00190749)
Timeframe: 12 weeks

Interventioncorrelation (Number)
Olanzapine-0.120
Risperidone0.006

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Change From Baseline to 12 Week Endpoint in Abnormal Involuntary Movement Scale Scores

A 12-item instrument assesses observed abnormal movements in different parts of body. Seven items are scored in a 5-point scale (0 = none/normal, 4 = severe) which evaluates abnormal movements in 3 main anatomic areas (orofacial area, extremities, and trunk). Total scores range from 0 to 28. Five collected elements are not used in this total. (NCT00190749)
Timeframe: baseline and 12 weeks

,
Interventionunits on a scale (Mean)
BaselineChange to last observation
Olanzapine0.480.04
Risperidone0.530.04

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Change in MRI-measured Subcutaneous Abdominal Fat

This study hypothesized that antipsychotic treatment would increase subcutaneous abdominal fat, as measured by abdominal magnetic resonance imaging (MRI), with larger adverse effects for olanzapine. (NCT00205699)
Timeframe: 12 weeks

InterventionChange in cm-squared (Mean)
Risperidone18.21
Olanzapine34.27
Aripiprazole15.84

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Change in Insulin-stimulated Glucose Rate of Disappearance (Glucose Rd)

This study hypothesized that antipsychotic treatment would decrease insulin sensitivity at muscle, as measured by the insulin-stimulated rate of disappearance of glucose (glucose Rd), with larger adverse effects for olanzapine. (NCT00205699)
Timeframe: 12 weeks

Interventionpercentage of % change (Mean)
Risperidone2.30
Olanzapine-29.34
Aripiprazole-30.26

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Change in Insulin-stimulated Glucose Rate of Appearance (Glucose Ra)

This study hypothesized that antipsychotic treatment would decrease hepatic insulin sensitivity, as measured by the rate of appearance of glucose (glucose Ra), with larger adverse effects for olanzapine. (NCT00205699)
Timeframe: 12 weeks

Interventionpercentage of % change (Mean)
Risperidone-2.50
Olanzapine-6.57
Aripiprazole-3.27

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Change in DEXA % Body Fat

This study hypothesized that antipsychotic treatment would increase percent total body fat, as measured by whole body dual energy x-ray absorptiometry (DEXA), with larger adverse effects for olanzapine. (NCT00205699)
Timeframe: 12 weeks

Interventionpercent body fat (Mean)
Risperidone1.81
Olanzapine4.12
Aripiprazole1.66

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Change in Insulin-stimulated Glycerol Rate of Appearance (Glycerol Ra)

This study hypothesized that antipsychotic treatment would decrease insulin sensitivity at adipose tissue, as measured by the insulin-stimulated rate of disappearance of glycerol (glycerol Ra), with larger adverse effects for olanzapine. (NCT00205699)
Timeframe: 12 weeks

Interventionpercentage of % change (Mean)
Risperidone-3.65
Olanzapine-8.29
Aripiprazole1.70

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Change in MRI-measured Visceral Abdominal Fat

This study hypothesized that antipsychotic treatment would increase visceral abdominal fat, as measured by abdominal magnetic resonance imaging (MRI), with larger adverse effects for olanzapine. (NCT00205699)
Timeframe: 12 weeks

InterventionChange in cm-squared (Mean)
Risperidone6.85
Olanzapine10.73
Aripiprazole12.04

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Change in the PANSS Psychopathology Subscale Score

"PANSS psychopathology subscale score equals sum of the 16-items scores(range:16-112). Each item has ( 1-7 units),1= absent psychosis symptom, 7= extreme symptom degree.Change in PANSS psychopathology subscale:score at month 24 minus score at randomization. Alleviation of general psychopathology symptoms are indicated by a negative change score." (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-4.2
Risperidone-4.4

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Change in the Positive and Negative Syndrome Scale (PANSS) Total Score

"PANSS total score equals sum of the 30-items scores (range: 30-210). Each item has ( 1-7 units), 1 indicates absent psychosis symptom, and 7 - extreme symptom degree. Change in PANSS total score : total score at month 24 minus total score at randomization.Alleviation of psychotic symptoms are indicated by a negative change in PANSS total score." (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-9.1
Risperidone-8.6

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Number of Participants With Potential Extrapyramidal Symptoms (EPS)

Number of participants with adverse events potentially associated with EPS collected by MedDRA Preferred Terms as akathisia, bradykinesia, drooling, dyskinesia, dystonia, extrapyramidal disorder, grimacing, muscle rigidity, parkinsonism, restlessness, tardive dyskinesia, tremor (NCT00206102)
Timeframe: From start of the study treatment to last dose plus 30 days

InterventionParticipants (Number)
Quetiapine Fumarate73
Risperidone106

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Number of Relapses of Schizophrenia or Schizoaffective Disorder

Relapse is defined as a hospital stay for psychiatric symptoms or a 2-point increase from baseline in the CGI severity score. CGI-S score ranges from 0-7 with 0 = Not Assessed, 1 = Normal, not at all and 7 = Among the most extremely ill subjects. (NCT00206102)
Timeframe: At Month 24

InterventionRelapses (Number)
Quetiapine Fumarate24
Risperidone33

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Presence of a Cortical (C) Type of Cataractogenic Potential Events in Participants as Assessed and Agreed by 2 Independent, Treatment-masked Ophthalmologists Using the Lens Opacities Classification System II (LOCS II ) Grading Scale

Presence of C type of cataractogenic potential event in participant was defined if any LOCS II grades of 2, 3, 4, 5 (with any grade of 0, trace,1 at randomization) assessed and agreed by 2 independent, treatment-masked ophthalmologists at any post-randomization assessment in one or both eyes. 0= no cataract; 5 is worst. There are no subscales. 0 is the best, 5 is the worst. (NCT00206102)
Timeframe: Randomization to Month 24

InterventionParticipants with C type event (Number)
Quetiapine Fumarate2
Risperidone8

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Change in Personal Evaluation of Transitions in Treatment (PETiT) Total Score

PETiT total score is the sum of the 30 items of PETiT questionnaire(range:0-60) on subjects perceived well-being, adherence, tolerability, satisfaction with treatment. Each item is rated by participant with a 3 point frequency scale:2=often, 1=sometimes, 0=never.Change in PETiT total score: total score at month 24 minus total score at randomization (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate1.2
Risperidone0.9

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Presence of a Nuclear Opalescence (N) Type of Cataractogenic Potential Events in Participants as Assessed and Agreed by 2 Independent, Treatment-masked Ophthalmologists Using the LOCS II Grading Scale

Presence of N type of cataractogenic potential event in Participants was defined if any LOCS II grades of 2, 3, 4 (with grade at rand equals 0,1), or if the LOCS II grades of 3,or 4 (with grade at randomization=2) assessed and agreed by 2 independent, treatment-masked ophthalmologists at any post-randomization assessment in one or both eyes. 0 is the best, 4 is the worst. (NCT00206102)
Timeframe: Randomization to Month 24

InterventionParticipants with N type event (Number)
Quetiapine Fumarate0
Risperidone2

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Presence of a Posterior Subcapsular (P) Type Cataractogenic Potential Events in Participants as Assessed and Agreed by 2 Independent, Treatment-masked Ophthalmologists Using the LOCS II Grading Scale

Presence of P type of cataractogenic potential event in participant was defined if any LOCS II grades of 1, 2, 3 , 4 (with grade=0 at randomization) assessed and agreed by 2 independent, treatment-masked ophthalmologists at any post-randomization assessment in one or both eyes. 0 is the best, 4 is the worst. (NCT00206102)
Timeframe: Randomization to Month 24

InterventionParticipants with P type event (Number)
Quetiapine Fumarate4
Risperidone7

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Change in the Clinical Global Impression - Severity of Illness (CGI-S) Score

CGI-S score is accessed on a seven-graded scale ranging from most extremely ill/ very much worse (7) to normal/very much improved (1) , 1 is best. Change : score at month 24 minus score at randomization. (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-0.7
Risperidone-0.5

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Change in Simpson-Angus Scale (SAS) Total Score

SAS total score is the sum of the 10 individual-item scores (range:0-40), with the score for each item ranging from 0 to 4, higher scores indicate greater severity of Parkinsonian symptoms. Change : total score at month 24 minus total score at randomization. Increase in Change of total score indicates an increase in extrapyramidal motor symptoms. (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-0.7
Risperidone-0.4

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Change in the PANSS Negative Subscale Score

"PANSS Negative subscale score equals sum of the 7-items scores(range:7-49). Each item has ( 1-7 units), 1 indicates absent psychosis symptom, and 7 - extreme symptom degree. Change in PANSS Negative subscale score:score at month 24 minus score at randomization. Alleviation of negative psychotic symptoms are indicated by a negative change score." (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-2.2
Risperidone-1.5

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Change in the PANSS Positive Subscale Score

"PANSS Positive subscale score equals sum of the 7-items scores(range:7-49). Each item has ( 1-7 units), 1 indicates absent psychosis symptom, and 7 - extreme symptom degree." (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-2.7
Risperidone-2.8

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Change in Barnes Akathisia Rating Scale (BARS) Global Score

BARS global score is the 4th individual-item score on the BARS scale, the Global Assessment of Akathisia, with the score ranging from 0 (no evidence of akathisia) to 5 (severe akathisia). Change : score at month 24 minus score at randomization. Increase in Change of BARS global score indicates an increase in akathisia. (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits of scale (Mean)
Quetiapine Fumarate-0.1
Risperidone0.1

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Change in Abnormal Involuntary Movement Scale (AIMS) Total Score

AIMS total score is the sum of the 10 individual-item scores(range:0-40), with the score for each item ranging from 0 to 4. Change : total score at month 24 minus total score at randomization. Increase in Change of total score indicates an increase in abnormal voluntary movements. The lower score means lower intensity of abnormal voluntary Movements. 0 is best, 4 is worst. Increase in Change of total score indicates an increase in abnormal voluntary Movements. (NCT00206102)
Timeframe: Randomization to Month 24

Interventionunits on scale (Mean)
Quetiapine Fumarate-0.2
Risperidone0.1

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Change From Baseline to Endpoint in Total Positive and Negative Syndrome Scale (PANSS) Score

"The neuropsychiatric symptoms of schizophrenia were assessed by means of the 30-item PANSS scale. The PANSS scale provides a total score (sum of the scores of all 30 items) and scores for 3 subscales, i.e., the positive subscale (7 items), the negative subscale (7 items), and the general psychopathology subscale (16 items).~Each item of the scale is to be scored on a scale of 1 (absent) to 7 (extreme)." (NCT00216476)
Timeframe: Assessed at each visit from the moment the subject was randomized to a treatment arm (baseline visit) until the end of treatment (Week 104 or earlier)

Interventionunits on a scale (Mean)
Risperidone LAI-9.3
Quetiapine-1.1
Aripiprazole-7.7

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Mean Relapse Free Period (Exploratory/Aripiprazole)

As for risperidone and quetiapine, relapse was defined as meeting any of the predefined criteria (adapted from Csernansky et al., 2002) on 2 consecutive evaluations during treatment, 3 to 5 days apart. Since aripiprazole was new on the market at the time the study was conducted, this aripiprazole analysis was exploratory. (NCT00216476)
Timeframe: Assessed at each visit from the moment the subject was randomized to a treatment arm (baseline visit) until the end of treatment (Week 104 or earlier)

Interventiondays (Mean)
Aripiprazole314

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Mean Relapse Free Period(Risperidone LAI Versus Quetiapine)

Relapse was defined as meeting any of the predefined criteria (adapted from Csernansky et al., 2002) on 2 consecutive evaluations during treatment, 3 to 5 days apart. The relapse rate in each treatment arm was estimated using the Kaplan-Meier method. (NCT00216476)
Timeframe: Assessed at each visit from the moment the subject was randomized to a treatment arm (baseline visit) until the end of treatment (Week 104 or earlier)

Interventiondays (Mean)
Risperidone LAI607
Quetiapine533

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Change From Baseline to Endpoint in Short-Form Health Survey 12 (SF-12) Scores

Quality of life was assessed by means of the 12-item SF-12® survey. Two parameters, i.e., PCS (physical component summary) and MCS (mental component summary) were calculated. Both components scores range from 0 to 100 with higher scores indicating better QOL. (NCT00216476)
Timeframe: Assessed at the moment the subject was randomized to a treatment arm (baseline visit) and after 1, 3, 6, 12, 18, and 24 months of treatment

,,
Interventionunits on a scale (Mean)
PCS scoreMCS score
Aripiprazole2.44.9
Quetiapine1.02.7
Risperidone LAI2.13.2

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Change From Baseline to Endpoint in Clinical Global Impression Scale (CGI) Score

The 7-point CGI scale of Severity (CGI-S) was used to assess the severity of a subject's psychotic condition (0= normal, not at all ill, 1= borderline, etc. and 6= among the most extremely ill subjects). (NCT00216476)
Timeframe: Assessed at each visit from the moment the subject was randomized to a treatment arm (baseline visit) until the end of treatment (Month 24 or earlier)

Interventionunits on a scale (Mean)
Risperidone LAI-0.3
Quetiapine0.1
Aripiprazole-0.1

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Change From Baseline in PANSS Total Score at Week 12

The PANSS is a specific scale for the measurement of the symptoms of schizophrenia. Symptoms of schizophrenia will be assessed using the 30-item PANSS scale. Each item of the scale is to be scored on a scale of 1 (absent) to 7 (extreme). The total score can range from 30 to 210. (NCT00216671)
Timeframe: at baseline and Week 12.

Interventionscores on a scale (Mean)
Early Initiation of Treatment-35.84
Late Initiation of Treatment-34.49

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Change From Baseline in PANSS Total Score at Week 6

The PANSS is a specific scale for the measurement of the symptoms of schizophrenia. Symptoms of schizophrenia will be assessed using the 30-item PANSS scale. Each item of the scale is to be scored on a scale of 1 (absent) to 7 (extreme). The total score can range from 30 to 210. (NCT00216671)
Timeframe: at baseline and Week 6.

Interventionscores on a scale (Mean)
Early Initiation of Treatment-27.48
Late Initiation of Treatment-27.96

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Change in Positive And Negative Syndrome Scale (PANSS) Total Score From Baseline to Endpoint

The PANSS is a specific scale for the measurement of the symptoms of schizophrenia. Symptoms of schizophrenia will be assessed using the 30-item PANSS scale. Each item of the scale is to be scored on a scale of 1 (absent) to 7 (extreme).The total score can range from 30 to 210. (NCT00216671)
Timeframe: at baseline and Week 26 or at premature discontinuation

Interventionscores on a scale (Mean)
Early Initiation of Treatment-38.37
Late Initiation of Treatment-37.24

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Change From Baseline to Endpoint in Global Assessment of Functioning (GAF)

Overall psychological, social, and occupational functioning is rated on a scale of mental health-illness from 1 being the worst functioning to 100 being the best. Impairment in functioning due to physical (or environmental) limitations must not be included in the rating. (NCT00216671)
Timeframe: at baseline and endpoint (week 26 or at premature discontinuation).

Interventionscores on a scale (Mean)
Early Initiation of Treatment19.65
Late Initiation of Treatment18.72

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Change From Baseline to Endpoint in Quality of Life Questionnaire SF-12

Short Form Health Survey: A generic dual-ie, mental and physical health-scale measure of quality of life. This is a 12-item subset of the SF-36 survey that measures the same 8 domains of health. As a brief, reliable measure of overall health status, the SF-12 is the instrument of choice in large population health surveys and has been used extensively as a screening tool. SF-12 will be filled in by the patient. The scores range from 0 to 100, where a zero score indicates the lowest level of health measured by the scales and 100 indicates the highest level of health. (NCT00216671)
Timeframe: at baseline, Weeks 6, 12, and endpoint (week 26 or at premature discontinuation).

,
Interventionscores on a scale (Mean)
Physical Component Summary (PCS)Mental Component Summary (MCS)
Early Initiation of Treatment2.763.25
Late Initiation of Treatment1.752.96

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Change From Baseline to Endpoint in Clinical Global Impression - Severity (CGI-S)

The CGI-S rating scale is used to rate the severity of a subject's psychotic condition on a 7-point scale ranging from 1 (not ill) to 7 (extremely severe). This scale permits a global evaluation of the subject's condition at a given time. (NCT00216671)
Timeframe: at baseline and endpoint (week 26 or at premature discontinuation).

Interventionscores on a scale (Mean)
Early Initiation of Treatment-1.91
Late Initiation of Treatment-2.03

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YMRS

Young Mania Rating Scale (YMRS) total scores change from baseline by treatment group. The YMRS total score ranges from 0 to 60 where higher scores indicate more severe mania, thus, a negative change (or decrease) from baseline indicates a reduction (or improvement) in manic symptoms. (NCT00221403)
Timeframe: 6 weeks

Interventionscore on a scale (Least Squares Mean)
Valproate (VPA)10
Risperidone18.82
Placebo4.29

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Working Memory

"California Verbal Learning Test (CVLT) trials 1 through 5 is a well established neuropsychological test of working memory. The maximum score is 80 which reflects a better outcome and the minimum score is 0 which reflects a worse outcome.~The only meaningful analyses with adequate statistical power that could be reported were of the 10 schizophrenia patients who met nonresponse criteria to ziprasidone. The overall enrollment of 35 subjects was insufficient to perform the originally planned analyses in a statistically valid manner." (NCT00225498)
Timeframe: 3 months

Interventionunits on a scale (Mean)
Ziprasidone44.8

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Abnormal Involuntary Movement Scale (AIMS)

The AIMS is a 12-item scale to provide a numeric measure to the observed abnormal movements in different parts of the body. Information is collected after a brief neurological examination and is scored on a 5-point scale (0=none, 4=severe). Ten items are scored in a 5-point scale (0 = none/normal, 4 = severe) which evaluates abnormal movements in three main anatomic areas (orofacial area, extremities, and trunk). Two items are yes/no questions regarding dental status. Total scores range from 0 to 42 with higher values indicating more severity. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42,35)Week 104 (n=35,29)
Oral Antipsychotic0.80.7
Risperidone Long-acting Injection (LAI)1.10.7

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Time to Relapse

"Time to relapse was calculated from the start of the maintenance phase to date of relapse according to Csernansky: Psychiatric hospitalization; increased level of psychiatric care from start of maintenance period and 25 percent increase in total PANSS score from first maintenance visit, or 10 points increase where PANSS at start of maintenance period was 40 or less; deliberate self-injury, suicidal or homicidal ideation; violent to others; property damage; or substantial clinical deterioration, defined as Clinical Global Impression of Change (CGI-C) score of 6 (much worse)." (NCT00246259)
Timeframe: Week 10 (post-stability) up to Week 104 or LRV

InterventionWeeks (Mean)
Risperidone Long-acting Injection (LAI)80.5
Oral Antipsychotic79.5

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Percentage of Participants With Relapse

"Relapse was defined according to Csernansky: Psychiatric hospitalization; increased level of psychiatric care from start of maintenance period and 25 percent increase in total PANSS score from first maintenance visit, or 10 points increase where PANSS at start of maintenance period was 40 or less; deliberate self-injury, suicidal or homicidal ideation; violent to others; property damage; or substantial clinical deterioration, defined as CGI-C score of 6 (much worse)." (NCT00246259)
Timeframe: Week 10 (post-stability) up to Week 104 or LRV

InterventionPercentage of participants (Number)
Risperidone Long-acting Injection (LAI)34.4
Oral Antipsychotic16.1

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Change From Baseline in Standardized Mental Component Scale Score in Short Form 36 (SF-36) at Week 104 or LRV

The SF-36 is a survey of participant health. It calculates two standardized scales: the standardized mental component scale and the standardized physical component scale. The standardized scales are calculated as weighted sums of the 8 scores, which are: vitality, physical functioning, bodily pain, general health perceptions, physical role functioning, emotional role functioning, social role functioning, and mental health. Each item is scored on a 0-100 range; and standardized mental component scale score is calculated as weighted average of individual item scores on a 0-100 range, where 100 signify highest level of functioning. The change from baseline in mental component scale score was reported. (NCT00246259)
Timeframe: Up to Week 104 or LRV

InterventionUnits on a scale (Mean)
Risperidone Long-acting Injection (LAI)0.6
Oral Antipsychotic4.7

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Change From Baseline in Drug Attitude Inventory (DAI-10) Score at Week 104 or LRV

The DAI, a 10-item scale to assess how the attitude of schizophrenia participants toward their medications may affect compliance. Respondents indicate 'true' or 'false' for each item. An overall calculated score ranged from -10 to 10, where a positive score indicated a positive subjective response (compliant), a negative score indicated non-compliance. Change: score at observation minus score at baseline. (NCT00246259)
Timeframe: Up to Week 104 or LRV

InterventionUnits on a scale (Mean)
Risperidone Long-acting Injection (LAI)-0.1
Oral Antipsychotic-0.2

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Number of Participants With Cognitive Assessment Using Trail A

Cognitive assessments were done using Trail test A which measured variety of functions, including motor speed, visual scanning, attention and visual motor integration. Participants must connect numbered circles in a variety of orders. (NCT00246259)
Timeframe: Week -2, 104 or LRV

,
InterventionParticipants (Number)
Week -2 (0-26 seconds)Week -2 (27-39 seconds)Week -2 (40-51 seconds)Week -2 (52+ seconds)Week -2 (Not reported)Week 104 (0-26 seconds)Week 104 (27-39 seconds)Week 104 (40-51 seconds)Week 104 (52+ seconds)Week 104 (Not reported)
Oral Antipsychotic149462167327
Risperidone Long-acting Injection (LAI)13166611594212

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Total Words Score Over Time

Controlled Word Association Test (COWAT) was used to assess verbal fluency. Participants are given 3 different letters of the alphabet and asked to say as many words beginning with each letter within a controlled time. Participants are then asked to identify as many words as possible in 3 different categories (animals, fruits and vegetables) within a specified period of time. The total score is a sum of all three categories scores. The total score ranges from 0-90, the higher the score the higher the verbal fluency. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=40, 31)Week 104 or LRV (n=30, 28)
Oral Antipsychotic59.965.4
Risperidone Long-acting Injection (LAI)62.463.1

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Simpson Angus Scale (SAS)

The SAS is a 10-item scale used to measure the symptoms of parkinsonism (slow movements) or parkinsonian side-effects related to the use of antipsychotic medications. The 10 items are rated on a 5-point scale (0=complete absence, 4=extreme presence) after a brief neurological examination and observation of the participants' gait (slow, shuffling walk). Total score is sum of individual item scores (range 0 to 40); higher score indicates more affected. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42,34)Week 104 (n=34,29)
Oral Antipsychotic1.21.0
Risperidone Long-acting Injection (LAI)1.11.0

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Number of Participants With Cognitive Assessments Using Trail B

Cognitive assessments were done using Trail test B, which measured variety of functions, including motor speed, visual scanning, attention and visual motor integration. In Trail B, 2 sets of circles contain numbers and letters, and the participant must connect them in alternating order. Trail B is also a measure of executive functions as it requires planning and decision-making. (NCT00246259)
Timeframe: Week -2, 104 or LRV

,
InterventionParticipants (Number)
Week -2 (0-65 Seconds)Week -2 (66-85 seconds)Week -2 (86-120 seconds)Week -2 (121+ seconds)Week -2 (Not reported)Week 104 (0-65 seconds)Week 104 (66-85 seconds)Week 104 (86-120 seconds)Week 104 (121+ seconds)Week 104 (Not reported)
Oral Antipsychotic1253132164537
Risperidone Long-acting Injection (LAI)1788811774212

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Change From Baseline in Young Mania Rating Scale (YMRS) at Week 104 or LRV

Co-morbid symptoms of mania are evaluated by change in YMRS Score which is an 11-item scale to assess symptoms of mania, Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 (the least) to 60 (the worst). (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42,35)Change at Week 104 or LRV (n=34,28)
Oral Antipsychotic4.3-1.5
Risperidone Long-acting Injection (LAI)4.0-1.1

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Change From Baseline in Social and Occupational Functioning Assessment Scale (SOFAS) at Week 104 or LRV

The SOFAS focused exclusively on participants' level of social and occupational functioning. The SOFAS is a 100 point single item scale that rates functioning of a participant. The scale values range from 1=most impaired to 100=healthiest individual. The scale also includes a rating point of 0=missing information. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42, 35)Change at Week 104 or LRV (n=34, 28)
Oral Antipsychotic49.59.5
Risperidone Long-acting Injection (LAI)53.44.6

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 104 or Last Reported Visit (LRV)

The PANSS provides a total score (sum of the scores of all 30 items) and scores for 3 subscales, the positive subscale (7 items), the negative subscale (7 items), and the general psychopathology subscale (16 items), each rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42, 35)Change at Week 104 or LRV (n=42, 34)
Oral Antipsychotic79.7-17.7
Risperidone Long-acting Injection (LAI)80.6-18.1

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Change From Baseline in Calgary Depression Symptom Scale (CDSS) Score at Week 104 or LRV

Co-morbid depressive symptoms are evaluated by change in CDSS Score which was developed to assess symptoms of depression in participants with schizophrenia (psychiatric disorder with symptoms of emotional instability, detachment from reality, often with delusions and hallucinations, and withdrawal into the self). It consists of 9 items, each scored from 0 (absent) to 3 (severe). The total score is a sum of the scores of each item and may range from 0 to 27. Higher score more severe pathology. Data presented here represents the change from baseline to endpoint. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42, 35)Change at Week 104 or LRV (n=34, 28)
Oral Antipsychotic3.5-1.0
Risperidone Long-acting Injection (LAI)3.70.1

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Change From Baseline Hamilton Anxiety Scale (HAM-A) Total Score at Week 104 or LRV

The HAM-A is a 14-item scale designed to measure anxiety in individuals. Each question reflects a symptom of anxiety and physical as well as mental symptoms are represented. The answers range from 0 which signifies a complete lack of that symptom to 4, which indicates a very severe show of anxiety with that symptom. Total score ranges from 0 to 56. Lower score indicates less affected. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionUnits on a scale (Mean)
Baseline (n=42, 35)Change at Week 104 or LRV (n=34, 28)
Oral Antipsychotic7.3-2.9
Risperidone Long-acting Injection (LAI)7.2-0.8

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Barnes Akathisia Rating Scale (BARS) Global Clinical Assessment

The BARS evaluates akathisia (feeling of restlessness) associated with the use of antipsychotic medications, including an objective and a subjective component plus a global impression. Components are rated on a scale of 0 (normal or absence of restlessness)-3 (intense restlessness) and 0 (absent)-5 (severe akathisia) for the global clinical assessment. Number of participants in each global clinical assessment scale are reported. (NCT00246259)
Timeframe: Baseline, Week 104 or LRV

,
InterventionParticipants (Number)
Baseline: Absent (n=42,35)Baseline: Questionable (n=42,35)Baseline: Mild Akathisia (n=42,35)Baseline: Moderate Akathisia (n=42,35)Baseline: Marked Akathisia (n=42,35)Week 104: Absent (n=35,29)Week 104: Questionable (n=35,29)Week 104: Mild Akathisia (n=35,29)Week 104: Moderate Akathisia (n=35,29)Week 104: Marked Akathisia (n=35,29)
Oral Antipsychotic218600252200
Risperidone Long-acting Injection (LAI)2911200217610

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Percentage of Participants Who Experienced a Clinical Exacerbation From Month 3 Post-Randomization

Clinical exacerbation is defined as hospitalization because of participant's schizophrenia (psychiatric disorder with symptoms of emotional instability, detachment from reality, delusions, hallucinations, and self withdrawal) or requiring change from current antipsychotic or initiation of adjunctive antipsychotic, 2-point worsening in Clinical Global Impression of Severity (CGI-S) or emergency room visit, deliberate self-injury, emergence of clinically significant suicidal ideation, utilization of treatment team services, violent behavior, requiring an increase in dose of existing antipsychotic as a result of poor symptom control. (NCT00256997)
Timeframe: Month 3 up to Month 24

InterventionPercentage of participants (Number)
Risperidone Long-Acting Injection (LAI)48.1
Oral Atypical Antipsychotic43.0

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Time to First Clinical Exacerbation

Time to first clinical exacerbation was calculated over the entire trial duration wherein clinical exacerbation is defined as hospitalization because of participant's schizophrenia or requiring change from current antipsychotic or initiation of an adjunctive antipsychotic, 2-point worsening in CGI-S or emergency room visit, deliberate self-injury, emergence of clinically significant suicidal ideation, utilization of treatment team services, violent behavior, requiring an increase in dose of existing antipsychotic as a result of poor symptom control. (NCT00256997)
Timeframe: Baseline up to Month 24

InterventionMonths (Mean)
Risperidone Long-acting Injection (LAI)10.4
Oral Atypical Antipsychotic11.2

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Change From Baseline in Assessment of Quality of Life (AQoL) Score at Month 24

"AQoL is defined as an Australian-developed participant delivered quality of life (QoL) instrument consisting of 15-questions in 5 scales measuring illness, independence, social relationships, physical senses and psychological well-being. Each of the 5 scales is calculated based on the answers to 3 questions. Each question is given an answer dependent utility score (0 [worst] to 1 [best] and then these scores are combined using a multiplicative model to get the normalized scale score value, each scale ranging between 0.0 (representing death) and 1.0 (representing full health). The scores for independent living, social relationships, physical senses and psychological well-being are combined to obtain the QoL utility score which refers to the value of a health state to the respondent where the lower boundary is -0.04 (representing QoL state worse than death), 0.00 (death equivalent QoL state) and to 1.00 (best possible QoL state)." (NCT00256997)
Timeframe: Baseline and Month 24

,
InterventionUnits on a scale (Mean)
Baseline: Illness score (n=79,84)Change at Month 24: Illness score (n=64,67)Baseline: Daily activity score(n=79,83)Change at Month 24: Daily activity score(n=64,67)Baseline: Social score (n=79,83)Change at Month 24: Social score (n=64,66)Baseline: Physical score (n=79,83)Change at Month 24: Physical score (n=64,67)Baseline: Psychological score (n=79,83)Change at Month 24: Psychological score (64,67)
Oral Atypical Antipsychotic0.3590.0350.872-0.0380.6130.0250.9160.0200.8630.023
Risperidone Long-acting Injection (LAI)0.3960.0910.8110.0510.6080.0600.8720.0650.8630.015

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Change From Baseline in Personal and Social Performance Scale (PSP) Total Score at Month 24

The PSP is 100-point validated clinician-rated scale that assesses degree of difficulty in 4 areas of functioning: socially useful activities, personal and social relationships, self-care, disturbing and aggressive behaviors rated on 6-point scale (1=absent to 6=very severe).Total transformed score from 1 to 100 is generated from raw score based on clinical interpretation of scores generated in 4 areas of functioning, with higher transformed score indicating better function. Total score is divided into 3 levels: 71-100 (mild difficulty); 31-70 (marked difficulty) and 1-30 (severe difficulty). (NCT00256997)
Timeframe: Baseline and End of Study (Month 24 or Early Termination [ET])

,
InterventionUnits on a scale (Mean)
Baseline: (n=79, 84)Change at Month 24/ET: (n=67,68)
Oral Atypical Antipsychotic55.08.4
Risperidone Long-acting Injection (LAI)54.25.2

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Total Score at Month 24

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia (psychiatric disorder with symptoms of emotional instability, detachment from reality, often with delusions and hallucinations, and withdrawal into the self) including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210, higher scores indicate worsening. (NCT00256997)
Timeframe: Baseline and Month 24

,
InterventionUnits on a scale (Mean)
Baseline (n=79, 85)Change at Month 24: Total score (n=67, 67)
Oral Atypical Antipsychotic76.5-12.4
Risperidone Long-acting Injection (LAI)77.6-9.6

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Number of Participants With Clinical Global Impression of Change (CGI-C)

The CGI-C is a assessment of change in global clinical status, defined as a sense of well-being and ability to function in daily activities. CGI-C scores range from 1 (very much improved) through to 7 (very much worse). Higher scores indicate worsening. (NCT00256997)
Timeframe: End of Study (Month 24 or Early Withdrawal [EW])

,
InterventionParticipants (Number)
Month 24/EW:At least minimally improved(n= 67,68)Month 24/EW: No change or worse (n=67,68)
Oral Atypical Antipsychotic3830
Risperidone Long-acting Injection (LAI)4819

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Number of Participants With Clinical Global Impression of Severity (CGI-S)

The CGI-S rating scale is used to rate the severity of a patient's psychotic condition on a 7-point scale. It is rated as follows: 1=Normal, not at all ill, 2=Borderline mentally ill, 3=Mildly ill, 4=Moderately ill, 5=Markedly ill, 6=Severely ill, and 7=Among the most extremely ill. Higher scores indicate worsening. (NCT00256997)
Timeframe: Baseline and End of Study (Month 24 or Early Withdrawal [EW])

,
Interventionparticipants (Number)
Baseline: Mild or better (n=79, 85)Baseline: Moderate, marked and severe (n=79, 85)Month 24/EW: Mild or better (n=67, 68)Month 24/EW:Moderate,marked and severe (n=67, 68)
Oral Atypical Antipsychotic26593929
Risperidone Long-acting Injection (LAI)18613631

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Number of Participants With Response to Resource Utilization Questionnaire (RUQ)

This questionnaire included questions asked to participants about any hospitalizations, visits to the emergency room or any other psychiatric treatment received in the previous month. Also the participants and/or primary health care contact or caregiver (or other modality to obtain accurate information) were telephoned on a monthly basis (1 month post Visit 2 through to end of study [Visit 6, Month 24]) by a member of the investigational staff and the resource utilization assessment was conducted over the phone. (NCT00256997)
Timeframe: Baseline up to Month 24

,
InterventionParticipants (Number)
Emergency room visits (total reports)Hospital admissions (total reports)Family doctor visits (total reports)Psychologist doctor visit (total reports)Social worker (total reports)Occupational therapist (total reports)Phychiatric day care (total reports)Phychiatrist (total reports)Visit by a home care nurse (total reports)Psychiatric nurse (total reports)Suicide/crisis services (total reports)Outpatient clinic (total reports)
Oral Atypical Antipsychotic29325813443013788581336
Risperidone Long-acting Injection (LAI)324259144328197415621331

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Percentage of Participants Who Experienced a Clinical Exacerbation

Clinical exacerbation is defined as hospitalization because of participant's schizophrenia or requiring change from current antipsychotic or initiation of an adjunctive antipsychotic, 2-point worsening in CGI-S or emergency room visit, deliberate self-injury, emergence of clinically significant suicidal ideation, utilization of treatment team services, violent behavior, requiring an increase in dose of existing antipsychotic as a result of poor symptom control. (NCT00256997)
Timeframe: Baseline up to Month 24

InterventionPercentage of participants (Number)
Risperidone Long-acting Injection (LAI)54.4
Oral Atypical Antipsychotic54.7

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Change From Baseline in Drug Attitude Inventory-10 (DAI-10) Item Scale Score at Week 96

The DAI-10 is a 10-item questionnaire to assess 1) subjective experience of medication and 2) attitudes and beliefs toward neuroleptics which may influence medication compliance in schizophrenia participants. It is the binary scale assessing the participant's subjective response. A 'compliant' response is scored as +1; a dysphoric response is scored as -1. A positive sum of items indicates a positive subjective response (SR); a negative sum of scores indicates a negative SR (non-compliant). The final score for each person at each time is the positive score minus the negative score. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
BaselineChange at Week 96
Risperidone Long-Acting Injection (RLAI)-0.220.28

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Change From Baseline in Global Assessment of Functioning (GAF) Score at Week 96

GAF is a 100-point tool rating overall psychological, social and occupational functioning of adults. The higher score range (91-100) refers to a superior functioning in a wide range of activities, and absence of symptoms. The lower score range (1-10) refers to persistent danger of severely hurting self or others; or persistent inability to maintain minimum personal hygiene; or serious suicidal act with clear expectation of death. Lower scores indicate worsening. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
BaselineChange at Week 96
Risperidone Long-Acting Injection (RLAI)44.328.86

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Change From Baseline in NCFT: Controlled Oral Word Association Test at Week 96

The Controlled Oral Word Associated Test is a measure of verbal fluency, which requires participants to generate words orally that begin with a given letter of the alphabet. Participants are given 1 min to name as many words as possible. Performance was calculated by the number of words generated in the 1-min period. This measure, requiring rapid and organized word retrieval, is a sensitive indicator of brain dysfunction. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionWords generated per min (Mean)
Baseline: corrected responseChange at Week 96: corrected response
Risperidone Long-Acting Injection (RLAI)10.250.00

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Change From Baseline in NCFT: Memory Quotient (MQ) at Week 96

MQ was obtained by adding up the results of verbal memory and visual memory test. The memory quotient will include learning curve, memory retention, retrieval efficiency, drawing/memory consistency, verbal/visual memory consistency and intelligence/memory consistency. The highest MQ is 160, which indicates excellent memory. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionMQ (Mean)
BaselineChange at Week 96
Risperidone Long-Acting Injection (RLAI)93.7110.70

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Change From Baseline in Clinical Global Impression-Severity (CGI-S) Score at Week 96

The CGI-S rating scale is used to rate the severity of a participant's psychotic condition on a 7-point scale. It is rated as follows: 1=Normal, not at all ill, 2=Borderline mentally ill, 3=Mildly ill, 4=Moderately ill, 5=Markedly ill, 6=Severely ill, and 7=Among the most extremely ill. Higher scores indicate worsening. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
BaselineChange at Week 96
Risperidone Long-Acting Injection (RLAI)4.62-0.89

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Change From Baseline in World Health Organization (WHO)-Quality of Life (QOL) at Week 96

The WHOQOL-BREF is a 26-item, self-report questionnaire and short version of WHOQOL-100, consisting of 4 domains: physical health (7 items), psychological health (6 items), social relationships (3 items), and environmental health (8 items); it also contains QOL and general health items. Domain scores are scaled in a positive direction (i.e. higher scores denote higher quality of life). The mean score of items within each domain is used to calculate the domain score. Each individual item of the WHOQOL-BREF is scored from 1=not at all to 5=completely on a response scale, which is stipulated as a 5-point ordinal scale. The scores are then transformed linearly to a scale of 0 (the worse quality of life) to 100 (the worse quality of life). (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
BaselineChange at Week 96
Risperidone Long-Acting Injection (RLAI)71.222.06

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Total Drug Induced Extra-Pyramidal Symptoms Scale (DIEPSS) Score

A scale used to assess the extrapyramidal symptoms attributable to antipsychotics. It consists of 9 items (8 to assess individual symptoms and 1 to assess global severity). Each item is assessed from 0 (none, normal) to 4 (severe). The total score is the sum of the 8 item scores, for a total range of 0 (normal) to 32 (severe). The items for the assessment of individual symptoms are classified into 4 categories of parkinsonism, akathisia, dystonia and dyskinesia. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
BaselineWeek 96 (n=12)
Risperidone Long-Acting Injection (RLAI)4.132.50

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Change From Baseline in NCFT: Trail Making Test (TMT)-Time at Week 96

TMT is attention, mental flexibility, visual search, motor function measure test. Test is divided into A and B types. Participants using a pencil or connect numbers in sequence (A-type), in turn, alternating between numbers and letters must be connected (B-type). The test measures the response time. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionSeconds (Mean)
Baseline: Trail A-timeChange at Week 96: Trail A-timeBaseline: Trail B-timeChange at Week 96: Trail B-time
Risperidone Long-Acting Injection (RLAI)39.83-3.1896.03-16.0

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Change From Baseline in NCFT: TMT-Error at Week 96

TMT is attention, mental flexibility, visual search, motor function measure test. Test is divided into A and B types. Participants using a pencil or connect numbers in sequence (A-type), in turn, alternating between numbers and letters must be connected (B-type). The test measures the the number of errors. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionErrors (Mean)
Baseline: Trail A-errorChange at Week 96: Trail A-errorBaseline: Trail B-errorChange at Week 96: Trail B-error
Risperidone Long-Acting Injection (RLAI)0.110.000.68-1.11

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Change From Baseline in Neurocognitive Function Test (NCFT): General Intelligence (Korean-Wechsler Adults Intelligence Scale [K-WAIS]) at Week 96

The K-WAIS is a Korean version of the Wechsler Adult Intelligence Scale-Revised (WAIS-R). It is an intelligence test that assess 3 general areas of intelligence quotients (IQ): verbal IQ, performance IQ and full-scale IQ (FSIQ). The verbal IQ includes: Digit Span, Vocabulary, and Arithmetic; performance IQ includes: Picture Arrangement and Block Design; and FSIQ is an IQ assessed by measuring an individual's overall level of general cognitive and intellectual functioning. The highest FSIQ is 160. The greater the quotient, higher the level of intelligence. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionIntelligence quotient (IQ) (Mean)
Baseline: GI, Digit Span (n=28)Change at Week 96: GI, Digit span (n=28)Baseline: GI, Vocabulary (n=29)Change at Week 96: GI, Vocabulary (n=29)Baseline: GI, Arithmetic (n=29)Change at Week 96: GI, Arithmetic (n=29)Baseline: GI, Picture arrange (n=29)Change at Week 96: GI, Picture arrange (n=29)Baseline: GI, Block Design (n=29)Change at Week 96: GI, Block Design (n=29)Baseline: GI, FSIQ (n=29)Change at Week 96: GI, FSIQ (n=29)
Risperidone Long-Acting Injection (RLAI)11.391.3612.281.1810.001.1810.102.3611.590.82106.0710.64

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Change From Baseline in Total Positive and Negative Syndrome Scale (PANSS) Score at Week 96

The PANSS is a 30-item scale consisting of 3 subscales, the positive subscale (7 items), the negative subscale (7 items), and the general psychopathology subscale (16 items) and it is designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 items are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 (absent) to 210 (extreme ill). Higher scores indicate worsening. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
BaselineChange at Week 96
Risperidone Long-Acting Injection (RLAI)73.0018.24

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Liverpool University Neuroleptic Side Effect Rating Scale (LUNSERS) Score

"The LUNSERS is a self-report measure of antipsychotic side effects. It consists of 51 questions, 41 questions on side effects and 10 questions are of red herrings to validate the results. Each question is rated on a 4-point scale, where 0=not at all; and 4=very much. The total neuroleptic side effect score is the sum of the scores for the side effects items (i.e. all items excluding the red herrings). Total side effects score ranges from 0 to 164, where 0 to 40=low side effect rating, 41 to 80=medium side effect rating and greater than 81=high side effect rating." (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnit on a scale (Mean)
BaselineWeek 96 (n=13)
Risperidone Long-Acting Injection (RLAI)101.3276.54

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Change From Baseline in NCFT: Rey Kim Memory Test- Korean-Rey Complex Figure Test (K-RCFT) at Week 96

The RCFT is a neuropsychological assessment designed to evaluate visual memory in participants. The RCFT is useful in evaluating the spatial perception and visual memory. The RCFT consists of 3 test conditions: Copy, Immediate Recall and Delayed Recall. At the first step, participants are given the RCFT stimulus card, and then asked to draw the same figure. Subsequently, they are instructed to draw what they remembered. Then, after a delay of 30 min, they are required to draw the same figure once again, a score of 2 points for each drawn element (a complete straight line or a circle) remembered correctly. The total score is the sum of points scored for each correctly drawn element and it ranges from 0 to 36. The maximum score indicates excellent visual memory. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionUnits on a scale (Mean)
Baseline: copyChange at Week 96: copyBaseline: immediate recallChange at Week 96: immediate recallBaseline: delayed recallChange at Week 96: delayed recall
Risperidone Long-Acting Injection (RLAI)15.11-0.108.752.209.181.70

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Change From Baseline in NCFT: Rey Kim Memory Test-Korean Auditory Verbal Learning Test (KAVLT) at Week 96

The KAVLT is a neuropsychological assessment designed to evaluate verbal memory in participants. The KAVLT is useful in evaluating the nature and severity of memory dysfunction and to track changes in memory function over time. The test is designed as a list-learning paradigm in which the participants hears a list of 15 words, and are asked to recall as many words from the list as possible. This procedure is carried out a total of 5 times. Then a second list of 15 words is presented, allowing the participants only 1 attempt to recall. Immediately following this, the participants are asked to remember as many words as possible from the first list. KAVLT consists of 2 test conditions: Delayed Recall and Delayed Recognition. The upper limit for 'words recalled' is 15, which represents better episodic memory. (NCT00269919)
Timeframe: Baseline and Week 96

InterventionWords recalled (Mean)
Baseline: Trial 1 (n=27)Change at Week 96: Trial 1 (n=27)Baseline: Trial 2 (n=28)Change at Week 96: Trial 2 (n=28)Baseline: Trial 3 (n=28)Change at Week 96: Trial 3 (n=28)Baseline: Trial 4 (n=28)Change at Week 96: Trial 4 (n=28)Baseline: Trial 5 (n=28)Change at Week 96: Trial 5 (n=28)Baseline: delayed recall (n=28)Change at Week 96: delayed recall (n=28)Baseline: delayed recognition (n=28)Change at Week 96: delayed recognition (n=28)
Risperidone Long-Acting Injection (RLAI)9.812.308.711.607.962.408.390.908.501.508.502.909.211.50

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Time in Remission

Time in remission for an individual subject was defined as the length of time (in days) that the remission criteria were maintained during the trial. Remission was defined as the simultaneous attainment of a score of 3 (mild), 2 (minimal), or 1 (absent) for all the following individual items from Positive and Negative Syndrome Scale (PANSS): delusions (P1), concept disorganization (P2), hallucinatory behavior (P3), unusual thought content (G9), mannerisms and posturing (G5), blunted affect (N1), passive/apathetic social withdrawal (N4), and lack of spontaneity and flow of conversation (N6). (NCT00299702)
Timeframe: Day 1 to last PANSS measurement

Interventiondays (Mean)
Risperdal Consta373.5
Abilify356.7

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Time to Relapse

Time to relapse was defined as the number of days from the date of first dose to the date of relapse, as determined by the Relapse Monitoring Board. (NCT00299702)
Timeframe: Day 1 to relapse

Interventiondays (Median)
Risperdal Consta131
Abilify113

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Percentage of Participants That Responded to Treatment

Brief Psychiatric Rating Scale-Anchored (BPRS-A) 4 items on this scale were examined to determine subjects responder status: Items 4. Conceptual Disorganization 8. Grandiosity 12. Hallucinations and 15. Unusual Thought Content. Scores range from-7 (not assessed) to 7 (very severe) Subjects with scores of 3 or less on all 4 items for 2 consecutive visits are deemed responders, subjects with 4 or greater and any of the aforementioned items for 2 consecutive study visits are non responders. Additionally, the subjects response on the Clinical Global Impressions Scale. A Clinical Global Improvement CGI) rating of much or very much improved on 2 consecutive ratings were deemed a responder. Percentages and confidence intervals were used to report response outcome. Response status was assessed throughout the duration of the study; a participant can be deemed a responder any time between weeks 1-week 12. The possible range for this outcome is a score of 4 to 28 (NCT00320671)
Timeframe: this outcome was assessed throughout the study.

Interventionpercentage of response (Number)
Percentage of Participants That Reposonded to Aripiprazole62.8
Percentage of Participants That Reposonded to Risperidone56.8

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Medication Adherence

5-point scale (1 = best adherence, 5= nonadherent) based on pill counts, MEMS cap readings, plasma assays, and psychiatrist judgments for oral risperidone and timing of injections for long-acting injectable risperidone averaged over study participation (NCT00330551)
Timeframe: Measured weekly throughout study participation, averaged over study participation

Interventionunits on a scale (Mean)
Long-acting Injectable Risperidone1.1
Oral Risperidone1.9

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Number of Participants Who Had an Exacerbation or Relapse of Psychotic Symptoms

Dichotomous measure: Presence of any of three psychotic relapse or exacerbation categories scored from the Brief Psychiatric Rating Scale (BPRS) occurring any time after randomization and until end of study participation (up to 12 mos.). (NCT00330551)
Timeframe: Occurrence after randomization and until end of study participation (up to 12 mos.)

InterventionParticipants (Count of Participants)
Long-acting Injectable Risperidone2
Oral Risperidone14

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Number of Participants Who Returned to Work or School (SAS Work Section)

The Social Adjustment Scale records the return to work or school and the number of weeks in work or school during each 3-month period. For this outcome, outcome as dichotomized as 0 if an individual did not return to work or school and 1 if they did return to competitive work or regular school enrollment. (NCT00330551)
Timeframe: Measured from Baseline to Month 12

InterventionParticipants (Count of Participants)
Long-acting Injectable Risperidone29
Oral Risperidone29

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Retention in Treatment

Number of days on the randomized medication before being switched to a different antipsychotic medication or dropping out of the medication trial. Possible range is 0 to 365, with higher numbers indicating better retention in treatment. (NCT00330551)
Timeframe: From baseline to 12 months

Interventiondays (Mean)
Long-acting Injectable Risperidone307.6
Oral Risperidone270.7

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Number of Weeks Maintaining Work or School (SAS)

Measured as the number of weeks in which a participant has competitive employment or attends regular school courses. Possible range is 0 to 52 weeks. (NCT00330551)
Timeframe: Cumulative total measured from Baseline to Month 12

Interventionweeks (Mean)
Long-acting Injectable Risperidone26.7
Oral Risperidone21.1

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Awareness of Illness, as Assessed by the Scale to Assess Unawareness of Mental Disorder-Revised (SUMD-R)

Rating scale based on clinician's interview of patient to determine level of lack of awareness of having a mental disorder. Range is from 1 (Aware) to 5 (Unaware), so lower scores indicate better outcome. (NCT00330551)
Timeframe: Baseline to 12 months

InterventionChange scores on 5-point rating scale (Mean)
Long-acting Injectable Risperidone.07
Oral Risperidone-.24

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Change in Global Functioning Scale: Role

10-point scale of work/school functioning. Scale range is from 1 (extreme role dysfunction) to 10 (superior role functioning). Measured by subtracting the baseline rating from the rating at 12 months. (NCT00330551)
Timeframe: Measured at Baseline and Month 12

InterventionChanges on a 10-point scale (Mean)
Long-acting Injectable Risperidone1.5
Oral Risperidone1.2

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MATRICS Consensus Cognitive Battery (MCCB) Overall Composite T Score

The MCCB Overall Composite T score is computed by the MCCB Computer Scoring Program from the raw scores for 10 individual cognitive tests. The mean for the general population of comparable age and sex is 50 with a standard deviation of 10. Higher scores indicate better cognitive functioning. The outcome measure was the change from baseline to 12 months, calculated as 12-month T score minus baseline T score. Higher values indicate better outcome. (NCT00330551)
Timeframe: Measured at baseline and 12 months

InterventionChange score: change in T scores (Mean)
Long-acting Injectable Risperidone3.5
Oral Risperidone4.4

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Number of Patients Discontinuing From the Study

(NCT00330863)
Timeframe: Measured throughout study up to 30 months

Interventionparticipants (Number)
Injectable81
Oral80

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Side Effects and Metabolic Measures

The highest severity of each of 24 adverse event (AE) that was assessed.over the 30 month study period. The mean severity on a scale of 1 (none) to 4 very severe symptom was recorded at each biweekly visit. Results for each variable are summarized over time so that each subject has a single mean severity rating for each AE. There is no named scale. Each of the side effects measured is named in ways that are clear to medical readers e.g anorexia. The range is 1 none to 4 very severe. Therefore, a higher scale score is worse. (NCT00330863)
Timeframe: Measured throughout study up to 30 months

,
Interventionunits on a scale (Mean)
Bruising easilyRashUrticaria (hives, itching)Blurred visionsedation/drowsinessRestlessnessInsomniaMalaise (weakness, fatigue)StiffnessTremorDizzinessHeadacheFeverSore ThroatDry MouthHypersalivationEnuresisConstipationDiarrheaAnorexia (loss of appetite)NauseaVomitingMenstrual IrregularityBreast tenderness/galactorrhea
Injectable1.431.531.601.762.342.482.382.222.011.771.821.991.271.642.361.761.631.751.651.891.781.481.621.39
Oral1.481.441.711.912.532.432.362.141.971.751.781.891.241.572.251.841.561.641.681.691.721.511.551.32

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Substantial Clinical Deterioration Measured by Psychotic Symptoms

Brief Psychiatric Rating Scale (BPRS) psychosis cluster. Score range is based on the score range for individual items rather than the factor total because is factors have different numbers of items. Score range is 1 -7 where 1 + no symptomatology and 7 = very severe symptoms. (NCT00330863)
Timeframe: Measured throughout study up to 30 months

Interventionunits on a scale (Least Squares Mean)
Injectable1.8
Oral2.0

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Work Behavior Inventory (WBI) Quality of Work/School Performance

Change in rating on quality of work/school performance based on patient, employer, and/or teacher reports. The Quality of Work rating at baseline was subtracted from the same rating at 12 mos. Higher scores are better outcome. (NCT00333177)
Timeframe: Baseline to 1 year

Interventionscore on a rating scale (Mean)
CT - RLAI-6.5
HBT - RLAI8.8
CT - Oral Ris-3.4
HBT - Oral Ris0.0

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Work/School Functioning (Global Functioning Scale: Role)

Changes in role functioning from baseline to 12 months. Ratings on a 10-point scale with 10 being best. (NCT00333177)
Timeframe: Baseline to 12 months

InterventionChanges on a 10-point scale (Mean)
CT - RLAI2.70
HBT - RLAI1.69
CT - Oral Ris2.43
HBT - Oral Ris0.18

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Work/School Functioning (Global Functioning Scale: Role)

Change in role functioning from baseline to the 6 month point (rated on a scale from 1= Extreme Role Dysfunction to 10 = Superior Role Functioning) is presented here. (NCT00333177)
Timeframe: Baseline to 6 months

InterventionChanges on a 10-point scale (Mean)
CT - RLAI2.90
HBT - RLAI0.92
CT - Oral Ris1.27
HBT - Oral Ris-0.82

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Retention in Treatment

Days after randomization that a participant continued to receive at least the assigned CT or HBT psychosocial treatment. If a participant needed to end the assigned medication condition (RLAI vs. Oral Ris), they continued in the psychosocial treatment so this outcome focused on the days in the assigned psychosocial treatment. Possible range is 1 to 365, with higher being a better outcome. (NCT00333177)
Timeframe: 12 months

Interventiondays (Mean)
CT - RLAI359.7
HBT - RLAI352.2
CT - Oral Ris332.4
HBT - Oral Ris348.3

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Maintenance of Work/School Attendance

Modified Work Section of the Social Adjustment Scale (SAS) was used to calculate the total number of weeks in school or competitive work. Range of possible values is 0 to 52, with higher numbers being better outcome. (NCT00333177)
Timeframe: 12 months

Interventionweeks (Mean)
CT - RLAI35.4
HBT - RLAI24.4
CT - Oral Ris26.7
HBT - Oral Ris12.0

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Exacerbation or Relapse of Psychotic Symptoms

Dichotomous measure: Presence of any of 3 psychotic relapse or exacerbation categories scored from the Brief Psychiatric Rating Scale (BPRS) occurring after randomization and until end of study participation (up to 12 months post baseline). BPRS was administered every two weeks throughout study participation. (NCT00333177)
Timeframe: Occurence after randomization and until end of study participation (up to 12 mos.)

Interventionparticipants (Number)
RLAI2
Oral Ris10

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Change in Motivation for Work/School

The Work Motivation scale is a factor score from the Work Personality Profile. The Work Personality Profile is a set of ratings based on interviewing the participant. Scores at each occasion can range from 8 to 32, with higher indicating better motivation. Scores reported here are changes from baseline to 12 months, which could range from -24 to 24 with higher being better. (NCT00333177)
Timeframe: Baseline to 12 months

Interventionscore on a scale (Mean)
CT - RLAI3.7
HBT - RLAI1.2
CT - Oral Ris-2.4
HBT - Oral Ris-1.9

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Awareness of Illness, as Assessed by the Scale to Assess Unawareness of Mental Disorder, Revised Version (SUMD-R)

Rating scale based on clinician's interview of patient to determine level of lack of awareness of having a mental disorder. Range is from 1 (Aware) to 5 (Unaware), so lower scores indicate better outcome. (NCT00333177)
Timeframe: 12 months after randomization

Interventionscore on a scale (Mean)
CT - RLAI1.25
HBT - RLAI3.29
CT - Oral Ris2.00
HBT - Oral Ris3.75

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Average Medication Non-adherence

5-point scale (1 = best adherence, 5= nonadherent) based on pill counts, Medication Event Monitoring System (MEMS) cap readings, plasma assays, and psychiatrist judgements for oral risperidone and timing of injections for long-acting injectable risperidone. Averaged over medication study participation. (NCT00333177)
Timeframe: Averaged over study participation (up to 12 months)

Interventionunits on a 5-point scale (Mean)
RLAI1.0
Oral Ris1.9

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Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Consensus Cognitive Battery (MCCB)

Values presented here are the changes in MCCB Overall Composite T scores from baseline to 12 months, with higher values representing better outcome. Raw test scores are used to generate T-scores and then the seven MCCB domains are combined to generate an Overall Composite T score. MCCB Overall Composite T scores have a mean in the general population of 50 with a standard deviation of 10. Thus, a positive change of 5 T scores is an improvement of half a standard deviation. (NCT00333177)
Timeframe: Measured at baseline and 12 months

InterventionT scores (Mean)
CT - RLAI6.7
HBT - RLAI0.9
CT - Oral Ris3.9
HBT - Oral Ris5.9

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Mean Change From Baseline to 10 Week Endpoint in Extrapyramidal Symptoms as Measured by the Abnormal Involuntary Movement Scale (AIMS)- Non-Global Total Score

A 12-item instrument assesses observed abnormal movements in different parts of body. Ten items are scored in a 5-point scale (0 = none/normal, 4 = severe) which evaluates abnormal movements in three main anatomic areas (orofacial area, extremities, and trunk). Two items are yes/no questions regarding dentures. Total scores range from 0 to 42. (NCT00337662)
Timeframe: Week 2 to Week 12

Interventionunits on a scale (Mean)
NEO-OLZ-0.38
NEO-RIS0.11
EO-RIS-0.16

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Mean Change From Baseline to 10 Week Endpoint in Extrapyramidal Symptoms as Measured by the Barnes Akathisia Rating Scale - Total Score

Evaluates akathisia associated with use of antipsychotic medications, includes objective and subjective component plus global impression rating for overall disorder. Components rated on scale of 0 to 3 for objective and subjective items and 0 to 5 for global clinical assessment, for total score of 0 (absence of akathisia) to 11 (severe akathisia). (NCT00337662)
Timeframe: Week 2 to Week 12

Interventionunits on a scale (Mean)
NEO-OLZ-0.31
NEO-RIS-0.13
EO-RIS-0.24

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Mean Change From Baseline to 10 Week Endpoint in Extrapyramidal Symptoms as Measured by the Modified Simpson-Angus Scale

Measures neuroleptic-induced parkinsonism. Total score consists of the sum of 10 items: 7 items (items 1, 3, 4, 7, 8, 9, 10) rated on a 4-point severity scale where 0=normal and 4=extreme, and 3 items (items 2, 5, 6) rated on a 2-point severity scale where 0=normal and 2=definitely abnormal/present. The total score ranges from 0 to 34. (NCT00337662)
Timeframe: Week 2 to Week 12

Interventionunits on a scale (Mean)
NEO-OLZ-0.06
NEO-RIS-0.03
EO-RIS-0.02

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Changes From Study Period II Baseline (Week 0) to Weeks 3, 4, 6, 8, and 12 in Positive and Negative Syndrome Scale (PANSS) Total Score in Early Onset Response and Not Early Onset Response-Risperidone Patients

Assesses positive symptoms, negative symptoms, and general psychopathology specifically associated with schizophrenia. Scale consists of 30 items. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). Sum of 30 items is PANSS total score and ranges from 30 to 210. Change = time point - single-blind baseline (Week 0). (NCT00337662)
Timeframe: Weeks 0, 3, 4, 6, 8, 12

,
Interventionunits on a scale (Least Squares Mean)
Change from Week 0 to Week 3Change from Week 0 to Week 4Change from Week 0 to Week 6Change from Week 0 to Week 8Change from Week 0 to Week 12
EO-RIS-30.80-32.53-32.90-34.10-35.09
NEO-RIS-11.90-14.81-16.23-18.10-18.62

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Changes From Study Period III Baseline (Week 2) to Weeks 3, 4, 6, 8, and 12 in Positive and Negative Syndrome Scale Total Score in Not Early Onset Response-Risperidone and Not Early Onset Response-Olanzapine Patients

Assesses positive symptoms, negative symptoms, and general psychopathology specifically associated with schizophrenia. Scale consists of 30 items. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). Sum of 30 items is PANSS total score and ranges from 30 to 210. Change = time point - double-blind baseline (Week 2). (NCT00337662)
Timeframe: Weeks 2, 3, 4, 6, 8, 12

,
Interventionunits on a scale (Least Squares Mean)
Change from Week 2 to Week 3Change from Week 2 to Week 4Change from Week 2 to Week 6Change from Week 2 to Week 8Change from Week 2 to Week 12
NEO-OLZ-5.85-9.67-13.06-14.73-17.02
NEO-RIS-6.94-9.82-11.25-13.13-13.53

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Number of Participants in the Not Early Onset-Risperidone and Not Early Onset-Olanzapine Groups Who Show a 50% or Greater Reduction in Positive and Negative Syndrome Scale Total Score From Baseline or Meet 'a Priori' Specified Criteria for Remission

'a priori' specified criteria for remission defined as a score of 3 (mild), 2 (minimal), or 1 (absent) on all of the following 8 PANSS items: delusions, conceptual disorganization, hallucinatory behavior, unusual thought content, mannerisms and posturing, blunted effect, passive/apathetic withdrawal, lack of spontaneity and flow of conversation. (NCT00337662)
Timeframe: Week 2 to Week 12

,
Interventionparticipants (Number)
>=50% Reduction - Yes>=50% Reduction - No
NEO-OLZ67112
NEO-RIS67122

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Number of Participants With Psychiatric Hospitalizations in the Early Onset and Not Early Onset-Risperidone Groups

Psychiatric Hospitalizations were measured by the Modified Schizophrenia Care and Assessment Program Health Questionnaire (SCAP-HQ) from which it could be determined the number of patients with a psychiatric episode that required an overnight stay in a hospital. (NCT00337662)
Timeframe: Week 2 to Week 12

,
Interventionparticipants (Number)
Required overnight stay in hospital: YesRequired overnight stay in hospital: No
EO-RIS10127
NEO-RIS9175

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Number of Participants With Treatment-Emergent Abnormal Fasting Laboratory Analytes Reported in >=2% of All Participants

Number of participants who experienced abnormal fasting laboratory values at any time during Study Period III. Laboratory reference ranges are dependent on the patient's gender, origin, and age. (NCT00337662)
Timeframe: Week 2 to Week 12

,,
Interventionparticipants (Number)
Low total bilirubinHigh creatine phosphokinaseHigh creatinineHigh hemoglobin A1cLow sodiumHigh prolactin
EO-RIS253247
NEO-OLZ562647
NEO-RIS314748

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The Number of Participants in the Early Onset (EO) and Not Early Onset-Risperidone (NEO-RIS) Groups Who Show a 20% or Greater Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score

The number of participants who experienced a 20% or greater reduction in their PANSS Total score during the 12 weeks they were on risperidone. (NCT00337662)
Timeframe: Week 0 to Week 12

,
Interventionparticipants (Number)
>=20% Reduction - Yes>=20% Reduction - No
EO-RIS11919
NEO-RIS9495

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Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Body Mass Index

Body mass index is an estimate of body fat based on body weight divided by height squared. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 to Week 12

,,
Interventionkilogram per square meter (Mean)
BaselineChange from Baseline
EO-RIS31.130.10
NEO-OLZ29.970.63
NEO-RIS31.050.43

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Vital Signs - Change From Baseline to 10 Week Endpoint in Standing Mean Arterial Pressure

Change from Study Period III baseline to endpoint in standing mean arterial pressure. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 and Week 12

,,
Interventionmm Hg (Mean)
BaselineChange from Baseline
EO-RIS94.60-1.94
NEO-OLZ93.530.68
NEO-RIS93.81-0.58

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Vital Signs - Change From Baseline to 10 Week Endpoint in Standing Diastolic Blood Pressure

Change from Study Period III baseline to endpoint in standing blood pressure. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 and Week 12

,,
Interventionmm Hg (Mean)
BaselineChange from Baseline
EO-RIS80.29-1.73
NEO-OLZ78.691.01
NEO-RIS78.57-0.20

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The Number of Participants in the Not Early Onset-Risperidone (NEO-RIS) and Not Early Onset-Olanzapine (NEO-OLZ) Groups Who Show a 20% or Greater Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score

The number of not early onset participants who experienced a 20% or greater reduction in PANSS Total Score at any time during the 12 weeks of combined Study Period II and Study Period III. (NCT00337662)
Timeframe: Week 0 to Week 12

,
Interventionparticipants (Number)
>=20% Reduction - Yes>=20% Reduction - No
NEO-OLZ9485
NEO-RIS9495

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Number of Participants in the Early Onset and Not Early Onset-Risperidone Groups Who Show a 50% or Greater Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Baseline or Meet 'a Priori' Specified Criteria for Remission

'a priori' specified criteria for remission defined as a score of 3 (mild), 2 (minimal), or 1 (absent) on all of the following 8 PANSS items: delusions, conceptual disorganization, hallucinatory behavior, unusual thought content, mannerisms and posturing, blunted effect, passive/apathetic withdrawal, lack of spontaneity and flow of conversation. (NCT00337662)
Timeframe: Week 0 to Week 12

,
Interventionparticipants (Number)
>=50% Reduction - Yes>=50% Reduction - No
EO-RIS8751
NEO-RIS67122

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Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Body Weight

Change from Study Period III baseline to endpoint in body weight. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 and Week 12

,,
Interventionkilograms (Mean)
BaselineChange from Baseline
EO-RIS90.670.30
NEO-OLZ88.281.85
NEO-RIS90.251.29

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Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Standing Systolic Blood Pressure

Change from Study Period III baseline to endpoint in standing systolic blood pressure. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 and Week 12

,,
Interventionmm Hg (Mean)
BaselineChange from Baseline
EO-RIS123.20-2.36
NEO-OLZ123.200.01
NEO-RIS124.30-1.35

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Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Standing Pulse Rate

Change from Study Period III baseline to endpoint in standing pulse rate. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 and Week 12

,,
Interventionbeats per minute (Mean)
BaselineChange from Baseline
EO-RIS82.39-0.56
NEO-OLZ85.57-1.13
NEO-RIS85.32-2.05

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Vital Signs - Mean Change From Baseline to 10 Week Endpoint in Sitting Pulse Rate

Changes from Study Period III baseline to endpoint in sitting pulse rate. Change = Endpoint minus baseline. (NCT00337662)
Timeframe: Week 2 and Week 12

,,
Interventionbeats per minute (Mean)
BaselineChange from Baseline
EO-RIS77.90-0.94
NEO-OLZ80.49-0.98
NEO-RIS80.84-2.52

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Change in Visceral Fat Mass From Baseline to Week 26

CT measured change in visceral fat mass from baseline to week 26 (mm^3) (NCT00338949)
Timeframe: Baseline and Week 26

Interventionmm^3 (Mean)
Control315
Switch392

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Change in Insulin Sensitivity Index From Baseline to Week 26 ((1/mU/L) x 1/Min)

As measured by frequently sampled intravenous glucose tolerance testing (units: 1/mU/L) x 1/Min) (NCT00338949)
Timeframe: Measured at Baseline and Week 26

Intervention(1/mU/L) x 1/Min (Mean)
Control0.072
Switch0.407

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Cocaine Craving

The University of Minnesota Cocaine Craving Scale was performed to assess cocaine craving. The scale contains 1 continuous scale for intensity and 2 categorical scales for frequency and duration of craving episodes. The continuous scale for craving intensity ranges from 0 (no craving at all in the past week) to 10 (a great deal of craving in the past week) (NCT00385801)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
PlaceboNA
RisperidoneNA

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Cocaine Use by Quantitative Urine Samples

After randomization, participants provided urine samples every week for the first 3 weeks and then every 2 weeks for 8 weeks, up to 7 samples per participant. The average visits with cocaine negative urine samples per participant are reported below (NCT00385801)
Timeframe: 12 weeks

Interventionvisit with negative UBE (Mean)
Placebo1.81
Risperidone Consta0.87

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Score on the Yale-Brown Obsessive Compulsive Scale (Y-BOCS)

Y-BOCS ranges from 0-40, with 0 meaning no symptoms and higher numbers meaning greater symptom severity (NCT00389493)
Timeframe: Week 0 and Week 8

,,
Interventionunits on a scale (Mean)
Y-BOCS score at Week 0Y-BOCS score at Week 8
Treatment With Exposure/Response Prevention27.213.0
Treatment With Pill Placebo25.923.1
Treatment With Risperidone26.122.6

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Quality of Life Enjoyment and Satisfaction Questionnaire-Short Form

QLESQ ranges from 14-70, with higher scores meaning more enjoyment and satisfaction with quality of life (NCT00389493)
Timeframe: Week 0 and Week 8

,,
Interventionunits on a scale (Mean)
QLESQ-SF Week 0QLESQ-SF Week 8
Treatment With Exposure/Response Prevention57.870.2
Treatment With Pill Placebo56.162.6
Treatment With Risperidone52.355.1

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Social Adjustment Scale-SR

SAS-SR yields a mean score between 1 and 5; the higher the score, the more severe the social adjustment problems (NCT00389493)
Timeframe: Week 0 and Week 8

,,
Interventionunits on a scale (Mean)
SAS-SR at Week 0SAS-SR at Week 8
Treatment With Exposure/Response Prevention2.31.9
Treatment With Pill Placebo2.22.1
Treatment With Risperidone2.32.2

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Brown Assessment of Beliefs (BABS)

"Scale ranges from 0 to 24 where 0 is beliefs are false and 24 is convinced beliefs = reality" (NCT00389493)
Timeframe: Week 0 and Week 8

,,
Interventionunits on a scale (Mean)
Week 0Week 8
Treatment With Exposure/Response Prevention6.12.4
Treatment With Pill Placebo5.34.3
Treatment With Risperidone5.74.5

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Hamilton Depression Rating Scale (Ham-D)

Ham-D ranges from 0=no symptoms to 52 with higher numbers indicating more severe depression (NCT00389493)
Timeframe: Week 0 and Week 8

,,
Interventionunits on a scale (Mean)
Ham-D at Week 0Ham-D at Week 8
Treatment With Exposure/Response Prevention7.87.8
Treatment With Pill Placebo7.77.7
Treatment With Risperidone9.88.0

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Time to Early Study Discontinuation for Any Reason

The robustness of the primary outcome analysis was tested by means of a sensitivity analysis: patients who discontinued the study during Period III for any reason were analyzed as having a recurrence of a mood episode at the time of their study discontinuation. The same survival analysis method as for the primary outcome was applied. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventiondays (Mean)
Risperidone LAI252.45
Placebo236.14
Olanzapine365.64

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Change From Double-blind Baseline to Endpoint in Young Mania Rating Scale (YMRS)

The 11-item YMRS was administered by an adequately trained clinician who did not provide psychotherapy or psycho-education to the patient. A severity rating was assigned to each of the items, based on the patient's subjective report of his or her condition over the previous 7 days or since the last visit (whichever was shorter) and the clinician's behavioral observations during the interview, with emphasis on the latter. The total YMRS score included the score of all 11 items ranging from 0 to 60, a higher score indicating a more severe condition. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventionunits on a scale (Mean)
Risperidone LAI2.9
Placebo8.0
Olanzapine1.7

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Change From Double-blind Baseline to Endpoint in Montgomery Åsberg Depression Rating Scale (MADRS)

The MADRS was assessed by an adequately trained clinician who did not provide psychotherapy or psycho-education to the patient. The scale consists of 10 items that cover all of the core depressive symptoms. Each item is scored from 0 to 6 and a total score is calculated by adding the scores of all 10 items. For each individual item as well as for the total score, a higher score represents a more severe condition. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventionunits on a scale (Mean)
Risperidone LAI5.1
Placebo6.1
Olanzapine2.0

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Time to Recurrence of an Elevated Mood (Hypomanic, Manic, or Mixed) Episode

Recurrences were classified as elevated mood or depressive by the investigator based on the patient's data at the time of the event. Time to recurrence of an elevated mood episode was estimated by means of the same survival analysis method as for the primary outcome. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventiondays (Mean)
Risperidone LAI357.41
Placebo323.14
Olanzapine448.03

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Time to Recurrence of a Mood Episode (Risperidone LAI Versus Placebo)

Recurrence was estimated using the Kaplan-Meier method and defined as meeting any of the following: DSM-IV-TR criteria for a hypomanic, manic, mixed, or depressive episode; in need of mood stabilizer, antipsychotic medication, benzodiazepine or antidepressant; requiring hospitalization for mood episode; either Young Mania Rating Scale (YMRS) >12 or Montgomery-Åsberg Depression Rating Scale (MADRS) >12 combined with Clinical Global Impression - Severity (CGI-S) >=4; in need of increase in study medication dose or supplementation with oral risperidone or another antipsychotic or mood stabilizer. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventiondays (Mean)
Risperidone LAI293.39
Placebo270.47

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Time to Recurrence of a Mood Episode (Exploratory/Olanzapine)

Recurrence was defined as for the risperidone LAI and placebo arms (meeting any of 5 criteria). Since the study was designed to compare the efficacy of risperidone LAI versus placebo, this olanzapine analysis was exploratory in nature. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventiondays (Mean)
Olanzapine414.04

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Time to Recurrence of a Depressive Episode

Recurrences were classified as elevated mood or depressive by the investigator based on the patient's data at the time of the event. Time to recurrence of a depressive episode was estimated by means of the same survival analysis method as for the primary outcome. (NCT00391222)
Timeframe: Assessed at every visit from the moment of randomization to a treatment arm (baseline Period III) until the end of treatment (Month 21 or earlier)

Interventiondays (Mean)
Risperidone LAI213.86
Placebo300.20
Olanzapine356.11

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AIMS

The Abnormal Involuntary Movement Scale (AIMS) assesses signs of tardive dyskinesia, a movement disorder that can occur with prolonged use of antipsychotic medication. The AIMS score ranges from 0 to 35, with higher scores indicating more severe symptoms. For each subject, the change in AIMS score between week 16 and randomization was calculated by subtraction, so that a positive value indicates an increase in AIMS over time. (NCT00417482)
Timeframe: Phase B, weeks 1-16 (study weeks 16-32)

Interventionunits on a scale (Mean)
Placebo0.03
Risperidone0.24

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Mini Mental State Exam (MMSE)

The MMSE assesses cognition. Scores range from 0-30, with higher scores indicating better cognition. For each subject, the change in MMSE between week 16 and baseline (randomization) was calculated by subtraction, so that a positive value indicates an increase in MMSE over time. (NCT00417482)
Timeframe: Phase B, weeks 1-16 (study weeks 16-32)

Interventionunits on a scale (Mean)
Placebo-0.13
Risperidone-0.77

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Weight

For each subject, the change in weight in pounds between week 16 and randomization was calculated by subtraction, so that a positive value indicates an increase in weight over time. (NCT00417482)
Timeframe: Phase B, weeks 1-16 (study weeks 16-32)

Interventionpounds (Mean)
Placebo0.32
Risperidone0.73

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Treatment Emergent Symptoms Scale (TESS)

The Treatment Emergent Symptom Scale (TESS) assesses 26 somatic symptoms. Total scores range from 0-26, with a score of 0 or 1 for each item. Higher scores indicate more somatic symptoms. For each subject, the change in TESS between week 16 and baseline (randomization) was calculated by subtraction, so that a positive value indicates an increase in TESS over time. (NCT00417482)
Timeframe: Phase B, weeks 1-16 (study weeks 16-32)

Interventionunits on a scale (Mean)
Placebo0.18
Risperidone0.21

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Relapse by Study Week 48

Same definition and criteria as the primary outcome (NCT00417482)
Timeframe: 16-32 weeks in Phase B (32-48 weeks in study)

Interventionparticipants (Number)
Arm 1: Risperidone - Risperidone2
Arm 2: Risperidone - Placebo13

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Relapse by Study Week 32

"A relapse occurred in Phase B (post-randomization) if both of the following criteria were met:~Increase in the Neuropsychiatric Inventory (NPI) core score of 30% or more OR a 5-point increase from the baseline NPI score at the end of Phase A~A score of 6 (much worse) or 7 (very much worse) on the Clinical Global Impression-Change (CGI-C) at any visit." (NCT00417482)
Timeframe: 0-16 weeks in Phase B (16-32 weeks in study)

Interventionparticipants (Number)
Phase B Arm 1: Risperidone-Risperidone15
Phase B Arm 2: Risperidone -Placebo8
Phase B Arm 3: Placebo-Placebo24

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Physical Self-Maintenance Scale (PSMS)

Physical Self-Maintenance Scale, which ranges from 1 to 30, with higher scores indicating WORSE functioning. For each subject, the change in PSMS between week 16 and randomization was calculated by subtraction, so that a positive value indicates an increase in PSMS (worse functioning) over time. (NCT00417482)
Timeframe: Phase B, weeks 1-16 (study weeks 16-32)

Interventionunits on a scale (Mean)
Placebo0.18
Risperidone0.80

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Extrapyramidal Signs (EPS)

Extrapyramidal signs, also known as Parkinsonian signs, refer to signs of tremor, rigidity, and bradykinesia (slowed movement) that are seen in Parkinson's disease. Assessment of extrapyramidal signs (EPS) were made with the use of the Simpson-Angus scale (which ranges from 1-40) with higher scores indicating more extrapyramidal signs. For each subject, the change in EPS between week 16 and baseline (randomization) was calculated by subtraction, so that a positive value indicates an increase in EPS over time. (NCT00417482)
Timeframe: Phase B, weeks 1-16 (study weeks 16-32)

Interventionunits on a scale (Mean)
Placebo-0.20
Risperidone0.34

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Efficacy Failure, Defined as Psychiatric Hospitalization, a 25 Percent Increase From Baseline on the Positive and Negative Syndrome Scale or Substantial Clinical Deterioration on the Clinical Global Impressions-Change (CGI-C)

(NCT00423878)
Timeframe: Measured at Month 6

Interventionparticipants (Number)
Switch Group22
Stay Group18

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Change in Non-HDL Cholesterol Level for Patients Assigned to Stay and Patients Assigned to Switch Over 24 Weeks

Change in non-HDL cholesterol measured at baseline and every 4 weeks for 24 weeks. The efficacy analysis corresponded to a comparison of change in non-HDL cholesterol from baseline to 24 weeks between treatment groups (stay versus switch). Repeated measurements mixed effects linear models were fit for the primary analysis. (NCT00423878)
Timeframe: 24 weeks

Interventionmg/dL non-HDL cholesterol (Least Squares Mean)
Switch Group-20.2
Stay Group-10.8

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Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Cognition Domains

"The following 8 scales are combined into a single index that is normalized with a mean score of 100 and a standard deviation of 10. Higher scores are considered better cognitive performance. No subscales scores are reported and a final standardized score is reported as the average of the standardized scores on each of these scales. Here is the listing of component scales that were translated into Chinese and used for this study:~Brief Assessment of Cognition in Schizophrenia (BACS): Symbol-Coding Trail Making Test: Part A Attention/Vigilance Continuous Performance Test-Identical Pairs (CPT-IP)* Wechsler Memory Scale®-3rd Ed. (WMS®-III): Spatial Span + Letter-Number Span Hopkins Verbal Learning Test-Revised™ (HVLT-R™) Brief Visuospatial Memory Test-Revised (BVMT-R™) Neuropsychological Assessment Battery® (NAB®): Mazes~Mayer-Salovey-Caruso Emotional Intelligence Test (MSCEIT™):" (NCT00435370)
Timeframe: end of 12 wk treatment

Interventionunits on a scale (Mean)
Tropisetron96
Placebo95

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Total Plasmalogen Levels in the Lipid Profile

Plasmalogens are a subclass of glycerophospholipids and ubiquitous constituents of cellular membranes and serum lipoproteins. Several neurological disorders show decreased level of plasmalogens. (NCT00466310)
Timeframe: Baseline

Interventionnmoles/gram (Mean)
First Episode Schizophrenics57.65
Recurrent Episode Schizophrenics59.57
Healthy Volunteers75

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Number of Participants Remaining on Metabolic Syndrome at Week 16

Metabolic syndrome is defined as the presence of at least 3 out of the following Adult Treatment Panel III-A (ATP III-A) criteria (all of which are to be assessed at the same visit): waist >102 cm in males, >88 cm in females; blood pressure (BP) systolic BP ≥130 or diastolic BP ≥85 mm Hg; fasting HDL <40 mg/dL in males, <50 mg/dL in females; fasting triglycerides ≥150 mg/dL; fasting glucose ≥100 mg/dL, and/or the start of a treatment for any of the parameters of metabolic syndrome during the course of the study. (NCT00508157)
Timeframe: Week 16

Interventionparticipants (Number)
Control Group22
Aripiprazole16

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Mean Percent Change From Baseline in Fasting Non-high Density Lipoprotein (HDL) Cholesterol at Week 16

Non-HDL cholesterol was calculated as fasting Total Cholesterol minus fasting HDL Cholesterol. (NCT00508157)
Timeframe: Baseline, Week 16

Interventionpercent change (Mean)
Control Group10.06
Aripiprazole-2.3

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Negative Symptoms Measured on Positive and Negative Syndrome Scale (PANSS)

The score for each subject was the sum of the ratings for five items on the negative-symptom subscale of the PANSS: 1) blunted affect, 2) emotional withdrawal, 3) poor rapport, 4) passive/apathetic social withdrawal, and 5) lack of spontaneity and flow of conversation. Each item (symptom) is rated on a scale from 1 = absence of negative symptom to 7 = extreme negative symptom. The sum of the ratings for the five items range from 5 to 35, with higher scores indicating more severe symptoms. The primary outcome measure is the mean of the sum of these ratings across subjects. (NCT00509067)
Timeframe: Measured at Baseline and Weeks 4, 8, 12, and 16

,
Interventionunits on a scale (Mean)
BaselineWeek 4Week 8Week 12Week 16
Galantamine/CDP Choline17.6317.0613.9314.9313.93
Placebos for Galantamine/CDP Choline18.2917.0817.2617.3216.05

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MATRICS Verbal Learning and Memory

The measure of verbal learning and memory is the Hopkins Verbal Learning Test. The score for each subject is the sum of the total number of words recalled correctly for Trials 1, 2, and 3. The measure is the mean of these scores at baseline, Week 8, and Week 16. (NCT00509067)
Timeframe: Measured at Baseline and Weeks 8 and 16

,
Interventionraw scores (Mean)
BaselineWeek 8Week 16
Galantamine and CDP-choline Group20.521.823.0
Placebo Group20.621.220.4

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Clinical Global Impression

The score for each subject was the mean rating on the severity item. The score of the item ranged from 1 (normal) to 7 (among most severely ill). (NCT00509067)
Timeframe: Measured at Baseline and Weeks 4, 8, 12, and 16

,
Interventionunits on a scale (Mean)
BaselineWeek 4Week 8Week 12Week 16
Galantamine and CDP-choline Group4.3243.673.873.8
Placebo Group4.383.924.0443.68

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Clamp Derived Insulin Sensitivity (mg/kg/Min)

This study hypothesized that antipsychotic treatment would decrease insulin sensitivity, with larger adverse effects for olanzapine. Insulin sensitivity describes how sensitive the body is to the effects of insulin. (NCT00515723)
Timeframe: The relevant time points include baseline and week 12.

,,,,
Interventionmg/kg/min (Mean)
BaselineWeek 12
Olanzapine4.393.62
Quetiapine5.285.08
Risperidone5.535.01
Total4.824.50
Ziprasidone4.334.45

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DEXA Total Fat

This study hypothesized that antipsychotic treatment would increase total body fat, as measured by whole body dual energy x-ray absorptiometry (DEXA), with larger adverse effects for olanzapine. (NCT00515723)
Timeframe: The relevant time points include baseline, week 6 and week 12.

,,,,
Interventionkilograms of body fat (Mean)
Baseline6 Weeks12 Weeks
Olanzapine32.2434.3835.45
Quetiapine28.8329.6030.10
Risperidone27.6628.2929.23
Total30.2531.0531.52
Ziprasidone31.6031.1830.66

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Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to the Week 6 Endpoint.

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Change from Baseline in MSQ Score at Week 6 Last Observation Carried Forward (LOCF)

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation2.5
PALI ER Delayed Initiation2.3
Overall2.4

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Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to Week 2 (Observed).

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Change from Baseline in MSQ Score at Week 2

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation2.0
PALI ER Delayed Initiation1.6
Overall1.8

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Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to Week 4 (Observed).

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Change from Baseline in MSQ Score at Week 4

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation2.4
PALI ER Delayed Initiation2.1
Overall2.3

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Medication Satisfaction Questionnaire (MSQ) Score Change From Baseline to Week 6 (Observed).

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Change from Baseline in MSQ Score at Week 6

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation2.5
PALI ER Delayed Initiation2.4
Overall2.5

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Modified COVI Anxiety Scale (m-COVI) Change From Baseline to the Week 6 Endpoint

The standard COVI Anxiety Scale is an investigator-assessed measure of the severity of anxiety symptoms on 4 items: verbal report, behavior, somatic symptoms, and relationship to study drug. Each dimension is assessed in 5 to 10 minutes using a 5-point scale as follows: 1=Not at all, 2=Somewhat, 3=Moderately, 4=Considerably, to 5=Very much. For this study, the standard COVI Anxiety Scale was modified to improve psychometric properties by incorporating anchor points for symptom severity, frequency, and duration and for functional impairment. Worst value is 20 and best value is 4. (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation-1.4
PALI ER Delayed Initiation-1.3
Overall-1.3

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Pittsburgh Sleep Quality Index (PSQI) Change From Baseline to the Week 6 Endpoint

The PSQI is a 2-part questionnaire that assesses sleep quality and disturbances in seven domains: subjective sleep quality, sleep latency, sleep duration, habitual sleep efficiency, sleep disturbances, use of sleep medication, and daytime dysfunction. Each domain is rated on a 4-point scale as follows: 0=Not during the past month, 1=Less than once a week, 2=Once or twice a week, 3=Three or more times a week. Total scores range from zero to 21; increasing scores indicate poorer sleep quality and total scores greater than 5 suggest significant sleep disturbance. (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation-2.3
PALI ER Delayed Initiation-2.2
Overall-2.3

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Positive and Negative Syndrome Scale (PANSS) Total Score Change From Baseline to Week 6 Endpoint

The PANSS is a 30-item scale designed to capture numerous symptoms of schizophrenia, including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale as follows: 1=Absent, 2=Minimal, 3=Mild,4=Moderate, 5=Moderate Severe, 6=Severe, 7=Extreme. This scale has been shown to be sensitive to changes associated with medication treatment. In addition to a total score, this assessment yields separate scores along a Positive Syndrome, a Negative Syndrome, and a General Psychopathology Scales. Worst value is 210, best value is 30. (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation-13.5
PALI ER Delayed Initiation-12.3
Overall-12.9

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Short Form-36 Health Survey (SF-36) Mental Health Composite Score Change From Baseline to the Week 6 Endpoint

The SF-36 is a well-validated and widely used quality-of-life instrument employed in numerous disease states, including schizophrenia. It is a self-administered survey that measures eight domains of health including: physical functioning, role limitations due to physical health (role-physical), bodily pain, general health perceptions, vitality, social functioning, role limitations due to emotional problems (role-emotional) and general mental health. Scoring of the SF-36 was based on the SF-36 Manual and Interpretation Guide. Worst value is 0 and best value is 100. (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionScores on a scale (Mean)
PALI ER Immediate Initiation6.7
PALI ER Delayed Initiation7.2
Overall7.0

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Short Form-36 Health Survey (SF-36) Physical Health Composite Score Change From Baseline to the Week 6 Endpoint

The SF-36 is a well-validated and widely used quality-of-life instrument employed in numerous disease states, including schizophrenia. It is a self-administered survey that measures eight domains of health including: physical functioning, role limitations due to physical health (role-physical), bodily pain, general health perceptions, vitality, social functioning, role limitations due to emotional problems (role-emotional) and general mental health. Scoring of the SF-36 was based on the SF-36 Manual and Interpretation Guide. Worst value is 0 and best value is 100. (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionScores on a scale (Mean)
PALI ER Immediate Initiation0.8
PALI ER Delayed Initiation2.1
Overall1.5

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Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 2 (Observed).

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Week 2

,,
InterventionParticipants (Number)
Satisfied (score 5-7)Dissatisfied (score 1-4)
Overall10682
PALI ER Delayed Initiation4352
PALI ER Immediate Initiation6330

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Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 4 (Observed).

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Week 4

,,
InterventionParticipants (Number)
Satisfied (score 5-7)Dissatisfied (score 1-4)
Overall13941
PALI ER Delayed Initiation6427
PALI ER Immediate Initiation7514

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Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 6 (Observed).

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Week 6

,,
InterventionParticipants (Number)
Satisfied (score 5-7)Dissatisfied (score 1-4)
Overall14824
PALI ER Delayed Initiation7116
PALI ER Immediate Initiation778

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Medication Satisfaction Questionnaire (MSQ) - Categorical Summary - Dichotomized Categories - Week 6 LOCF.

The MSQ is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). (NCT00535132)
Timeframe: Week 6 LOCF

,,
InterventionParticipants (Number)
Satisfied (score 5-7)Dissatisfied (score 1-4)
Overall15833
PALI ER Delayed Initiation7521
PALI ER Immediate Initiation8312

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Treatment Satisfaction Questionnaire for Medication (TSQM) Global Satisfaction Score Change From Baseline to the Week 6 Endpoint

"The TSQM is a 14-item subject-assessed evaluation of treatment medication including 4 factors, Effectiveness (items 1-3), Side Effects (items 4-8), Convenience (items 9-11)and Global Satisfaction (items 12-14). Item 14 states taking all things into account, how satisfied or dissatisfied are you with this medication? and utilizes the following responses on a 7-point Likert scale: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 0 and best value is 100." (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation30.2
PALI ER Delayed Initiation26.4
Overall28.3

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Clinical Global Impression - Severity (CGI-S) Change From Baseline to Week 6 Endpoint

"The CGI-S rating scale is a 7 point global assessment that measures the clinician's impression of the severity of illness exhibited by a subject. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill subjects. Worst value is 7 and best value is 1." (NCT00535132)
Timeframe: Change from Baseline to Week 6 LOCF

InterventionPoints on a scale (Mean)
PALI ER Immediate Initiation-0.8
PALI ER Delayed Initiation-0.8
Overall-0.8

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Positive and Negative Symptom Scale (PANSS) Total Score at Baseline

PANSS assesses the positive symptoms, negative symptoms, and general psychopathology specifically associated with schizophrenia. The scale consists of 30 items. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). The sum of the 30 items is defined as the PANSS total score and ranges from 30 to 210; higher score indicates greater severity. (NCT00563706)
Timeframe: Baseline

Interventionunits on a scale (Mean)
Placebo94.74
Vabicaserin 50 mg94.24
Vabicaserin 100 mg96.88
Vabicaserin 150 mg101.33
Vabicaserin 200 mg93.06
Vabicaserin 300 mg94.39
Vabicaserin 400 mg92.83
Vabicaserin 600 mg95.54
Risperidone91.43

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Change From Baseline in Positive and Negative Symptom Scale (PANSS) Total Score at Day 28

PANSS assesses the positive symptoms, negative symptoms, and general psychopathology specifically associated with schizophrenia. The scale consists of 30 items. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). The sum of the 30 items is defined as the PANSS total score and ranges from 30 to 210; higher score indicates greater severity. (NCT00563706)
Timeframe: Baseline, Day 28

Interventionunits on a scale (Least Squares Mean)
Placebo-17.03
Vabicaserin 50 mg-4.72
Vabicaserin 100 mg-10.26
Vabicaserin 150 mg-5.41
Vabicaserin 200 mg-13.42
Vabicaserin 300 mg-6.13
Vabicaserin 400 mg-13.84
Vabicaserin 600 mg-7.30
Risperidone-15.59

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Number of Participants Demonstrating Improvement in Psychiatric Symptoms Using the BPRS, CGIS, and SANS at 24 Weeks

"Based on the small sample size, it was not possible to test the differences between the two groups for statistical significance. Data on psychiatric symptoms were gathered using Brief Psychiatric Rating Scale (BPRS; weekly), Clinical Global Impressions Scale (CGIS; weekly) and Schedule for the Assessment of Negative Symptoms (SANS; bi-weekly). At the end of the study, graphs were plotted showing severity of symptoms and rated as Improved, Unchanged, or Worse by a pair of expert judges. Raters were instructed to rate the graph Improved or Worsened if it appeared to be >20% better or worse and to rate it Unchanged if there was little or no change (less than ~20%)." (NCT00573287)
Timeframe: 24 weeks

,
Interventionparticipants (Number)
BPRSSANSCGIS
Clozapine441
Risperidone322

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Number of Participants Demonstrating Improvement in Substance Use

"Based on the small sample size, it was not possible to test the differences between the two groups for statistical significance. Data on cannabis use were gathered weekly using the Timeline Follow-back (TLFB) method. At the end of the study, graphs were plotted showing days of cannabis use per week and rated as Improved, Unchanged, or Worse by a pair of expert judges. Raters were instructed to rate the graph Improved or Worsened if it appeared to be >20% better or worse and to rate it Unchanged if there was little or no change (less than ~20%)." (NCT00573287)
Timeframe: 24 weeks

Interventionparticipants (Number)
Clozapine3
Risperidone3

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Change in Clinical Global Impression Severity (CGI-S)

"Investigator evaluation of severity of illness and functional impairment on a 7-point scale (1=not ill, 2=very mild, 3=mild, 4=moderate, 5=marked, 6=severe, 7=extremely severe)." (NCT00576732)
Timeframe: Baseline and 6 weeks

Interventionunits on a scale (Mean)
Placebo-0.3
Risperidone Low Dose-0.4
Risperidone High Dose-1.0

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Change in Aberrant Behavior Checklist Irritability (ABC-I) Subscale

Measure of irritability symptoms of autism. Score range 0 to 45 (lower score = lesser severity). (NCT00576732)
Timeframe: Baseline and 6 weeks

Interventionunits on a scale (Mean)
Placebo-3.5
Risperidone Low Dose-7.4
Risperidone High Dose-12.4

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Change in Insulin Resistance (IR) at 6 Weeks

Insulin resistance calculated using the homeostatic model assessment 1 (HOMA1)formula: fasting glucose (mmol/L) times fasting insulin (uU/L) divided by 22.5. HOMA-IR is a widely used clinical tool for estimating insulin resistance based upon the balance between glucose output and insulin secretion. Normal values should be close to 1, while an increase indicates a decrease in insulin sensitivity (or increase in insulin resistance), a potential predictor for the development of Type 2 Diabetes Mellitus. (NCT00576732)
Timeframe: Baseline and 6 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo0.36
Risperidone Low Dose-0.10
Risperidone High Dose0.45

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Change in Fasting Glucose (mg/dL) at 6 Weeks

(NCT00576732)
Timeframe: Baseline and 6 weeks

Interventionmg/dL (Mean)
Placebo-0.4
Risperidone Low Dose-0.1
Risperidone High Dose-0.3

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Change in Fasting Glucose (mg/dL) at 6 Months

(NCT00576732)
Timeframe: Baseline and 6 months

Interventionmg/dL (Mean)
Placebo/RIS4.0
Ris Low Dose/RIS3.5
Ris High Dose/RIS2.3

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Change in Insulin Resistance (IR) at 6 Months

Insulin resistance calculated using the homeostatic model assessment 1 (HOMA1) formula: fasting glucose (mmol/L) times fasting insulin (uU/L) divided by 22.5. HOMA-IR is a widely used clinical tool for estimating insulin resistance based upon the balance between glucose output and insulin secretion. Normal values should be close to 1, while an increase indicates a decrease in insulin sensitivity (or increase in insulin resistance), a potential predictor for the development of Type 2 Diabetes Mellitus. (NCT00576732)
Timeframe: Baseline and 6 months

Interventionunits on a scale (Mean)
Placebo/RIS0.09
Ris Low Dose/RIS0.36
Ris High Dose/RIS0.75

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Number of Participants Who Had at Least 25% Improvement in ABC-I

ABC-I is a measure of irritability symptoms of autism with score range 0 to 45 (lower score = lesser severity). (NCT00576732)
Timeframe: 6 weeks

Interventionparticipants (Number)
Placebo14
Risperidone Low Dose15
Risperidone High Dose24

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Number of Participants Who Had Clinical Global Impression Change Ratings of Much or Very Much Improved.

"Investigator impression of change over time from double-blind baseline on a 7-point scale (1=very much improved, 2=much improved, 3=minimally improved, 4=no change, 5=minimally worse, 6=much worse, 7=very much worse)." (NCT00576732)
Timeframe: 6 weeks

Interventionparticipants (Number)
Placebo5
Risperidone Low Dose5
Risperidone High Dose19

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Exon Expression Positively or Negatively Correlated With Percentage Improvement in ABC-I

"Affymetrix GeneChip Human Exon 1.0 ST Arrays (Affymetrix, Santa Clara, CA, USA) were used to obtain gene expression values. Raw data (Affymetrix.CEL files) was imported into Partek Genomics Suite 6.4 (Partek, St Louis, MO, USA). Probe summarization and probe set normalization were performed using robust multichip average, which included background correction, quantile normalization, log2 transformation and median polish probe set summarization.~Exons in genes correlated with percentage improvement on the Aberrant Behavior Checklist Irritability subscale were identified." (NCT00584701)
Timeframe: Baseline, 8 Weeks

InterventionNumber of Correlated Genes (Number)
Risperidone5

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Percent Change of ABC - Irritability Subscale Score

"Aberrant Behavior Checklist-Irritability (ABC-I)subscale: measure of assessing changes in symptoms of irritability in children with autism (survey that was normed on a developmentally delayed population of children and adults and is usually completed by a parent or caregiver. There are 45 items that are rated on a 4-point scale from no problem to major problem. ABC-I scores ranges from 0 (best) to 45 (worst). A negative change signifies improvement.~We measured percent change of ABC-I scores from 8 weeks after risperidone treatment compared to baseline." (NCT00584701)
Timeframe: Baseline, 8 weeks

Interventionpercent change in scores (Mean)
Active Risperidone-44.5

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The Change From Baseline in the PSP Score

The PSP scale is used to assess the degree of dysfunction a patient exhibits over a 7-day period within 4 domains of behavior: socially useful activities, personal and social relationships, self-care, and disturbing and aggressive behavior. The results of the assessment are converted to a numeric score. A score between 71 and 100 indicates a mild degree of difficulty; a score between 31 and 70 indicates a moderate degree of dysfunction, and a patient with a score of 30 or less has functioning so poor he or she requires intensive supervision. (NCT00589914)
Timeframe: Baseline to the last postrandomization assessment in the double-blind treatment period (approximately 13 weeks)

InterventionScores on a scale (Mean)
R0926708.5
RISPERDAL CONSTA8.8

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Change in the Positive and Negative Syndrome Scale (PANSS) Total Score for Schizophrenia

The PANSS scale is used to assess the neuropsychiatric symptoms of schizophrenia. The 30-item PANSS scale provides a total score (sum of the scores of all 30 items) and scores for 3 subscales, the positive subscale (7 items), the negative subscale (7 items),and the general psychopathology subscale (16 items), each item rated on a scale of 1 (absent) to 7 (extreme). (NCT00589914)
Timeframe: Baseline to the last postrandomization assessment in the double-blind treatment period (approximately 13 weeks)

InterventionScores on a scale (Mean)
R092670-18.6
RISPERDAL CONSTA-17.9

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The Change From Baseline for the CGI-S Score

The CGI-S rating scale is used to rate the severity of a patient's psychotic condition on a 7-point scale ranging from 1 (not ill) to 7 (extremely severe). This scale permits a global evaluation of the patient's condition at a given time. A qualified rater administered the CGI-S. (NCT00589914)
Timeframe: Baseline to the last postrandomization assessment in the double-blind treatment period (approximately 13 weeks)]

InterventionScores on a scale (Mean)
R092670-0.9
RISPERDAL CONSTA-0.9

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The Remission Rate in Both the Quetiapine XR Group and the Risperidone Group at Month 12 in the ITT Population

Remission was defined as a SWN-K total score greater than or equal to 80. The reported population is participants who showed remission over, time from baseline to Month 12 (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR139
Risperidone128

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The Safety and Tolerability of Quetiapine XR vs Risperidone by Evaluating the Number of Participants at Month 12 in Safety Population With Individual Symptoms Assessed by the Modified Udvalg for Kliniske Undersogelser, Side Effect Rating Scale: Neurologic

Symptoms are graded according to degree (not present to severe) and causal relationship (improbable, possible, probable). An individual AE is defined as an AE with a worse degree compared with Baseline and with a possible or probable relationship to study drug. (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR4
Risperidone20

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The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Time Between First Study Drug Intake and First Hospitalization for Patients With 1 Hospitalization in the ITT Population

(NCT00600756)
Timeframe: 12 months

InterventionDays (Mean)
Quetiapine XR144.3
Risperidone152.8

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants With a Treatment-emergent Adverse Event (TEAEs) at Month 12 in the Safety Population

Treatment-emergent adverse events are defined as adverse events that occurred after the first intake of the study medication (or on the same day). (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR238
Risperidone258

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The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Mean Number of Lost School/Work Days at Month 12 in the ITT Population

"Workers and students are defined from the modified vocational status index excluding subjects Retired or Unemployed, whether or not expected to work." (NCT00600756)
Timeframe: 12 months

InterventionDays (Mean)
Quetiapine XR10
Risperidone6.7

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The Effect of Quetiapine XR Versus Risperidone by Evaluating the Relapse Rate at Month 12 in the ITT Population

Relapse is defined as at least one increase of greater than or equal to 2 points on the CGI-SCH overall severity score during the treatment period or at least one hospitalization due to psychiatric disorders during the treatment period. (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR43
Risperidone31

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The Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population on Core Schizophrenic and Depressive Symptoms by Evaluating the Change From Baseline in the Calgary Depression Scale for Schizophrenia (CDSS) Total Score

The CDSS total score is the sum of 9 questions and ranges from 0 to 27. The higher the score, the more severe are the symptoms. (NCT00600756)
Timeframe: 12 months

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR-4.7
Risperidone-3.7

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The Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population on Core Schizophrenic and Depressive Symptoms by Evaluating the Change From Baseline in CGI-SCH Overall Severity Score (Improved).

For the CGI-SCH overall severity of illness, the score ranged from 1 (normal, not ill) to 7 (among the most severely ill). CGI-SCH score was divided into 3 classes: worsening (change score>0), stable (change score=0) and improved (change score<0). Change from baseline in CGI-SCH overall severity of illness in number of participants with CGI-SCH overall severity score improvement. (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR176
Risperidone178

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants Who Had at Least 1 Extra-pyramidal TEAE at Month 12 in the Safety Population

Treatment-emergent adverse events are defined as adverse events that occurred after the first intake of the study medication (or on the same day). (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR38
Risperidone83

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Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Mental Functioning at Month 12 in the ITT Population.

The SWN-K total score is the sum of 5 subscores (4 questions each): physical functioning, social integration, mental functioning, self-control, and emotional regulation. The subscores are rated using a 6-point scale (the higher the grade, the better the response). Possible subscores range from 4 to 24. (NCT00600756)
Timeframe: Baseline and 12 months

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR4.9
Risperidone3.9

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The Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population on Core Schizophrenic and Depressive Symptoms by Evaluating the Change From Baseline in CGI-SCH Overall Severity Score

For the CGI-SCH (Clinical Global Impression-Schizophrenia severity of illness scale) overall severity of illness, the score ranged from 1 (normal, not ill) to 7 (among the most severely ill). Change from baseline in CGI-SCH score was divided into 3 classes: worsening (change score>0), stable (change score=0) and improved (change score<0). (NCT00600756)
Timeframe: 12 months

InterventionScores on a scale (Mean)
Quetiapine XR3.8
Risperidone3.9

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The Compliance of Patients Taking Quetiapine XR Versus Risperidone at Month 12 by Evaluating the Number of Participants Who Returned Study Drug at Month 12 in the ITT Population

(NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR270
Risperidone249

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Responder Rate at Month 6 in the Per Protocol Population Using the Subjective Well-being Under Neuroleptics Scale, Short Version (SWN-K) Total Score

The SWN-K is comprised of 20 questions, rated on a 6-point scale from 1 (not at all) to 6 (very much). Scores range from 20 to 120, with higher scores implying higher subjective well-being. A responder is defined as a subject with an increase of 10 points or 20% from baseline in SWN-K total score (non-inferiority limit of -9.7% in responder rate) (NCT00600756)
Timeframe: 6 months

InterventionParticipants (Number)
Quetiapine XR136
Risperidone158

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The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Participants With at Least 1 Hospitalization Due to Psychiatric Disorders at Month 12 in the ITT Population

All hospitalizations due to psychiatric disorders during the study (i.e. from Visit 1 to Termination date + 30 days) in inpatients units, in emergency wards, and in day clinics. (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR37
Risperidone21

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Number of Participants Using Antidepressants at Month 12 in the ITT Population

"The number of participants who were taking at least 1 antidepressant at Month 12. Antidepressants are all concomitant medications classified in the Anatomical Therapeutic Chemical(ATC)Subgroup N06-Antidepressants." (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR72
Risperidone63

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Change From Baseline in Mean Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Total Score at Month 12 in the Per Protocol Population

The SWN-K is comprised of 20 questions, each of which is rated using a 6-point scale ranging from 1 (not at all) to 6 (very much). Possible scores range from 20 to 120, with higher scores implying higher subjective well-being. (NCT00600756)
Timeframe: Baseline and Month 12

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR23.2
Risperidone21.1

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To Evaluate the Effect of Quetiapine XR Versus Risperidone at Month 12 in the ITT Population Regarding Health Economics Outcomes by Evaluating the Functional Improvement Rate of the Modified Vocational Status Index/ Location Code Index: Stable State

Stable State was defined as having the same status in occupational and residential status as at Baseline. (NCT00600756)
Timeframe: 12 months

InterventionParticipants with stable state (Number)
Quetiapine XR160
Risperidone171

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants Who Discontinued the Study Because of an TEAE at Month 12 in the Safety Population

Treatment-emergent adverse events are defined as adverse events that occurred after the first intake of the study medication (or on the same day). (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR57
Risperidone48

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants at Month 12 in the Safety Population With Individual Symptoms Assessed by the Modified UKU: Sexual Dysfunction in Men

Symptoms are graded according to degree (not present to severe) and causal relationship (improbable, possible, probable). Sexual dysfunction in men is defined as number of men who show the individual adverse event (AE) sexual dysfunction. An individual AE sexual dysfunction is defined as an AE with a worse degree of sexual dysfunction compared with baseline and with a possible or probable relationship to study drug. (NCT00600756)
Timeframe: Month 12

InterventionParticipants (Number)
Quetiapine XR9
Risperidone13

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants Who Had at Least 1 Cardiac TEAE at Month 12 in the Safety Population

Treatment-emergent adverse events are defined as adverse events that occurred after the first intake of the study medication (or on the same day). (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR22
Risperidone17

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Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Social Integration at Month 12 in the ITT Population.

The SWN-K total score is the sum of 5 subscores (4 questions each): physical functioning, social integration, mental functioning, self-control, and emotional regulation. The subscores are rated using a 6-point scale (the higher the grade, the better the response). Possible subscores range from 4 to 24. (NCT00600756)
Timeframe: Baseline and 12 months

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR4.6
Risperidone4.0

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Change From Baseline in Mean Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Total Score at Month 12 in the Intent-to-Treat (ITT) Population

The SWN-K is comprised of 20 questions, each of which is rated using a 6-point scale ranging from 1 (not at all) to 6 (very much). Possible scores range from 20 to 120, with higher scores implying higher subjective well-being. (NCT00600756)
Timeframe: Baseline and Month 12

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR22.7
Risperidone19.4

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Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Self-control at Month 12 in the ITT Population.

The SWN-K total score is the sum of 5 subscores (4 questions each): physical functioning, social integration, mental functioning, self-control, and emotional regulation. The subscores are rated using a 6-point scale (the higher the grade, the better the response). Possible subscores range from 4 to 24. (NCT00600756)
Timeframe: Baseline and 12 months

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR4.1
Risperidone3.8

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Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Physical Functioning at Month 12 in the ITT Population.

The SWN-K total score is the sum of 5 subscores (4 questions each): physical functioning, social integration, mental functioning, self-control, and emotional regulation. The subscores are rated using a 6-point scale (the higher the grade, the better the response). Possible subscores range from 4 to 24. (NCT00600756)
Timeframe: Baseline and 12 months

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR4.9
Risperidone4.0

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The Effect of Quetiapine XR Versus Risperidone Regarding Health Economics Outcomes by Evaluating the Number of Participants Using Other Psychotropic Medications at Month 12 in the ITT Population

Other psychotropic medications include antiepileptics, anti-parkinson drugs, antipsychotics, and antidepressants. (NCT00600756)
Timeframe: 12 months

InterventionParticipants (Number)
Quetiapine XR138
Risperidone141

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Change From Baseline in the Subjective Well-Being Under Neuroleptic Treatment Scale (SWN-K) Subscale Score: Emotional Regulation at Month 12 in the ITT Population.

The SWN-K total score is the sum of 5 subscores (4 questions each): physical functioning, social integration, mental functioning, self-control, and emotional regulation. The subscores are rated using a 6-point scale (the higher the grade, the better the response). Possible subscores range from 4 to 24. (NCT00600756)
Timeframe: Baseline and 12 months

InterventionScores on a scale (Least Squares Mean)
Quetiapine XR4.5
Risperidone3.9

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Number of Subjects Who Had an Unscheduled Visits Due to Worsening of Schizophrenia, Dose Change, or Adverse Event at Month 12 in the ITT Population

Unscheduled visits due to worsening of schizophrenia, dose change or adverse event including the hospitalizations due to psychiatric disorders during the study (i.e. from Visit 1 to Termination date + 30 days) in inpatients units, in emergency wards and in day clinics. (NCT00600756)
Timeframe: Month 12

InterventionParticipants (Number)
Quetiapine XR94
Risperidone70

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Participants at Month 12 in the Safety Population With Individual Symptoms Assessed by the Modified UKU: Hyperprolactinaemia in Women

Symptoms are graded according to degree (not present to severe) and causal relationship (improbable, possible, probable). Hyperprolactinaemia in women is defined as number of women who show the individual adverse event (AE) hyperprolactinaemia. An individual AE Hyperprolactinaemia is defined as an AE with a worse degree of hyperprolactinaemia compared with baseline and with a possible or probable relationship to study drug. (NCT00600756)
Timeframe: Month 12

InterventionParticipants (Number)
Quetiapine XR0
Risperidone10

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Number of Extra-pyramidal Events at Month 12 in the Safety Population

Extra-pyramidal events include tremor, hypokinesia, muscle rigidity, hyperkinesia, and extrapyramidal disorder. (NCT00600756)
Timeframe: 12 months

InterventionEvents (Number)
Quetiapine XR51
Risperidone112

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The Safety and Tolerability of Quetiapine XR Versus Risperidone by Evaluating the Mean Change From Baseline to Month 12 in Prolactin Levels in the Safety Population

The normal range for men is 0 to 14, and for women is 0 to 24. (NCT00600756)
Timeframe: 12 months

Interventionng/mL (Mean)
Quetiapine XR-7.735
Risperidone15.990

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Percentage of Participants Who Responded to PANSS Total Score at Day 92 or Early Withdrawal

A responder is defined as a participant who improved from baseline in the PANSS total score by 30 percent or more. (NCT00604279)
Timeframe: Day 92 or early withdrawal

InterventionPercentage of participants (Number)
Paliperidone Palmitate70.7
Risperidone Long Acting Injection (LAI)78.4

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Day 92 or Early Withdrawal

The PANSS provides a total score (sum of the scores of all 30 items) and scores for 3 subscales, the positive subscale (7 items), the negative subscale (7 items), and the general psychopathology subscale (16 items), each rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 (absent) to 210 (extreme psychopathology). Higher change scores indicate worsening. (NCT00604279)
Timeframe: Baseline, Day 92 or early withdrawal

,
InterventionUnits on scale (Mean)
BaselineChange at Day 92 or Early Withdrawal
Paliperidone Palmitate82.1-23.6
Risperidone Long Acting Injection (LAI)84.4-26.9

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Change From Baseline in Personal and Social Performance (PSP) Score at Day 92 or Early Withdrawal

This PSP assesses the degree of a participant's dysfunction within 4 domains of behavior: socially useful activities, personal and social relationships, self-care, and disturbing and aggressive behavior. The score ranges from 1 to 100, divided into 10 equal intervals to rate the degree of difficulty (1, absent to 4, very severe) in each of the 4 domains. Based on the four domains there will be one total score. Participants with a score of 71 to 100 have a mild degree of difficulty; from 31 to 70, varying degrees of disability; <= 30, functioning so poorly as to require intensive supervision. (NCT00604279)
Timeframe: Baseline, Day 92 or early withdrawal

,
InterventionUnits on scale (Mean)
BaselineChange at Day 92 or Early Withdrawal
Paliperidone Palmitate47.816.8
Risperidone Long Acting Injection (LAI)45.318.6

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Change From Baseline in Clinical Global Impression-Severity (CGI-S) Score at Day 92 or Early Withdrawal

"The CGI-S rating scale is a 7 point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher change scores indicate worsening." (NCT00604279)
Timeframe: Baseline, Day 92 or early withdrawal

,
InterventionUnits on scale (Mean)
BaselineChange at Day 92 or Early Withdrawal
Paliperidone Palmitate4.9-1.5
Risperidone Long Acting Injection (LAI)5.0-1.7

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Change From Baseline in the Sleep Visual Analog Scale (VAS) Score at Day 92 or Early Withdrawal

The self-administered sleep VAS scale (0-100 millimeter [mm]) rates quality of sleep (QoS) and daytime drowsiness (DD). Participants indicate mark on the scale to represent how well they have slept in the previous 7 days, score ranges from 0 mm (very badly) to 100 mm (very well); and how often they have felt drowsy within the previous 7 days, from 0 mm (not at all) to 100 mm (all the time). (NCT00604279)
Timeframe: Baseline, Day 92 or early withdrawal

,
Interventionmillimeter (mm) (Mean)
QoS, BaselineQoS, Change at Day 92 or Early WithdrawalDD, BaselineDD, Change at Day 92 or Early Withdrawal
Paliperidone Palmitate64.18.229.9-4.1
Risperidone Long Acting Injection (LAI)66.610.029.6-4.9

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Change From Baseline to Week 12 of HAM-D Score

21-item scale for depression. Symptoms are rated finely (on a 5-point scale: absent; doubtful or trivial; mild: moderate severe) or coarsely (on a 3- point scale: absent; doubtful or mild; obvious, distinct, or severe).Total score range 0- 66, higher values represent worse outcome.Number of participants refers to valid for efficacy per protocol. Change:total score at week 12 minus total score at baseline. (NCT00640562)
Timeframe: 12 weeks from baseline to last visit

InterventionScore on scale (Mean)
Seroquel XR-29.83
Risperidone-23.02

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Change From Baseline to Week 12 of Drug Attitude Inventory 10 Item Scale (DAI 10) Score

These items are presented as self-report statements with which the patient agrees or disagrees. Each response is scored as +1 if correct or -1 if incorrect. The final score is the grand total of the positive and negative points. A positive score means a positive subjective response. A negative total score means a negative subjective response (NCT00640562)
Timeframe: 12 week from baseline to last visit

Interventionscore on scale (Least Squares Mean)
Seroquel XR86.38
Risperidone76.64

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Change From Baseline to Week 12 of Calgary Depression Scale for Schizophrenia (CDSS) Score.

"The CDSS scale is used to assess the level of depression in schizophrenia and to estimate the severity of depressive symptoms.~CDSS has 9 items rated on four-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Anchor point descriptions are provided to aid differentiation between each item score. The first eight items are rated on basis of patients' responses to questions; the 9 item is based on clinician's assessment.~The sum score is derived by adding the point score of all items (from 0 to 27 points); total score 4-5 is considered for minor depression and 6-7 score for major depression." (NCT00640562)
Timeframe: 12 week from baseline to last visit

InterventionScore on a scale (Least Squares Mean)
Seroquel XR7.31
Risperidone5.53

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Concomitant Use of Antidepressive Drugs From Baseline to Week 12

Number of concomitant users of antidepressive drugs during the study; the number of participants analyzed refers to safety population, that is to overall participants excluding 6 participants who did not assume any study drug administration (NCT00640562)
Timeframe: 12 week from baseline to last visi

InterventionParticipants (Number)
Seroquel XR12
Risperidone11

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Change From Baseline in the Simpson Angus Scale (SAS) Total Score to Week 12 as an Indication of Neurological Side Effects Section

"Extrapyramidal Side Effects (EPS) will be assessed using the Simpson-Angus Scale (SAS; Simpson GN et al 1970) . The CRF is source data for these assessments and day 0 is considered as baseline.~The SAS scale, containing 10 items, will be rated on a five-point scale where 0 is normal and 4 are severe symptoms. Min score =0, max score 40~Change from start of treatment (day 0) will be calculated as the visit score minus the score at start of treatment for each of the neurological assessments." (NCT00640562)
Timeframe: 12 weeks from baseline to last visit

Interventionscore on scale (Mean)
Seroquel XR2.74
Risperidone3.88

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Concomitant Use of Antidepressive Drugs From Baseline to Week 12

Number of concomitant users of antidepressive drugs during the study; the number of participants analyzed refers to ITT/safety population, that is to overall participants excluding the 6 participants who did not assume any study drug administration (NCT00640562)
Timeframe: Change of drug use from baseline to last visi

InterventionParticipants (Number)
Seroquel XR14
Risperidone17

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Change From Screening Visit to Week 12 of Prolactin Live

Plasma prolactin live was drawn prior to morning meal at the screening visit at the last visit (NCT00640562)
Timeframe: 12 week from screening visit to last visit

InterventionKG (Least Squares Mean)
Seroquel XR61.20
Risperidone90.80

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CGI- Global Improvement Mean Score at Week 12

"The CGI-S subset ranges from 1 to 7 such that a score of 1 indicates normal, not at all ill, while a score of 7 indicates among the most extremely ill of patients. The change from start of treatment (baseline V2) in the Severity of Illness will be calculated by subtracting the score at start of treatment (baseline V2) from the following visits" (NCT00640562)
Timeframe: 12week: descriptive statistic of CGI by visit and treatment

Interventionscore on a scale (Mean)
Seroquel XR91
Risperidone88

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Body Mass Index (BMI) at Week 12

Patient weight and height have been be collected in order to assess the Body Mass Index (BMI). The mean BMI values reported are assessed after 12 weeks of treatment. (NCT00640562)
Timeframe: 12 week

InterventionKg/m^2 (Mean)
Seroquel XR29.07
Risperidone28.80

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- Change From Baseline to Week 12 of Clinical Global Impression (CGI- Severity of Illness) Score

"The CGI-S subset ranges from 1 to 7 such that a score of 1 indicates normal, not at all ill, while a score of 7 indicates among the most extremely ill of patients. The change from start of treatment (baseline V2) in the Severity of Illness will be calculated by subtracting the score at start of treatment (baseline V2) from the following visits" (NCT00640562)
Timeframe: 12 weeks from baseline to last visit

InterventionScore on scale (Least Squares Mean)
Seroquel XR-1.50
Risperidone-1.04

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Change From Baseline to Week 12 of PANSS Score

30-item scale where each symptom is rated on a severity ranging from 1-7. Symptoms are categorized into 7 items referring to positive, 7 items referring to negative and 16 general psychotic. Total score range 30- 210, higher values represent worse outcome. Number of participants analyzed refers to valid for efficacy per protocol population. (NCT00640562)
Timeframe: 12 weeks from baseline to last visit

Interventionscore on scale (Mean)
Seroquel XR102.26
Risperidone100.51

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Number of Participants With Adverse Events.

(NCT00641745)
Timeframe: 12 months

Interventionparticipants (Number)
Lurasidone395
Risperidone189

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Change From Baseline to Week 6 in the PANSS Total Score

The Positive and Negative Syndrome Scale (PANSS) is a 30-item rating scale that assesses the positive and negative symptoms of individuals with schizophrenia. Responses to the 30 items are based on a structured clinical interview with the patient and on supporting clinical information obtained from family, hospital staff, or other reliable informants. Of the 30 psychiatric parameters measured by the scale, 7 assess positive symptoms (eg, delusions, grandiosity); 7 assess negative symptoms (eg, blunted affect, emotional withdrawal); and 16 assess general psychopathology (eg, poor attention, active social avoidance). Each item is scored on a 7-point scale (1 = absent, 2 = minimal, 3 = mild, 4 = moderate, 5 = moderately severe, 6 = severe, and 7 = extreme). The PANSS total score can range from 30 to 210. A higher score indicates worse symptoms. A negative change score indicates improvement. (NCT00694707)
Timeframe: Baseline to Week 6

,,,,
InterventionUnits on a scale (Mean)
BaselineChange at Week 6
Cariprazine 1.5 mg97.1-17.3
Cariprazine 3.0 mg97.2-18.7
Cariprazine 4.5 mg96.7-20.2
Placebo97.3-9.5
Risperidone 4.0 mg98.1-25.3

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Change From Baseline to Week 6 in the CGI-S Score

The Clinical Global Impressions-Severity (CGI-S) scale is a 7-point scale that measures the overall severity of the illness compared with the severity of illness in other patients the Investigator has observed. The Investigator assesses the severity of the patient's illness as one of the following: 1 = Normal, not at all ill; 2 = Borderline ill; 3 = Mildly ill; 4 = Moderately ill; 5 = Markedly ill; 6 = Severely ill; 7 = Among the most extremely ill patients. The CGI-S score can range from 1 to 7. A higher score indicates more severe illness. A negative change score indicates improvement. (NCT00694707)
Timeframe: Baseline to Week 6

,,,,
InterventionUnits on a scale (Mean)
BaselineChange at Week 6
Cariprazine 1.5 mg4.7-0.9
Cariprazine 3.0 mg4.9-1.1
Cariprazine 4.5 mg4.8-1.2
Placebo4.9-0.6
Risperidone 4.0 mg4.8-1.4

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Change From Baseline in Body Weight

(NCT00698022)
Timeframe: Baseline and 28 days

Interventionkilograms (Mean)
Mifepristone Plus Risperidone2.32
Risperidone Plus Mifepristone-matched Placebo4.23
Risperidone-matched Placebo Plus Mifepristone2.87

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Percentage of Participants With One or More Adverse Events

(NCT00698022)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Mifepristone Plus Risperidone29
Risperidone Plus Mifepristone-matched Placebo27
Risperidone-matched Placebo Plus Mifepristone13

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Percentage of Participants With <5% and <7% Increase From Baseline in Body Weight

(NCT00698022)
Timeframe: Baseline and 28 days

,,
InterventionParticipants (Count of Participants)
<5% increase in body weight<7% increase in body weight
Mifepristone Plus Risperidone913
Risperidone Plus Mifepristone-matched Placebo310
Risperidone-matched Placebo Plus Mifepristone811

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Percentage of Participants Discontinued From the Study Due to an Adverse Event

(NCT00698022)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Mifepristone Plus Risperidone5
Risperidone Plus Mifepristone-matched Placebo4
Risperidone-matched Placebo Plus Mifepristone1

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Proportion of Participants With TEAEs Leading to Discontinuation

(NCT00711269)
Timeframe: From Baseline to up to 8 weeks

InterventionParticipants (Count of Participants)
SM-13496 (Lurasidone HCl) 40-mg Group18
SM-13496 (Lurasidone HCl) 80-mg Group18
Placebo Group27
Risperidone Group7

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Change From Baseline in the PANSS Negative Subscales at Week 6

The PANSS is comprised of 30 items and three subscales. The Negative subscale contains seven questions to assess blunted effect, emotional withdrawal, poor rapport, passive/apathetic social withdrawal, lack of motivation, and similar symptoms. An anchored Likert scale from 1-7, where values of 2 and above indicate the presence of progressively more severe symptoms, is used to score each item. The PANSS Negative subscale score is the sum of all 7 items and ranges from 7 through 49. A higher score is associated with greater illness severity. (NCT00711269)
Timeframe: Baseline and Week 6 (LOCF)

Interventionunits on a scale (Least Squares Mean)
SM-13496 (Lurasidone HCl) 40-mg Group-1.6
SM-13496 (Lurasidone HCl) 80-mg Group-1.7
Placebo Group-0.9
Risperidone Group-1.7

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Change From Baseline in the PANSS General Psychopathology Subscales at Week 6 (LOCF)

The PANSS is comprised of 30 items and three subscales. The General Psychopathology subscale addresses other 16 symptoms such as anxiety, somatic concern, and disorientation. An anchored Likert scale from 1-7, where values of 2 and above indicate the presence of progressively more severe symptoms, is used to score each item. The PANSS General Psychopathology subscale score is the sum of all 16 items and ranges from 16 through 112. A higher score is associated with greater illness severity. (NCT00711269)
Timeframe: Baseline and Week 6 (LOCF)

Interventionunits on a scale (Least Squares Mean)
SM-13496 (Lurasidone HCl) 40-mg Group-2.4
SM-13496 (Lurasidone HCl) 80-mg Group-1.2
Placebo Group-1.0
Risperidone Group-2.6

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Proportion of Participants With Treatment-emergent Serious Adverse Events (SAEs)

Proportion of participants with treatment-emergent adverse events. An adverse event was considered serious if it met one or more of the following criteria: Resulted in death; Was life-threatening (i.e., a patient was at immediate risk of death at the time of the event, not an event where occurrence in a more severe form might have caused death); Required in-patient hospitalization or prolongation of existing hospitalization; Resulted in persistent or significant disability/incapacity; Was a congenital anomaly/birth defect; Was considered to be an important medical event. (NCT00711269)
Timeframe: From Baseline to up to 8 weeks

InterventionParticipants (Count of Participants)
SM-13496 (Lurasidone HCl) 40-mg Group8
SM-13496 (Lurasidone HCl) 80-mg Group7
Placebo Group10
Risperidone Group2

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Change From Baseline in the PANSS Positive Subscales at Week 6 (LOCF)

The PANSS is comprised of 30 items and three subscales. The Positive subscale contains seven questions to assess delusions, conceptual disorganization, hallucinations behavior, excitement, grandiosity, suspiciousness/persecution, and hostility. An anchored Likert scale from 1-7, where values of 2 and above indicate the presence of progressively more severe symptoms, is used to score each item. The PANSS Positive subscale score is the sum of all 7 items and ranges from 7 through 49. A higher score is associated with greater illness severity. (NCT00711269)
Timeframe: Baseline and Week 6 (LOCF)

Interventionunits on a scale (Least Squares Mean)
SM-13496 (Lurasidone HCl) 40-mg Group-2.0
SM-13496 (Lurasidone HCl) 80-mg Group-1.4
Placebo Group-0.6
Risperidone Group-2.9

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Change From Baseline in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 6 (LOCF)

The PANSS is an interview-based measure of the severity of psychopathology in adults with psychotic disorders. The measure is comprised of 30 items and three subscales: the Positive subscale contains seven questions to assess delusions, conceptual disorganization, hallucinations behavior, excitement, grandiosity, suspiciousness/persecution, and hostility; the Negative subscale contains seven questions to assess blunted effect, emotional withdrawal, poor rapport, passive/apathetic social withdrawal, lack of motivation, and similar symptoms; and the General Psychopathology subscale addresses other symptoms such as anxiety, somatic concern, and disorientation. An anchored Likert scale from 1-7, where values of 2 and above indicate the presence of progressively more severe symptoms, is used to score each item. The PANSS total score is the sum of all 30 items and ranges from 30 through 210. A higher score is associated with greater illness severity. (NCT00711269)
Timeframe: Baseline and Week 6 [Last Observation Carried Forward (LOCF)]

Interventionunits on a scale (Least Squares Mean)
SM-13496 (Lurasidone HCl) 40-mg Group-6.1
SM-13496 (Lurasidone HCl) 80-mg Group-4.3
Placebo Group-2.5
Risperidone Group-7.1

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Proportion of Participants With Treatment-emergent Adverse Events (TEAEs)

Proportion of participants with treatment-emergent adverse events. An adverse event was defined as any untoward medical occurrence in a study participant who was taking a medicinal (investigational) product. Treatment-emergent adverse events (TEAEs) were defined as adverse events with a start date on or after the date of the first dose through the end of follow-up, or adverse events occurring before the date of first dose and worsening during the treatment or follow-up period. (NCT00711269)
Timeframe: From Baseline to up to 8 weeks

InterventionParticipants (Count of Participants)
SM-13496 (Lurasidone HCl) 40-mg Group105
SM-13496 (Lurasidone HCl) 80-mg Group103
Placebo Group101
Risperidone Group53

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QTc Measurement

Information regarding the Outcome Measure being a Primary or Secondary, is unavailable. (NCT00712270)
Timeframe:

Interventionmilliseconds (Mean)
QTc Pre-treatment for Entire Study Population381
QTc Post-treat for Entire Study Population389

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Actigraphic Measurement of Treatment Conditions

The child's impulsivity and inability to sleep represented a significant symptom and risk factor. Impulsivity and sleep will be actigraphically assessed by treatment conditions. (NCT00723580)
Timeframe: May 12- July 14, 2010

Interventionactivity (Mean)
Baseline No Medication Midnight to 1:00 AMrisperidone .5 mg t.i.d. Midnight to 1:00 AM
Actigraphic (Activity Count) Measurement of Sleep and Activity55.029.94

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Weight Gain

Weight gain from baseline to last observation up to 12 weeks. Last observation carried to 12 weeks. (NCT00746252)
Timeframe: These measurements are done biweekly from baseline up until 12 weeks

Interventionpounds (Mean)
Risperidone8.5
Aripiprazole6.65

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NCBRF-TIQ D-Total Score

"Parent ratings of aggression and hostility on the Nisonger Child Behavior Rating Form-Typical IQ (NCBRF-TIQ) D-Total Score. The NCBRF provides 1 prosocial subscale (Positive/Social) and 6 problem behavior subscales (Conduct Problem, Oppositional Behavior, Hyperactive, Inattentive, Overly Sensitive, and Withdrawn/Dysphoric). The NCBRF has excellent internal consistency, distinguishes between controls and subjects with DBDs. Conduct Problem and Oppositional Behavior subscales map closely to DSM-IV-TR symptoms of CD and ODD; they were scored together to form a variable called the D-Total.~For the NCBRF D-Total, higher scores reflect worse behavior. Each subscale is scored by taking the rating (0 [did not occur or was not a problem] to 3 [occurred a lot or was a very severe problem]) for all component items. The D-Total score was computed by adding the 6 scores from the Oppositional subscale and the 10 items from the Conduct Problem subscale. Thus D-Total scores could range from 0-69." (NCT00796302)
Timeframe: Measured at baseline and Weeks 3, 4, 5, 6, 7, 8, 9

,
Interventionunits on a scale (Mean)
BaselineWeek 3Week 4Week 5Week 6Week 7Week 8Week 9
Augmented (Stimulant + PMT + Risperidone)42.125.917.112.113.813.011.710.7
Basic (Stimulant + PMT + Placebo)43.524.922.420.120.716.817.817.8

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Clinical Global Impressions Scale for Severity of Illness

Using this clinician rating scale the severity of the illness is scored from 1= normal to 7= extremely ill. This scale was used at baseline and Weeks 1, 2, 3, 4, 5, 6, 7, 8, & 9. Only endpoint (week 9 or subject's last visit) Clinical Global Impressions Scale for Severity of Illness scores are reported below. (NCT00796302)
Timeframe: Measured at endpoint visit

,
Interventionparticipants (Number)
Normal/Borderline/Mildly ill at endpointModerately/Markedly/Severely ill at endpoint
Augmented (Stimulant + PMT + Risperidone)5622
Basic (Stimulant + PMT + Placebo)4934

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Antisocial Behavior Scale - Reactive Aggression Subscale

The Antisocial Behavior Scale (ABS) is a 28-item scale that contains 10 Proactive Aggression items and six Reactive Aggression items. Each item is rated on a 3-point scale, ranging from 1 (Never) to 3 (Very often). Thus, scores on the Reactive Aggression subscale can range from 6 through 18; with higher scores indicating more reactive aggression. (NCT00796302)
Timeframe: Measured at baseline and Week 9

,
Interventionunits on a scale (Mean)
BaselineWeek 9
Augmented (Stimulant + PMT + Risperidone)15.511.0
Basic (Stimulant + PMT + Placebo)15.912.3

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Clinical Global Impressions Scale for Improvement

"Using this clinician rating scale the patient's improvement is scored on a 7-point scale which ranges from very much improved (1), through no change (4), to very much worse (7). This scale was used at baseline and Weeks 1, 2, 3, 4, 5, 6, 7, 8, & 9. Only endpoint (week 9 or subject's last visit) Clinical Global Impressions Scale for Improvement scores are reported below." (NCT00796302)
Timeframe: Measured at endpoint visit

,
Interventionparticipants (Number)
Much or very much improved at endpointMinimally improved at endpointUnchanged or worse at endpoint
Augmented (Stimulant + PMT + Risperidone)63116
Basic (Stimulant + PMT + Placebo)58223

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Body Mass Index (BMI) Z-score Change

(NCT00806234)
Timeframe: Change from baseline to 24 weeks

InterventionZ Score (Least Squares Mean)
Healthy Lifestyle Information0.040
Switch Treatment + Healthy Lifestyle Instruction-0.112
Metformin Treatment + Healthy Lifestyle Instruction-0.088

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Change in Low Density Lipoprotein (LDL) Cholesterol Level

(NCT00806234)
Timeframe: From Baseline to Week 24

Interventionmg/dL (Least Squares Mean)
Healthy Lifestyle Information3.6
Switch Treatment + Healthy Lifestyle Instruction-8.1
Metformin Treatment + Healthy Lifestyle Instruction-4.1

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Change in Whole Body Insulin Sensitivity Index

(NCT00806234)
Timeframe: Change from baseline to 24 weeks

InterventionmU/L (Least Squares Mean)
Healthy Lifestyle Information0.74
Switch Treatment + Healthy Lifestyle Instruction0.42
Metformin Treatment + Healthy Lifestyle Instruction-0.34

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Triglyceride Levels

(NCT00806234)
Timeframe: Change from baseline to 24 weeks

Interventionmg/dL (Least Squares Mean)
Healthy Lifestyle Information0.2
Switch Treatment + Healthy Lifestyle Instruction16.6
Metformin Treatment + Healthy Lifestyle Instruction14.7

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Change From Baseline in Pulse Rate at 52 Weeks Endpoint

LS Mean of change from baseline in pulse rate is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline value and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

,
Interventionbeats per minute (bpm) (Least Squares Mean)
Supine PulseStanding Pulse
LY2140023-1.62-2.16
Standard-of-Care (SOC)-2.44-2.41

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Number of Participants With Potentially Clinically Significant Changes in QT Intervals Electrocardiograms (ECGs)

"A potentially clinically significant QT interval (high) is defined as a value meeting the criteria of (> 450 millisecond [ms]) at anytime during the active treatment phase, provided it does not meet the criteria at baseline.~(analysis for Study Period III only)" (NCT00845026)
Timeframe: Baseline through 24 weeks

Interventionparticipants (Number)
LY21400233
Standard-of-Care (SOC)4

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Percentage of Participants With Remission (Rate of Remission) at Week 24 Endpoint

Remission is defined as endpoint score of mild or better (≤3) for each of the following PANSS items: delusions, conceptual disorganization, hallucinatory behavior, social withdrawal, blunted affect, lack of spontaneity and flow of conversation, mannerisms and posturing, and unusual thought content. PANSS assesses the positive and negative symptoms and general psychopathology specifically associated with schizophrenia. The scale consists of 30 items. Each item is rated from 1 (symptom not present) to 7 (extremely severe). The sum of the 30 items is the PANSS total score and ranges 30 - 210. (Analysis for Study Period III only) (NCT00845026)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
LY214002315.0
Standard-of-Care (SOC)22.7

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Percentage of Participants With Response (Rate of Response) at 6 and 24 Weeks Endpoints

Response is defined as reduction ≥ 30% from baseline on PANSS Total Score (Each PANSS item transformed to a 0-6 scale first). PANSS assesses the positive symptoms, negative symptoms, and general psychopathology specifically associated with schizophrenia. The scale consists of 30 items. Each item is rated on an original scale from 1 (symptom not present) to 7 (symptoms extremely severe). The sum of the 30 items is defined as the PANSS total score and ranges from 30 to 210. Higher scores indicate greater severity of illness. (Analysis for Study Period III only) (NCT00845026)
Timeframe: 6 and 24 weeks

,
Interventionpercentage of participants (Number)
6 weeks24 weeks
LY214002335.026.7
Standard-of-Care (SOC)31.337.5

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Number of Participants With Treatment-Emergent Change in Neurological Examination

An increase in score from baseline was considered a treatment-emergent change, unless stated otherwise. Tremor: 0 (absent) - 3 (interferes with motor function); Nystagmus: 0 (absent) - 3 (present on forward gaze); Reflexes: 0 (absent) - 4 (clonic) with normal being a score 2, decrease or increase in score was considered change. Finger-nose and gait tests: 0 (normal) - 1(abnormal); Romberg's sign: (0) absent - (1) present; Muscular strength: 0 (no contraction)-5 (full/normal resistance), decrease in score was considered change; Myoclonic jerks: 0 (absent) - 3 (frequent). (NCT00845026)
Timeframe: Baseline through 52 weeks

,
Interventionparticipants (Number)
TremorNystagmusIncreased reflexesDecreased reflexesAbnormal finger-nose testRomberg's signAbnormal GaitDecreased muscle strengthMyoclonus
LY2140023161792020471
Standard-of-Care (SOC)2312628011110

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Time to Discontinuation Due to Adverse Event (AE)

(NCT00845026)
Timeframe: Baseline through 24 weeks

Interventiondays (Mean)
LY214002393.02
Standard-of-Care (SOC)116.86

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Number of Participants With Suicidal Behaviors and Ideations Baseline Through 52 Weeks

"Columbia Suicide Rating Scale (C-SSRS): scale capturing occurrence, severity, and frequency of suicide-related thoughts and behaviors. Number of participants with suicidal behaviors and ideations are provided. Suicidal behavior: a yes answer to any of 5 suicidal behavior questions: preparatory acts or behavior, aborted attempt, interrupted attempt, actual attempt, and completed suicide. Suicidal ideation: a yes answer to any one of 5 suicidal ideation questions, which includes wish to be dead, and 4 different categories of active suicidal ideation. There are no scores on a scale reported, rather, number of patients who reported yes as described above." (NCT00845026)
Timeframe: Baseline through 52 weeks

,
Interventionparticipants (Number)
Suicidal ideationSuicidal behavior/acts
LY214002380
Standard-of-Care (SOC)162

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Number of Participants With Shift From Baseline to Maximum Post-Baseline Grading in Electroencephalograms (EEGs)

EEG scoring by a central neurologist is done by the following definitions: E0=Normal; E1(within normal)=fewer than 3 focal abnormalities or non-epileptiform abnormalities; E2(questionably epileptiform)=3-10 focal discharges and/or 1-10 multifocal or generalized discharges; E3=(clearly epileptiform)= Sharp/slow complex, runs of epileptiform abnormalities, greater than 10 total epileptiform discharges; and E4= seizure. Decreased= maximum (max) post-baseline (PB) EEG grading< baseline EEG grading; Increased= max PB EEG grading> baseline EEG grading; Same=no change from baseline to max PB result. (NCT00845026)
Timeframe: Baseline through 52 weeks

,
Interventionparticipants (Number)
DecreasedSameIncreased
LY2140023117418
Standard-of-Care (SOC)87733

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Change From Baseline in Measurement and Treatment Research to Improve Cognition in Schizophrenia Consensus Cognitive Battery (MCCB): Overall Composite T-Score at 52 Weeks Endpoint

The MCCB assesses cognitive function in 7 domains important in schizophrenia. The MCCB overall composite score is calculated by summing age- and gender-corrected T-scores of all the domains and then standardizing the sum to a T-score, where the mean is 50 and a standard deviation is 10. A higher score indicates better performance. LS Mean of change from baseline is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline score and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY21400235.29
Standard-of-Care (SOC)8.19

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Change From Baseline in EuroQoL Questionnaire-5 Dimension (EQ-5D) at 52 Weeks Endpoint

The EQ-5D is a quality-of-life (QoL) instrument with 2 parts: a health status profile and a visual analog scale (VAS). The profile rates patients' health state in 5 domains and each of them ranges 1-3. The outcomes on the 5 domains are mapped to an index with range 0-1. The higher score indicates a better health state. The VAS is used to indicate the patient's health status with range 0=worst and 100=best. LS means are from a MMRM model with the effects of treatment, gender, investigator site, visit, treatment-by-visit interaction, baseline score and baseline score by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

,
Interventionunits on a scale (Least Squares Mean)
Visual Analog Scale (n=107, 120)Index Score (n=107, 119)
LY21400234.830.03
Standard-of-Care (SOC)12.840.10

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Change From Baseline in Blood Pressure (BP) at 52 Weeks Endpoint

Least Square (LS) Mean of change from baseline in BP is from a mixed model repeated measures (MMRM) model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline value and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

,
Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Supine Diastolic BPStanding Diastolic BPSupine Systolic BPStanding Systolic BP
LY21400232.495.572.844.65
Standard-of-Care (SOC)0.871.103.471.93

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Change From Baseline in Clinical Global Impression Severity Scale (CGI-S) at 52 Weeks Endpoint

The CGI-S scale measures severity of illness at the time of assessment compared with start of treatment. Scores range from 1 (normal, not at all ill) to 7 (among the most extremely ill patients). LS Mean of change from baseline is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline score and baseline-by-visit interaction. Higher CGI-S score means worse symptoms. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY2140023-0.27
Standard-of-Care (SOC)-0.81

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Number of Participants With Potentially Clinical Significant Change in Lipids Level

Treatment-emergent changes in lab results on lipids level were analyzed using the American Diabetes Association (ADA 2001) and National Cholesterol Education Program (NCEP ATP III) guidelines. Total cholesterol Normal to High is <200 mg/dL at baseline and ≥240 mg/dL post-baseline. Low-density lipoprotein (LDL) cholesterol Normal to High is <100 mg/dL at baseline and ≥160 mg/dL post-baseline. High-density lipoprotein (HDL) cholesterol Normal to Low is ≥40 mg/dL at baseline and <40 mg/dL post-baseline. Triglycerides Normal to High is <150 mg/dL at baseline and ≥200 mg/dL post-baseline. (NCT00845026)
Timeframe: Baseline through 52 weeks

,
Interventionparticipants (Number)
Total cholesterol Normal to High (n=56, 59)LDL cholesterol Normal to High (n=20, 22)HDL cholesterol Normal to Low (n=74, 91)Triglycerides Normal to High (n=58, 77)
LY214002330167
Standard-of-Care (SOC)602321

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Change From Baseline in Barnes Akathisia Scale (BAS) Global Score at 52 Weeks Endpoint

The BAS rates drug induced akathisia symptoms. Akathisia is rated on a 4-point scale, with 0 being no akathisia and 3 being severe akathisia. A global clinical assessment of akathisia is then scored on a 6-point scale, with 0 being no evidence of akathisia and 5 being severe akathisia. LS mean of change from baseline in BAS global score is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY2140023-0.06
Standard-of-Care (SOC)-0.08

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Change From Baseline in 16-Item Negative Symptoms Assessment (NSA-16) Total Score at 52 Weeks Endpoint

"The NSA-16 is used to rate behaviors (not psychopathology) associated with negative symptoms of schizophrenia and rates patients on 16 anchors, each of which is rated 1 to 6. The total score is their sum and ranges from 16 to 96. Higher scores indicate greater severity of illness. LS Mean of change from baseline is from a MMRM model which includes treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline score and baseline-by-visit interaction." (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY2140023-2.86
Standard-of-Care (SOC)-7.81

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Change From Baseline in Weight at 52 Weeks Endpoint

LS Mean of change from baseline in weight is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline weight and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionkilogram (kg) (Least Squares Mean)
LY2140023-4.76
Standard-of-Care (SOC)3.88

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Change From Baseline in University of California-San Diego (UCSD) Performance-Based Skills Assessment-B (UPSA-B) Total Score at 52 Weeks Endpoint

The UPSA-B is a performance-based assessment of improvement in functional capacity. Patients are asked to role-play tasks in 2 areas of functioning: communication and finances. Scores are assigned for each of the 2 subscales and a provided formulae is used to calculated an UPSA-B Total Score (range = 0-100). The higher score indicates a better performance. LS mean of change from baseline is from a MMRM model which includes the effects of treatment, gender, investigator site, visit, treatment-by-visit interaction, baseline score and baseline score by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY214002311.82
Standard-of-Care (SOC)12.84

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Change From Baseline in Subjective Well-Being Under Neuroleptic Treatment-Short Form (SWN-S) Total Score at 52 Weeks Endpoint

Measures subjective well-being for previous 7 days. 20 items covering 5 health domains (subscales) (4 items each): emotional regulation, self-control, mental functioning, social integration, and physical functioning. Individual scores range from 1 (not at all) to 6 (very much). Subscale scores range from 4 to 24. Total score ranges from 20 to 120. LS mean of change from baseline is from a MMRM model which includes the effects of treatment, gender, investigator site, visit, treatment-by-visit interaction, baseline score and baseline score by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY21400231.11
Standard-of-Care (SOC)4.15

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Change From Baseline in Simpson-Angus Scale (SAS) Total Score at 52 Weeks Endpoint

The SAS is used to measure Parkinsonian type symptoms in patients exposed to antipsychotics. The scale consists of 10 items each rated on a 5-point scale, with 0 meaning complete absence of the condition and 4 meaning the presence of the condition in extreme form. The range of possible total score is 0-40. LS Mean of change from baseline in the SAS total score is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY2140023-0.87
Standard-of-Care (SOC)-0.82

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) at 52 Weeks Endpoint

Assesses the positive and negative symptoms and general psychopathology associated with schizophrenia. The scale consists of 30 items. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). The sum of the 30 items is defined as the PANSS total score and ranges from 30 to 210. LS Mean of change from baseline is from a mixed model repeated measures (MMRM) model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline score and baseline-by-visit interaction. Higher PANSS scores mean worse symptoms. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY2140023-4.54
Standard-of-Care (SOC)-21.47

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Change From Baseline in Personal and Social Performance (PSP) at 52 Weeks Endpoint

The Personal and Social Performance (PSP) scale is a 100-point, single-item, clinician-rated scale to assess 4 domains of functioning, including personal and social relationships, socially useful activities, self care, and disturbing and aggressive behaviors. Score ranges from 1-100. The higher score indicates a better health state. LS Mean of changes from baseline is from a MMRM model which includes the effects of treatment, gender, investigator site, visit, treatment-by-visit interaction, baseline score and baseline score by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY21400236.47
Standard-of-Care (SOC)10.71

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Change From Baseline in Number of Psychiatric Visits at 24 Weeks Endpoint

Change in number of psychiatric visits between the 6 months prior to the active treatment phase and psychiatric visits reported during the active treatment phase was summarized. Treatment groups were compared on change using the analysis of covariance (ANCOVA) model. The model has baseline as a covariate, and investigative site, gender, and treatment as fixed effects. (Analysis for Study Period III only) (NCT00845026)
Timeframe: Baseline, 24 weeks

Interventionvisits (Least Squares Mean)
LY2140023-2.60
Standard-of-Care (SOC)-2.95

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Number of Participants With Potentially Clinical Significant Change in Fasting Glucose Level

Treatment-emergent changes in lab results on fasting glucose were analyzed using the American Diabetes Association (ADA 2001) and National Cholesterol Education Program (NCEP ATP III) guidelines. Glucose Normal to High is <100 milligram/deciliter (mg/dL) at baseline and ≥126mg/dL post-baseline. (NCT00845026)
Timeframe: Baseline through 52 weeks

Interventionparticipants (Number)
LY21400238
Standard-of-Care (SOC)13

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Change From Baseline in Montgomery-Asberg Depression Rating Scale (MADRS) Total Score at 52 Weeks Endpoint

The MADRS is a rating scale for severity of depressive mood symptoms. The MADRS has a 10-item checklist. Items are rated on a scale of 0-6, for a total score range of 0 (low severity of depressive symptoms) to 60 (high severity of depressive symptoms). LS Mean of changes from baseline is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline score and baseline-by-visit interaction. Higher MADRS scores mean worse symptoms. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY21400232.72
Standard-of-Care (SOC)-2.82

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Change From Baseline in Abnormal Involuntary Movement Scale (AIMS) Total Score at 52 Weeks Endpoint

The AIMS is a 12-item scale designed to record the occurrence of dyskinetic movements. Items 1 to 10 are rated 0 - 4, with 0 being no dyskinetic movements and 4 being severe dyskinetic movements. Items 11 and 12 are yes/no questions regarding the dental condition of a subject. The total score is the sum of items 1-7 and ranges from 0-28. LS means of change from baseline in the AIMS total score is from a MMRM model which includes the effects of treatment, gender, investigative site, visit, treatment-by-visit interaction, baseline and baseline-by-visit interaction. (NCT00845026)
Timeframe: Baseline, 52 weeks

Interventionunits on a scale (Least Squares Mean)
LY21400230.13
Standard-of-Care (SOC)-0.23

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Percentage of Participants With Relapse (Rate of Relapse)

Relapse is defined as an increase in at least one PANSS positive item to a score>5 and an absolute increase of ≥2 points on that item post randomization , or hospitalization for any psychiatric condition, or active suicidal ideation or suicidal behavior as captured by the C-SSRS. PANSS assesses the positive and negative symptoms and general psychopathology specifically associated with schizophrenia. The scale consists of 30 items. Each item is rated from 1 (symptom not present) to 7 (symptoms extremely severe). The sum of the 30 items is defined as the PANSS total score and ranges from 30-210. (NCT00845026)
Timeframe: Baseline through 52 weeks

Interventionpercentage of participants (Number)
LY214002326.2
Standard-of-Care (SOC)16.8

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Cause-specific Mortality: Number of Participants With Completed Suicides - MedDRA

The analysis was based on all deaths from the WRT+30 days period using the classification based upon MedDRA terminology, that is, as reported by the investigator (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole13
Risperidone21

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Cause-specific Mortality: Number of Participants With Completed Suicides - ISC

"The analysis was based on all deaths from the WRT+30 days period using the classification performed by the ISC.~The ISC reviewed and classified those adverse events which resulted in death or hospitalisation or were possible suicide attempts and this review was blinded to exposure. The definition of cardiac death was intentionally wide; sudden or unexplained deaths were assumed to be cardiac if there was no non-cardiac explanation. To ensure consistent evaluation and classification, the ISC decided a priori to classify all instances of self harm as possible suicide." (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole14
Risperidone21

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Cause-specific Mortality: Number of Participants With Cardiac Deaths - ISC

"The analysis was based on all deaths from the WRT+30 days period using the classification performed by the ISC.~The ISC reviewed and classified those adverse events which resulted in death or hospitalisation or were possible suicide attempts and this review was blinded to exposure. The definition of cardiac death was intentionally wide; sudden or unexplained deaths were assumed to be cardiac if there was no non-cardiac explanation. To ensure consistent evaluation and classification, the ISC decided a priori to classify all instances of self harm as possible suicide." (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole31
Risperidone12

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Cause-specific Mortality: Number of Participants With Cardiac Deaths - MedDRA

The analysis was based on all deaths from the WRT+30 days period using the classification based upon the Medical Dictionary for Regulatory Activities (MedDRA) terminology, that is, as reported by the investigator (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole17
Risperidone8

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Number of Participants With Suicide Attempts (Fatal and Non-fatal) - MedDRA

The analysis was based on all suicides and suicide attempts from the WRT+30 days period using the classification based upon MedDRA terminology, that is, as reported by the investigator (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole43
Risperidone65

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Number of Participants With All-cause Mortality

The analysis was based on all deaths from the Whole Randomised Treatment (WRT)+30 days period and the Only Randomised Treatment (ORT) period, respectively (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

,
Interventionparticipants (Number)
Number of deaths (WRT+30 days)Number of deaths (ORT)
Risperidone6144
Sertindole6440

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Second Primary Outcome: Number of Participants With Cardiac Events, Including Arrhythmias, Requiring Hospitalisation

Second primary endpoint: a serious adverse event where the patient was hospitalised and for which the Independent Safety Committee (ISC) classified the event as a cardiac event with documented arrhythmia. The analysis of this outcome was not performed due to low number of events. The presented analysis is a replacement analysis using all cardiac events, including arrhythmias, that required hospitalisation (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole10
Risperidone6

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Number of Participants With Suicide Attempts (Fatal and Non-fatal) - ISC

"The analysis was based on all suicides and suicide attempts from the WRT+30 days period using the classification performed by the ISC.~The ISC reviewed and classified those adverse events which resulted in death or hospitalisation or were possible suicide attempts and this review was blinded to exposure. The definition of cardiac death was intentionally wide; sudden or unexplained deaths were assumed to be cardiac if there was no non-cardiac explanation. To ensure consistent evaluation and classification, the ISC decided a priori to classify all instances of self harm as possible suicide." (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole68
Risperidone76

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Number of Participants With Discontinuation of Treatment for Any Reason Other Than Study Closure

The analysis was based on time from start of study drug until stop of study drug for any reason other than sponsor closure of the study (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole3136
Risperidone2597

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Cause-specific Mortality: Number of Participants With Other Than Cardiac Deaths and Completed Suicides - MedDRA

The analysis was based on all deaths from the WRT+30 days period using the classification based upon MedDRA terminology, that is, as reported by the investigator (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole34
Risperidone32

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Cause-specific Mortality: Number of Participants With Other Than Cardiac Deaths and Completed Suicides - ISC

"The analysis was based on all deaths from the WRT+30 days period using the classification performed by the ISC.~The ISC reviewed and classified those adverse events which resulted in death or hospitalisation or were possible suicide attempts and this review was blinded to exposure. The definition of cardiac death was intentionally wide; sudden or unexplained deaths were assumed to be cardiac if there was no non-cardiac explanation. To ensure consistent evaluation and classification, the ISC decided a priori to classify all instances of self harm as possible suicide." (NCT00856583)
Timeframe: As study design allowed patients to continue study drug until the study was closed, many patients were followed for several years, with an overall median time period of approximately 14 months

Interventionparticipants (Number)
Sertindole19
Risperidone28

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Number of Participants With Death, Serious Adverse Events (SAEs), Adverse Events (AEs) Leading to Discontinuation, and 1 or More AEs

AE=any new untoward medical event or worsening of a preexisting medical condition that may or may not be causally related to treatment. SAE=any untoward medical occurrence that at any dose results in death; is life-threatening, a congenital anomaly/birth defect, or an important medical event; requires or prolongs inpatient hospitalization, or results in persistent or significant incapacity or drug dependency or abuse. (NCT00857818)
Timeframe: Baseline to Week 16, continuously

,
InterventionParticipants (Number)
DeathsSAEsAEs leading to discontinuation1 or more AEs
Aripiprazole02311
Control Group (Olanzapine, Risperidone, or Quetiapine)0006

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Mean Percent Change From Baseline in Fasting Non-high Density Lipoprotein (Non-HDL) Cholesterol Levels

Based on Last Observation Carried Forward data. Non-HDL cholesterol is defined as the difference between total cholesterol and high-density lipoprotein (HDL) cholesterol levels. Fasting non-HDL cholesterol is defined as the measured fasting HDL cholesterol level subtracted from the measured fasting total cholesterol level. (NCT00857818)
Timeframe: Baseline to Weeks 4, 8, and 16

,
InterventionPercentage of change (Mean)
Week 4Week 8Week 16
Aripiprazole-7.54-18.45-14.72
Control Group (Olanzapine, Risperidone, or Quetiapine)0.19-4.44-2.47

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Mean Baseline Fasting Non-HDL Levels

(NCT00857818)
Timeframe: At baseline (Day 1)

Interventionmg/dL (Mean)
Aripiprazole176.07
Control Group (Olanzapine, Risperidone, or Quetiapine)167.14

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Percentage of Paliperidone or Risperidone Dopamine D2 Receptor Occupancies

(NCT00934635)
Timeframe: Visit 3 (on day 3)

Interventionpercentage (Number)
Paliperidone ER 9 mg Tablet Followed by PET Scan in 2 Hours0
Control0

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Change From Baseline in Abnormal Involuntary Movement Scale (AIMS) Score at Week 52

The AIMS rates the severity of involuntary movements from 0 (none) to 4 (severe), including facial and oral movements, extremity movements, trunk movements, global and judgments, and 2 additional items concerning dental status (yes/no). A total score (ranging from 0 to 28) will be calculated as the sum of items 1 to 7. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Median)
Baseline (n=20,25)Change at Week 52 (n=19,20)
Risperidone Long Acting Injectables00
Risperidone Tablets00

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Change From Baseline in Barnes Akathisia Rating Scale (BARS) Score at Week 52

The BARS includes an objective rating, 2 subjective ratings of symptoms of akathisia (awareness of restlessness and reported distress related to restlessness: ranging from 0 to 3), and a global clinical rating of akathisia (GCRA), ranging from 0 (absent) to 5 (severe). The global rating score, that is scored separately, is the most relevant measure of severity of akathisia. Higher scores denote worsening akathisia. (NCT00992407)
Timeframe: Baseline and Week 52

,
InterventionUnits on a scale (Mean)
Restlessness total score: Baseline(n=20,25)GCRA: Baseline(n=20,25)Restlessness total score:Change at Week52(n=19,22)GCRA: Change at Week 52(n=19,22)
Risperidone Long Acting Injectables0.800.40-0.160.05
Risperidone Tablets0.400.320.00-0.09

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Change From Baseline in Clinical Global Impression-Severity Scale (CGI-S) Score at Week 52

"The CGI rating scale is a 7-point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
BaselineChange at Week 52
Risperidone Long Acting Injectables3.4-0.6
Risperidone Tablet2.8-0.7

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Change From Baseline in Continuous Performance Task (CPT) Based on Neurocognitive Function Test (NCFT) at Week 52

The NCFT is neuropsychological test which measures psychological functions. The CPT assessed CPT (Omissions) and CPT (Commissions). Omission errors indicate the number of times the target was presented, but the participant did not respond/click the mouse. High omission rates indicate that the participant is either not paying attention (distractibility) to stimuli or has a sluggish response. Commission errors indicate the number of times the participant responded but no target was presented. A fast reaction time and high commission error rate points to difficulties with impulsivity. A slow reaction time with high commission and omission errors indicates inattention in general. (NCT00992407)
Timeframe: Baseline and Week 52

,
InterventionErrors (Mean)
CPT (Omissions):Baseline (n=11,15)CPT (Comissions):Baseline (n=11,15)CPT (Omissions):Change at Week 52 (n=7,12)CPT (Comissions):Change at Week 52 (n=7,12)
Risperidone Long Acting Injectables11.017.41.6-3.9
Risperidone Tablets14.229.3-12.2-0.6

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Change From Baseline in Personal and Social Performance (PSP) Scale Score at Week 52

The PSP assesses degree of participant's dysfunction within 4 domains of behavior, socially useful activities, personal and social relationships, self-care, and disturbing and aggressive behavior. The score ranges from 1 to 100, divided into 10 equal intervals to rate degree of difficulty (1=absent to 6=very severe) in each of 4 domains. Based on the 4 domains there will be one total score. Participants with a score of 71 to 100 have a mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
BaselineChange at Week 52
Risperidone Long Acting Injectables50.655.35
Risperidone Tablets58.715.96

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Change From Baseline in Number of Outpatient Clinic Visits at Week 52

Healthcare economics questionnaire consists of 13-Questions, which measured disease burden on participant; out of which 1 question is related to number of outpatient clinic visits. Mean-calculations were done for all questions. Higher value indicates more disease burden. Change from Baseline is the value at Week 52 minus value at Baseline. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionnumber of visits (Mean)
Outpatient clinic visits:Baseline(n=13,20)Outpatient clinic visits:Change at Week 52(n=7,14)
Risperidone Long Acting Injectables4.72.4
Risperidone Tablets4.41.1

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Change From Baseline in Trail Making Test Based on Neurocognitive Function Test (NCFT) at Week 52

The NCFT is neuropsychological test which measures psychological functions. The Trail Making Test is composed of two Parts, A and B. Part A consists of 25 circles printed on a sheet of paper. Each circle contains a number from 1 to 25. The participant's task is to connect the circles with a pencil line as quickly as possible, beginning with the number 1 and proceeding in numerical sequence. Part B consists of 25 circles numbered from 1 to 13 and lettered from A to L. The task in Part B is to connect the circles, in sequence, alternating between numbers and letters. Here, mean number of seconds are represented required to complete each Part. (NCT00992407)
Timeframe: Baseline and Week 52

,
InterventionSeconds (Mean)
Trail A Making Test:Baseline (n=11,15)Trail B Making Test:Baseline (n=11,15)Trail A Making Test:Change at Week 52 (n=7,12)Trail B Making Test:Change at Week 52 (n=7,12)
Risperidone Long Acting Injectables52.6146.05.9-32.3
Risperidone Tablets50.7147.3-7.8-19.5

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Change From Baseline in Total Outpatients and Inpatients Hours at Week 52

Healthcare economics questionnaire consists of 13-Questions, which measured disease burden on participant; out of which 2 questions are related to total outpatients and inpatients hours. Total outpatients hours and total inpatient hours indicate the total hours spent by outpatients and inpatients respectively at Investigator site.Mean-calculations were done for all questions. Higher value indicates more disease burden. Change from Baseline is the value at Week 52 minus value at Baseline. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionhours (Mean)
Total outpatients hours:Baseline(n=9,13)Total inpatient hours:Baseline(n=5,8)Total outpatients hours:Change at Week 52(n=4,9)Total inpatient hours:Change at Week 52(n=0,3)
Risperidone Long Acting Injectables1.71.40.10.0
Risperidone Tablets1.61.4-0.2-1.0

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Change From Baseline in Theory of Mind (TOM) Scale Score at Week 52

The TOM scale is used to assess the ability of participant to infer other's mental states. It includes recognition that other individuals experience thoughts, feelings, intentions, and desires. It is measured by cartoon task, score ranging from 0-30 and stork task which includes stork task set A (false belief), stork task set B (double bluff, white lie, persuasion, misunderstanding), and physical story, score ranging from 0-12, 0-26 and 0-24 respectively. Higher score indicates improvement. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
Cartoon task:Baseline (n=11,13)Stork Task Set A: Baseline (n=9,12)Stork Task Set B: Baseline (n=11,14)Cartoon task:Change at Week 52(n=7,11)Stork Task Set A:Change at Week 52(n=7,11)Stork Task Set B:Change at Week 52(n=4,8)Physical story: Baseline (n=11,14)Physical story:Change at Week 52(n=7,11)
Risperidone Long Acting Injectables13.86.014.25.01.01.012.01.4
Risperidone Tablets18.56.615.52.70.81.513.62.1

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Change From Baseline in Social Functioning Scale (SFS) Score at Week 52

Social Functioning Scale (SFS) scores from 0 to 223 wherein, following categories were involved: Social Engagement (Score Range 0-15); Interpersonal Communication (Score Range 0-9); Recreational Activities (Score Range 0-45); Social Activities (Score Range 0-66; Independence Competence (Score Range 0-39); Independence Performance (Score Range 0-39); Occupational Activity (Score Range 0-10). Total score is sum of all sub scores and higher score indicates better level of social functioning. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
Baseline (n=16, 23)Change at Week 52 (n=4,14)
Risperidone Long Acting Injectables99.62.3
Risperidone Tablets103.59.6

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Change From Baseline in Simpson and Angus Rating Scale (SAS) Score at Week 52

The SAS rates 10 items from 0 (normal) to 4 (extreme), including gait, arm dropping, shoulder shaking, elbow rigidity, wrist rigidity, leg pendulousness, head rotation, Glabellar tap, tremor and salivation. The SAS global score is the average score (total sum of items score divided by the number of items) and ranges between 0 and 4, where the higher score denotes more severe condition of extra pyramidal symptoms. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Median)
Baseline (n=20,25)Change at Week 52 (n=19,22)
Risperidone Long Acting Injectables00
Risperidone Tablets00

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Change From Baseline in Verbal Working Memory (VWM) Response Based on Neurocognitive Function Test (NCFT) at Week 52

The NCFT is neuropsychological test which measures psychological functions. The VWM was measured by Korean-Wechsler Adults Intelligence Scale (K-WAIS), which consists of two subscales, the Verbal scale (6 subtests) and the Performance scale (5 subtests). The verbal tests were: information, comprehension, arithmetic, digit span, similarities, and vocabulary. Arithmetic and Digit Span test of Verbal WAIS scales was conducted. Arithmetic test (arithmetic questions were asked orally) involved calculations that measured concentration while manipulating mental mathematical problems. Digit span test (children were asked to repeat the orally given sequences of numbers either as heard or in reverse order) measured attention, concentration, and mental control. Here, mean number of correct responses in limited time period are reported for arithmetic (calculation) and Digit span. Increase in number of correct response indicates improvement. (NCT00992407)
Timeframe: Baseline and Week 52

,
InterventionCorrect responses (Mean)
VWM (Calculation):Baseline (n=11,14)VWM (Numbers):Baseline (n=11,14)VWM (Calculation):Change at Week 52 (n=7,12)VWM (Numbers):Change at Week 52 (n=7,12)
Risperidone Long Acting Injectables7.511.62.01.3
Risperidone Tablets9.311.81.02.3

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Change From Baseline in Global Assessment of Functioning (GAF) Test Score at Week 52

The GAF is a 100-point tool rating overall psychological, social and occupational functioning of adults. The higher score range (91 to 100) refers to a superior functioning in a wide range of activities, and absence of symptoms. The lower score range (1 to 10) refers to persistent danger of severely hurting self or others; or persistent inability to maintain minimum personal hygiene; or serious suicidal act with clear expectation of death. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
Baseline (n=17,24)Change at Week 52 (n=8,17)
Risperidone Long Acting Injectables58.35.4
Risperidone Tablets63.45.7

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Change From Baseline in Working Memory Based on Neurocognitive Function Test (NCFT) at Week 52

The NCFT is neuropsychological test which measures psychological functions. Working memory was assessed using Controlled Oral Word Association Test (COWAT) which measured verbal fluency and is a sub-test of the multilingual aphasia examination. The COWAT uses the three letter set of C, F, and L to assess phonemic fluency. Individuals are given 1 minute to name as many words as possible beginning with one of the letters. The procedure is then repeated for the remaining two letters. More words indicate improvement. (NCT00992407)
Timeframe: Baseline and Week 52

,
InterventionWords (Mean)
WM (Digital Span):Baseline (n=10,12)WM (Coris Block): Baseline (n=8,13)WM (Digital Span):Change at Week 52 (n=6,10)WM (Coris Block): Change at Week 52 (n=5,9)
Risperidone Long Acting Injectables11.610.51.04.6
Risperidone Tablets14.314.90.5-0.7

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Change From Baseline in Scale to Assess Unawareness of Mental Disorder (SUMD) Score at Week 52

The SUMD scale is a semi-structured scale that assesses participant's awareness of and insight into their illness, that is, the present level of insight. SUMD total score ranges from 0-27, with higher scores indicating poorer insight. The scale consists of nine items score ranging from 1 to 3, with higher scores indicating poorer insight. Score for each item is summed to produce the total score. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
Baseline (n=17,24)Change at Week 52 (n=6,17)
Risperidone Long Acting Injectables12.1-4.8
Risperidone Tablets10.6-3.5

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Change From Baseline in Psychosocial Well-being Index (PWI) Score at Week 52

Psychosocial Well-being Index (PWI) is a questionnaire about how the participant feels and how the things had been going with them. Total score ranges from 0 to 135, where lower score indicates worsening. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
Baseline (n=16,22)Change at Week 52 (n=9,18)
Risperidone Long Acting Injectables93.810.7
Risperidone Tablets96.00.7

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Change From Baseline in Members for Outpatients, Members Visiting Inpatients, Affected Members and Visiting Inpatients at Week 52

Healthcare economics questionnaire consists of 13-Questions, which measured disease burden on participant; out of which 4 questions are related to number of members for outpatients, number of members visiting inpatients, number of affected members and number of visiting inpatients. Mean-calculations were done for all questions. Higher value indicates more disease burden. Change from Baseline is the value at Week 52 minus value at Baseline. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionparticipants (Mean)
Members for outpatients:Baseline(n=13,16)Members visiting inpatients (MVI):Baseline(n=6,9)Affected members:Baseline(n=11,14)Visiting inpatients:Baseline(n=7,8)Members for outpatients:Change at Week 52(n=8,13)MVI:Change at Week52(n=0,3)Affected members:Change at Week52(n=4,10)Visiting inpatients:Change at Week52(n=0,3)
Risperidone Long Acting Injectables0.82.20.66.0-0.30-0.30
Risperidone Tablets0.72.90.76.1-0.3-2.7-0.4-5.0

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Change From Baseline in Emotional & Social Functioning Scale (SFS) Score at Week 52

For emotional and SFS, mean scores of neuroticism-extroversion-openness (NEO) personality test, relationship style questionnaire (RSQ), state-trait anger expression inventory (STAXI), positive affect and negative affect schedule (PANAS), emotional intelligence (EI), beck depression inventory (BDI), and beck anxiety inventory (BAI) scales were calculated. Score ranges for each category as:60-300 for NEO, 30-150 for RSQ, 20-80 for STAXI, 20-100 for PANAS, 8-172 for EI, 0-63 for BDI and BAI. Higher score indicates improvement. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
NEO personality test: Baseline (n=16,21)EI: Baseline (n=16,21)RSQ: Baseline (n=16,21)STAXI: Baseline (n=16,21)PANAS: Baseline (n=16,21)BDI: Baseline (n=16,21)BAI: Baseline (n=16,21)NEO personality test:Change at Week 52 (n=9,17)RSQ: Change at Week 52 (n=9,17)STAXI:Change at Week 52 (n=9,17)PANAS: Change at Week 52 (n=9,17)EI: Change at Week 52 (n=9,17)BDI:Change at Week 52 (n=9,17)BAI: Change at Week 52 (n=9,17)
Risperidone Long Acting Injectables178.7151.484.137.455.114.817.9-1.1-4.10.3-2.82.21.70.9
Risperidone Tablets173.7152.987.131.751.016.915.32.2-8.5-0.2-2.82.4-6.3-3.9

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Change From Baseline in Drug Attitude Inventory-10 (DAI-10) Score at Week 52

The DAI-10 is a 10-item questionnaire to assess 1) subjective experience of drug and 2) attitudes and beliefs toward neuroleptics which may influence compliance in schizophrenia participants. Score ranges from (-) 10 to 10. It is the binary scale assessing the participant's subjective response. A 'compliant' response is scored as +1; a dysphoric response is scored as -1. A positive sum of items indicates a positive subjective response (SR); a negative sum of scores indicates a negative SR (non-compliant). (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
Baseline (n=15,18)Change at Week 52 (n=7,15)
Risperidone Injection4.1-4.7
Risperidone Tablet5.0-1.1

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Change From Baseline in Days of Hospitalization, Number of Days Affected by Participants and Family, at Week 52

Healthcare economics questionnaire consists of 13-Questions, which measured disease burden on participant; out of which 3 questions are related to days of hospitalization, number of days affected by participants and family per participant within reporting interval score. Mean-calculations were done for all questions. Change from Baseline is the value at Week 52 minus value at Baseline. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventiondays (Mean)
Hospitalization days:Baseline(n=11,18)Days affected:Baseline(n=8,11)Family affected days:Baseline(n=9,12)Hospitalization days:Change at Week 52(n=3,12)Days affected:Change at Week 52(n=3,10)Family affected days:Change at Week 52(n=4,10)
Risperidone Long Acting Injectables19.434.02.9-14.0-30.0-0.3
Risperidone Tablets9.824.32.0-10.0-25.3-1.5

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Score at Week 52

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT00992407)
Timeframe: Baseline and Week 52

,
Interventionunits on a scale (Mean)
BaselineChange at Week 52
Risperidone Long Acting Injectables78.0-11.7
Risperidone Tablets69.5-13.0

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Height (cm) Z-score at Study Visit

Height (cm) measured at the study visit was converted to a Z-score based on the US Center for Disease Control 2000 growth charts for US subjects and European growth charts for ex-US subjects. A z-score indicates how many standard deviations a subject is away from the expected height for the subject's age and gender. (NCT01050582)
Timeframe: One single study visit, approximately one week after informed consent has been obtained

Interventionz-score (Mean)
Risperidone0.40
Other Atypical Antipsychotics0.09

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Age (Years) at Current Tanner Stage

Tanner stage is an evaluation of pubertal development with values ranging from 1 (pre-pubertal) to 5 (adult). A standardized, validated tool containing standardized pictures and written descriptions of the stages of pubic hair development, breast development for girls, and genital development for boys was used by physicians to make their assessment. (NCT01050582)
Timeframe: One single study visit, approximately one week after informed consent has been obtained

,
Interventionyears (Mean)
Tanner Stage 1Tanner Stage 2Tanner Stage 3Tanner Stage 4Tanner Stage 5
Other Atypical Antipsychotics10.311.212.215.015.0
Risperidone10.211.313.114.915.1

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Time to First Treatment Failure

Time to first treatment failure was the time from participant randomization to the first treatment failure, which was a composite endpoint consisting of any of the following events: arrest/incarceration, psychiatric hospitalization, discontinuation of antipsychotic treatment due to safety or tolerability, treatment supplementation with another antipsychotic due to inadequate efficacy, discontinuation of antipsychotic treatment due to inadequate efficacy, increase in level of psychiatric services to prevent imminent psychiatric hospitalization, suicide. A Treatment Failure Event Monitoring Board (EMB), blinded to individual participant treatment assignment, determined the occurrence and date of the first treatment failure event. (NCT01157351)
Timeframe: From date of randomization up to Month 15

InterventionDays (Median)
Paliperidone Palmitate416
Oral Antipsychotics226

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Percentage of Participants in Each Event Category of First Treatment Failure

First treatment failure was a composite endpoint consisting of any of the following events: arrest/incarceration, psychiatric hospitalization, discontinuation (D/C) of antipsychotic treatment due to safety or tolerability, treatment supplementation with another antipsychotic due to inadequate efficacy, discontinuation of antipsychotic treatment due to inadequate efficacy, increase in level of psychiatric services to prevent imminent psychiatric hospitalization, suicide. A Treatment Failure Event Monitoring Board (EMB), blinded to individual participant treatment assignment, determined the occurrence and date of the first treatment failure event. Percentage of participants who experienced treatment failure due to any event and for each specific category of event were assessed. (NCT01157351)
Timeframe: From date of randomization up to Month 15

,
Interventionpercentage of participants (Number)
Treatment Failure Due to Any EventArrest/incarcerationPsychiatric hospitalizationD/C due to safety/tolerabilityTreatment supplementationD/C due to inadequate efficacyIncrease in level of psychiatric servicesSuicide
Oral Antipsychotics53.729.411.93.72.84.11.80
Paliperidone Palmitate39.821.28.06.62.20.41.30

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Change From Baseline in Clinical Global Impression - Severity (CGI-S) Score During Overall Treatment Duration

The CGI-S rating scale was a 7-point global assessment of symptom severity with scores determined by clinician as follows: 1=Not ill, 2=Very Mild, 3= Mild, 4= Moderate, 5= Marked, 6= Severe, and 7= Extremely Severe. The higher the score the worse the illness. (NCT01157351)
Timeframe: Baseline up to Month 15

InterventionUnits on a scale (Least Squares Mean)
Paliperidone Palmitate-0.48
Oral Antipsychotics-0.43

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Change From Baseline in Personal and Social Performance (PSP) Total Score During Overall Treatment Duration

The PSP score assesses the degree of difficulty a participant exhibit over a 1 month period within 4 domains of behavior: a) socially useful activities, b) personal and social relationships, c) self-care, and d) disturbing and aggressive behavior. The investigators rate participants' degree of difficulty in each of the 4 domains using a 6-point Likert scale (from 0=absent to 5=very severe). The domain ratings were then transformed to PSP total score ranging from 1 to 100. Higher PSP total scores denote better functioning. A score between 71 and 100 represents normal to mild degree of dysfunction; a score between 31 and 70 represents varying degree of difficulty; and a score <=30 represents poor function that requires intensive supervision. (NCT01157351)
Timeframe: Baseline up to Month 15

InterventionUnits on a scale (Least Squares Mean)
Paliperidone Palmitate5.75
Oral Antipsychotics5.36

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Time to First Psychiatric Hospitalization

"A time-to parameter looking only at 1 component event of treatment failure: psychiatric hospitalization. Time to first psychiatric hospitalization was admission date of the psychiatric hospitalization recorded in the Assessment of Treatment Failure - Psychiatric Hospitalization." (NCT01157351)
Timeframe: From date of randomization up to Month 15

InterventionDays (Median)
Paliperidone PalmitateNA
Oral AntipsychoticsNA

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Time to First Psychiatric Hospitalization or Arrest/Incarceration

A time to parameter looking only at 2 component events of treatment failure: arrest or incarceration, and psychiatric hospitalization. An arrest was defined as the taking of a participant into custody by legal authority, for any reason. Incarceration was defined as involuntary confinement by an officer of the law. Psychiatric hospitalization was an inpatient psychiatric hospitalization that occurred due to the participant's clinically significant worsening of symptoms of schizophrenia. (NCT01157351)
Timeframe: From date of randomization up to Month 15

InterventionDays (Median)
Paliperidone PalmitateNA
Oral Antipsychotics274

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Number of Participants With Response to Columbia-Suicide Severity Rating Scale (C-SSRS)

"Data relevant to the assessment of suicidality is mapped to the Columbia Classification Algorithm of Suicide Assessment (C-CASA) event codes. C-SSRS assesses whether participant experiences following: suicide attempt (Event code 2) (Response of Yes on actual attempt), preparatory acts toward imminent suicidal behavior (Event code 3) (Yes on aborted attempt, interrupted attempt, preparatory acts or behavior), suicidal ideation (Event code 4) (Yes on wish to be dead, non-specific active suicidal thoughts, active suicidal ideation with methods without intent to act/some intent to act without specific plan or with specific plan and intent), self-injurious behavior, no suicidal intent (Event code 7) (Yes on Has participant engaged in non-suicidal self-injurious behavior). Number of participants with Yes response for above mentioned categories are assessed. Baseline is defined as the Week 0 measurement." (NCT01175135)
Timeframe: Baseline, Week 1, 2, 3, 4, Follow-up (FU) (7 to 10 days after administration of last dose of study medication)

,,,
Interventionparticipants (Number)
Baseline: Event code 2Baseline: Event code 3Baseline: Event code 4Baseline: Event code 7Week 1: Event code 2Week 1: Event code 3Week 1: Event code 4Week 1: Event code 7Week 2: Event code 2Week 2: Event code 3Week 2: Event code 4Week 2: Event code 7Week 3: Event code 2Week 3: Event code 3Week 3: Event code 4Week 3: Event code 7Week 4: Event code 2Week 4: Event code 3Week 4: Event code 4Week 4: Event code 7FU: Event code 2FU: Event code 3FU: Event code 4FU: Event code 7
PF-02545920 15 mg104101400030002000300000
PF-02545920 5 mg111000000010000000300010
Placebo123000000010001000000000
Risperidone 3 mg001000000000000000100010

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Number of Participants With Clinically Significant Findings in Vital Signs and Electrocardiogram (ECG)

Clinically significant findings based on investigator's discretion were assessed in vital sign parameters (including pulse rate, blood pressure and body temperature) and ECG parameters (including respiratory rate, heart rate, PR interval, QRS interval, QT interval, QT corrected using Bazett's correction [QTcB] interval, and QT corrected using Fridericia's correction [QTcF]). (NCT01175135)
Timeframe: Baseline up to end of study (7 to 10 days after administration of last dose of study medication)

Interventionparticipants (Number)
PF-02545920 5 mg0
PF-02545920 15 mg0
Risperidone 3 mg0
Placebo0

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Number of Participants With Clinically Significant Laboratory Test Abnormalities for Fasting Insulin, High Density Lipoprotein (HDL), Low Density Lipoprotein (LDL), Cholesterol, Triglycerides, Hemoglobin Type A1c (HbA1c) and Prolactin

Clinically significant findings based on investigator's discretion were assessed in laboratory parameters (including fasting insulin, high-density lipoprotein [HDL], low-density lipoprotein [LDL], Cholesterol, Triglycerides, glycosylated hemoglobin type A1c [HbA1c] and Prolactin). (NCT01175135)
Timeframe: Day 1 up to Week 4

Interventionparticipants (Number)
PF-02545920 5 mg0
PF-02545920 15 mg0
Risperidone 3 mg0
Placebo0

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Number of Participants With Laboratory Test Abnormalities

Criteria for abnormality:hematology: hemoglobin, hematocrit, red blood cell count: less than(<) 0.8*lower limit of normal (LLN); mean corpuscular volume; mean corpuscular hemoglobin, mean corpuscular hemoglobin concentration: <0.9*LLN,>1.1*upper limit of normal (ULN); platelets: <0.5*LLN,>1.75*ULN, white blood cell count: <0.6*LLN, >1.5*ULN; lymphocytes, total neutrophils: <0.8*LLN, >1.2*ULN; eosinophils, basophils, monocytes: >1.2*ULN; coagulation: activated partial thromboplastin time, prothrombin, prothrombin international ratio: >1.1*ULN; liver function: bilirubin: >1.5*ULN; aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase: >3.0*ULN; protein, albumin: <0.8*LLN>1.2*ULN; renal function:blood urea nitrogen,creatinine: >1.3*ULN; uric acid: >1.2*ULN; electrolytes: sodium, potassium, chloride, calcium, bicarbonate: <0.9*LLN,>1.1*ULN; urinalysis: pH<4.5, >8; glucose, protein, blood, ketones, urobilinogen, bilirubin, nitrite; Other(glucose: <0.6*LLN,>1.5*ULN) (NCT01175135)
Timeframe: Screening up to end of study (7 to 10 days after administration of last dose of study medication)

Interventionparticipants (Number)
PF-02545920 5 mg55
PF-02545920 15 mg58
Risperidone 3 mg34
Placebo56

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Proportion of Participants With Dystonia Adverse Events

Participants were assessed for presence of symptoms for any one of the following: dystonia, oromandibular dystonia, and oculogyric crisis. (NCT01175135)
Timeframe: Baseline up to end of study (7 to 10 days after administration of last dose of study medication)

Interventionproportion of participants (Number)
PF-02545920 5 mg0.01
PF-02545920 15 mg0.08
Risperidone 3 mg0.00
Placebo0.04

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Change From Baseline in Abdominal Girth at Week 4

(NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventioncentimeter (cm) (Mean)
BaselineChange at Week 4
PF-02545920 15 mg97.20.70
PF-02545920 5 mg96.50.71
Placebo93.50.74
Risperidone 3 mg95.63.33

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Change From Baseline in Body Weight at Week 4

(NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionkilogram (kg) (Mean)
BaselineChange at Week 4
PF-02545920 15 mg87.5-1.23
PF-02545920 5 mg86.10.18
Placebo84.31.04
Risperidone 3 mg83.92.69

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Change From Baseline in Global Assessment of Functioning (GAF) Score at Week 4

GAF is a 100-point, clinician rated single item scale that rates the severity of illness-related impairment in psychological, social and occupational functioning of participants on a hypothetical continuum of mental illness to mental health. The scale values range from 1 to 100 with lower score indicating greater severity of illness and is divided into 10 equal intervals (descriptors): from 1-10 (persistent danger of hurting self - serious suicidal acting with clear expectations of death) to 91-100 (superior functioning - no symptoms). Each descriptor has a nine-point range to allow for some variability of severity within the descriptor. (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 4
PF-02545920 15 mg38.56.9
PF-02545920 5 mg38.46.3
Placebo38.26.3
Risperidone 3 mg38.77.7

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Change From Baseline in Clinical Global Impression - Severity (CGI-S) Score at Week 4

"CGI-S: 7-point clinician rated scale to assess severity of participant's current illness state. Clinician responded to a question Considering your total clinical experience with this particular population, how mentally ill is your patient at this time? on the following scores: 1 (normal - not ill at all), 2 (borderline mentally ill), 3 (mildly ill), 4 (moderately ill), 5 (markedly ill), 6 (severely ill), 7 (among the most severely ill participants). Higher score = more affected." (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 4
PF-02545920 15 mg5.0-0.7
PF-02545920 5 mg5.0-0.7
Placebo5.0-0.6
Risperidone 3 mg4.9-0.8

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Change From Baseline in Extrapyramidal Symptom Rating Scale-Abbreviated (ESRS-A) Parameter Scores at Week 4

ESRS-A is a clinician rated scale consisting of 24 items to assess severity of extra-pyramidal symptoms for following parameters: parkinsonism (10 items), dystonia (6 items), dyskinesia (6 items) and akathisia (2 items). Each item is scored on a 6-point Likert scale (0=absent, 1=minimal, 2=mild, 3=moderate, 4=severe, 5=extreme). Total score for a parameter is average of individual item scores included under the parameter, ranging from 0 to 5, with higher score = more affected. (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
Baseline: ParkinsonismBaseline: DystoniaBaseline: DyskinesiaBaseline: AkathisiaChange at Week 4: ParkinsonismChange at Week 4: DystoniaChange at Week 4: DyskinesiaChange at Week 4: Akathisia
PF-02545920 15 mg0.5000.0000.0950.0680.0860.2070.2070.328
PF-02545920 5 mg0.2570.0950.1220.1620.1430.0000.0160.032
Placebo0.4730.0270.1350.243-0.1900.032-0.032-0.095
Risperidone 3 mg0.1940.0000.1940.111-0.0380.0000.0380.154

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Number of Participants With Abnormal White Blood Cell (WBC) Count and Absolute Neutrophil Count (ANC)

Pre-defined criteria was established for WBC Count (less than 0.6 times the lower limit of normal) and absolute neutrophil count (less than 0.8 times the lower limit of normal) to define the values that would be identified as abnormal. (NCT01175135)
Timeframe: Day 1 up to Week 4

,,,
Interventionparticipants (Number)
WBCANC
PF-02545920 15 mg06
PF-02545920 5 mg06
Placebo08
Risperidone 3 mg00

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 4

PANSS assesses the positive symptoms, negative symptoms, and general psychopathology specifically associated with schizophrenia. The scale consists of 30 items. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). The sum of the 30 items is defined as the PANSS total score and ranges from 30 to 210; higher score indicates greater severity. (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 4
PF-02545920 15 mg97.7-13.8
PF-02545920 5 mg98.1-15.3
Placebo97.2-12.6
Risperidone 3 mg97.4-17.9

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Positive, Negative, and General Subscales Score at Week 4

PANSS - positive, negative, and general subscales assesses positive, negative and general psychopathological symptoms associated with schizophrenia respectively. Seven (7) items each make up the positive scale (for example; delusions, conceptual disorganization, and hallucinatory behavior) and negative scale (for example; blunted affect, emotional withdrawal, poor rapport, passive/apathetic social withdrawal) and 16 items make up the general scale (for example; somatic concern, anxiety, guilt feelings, mannerisms and posturing, motor retardation, uncooperativeness, disorientation, poor impulse control, pre-occupation). Each item is rated on a 7-point Likert scale from 1 (symptom not present) to 7 (symptoms extremely severe). Total scores range for positive as well as negative subscale is 7 to 49 and for general subscale is 16 to 112; higher subscale score indicates greater severity. (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
Baseline: Positive ScoreBaseline: Negative ScoreBaseline: General ScoreChange at Week 4: Positive ScoreChange at Week 4: Negative ScoreChange at Week 4: General Score
PF-02545920 15 mg26.123.448.2-4.5-2.2-7.1
PF-02545920 5 mg26.923.447.9-5.0-2.7-7.5
Placebo26.823.247.2-4.5-1.5-6.6
Risperidone 3 mg26.624.046.8-6.7-2.7-8.6

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Marder Factors Score at Week 4

PANSS is a 30-item scale to assess the neuropsychiatric symptoms of schizophrenia. The symptoms are rated on a 7-point scale from 1 (absent) to 7 (extreme psychopathology). PANSS Marder positive symptoms subscale consists of 8 items with total score equal to sum of 8 items ranging from 8-56; Marder negative symptoms subscale and Marder disorganized thoughts (Dis. Thought) subscale, each consists of 7 items with total score equal to sum of 7 items each, ranging from 7-49, Marder uncontrolled hostility/excitement (Uncon. Hos/Exc) subscale and Marder anxiety/depression (Anx/Dep) subscale, each consists of 4 items with total score equal to sum of 4 items each ranging from 4-28. Higher subscale score indicates greater severity. (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
Baseline: Positive scoreBaseline: Negative ScoreBaseline: Dis. Thought ScoreBaseline: Uncon. Hos/Exc ScoreBaseline: Anx/Dep ScoreChange at Week 4: Positive scoreChange at Week 4: Negative ScoreChange at Week 4:Dis. Thought ScoreChange at Week 4:Uncon.Hos/ExcScoreChange at Week 4: Anx/DepScore
PF-02545920 15 mg30.623.321.09.813.0-5.0-2.9-2.3-0.9-2.6
PF-02545920 5 mg30.923.020.410.413.5-5.5-3.0-2.5-1.2-2.9
Placebo31.023.020.310.012.9-4.6-2.3-1.9-1.0-2.9
Risperidone 3 mg30.322.921.310.612.4-6.2-2.5-3.0-2.4-3.8

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) - Derived Brief Psychiatric Rating Scale (BPRS) Core Score at Week 4

PANSS is a 30-item scale to assess the neuropsychiatric symptoms of schizophrenia. PANSS derived BPRS is an 18-item clinician rated scale which assesses symptoms such as hostility, suspiciousness, hallucinations, grandiosity, and a number of other psychiatric symptoms. Items scored on a 7-point scale (1=not present and 7=extremely severe), with higher score indicating greater severity of symptom. BPRS core score consists of 4 items (Conceptual disorganization, Hallucinatory behavior, Suspiciousness/persecution, Unusual thought content) with total score equal to sum of the 4 items, ranging from 4 to 28, with higher score indicating greater severity. (NCT01175135)
Timeframe: Baseline, Week 4

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 4
PF-02545920 15 mg17.3-3.4
PF-02545920 5 mg17.4-3.7
Placebo17.3-3.2
Risperidone 3 mg17.2-4.7

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Treatment Satisfaction Questionnaire for Medication (TSQM) Score

TSQM assesses the participant's level of satisfaction with study medication. It consists of a 14-item questionnaire which comprises of 3 specific scales (effectiveness, side effects, convenience) and 1 global satisfaction scale. Effectiveness, convenience and global satisfaction scale are rated on a 7-point scale (0= Extremely Dissatisfied, 1= Very Dissatisfied, 2= Dissatisfied, 3= Somewhat Satisfied, 4= Satisfied, 5= Very Satisfied, 6= Extremely Satisfied) and side effects are rated on a 5-point scale (0= Extremely Dissatisfied, 1=Very Dissatisfied, 2= Somewhat Dissatisfied, 3= Slightly Dissatisfied, 4= Not at all Dissatisfied). Scale scores are transformed into scores ranging from 0 to 100, with a higher score indicating more satisfaction. (NCT01175135)
Timeframe: Week 4

,,,
Interventionunits on a scale (Mean)
EffectivenessSide-EffectsConvenienceGlobal Satisfaction
PF-02545920 15 mg51.9079.2068.3751.02
PF-02545920 5 mg53.6886.4370.4656.84
Placebo53.7087.4166.8349.48
Risperidone 3 mg63.3787.3075.6966.07

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Number of Participants With Clinically Significant Changes in Physical Examinations

Clinically significant findings in physical examinations based on investigator's discretion were assessed. Screening was the 7 day time (from Day -8 to Day -2) before dosing on Day 1. Number of participants with clinically significant changes in physical examinations compared to screening was assessed. (NCT01175135)
Timeframe: Screening, Week 4

Interventionparticipants (Number)
PF-02545920 5 mg0
PF-02545920 15 mg0
Risperidone 3 mg0
Placebo0

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Clinical Global Impression - Improvement (CGI-I) Score

"CGI-I: 7-point clinician rated scale ranging from 1 (very much improved) to 7 (very much worse). Clinician responded to a question: Compared to your subject's condition at the beginning of treatment, how much has your subject changed? Compared to Baseline (Day 1), improvement was defined as score of 1 (very much improved), 2 (much improved), or 3 (minimally improved) on the scale. Higher score = more affected." (NCT01175135)
Timeframe: Week 4

Interventionunits on a scale (Mean)
PF-02545920 5 mg3.1
PF-02545920 15 mg3.3
Risperidone 3 mg2.7
Placebo3.2

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Change From Baseline in Movement Disorder Burden Score for Dystonia (MDBS-D) at Week 4

MDBS-D score reflects the numbers and durations of movement disorder adverse events for dystonia, the severity of the events, required treatment, and the total number of days the participant received study treatment. MDBS-D score = (S * D * C)/TTD; where S= Movement Disorder Severity Score for Dystonia (possible values: 1 [mild]; 2 [moderate]; 3 [severe]), D=adverse event duration (in days), C=concomitant medication factor (C=1.5 if an anti-cholinergic or beta blocker is used for the treatment of a movement disorder; C=1 if no concomitant medication is used), TTD=total treatment days for the participant. Value for MDBS score may range from zero to infinity. A higher MDBS-D score indicates a greater movement disorder adverse event liability compared to baseline. (NCT01175135)
Timeframe: Baseline, Week 4

Interventionunits on a scale (Mean)
PF-02545920 5 mg0.0019
PF-02545920 15 mg0.0163
Risperidone 3 mg0.0000
Placebo0.0126

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Assessment of Adverse Events by Objective Rating Scales and Self Report Scales

"DIEPSS(Drug-Induced Extrapyramidal Symptoms Scale), VAS(Visual analog scale);mental sedation (alert-drowsy, muzzy-clear headed, mentally slow-quick witted, attentive-dreamy), physical sedation (strong-feeble, well coordinated-clumsy, lethargic-energetic, incompetent-proficient), tranquilization (calm-excited, contented-discontented, troubled-tranquil, tense-relaxed), and other types of feelings (happy-sad, antagonistic-amicable, interested-bored, withdrawn-gregarious) Minimum of VAS(Mental sedation score,Physical sedation score,Total score) is 0, Maximum is 10.~VAS-total score is average of all subscale scores. Minimum of DIEPSS is 0, Maximum is 4. The higher number is worse outcome. The score ranges are for subscale score. This outcome measure is reporting a change between baseline and 2hr after third medication." (NCT01284959)
Timeframe: baseline and 2hr after third medication

,,
Interventionunits on a scale (Mean)
VAS-Total scoreVAS-Mental sedation scoreVAS-Physical sedation scoreDIEPSS-Bradykinesia score
Paliperidone ER4.114.784.080.20
Placebo3.353.853.230.08
Risperidone5.416.055.780.60

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Assessment of Adverse Events by Objective Rating Scales and Self Report Scales

DIEPSS(Drug-Induced Extrapyramidal Symptoms Scale), VAS(Visual analog scale);mental sedation (alert-drowsy, muzzy-clear headed, mentally slow-quick witted, attentive-dreamy), physical sedation (strong-feeble, well coordinated-clumsy, lethargic-energetic, incompetent-proficient), tranquilization (calm-excited, contented-discontented, troubled-tranquil, tense-relaxed), and other types of feelings (happy-sad, antagonistic-amicable, interested-bored, withdrawn-gregarious) Minimum of VAS is 0, Maximum is 10 Minimum of DIEPSS is 0, Maximum is 4 The higher number is worse outcome. The score ranges are for subscale score. This outcome measure is reporting a change between baseline and 50hr after third medication. (NCT01284959)
Timeframe: baseline and 50hr after third medication

,,
Interventionunits on a scale (Mean)
VAS-Total scoreVAS-Mental sedation scoreVAS-Physical sedation scoreDIEPSS-Bradykinesia score
Paliperidone ER3.423.603.350.10
Placebo3.744.213.690
Risperidone6.156.536.250.25

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Assessment of Cognitive Functioning-1

"CNT(Computerized Neuro-Cognitive Function Test System); The tests included a word fluency test. All of the assessments except the CNT were conducted immediately prior to administration of the medication and at 2 (for risperidone and placebo) or 24 h (for paliperidone ER) after the first and third administrations of the study medications.~Minimum of Wisconsin card sorting test-Category completed is 0, Maximum is 6, the lower number is worse outcome.~Minimum of Wisconsin card sorting test-Perseverative response and Trials to complete is 0, Maximum is 128, the lower number is worse outcome.~Minimum of Wisconsin card sorting test-Perseverative error is 0, Maximum is 128, the higher number is worse outcome.~Minimum of Word-fluency test is 0 and no maximum value, the higher number is better outcome.~The score ranges are for subscale score. This outcome measure is reporting a change between baseline and 50hr after third medication." (NCT01284959)
Timeframe: baseline and 50hr after third medication

,,
Interventionscores on a scale (Mean)
Word-fluency test-AnimalWord-fluency test-Stationery"Word-fluency test-ㄱ""Word-fluency test-ㅅ""Word-fluency test-ㅇ"
Paliperidone ER23.5023.6017.1016.4016.70
Placebo25.4226.0019.7518.2517.17
Risperidone22.2222.5617.4417.4416.11

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Assessment of Cognitive Functioning-2

"CNT(Computerized Neuro-Cognitive Function Test System); The tests included the Stroop test, Trail-Making Test B (TMT B). All of the assessments except the CNT were conducted immediately prior to administration of the medication and at 2 (for risperidone and placebo) or 24 h (for paliperidone ER) after the first and third administrations of the study medications Minimum of Stroop test is 0, no maximum limit, the higher number is worse outcome.~Minimum of Trail making test B is 0 and no maximum limit, the higher number is worse outcome.~The score ranges are for subscale score. This outcome measure is reporting a change between baseline and 50hr after third medication." (NCT01284959)
Timeframe: baseline and 50hr after third medication

,,
Interventionmilliseconds (Mean)
Stroop test-ColorStroop test-Word-colorStroop test-Interference scoreTrail making test B
Paliperidone ER12.6818.315.6331.10
Placebo13.0917.534.4428.42
Risperidone15.4021.846.4329.78

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Assessment of Cognitive Functioning-3

"CNT(Computerized Neuro-Cognitive Function Test System); The tests included Wisconsin Card-Sorting Test (WCST). All of the assessments except the CNT were conducted immediately prior to administration of the medication and at 2 (for risperidone and placebo) or 24 h (for paliperidone ER) after the first and third administrations of the study medications.~Minimum of Wisconsin card sorting test-Category completed is 0, Maximum is 6, the lower number is worse outcome.~Minimum of Wisconsin card sorting test-Perseverative response and Trials to complete is 0, Maximum is 128, the lower number is worse outcome.~Minimum of Wisconsin card sorting test-Trials to complete first category trials is 0, Maximum is 128 and minimum of Wisconsin card sorting test-Perseverative error is 0, Maximum is 128, the higher number is worse outcome.~The score ranges are for subscale score. This outcome measure is reporting a change between baseline and 50hr after th" (NCT01284959)
Timeframe: baseline and 50hr after third medication

,,
Interventiontrials (Mean)
Wisconsin card sorting test-Category completedWisconsin card sorting test-Perseverative responseWisconsin card sorting test-Perseverative errorWCST-Trials to complete first category trials
Paliperidone ER6.0010.106.5012.10
Placebo6.0013.089.6711.75
Risperidone6.0014.1110.0014.00

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Assessment of Negative Symptoms and Neuroleptic Induced Deficit Syndromes by Objective Rating Scales

"SANS(Scale for the Assessment of Negative Symptoms), NIDSS(Neuroleptic induced Deficit Syndrome Scale) In NIDSS, the average of number 1 to 5 is blunted affect, the average of number 16 to 20 is avolition, the average of number 6 to 15 is cognition, the average of all score is total.~Minimum of NIDSS(avolition, blunted affect, cognition, total) is -3, maximum is +3.(subscale score and total) '+' is better outcome, '-' is worse outcome. Minimum of SANS-Global score for alogia and blunted affect is 0, Maximum of SANS-Global score for alogia and blunted affect is 5 The higher number is worse outcome. The zeros are measured and Calcuated value This outcome measure is reporting a change between baseline and 2hr after third medication." (NCT01284959)
Timeframe: baseline and 2hr after third medication

,,
Interventionunits on a scale (Mean)
NIDSS-AvolitionNIDSS-Blunted AffectNIDSS-CognitionNIDSS-TotalSANS-Global score for alogiaSANS-Global score for blunted affect
Paliperidone ER-0.66-0.24-0.38-0.4200.10
Placebo-0.280.020.02-0.0600
Risperidone-1.30-0.70-0.54-0.770.670.67

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Symptoms Assessment by Objective Rating Scales

SANS(Scale for the Assessment of Negative Symptoms), NIDSS(Neuroleptic induced Deficit Syndrome Scale) Minimum of NIDSS is -3, maximum of NIDSS is +3. '+' is better outcome, '-' is worse outcome. Minimum of SNAS-Global score is 0, Maximum of SNAS-Global score is 5 The higher number is worse outcome. The zeros are measured and Calcuated value. The score ranges are for subscale score. This outcome measure is reporting a change between baseline and 50hr after third medication. (NCT01284959)
Timeframe: baseline and 50hr after third medication

,,
Interventionunits on a scale (Mean)
NIDSS-AvolitionNIDSS-Blunted AffectNIDSS-CognitionNIDSS-TotalSANS-Global score for alogiaSANS-Global score for blunted affect
Paliperidone ER0.140.040.280.1900
Placebo-0.37-0.27-0.26-0.2900
Risperidone-0.85-0.70-0.66-0.720.130.25

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Changes in the Irritability Subscale of the Larger ABC (Abberent Behavior Checklist) That Occur From Baseline to 10 Weeks

"Multi-center, blinded clinical trial to evaluate biomarkers as predictors of efficacy and safety in children with autistic disorder to risperidone, an atypical antipsychotic drug and aripiprazole, an antipsychotic having a unique clinical and receptor-binding profile.~The major outcome measure was the score on the Irritability subscale of the Aberrant Behavior Checklist (ABC-I) . The ABC has 58 items describing some aspect of behavior and the Irritability sub-scale has 15 items, each completed by a parent or caregiver under the supervision of an investigator. Scores on each item range from 0 = no problem and 3 = severe problem (range of total scores 0 to 45). A fall in scores indicates behavioral improvement." (NCT01333072)
Timeframe: baseline to 10 weeks

Interventionunits on a scale (Mean)
Risperidone12.7
Aripiprazole14.1

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Cognition

To evaluate the cognitive benefits of treatment with CYP-1020 (formerly known as BL-1020) compared to risperidone after 6 weeks of treatment in patients experiencing acute exacerbation of schizophrenia. Assessed by calculating difference between CYP-1020 and Risperidone on mean change from baseline to Week 6 endpoint on MATRICS Consensus Cognition Battery (MCCB) normative composite score. MCCB is a neuropsychological test battery that comprises 10 measures of 7 different cognitive areas including speed of processing, verbal learning, memory-verbal and non verbal reasoning and problem solving, visual learning, social cognition, attention/vigilance.The study was terminated after the interim analysis. MCBB total score ranges from -50 to 150. Change from Baseline by Visit (LOCF)Higher score means better cognitive functioning. (NCT01363349)
Timeframe: Baseline and 6 weeks

,
InterventionScores on a scale (Mean)
MCCB Baseline ScoreMCCB Week 6 Score
CYP-10208.713.5
Risperidone8.212.5

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Timeline Followback Assessing Number of Drinks Per Week

Alcohol/other substance use (including tobacco) will be assessed primarily by weekly self-report using the Timeline Followback (TLFB) method enhanced by procedures to strengthen the reliability and validity of this measure. It involves asking participants to retrospectively estimate their alcohol and other substance use. (NCT01411085)
Timeframe: Weekly for 14 weeks, using data from last 8 weeks

InterventionDrinks per week (Mean)
Risperidone + Desipramine35.9

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Change From Baseline in PANSS(Positive and Negative Syndrome Scale) Total Score at Week 8

Mean change in Positive and Negative Syndrome Scale total score from baseline to Week 8 at the end of treatment. PANSS is an interview-based measure of the severity of psychopathology in adults with psychotic disorders. It have 30 evaluation items, which include 7 positive sub-scale, 7 negative sub-scale and 16 general psychopathology sub-scale on a score of 1 to 7. The total score is the sum of the 30 scale items. The minimum score is 30 and the maximum score is 210. Patient with PANSS total scores<70 is the normal,but the scores>120 is more serious.Change=(Week 8 Score - Baseline score) (NCT01516424)
Timeframe: From baseline to the end of study、week 8(day 56)or before other antipsychotic taken.

,
Interventionscore on a scale (Mean)
ITT analysis: At the end of treatmentPPS analysis: At the end of treatment
Blonanserin-30.59-33.71
Risperidone-33.56-36.31

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Change in the Clinical Global Impression-Severity (CGI-S) Score at Week 6

CGI-S is a 7-point scale to assess the global severity of the participant's illness. CGI-S scores range from 1 (normal, not ill at all) to 7 (extremely ill). (NCT01625000)
Timeframe: Baseline and Week 6

Interventionunits on a scale (Least Squares Mean)
MP-214 3mg-0.7
MP-214 6mg-0.8
MP-214 9mg-0.7
Risperidone 4mg-1.2
Placebo-0.6

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Change in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 6

PANSS score is a 30-item rating scale to assess both the positive and negative symptom syndromes of patients with schizophrenia. Each item is scored on a 7-point scale, from 1 (absent) to 7 (extreme). The PANSS total score of the 30 PANSS items ranges from 30 to 210. High scores indicate greater severity of symptoms. (NCT01625000)
Timeframe: Baseline and Week 6

Interventionunits on a scale (Least Squares Mean)
MP-214 3mg-10.4
MP-214 6mg-13.8
MP-214 9mg-14.0
Risperidone 4mg-20.2
Placebo-9.5

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Number of Participants With Adverse Events as a Measure of Safety and Tolerability

(NCT01625897)
Timeframe: Up to 60 weeks

InterventionParticipants (Count of Participants)
MP-214 1.5-9mg78
Risperidone 2-12mg42

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Number of Participants With Adverse Events as a Measure of Safety and Tolerability

The Numbers show Subjects with at least one Adverse Event (NCT01626872)
Timeframe: Up to 60 weeks (Treatment Period (48 weeks) and Follow-up Period (12 weeks))

InterventionParticipants (Count of Participants)
MP-214 3mg67
MP-214 6mg92
MP-214 9mg50

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Average Over Time of Frequency of Cannabis Use

Frequency of cannabis use is obtained each week retrospectively as the number of days of cannabis use during the prior week (assessed using the Timeline Followback). Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT01639872)
Timeframe: 12 weeks

Interventiondays of cannabis use during prior week (Number)
Clozapine4.26
Risperidone4.58

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Average Over Time of Intensity of Cannabis Use (Used to Evaluate Treatment Efficacy)

Intensity of cannabis use is obtained each week retrospectively as the number of joints smoked during the prior week (assessed using the Timeline Followback). Mixed models are used to obtain estimates of efficacy from the partial data provided by each subject while adherent to assigned treatment (under the 'missing at random' assumption). The 'explanatory' estimands (target of the mixed model estimation) are defined in terms of population quantities that would have occurred had all subjects remained on assigned treatment throughout the study. The point estimate for each arm is reported under Number. (NCT01639872)
Timeframe: 12 weeks

Interventionjoints smoked during the prior week (Number)
Clozapine10.21
Risperidone10.2

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Total Risperidone PK: Percent Fluctuation Over the Secondary Peak

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~The degree of fluctuation of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cavg, expressed as a percentage.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionpercentage of average concentration (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg122.350101.788
Cohort 2, RBP-7000 90 mg122.042101.666
Cohort 3, RBP-7000 120 mg151.29496.489

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Total Risperidone PK: Percent Fluctuation Over the PK Profile

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~The degree of fluctuation of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cavg, expressed as a percentage.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionpercentage of average concentration (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg151.211108.226
Cohort 2, RBP-7000 90 mg135.238102.396
Cohort 3, RBP-7000 120 mg153.386114.008

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Total Risperidone PK: Minimum Plasma Concentration (Cmin) Over the Secondary Peak

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Minimum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg4.8675.028
Cohort 2, RBP-7000 90 mg5.64210.534
Cohort 3, RBP-7000 120 mg9.15913.735

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Total Risperidone PK: Minimum Plasma Concentration (Cmin) Over the PK Profile

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Minimum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg4.8675.028
Cohort 2, RBP-7000 90 mg5.64210.534
Cohort 3, RBP-7000 120 mg9.15911.938

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Total Risperidone PK: Maximum Plasma Concentration Over the Secondary Peak (Cmax)

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Maximum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29) Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg16.86717.885
Cohort 2, RBP-7000 90 mg21.41530.804
Cohort 3, RBP-7000 120 mg32.23538.300

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Risperidone PK: Maximum Plasma Concentration (Cmax) During Initial Peak

"Cmax determined directly from individual concentration-time data.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionng/mL (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg6.2804.955
Cohort 2, RBP-7000 90 mg5.4606.680
Cohort 3, RBP-7000 120 mg6.4707.145

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Total Risperidone PK: Average Plasma Concentration Over the Secondary Peak (Cavg, Day 2-29)

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~The average of plasma concentrations in the plateau, calculated as AUC Day 2-29/time~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg9.54812.710
Cohort 2, RBP-7000 90 mg11.93716.958
Cohort 3, RBP-7000 120 mg15.43423.896

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Total Risperidone PK: Average Plasma Concentration (Cavg) Over the PK Profile

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~The average of plasma concentrations calculated as AUCtau/ tau (tau = 28 days)~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg9.68212.749
Cohort 2, RBP-7000 90 mg12.34216.440
Cohort 3, RBP-7000 120 mg18.74223.784

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Total Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to Time Tau (Where Tau=28 Days) (AUCtau)

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~AUCtau calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionhr*ng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg6506.08567.1
Cohort 2, RBP-7000 90 mg8293.811047.7
Cohort 3, RBP-7000 120 mg12594.715982.6

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Total Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24)

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~AUC0-24 calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionhr*ng/mL (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg335.4276.5
Cohort 2, RBP-7000 90 mg437.5415.1
Cohort 3, RBP-7000 120 mg466.2497.5

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Total Risperidone PK: Area Under the Plasma Concentration-Time Curve From Day 2-29 Post Injection (AUC Day 2-29)

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Area under plasma concentration-time curve from 24 hours (Day 2) to the last quantifiable collection during dosing interval (28 days); calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 at time of study drug administration." (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionhr*ng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg6186.98236.4
Cohort 2, RBP-7000 90 mg7735.110988.6
Cohort 3, RBP-7000 120 mg10001.415484.3

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Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the Secondary Peak

"Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionhours (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg120.000204.000
Cohort 2, RBP-7000 90 mg216.000216.00
Cohort 3, RBP-7000 120 mg192.000180.000

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Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the PK Profile

"Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionhours (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg6.00018.000
Cohort 2, RBP-7000 90 mg168.000192.000
Cohort 3, RBP-7000 120 mg192.000180.000

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Risperidone PK: Time of Maximum Plasma Concentration (Tmax) During Initial Peak

"Tmax determined directly from individual concentration-time data.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionhours (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg6.0006.000
Cohort 2, RBP-7000 90 mg6.0006.000
Cohort 3, RBP-7000 120 mg4.0004.483

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Risperidone PK: Swing Over the Secondary Peak

"The swing of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cmin.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionratio (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg2.6443.736
Cohort 2, RBP-7000 90 mg2.6802.652
Cohort 3, RBP-7000 120 mg3.8132.698

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Risperidone PK: Swing Over the PK Profile

"The swing of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cmin.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionratio (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg4.5754.077
Cohort 2, RBP-7000 90 mg4.1512.863
Cohort 3, RBP-7000 120 mg4.9383.159

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Risperidone PK: Percent Fluctuation Over the Secondary Peak

"The degree of fluctuation of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cavg, expressed as a percentage.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionpercentage of average concentration (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg134.805136.691
Cohort 2, RBP-7000 90 mg134.898125.387
Cohort 3, RBP-7000 120 mg141.030138.380

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Risperidone PK: Percent Fluctuation Over the PK Profile

"The degree of fluctuation of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cavg, expressed as a percentage.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionpercentage of average concentration (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg190.745147.252
Cohort 2, RBP-7000 90 mg215.048140.688
Cohort 3, RBP-7000 120 mg173.609143.652

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Risperidone PK: Minimum Plasma Concentration (Cmin) Over the Secondary Peak

"Minimum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg0.8291.230
Cohort 2, RBP-7000 90 mg1.0702.100
Cohort 3, RBP-7000 120 mg1.7202.415

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Risperidone PK: Minimum Plasma Concentration (Cmin) Over the PK Profile

"Minimum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg0.8291.230
Cohort 2, RBP-7000 90 mg1.0602.100
Cohort 3, RBP-7000 120 mg1.7202.415

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Risperidone PK: Maximum Plasma Concentration Over the Secondary Peak (Cmax)

"Maximum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29) Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg3.1205.220
Cohort 2, RBP-7000 90 mg5.9507.010
Cohort 3, RBP-7000 120 mg7.95012.125

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Risperidone PK: Maximum Plasma Concentration (Cmax) Over the PK Profile

"Maximum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg6.2805.720
Cohort 2, RBP-7000 90 mg7.5207.490
Cohort 3, RBP-7000 120 mg9.27012.125

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9-hydroxyrisperidone PK: Average Plasma Concentration (Cavg) Over the PK Profile

"The average of plasma concentrations calculated as AUCtau/ tau (tau = 28 days)~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg7.3328.242
Cohort 2, RBP-7000 90 mg8.34412.718
Cohort 3, RBP-7000 120 mg14.67617.361

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9-hydroxyrisperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to Time Tau (Where Tau=28 Days) (AUCtau)

"AUCtau calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionhr*ng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg4927.05538.3
Cohort 2, RBP-7000 90 mg5607.58546.7
Cohort 3, RBP-7000 120 mg9862.211666.9

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9-hydroxyrisperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24)

"AUC0-24 calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionhr*ng/mL (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg237.0169.2
Cohort 2, RBP-7000 90 mg251.1263.4
Cohort 3, RBP-7000 120 mg404.8342.6

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9-hydroxyrisperidone PK: Area Under the Plasma Concentration-Time Curve From Day 2-29 Post Injection (AUC Day 2-29)

"Area under plasma concentration-time curve from 24 hours (Day 2) to the last quantifiable collection during dosing interval (28 days); calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionhr*ng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg4696.85388.2
Cohort 2, RBP-7000 90 mg5222.98311.7
Cohort 3, RBP-7000 120 mg7891.011786.5

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Total Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Maximum Plasma Concentrations (Rac(Cmax))

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Accumulation index in terms of Cmax calculated as ratio of Cmax injection 3 / injection 1.~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

Interventionratio (Median)
Cohort 1, RBP-7000 60 mg0.976
Cohort 2, RBP-7000 90 mg1.525
Cohort 3, RBP-7000 120 mg1.105

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Total Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Area Under the Plasma Concentration Curve (Rac(AUC))

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Accumulation index in terms of AUC calculated as ratio of AUCtau injection 3 / injection 1. Tau = 28 days.~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

Interventionratio (Median)
Cohort 1, RBP-7000 60 mg1.1
Cohort 2, RBP-7000 90 mg1.6
Cohort 3, RBP-7000 120 mg1.2

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Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Maximum Plasma Concentrations (Rac(Cmax))

"Accumulation index in terms of Cmax calculated as ratio of Cmax injection 3 / injection 1.~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

Interventionratio (Median)
Cohort 1, RBP-7000 60 mg1.049
Cohort 2, RBP-7000 90 mg1.214
Cohort 3, RBP-7000 120 mg1.155

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Risperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Area Under the Plasma Concentration Curve (Rac(AUC))

"Accumulation index in terms of AUC calculated as ratio of AUCtau injection 3 / injection 1. Tau = 28 days.~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

Interventionratio (Median)
Cohort 1, RBP-7000 60 mg1.1
Cohort 2, RBP-7000 90 mg1.7
Cohort 3, RBP-7000 120 mg1.1

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9-hydroxyrisperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Maximum Plasma Concentrations (Rac(Cmax))

"Accumulation index in terms of Cmax calculated as ratio of Cmax injection 3 / injection 1.~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

Interventionratio (Median)
Cohort 1, RBP-7000 60 mg0.997
Cohort 2, RBP-7000 90 mg1.442
Cohort 3, RBP-7000 120 mg1.076

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9-hydroxyrisperidone PK: Maximum Plasma Concentration (Cmax) During Initial Peak

"Cmax determined directly from individual concentration-time data.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionng/mL (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg11.1009.470
Cohort 2, RBP-7000 90 mg12.90012.900
Cohort 3, RBP-7000 120 mg17.50017.450

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9-hydroxyrisperidone PK: Maximum Plasma Concentration (Cmax) Over the PK Profile

"Maximum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg12.30013.450
Cohort 2, RBP-7000 90 mg15.60021.200
Cohort 3, RBP-7000 120 mg22.40029.600

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9-hydroxyrisperidone PK: Maximum Plasma Concentration Over the Secondary Peak (Cmax)

"Maximum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29) Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg12.30013.450
Cohort 2, RBP-7000 90 mg15.60021.200
Cohort 3, RBP-7000 120 mg22.30029.600

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9-hydroxyrisperidone PK: Minimum Plasma Concentration (Cmin) Over the PK Profile

"Minimum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg3.9404.180
Cohort 2, RBP-7000 90 mg4.2406.580
Cohort 3, RBP-7000 120 mg6.6908.365

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9-hydroxyrisperidone PK: Minimum Plasma Concentration (Cmin) Over the Secondary Peak

"Minimum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg3.9404.180
Cohort 2, RBP-7000 90 mg4.2507.660
Cohort 3, RBP-7000 120 mg7.06011.450

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9-hydroxyrisperidone PK: Percent Fluctuation Over the PK Profile

"The degree of fluctuation of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cavg, expressed as a percentage.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionpercentage of average concentration (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg120.024121.077
Cohort 2, RBP-7000 90 mg124.696106.728
Cohort 3, RBP-7000 120 mg142.828122.701

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9-hydroxyrisperidone PK: Percent Fluctuation Over the Secondary Peak

"The degree of fluctuation of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cavg, expressed as a percentage.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionpercentage of average concentration (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg112.945106.055
Cohort 2, RBP-7000 90 mg127.274104.207
Cohort 3, RBP-7000 120 mg141.300101.956

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9-hydroxyrisperidone PK: Swing Over the PK Profile

"The swing of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cmin.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionratio (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg1.9842.901
Cohort 2, RBP-7000 90 mg2.0412.142
Cohort 3, RBP-7000 120 mg2.6332.240

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9-hydroxyrisperidone PK: Average Plasma Concentration Over the Secondary Peak (Cavg, Day 2-29)

"The average of plasma concentrations in the plateau, calculated as AUC Day 2-29/time~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg7.2488.315
Cohort 2, RBP-7000 90 mg8.06012.827
Cohort 3, RBP-7000 120 mg12.17718.189

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9-hydroxyrisperidone PK: Swing Over the Secondary Peak

"The swing of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cmin.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionratio (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg1.9362.018
Cohort 2, RBP-7000 90 mg2.0411.991
Cohort 3, RBP-7000 120 mg2.6331.595

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9-hydroxyrisperidone PK: Accumulation Index Between Injections 1 and 3 In Terms of Area Under the Plasma Concentration Curve (Rac(AUC))

"Accumulation index in terms of AUC calculated as ratio of AUCtau injection 3 / injection 1. Tau = 28 days.~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

Interventionratio (Median)
Cohort 1, RBP-7000 60 mg1.1
Cohort 2, RBP-7000 90 mg1.5
Cohort 3, RBP-7000 120 mg1.2

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Total Risperidone PK: Maximum Plasma Concentration (Cmax) During Initial Peak

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Cmax determined directly from individual concentration-time data.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionng/mL (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg16.34314.549
Cohort 2, RBP-7000 90 mg19.41516.973
Cohort 3, RBP-7000 120 mg24.40022.852

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Summary of Participants With Treatment-Emergent Adverse Events (TEAE)

"An adverse event (AE) is defined as any study-related event that represents a change (positive or negative) in frequency or severity from a baseline (prestudy) event (if any), regardless of the presence of causal relationship or medical significance. Treatment-emergent adverse events are defined as any adverse event with a start date on or after the first study dose date. AEs are determined by the Investigator to be related or not related to the study drug.~A serious AE (SAE) is defined by federal regulation as any AE occurring at any dose that results in any of the following outcomes: death, life-threatening AE, hospitalization or prolongation of existing hospitalization, a persistent or significant disability/incapacity, or a congenital anomaly/birth defect. Although a subject may have had 2 or more adverse experiences the subject is counted only once in a category. The same subject may appear in different categories." (NCT01677377)
Timeframe: Day 1 to Day 106

,,
InterventionParticipants (Count of Participants)
No TEAEs1 or more TEAEsRelated TEAEsSerious TEAEsSerious, related TEAETEAE causing discontinuationDeath
Cohort 1, RBP-7000 60 mg41160000
Cohort 2, RBP-7000 90 mg411110000
Cohort 3, RBP-7000 120 mg7841000

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Total Risperidone PK: Maximum Plasma Concentration (Cmax) Over the PK Profile

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Maximum plasma concentrations determined directly from individual concentration-time data.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg16.87817.885
Cohort 2, RBP-7000 90 mg22.82530.804
Cohort 3, RBP-7000 120 mg32.23538.300

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Total Simpson-Angus Scale (SAS) Score at Baseline and Days 28, 56, 84 and 106

The switch from oral risperidone to RBP-7000 subcutaneous injections for safety markers used SAS. The SAS is a 10-item scale used to detect the presence of drug induced parkinsonism and extrapyramidal side effects, and evaluates symptom severity. The ten items focus on rigidity rather than bradykinesia, and do not assess subjective rigidity or slowness. Items are rated for severity on a 0 to 4 scale with 0=normal and 4=extreme description of the particular side effect. The total range is 0=no side effects observed to 40 = extreme of each of the 10 side effects. (NCT01677377)
Timeframe: Baseline (Day -1), Days 28, 56, 84, and End of Study (Day 106 or early termination visit)

,,
Interventionunits on a scale (Median)
BaselineDay 28Day 56Day 84Day 106
Cohort 1, RBP-7000 60 mg0.00.00.00.00.0
Cohort 2, RBP-7000 90 mg0.00.00.00.00.0
Cohort 3, RBP-7000 120 mg0.00.00.00.00.0

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Total Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the Secondary Peak

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionhours (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg168.000228.000
Cohort 2, RBP-7000 90 mg264.000264.067
Cohort 3, RBP-7000 120 mg192.000216.000

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9-hydroxyrisperidone PK: Time of Maximum Plasma Concentration (Tmax) During Initial Peak

"Tmax determined directly from individual concentration-time data.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionhours (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg4.00024.000
Cohort 2, RBP-7000 90 mg6.00024.000
Cohort 3, RBP-7000 120 mg6.00024.000

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9-hydroxyrisperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the PK Profile

"Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionhours (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg168.000216.000
Cohort 2, RBP-7000 90 mg168.000264.000
Cohort 3, RBP-7000 120 mg192.000216.000

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9-hydroxyrisperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the Secondary Peak

"Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionhours (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg216.000228.000
Cohort 2, RBP-7000 90 mg168.000264.000
Cohort 3, RBP-7000 120 mg216.000216.000

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Clinical Global Impression (CGI) Scores (Severity of Illness and Global Improvement) at Baseline and Days 28, 56, 84 and 106

"The switch from oral risperidone to RBP-7000 subcutaneous injections for efficacy markers used CGI scores. The CGI is used in the assessment of global illness severity and change in clinical condition over time in psychiatric patients.~Severity of illness is measured on a 7-point scale with 1=normal, not at all ill and 7=among the most extremely ill patients.~Global improvement is measured on a 7-point scale with 1=very much improved, 4=no change and 7=very much worse as compared to the severity of illness at baseline." (NCT01677377)
Timeframe: Baseline (Day -1), Days 28, 56, 84, and End of Study (Day 106 or early termination visit)

,,
Interventionunits on a scale (Median)
Baseline: Severity of illnessDay 28: Severity of illnessDay 28: Global improvementDay 56: Severity of illnessDay 56: Global improvementDay 84: Severity of illnessDay 84: Global improvementDay 106: Severity of illnessDay 106: Global improvement
Cohort 1, RBP-7000 60 mg3.03.04.03.04.03.04.03.04.0
Cohort 2, RBP-7000 90 mg3.03.04.03.04.03.04.03.04.0
Cohort 3, RBP-7000 120 mg3.03.04.03.04.03.04.03.04.0

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Global Assessment of the Abnormal Involuntary Movement Scale (AIMS) for Tardive Dyskinesia at Baseline and Days 28, 56, 84 and 106

"The switch from oral risperidone to RBP-7000 subcutaneous injections for safety markers used AIMS. The AIMS is a scale that aids in the early detection and ongoing monitoring of tardive dyskinesia, a movement disorder that can result from long-term treatment with antipsychotic medication. By assessing the participant's body movement in specific positions requiring rotation, a psychiatrist is able to determine whether abnormal facial or body movements exist.~The total score is the sum of 7 questions assessing movement plus 3 questions representing global assessments on the overall level of involuntary movement severity, incapacitation due to involuntary movement, and patient's awareness of involuntary movement. Each of the 10 questions are scored on a 0 (none) - 4 (extremely severe) scale. Plus two dental status questions are scored on a 0 (no) - 1 (yes) scale. The total score is therefore a scale of 0 (normal) - 42 (advanced tardive dyskinesia)." (NCT01677377)
Timeframe: Baseline (Day -1), Days 28, 56, 84, and End of Study (Day 106 or early termination visit)

,,
Interventionunits on a scale (Median)
BaselineDay 28Day 56Day 84Day 106
Cohort 1, RBP-7000 60 mg1.01.01.00.51.0
Cohort 2, RBP-7000 90 mg0.00.00.00.00.0
Cohort 3, RBP-7000 120 mg1.01.01.01.00.5

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Global Clinical Assessment of Akathisia Using the Barnes Akathisia Scale (BAS) at Baseline and Days 28, 56, 84 and 106

The BAS is a scale that detects the presence and severity of any drug induced akathisia. The scale measures objective and subjective effects such as restlessness and awareness of restlessness, respectively. Participants are observed while seated, then while standing and engaged in neutral conversation. Symptoms observed during additional situations, such as participant behavior on the ward, may also be rated. Subjective phenomena should be elicited through direct questioning of the participant. The global clinical assessment is reported on a scale of 0 to 5, where 0 = absent and 5 = severe akathisia. (NCT01677377)
Timeframe: Baseline (Day -1), Days 28, 56, 84, and End of Study (Day 106 or early termination visit)

,,
Interventionunits on a scale (Median)
BaselineDay 28Day 56Day 84Day 106
Cohort 1, RBP-7000 60 mg0.00.00.00.00.0
Cohort 2, RBP-7000 90 mg0.00.00.00.00.0
Cohort 3, RBP-7000 120 mg0.00.00.00.00.0

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Participants With Suicidal Ideation or Behavior as Identified Using the Columbia-Suicide Severity Rating Scale (C-SSRS) Score at Baseline and Days 28, 56, 84 and 106

"The C-SSRS is a scale developed by the National Institute of Mental Health trial group as a counterpart to the FDA's categorization of suicidal events. It was developed by a careful review and consequent categorization of thoughts and behavior that were statistically identified as significantly related to suicidal behavior. The scale captures the occurrence, severity, and frequency of suicide-related thoughts and behaviors throughout lifetime at screening, baseline, and for the time interval since last administration for repeat administrations during a study.~This outcome reports the number of participants with suicidal ideation or behavior." (NCT01677377)
Timeframe: Baseline (Day -1), Days 28, 56, 84, and End of Study (Day 106 or early termination visit)

,,
InterventionParticipants (Count of Participants)
Baseline: Suicidal ideation or behaviorDay 28: Suicidal ideation or behaviorDay 56: Suicidal ideation or behaviorDay 84: Suicidal ideation or behaviorDay 106: Suicidal ideation or behavior
Cohort 1, RBP-7000 60 mg00100
Cohort 2, RBP-7000 90 mg01000
Cohort 3, RBP-7000 120 mg01000

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Positive and Negative Syndrome Scale (PANSS) Scores at Baseline and Days 28, 56, 84 and 106

"The switch from oral risperidone to RBP-7000 subcutaneous injections for efficacy markers used the PANSS scores. The PANSS assessment is a medical scale designed to measure symptom severity among patients with schizophrenia. Each item is rated on a scale of 1=absent to 7=extreme. PANSS consists of three components:~The General Psychopathology Scale consists of 16 questions with a total range of 16 (no schizophrenia symptoms) to 112 (extreme schizophrenia symptoms).~Both the Positive Scale and the Negative Scale consists of 7 questions with a total range of 7 (no schizophrenia symptoms) to 49 (extreme symptoms) on each scale.~The PANSS range for assuring stability was a total PANSS General Psychopathology Scale score of 70 or less, with no score of 4 on any of the 7 questions in the Positive scale." (NCT01677377)
Timeframe: Baseline (Day -1), Days 28, 56, 84, and End of Study (Day 106 or early termination visit)

,,
Interventionunits on a scale (Median)
Baseline: General Psychopathology ScaleBaseline: Positive ScaleBaseline: Negative ScaleDay 28: General Psychopathology ScaleDay 28: Positive ScaleDay 28: Negative ScaleDay 56: General Psychopathology ScaleDay 56: Positive ScaleDay 56: Negative ScaleDay 84: General Psychopathology ScaleDay 84: Positive ScaleDay 84: Negative ScaleDay 106: General Psychopathology ScaleDay 106: Positive ScaleDay 106: Negative Scale
Cohort 1, RBP-7000 60 mg27.013.015.028.013.016.028.013.017.028.013.515.526.013.014.0
Cohort 2, RBP-7000 90 mg24.014.018.026.012.017.026.013.018.025.012.517.523.512.018.0
Cohort 3, RBP-7000 120 mg27.013.018.027.012.018.025.011.517.525.012.516.026.514.018.0

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Risperidone PK: Area Under the Plasma Concentration-Time Curve From Day 2-29 Post Injection (AUC Day 2-29)

"Area under plasma concentration-time curve from 24 hours (Day 2) to the last quantifiable collection during dosing interval (28 days); calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionhr*ng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg1198.22204.6
Cohort 2, RBP-7000 90 mg1544.92494.8
Cohort 3, RBP-7000 120 mg2937.33476.6

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Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24)

"AUC0-24 calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionhr*ng/mL (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg103.898.7
Cohort 2, RBP-7000 90 mg87.8107.1
Cohort 3, RBP-7000 120 mg99.5127.0

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Risperidone PK: Area Under the Plasma Concentration-Time Curve From Time Zero to Time Tau (Where Tau=28 Days) (AUCtau)

"AUCtau calculated using the linear trapezoidal rule.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionhr*ng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg1250.92144.6
Cohort 2, RBP-7000 90 mg1663.42647.1
Cohort 3, RBP-7000 120 mg3099.43621.2

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Risperidone PK: Average Plasma Concentration (Cavg) Over the PK Profile

"The average of plasma concentrations calculated as AUCtau/ tau (tau = 28 days)~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionng/mL (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg1.8613.191
Cohort 2, RBP-7000 90 mg2.4753.939
Cohort 3, RBP-7000 120 mg4.6125.389

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Total Risperidone PK: Time of the Maximum Plasma Concentration (Tmax) Over the PK Profile

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionhours (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg168.000216.00
Cohort 2, RBP-7000 90 mg215.833264.067
Cohort 3, RBP-7000 120 mg192.000216.000

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Total Risperidone PK: Time of Maximum Plasma Concentration (Tmax) During Initial Peak

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~Tmax determined directly from individual concentration-time data.~Results are reported across two timeframes:~Initial Peak, Injection 1 (Day 1 injection to 24 hours after injection)~Initial Peak, Injection 3 (Day 57 injection to 24 hours after injection)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-2, Day 57-58

,,
Interventionhours (Median)
Initial Peak, Injection 1Initial Peak, Injection 3
Cohort 1, RBP-7000 60 mg6.00017.917
Cohort 2, RBP-7000 90 mg6.00024.000
Cohort 3, RBP-7000 120 mg6.00024.000

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Total Risperidone PK: Swing Over the Secondary Peak

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~The swing of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cmin.~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionratio (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg2.0482.412
Cohort 2, RBP-7000 90 mg2.0171.914
Cohort 3, RBP-7000 120 mg2.9281.679

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Total Risperidone PK: Swing Over the PK Profile

"Total risperidone concentration (risperidone and 9-hydroxyrisperidone) was determined by adding risperidone concentration to risperidone-equivalent concentration (obtained from the 9-hydroxyrisperidone data). Total risperidone concentration was calculated using the molecular weights of 410 for risperidone and 426 for 9-hydroxyrisperidone:~[Total Risperidone] = [Risperidone] + (410/426) * [9-hydroxyrisperidone]~The swing of total risperidone plasma concentrations calculated as (Cmax - Cmin) / Cmin.~Results are reported across two timeframes:~Overall, Injection 1 (Day 1 injection to Day 28)~Overall, Injection 3 (Day 57 injection to Day 84)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 1-28, Day 57-84

,,
Interventionratio (Median)
Overall, Injection 1Overall, Injection 3
Cohort 1, RBP-7000 60 mg2.5022.588
Cohort 2, RBP-7000 90 mg2.1502.052
Cohort 3, RBP-7000 120 mg2.9282.019

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Risperidone PK: Average Plasma Concentration Over the Secondary Peak (Cavg, Day 2-29)

"The average of plasma concentrations in the plateau, calculated as AUC Day 2-29/time~Results are reported across two timeframes:~Secondary Peak, Injection 1 (Day 2 - Day 29)~Secondary Peak, Injection 3 (Day 58 - Day 85)~The PK sampling schedule was:~Days 1 and 57: within 15 minutes prior to dosing, and at 1, 2, 3, 4, 6, and 12 hours post-dose~Days 2, 4, 6, 8-12, 15, 18, 22, 25, 58, 60, 62, 64-68, 71, 74, 78, 81 once each day at same time of day as study drug administration" (NCT01677377)
Timeframe: Day 2-29, Day 58-85

,,
Interventionng/mL (Median)
Secondary Peak, Injection 1Secondary Peak, Injection 3
Cohort 1, RBP-7000 60 mg1.8493.402
Cohort 2, RBP-7000 90 mg2.3843.850
Cohort 3, RBP-7000 120 mg4.5335.365

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Clinical Global Impressions (CGI) - Disease Severity Score

"The CGI rating scale is a 7-point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 indicates to normal, not at all ill and a rating of 7 indicates among the most extremely ill participants. Higher scores indicate worsening." (NCT01726335)
Timeframe: Baseline and Week 2, 4, 8, 16, 24, 38 and 50

InterventionUnits on a scale (Mean)
BaselineWeek 2Week 4Week 8Week 16Week 24Week 38Week 50
Risperidone Prolonged Release3.553.373.303.213.102.922.943.19

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 4

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 4

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release53.82

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 50

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 50

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release49.72

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 8

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 8

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release51.28

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Drug Attitude Inventory (DAI-10)

The DAI-10 is a 10-item questionnaire to assess 1) subjective experience of drug and 2) attitudes and beliefs toward neuroleptics which may influence compliance in schizophrenia participants. It is the binary scale assessing the participant's subjective response. A 'compliant' response is scored as +1; a dysphoric response is scored as -1. A positive sum of items indicates a positive subjective response (SR); a negative sum of scores indicates a negative SR (non-compliant). The final score is the grand total of the positive and negative points. Total score ranges from (-) 10 to (+) 10, higher score indicates positive SR (compliant) and lower score indicates negative SR (non-compliant). (NCT01726335)
Timeframe: Screening, and Week 8, 24 and 50

InterventionUnits on a scale (Mean)
ScreeningWeek 8Week 24Week 50
Risperidone Prolonged Release2.784.454.595.07

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Extrapyramidal Symptoms Rating Scale (ESRS) Total Score

The ESRS is used to assess four types of drug-induced movement disorders administered as a questionnaire. Score range from 0 to 6 (0 is absent and 6 is extremely severe). (NCT01726335)
Timeframe: Baseline and Week 2, 4, 8, 16, 24 and 50

InterventionUnits on a scale (Mean)
BaselineWeek 2Week 4Week 8Week 16Week 24Week 50
Risperidone Prolonged Release0.4600.4160.2720.2890.2710.2210.089

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Global Assessment of Functioning (GAF) Scale Score

The GAF scale is a 100-point tool rating overall psychological, social and occupational functioning of adults. The higher score range (91-100) refers to a superior functioning in a wide range of activities, and absence of symptoms. The lower score range (1-10) refers to persistent danger of severely hurting self or others; or persistent inability to maintain minimum personal hygiene; or serious suicidal act with clear expectation of death. (NCT01726335)
Timeframe: Screening, and Week 8, 16, 24, 38 and 50

InterventionUnits on a scale (Mean)
ScreeningWeek 8Week 16Week 24Week 38Week 50
Risperidone Prolonged Release62.667.572.571.473.968.6

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Personal and Social Performance (PSP) Scale Score

The PSP scale assesses the degree of a participant's dysfunction (ranging from i [absent] to vi [very severe) within 4 domains of behavior: socially useful activities, personal and social relationships, self-care, disturbing and aggressive behavior. The overall score ranges from 1 to 100. Based on the 4-domains there was one total score. Participants with a score of 71 to 100 had a mild degree of difficulty; from 31 to 70, varying degrees of disability; participants with scores of 30 or less function so poorly as to require intensive supervision. (NCT01726335)
Timeframe: Screening, and Week 8, 16, 24, 38 and 50

InterventionUnits on a scale (Mean)
ScreeningWeek 8Week 16Week 24Week 38Week 50
Risperidone Prolonged Release60.066.472.671.771.869.1

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Short Form-36 (SF-36) - Quality of Life

The SF-36 is a survey of participant health. It consists of eight scaled scores, which are the weighted sums of the questions in their section. The eight sections are: vitality, physical functioning, bodily pain, general health perceptions, physical role functioning, emotional role functioning, social role functioning, and mental health. Each item is scored on a 0-100 range so that the lowest and highest possible scores are set at 0 and 100, respectively. All items are scored so that a high score defines a more favorable health state. (NCT01726335)
Timeframe: Baseline and Week 50

InterventionUnits on a scale (Mean)
Functional capacity : BaselinePhysical aspect : BaselinePain : BaselineHealth General State : BaselineVitality : BaselineSocial Aspect : BaselineEmotional Aspect : BaselineMental Health : BaselineFunctional capacity : Week 50Physical aspect : Week 50Pain : Week 50Health General State : Week 50Vitality : Week 50Social Aspect : Week 50Emotional Aspect : Week 50Mental Health : Week 50
Risperidone Prolonged Release79.248.273.760.753.856.134.958.967.952.975.462.753.159.955.056.6

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 24

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 24

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release48.95

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 2

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 2

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release55.53

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 38

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 38

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release47.40

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Positive and Negative Syndromes Scale (PANSS) Total Score at Week 16

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01726335)
Timeframe: Week 16

InterventionUnits on a scale (Mean)
Risperidone Prolonged Release50.55

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Treatment Response

The primary outcome measure will be the total Brief Psychiatric Rating Scale Score. The range of the BPRS is 0 to 126 with higher scores indicated more psychological symptoms. (NCT01786239)
Timeframe: 16 weeks

,
Interventionunits on a scale (Least Squares Mean)
Baseline BPRS ScoreWeek 16 BPRS Score
Omega-3 Capsules & Risperidone41.6422.5868
Placebo & Risperidone42.3827.2235

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BMI Z-scores

(NCT01844700)
Timeframe: baseline to week 12

,
InterventionBMI z-score (Mean)
baselineweek 12 (n=1, n=2)
Aripiprazole, Quetiapine, Risperidone-0.370.38
Ziprasidone-0.510.22

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Percent Weight Change Compared to Baseline Weight

(NCT01844700)
Timeframe: baseline to week 12

Interventionpercentage of weight change (Mean)
Ziprasidone11.58
Aripiprazole, Quetiapine, Risperidone5.66

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Weight Change

(NCT01844700)
Timeframe: baseline to week 12

,
Interventionlbs (Mean)
baselineweek 12 (n=1,2)
Aripiprazole, Quetiapine, Risperidone118.5141
Ziprasidone120.5151

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BMI Percentile

(NCT01844700)
Timeframe: baseline to week 12

,
InterventionBMI percentile (Mean)
baselineweek 12 (n=1, n=2)
Aripiprazole, Quetiapine, Risperidone37.6762.5
Ziprasidone3259

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 26

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210, higher scores indicate worsening. Change at Week 26 score is calculated as Baseline score minus Week 26 score. (NCT01855074)
Timeframe: Baseline and Week 26

InterventionUnits on a scale (Mean)
Baseline (n=78)Change at Week 26 (n=66)
Risperidone68.928.1

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Global Assessment of Functioning (GAF) Score

The GAF is a 100-point tool to measure overall psychological, social and occupational functioning of adults. The higher score range (91 to 100) refers to a superior functioning in a wide range of activities, and absence of symptoms. The lower score range (1 to 10) refers to persistent danger of severely hurting self or others; or persistent inability to maintain minimum personal hygiene; or serious suicidal act with clear expectation of death. (NCT01855074)
Timeframe: Baseline and Week 26

InterventionUnits on a scale (Mean)
Baseline (n=78)Week 26 (n=66)
Risperidone56.569.4

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Extrapyramidal Symptom Rating Scale (ESRS) Score

An ESRS scale is used to assess the extrapyramidal symptoms attributable to antipsychotics. It consists of 8 items to assess individual symptoms and each item is assessed from 0 (none, absent) to 4 (severe). The total score is the sum of the 8 item scores, for a total range of 0 (normal) to 32 severe). The items for the assessment of individual symptoms are classified into 4 categories of parkinsonism, akathisia, dystonia and dyskinesia. (NCT01855074)
Timeframe: Baseline and Week 26

InterventionUnits on a scale (Mean)
BaselineWeek 26
Risperidone12.99.2

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Clinical Global Impressions (CGI) - Disease Severity Score

"The CGI rating scale is a 7-point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants, higher scores indicate worsening." (NCT01855074)
Timeframe: Baseline and Week 26

InterventionUnits on a scale (Mean)
Baseline (n=78)Week 26 (n=66)
Risperidone4.22.9

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Patient Satisfaction With Treatment

Participants' were assessed for their satisfaction with the current antipsychotic treatment on a 5-point scale/questionnaire: very good, good, reasonable, moderate or poor. (NCT01855074)
Timeframe: Baseline and Week 26

InterventionParticipants (Number)
Baseline; Very good (n=78)Week 26; Very good (n=66)Baseline; Good (n=78)Week 26; Good (n=66)Baseline; Moderate (n=78)Week 26; Moderate (n=66)Baseline; Poor (n=78)Baseline; Very poor (n=78)Baseline; No available (n=78)
Risperidone216134042101911

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Short Form-36 (SF-36) - Quality of Life Score

The SF-36 is a standardized survey evaluating 8 aspects of functional health and well being: vitality, physical function, social function, physical role, emotional role, bodily pain, general health, mental health. Each item is scored on a scale ranging from 0-100 (100=highest level of functioning). (NCT01855074)
Timeframe: Baseline and Week 26

InterventionUnits on a scale (Mean)
Baseline; Physical function (n=78)Week 26; Physical function (n=66)Baseline; Physical role (n=78)Week 26; Physical role (n=66)Baseline; Body pain (n=78)Week 26; Body pain (n=66)Baseline; General health (n=78)Week 26; General health (n=66)Baseline; Vitality (n=78)Week 26; Vitality (n=66)Baseline; Social function (n=78)Week 26; Social function (n=66)Baseline; Emotional role (n=78)Week 26; Emotional role (n=66)Baseline; Mental health (n=78)Week 26; Mental health (n=66)
Risperidone78.390.541.075.486.294.751.767.851.758.649.074.132.173.250.759.9

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Total Personal and Social Performance (PSP) Score

The PSP is a clinician-rated scale that reflects social functioning in 4 domains of behavior (socially useful activities including work and study, personal and social relationships, self care, and disturbing and aggressive behaviors). The total score ranges from 1 to 100 (score of 71 to 100 will have a mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision) divided into 10 equal intervals to rate the degree of difficulty (i=absent to vi=very severe) in each of the 4 domains. (NCT01894984)
Timeframe: Baseline and Week 24

,
Interventionunits on a scale (Mean)
BaselineWeek 24
Oral Atypical Anti-psychotic52.982.3
Risperidone52.188.0

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Number of Participants With Reasons for Discontinuation From Study Treatment

Number of participants with reasons for discontinuation from study treatment is reported here because participants provided multiple reasons for discontinuation. (NCT01894984)
Timeframe: Month 6

,
InterventionParticipants (Number)
Physician DecisionAdverse eventLack of efficacyDiscontinuation from Treatment (more than 4 weeks)Added other anti-psychoticsChange to other anti-psychoticsLost to follow-upWithdrawal by participantOther (unspecified)
Oral Atypical Anti-psychotic11327318390106
Risperidone142410651057674128

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Percentage of Participants With Relapse at Week 24

Percentage of participants with relapse was assessed wherein relapse was defined as hospitalization due to the aggravation of psychiatric symptoms of disease condition. (NCT01894984)
Timeframe: Week 24

InterventionPercentage of Participants (Number)
Risperidone0.5
Oral Atypical Anti-psychotic1.6

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Percentage of Participants Attaining Remission Criteria

Remission is defined as a clinical status where for each core symptoms (that are, delusions, conceptual disorganization, hallucinatory behavior, mannerisms and posturing unusual thought content, blunted affect, passive or apathetic social withdrawal and lack of spontaneity and flow of conversation) were assessed at a low-mild symptom intensity level, where such absent, borderline, or mild symptoms do not influence an individual's behavior. (NCT01894984)
Timeframe: Month 6

InterventionPercentage of Participants (Number)
Risperidone46
Oral Atypical Anti-psychotic68

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Clinical Global Impressions-Severity (CGI-S) Score

"The CGI-S rating scale is a 7-point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT01894984)
Timeframe: Baseline and Week 24

,
Interventionunits on a scale (Mean)
BaselineWeek 24
Oral Atypical Anti-psychotic4.62.1
Risperidone4.51.5

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Week 24

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score consists of the sum of all 30 PANSS items and ranges from 30 to 210. Higher scores indicate worsening. (NCT01894984)
Timeframe: Baseline and Week 24

,
Interventionunits on a scale (Mean)
BaselineChange at Week 24
Oral Atypical Anti-psychotic72.3-38.2
Risperidone74.7-36.5

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Feedback-based Probabilistic Classification Task

On each trial, participants will view one of four images and will be asked to guess whether it belongs to Category A or B. For each participant, the four images will be randomly assigned to be stimuli S1, S2, S3 and S4 (these are abstract visual stimuli denoted with numbers (stiumulus 1, stimulus 2, etc). A different set of similar images (S5-S8; S9-S12, etc) will be used for repeated testing. On any given trial, stimuli S1 and S3 will belong to Category A with 90% probability and to Category B with 10% probability, while stimuli S2 and S4 will belong to Category B with 90% probability and to Category A with 10% probability. Stimuli S1 and S2 will be used in the reward-learning task and S3 and S4 in punishment-learning task. Two stimuli per valence will be employed in order to balance category outcome frequencies, so that one stimulus in each task will be associated with each outcome. (NCT01931059)
Timeframe: Before every MRI except the 2nd and 4th which will occur during the MRI (5 times - 3 consecutive days)

Interventionpercentage of correct response (Mean)
ON - PUNISHMENT52.86
OFF - PUNISHMENT71.43
ON - REWARD61.43
OFF - REWARD70.00

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Repeatable Battery for the Assessment of Neuropsychological Status

"This will measure the subject's cognitive performance. RBANS is a well-characterized repeatable battery to measure a wide array of cognitive performance in different cognitive domains. We will use Total Score in RBANS: five index scores are computed from the RBANS (immediate memory, language, visuospatial, attention, delayed memory) that are combined to provide the Total Score. The Total Score is expressed as a standardized score normalized to a population mean of 100, with a standard deviation of 15 (possible scores 40-135). Higher scores reflect better performance. More detailed information is available: Randolph C, Tierney MC, Mohr E, Chase TN (June 1998). The Repeatable Battery for the Assessment of Neuropsychological Status (RBANS): preliminary clinical validity. J Clin Exp Neuropsychol. 20 (3): 310-9. doi:10.1076/jcen.20.3.310.823. PMID 9845158.~Here we calculated the difference of T-scaled total RBANS score between risperidone day and placebo day in all participants" (NCT01931059)
Timeframe: The change of RBANS scores between placebo and treatment conditions on two consecutive days

InterventionRBANS T-Scale point difference (Mean)
Risperidone Then Placebo-1.5
Placebo Then Risperidone-0.5

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Simpson-Angus Extrapyramidal Side Effects Scale

The secondary outcome measures are the scores from side effect scales (Simpson-Angus Extrapyramidal Side Effects. It will measured in synchrony with Repeated Battery for the Assessment of Neuropsychological Status to explore if any of these measures would correlate with network changes in the brain. The Simpson-Angus scale is 0 if there is no extrapyramidal side effects, and is higher the worst the symptoms are. (NCT01931059)
Timeframe: 2 times on risperidone day and on placebo day

Interventionunits on a scale (Mean)
Risperidone Then Placebo0
Placebo Then Risperidone0

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Mean Change From Baseline to Week 6 in Positive and Negative Syndrome Scale (PANSS) Total Scores.

Mean change in Positive and Negative Syndrome Scale total score from baseline to Week 6 at the end of treatment. PANSS is an interview-based measure of the severity of psychopathology in adults with psychotic disorders. It have 30 evaluation items, which include 7 positive sub-scale, 7 negative sub-scale and 16 general psychopathology sub-scale on a score of 1 to 7. The total score is the sum of the 30 scale items. The minimum score is 30 and the maximum score is 210. Patient with PANSS total scores<70 is the normal,but the scores>120 is more serious. (NCT02002832)
Timeframe: From baseline to Week 6(day 42).

Interventionunits on a scale (Least Squares Mean)
Lurasidone Group-31.2
Risperidone Group-34.9

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Mean Clinical Global Impression Scale-Improvement (CGI-I) Score at Week 6.

"The Clinical Global Impression Scale-Improvement (CGI-I) Score is a 7 point scale that requires the clinician to assess how much the patient's illness has improved or worsened relative to baseline state at the beginning of the intervention. Response is rated as one of the following, in which higher scores indicate less improvement or worsening:~1=Very much improved, 2=Much improved, 3=Minimally improved, 4=No change, 5=Minimally worse, 6=Much worse, and 7=Very much worse." (NCT02002832)
Timeframe: From baseline to Week 6(day 42).

Interventionunits on a scale (Least Squares Mean)
Lurasidone Group2.0
Risperidone Group1.9

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Area Under the Curve Extrapolated to Infinity (AUC∞) for Active Moiety

(NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

Interventionh*ng/mL (Geometric Mean)
Gluteus (Risperidone ISM)21100
Deltoid (Risperdione ISM)22700

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Area Under the Curve to the Last Quantified Concentration (AUClast) for Active Moiety

(NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

Interventionh*ng/mL (Geometric Mean)
Gluteus (Risperidone ISM)21300
Deltoid (Risperdione ISM)23300

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PTF for Active Moiety

Peak to Trough Fluctuation ratio for the Active Moiety (NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

,
InterventionRatio (Geometric Mean)
Dose 1Dose 2Dose 3
Deltoid (Risperdione ISM)1.761.881.82
Gluteus (Risperidone ISM)0.9991.891.39

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Accumulation Ratio (RA) for Active Moiety

Defined as AUC (0-28 days) after the 4th dose divided by the AUC (0-28 days) of the first dose. (NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

InterventionRatio (Geometric Mean)
Gluteus (Risperidone ISM)1.15
Deltoid (Risperdione ISM)1.14

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Trough Plasma Concentration (Cmin) for Active Moiety

(NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

,
Interventionng/mL (Geometric Mean)
Dose 1Dose 2Dose 3Dose 4
Deltoid (Risperdione ISM)7.08.6010.29.52
Gluteus (Risperidone ISM)11.17.869.9712.6

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Positive and Negative Syndrome Scale (PANSS) Total Score

"The change in PANSS score from Baseline by visit 48.~The PANSS combines 3 subscales: The positive scale (7 items), the negative scale (7 items) and the general psychopathology scale (16 items).~PANSS Items Scores: 1 = Absent, 2 = Minimal, 3 = Mild, 4 = Moderate, 5 = Moderate Severe, 6 = Severe, 7 = Extreme.~Subscales are summed to compute a total score Range for each of the subscales: Positive scale (7-49); Negative scale (7-49); General psychopathology scale (16-112) Range for the PANSS total scale: 30-210 PANSS total score ≤70: stable schizophrenia PANSS total score between >70: decompensated schizophrenia" (NCT02086786)
Timeframe: Baseline, Days 5, 7, 10, 14, 18, and 21 post Dose 1; Dose 2, 3 and 4 post dose; Days 5, 7, 10, 14, 18, and 21 post Dose 2, 3, and 4; Days 25, 28, 32, 37, 42, 60, 75, 90, and 105 post Dose 4; Day 120 post Dose 4 or early termination.

,
Interventionpoints (Mean)
Baseline (Day -1)Visit 48 (Day 120 post Dose 4)
Deltoid (Risperdione ISM)6061
Gluteus (Risperidone ISM)5859

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Time to Peak Concentration (Tmax) for Active Moiety

(NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

,
Interventionh (Median)
Dose 1Dose 2Dose 3Dose 4
Deltoid (Risperdione ISM)48.024.024.048.0
Gluteus (Risperidone ISM)48.024.048.024.0

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Peak Plasma Concentration (Cmax) for Active Moiety

(NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

,
Interventionng/mL (Geometric Mean)
Dose 1Dose 2Dose 3Dose 4
Deltoid (Risperdione ISM)54.161.061.057.7
Gluteus (Risperidone ISM)39.653.248.647.4

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AUCτ for Active Moiety

AUCτ is the area under the curve over the dosing interval (τ), where the dosing interval is 28 days (NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

,
Interventionh*ng/mL (Geometric Mean)
Dose 1Dose 2Dose 3Dose 4
Deltoid (Risperdione ISM)16300180001820018500
Gluteus (Risperidone ISM)14100154001660017300

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Terminal Half-life (t1/2) for Active Moiety

(NCT02086786)
Timeframe: Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

Interventionh (Geometric Mean)
Gluteus (Risperidone ISM)163
Deltoid (Risperdione ISM)269

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Mixed Model for Repeated Measures (MMRM) Analysis of Change From Baseline to End of Treatment in the Positive and Negative Syndrome Scale (PANSS) Total Score

"The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor judgement, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score is the sum of all 30 PANSS items and ranges from 30 to 210, with 30 indicating absence of symptoms of schizophrenia and 210 indicating extreme ratings of all 30 symptoms. Negative change from baseline scores indicate improvements in symptoms.~Estimates (least square means and standard errors), 2-sided confidence intervals, and -1-sided P values are based on a repeated-measures linear regression model of the change from baseline score, with fixed effects for visit as a categorical variable, baseline score, treatment and treatment by visit interaction, assuming an unstructured covariance matrix." (NCT02109562)
Timeframe: Day 1 prior to treatment (Baseline), Days 15, 29, 43 and 57 or early discontinuation

Interventionunits on a scale (Least Squares Mean)
RBP-7000 90 mg-15.367
RBP-7000 120 mg-16.456
Placebo-9.219

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Mixed Model for Repeated Measures (MMRM) Analysis of Change From Baseline to End of Treatment in Clinical Global Impression - Severity Scale (CGI-S)

"The CGI-S rating scale is a 7-point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Negative change from baseline scores indicate improvement in the severity of illness.~Estimates (least square means and standard errors), 2-sided confidence intervals, and -1-sided P values are based on a repeated-measures linear regression model of the change from baseline score, with fixed effects for visit as a categorical variable, baseline score, treatment and treatment by visit interaction, assuming an unstructured covariance matrix." (NCT02109562)
Timeframe: Day 1 prior to treatment (Baseline), Days 15, 29, 43 and 57 or early discontinuation

Interventionunits on a scale (Least Squares Mean)
RBP-7000 90 mg-0.868
RBP-7000 120 mg-0.914
Placebo-0.518

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Summary of Participants With Treatment-Emergent Adverse Events (TEAE)

"An adverse event (AE) is defined as any study-related event that represents a change (positive or negative) in frequency or severity from a baseline (prestudy) event (if any), regardless of the presence of causal relationship or medical significance. Treatment-emergent adverse events are defined as any adverse event with a start date on or after the first study dose date. AEs are determined by the Investigator to be related or not related to the study drug.~A serious AE (SAE) is defined by federal regulation as any AE occurring at any dose that results in any of the following outcomes: death, life-threatening AE, hospitalization or prolongation of existing hospitalization, a persistent or significant disability/incapacity, or a congenital anomaly/birth defect. Although a subject may have had 2 or more adverse experiences the subject is counted only once in a category. The same subject may appear in different categories." (NCT02109562)
Timeframe: Day 1 to Week 8

,,
InterventionParticipants (Count of Participants)
No TEAEs1 or more TEAEsRelated TEAESerious TEAESerious, related TEAETEAE causing discontinuationDeath
Placebo3781501030
RBP-7000 120 mg2691651020
RBP-7000 90 mg3481580000

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Participants With Treatment-Emergent Adverse Events (TEAE)

"An adverse event (AE) is defined as any study-related event that represents a change (positive or negative) in frequency or severity from a baseline (prestudy) event (if any), regardless of the presence of causal relationship or medical significance. Treatment-emergent adverse events are defined as any adverse event with a start date on or after the first study dose date. AEs are determined by the Investigator to be related or not related to the study drug.~A serious AE (SAE) is defined by federal regulation as any AE occurring at any dose that results in any of the following outcomes: death, life-threatening AE, hospitalization or prolongation of existing hospitalization, a persistent or significant disability/incapacity, or a congenital anomaly/birth defect. Although a subject may have had 2 or more adverse experiences the subject is counted only once in a category. The same subject may appear in different categories." (NCT02203838)
Timeframe: Day 1 up to week 52

,,,
InterventionParticipants (Count of Participants)
1 or more TEAE>=1 TEAE related to study drug>=1 serious TEAE>=1 serious and related TEAETEAE leading to dose modificationTEAE leading to discontinuationTEAE leading to death
De Novo Participants30623225038473
Rollover Placebo211230261
Rollover RBP-7000 120 mg181230220
Rollover RBP-7000 90 mg221430130

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Change From Baseline in Clinical Global Impression - Severity Scores (CGI-S) to Days 29, 169 and End of Study

"The CGI-S rating scale is a 7-point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Negative change from baseline scores indicate improvement in the severity of illness." (NCT02203838)
Timeframe: Baseline (Day 0), Baseline (Day 0), Day 29, Day 169 and End of Study (approximately Week 52)

,,,
Interventionunits on a scale (Mean)
Day 29Day 169End of Study
De Novo Participants-0.0-0.1-0.2
Rollover Placebo-0.3-0.3-1.0
Rollover RBP-7000 120 mg-0.1-0.4-0.3
Rollover RBP-7000 90 mg-0.2-0.3-0.5

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Subscale Scores to End of Study

"PANSS subscales:~Positive scale assesses 7 items: delusions, conceptual disorganization, hallucinations, excitement, grandiosity, suspiciousness/persecution, and hostility. Scale: 7 (absent) to 49 (extreme psychopathology)~Negative scale assesses 7 items: blunted affect, emotional withdrawal, poor rapport, passive/apathetic social withdrawal, difficulty in abstract thinking, lack of spontaneity and flow of conversation, and stereotyped thinking. Scale: 7 (absent) to 49 (extreme psychopathology)~General Psychopathology scale assesses 16 items: somatic concern, anxiety, guilt feelings, tension, mannerisms and posturing, depression, motor retardation, uncooperativeness, unusual thought content, disorientation, poor attention, lack of judgment and insight, disturbance of volition, poor impulse control, preoccupation, and active social avoidance. Scale: 16 (absent) to 112 (extreme psychopathology) Negative change from baseline scores indicate improvements." (NCT02203838)
Timeframe: Baseline (Day 0), End of Study (approximately Week 52)

,,,
Interventionunits on a scale (Mean)
Positive subscaleNegative subscaleGeneral Psychopathology subscale
De Novo Participants-1.31.3-0.4
Rollover Placebo-7.8-4.0-8.3
Rollover RBP-7000 120 mg-3.7-0.9-6.4
Rollover RBP-7000 90 mg-3.7-4.1-4.7

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Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score to Days 29, 169 and End of Study

The PANSS is a 30-item scale designed to assess various symptoms of schizophrenia including delusions, grandiosity, blunted affect, poor judgement, poor attention, and poor impulse control. The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score is the sum of all 30 PANSS items and ranges from 30 to 210, with 30 indicating absence of symptoms of schizophrenia and 210 indicating extreme ratings of all 30 symptoms. Negative change from baseline scores indicate improvements in symptoms. (NCT02203838)
Timeframe: Baseline (Day 0), Day 29, Day 169 and End of Study (approximately Week 52)

,,,
Interventionunits on a scale (Mean)
Day 29Day 169End of Study
De Novo Participants-1.2-1.2-0.4
Rollover Placebo-4.8-8.2-20.2
Rollover RBP-7000 120 mg-2.4-9.4-10.9
Rollover RBP-7000 90 mg-8.3-10.0-12.5

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Participants With Markedly Abnormal Weight Gain Anytime During the Study as Compared to Baseline

Participants who were found to have gain >=7% and >=10% of their baseline weight at any point during the study (including unscheduled assessments) once treatment began. (NCT02203838)
Timeframe: Baseline (Day 0), Treatment (Day 1 up to Week 52)

,,,
InterventionParticipants (Count of Participants)
>=7% increase from baseline>=10% increase from baseline
De Novo Participants10667
Rollover Placebo33
Rollover RBP-7000 120 mg54
Rollover RBP-7000 90 mg42

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Part 2 (Disease Progression): Change From Baseline in Visual Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess visual learning score of participants. The range of visual learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.3
Part-2: OAP1.4

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Part 2 (Disease Progression): Change From Baseline in Verbal Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess verbal learning score of participants. The range of verbal learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.3
Part-2: OAP1.0

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Part 2 (Disease Progression): Change From Baseline in Speed of Processing Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess speed of processing score of participants. The range of speed of processing T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.8
Part-2: OAP3.5

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Part 2 (Disease Progression): Change From Baseline in Social Cognition Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess social cognition score of participants. The range of social cognition score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)0.3
Part-2: OAP1.6

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Part 2 (Disease Progression): Change From Baseline in Reasoning and Problem Solving: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess reasoning and problem solving of participants. The range of reasoning and problem solving T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)0.2
Part-2: OAP2.8

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Part 2 (Disease Progression): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Total Score

The Medication Satisfaction Questionnaire (MSQ) is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). Total score ranges from 1 to 7. Higher score indicate improvement. (NCT02431702)
Timeframe: Baseline and endpoint Part 2 (up to 9 Months)

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP0.1

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Part 2 (Disease Progression): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Each domain was assessed on a 6-point scale, from 1 (absent) to 6 (very severe) (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe). PSP total score was calculated as sum of all the domain scores and ranges from 1 to 100. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. Higher score indicate better performance. (NCT02431702)
Timeframe: Baseline and Month 9

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)2.5
Part-2: OAP2.9

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Part 2 (Disease Progression): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Month 9

InterventionT-score (Least Squares Mean)
Part-2: Paliperidone Palmitate (PP)2.0
Part-2: OAP2.8

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Part 2 (Disease Progression): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score

"The Clinical Global Impression Severity (CGI-S) rating scale is used to rate the severity of a participant's overall clinical condition on a 7 point scale. The score ranges from 1 to 7, where 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT02431702)
Timeframe: Baseline, up to 9 Months of Part 2

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP-0.3

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Part 2 (Disease Progression): Change From Baseline in Attention/Vigilance Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess attention/vigilance score of participants. The range of attention/vigilance score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)3.2
Part-2: OAP0.7

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Part 2 (Disease Progression): Change From Baseline in Adjusted Intracortical Myelin (ICM) Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and Day 260

Interventionratio (Mean)
Part-2: Paliperidone Palmitate (PP)-0.001
Part-2: OAP-0.004

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Part 3 (EDP): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by CRDPSS

The CRDPSS is an 8-item measure that assesses the severity of mental health symptoms that are important across psychotic disorders, including delusions, hallucinations, disorganized speech, abnormal psychomotor behavior, negative symptoms. Each item on the measure is rated on a 5-point scale (0=none; 1=equivocal; 2=present, but mild; 3=present and moderate; and 4=present and severe). Total Score is taken as summation. A higher score indicates a more severe condition. Worsened or improved is defined as increase or decrease compared to baseline. (NCT02431702)
Timeframe: Baseline, up to 18 Months

InterventionParticipants (Count of Participants)
Hallucinations72513609Hallucinations72513610Delusions72513609Delusions72513610Disorganized Speech72513609Disorganized Speech72513610Abnormal Psychomotor Behavior72513609Abnormal Psychomotor Behavior72513610Negative Symptoms72513609Negative Symptoms72513610Impaired Cognition72513609Impaired Cognition72513610Mania72513609Mania72513610Depression72513609Depression72513610
WorsenedUnchangedImproved
Part 3-PP to PP3
Part 3-OAP to OAP8
Part 3-PP to PP27
Part 3-OAP to OAP29
Part 3-PP to PP11
Part 3-OAP to OAP10
Part 3-PP to PP6
Part 3-PP to PP21
Part 3-OAP to OAP20
Part 3-PP to PP14
Part 3-OAP to OAP17
Part 3-PP to PP2
Part 3-OAP to OAP36
Part 3-PP to PP12
Part 3-PP to PP4
Part 3-OAP to OAP2
Part 3-PP to PP32
Part 3-OAP to OAP37
Part 3-PP to PP5
Part 3-OAP to OAP4
Part 3-OAP to OAP22
Part 3-PP to PP19
Part 3-OAP to OAP21
Part 3-PP to PP10
Part 3-OAP to OAP9
Part 3-OAP to OAP23
Part 3-PP to PP17
Part 3-OAP to OAP15
Part 3-PP to PP0
Part 3-OAP to OAP3
Part 3-PP to PP40
Part 3-OAP to OAP39
Part 3-PP to PP1
Part 3-OAP to OAP5
Part 3-PP to PP7
Part 3-OAP to OAP6
Part 3-PP to PP26
Part 3-PP to PP8
Part 3-OAP to OAP12

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Part 2 (Disease Progression): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by Clinician-Rated Dimensions of Psychosis Symptom Severity Scale (CRDPSS)

The CRDPSS is an 8-item measure that assesses the severity of mental health symptoms that are important across psychotic disorders, including delusions, hallucinations, disorganized speech, abnormal psychomotor behavior, negative symptoms. Each item on the measure is rated on a 5-point scale (0=none; 1=equivocal; 2=present, but mild; 3=present and moderate; and 4=present and severe). Total Score is taken as summation. A higher score indicates a more severe condition. Worsened or improved is defined as increase or decrease compared to baseline. (NCT02431702)
Timeframe: Baseline, up to 9 Months

InterventionParticipants (Count of Participants)
Hallucinations72513608Hallucinations72513614Delusions72513614Delusions72513608Disorganized Speech72513614Disorganized Speech72513608Abnormal Psychomotor Behavior72513614Abnormal Psychomotor Behavior72513608Negative Symptoms72513608Negative Symptoms72513614Impaired Cognition72513614Impaired Cognition72513608Mania72513608Mania72513614Depression72513608Depression72513614
UnchangedImprovedWorsened
Part-2: OAP19
Part-2: Paliperidone Palmitate (PP)29
Part-2: OAP73
Part-2: Paliperidone Palmitate (PP)14
Part-2: OAP33
Part-2: Paliperidone Palmitate (PP)10
Part-2: OAP20
Part-2: Paliperidone Palmitate (PP)23
Part-2: OAP70
Part-2: OAP35
Part-2: OAP13
Part-2: Paliperidone Palmitate (PP)36
Part-2: OAP85
Part-2: Paliperidone Palmitate (PP)12
Part-2: OAP27
Part-2: Paliperidone Palmitate (PP)9
Part-2: OAP14
Part-2: Paliperidone Palmitate (PP)37
Part-2: OAP86
Part-2: Paliperidone Palmitate (PP)4
Part-2: OAP25
Part-2: Paliperidone Palmitate (PP)16
Part-2: OAP61
Part-2: Paliperidone Palmitate (PP)17
Part-2: OAP39
Part-2: Paliperidone Palmitate (PP)13
Part-2: OAP29
Part-2: Paliperidone Palmitate (PP)22
Part-2: OAP52
Part-2: Paliperidone Palmitate (PP)15
Part-2: OAP44
Part-2: Paliperidone Palmitate (PP)1
Part-2: OAP7
Part-2: Paliperidone Palmitate (PP)47
Part-2: OAP107
Part-2: Paliperidone Palmitate (PP)2
Part-2: OAP11
Part-2: Paliperidone Palmitate (PP)7
Part-2: OAP28
Part-2: Paliperidone Palmitate (PP)33
Part-2: OAP74
Part-2: OAP23

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Part-2 (Disease Progression): Time to First Treatment Failure

Treatment failure is defined as the time from participant's randomization to first treatment failure, which was a composite endpoint consisting of any of the following: 1) Psychiatric hospitalization due to worsening symptoms; 2) Any deliberate self-injury, suicidal ideation or behavior, homicidal ideation or violent behavior that is clinically significant and needs immediate intervention as determined by the study physician; 3) New arrest/incarceration; 4) Discontinuation of antipsychotic treatment due to inadequate efficacy as determined by the study physician; 5) Discontinuation of antipsychotic treatment due to safety or tolerability as determined by the study physician; 6) Treatment supplementation with another antipsychotic due to inadequate efficacy as determined by the study physician; 7) Increase in the level of psychiatric services in order to prevent imminent psychiatric hospitalization as determined by the study physician. (NCT02431702)
Timeframe: From Day 1 up to 9 Months

Interventiondays (Median)
Part-2: Paliperidone Palmitate (PP)NA
Part-2: OAPNA

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Part 3 (Extended Disease Progression [EDP]): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP1.6
Part 3-OAP to OAP3.2

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Part 3 (EDP): Time to First Treatment Failure

Treatment failure is defined as the time from participant's randomization to first treatment failure, which was a composite endpoint consisting of any of the following: 1) Psychiatric hospitalization due to worsening symptoms; 2) Any deliberate self-injury, suicidal ideation or behavior, homicidal ideation or violent behavior that is clinically significant and needs immediate intervention as determined by the study physician; 3) New arrest/incarceration; 4) Discontinuation of antipsychotic treatment due to inadequate efficacy as determined by the study physician; 5) Discontinuation of antipsychotic treatment due to safety or tolerability as determined by the study physician; 6) Treatment supplementation with another antipsychotic due to inadequate efficacy as determined by the study physician; 7) Increase in the level of psychiatric services in order to prevent imminent psychiatric hospitalization as determined by the study physician. (NCT02431702)
Timeframe: From Day 1 Up to 18 Months

Interventiondays (Median)
Part 3-PP to PPNA
Part 3-OAP to OAPNA

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Part 3 (EDP): Change From Baseline in Working Memory Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess working memory of participants. The range of working memory score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP-1.7
Part 3-OAP to OAP0.7

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Part 3 (EDP): Change From Baseline in Visual Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess visual learning score of participants. The range of visual learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP0.2
Part 3-OAP to OAP-0.2

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Part 3 (EDP): Change From Baseline in Verbal Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess verbal learning score of participants. The range of verbal learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP0.3
Part 3-OAP to OAP0.8

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Part 3 (EDP): Change From Baseline in Speed of Processing Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess speed of processing score of participants. The range of speed of processing score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP2.5
Part 3-OAP to OAP4.9

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Part 3 (EDP): Change From Baseline in Social Cognition Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess social cognition score of participants. The range of social cognition score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP-0.2
Part 3-OAP to OAP1.4

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Part 3 (EDP): Change From Baseline in Reasoning and Problem Solving: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess reasoning and problem solving score of participants. The range of reasoning and problem solving T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP3.4
Part 3-OAP to OAP4.7

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Part 3 (EDP): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Score

The Medication Satisfaction Questionnaire (MSQ) is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). Total score ranges from 1 to 7. Higher score indicate improvement. (NCT02431702)
Timeframe: Baseline, up to 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP0.3
Part 3-OAP to OAP0.4

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Part 3 (EDP): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Each domain was assessed on a 6-point scale, from 1 (absent) to 6 (very severe) (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe). PSP total score was calculated as sum of all the domain scores and ranges from 1 to 100. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. Higher score indicate better performance. (NCT02431702)
Timeframe: Baseline and 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP7.5
Part 3-OAP to OAP7.0

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Part 3 (EDP): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score

"The Clinical Global Impression Severity (CGI-S) rating scale is used to rate the severity of a participant's overall clinical condition on a 7 point scale. The total score ranges from 1 to 7, where 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT02431702)
Timeframe: Baseline, up to 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP-0.7
Part 3-OAP to OAP-0.7

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Part 3 (EDP): Change From Baseline in Attention/Vigilance Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess attention/vigilance score of participants. The range of attention/vigilance score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP2.4
Part 3-OAP to OAP0.7

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Part 3 (EDP): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and 18 Months

Interventionratio (Mean)
Part 3-PP to PP-0.001
Part 3-OAP to OAP-0.003

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Part 3 (Disease Modification): Personal and Social Performance (PSP) Total Observed Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Score ranges from 1 to 100, divided into 10 equal intervals to rate degree of difficulty (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe) in each of the 4 domains. Based on 4 domains there will be 1 transformed total score. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. (NCT02431702)
Timeframe: Month 9 of Part 3

Interventionunits on a scale (Least Squares Mean)
Part 3-PP to PP67.6
Part 3- OAP to PP (or Delayed-Start PP)66.1
Part 3-OAP to OAP66.6

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Part 3 (Disease Modification): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part 3- PP to PP-0.7
Part 3- OAP to PP (or Delayed-Start PP)-0.2
Part 3-OAP to OAP0.5

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Part 3 (Disease Modification): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (SE MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and Month 9 of Part 3

Interventionratio (Least Squares Mean)
Part 3-PP to PP-0.7
Part 3- OAP to PP (or Delayed-Start PP)-0.2
Part 3-OAP to OAP0.5

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Part 2 (Disease Progression): Change From Baseline in Working Memory Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess working memory of participants. The range of working memory score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP-0.8

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Number of Participants With Medication Treatment Modifications (MTM)

Information on MTMs derived from data collected in the clinical assessment of the schizophrenia patient (CASP) questionnaire. The CASP captured changes in medications, changes in psychosocial treatments, visit frequency, and the need for any acute interventions. The CASP comprised of 3 sections covering several parameters. The CASP captured changes in treatment options which was used to compute MTM, as well as factors in clinical decision making and the influence of antipsychotic medication plasma levels (AMPL), when they were available, on clinical decision making. (NCT02462473)
Timeframe: Up to Week 12

InterventionParticipants (Number)
Cohort 14

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Adherence to Antipsychotic Medication as Assessed by Brief Adherence Rating Scale (BARS) at Week 0 and 12

The BARS is a 4-item scale that includes 3 questions and an overall visual analog rating scale that assesses participant's knowledge about his/her medication. The key measure of adherence is the visual analog scale and assesses the percentage of doses taken by the participants in the past month (0 percent [%] - 100%). The 3 questions include: number of prescribed doses per day, number of days in the past month when the participant did not take the prescribed doses, and the number of days in the past month when the participant took less than the prescribed dose. Due to early study termination collected data was not summarized. Hence, individual data for each participant was reported. (NCT02462473)
Timeframe: Week 0, Week 12

Interventionpercent adherence (Number)
Participant 1 (Week 0)Participant 1 (Week 12)Participant 2 (Week 0)Participant 2 (Week 12)Participant 3 (Week 0)Participant 3 (Week 12)Participant 4 (Week 0)Participant 5 (Week 0)Participant 5 (Week 12)Participant 6 (Week 0)Participant 6 (Week 12)Participant 7 (Week 0)Participant 7 (Week 12)Participant 8 (Week 0)Participant 8 (Week 12)Participant 9 (Week 0)Participant 9 (Week 12)
Cohort 110010010010010010097939090969095100100100100

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Clinician's Rating Scale of Adherence (CRS) Score at Week 0 and 12

The CRS is an ordinal scale filled by the clinician. The scores range from 1 to 7 that were used to quantify the clinician's assessment of treatment adherence by the patient. Higher scores indicate greater adherence. Due to early study termination collected data was not summarized. Hence, individual data for each participant was reported. (NCT02462473)
Timeframe: Week 0, Week 12

Interventionunits on a scale (Number)
Participant 1 (Week 0)Participant 1 (Week 12)Participant 2 (Week 0)Participant 2 (Week 12)Participant 3 (Week 0)Participant 3 (Week 12)Participant 4 (Week 0)Participant 5 (Week 0)Participant 5 (Week 12)Participant 6 (Week 0)Participant 6 (Week 12)Participant 7 (Week 0)Participant 7 (Week 12)Participant 8 (Week 0)Participant 8 (Week 12)Participant 9 (Week 0)Participant 9 (Week 12)
Cohort 177777777777777777

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Clinical Global Impression-Severity (CGI-S) Score at Week 0 and 12

Clinical Global Impression-Severity (CGI-S) rating scale used to rate the severity of a participant's overall clinical condition on a 7-point scale ranging from 1 (not ill) to 7 (extremely severe). Due to early study termination collected data was not summarized. Hence, individual data for each participant was reported. (NCT02462473)
Timeframe: Week 0, Week 12

Interventionunits on a scale (Number)
Participant 1 (Week 0)Participant 1 (Week 12)Participant 2 (Week 0)Participant 2 (Week 12)Participant 3 (Week 0)Participant 3 (Week 12)Participant 4 (Week 0)Participant 5 (Week 0)Participant 5 (Week 12)Participant 6 (Week 0)Participant 6 (Week 12)Participant 7 (Week 0)Participant 7 (Week 12)Participant 8 (Week 0)Participant 8 (Week 12)Participant 9 (Week 0)Participant 9 (Week 12)
Cohort 143434453333344333

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Dimensions of Psychosis Symptom Severity Scale (DPSS) Total Score at Week 0 and 12

The DPSS is a clinician-rated scale used to rate 8 domains commonly seen in patients with psychotic disorders. Each domain was rated on a 5-point scale (0 to 4) with anchored description of endpoints. Total score was computed by summing the scores of individual items (range of 0-32). Higher scores represent more severe condition. Due to early study termination collected data was not summarized. Hence, individual data for each participant was reported. (NCT02462473)
Timeframe: Week 0, Week 12

Interventionunits on a scale (Number)
Participant 1 (Week 0)Participant 1 (Week 12)Participant 2 (Week 0)Participant 2 (Week 12)Participant 3 (Week 0)Participant 3 (Week 12)Participant 4 (Week 0)Participant 5 (Week 0)Participant 5 (Week 12)Participant 6 (Week 0)Participant 6 (Week 12)Participant 7 (Week 0)Participant 7 (Week 12)Participant 8 (Week 0)Participant 8 (Week 12)Participant 9 (Week 0)Participant 9 (Week 12)
Cohort 11248288149474584446

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Antipsychotic Medication Plasma Levels (AMPL) During the Active Assessment Phase at Week 12

AMPL of the individual participant during the active assessment phase was reported. (NCT02462473)
Timeframe: Week 12

Interventionnanogram per milliliter (Number)
Participant 1- ARIPIPRAZOLEParticipant 1- DEHYDROARIPIPRAZOLEParticipant 2- OLANZAPINEParticipant 2- PALIPERIDONEParticipant 3- 7-OH QUETIAPINEParticipant 3-NORQUETIAPINEParticipant 3-QUETIAPINEParticipant 3-QUETIAPINE SULFOXIDEParticipant 5-7-OH QUETIAPINEParticipant 5-NORQUETIAPINEParticipant 5-QUETIAPINEParticipant 5-QUETIAPINE SULFOXIDEParticipant 6-ARIPIPRAZOLEParticipant 6-DEHYDROARIPIPRAZOLEParticipant 7-PALIPERIDONEParticipant 7-RISPERIDONEParticipant 8-ARIPIPRAZOLEParticipant 8-DEHYDROARIPIPRAZOLEParticipant 9- 7-OH QUETIAPINEParticipant 9- NORQUETIAPINEParticipant 9- PALIPERIDONEParticipant 9- QUETIAPINEParticipant 9- QUETIAPINE SULFOXIDEParticipant 9- RISPERIDONE
Cohort 1596.00139.0027.3045.1043.10660.00280.00660.007.72153.0050.30321.00464.00112.0031.0026.20168.0033.000.2002.000.1002.002.000.100

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Number of Participants With Factors Considered in Clinical Decision as Assessed by Clinical Assessment of the Schizophrenia Patient (CASP)

The CASP and data on concomitant medications and psychosocial treatments were used to evaluate the impact of AMPL results on other aspects of clinical decision making. (NCT02462473)
Timeframe: Up to Week 12

Interventionparticipants (Number)
Side Effects Of MedicationAttitude Toward TreatmentReport of Increased SymptomsReport of Decrease in SymptomsPatient Still SymptomaticPatient Ideation
Cohort 1324311

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Patient Satisfaction Survey (PSS) Total Score at Week 0 and 12

The PSS is a brief scale designed to capture a psychiatric patient's satisfaction with a clinician. The scale covers 6 domains: Trust (3 items), Communication (3 items), Exploration of Ideas/Options (2 items), Body Language (2 items), Active Listening (4 items), and Miscellaneous Items (6 items). Out of the 20 items, the first 19 are scored on a 5-point Likert Scale (1=strongly disagree, 2=disagree, 3=satisfactory, 4=agree, 5=strongly agree). The last question (6f) is a free-response question asking for input on how the clinician might improve. Sum of scores of individual items give a total score (range 9-95). Higher scores indicate greater degree of satisfaction. Due to early study termination collected data was not summarized. Hence, individual data for each participant was reported. (NCT02462473)
Timeframe: Week 0, Week 12

Interventionunits on a scale (Number)
Participant 1 (Week 0)Participant 1 (Week 12)Participant 2 (Week 0)Participant 2 (Week 12)Participant 3 (Week 0)Participant 3 (Week 12)Participant 4 (Week 0)Participant 5 (Week 0)Participant 5 (Week 12)Participant 6 (Week 0)Participant 6 (Week 12)Participant 7 (Week 0)Participant 7 (Week 12)Participant 8 (Week 0)Participant 8 (Week 12)Participant 9 (Week 0)Participant 9 (Week 12)
Cohort 17676525757574866647676767263727176

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Response at Week 10, Defined as ≥50% Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Randomization

PANSS total score administered by the investigator. It included 3 sub-scales with a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A higher score corresponded to a worse severity of schizophrenia. A reduction in score indicates improvement. (NCT02717195)
Timeframe: From Randomization to Week 10

InterventionParticipants (Count of Participants)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg10
DBT Period, Lu AF35700 20 mg4
DBT Period, Continued Treatment From PC Period6

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Change From Randomization to Week 10 in Positive and Negative Syndrome Scale (PANSS) Total Score

PANSS total score administered by the investigator. It included 3 sub-scales with a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A higher score corresponded to a worse severity of schizophrenia. (NCT02717195)
Timeframe: From Randomization to Week 10

Interventionunits on a scale (Mean)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg-10.01
DBT Period, Lu AF35700 20 mg-8.22
DBT Period, Continued Treatment From PC Period-9.90

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Response at Week 10, Defined as ≥40% Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Randomization

PANSS total score administered by the investigator. It included 3 sub-scales with a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A higher score corresponded to a worse severity of schizophrenia. A reduction in score indicates improvement. (NCT02717195)
Timeframe: From Randomization to Week 10

InterventionParticipants (Count of Participants)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg23
DBT Period, Lu AF35700 20 mg15
DBT Period, Continued Treatment From PC Period16

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Response at Week 10, Defined as ≥30% Reduction in PANSS Total Score From Randomization

Positive and Negative Syndrome Scale (PANSS) total score administered by the investigator. It included 3 sub-scales with a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A higher score corresponded to a worse severity of schizophrenia. A reduction in score indicates improvement. (NCT02717195)
Timeframe: From Randomization to Week 10

InterventionParticipants (Count of Participants)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg42
DBT Period, Lu AF35700 20 mg30
DBT Period, Continued Treatment From PC Period45

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Response at Week 10, Defined as ≥20% Reduction in PANSS Total Score, PANSS (Positive and Negative Syndrome Scale) Total Score ≤70, CGI-S (Clinical Global Impression Scale - Severity of Illness) Score <4

"PANSS total score administered by the investigator. It included 3 sub-scales with a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A higher score corresponded to a worse severity of schizophrenia. A reduction in score indicates improvement.~The Clinical Global Impression scale - severity of illness (CGI-S) is administered by the investigator. The patient is rated on a 7-point scale ranging from 1 (Normal - not at all ill) to 7 (among the most extremely ill patients). A reduction in scale indicates improvement." (NCT02717195)
Timeframe: From Randomization to Week 10

InterventionParticipants (Count of Participants)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg21
DBT Period, Lu AF35700 20 mg18
DBT Period, Continued Treatment From PC Period12

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Change From Randomization to Week 10 in PSP Total Personal and Social Performance (PSP) Total Score

PSP is a clinician-rated scale designed and validated to measure a patient's current level of social functioning. It consists of 4 items: socially useful activities, personal and social relationships, self-care, and disturbing and aggressive behaviours. Each items were assessed on a 6-point scale, from 1 (absent) to 6 (very severe). PSP score was calculated as sum of all the items on the scale and ranged from 4 to 100. A higher score represents more severe functional impairment. (NCT02717195)
Timeframe: From Randomization to Week 10

Interventionunits on a scale (Mean)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg4.90
DBT Period, Lu AF35700 20 mg3.23
DBT Period, Continued Treatment From PC Period3.94

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Change From Randomization to Week 10 in Global Clinical Impression - Severity of Illness (CGI-S) Score

CGI-S provides the clinician's impression of the patient's current state of mental illness. The clinician uses his or her clinical experience of this patient population to rate the severity of the patient's current mental illness on a 7-point scale ranging from 1 (Normal - not at all ill) to 7 (among the most extremely ill patients). Higher scores indicate worsening. (NCT02717195)
Timeframe: From Randomization to Week 10

Interventionunits on a scale (Mean)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg-0.59
DBT Period, Lu AF35700 20 mg-0.54
DBT Period, Continued Treatment From PC Period-0.57

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Response at Week 10, Defined as ≥20% Reduction in Positive and Negative Syndrome Scale (PANSS) Total Score From Randomization

PANSS total score administered by the investigator. It included 3 sub-scales with a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A higher score corresponded to a worse severity of schizophrenia. A reduction in score indicates improvement. (NCT02717195)
Timeframe: From Randomization to Week 10

InterventionParticipants (Count of Participants)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg82
DBT Period, Lu AF35700 20 mg59
DBT Period, Continued Treatment From PC Period77

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Overall Survival

Defined as the time from screening to death if the patient dies within the period that the site is open (NCT02875340)
Timeframe: 6 months

Interventionweeks (Mean)
VAL401 Treatment - Intention to Treat Group7.8
VAL401 Treatment - Per Protocol Group10.9

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Peak Plasma Concentration (Cmax)

Assessment of Cmax in collected blood samples on Day 1 and Day 15 of Cycle 1, collected at time points: pre-dose (0h) then 10, 15, 30 minutes, 1, 2, 4, 8, 10 and 24 hours after administration of VAL401. (NCT02875340)
Timeframe: 1 Day and 2 weeks

Interventionng/mL (Mean)
VAL401 Treatment - Day 130.5
VAL401 Treatment - Day 15 (2 mg)20
VAL401 Treatment - Day 15 (6 mg)102
VAL401 Treatment - Day 15 (8 mg)464

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Plasma VAL401 Half-life (t 1/2)

Assessment of plasma half-life of VAL401 (t 1/2) in collected blood samples on Day 1 and Day 15 of Cycle 1, collected at time points: pre-dose (0h) then 10, 15, 30 minutes, 1, 2, 4, 8, 10 and 24 hours after administration of VAL401. (NCT02875340)
Timeframe: 1 Day and 2 weeks

Interventionhours (Mean)
VAL401 Treatment - Day 19
VAL401 Treatment - Day 15 (2 mg)26
VAL401 Treatment - Day 15 (6 mg)30
VAL401 Treatment - Day 15 (8 mg)16

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Progression-free Survival (PFS)

PFS is defined as the time from screening to disease progression (or death if the patient died before progression), with progression date nominally defined as the date the patient was withdrawn from the trial, where the Principal Investigator has determined by their professional discretion the patient has symptomatic disease progression. (NCT02875340)
Timeframe: 6 months

Interventionweeks (Mean)
VAL401 Treatment - Intention to Treat Group5.2
VAL401 Treatment - Per Protocol Group7.2

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Trough Plasma Concentration (Cmin)

Assessment of trough plasma concentration (Cmin) in collected blood samples on Day 1 and Day 15 of Cycle 1, collected at time points: pre-dose (0h) then 10, 15, 30 minutes, 1, 2, 4, 8, 10 and 24 hours after administration of VAL401. (NCT02875340)
Timeframe: 1 Day and 2 weeks

Interventionng/mL (Mean)
VAL401 Treatment - Day 110.125
VAL401 Treatment - Day 15 (2 mg)11
VAL401 Treatment - Day 15 (6 mg)35
VAL401 Treatment - Day 15 (8 mg)111

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Number of Patients With Disease Control

"Objective tumour response rates according to RECIST 1.1 for target lesions and assessed by CT:~Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Progressive Disease (PD): At least a 20% increase in the sum of diameters of target lesions; Stable Disease (SD): Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD." (NCT02875340)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Participants receiving mid-treatment CT scanPrimary target tumour increased by 10% or lessParticipants demonstrating Complete ResponseParticipants demonstrating Partial ResponseParticipants demonstrating Progressive diseaseParticipants demonstrating Stable Disease
VAL401 Treatment220002

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Number of Participants Reporting Adverse Events and Serious Adverse Events

Ongoing evaluation of Adverse Events during treatment with VAL401. Events assessed for number of patients affected, severity of event, likelihood of event being related to the drug treatment and whether the event is an expected/known side effect of Risperidone. (NCT02875340)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Adverse Events reported72513356Serious Adverse Events Reported72513356
Number participants reporting eventsNumber participants reporting no events
VAL401 Treatment8
VAL401 Treatment0
VAL401 Treatment1
VAL401 Treatment7

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Patient Quality of Life During VAL401 Treatment

Changes in patient quality of life measured by EORTC Health-related Quality of Life (HRQoL) assessment questionnaire QLQ-C30 (Cancer specific questionnaire). (NCT02875340)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
ECOG data72513356Improvement in pain72513356Improvement in Insomnia72513356Improvement in lack of appetite72513356Improvement in nausea/vomiting72513356Improvement in fatigue72513356Improvement in irritability72513356Improvement in depression72513356Improvement in anxiety72513356Improvement in diarrhoea72513356
Status maintainedNot measuredStatus deterioratedStatus improved
VAL401 Treatment4
VAL401 Treatment0
VAL401 Treatment3
VAL401 Treatment2
VAL401 Treatment1

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"Number of Participants With Response to Treatment"

"Response to treatment was defined as a 50% reduction from baseline scores in Hamilton Rating Scale for Depression (HRSD)and Young Mania Rating Scale (YMRS) scales HRSD was developed to evaluate and quantify depression.Its abbreviated version,. Scoring is based on the 17-item scale and scores of 0-7 are considered as being normal. The cutoff points are: 8-17 for mild depression,18-24 for moderate depression, and 25 or more for severe depression. The maximum score being 52 on the 17-point scale.~YMRS is is the most widely used assessment tool for manic symptoms. The scale consists of 11 items .The YMRS follows the style of the Hamilton Rating Scale for Depression (HAM-D) with each item given a severity rating. There are four items that are graded on a 0 to 8 scale (irritability, speech, thought content, and disruptive/agressive behavior), while the remaining seven items are graded on a 0 to 4 scale. Scores of YMRS > 20 generates indicate mania" (NCT02918097)
Timeframe: 8 weeks

InterventionParticipants (Count of Participants)
Lithium Carbonate65

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Number of Participants With Remission to Treatment

The remission outcome was established as obtaining three consecutive visits with scores of values considered asymptomatic Hamilton Rating Scale for Depression(HRSD <7 points) and Young Mania Rating Scale (YMRS <6 points) during the trial. The subjects that were asymptomatic for at least 6-8 month were considered to be in partial remission and complete if at least 12 months without symptoms, according to Diagnostic and Statistical Manual of Mental Disorders (DSM-IV). (NCT02918097)
Timeframe: 8 months

InterventionParticipants (Count of Participants)
Lithium Carbonate21

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Quality of Life Instrument Scores

"Quality of Life - WHOQOL -BREF instrument scores~scores 0-20 . higher scores mean a better outcome." (NCT02918097)
Timeframe: 12 weeks

Interventionscore on a scale (Mean)
Lithium Carbonate10.58

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Number of Participants With Relapse

The definition of relapse is as follows 1.50% or greater increase in total DIEPSS score, 2. an increase in the total PANSS score of 25% or more from baseline, 3. deliberate self-injury, 4. emergence of clinically significant suicidal ideation, 5. violent behavior resulting in clinically significant injury to another person or property damage. (NCT03019887)
Timeframe: One year after the baseline cognitive function test or three months after the end of dose reduction, whichever came first.

InterventionParticipants (Count of Participants)
Dose Reduction130

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Least Squares Mean (LSM) Change From Baseline in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 4

The LSM change from baseline at week 4 was assessed for PANSS total score. The PANSS assesses the severity of schizophrenia symptoms through a clinician-rated inventory of 30 items organized in 3 subscales: 1) positive subscale (7 items); 2) negative subscale (7 items); and 3) general psychopathology subscale (16 items). For each item, symptoms are scored from 1 (absent) to 7 (extreme) and sum to a total PANSS score (range: 30-210). Higher scores reflect more severe symptoms of schizophrenia. Further, reduced symptom severity over time is reflected by decreases in score. (NCT03055338)
Timeframe: Baseline and Week 4

InterventionScore on a Scale (Least Squares Mean)
MK-8189-14.6
Risperidone-17.2
Placebo-10.0

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Percentage of Participants Experiencing an Adverse Event (AE)

The percentage of participants experiencing an AE was assessed. An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product or protocol-specified procedure, whether or not considered related to the medicinal product or protocol-specified procedure. Any worsening of a preexisting condition that is temporally associated with the use of the Sponsor's product, is also an AE. (NCT03055338)
Timeframe: Up to 6 weeks

InterventionPercentage of Participants (Number)
MK-818971.1
Risperidone77.8
Placebo53.9

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Percentage of Participants Discontinuing Study Treatment Due to an Adverse Event

The percentage of participants discontinuing study treatment due to an AE was assessed. An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product or protocol-specified procedure, whether or not considered related to the medicinal product or protocol-specified procedure. Any worsening of a preexisting condition that is temporally associated with the use of the Sponsor's product, is also an AE. (NCT03055338)
Timeframe: Up to 4 weeks

InterventionPercentage of Participants (Number)
MK-81896.7
Risperidone8.9
Placebo7.9

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Least Squares Mean (LSM) Change From Baseline in the Clinical Global Impression-Severity of Illness (CGI-S) Score at Week 4

The LSM change from baseline at week 4 was assessed for CGI-S score. The CGI-S is a 7-point clinician-rated scale for assessing the global severity of the participant's illness. Possible CGI-S scores range from 1 (participant normal, not ill) to 7 (participant extremely ill). Further, a decrease in CGI-S score indicates reduced severity of the participant's illness. (NCT03055338)
Timeframe: Baseline and Week 4

InterventionScore on a Scale (Least Squares Mean)
MK-8189-0.9
Risperidone-1.0
Placebo-0.7

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PSP Total Score From Baseline at Each Post-baseline Assessment Time Point

"Personal and Social Performance Scale (PSP) total score mean change from baseline at each post-baseline assessment time point.~The PSP is a 100-point single-item rating scale that is based on 4 domains: family and social functioning, self-care, work and socially useful activities, and disturbing and aggressive behaviors. Each domain is rated in 6 degrees of severity (absent, mild, manifest, marked, severe, very severe). On the PSP scale, higher scores indicate better social functioning: 71-100 indicates mild to no functional impairment; 31-70 varying degrees of disability and 1-30, minimal functioning needing intense support and/or supervision. Participants with a PSP total score of 71 to 100 were considered to have mild functional difficulty. Scores of 31 to 70 represented varying degrees of disability (31 to 70) and ratings of 1 to 30 indicated minimal functioning that required intense support and/or supervision." (NCT03160521)
Timeframe: Day 1 (Baseline), Days 29, 57 and 85 (or the last post-baseline assessment)

,
Interventionscore on a scale (Mean)
BaselineStudy Day 29Study Day 57Study Day 85
Placebo50.4655.3757.0754.54
Risperidone ISM49.9359.0361.3360.60

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Plasma PK Parameters

"Plasma PK Parameters of Risperidone Active Moiety~Cmax values are estimated and based on the plasma level of Day 3 for each dosing Interval; Cmin are the trough levels of Day 29, which is at the end of each dosing Interval;" (NCT03160521)
Timeframe: Day 3 and Day 29 after Dose 1, 2 and 3

,
Interventionng/mL (Mean)
Dose 1/Estimated Cmax/Day 3Dose 1/Estimated Cmin/Day 29Dose 2/Estimated Cmax/Day 3Dose 2/Estimated Cmin/Day 29Dose 3/Estimated Cmax/Day 3Dose 3/Estimated Cmin/Day 29
Risperidone ISM 100 mg32.0026.7153.4427.2350.0926.14
Risperidone ISM 75 mg27.6119.2138.9517.4637.1620.16

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PANSS Total Score Mean Change From Baseline to Endpoint

"The Positive and Negative Syndrome Scale (PANSS) is a 30-item clinician-rated instrument for assessing the symptoms of schizophrenia.The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score is the sum of all 30 PANSS items and ranges from 30 to 210, with 30 indicating absence of symptoms of schizophrenia and 210 indicating extreme ratings of all 30 symptoms. Negative change from baseline scores indicate improvements in symptoms whereas higher scores mean a worse outcome.~Endpoint is defined as study day 85 or the last post-baseline assessment if early discontinuation." (NCT03160521)
Timeframe: Day 1 (Baseline) and Day 85 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Risperidone ISM 75 mg-24.6
Risperidone ISM 100 mg-24.7
Placebo-11.0

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PANSS Response Rate at Endpoint

"The definition of Positive and Negative Syndrome Scale (PANSS) response was a decrease from baseline in PANSS total score of ≥ 30% (improvement of symptoms).~Endpoint is defined as study day 85 or the last post-baseline double-blind assessment if early discontinuation." (NCT03160521)
Timeframe: Day 85 or the last post-baseline assessment

Interventionpercentage of participants (Number)
Risperidone ISM 75 mg41.9
Risperidone ISM 100 mg34.9
Placebo9.1

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PANSS Positive Subscale Mean Change From Baseline to Endpoint

"The PANSS consisted of three subscales that contained a total of 30 symptom constructs. For each symptom construct, severity is rated on a 7-point scale, with a score of 1 indicated the absence of symptoms and a score of 7 indicated extremely severe symptoms. In positive subscale, the 7 positive symptom constructs were: delusions, conceptual disorganization, hallucinatory behavior, excitement, grandiosity, suspiciousness/persecution, and hostility.~PANSS Positive Subscale Score ranges from 7 (absence of symptoms) to 49 (extremely severe symptoms).~Endpoint is defined as study day 85 or the last post-baseline assessment if early discontinuation." (NCT03160521)
Timeframe: Day 1 (Baseline) and Day 85 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Risperidone ISM 75 mg-8.0
Risperidone ISM 100 mg-8.7
Placebo-4.1

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SWN-20 Total Score From Baseline at Each Post-baseline Assessment Time Point

"20-item Subjective Well-Being Under Neuroleptics Treatment Scale (SWN-20) total score mean change from baseline at each post-baseline assessment time point.~The SWN is a 38-item instrument to measure subjective effects of neuroleptic medications in patients with schizophrenia and consists of 20 positive statements and 18 negative statements. The short form of the SWN, the 20-item SWN-20, was developed in order to allow for quick assessment of subjective side effects in a clinical setting. Like in the original SWN, with the SWN-20 the patient is asked to rate well-being items that have been identified as related to antipsychotic treatment on a 6-point scale ranging from Not at all to Very much. The SWN-20 is scored on a scale ranging from 20 to 120, with higher scores indicating better health-related quality of life (HRQL). The SWN-20 contains five 4-item subscales: mental functioning, self-control, emotional regulation, physical functioning, and social integration. Eac" (NCT03160521)
Timeframe: Day 1 (Baseline), Days 29, 57 and 85 or the last post-baseline assessment

,
Interventionscore on a scale (Mean)
BaselineDay 29Day 57Day 85
Placebo80.2883.2386.3285.50
Risperidone ISM80.8686.9088.2689.14

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PANSS General Psychopathology Subscale Mean Change From Baseline to Endpoint

"The PANSS consisted of three subscales that contained a total of 30 symptom constructs. For each symptom construct, severity is rated on a 7-point scale, with a score of 1 indicated the absence of symptoms and a score of 7 indicated extremely severe symptoms. The general psychopathology scale consists of 16 items which measure somatic concern, anxiety, guilt feelings, tension, mannerisms and posturing, depression, motor retardation, uncooperativeness, unusual thought content, disorientation, poor attention, lack of judgment and insight, disturbance of volition, poor impulse control, preoccupation and active social avoidance. PANSS General Psychopathology Subscale Score ranges from 16 (absence of symptoms) to 112 (extremely severe symptoms).~Endpoint is defined as study day 85 or the last post-baseline assessment if early discontinuation." (NCT03160521)
Timeframe: Day 1 (Baseline) and Day 85 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Risperidone ISM 75 mg-12.8
Risperidone ISM 100 mg-12.4
Placebo-5.6

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Overall Response Rate at Endpoint

"Overall response was defined as either PANSS total score ≥ 30% decrease from baseline, or CGI-I score of 2 (much improved) or 1 (very much improved).~Endpoint is defined as study day 85 or the last post-baseline assessment if early discontinuation." (NCT03160521)
Timeframe: Day 85 or the last post-baseline assessment

Interventionpercentage of participants (Number)
Risperidone ISM 75 mg59.7
Risperidone ISM 100 mg54.3
Placebo20.5

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CGI-S Total Score Mean Change From Baseline to Endpoint

"The Clinician Global Impression - Severity (CGI-S) score is a 7-point clinician-rated scale for assessing the global severity of the illness. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Negative change from baseline scores indicate improvement in the severity of illness whereas higher scores mean a worse outcome.~Endpoint is defined as study day 85 or the last post-baseline assessment if early discontinuation." (NCT03160521)
Timeframe: Day 1 (Baseline) and Day 85 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Risperidone ISM 75 mg-1.3
Risperidone ISM 100 mg-1.3
Placebo-0.6

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CGI-I Score Mean at Endpoint

"The Clinical Global Impression - Improvement (CGI-I) Score consists of a single 7-point rating score total improvement, regardless of whether or not the change it is due entirely to drug treatment.~Scores are: 1, Very much improved; 2, Much improved; 3, Minimally improved; 4, No change; 5, Minimally worse; 6, Much worse; or 7, Very much worse.~Endpoint is defined as study day 85 or the last post-baseline double-blind assessment if early discontinuation." (NCT03160521)
Timeframe: Day 1 (Baseline) and Day 85 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Risperidone ISM 75 mg2.5
Risperidone ISM 100 mg2.5
Placebo3.3

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PANSS Negative Subscale Mean Change From Baseline to Endpoint

"The PANSS consisted of three subscales: a total of 30 symptom constructs. For each symptom construct, severity was rated on a 7-point scale, with a score of 1 indicated- absence of symptoms and a score of 7 indicated- extremely severe symptoms. The PANSS negative subscale score was the sum of the rating scores for the 7 negative scale items from the PANSS panel. The 7 negative symptom constructs were: blunted affect, emotional withdrawal, poor rapport, passive apathetic withdrawal, difficulty in abstract thinking, lack of spontaneity and flow of conversation and stereotyped thinking. PANSS Negative Subscale Score ranges from 7 (absence of symptoms) to 49 (extremely severe symptoms).~Endpoint is defined as study day 85 or the last post-baseline assessment if early discontinuation." (NCT03160521)
Timeframe: Day 1 (Baseline) and Day 85 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Risperidone ISM 75 mg-3.8
Risperidone ISM 100 mg-3.7
Placebo-1.7

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Change From Randomization to Week 8 in Global Clinical Impression - Severity of Illness (CGI-S) Score

CGI-S provides the clinician's impression of the patient's current state of mental illness. The clinician uses his or her clinical experience of this patient population to rate the severity of the patient's current mental illness on a 7-point scale ranging from 1 (normal - not at all ill) to 7 (among the most extremely ill patients). Higher scores indicate worsening (NCT03230864)
Timeframe: From Randomization to Week 8

Interventionunits on a scale (Mean)
DBT, Lu AF35700 10 mg-0.18
DBT, Continued Treatment-0.37

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Change From Randomization to Week 8 in 16-item Negative Symptom Assessment (NSA-16 Total) Score

The NSA-16 is a clinician-rated scale designed to assess the presence, severity, and range of negative symptoms associated with schizophrenia. The NSA-16 consists of 16 items arranged in 5 subdomains: communication dysfunction (items 1 to 4), emotional/affective dysfunction (items 5 to 7), dysfunction in sociality (items 8 to 10), motivational/hedonic dysfunction (items 11 to 14), and reduced psychomotor activity (items 15 and 16), and a Global Negative Symptom Rating. NSA-16 items are rated on a 6-point scale from 1 (behaviour is normal) to 6 (behaviour severely reduced), and a score of 9 if the item is not-rateable. The Global Negative Symptom Rating is rated from 1 (no evidence of symptoms) to 7 (extremely severe symptoms). The 16 items are summed to yield a total score ranging from 16 to 96 and the global rating ranges from 1 to 7. (NCT03230864)
Timeframe: From Randomization to Week 8

Interventionunits on a scale (Mean)
DBT, Lu AF35700 10 mg-2.99
DBT, Continued Treatment-3.14

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Response

Response is defined as a ≥20% reduction in PANSS total score from Randomization (NCT03230864)
Timeframe: at Week 8

InterventionParticipants (Count of Participants)
DBT, Lu AF35700 10 mg6
DBT, Continued Treatment13

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Change From Randomization to Week 8 in Positive and Negative Syndrome Scale (PANSS) Total Score

PANSS total score administered by the investigator. It included a total of 30 items that evaluated the Positive Symptoms subscale, the Negative Symptoms subscale, the General Psychopathology subscale. Each item is rated from 1 (symptom not present) to 7 (symptom extremely severe). PANSS total score was calculated as sum of all the items on the scale and ranged from 30 to 210. A negative score indicates an improvement compared to Randomization. (NCT03230864)
Timeframe: From Randomization to Week 8

Interventionunits on a scale (Mean)
Double-blind Treatment (DBT) Period, Lu AF35700 10 mg-4.71
DBT, Continued Treatment From PC Period-10.19

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Change From Randomization to Week 8 in PANSS Marder Negative Factor Score

The PANSS Negative Factor score is a subset of the PANSS assessing negative symptoms of schizophrenia. The factor consist of the seven items: blunted affect, emotional withdrawal, poor rapport, passive social withdrawal, lack of spontaneity, motor retardation, and active social avoidance which are each rated on a 7-point scale, from 1=absent to 7=extreme. The PANSS Negative Factor score (7 items) range from 7 to 49 with a higher score indicating greater severity of symptoms. (NCT03230864)
Timeframe: From Randomization to Week 8

Interventionunits on a scale (Mean)
DBT, Lu AF35700 10 mg-1.51
DBT, Continued Treatment-1.74

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Number of Participants Who Maintain Stability at the Endpoint

Stability is defined as meeting all of the following criteria for at least 4 consecutive weeks: outpatient status; PANSS total score ≤80; minimal presence of specific psychotic symptoms on the PANSS, as measured by a score of ≤4 on each of the following items: conceptual disorganization, suspiciousness, hallucinatory behavior, and unusual thought content; Clinical Global Impression of Severity (CGI-S) score ≤4 (moderately ill); and CGI-SS score ≤2 (mildly suicidal) on Part 1 and ≤5 (minimally worsened) on Part 2. The last valid participant assessment was used as the endpoint. (NCT03503318)
Timeframe: At the endpoint (up to 108 weeks)

InterventionParticipants (Count of Participants)
Placebo110
TV-46000 q1m159
TV-46000 q2m143

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Number of Participants Achieving Remission at the Endpoint

The remission was achieved for participants who did not relapse during the study and for over a period of at least 6 months preceding the endpoint, maintained scores of = 3 on each of the 8 specific PANSS items: P1 (delusions), G9 (unusual thought content), P3 (hallucinatory behavior), P2 (conceptual disorganization), G5 (mannerisms/posturing), N1 (blunted affect), N4 (social withdrawal), and N6 (lack of spontaneity). The last valid participant assessment was used as the endpoint. (NCT03503318)
Timeframe: At Endpoint (up to 108 weeks)

InterventionParticipants (Count of Participants)
Placebo30
TV-46000 q1m39
TV-46000 q2m42

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Plasma Concentration of Risperidone, 9-OH-risperidone, and Total Active Moiety (Sum of Risperidone and 9-OH-risperidone)

(NCT03503318)
Timeframe: 1 hour prior to dosing at Baseline (Day 1) and at the end of treatment visit (up to 108 weeks)

,,
Interventionng/mL (Mean)
Risperidone at BaselineRisperidone at the End of Treatment9-OH-Risperidone at Baseline9-OH-Risperidone at the End of TreatmentTotal Active Moiety at BaselineTotal Active Moiety at the End of Treatment
Placebo4.6941.32314.9652.98219.0604.078
TV-46000 q1m6.45213.21518.47326.20224.20038.429
TV-46000 q2m5.3648.83815.18717.77819.94525.947

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Number of Participants Reporting Suicidal Behavior and Suicidal Ideation Using Columbia-Suicide Severity Rating Scale (C-SSRS) at Baseline and Post-Baseline

"The C-SSRS is a semi-structured interview that captures the occurrence, severity, and frequency of suicide-related thoughts and behaviors. Suicidal behavior was defined as a yes answer to any of 5 suicidal behavior questions: preparatory acts or behavior, aborted attempt, interrupted attempt, actual attempt, and completed suicide. Suicidal ideation was defined as a yes answer to any one of 5 suicidal ideation questions: wish to be dead, and 4 different categories of active suicidal ideation." (NCT03503318)
Timeframe: Baseline, post-baseline (up to 108 weeks)

,,
InterventionParticipants (Count of Participants)
Baseline: Suicidal behaviorBaseline: Suicidal ideationPost-baseline: Suicidal behaviorPost-baseline: Suicidal ideation
Placebo06312
TV-46000 q1m0517
TV-46000 q2m37112

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Change From Baseline in Total Barnes Akathisia Rating Scale (BARS) Score at the End of Treatment

The BARS is an instrument that assesses the severity of drug-induced akathisia. The BARS includes 3 items for rating objective restless movements, subjective restlessness, and any subjective distress associated with akathisia that were scored on a 4-point scale of 0 (normal/no distress) to 3 (constant restlessness/severe distress). Total score was the sum of scores of each item and ranged from 0-9, with higher scores indicating greater severity of akathisia. (NCT03503318)
Timeframe: Baseline, end of treatment (up to 108 weeks)

,,
Interventionunits on a scale (Mean)
BaselineChange at the End of Treatment
Placebo0.2-0.1
TV-46000 q1m0.10.0
TV-46000 q2m0.2-0.1

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Change From Baseline in Total Abnormal Involuntary Movement Scale (AIMS) Score at the End of Treatment

The AIMS is a 14-item scale that includes assessments of orofacial movements, extremity and truncal dyskinesia, examiner's judgment of global severity, subjective measures of awareness of movements and distress, and a yes/no assessment of problems concerning teeth and/or dentures. Total AIMS score is a sum of item 1 through 7. Items 1 through 7 include facial and oral movements (Items 1-4), extremity movements (Items 5-6), and trunk movements (Item 7). Each item was rated on a 0 (no dyskinesia) to 4 (severe dyskinesia) scale. Total AIMS score for Items 1-7 ranged from 0 to 28; with higher scores indicating greater severity of the condition. (NCT03503318)
Timeframe: Baseline, end of treatment (up to 108 weeks)

,,
Interventionunits on a scale (Mean)
BaselineChange at the End of Treatment
Placebo0.40.0
TV-46000 q1m0.50.1
TV-46000 q2m0.20.1

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Change From Baseline in Simpson-Angus Scale (SAS) Mean Score at the End of Treatment

The SAS is a 10-item instrument for the assessment of neuroleptic-induced parkinsonism. The items on the scale include measurements of hypokinesia, rigidity, glabellar reflex, tremor, and salivation. Each item was rated on a 5-point scale (0 [None/Normal] to 4 [Extreme/Severe]). The mean score was calculated by adding the individual item scores and dividing by 10. The total mean score ranged from 0-4, with a higher score indicating greater severity of symptoms. (NCT03503318)
Timeframe: Baseline, end of treatment (up to 108 weeks)

,,
Interventionunits on a scale (Mean)
BaselineChange at the End of Treatment
Placebo0.070.04
TV-46000 q1m0.090.02
TV-46000 q2m0.060.00

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Change From Baseline in Schizophrenia Quality of Life Scale (SQLS) Total Score at the Endpoint and End of Treatment

The SQLS comprises 33 items categorized in 2 domains: psychosocial feelings (20 items) and cognition and vitality (13 items). The items were scored on a 5-point scale (1 - never, 2 - rarely, 3 - sometimes, 4 - often, 5 - always). Individual domain and total scores were standardized by scoring algorithm to a 0 (best health status) to 100 (worst health status) scale, with higher scores indicating comparatively lower quality of life. The last valid participant assessment was used as the endpoint. (NCT03503318)
Timeframe: Baseline, endpoint and end of treatment (up to Week 108)

,,
Interventionunits on a scale (Mean)
BaselineChange at the EndpointChange at the End of Treatment
Placebo34.00.9-2.3
TV-46000 q1m33.1-4.5-7.2
TV-46000 q2m34.2-4.1-7.3

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Change From Baseline in Drug Attitudes Inventory 10-item Version (DAI-10) Total Score at the Endpoint and End of Treatment

"The DAI-10 is a 10-item questionnaire to assess 1) subjective experience of drug and 2) attitudes and beliefs toward neuroleptics which may influence compliance in schizophrenia participants. The DAI-10 contains 6 items (1, 3, 4, 7, 9, and 10) that a participant who was fully adherent to the prescribed medication answered as True and 4 items (2, 5, 6, and 8) that a participant who was fully adherent to the prescribed medication answered as False. A correct answer was scored +1 and an incorrect answer was scored -1. The total score was the sum of pluses and minuses, which ranged from -10 to 10 in increments of 2. A positive total score indicated a positive subjective response (compliant) and a negative total score indicated a negative subjective response (non-compliance). Higher scores denoted better compliance. The last valid participant assessment was used as the endpoint." (NCT03503318)
Timeframe: Baseline, endpoint and end of treatment (up to Week 108)

,,
Interventionunits on a scale (Mean)
BaselineChange at the EndpointChange at the End of Treatment
Placebo6.1-0.8-0.9
TV-46000 q1m5.80.10.3
TV-46000 q2m5.7-0.30.3

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Change From Baseline in Clinical Global Impression-Severity of Suicidality (CGI-SS) Score at the End of Treatment

The CGI-SS scale provides an overall clinician-rated assessment of the risk of suicidality. The CGI-SS consists of a 5-point scale in Part 1 (the most severe level of suicidality experience) ranging from 1 (not at all suicidal) to 5 (attempted suicide) and a 7-point scale in Part 2 (change in participant suicidality) ranging from 1 (very much improved) to 7 (very much worse). (NCT03503318)
Timeframe: Baseline, end of treatment (up to 108 weeks)

,,
Interventionunits on a scale (Mean)
The most severe level of suicidality experience at BaselineChange in participant suicidality at the End of Treatment
Placebo1.04.0
TV-46000 q1m1.04.0
TV-46000 q2m1.04.0

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Change From Baseline in Calgary Depression Scale for Schizophrenia (CDSS) Score at the End of Treatment

The CDSS is specifically designed to assess the level of depression separate from the positive, negative, and EPS in schizophrenia. This clinician-administered instrument consists of 9 items, each rated on a 4-point scale from 0 (absent) to 3 (severe) that were added together to form the total CDSS depression score of the participant. The total score ranged from 0-27, with higher scores indicating greater severity of the condition. (NCT03503318)
Timeframe: Baseline, end of treatment (up to 108 weeks)

,,
Interventionunits on a scale (Mean)
BaselineChange at the End of Treatment
Placebo1.6-0.4
TV-46000 q1m1.3-0.3
TV-46000 q2m1.5-0.8

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Time to Impending Relapse (Number of Participants With Impending Relapse) in the Adolescent Participants

Relapse was defined as 1 or more of the following items: • CGI-I of ≥5, and - an increase of any of the 4 PANSS items: conceptual disorganization, hallucinatory behavior, suspiciousness, and unusual thought content, to a score of >4 with an absolute increase of ≥2 on specific item since randomization, or - an increase in any of the 4 individual PANSS items to a score of >4 and an absolute increase of ≥4 on combined score of 4 items since randomization; • hospitalization due to worsening of psychotic symptoms; • CGI-SS of 4 (severely suicidal) or 5 (attempted suicide) on Part 1 and/or 6 (much worse) or 7 (very much worse) on Part 2; • violent behavior resulting in clinically significant self-injury, injury to another person, or property damage. Data is presented as distribution of relapsing participants (adolescents) (number of participants with impending relapse). (NCT03503318)
Timeframe: From randomization up to 108 weeks

InterventionParticipants (Count of Participants)
TV-46000 q2m1

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Time to Impending Relapse (Number of Participants With Impending Relapse) for Intent-to-treat [ITT] Analysis Set

Relapse was defined as 1 or more of the following items: • Clinical Global Impression-Improvement (CGI-I) of ≥5, and - an increase of any of the 4 Positive and Negative Syndrome Scale (PANSS) items: conceptual disorganization, hallucinatory behavior, suspiciousness, and unusual thought content, to a score of >4 with an absolute increase of ≥2 on specific item since randomization, or - an increase in any of the 4 individual PANSS items to a score of >4 and an absolute increase of ≥4 on combined score of 4 items since randomization; • hospitalization due to worsening of psychotic symptoms; • Clinical Global Impression-Severity of Suicidality (CGI-SS) of 4 (severely suicidal) or 5 (attempted suicide) on Part 1 and/or 6 (much worse) or 7 (very much worse) on Part 2; • violent behavior resulting in clinically significant self-injury, injury to another person, or property damage. Data is presented as distribution of relapsing participants (number of participants with impending relapse). (NCT03503318)
Timeframe: From randomization up to 108 weeks

InterventionParticipants (Count of Participants)
Placebo53
TV-46000 q1m13
TV-46000 q2m23

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Time to Impending Relapse (Number of Participants With Impending Relapse) for Extended ITT [eITT] Analysis Set

Relapse was defined as 1 or more of the following items: • CGI-I of ≥5, and - an increase of any of the 4 PANSS items: conceptual disorganization, hallucinatory behavior, suspiciousness, and unusual thought content, to a score of >4 with an absolute increase of ≥2 on specific item since randomization, or - an increase in any of the 4 individual PANSS items to a score of >4 and an absolute increase of ≥4 on combined score of 4 items since randomization; • hospitalization due to worsening of psychotic symptoms; • CGI-SS of 4 (severely suicidal) or 5 (attempted suicide) on Part 1 and/or 6 (much worse) or 7 (very much worse) on Part 2; • violent behavior resulting in clinically significant self-injury, injury to another person, or property damage. Data is presented as distribution of relapsing participants (adults and adolescents) (number of participants with impending relapse). (NCT03503318)
Timeframe: From randomization up to 108 weeks

InterventionParticipants (Count of Participants)
Placebo53
TV-46000 q1m13
TV-46000 q2m24

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Proportion of Participants With Impending Relapse

Relapse was defined as 1 or more of the following items: • CGI-I of ≥5, and - an increase of any of the 4 PANSS items: conceptual disorganization, hallucinatory behavior, suspiciousness, and unusual thought content, to a score of >4 with an absolute increase of ≥2 on specific item since randomization, or - an increase in any of the 4 individual PANSS items to a score of >4 and an absolute increase of ≥4 on combined score of 4 items since randomization; • hospitalization due to worsening of psychotic symptoms; • CGI-SS of 4 (severely suicidal) or 5 (attempted suicide) on Part 1 and/or 6 (much worse) or 7 (very much worse) on Part 2; • violent behavior resulting in clinically significant self-injury, injury to another person, or property damage. Impending relapse rate at Week 24 was estimated using the Kaplan-Meier product estimate. (NCT03503318)
Timeframe: Week 24

Interventionproportion of participants (Number)
Placebo0.28
TV-46000 q1m0.07
TV-46000 q2m0.11

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Observed Rate of Impending Relapse (Number of Participants With Impending Relapse) at the Endpoint

Relapse was defined as 1 or more of the following items: • CGI-I of ≥5, and - an increase of any of the 4 PANSS items: conceptual disorganization, hallucinatory behavior, suspiciousness, and unusual thought content, to a score of >4 with an absolute increase of ≥2 on specific item since randomization, or - an increase in any of the 4 individual PANSS items to a score of >4 and an absolute increase of ≥4 on combined score of 4 items since randomization; • hospitalization due to worsening of psychotic symptoms; • CGI-SS of 4 (severely suicidal) or 5 (attempted suicide) on Part 1 and/or 6 (much worse) or 7 (very much worse) on Part 2; • violent behavior resulting in clinically significant self-injury, injury to another person, or property damage. Observed rate of impending relapse was calculated as the number of participants who relapsed by endpoint divided by the number of participants in each treatment group, using the last valid participant assessment as the endpoint. (NCT03503318)
Timeframe: At the Endpoint (up to 108 weeks)

InterventionParticipants (Count of Participants)
Placebo53
TV-46000 q1m13
TV-46000 q2m23

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. TEAEs were defined as AEs occurring after the first dose of the study drug until 120 days after the last dose of study drug. Serious AEs were defined as death, a life-threatening AE, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, or an important medical event that jeopardized participant and required medical intervention to prevent 1 of the outcomes listed in this definition. A summary of other non-serious AEs and all serious AEs, regardless of causality is located in Reported AE section. (NCT03503318)
Timeframe: From randomization up to 120 days after last dose of study drug (up to Week 125)

InterventionParticipants (Count of Participants)
Placebo92
TV-46000 q1m111
TV-46000 q2m121

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Change From Baseline to Week 12/EoT in University of California San Diego Performance-based Skills Assessment-2 Extended Range (UPSA-2-ER) Total Score

The UPSA-2-ER assesses the functional abilities of the participant with schizophrenia in 6 domains: household management, communication, financial skills, transportation, comprehension/planning and medication management. The UPSA-2-ER total score has a range from 0 to 105. A higher score indicates less impairment. (NCT03557931)
Timeframe: Baseline and week 12/EoT

Interventionunits on a scale (Least Squares Mean)
Placebo3.11
ASP4345 50 mg3.86
ASP4345 150 mg2.56

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Number of Participants With Clinically Significant Differences in Simpson Angus Scale (SAS) Values

SAS scale consists of 10 items including 7 items that address bradykinesia-rigidity and additional single items for tremor, glabellar tap, and salivation. Each item represents a specific physical condition and is rated on a 5-point category rating scale ranging from 0 (complete absence of the condition) to 4 (the condition is present to an extreme degree).The total score is obtained by adding the scores for the 10 individual items making the maximum possible score is 40. Higher scores are indicative of more severe Parkinsonian-type symptoms. (NCT03557931)
Timeframe: Baseline, week 6 and week 12

,,
Interventionparticipants (Number)
BaselineWeek 6Week 12
ASP4345 150 mg000
ASP4345 50 mg000
Placebo000

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Number of Participants With Clinically Significant Differences in Barnes Akathisia Rating Scale (BARS) Values

BARS is used to rate observable, restless movements of drug induced akathisia and subjective awareness of restlessness and any distress associated with the akathisia. BARS consists of the following 4 items: objective assessment of akathisia symptoms, subjective assessment of the participants's awareness of inner restlessness, distress restlessness, and global clinical assessment of akathisia. First three items are rated on a 4-point scale ranging from 0 (no abnormal movements or absence of inner restlessness or no distress) to 3 (severe akathisia or awareness of intense compulsion to move most of the time or severe distress). The last item, the global clinical assessment of akathisia, is rated on a 6-point scale, ranging from 0 (no evidence of akathisia) to 5 (severe akathisia). Total BARS score ranges from 0 to 14 with a higher score representing worse results. (NCT03557931)
Timeframe: Baseline, week 6 and week 12

,,
Interventionparticipants (Number)
BaselineWeek 6Week 12
ASP4345 150 mg000
ASP4345 50 mg000
Placebo000

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Number of Participants With Clinically Significant Differences in Abnormal Involuntary Movement Scale (AIMS) Values

AIMS is a 14-item scale. Items 1 to 8 are rated on a 5-point scale ranging from 0 (no dyskinetic movements) to 4 (severe dyskinetic movements). Item 9 assesses the participant's incapacitation due to abnormal movements, and item 10 assesses the participant's awareness of the abnormal movements and associated distress. Items 9 and 10 are rated on 5-point scales ranging from 0 (none or no awareness) to 4 (severe or aware, severe distress). Items 11 to 14 are yes/no questions regarding the global judgement and dental status of the participant. The total score is the sum of the scores for the 14 items and the possible total score ranges from 0 to 44. A higher total score is indicative of more severe dyskinetic movements. (NCT03557931)
Timeframe: Baseline, week 6 and week 12

,,
Interventionparticipants (Number)
BaselineWeek 6Week 12
ASP4345 150 mg000
ASP4345 50 mg000
Placebo000

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Number of Participants With Adverse Event (AE)

Treatment emergent adverse event (TEAE) is defined as an AE observed after starting administration of the study drug and 28 days after the last dose of study drug. A study drug-related TEAE is defined as any TEAE with at least possible relationship to study treatment as assessed by the investigator or with missing assessment of the causal relationship. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. Safety was assessed by AEs, which included abnormalities identified during a medical test (e.g. laboratory tests, vital signs, electrocardiogram, metabolic parameters etc.) if the abnormality induced clinical signs or symptoms, needed active intervention, interruption or discontinuation of study medication or was clinically significant. (NCT03557931)
Timeframe: Baseline up to end of study (EoS) (week 14)

,,
Interventionparticipants (Number)
TEAEDrug-Related TEAEsSerious TEAEsDrug-Related Serious TEAE
ASP4345 150 mg281110
ASP4345 50 mg281330
Placebo451110

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Change From Baseline to Week 12/End of Treatment (EoT) in Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Consensus Cognitive Battery (MCCB) Neurocognitive Composite Score

The MCCB is a cognitive battery to assess 7 domains recommended by the MATRICS initiative (i.e., working memory, verbal learning, speed of processing, attention/vigilance, visual learning, social cognition, reasoning and problem solving). The MCCB neurocognitive composite score is a standardized mean of the six domain scores (excluding social cognition). Raw scores are converted to age and sex adjusted t-scores which are standardized to normative data, and have a mean of 50 and standard deviation of 10 in the general healthy population. A higher score indicates less impairment. (NCT03557931)
Timeframe: Baseline and week 12/end of treatment (EoT)

InterventionT-score (Least Squares Mean)
Placebo1.15
ASP4345 50 mg1.34
ASP4345 150 mg0.87

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Number of Participants With Clinically Significant Differences in Columbia-Suicide Severity Rating Scale (C-SSRS) Values

The C-SSRS is a questionnaire used for suicide risk assessment. Affirmative or negative responses are provided to items 1 to 5 for suicidal ideation (1. Wish to be dead, 2. Non-specific active suicidal thoughts, 3. Active suicidal ideation with any methods [not plan] without intent to act, 4. Active suicidal ideation with some intent to act, without specific plan, 5. Active suicidal ideation with specific plan and intent) and items 6 to 10 for suicide behavior (6. Preparatory acts or behavior, 7. Aborted attempt, 8. Interrupted attempt, 9. Actual attempt, 10. Completed suicide). (NCT03557931)
Timeframe: Baseline up to EoS (week 14)

Interventionparticipants (Number)
Placebo0
ASP4345 50 mg0
ASP4345 150 mg0

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Concentration at Trough Level (Ctrough) for ASP4345

Ctrough concentration for ASP4345 was reported. (NCT03557931)
Timeframe: Predose: day 7, day 14, day 21, day 42 and day 84/EoT

,
Interventionnanogram per milliliter (ng/mL) (Mean)
Day 7 Pre-doseDay 14 Pre-doseDay 21 Pre-doseDay 42 Pre-doseDay 84 Pre-dose
ASP4345 150 mg483.84428.88384.48471.78433.56
ASP4345 50 mg175.041182.903172.040207.145204.914

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Percentage Of Days With Good Patch Coverage

The DMS includes a drug-device combination of a CoE product, a wearable sensor patch, and application software (smartphone) to record activity and rest and mark events through the act of ingestion. The CoE product consists of an approved antipsychotic medication enclosed with an Ingestible Sensor Pill (miniature ingestible event marker in tablet [MIT]). The sensor patch detects and records each MIT ingestion, as well as other physiologic and behavioral data. Good patch coverage for a specific day was defined as having either at least 80% patch data available (80% of the day the patch was worn and data was collected as noted via the accelerometer channel) or the MIT was detected within the 24-hour period, for each day while the participant was in the trial. The percentage of days was calculated as the number of days with good patch coverage divided by the total number of trial days for each participant. Descriptive statistics were performed for this outcome measure. (NCT03568500)
Timeframe: Up to 8 weeks

Interventionpercentage of days (Mean)
Schizophrenia64.34
Schizoaffective Disorder62.99
First Episode Psychosis62.51
Total63.37

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Participant Adherence

The DMS includes a drug-device combination of a CoE product, a wearable sensor patch, and application software (smartphone) to record activity and rest and mark events through the act of ingestion. The CoE product consists of an approved antipsychotic medication enclosed with an Ingestible Sensor Pill (MIT). The sensor patch detects and records each MIT ingestion, as well as other physiologic and behavioral data. Participant adherence was measured as the detected MITs over the expected MITs ingested during the trial days with good patch coverage. The more the participant successfully engaged in a number of processes across the 8-week trial, the greater the measured adherence. Descriptive statistics were performed for this outcome measure. (NCT03568500)
Timeframe: Up to 8 weeks

Interventionpercentage of MITs (Mean)
Schizophrenia88.94
Schizoaffective Disorder72.29
First Episode Psychosis91.04
Total86.57

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PANSS Negative Subscale Mean Change From Baseline to Endpoint

"The PANSS consisted of three subscales: a total of 30 symptom constructs. For each symptom construct, severity was rated on a 7-point scale, with a score of 1 indicated- absence of symptoms and a score of 7 indicated- extremely severe symptoms. The PANSS negative subscale score was the sum of the rating scores for the 7 negative scale items from the PANSS panel. The 7 negative symptom constructs were: blunted affect, emotional withdrawal, poor rapport, passive apathetic withdrawal, difficulty in abstract thinking, lack of spontaneity and flow of conversation and stereotyped thinking. PANSS Negative Subscale Score ranges from 7 (absence of symptoms) to 49 (extremely severe symptoms).~Endpoint is defined as study day 365 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Baseline and Day 365 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Rollover Placebo/Risperidone ISM 75 mg-4.6
Risperidone ISM 75 mg/Risperidone ISM 75 mg-2.2
De Novo/Risperidone ISM 75 mg-0.3
Rollover Placebo/Risperidone ISM 100 mg-2.9
Risperidone ISM 100/Risperidone ISM 100-2.1
De Novo/Risperidone ISM 100 mg-0.7

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PANSS General Psychopathology Subscale Mean Change From Baseline to Endpoint

"The PANSS consisted of three subscales that contained a total of 30 symptom constructs. For each symptom construct, severity is rated on a 7-point scale, with a score of 1 indicated the absence of symptoms and a score of 7 indicated extremely severe symptoms. The general psychopathology scale consists of 16 items which measure somatic concern, anxiety, guilt feelings, tension, mannerisms and posturing, depression, motor retardation, uncooperativeness, unusual thought content, disorientation, poor attention, lack of judgment and insight, disturbance of volition, poor impulse control, preoccupation and active social avoidance. PANSS General Psychopathology Subscale Score ranges from 16 (absence of symptoms) to 112 (extremely severe symptoms).~Endpoint is defined as study day 356 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Baseline and Day 365 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Rollover Placebo/Risperidone ISM 75 mg-12.4
Rollover Risperidone ISM 75mg/Risperidone ISM 75mg-5.4
De Novo/Risperidone ISM 75mg0.2
Rollover Placebo/Risperidone ISM 100 mg-9.4
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg-3.9
De Novo/Risperidone ISM 100 mg-2.5

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Clinician Global Impression - Improvement (CGI-I) Score

"The Clinical Global Impression - Improvement (CGI-I) is a single 7-point rating score total improvement, regardless of whether or not the change it is due entirely to drug treatment. Raters select one response based on the following question, Compared to your patient's condition at the beginning of treatment, how much has your patient changed? Scores are: 1, Very much improved; 2, Much improved; 3, Minimally improved; 4, No change; 5, Minimally worse; 6, Much worse; or 7, Very much worse.~Endpoint is defined as study day 365 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Day 365 (or the last post-baseline assessment)

Interventionscore on a scale (Mean)
Rollover Placebo/Risperidone ISM 75 mg2.3
Rollover Risperidone ISM 75mg/Risperidone ISM 75mg2.9
De Novo/Risperidone ISM 75mg3.7
Rollover Placebo/Risperidone ISM 100 mg2.4
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg2.9
De Novo/Risperidone ISM 100 mg3.1

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TEAEs Leading to Study Drug Discontinuation

TEAEs which resulted in permanent study drug discontinuation (NCT03870880)
Timeframe: Up to Day 365 (or the last post-baseline assessment)

,
InterventionParticipants (Count of Participants)
AkathisiaDiabetes mellitusExtrapyramidal disorderGynaecomastiaHepatic SteatosisHepatocellular injuryLibido decreasedSchizophreniaSuicidal ideationWeight increased
Risperidone ISM 100 mg1001110500
Risperidone ISM 75 mg0110001211

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Overall Response Rate at Endpoint

"Overall response was defined as either PANSS total score ≥ 30% decrease from baseline, or CGI-I score of 2 (much improved) or 1 (very much improved).~Endpoint is defined as study day 365 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Day 365 (or the last post-baseline assessment)

Interventionpercentage of participants (Number)
Rollover Placebo/Risperidone ISM 75 mg74.1
Rollover Risperidone ISM 75mg/Risperidone ISM 75mg44.8
De Novo/Risperidone ISM 75mg9.7
Rollover Placebo/Risperidone ISM 100 mg64.3
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg45.9
De Novo/Risperidone ISM 100 mg20.0

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Clinician Global Impression - Severity (CGI-S) Total Score Mean Change From Baseline to Endpoint

"The Clinician Global Impression - Severity (CGI-S) score is a 7-point clinician-rated scale for assessing the global severity of the illness. A rating of 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Negative change from baseline scores indicate improvement in the severity of illness whereas higher scores mean a worse outcome.~Endpoint is defined as study day 365 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Baseline and Day 365 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Rollover Placebo/Risperidone ISM 75 mg-1.3
Rollover Risperidone ISM 75mg/Risperidone ISM 75mg-0.5
De Novo/Risperidone ISM 75mg0.0
Rollover Placebo/Risperidone ISM 100 mg-1.0
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg-0.3
De Novo/Risperidone ISM 100 mg-0.1

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PANSS Positive Subscale Mean Change From Baseline to Endpoint

"The PANSS consisted of three subscales that contained a total of 30 symptom constructs. For each symptom construct, severity is rated on a 7-point scale, with a score of 1 indicated the absence of symptoms and a score of 7 indicated extremely severe symptoms. In positive subscale, the 7 positive symptom constructs were: delusions, conceptual disorganization, hallucinatory behavior, excitement, grandiosity, suspiciousness/persecution, and hostility.~PANSS Positive Subscale Score ranges from 7 (absence of symptoms) to 49 (extremely severe symptoms).~Endpoint is defined as study day 365 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Baseline and Day 365 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Rollover Placebo/Risperidone ISM 75 mg-6.0
Rollover Risperidone 75 mg/Risperidone 75 mg-3.3
De Novo/Risperidone ISM 75 mg-0.6
Rollover Placebo/Risperidone ISM 100 mg-6.5
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg-2.6
De Novo/Risperidone ISM 100 mg-1.6

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Patients With Treatment Emergent Adverse Events (TEAEs)

"An Adverse event (AE) is any symptom, physical sign, syndrome, or disease that either emerges during the study (from the informed consent form signature) or, if present at screening, worsens during the study, regardless of the suspected cause of the event.~The treatment-emergent AEs (TEAEs) are defined as events that are newly occurring or worsening from the time of the first dose of the intramuscular study drug." (NCT03870880)
Timeframe: Up to Day 365 (or the last post-baseline assessment)

,
InterventionParticipants (Count of Participants)
Patients with at least one TEAEPatients with at least one treatment-related TEAEPatients with at least one serious TEAEPatients with at least one TEAE leading to treatment discontinuationPatients with at least one TEAE leading to death
Risperidone ISM 100 mg5941580
Risperidone ISM 75 mg8143671

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Relapse Rate

Relapse was defined as either increase from baseline in PANSS total score ≥30% or rehospitalization for psychotic symptoms or use of adjunctive antipsychotic medication after stabilization. (NCT03870880)
Timeframe: Day 365 (or the last post-baseline assessment)

Interventionpercentage of participants (Number)
Rollover Placebo/Risperidone ISM 75 mg11.1
Rollover Risperidone ISM 75mg/Risperidone ISM 75mg10.3
De Novo/Risperidone ISM 75mg12.9
Rollover Placebo/Risperidone ISM 100 mg0
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg13.1
De Novo/Risperidone ISM 100 mg20.0

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PANSS Total Score Mean Change From Baseline to Endpoint

"The Positive and Negative Syndrome Scale (PANSS) is a 30-item clinician-rated instrument for assessing the symptoms of schizophrenia.The 30 symptoms are rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme psychopathology). The PANSS total score is the sum of all 30 PANSS items and ranges from 30 to 210, with 30 indicating absence of symptoms of schizophrenia and 210 indicating extreme ratings of all 30 symptoms. Negative change from baseline scores indicates improvements in symptoms whereas higher scores mean a worse outcome.~Endpoint is defined as study day 365 or the last post-baseline assessment if early discontinuation." (NCT03870880)
Timeframe: Baseline and Day 365 (or the last post-baseline assessment)

Interventionunits on a scale (Mean)
Rollover Placebo/Risperidone ISM 75 mg-22.9
Rollover Risperidone ISM 75mg/Risperidone ISM 75mg-11.0
De Novo/Risperidone ISM 75mg-0.8
Rollover Placebo/Risperidone ISM 100 mg-18.9
Rollover Risperidone ISM 100 mg/Risperidone ISM 100 mg-8.7
De Novo/Risperidone ISM 100 mg-4.8

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Number of Participants With SAEs

An AE was defined as any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. SAEs were defined as death, a life-threatening AE, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, or an important medical event that jeopardized participant and required medical intervention to prevent 1 of the outcomes listed in this definition. A summary of other non-serious AEs and all serious AEs, regardless of causality is located in Reported AE section. The safety analysis set included all participants who received at least 1 dose of TV46000 in TV-46000-CNS-30072 study or in TV46000-CNS-30078 study. (NCT03893825)
Timeframe: Baseline up to Week 64

InterventionParticipants (Count of Participants)
TV-46000 q1m8
TV-46000 q2m11

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Number of Participants With Adverse Events (AEs)

An AE was defined as any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. Serious adverse events (SAEs) were defined as death, a life-threatening AE, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, or an important medical event that jeopardized participant and required medical intervention to prevent 1 of the outcomes listed in this definition. A summary of other non-serious AEs and all serious AEs, regardless of causality is located in Reported AE section. (NCT03893825)
Timeframe: Baseline up to Week 64

InterventionParticipants (Count of Participants)
TV-46000 q1m64
TV-46000 q2m74

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Number of Participants Who Were Withdrawn From the Treatment

The number of participants who were withdrawn from the treatment due to any reason has been reported. The safety analysis set included all participants who received at least 1 dose of TV46000 in TV-46000-CNS-30072 study or in TV46000-CNS-30078 study. (NCT03893825)
Timeframe: Baseline up to Week 64

,
InterventionParticipants (Count of Participants)
DeathAdverse eventWithdrawal by participantNon-compliance with study drugProtocol deviationLost-to-follow upLack of efficacyRelapseOther
TV-46000 q1m22211251311
TV-46000 q2m15250170311

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Percent Fluctuation in Concentration Over the Dosing Interval

Plasma concentration variation of risperidone, 9-OH and total active moiety over the dosing interval was measured by percent fluctuation after oral dosing and SC doses 1, 3 and 4 at steady state. (NCT03978832)
Timeframe: Calculated over the dosing interval (0-12 hours on Day -1, or 0-672 hours after Dose 1, 3 or 4)

Interventionpercentage of fluctuation (Geometric Mean)
Risperidone after oral dosingRisperidone after Dose 1Risperidone after Dose 3Risperidone after Dose 49-OH after oral dosing9-OH after Dose 19-OH after Dose 39-OH after Dose 4Total active moiety after oral dosingTotal active moiety after Dose 1Total active moiety after Dose 3Total active moiety after Dose 4
Oral Risperidone Followed by PERSERIS253.335174.653135.267190.11746.787115.645115.286116.85271.468115.113106.210118.435

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Maximum Plasma Concentration Over the Dosing Interval

Maximum observed plasma concentration of risperidone, 9-hydroxyrisperidone (9-OH) and total active moiety over the dosing interval after oral dosing and SC doses 1, 3 and 4 (NCT03978832)
Timeframe: Calculated over the dosing interval (0-12 hours on Day -1, or 0-672 hours after Dose 1, 3 or 4)

Interventionng/mL (Geometric Mean)
Risperidone after oral dosingRisperidone after Dose 1Risperidone after Dose 3Risperidone after Dose 49-OH after oral dosing9-OH after Dose 19-OH after Dose 39-OH after Dose 4Total active moiety after oral dosingTotal active moiety after Dose 1Total active moiety after Dose 3Total active moiety after Dose 4
Oral Risperidone Followed by PERSERIS14.05216.74318.63529.82145.46445.28556.47652.24058.45358.31770.59777.219

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Columbia-Suicide Severity Rating Scale (C-SSRS)-Change

Significant changes from baseline in C-SSRS scores were reported as adverse events. The C-SSRS is based on a categorization of thoughts and behavior that are identified as related to suicidal behavior. The scale captures the occurrence, severity and frequency of suicide related thoughts and behaviors throughout lifetime at screening and for the time interval since last administration during a study. Responses are indicated as yes (thought or behavior did occur) or no (thought or behavior did not occur). If a yes response is received, then follow up questions are asked. The outcome of the C-SSRS is a numerical score obtained from each of the categories. Scores can range from 0-25, indicating the intensity rating, and any score greater than 0 may indicate the need for mental health intervention. Higher scores indicate greater intensity (i.e. worse outcome). (NCT03978832)
Timeframe: Screening through EOS (Day 113)

Interventionscore on a scale (Mean)
Change in Maximum Suicidal Ideation at Dose 1/Day 8Change in Maximum Suicidal Ideation at EOSChange in Suicidal Ideation Intensity Score at Dose 1/Day 8Change in Suicidal Ideation Intensity Score at EOSChange in Maximum Suicidal Behavior at Dose 1/Day 8Change in Maximum Suicidal Behavior at EOS
Oral Risperidone Followed by PERSERIS0.00.00.00.00.00.0

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Clinical Global Impression-Severity of Illness Scale (CGI-S)

Clinical outcome (efficacy endpoint) as measured by change from baseline in CGI-S scores was measured. The CGI-S is a measurement of the total severity of illness where one question is assessed. Responses range from 0 (not assessed) to 7 (most extremely ill). (NCT03978832)
Timeframe: Baseline through EOS (Day 113)

Interventionscore on a scale (Mean)
Change from baseline: Dose 1/Day 2Change from baseline: Dose 1/Day 8Change from baseline: Dose 1/Day 15Change from baseline: Dose 1/Day 22Change from baseline: Dose 2/Day 29Change from baseline: Dose 2/Day 50Change from baseline: Dose 3/Day 57Change from baseline: Dose 4/Day 85Change from baseline: EOS/Day 113
Oral Risperidone Followed by PERSERIS-0.10.00.00.00.00.00.10.10.0

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Average Plasma Concentration (Cavg) Over the Dosing Interval of Risperidone, 9-OH and Total Active Moiety

Average plasma concentration of risperidone, 9-hydroxyrisperidone (9-OH) and total active moiety over the dosing interval after oral dosing and SC doses 1, 3 and 4. (NCT03978832)
Timeframe: Calculated over the dosing interval (0-12 hours on Day -1, or 0-672 hours after Dose 1, 3 or 4).

Interventionng/mL (Geometric Mean)
Risperidone after oral dosingRisperidone after Dose 1Risperidone after Dose 3Risperidone after Dose 49-OH after oral dosing9-OH after Dose 19-OH after Dose 39-OH after Dose 4Total active moiety after oral dosingTotal active moiety after Dose 1Total active moiety after Dose 3Total active moiety after Dose 4
Oral Risperidone Followed by PERSERIS5.0307.45410.20011.61836.06626.14833.03930.72340.82334.07744.04943.729

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Area Under the Plasma Concentration-time Curve Over the Dosing Interval

Area under the plasma concentration-time curve (AUC) was measured for risperidone, 9-OH and total active moiety. (NCT03978832)
Timeframe: Calculated over the dosing interval (0-12 hours on Day -1, or 0-672 hours after Dose 1, 3 or 4).

Interventionhr*ng/mL (Geometric Mean)
Risperidone after oral dosingRisperidone after Dose 1Risperidone after Dose 3Risperidone after Dose 49-OH after oral dosing9-OH after Dose 19-OH after Dose 39-OH after Dose 4Total active moiety after oral dosingTotal active moiety after Dose 1Total active moiety after Dose 3Total active moiety after Dose 4
Oral Risperidone Followed by PERSERIS60.3545021.1916854.8557762.268432.80117615.9722203.3120527.19489.88822955.7429602.7229217.83

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The Number of Participants With TEAEs as Assessed by Local Injection Site*

The injection site was evaluated for adverse events by observation and examination by appropriately trained personnel. (NCT03978832)
Timeframe: First injection at Day 1 until Day 120

InterventionParticipants (Count of Participants)
Oral Risperidone Followed by PERSERIS1

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The Number of Participants With TEAEs as Assessed by Changes in ECG

ECGs were performed, and clinically significant changes in parameters were reported as adverse events (AE). ECGs were performed after 5 minutes of rest, and ECG parameters including QT interval, PR interval, QRS interval and heart rate was recorded. The ECG measurements were evaluated during the visit and determination of whether any abnormalities were AEs was made by the investigator or a medically qualified designee. If determined to be an AE, the measurement was repeated at appropriate intervals until the value returned to an acceptable range and the subject was clinically stable, a specific diagnosis was established, or the condition otherwise explained. (NCT03978832)
Timeframe: Time participants sign the informed consent form throughout the study until EOS (Day 113)

InterventionParticipants (Count of Participants)
Oral Risperidone Followed by PERSERIS0

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The Number of Participants With TEAEs as Assessed by Changes in Body Weight

Body weight, with shoes off, was measured and clinically significant changes in weight was reported as adverse events (AE). Determination of whether the changes were AEs was made by the investigator or a medically qualified designee. If determined to be an AE, the measurement was repeated at appropriate intervals until the value returned to an acceptable range and the subject was clinically stable, a specific diagnosis was established, or the condition otherwise explained. (NCT03978832)
Timeframe: Time subjects sign the informed consent form throughout the study until EOS (Day 113)

InterventionParticipants (Count of Participants)
Oral Risperidone Followed by PERSERIS1

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Positive and Negative Syndrome Scale (PANSS)

"Clinical outcome (efficacy endpoint) as measured by change from baseline in PANSS scores was measured. PANSS is a medical scale designed to measure schizophrenia symptom severity utilizing a 30 item, 7-point rating scheme. The PANSS Is scored by a summation of ratings across items, with a total potential range of 7-210; higher results indicate greater severity of illness.~Only total score changes from baseline are reported here." (NCT03978832)
Timeframe: Baseline, defined as last assessment prior to first injection, through Day 113 (EOS)

Interventionscore on a scale (Mean)
Total score change from baseline: Dose 1 Day 2Total score change from baseline: Dose 1 Day 8Total score change from baseline: Dose 1 Day 15Total score change from baseline: Dose 1 Day 22Total score change from baseline: Dose 2 Day 29Total score change from baseline: Dose 2 Day 50Total score change from baseline: Dose 3 Day 57Total score change from baseline: Dose 4 Day 85Total score change from baseline: Day 113-EOS
Oral Risperidone Followed by PERSERIS-0.20.90.7-0.4-0.9-0.5-2.9-0.91.6

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The Number of Participants With TEAEs as Assessed by Changes in Laboratory Testing

Laboratory testing was performed by the local clinical laboratory accredited by the College of American Pathologists, and clinically significant changes from baseline were reported as AEs. Subjects were expected to fast for a minimum of 8 hours prior to blood draws for all laboratory assessments except at the screening visit. Prior to entering the study, any abnormal laboratory test results were to be considered not clinically significant. Any abnormal hematology, serum chemistry or urinalysis test result after study drug intake that was determined by the investigator or a medically qualified designee to be clinically significant was reported as an AE. If determined to be an AE, the measurement was repeated at appropriate intervals until the value returned to an acceptable range or it was determined that resolution was not expected. (NCT03978832)
Timeframe: Time subjects sign the informed consent form throughout the study until end of study (EOS) visit (Day 113)

InterventionParticipants (Count of Participants)
Oral Risperidone Followed by PERSERIS3

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Trough Plasma Concentration

Trough (pre-dose) plasma concentrations were measured for risperidone, 9-OH and total active moiety for SC doses 1, 3 and 4 (NCT03978832)
Timeframe: Calculated over the dosing interval (0-672 hours) after Dose 1, 3 or 4.

Interventionng/mL (Geometric Mean)
Risperidone after Dose 1Risperidone after dose 3Risperidone after Dose 49-OH after dose 19-OH after dose 39-OH after dose 4Total active moiety after dose 1Total active moiety after dose 3Total active moiety after dose 4
Oral Risperidone Followed by PERSERIS1.7665.0664.96633.69620.32617.98335.55325.46823.125

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Minimum Plasma Concentration Over the Dosing Interval

Minimum observed plasma concentration of risperidone, 9-hydroxyrisperidone (9-OH) and total active moiety over the dosing interval after oral dosing and SC doses 1, 3 and 4 (NCT03978832)
Timeframe: Calculated over the dosing interval (0-12 hours on Day -1, or 0-672 hours after Dose 1, 3 or 4).

Interventionng/mL (Geometric Mean)
Risperidone after oral dosingRisperidone after Dose 1Risperidone after Dose 3Risperidone after Dose 49-OH after oral dosing9-OH after Dose 19-OH after Dose 39-OH after Dose 4Total active moiety after oral dosingTotal active moiety after Dose 1Total active moiety after Dose 3Total active moiety after Dose 4
Oral Risperidone Followed by PERSERIS1.0663.0174.5195.02027.70513.92216.95114.82028.32917.85222.25022.063

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Assessment of Local Injection Site Tolerability*

Injection site tolerability was measured by injection site grading for redness, induration, swelling and tenderness/pain. These were graded on a scale from 0 to 4 for severity (none, mild, moderate, severe and potentially life-threatening) (NCT03978832)
Timeframe: First injection at Day 1 until last injection administered at Day 85

InterventionParticipants (Count of Participants)
Dose 1 injection site pain grade72408348Dose 2 injection site pain grade72408348Dose 3 injection site pain grade72408348Dose 4 injection site pain grade72408348Dose 1 injection site tenderness grade72408348Dose 2 injection site tenderness grade72408348Dose 3 injection site tenderness grade72408348Dose 4 injection site tenderness grade72408348Dose 1 injection site erythema/redness grade72408348Dose 2 injection site erythema/redness grade72408348Dose 3 injection site erythema/redness grade72408348Dose 4 injection site erythema/redness grade72408348Dose 1 injection site induration/swelling grade72408348Dose 2 injection site induration/swelling grade72408348Dose 3 injection site induration/swelling grade72408348Dose 4 injection site induration/swelling grade72408348
NoneMild
Oral Risperidone Followed by PERSERIS22
Oral Risperidone Followed by PERSERIS19
Oral Risperidone Followed by PERSERIS21
Oral Risperidone Followed by PERSERIS18
Oral Risperidone Followed by PERSERIS2
Oral Risperidone Followed by PERSERIS13
Oral Risperidone Followed by PERSERIS3
Oral Risperidone Followed by PERSERIS20
Oral Risperidone Followed by PERSERIS16
Oral Risperidone Followed by PERSERIS0
Oral Risperidone Followed by PERSERIS23
Oral Risperidone Followed by PERSERIS15
Oral Risperidone Followed by PERSERIS1
Oral Risperidone Followed by PERSERIS14

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Safety as Measured by Columbia-Suicide Severity Rating Scale (C-SSRS) Scores

Safety of treatment was measured by characterization of thoughts and behavior related to suicidal behavior. This was assessed by administration of the C-SSRS at designated visits. The scale captures the occurrence, severity and frequency of suicide related thoughts and behaviours throughout lifetime at screening and for the time interval since last administration during a study. Questions solicit the type of information needed to determine if a suicide-related thought or behavior occurred. (NCT03978832)
Timeframe: Screening through EOS (Day 113)

InterventionParticipants (Count of Participants)
Any Suicidal Ideation - Lifetime72408348Any Suicidal Ideation - Past 6 months72408348Any Suicidal Ideation - EOS72408348Any Suicidal Behavior - Lifetime72408348Any Suicidal Behavior - Past 6 months72408348Any Suicidal Behavior - EOS72408348Any Suicidal Ideation or Behavior - Lifetime72408348Any Suicidal Ideation or Behavior - Past 6 months72408348Any Suicidal Ideation or Behavior - EOS72408348
YesNo
Oral Risperidone Followed by PERSERIS15
Oral Risperidone Followed by PERSERIS23
Oral Risperidone Followed by PERSERIS17
Oral Risperidone Followed by PERSERIS6
Oral Risperidone Followed by PERSERIS8
Oral Risperidone Followed by PERSERIS20
Oral Risperidone Followed by PERSERIS14
Oral Risperidone Followed by PERSERIS0

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The Number of Participants With TEAEs as Assessed by Changes in Vital Signs

Vital sign measurement was performed, including orthostatic blood pressure, and clinically significant changes were reported as adverse events (AE). Vital sign measurement also included measurement of pulse rate, oral temperature and respiratory rate. Determination of whether the changes were AEs was made by the investigator or a medically qualified designee. If determined to be an AE, the measurement was repeated at appropriate intervals until the value returned to an acceptable range and the subject was clinically stable, a specific diagnosis was established, or the condition otherwise explained. (NCT03978832)
Timeframe: Time subjects sign the informed consent form throughout the study until EOS (Day 113)

InterventionParticipants (Count of Participants)
Oral Risperidone Followed by PERSERIS1

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Time to Occurrence of Maximum Concentration

Time to maximal observed plasma concentration (Tmax) for risperidone, 9-OH, and total active moiety after oral dosing and SC doses 1, 3 and 4. (NCT03978832)
Timeframe: Calculated over the overall dosing interval (0-12 hours on Day -1, or 0-672 hours after Dose 1, 3 or 4).

Interventionhr (Median)
Risperidone after oral dosingRisperidone after Dose 1Risperidone after Dose 3Risperidone after Dose 49-OH after oral dosing9-OH after Dose 19-OH after Dose 39-OH after Dose 4Total active moiety after oral dosingTotal active moiety after Dose 1Total active moiety after Dose 3Total active moiety after Dose 4
Oral Risperidone Followed by PERSERIS1.0240.175143.86512.0501.990204.515182.535118.1201.010239.665182.535192.100

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The Number of Participants With TEAEs as Assessed by Extrapyramidal Symptoms (EPS) of Anti-psychotic Drug Treatment

Safety of treatment was measured by administration of symptom questionnaires including AIMS, Barnes Akathisia Rating Scale (BARS) and Simpson-Angus Scale (SAS), as well as by assessment by the investigator or suitably qualified medical designee. The AIMS is a tool that aids in early detection and ongoing monitoring of tardive dyskinesia, a movement disorder. The BARS is a 4-item scale that detects the presence and severity of any drug-induced restlessness. The SAS is a 10-item scale used to detect the presence of drug-induced Parkinsonism (movement disorder seen in Parkinson's disease) and extrapyramidal side effects and evaluates symptom severity. Extrapyramidal symptoms include involuntary or uncontrollable movements, tremors, and muscle contractions. (NCT03978832)
Timeframe: Time subjects sign the informed consent form throughout the study until EOS (Day 113)

InterventionParticipants (Count of Participants)
AkathisiaDyskinesiaParkinsonian gaitTremor
Oral Risperidone Followed by PERSERIS1211

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Steady-state Average Plasma Concentration (Cavg,ss) of Risperidone and Total Active Moiety

Cavg,ss for risperidone and total active moiety after oral and SC administration (NCT03978832)
Timeframe: 0-12 hours post-dose on Day -1, and 0-672 hours after Dose 3

Interventionng/mL (Geometric Mean)
Risperidone after oral dosingRisperidone after Dose 3Total active moiety after oral dosingTotal active moiety after Dose 3
Oral Risperidone Followed by PERSERIS5.15010.20043.73044.049

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Mean Change From Baseline in the Positive and Negative Syndrome Scale (PANSS) Total Score at Week 4

The PANSS is a 30-item rating scale that evaluates positive, negative, and other symptoms in patients with schizophrenia. The Positive subscale is a 7-item scale that assesses features in schizophrenia that are not present in a normal mental state. The Negative subscale is a 7-item scale that assesses features absent in schizophrenia but present in those with a normal mental state. Items are rated on a 7-point scale, where 1 = absent and 7 = extreme, for a maximum score of 49 for each scale. The General subscale is a 16-item scale that assesses the overall severity of schizophrenia and the risk of aggression. Items are rated on the same scale, with a minimum score of 16 and a maximum score of 112. Total scores are calculated by adding subscale scores together, for a minimum score of 30 and a maximum score of 210. Higher scores indicate higher severity. (NCT04512066)
Timeframe: Week 4 (Day 28)

,,,
InterventionUnits on a scale (Mean)
BaselineDay 28
Placebo99.3888.69
Risperidone 4 mg100.0378.04
RO6889450 150 mg100.5385.18
RO6889450 45 mg98.5488.94

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PANSS Total Score at Week 12

The PANSS is a 30-item rating scale that evaluates positive, negative, and other symptoms in patients with schizophrenia. The Positive subscale is a 7-item scale that assesses features in schizophrenia that are not present in a normal mental state. The Negative subscale is a 7-item scale that assesses features absent in schizophrenia but present in those with a normal mental state. Items are rated on a 7-point scale, where 1 = absent and 7 = extreme, for a maximum score of 49 for each scale. The General subscale is a 16-item scale that assesses the overall severity of schizophrenia and the risk of aggression. Items are rated on the same scale, with a minimum score of 16 and a maximum score of 112. Total scores are calculated by adding subscale scores together, for a minimum score of 30 and a maximum score of 210. Higher scores indicate higher severity. (NCT04512066)
Timeframe: Week 12

,,,,
InterventionUnits on a scale (Mean)
BaselineWeek 12
Placebo - RO6889450 150 mg99.1276.73
Placebo - RO6889450 45 mg103.4475.10
Risperidone 4 mg100.3067.74
RO6889450 150 mg99.0079.30
RO6889450 45 mg98.6676.25

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Plasma Concentration of RO6889450

(NCT04512066)
Timeframe: Day 7 - Day 336

,
Interventionng/mL (Geometric Mean)
Day 28Day 42Day 56Day 84
Placebo - RO6889450 150 mg212.27274.58217.65165.99
Placebo - RO6889450 45 mg49.6759.9970.9977.11

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Plasma Concentration of RO6889450

(NCT04512066)
Timeframe: Day 7 - Day 336

,
Interventionng/mL (Geometric Mean)
Day 7Day 14Day 28Day 42Day 56Day 84Day 168Day 336
RO6889450 150 mg423.83463.21419.41390.65237.42265.09733.98139.71
RO6889450 45 mg99.5091.5394.57108.57108.5992.2495.394.13

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Proportion of Participants With at Least 20% or 50% Improvement From Baseline in the PANSS Total Score

The PANSS is a 30-item rating scale that evaluates positive, negative, and other symptoms in patients with schizophrenia. The Positive subscale is a 7-item scale that assesses features in schizophrenia that are not present in a normal mental state. The Negative subscale is a 7-item scale that assesses features absent in schizophrenia but present in those with a normal mental state. Items are rated on a 7-point scale, where 1 = absent and 7 = extreme, for a maximum score of 49 for each scale. The General subscale is a 16-item scale that assesses the overall severity of schizophrenia and the risk of aggression. Items are rated on the same scale, with a minimum score of 16 and a maximum score of 112. Total scores are calculated by adding subscale scores together, for a minimum score of 30 and a maximum score of 210. Higher scores indicate higher severity. (NCT04512066)
Timeframe: Baseline to Week 12

,,,
InterventionProportion expressed as percentage (Number)
20% improvement - Week 120% improvement - Week 220% improvement - Week 320% improvement - Week 450% improvement - Week 150% improvement - Week 250% improvement - Week 350% improvement - Week 4
Placebo18.126.431.930.602.82.88.3
Risperidone 4 mg25.443.759.259.22.84.214.114.1
RO6889450 150 mg27.936.838.236.81.54.42.98.8
RO6889450 45 mg26.224.632.332.31.53.17.77.7

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Proportion of Participants With at Least 20% or 50% Improvement in the PANSS Total Score up to Week 12

The PANSS is a 30-item rating scale that evaluates positive, negative, and other symptoms in patients with schizophrenia. The Positive subscale is a 7-item scale that assesses features in schizophrenia that are not present in a normal mental state. The Negative subscale is a 7-item scale that assesses features absent in schizophrenia but present in those with a normal mental state. Items are rated on a 7-point scale, where 1 = absent and 7 = extreme, for a maximum score of 49 for each scale. The General subscale is a 16-item scale that assesses the overall severity of schizophrenia and the risk of aggression. Items are rated on the same scale, with a minimum score of 16 and a maximum score of 112. Total scores are calculated by adding subscale scores together, for a minimum score of 30 and a maximum score of 210. Higher scores indicate higher severity. (NCT04512066)
Timeframe: Weeks 4, 8, and 12

,,,,
InterventionProportion expressed as a percentage (Number)
Week 4Week 8Week 12
Placebo - RO6889450 150 mg36.028.028.0
Placebo - RO6889450 45 mg40.036.028.0
Risperidone 4 mg75.569.850.9
RO6889450 150 mg53.337.828.9
RO6889450 45 mg46.343.948.8

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Participants Ready for Discharge From First Randomized Treatment Intake to Readiness for Discharge as Assessed by the Readiness for Discharge Questionnaire (RDQ) at 4-Week Treatment

The RDQ is a tool used to assess inpatients with schizophrenia on their readiness for discharge from inpatient treatment. It consists of five items that assess suicidality/homicidality, control of aggression/impulsivity, activities of daily living, medication-taking, and delusions/hallucinations interfering with functioning and global status. An additional item examines the overall clinical state of the patient and the final question assesses readiness for discharge. The values reported are the proportion (expressed as a percentage) of participants in each analysis group considered ready for discharge according to the RDQ. (NCT04512066)
Timeframe: after 4-week treatment

InterventionPercentage of participants (Number)
Placebo88.9
RO6889450 45 mg83.1
RO6889450 150 mg89.7
Risperidone 4 mg97.2

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CGI-I up to Week 12

The CGI-I measures change from the baseline state at subsequent visits using a 7-point scale, where 1 = very much improved and 7 = very much worse. (NCT04512066)
Timeframe: Up to Week 12

,,,,
InterventionUnits on a scale (Mean)
Day 7Week 12
Placebo - RO6889450 150 mg3.762.73
Placebo - RO6889450 45 mg3.542.33
Risperidone 4 mg3.382.00
RO6889450 150 mg3.562.65
RO6889450 45 mg3.542.30

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Change From Baseline in PANSS Factor Scores at Week 4

PANSS factors are modified groupings of the 30 PANSS items from the original three subscales (positive, negative, and general psychopathology). Each item is rated on a scale of 1 (absent) to 7 (most extreme). The positive symptom factor contains 8 items (score range 8-56); the negative symptom and disorganized thought/cognition factors contain 7 items (score range 7-49); the uncontrolled hostility/excitement, expressive deficit, and anxiety/depression factors contain 4 items (score range 4-28); and the avolition domain contains 3 items (score range 3-21). The negative and positive totals each have a range of 7-49 and the general total has a range of 16-112. Higher scores indicate higher symptom severity. (NCT04512066)
Timeframe: Week 4 (Day 28)

,,,
InterventionUnits on a scale (Mean)
Anxiety/Depression - BaselineAnxiety/Depression - Day 28Avolition - BaselineAvolition - Day 28Disorganized thought/Cognition - BaselineDisorganized thought/Cognition - Day 28Expressive deficit - BaselineExpressive deficit - Day 28Totals general - BaselineTotals general - Day 28Negative symptom factor score - BaselineNegative symptom factor score - Day 28Totals negative - BaselineTotals negative - Day 28Positive symptom factor score - BaselinePositive symptom factor score - Day 28Totals positive - BaselineTotals positive - Day 28Uncontrolled hostility/excitement - BaselineUncontrolled hostility/excitement - Day 28
Placebo11.589.5615.9914.0421.8619.6910.8910.8148.4242.4323.5821.6324.1022.6531.4027.7226.8623.6110.9410.09
Risperidone 4 mg12.588.5016.2012.9321.4517.0710.2310.7148.8937.0723.3420.3923.6521.4531.1524.2127.4919.5211.517.86
RO6889450 150 mg11.549.0616.3813.7322.5019.4110.9010.1648.6840.4323.8120.8024.5922.5332.0326.6327.2622.2210.659.27
RO6889450 45 mg12.919.8815.8613.6721.4320.6310.3110.6948.6943.7123.0221.2723.6521.8230.6628.0626.2023.4110.529.10

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CGI-S up to Week 12

The CGI-S measures global severity of illness at a given point in time using a 7-point scale, where 1 = no symptoms and 7 = very severe symptoms. (NCT04512066)
Timeframe: Up to Week 12

,,,,
InterventionUnits on a scale (Mean)
BaselineWeek 12
Placebo - RO6889450 150 mg5.163.73
Placebo - RO6889450 45 mg5.283.33
Risperidone 4 mg5.263.06
RO6889450 150 mg5.163.90
RO6889450 45 mg5.053.56

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Change From Baseline in Clinical Global Impression Severity (CGI-S) Scores

The CGI-S measures global severity of illness at a given point in time using a 7-point scale, where 1 = no symptoms and 7 = very severe symptoms. (NCT04512066)
Timeframe: Week 4 (Day 28)

,,,
InterventionUnits on a scale (Mean)
BaselineDay 28
Placebo5.134.42
Risperidone 4 mg5.273.88
RO6889450 150 mg5.254.29
RO6889450 45 mg5.094.35

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Clinical Global Impression - Improvement (CGI-I) Scores

The CGI-I measures change from the baseline state at subsequent visits using a 7-point scale, where 1 = very much improved and 7 = very much worse. (NCT04512066)
Timeframe: Week 4 (Day 28)

,,,
InterventionUnits on a scale (Mean)
Day 7Day 14Day 21Day 28
Placebo3.873.633.473.27
Risperidone 4 mg3.402.992.792.43
RO6889450 150 mg3.563.333.132.96
RO6889450 45 mg3.603.393.283.27

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PK of 9-Hydroxyrisperidone (Cmax).

To characterize exposure (Cmax) of 9-Hydroxyrisperidone during the switch to LYN-005. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

Interventionng/mL (Geometric Mean)
LYN-005 14 mg (A)20.8
LYN-005 14 mg (B)16.1
LYN-005 14 mg (C)15.6
Risperidone 2 mg (A)15.5
Risperidone 2 mg (B)17.5
Risperidone 2 mg (C)16.9
LYN-005 28 mg (A)16.0
LYN-005 28 mg (B)24.7
LYN-005 28 mg (C)22.5
Risperidone 4 mg (A)39.6
Risperidone 4 mg (B)35.7
Risperidone 4 mg (C)36.2

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PK of Risperidone (Cmax).

To characterize exposure (Cmax) of risperidone during the switch to LYN-005. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

Interventionng/mL (Geometric Mean)
LYN-005 14 mg (A)11.7
LYN-005 14 mg (B)4.44
LYN-005 14 mg (C)4.07
Risperidone 2 mg (A)9.97
Risperidone 2 mg (B)12.3
Risperidone 2 mg (C)15.6
LYN-005 28 mg (A)21.2
LYN-005 28 mg (B)6.87
LYN-005 28 mg (C)7.39
Risperidone 4 mg (A)17.0
Risperidone 4 mg (B)13.5
Risperidone 4 mg (C)14.0

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Active Moiety PK (AUC0-24, AUC0-168)

Active moiety AUC (risperidone and 9-hydroxyrisperidone combined) after repeat weekly doses of LYN-005 ER capsules relative to IR risperidone tablets at 2 dose levels. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

,,,,,,,
Interventionh*ng/mL (Geometric Mean)
AUC0-24
LYN-005 14 mg (A)377
Risperidone 4 mg (B)753
Risperidone 4 mg (C)687
LYN-005 28 mg (A)472
Risperidone 2 mg (A)301
Risperidone 2 mg (B)326
Risperidone 2 mg (C)359
Risperidone 4 mg (A)732

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Active Moiety PK (AUC0-24, AUC0-168)

Active moiety AUC (risperidone and 9-hydroxyrisperidone combined) after repeat weekly doses of LYN-005 ER capsules relative to IR risperidone tablets at 2 dose levels. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

,,,
Interventionh*ng/mL (Geometric Mean)
AUC0-24AUC0-168
LYN-005 14 mg (B)3611820
LYN-005 28 mg (C)5682950
LYN-005 28 mg (B)5753350
LYN-005 14 mg (C)3712120

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PK of 9-Hydroxyrisperidone (AUC0-24h, AUC0-168h).

To characterize exposure (AUC0-24h, AUC0-168h) of 9-Hydroxyrisperidone during the switch to LYN-005. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

,,,,,,,
Interventionh*ng/mL (Geometric Mean)
AUC0-24h
LYN-005 14 mg (A)315
LYN-005 28 mg (A)268
Risperidone 2 mg (A)243
Risperidone 2 mg (B)262
Risperidone 2 mg (C)265
Risperidone 4 mg (A)641
Risperidone 4 mg (B)665
Risperidone 4 mg (C)645

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Participants With at Least One Treatment Emergent Adverse Event (TEAE).

Incidence of treatment emergent adverse events (TEAEs) reported as participants with at least one treatment emergent adverse event (TEAE). (NCT04567524)
Timeframe: 35 days

InterventionNumber of Participants with TEAEs (Number)
LYN-005 14mg10
LYN-005 28mg8
Overall LYN-00518
Risperidone 2 mg1
Risperidone 4 mg1
Overall Risperidone2

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Active Moiety Tmax

Active Moiety Tmax (h) (risperidone and 9-hydroxyrisperidone combined) after repeat weekly doses of LYN-005 ER capsules relative to IR risperidone tablets at 2 dose levels. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

Interventionhours (Geometric Mean)
LYN-005 14 mg (A)1.9
LYN-005 14 mg (B)23.7
LYN-005 14 mg (C)23.8
Risperidone 2 mg (A)3.0
Risperidone 2 mg (B)1.5
Risperidone 2 mg (C)3.0
LYN-005 28 mg (A)1.0
LYN-005 28 mg (B)24.1
LYN-005 28 mg (C)23.8
Risperidone 4 mg (A)2.1
Risperidone 4 mg (B)4.0
Risperidone 4 mg (C)2.0

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PK of 9-Hydroxyrisperidone (AUC0-24h, AUC0-168h).

To characterize exposure (AUC0-24h, AUC0-168h) of 9-Hydroxyrisperidone during the switch to LYN-005. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

,,,
Interventionh*ng/mL (Geometric Mean)
AUC0-24hAUC0-168h
LYN-005 14 mg (B)2681530
LYN-005 14 mg (C)3021770
LYN-005 28 mg (B)4412720
LYN-005 28 mg (C)5232090

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PK of Risperidone (AUC0-24h, AUC0-168).

To characterize exposure (AUC0-24h, AUC0-168) of risperidone during the switch to LYN-005. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

,,,,,,,
Interventionh*ng/mL (Geometric Mean)
AUC0-24h
LYN-005 14 mg (A)54.9
LYN-005 28 mg (A)113
Risperidone 2 mg (A)43.4
Risperidone 2 mg (B)47.7
Risperidone 2 mg (C)86.2
Risperidone 4 mg (A)87.1
Risperidone 4 mg (B)82.4
Risperidone 4 mg (C)84.4

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PK of Risperidone (AUC0-24h, AUC0-168).

To characterize exposure (AUC0-24h, AUC0-168) of risperidone during the switch to LYN-005. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

,,,
Interventionh*ng/mL (Geometric Mean)
AUC0-24hAUC0-168
LYN-005 14 mg (B)65.8227
LYN-005 14 mg (C)65.2306
LYN-005 28 mg (B)111806
LYN-005 28 mg (C)119453

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Total Number of Treatment Emergent Adverse Events (TEAEs).

Incidence of treatment emergent adverse events (TEAEs) reported as total number of TEAEs. (NCT04567524)
Timeframe: 35 days

InterventionNumber of Experienced TEAEs (Number)
LYN-005 14mg15
LYN-005 28mg21
Overall LYN-00536
Risperidone 2 mg2
Risperidone 4 mg2
Overall Risperidone4

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Active Moiety PK (Cmax)

Active moiety Cmax (risperidone and 9-hydroxyrisperidone combined) after repeat weekly doses of LYN-005 Extended Release (ER) capsules relative to Immediate Release (IR) risperidone tablets at 2 dose levels. (NCT04567524)
Timeframe: Reported data was obtained following multiple dose administration of 3 weekly doses [(IR, Day-1), (ER, Week 1), ER Week 3)] of 14 or 28 mg risperidone LYN-005 capsules to assess extended release PK.

Interventionng/mL (Geometric Mean)
LYN-005 14 mg (A)31.0
LYN-005 14 mg (B)20.0
LYN-005 14 mg (C)18.6
Risperidone 2 mg (A)24.8
Risperidone 2 mg (B)30.3
Risperidone 2 mg (C)31.2
LYN-005 28 mg (A)24.6
LYN-005 28 mg (B)31.2
LYN-005 28 mg (C)30.4
Risperidone 4 mg (A)54.1
Risperidone 4 mg (B)46.3
Risperidone 4 mg (C)48.8

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