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alprazolam

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Description

Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug. [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 CID2118
CHEMBL ID661
CHEBI ID2611
SCHEMBL ID8398
MeSH IDM0000806

Synonyms (181)

Synonym
BIDD:GT0475
51339-48-1
AC-18721
BIDD:PXR0150
HMS3393A10
4h-s-triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-1-methyl-6-phenyl-
4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-1-methyl-6-phenyl-
smr000149316
MLS000559000
xanax xr
panistat
tgar01p
u-31889
staccato-alprazolam
ap-1002
xanax
niravam
az-002
8-chloro-1-methyl-6-phenyl-4h-s-triazolo(4,3-a)(1,4)benzodiazepine
CHEBI:2611 ,
8-chloro-1-methyl-6-phenyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
28981-97-7
alprazolam
C06817
MLS000759485
NCGC00159466-02
NCGC00159466-03
DB00404
8-chloro-1-methyl-6-phenyl-4h-s-triazolo[4,3-a][1,4]benzodiazepine
xanax (tn)
D00225
alprazolam (jp17/usp/inn)
tafil
4h-(1,2,4)triazolo(4,3-alpha)(1,4)benzodiazepine, 8-chloro-1-methyl-6-phenyl-
8-chloro-1-methyl-6-phenyl-4h-s-triazolo(4,3-alpha)(1,4)benzodiazepine
4h-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-1-methyl-6-phenyl-
alprazolamum
panix
apo-alpraz
pharnax
trankimazin
zolarem
anpress
alzam
ralozam
helex
intensol
alprox
tranquinal
zoldac
u 31889
tensivan
dea no. 2882
zoldax
gen-alprazolan
solanax
esparon
d 65mt
zaxan
alpaz
alprazolam extended release tablets
alpronax
mialin
zanapam
nu-alpraz
algad
prazolan
alprazolamum [inn-latin]
cassadan
alzon
tus-1
zacetin
unilan
alprazolan
xanor
frontal
zenax
alcelam
alplax
ksalol
constan
valeans
neurol
relaxol
bestrol
hsdb 7207
zotran
alprax
prazam
einecs 249-349-2
prinox
alzolam
restyl
xanagis
alprazolam intensol
brn 1223125
u-31,889
tricalma
novo-alprazol
alpram
HMS2051A10
u 31,889
alprazolam civ
CHEMBL661 ,
nsc-760140
AKOS005066050
bdbm50001728
cas-28981-97-7
dtxcid102577
tox21_111692
dtxsid4022577 ,
A819702
8-chloranyl-1-methyl-6-phenyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
MLS001423979
nsc760140
pharmakon1600-01502395
STK590494
08h ,
CCG-100855
tus 1
xanolam
zopic
zolam
xanax ts
nsc 760140
tafil d
yu55mq3izy ,
alprazolam [usan:usp:inn:ban:jan]
zopax
unii-yu55mq3izy
alprazolam [ep impurity]
alprazolam [usp monograph]
alprazolam [mart.]
alprazolam [ep monograph]
alprazolam [vandf]
alprazolam [mi]
4h-(1,2,4)triazolo(4,3-.alpha.)(1,4)benzodiazepine, 8-chloro-1-methyl-6-phenyl-
alprazolam [orange book]
alprazolam [inn]
alprazolam [usan]
alprazolam [hsdb]
alprazolam [who-dd]
alprazolam [jan]
8-chloro-1-methyl-6-phenyl-4h-s-triazolo[4,3-alpha][1,4]benzodiazepine
gtpl7111
BRD-K32398298-001-01-4
8-chloro-1-methyl-6-phenyl-4h-s-triazolo [4,3-a] [1,4] benzodiazepine
8-chloro-6-phenyl-1-methyl-4h-s-triazolo-[4,3-a][1,4]benzodiazepine
8-chloro-1-methyl-6-phenyl-4h-s-triazolo [4,3-a][1,4] benzodiazepine
NC00105
BBL028160
SCHEMBL8398
3U5J
W-107015
12-chloro-3-methyl-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene
alprazolam, european pharmacopoeia (ep) reference standard
alprazolam 1.0 mg/ml in methanol
alprazolam 0.1 mg/ml in methanol
Q319877
(z)-8-chloro-1-methyl-6-phenyl-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine
1246182-61-5
BCP28608
alprazolamextended-release
alprazolamum (latin)
alprazolamxr
alprazolamum (inn-latin)
alprazolam (usan:usp:inn:ban:jan)
alprazolam (mart.)
xanaxxr
alprazolam c-iv
8-chloro-1-methyl-6-phenyl-4h-s-triazolo
apo-alpzar
n05ba12
alprazolam (ep monograph)
alprazolam (usp monograph)
alprazolamer
alprazolamextended release
8-chloro-1-methyl-6-phenyl-4h-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine
alprazolam (ep impurity)
bnzb - human serum, benzodiazepine mix b
alprazolam, 1mg/ml in methanol

Research Excerpts

Overview

Alprazolam is an anxiolytic compound that can lead to psychological and physiological dependence especially with prolonged use. When coingested with ethanol, alprazalam can increase behavioral irritability and aggression. Alprazlam is commonly prescribed for the treatment of anxiety and other related disorders.

ExcerptReferenceRelevance
"Alprazolam is an anxiolytic compound that can lead to psychological and physiological dependence especially with prolonged use. "( Physiologically based pharmacokinetic and pharmacodynamic modelling of alprazolam: Implications for anxiety and addiction.
Burkat, PM, 2023
)
2.59
"Alprazolam is a commonly used benzodiazepine in clinical practice, and when coingested with ethanol, alprazolam can increase behavioral irritability and aggression. "( Influence of ethanol on the metabolism of alprazolam.
Huang, Z; Rao, Y; Wang, H; Xu, Z; Zhao, ZQ, 2018
)
2.19
"Alprazolam is a common medication for anxiolysis."( Association of alprazolam with major cardiovascular events in patients with hypertension.
Ho, SW; Huang, JY; Kornelius, E; Ku, MS; Tai, CL; Teng, YH; Tsai, MC; Wang, BY; Yeh, CB, 2020
)
1.63
"Alprazolam is a short-acting benzodiazepine that attenuates tremors in ET."( Effects of alprazolam on cortical activity and tremors in patients with essential tremor.
Benito-León, J; Gallego, JA; González de la Aleja, J; Ibáñez, J; Rocon, E; Romero, JP; Saíz-Díaz, RA, 2014
)
1.51
"Alprazolam is a triazolobenzodiazepine used in panic disorders and other anxiety states. "( Chromosomal and nuclear alterations in root tip cells of allium cepa L. Induced by alprazolam.
Kurteshi, K; Metovic, A; Musanovic, J; Nefic, H, 2013
)
2.06
"Alprazolam is a benzodiazepine that is commonly prescribed for the treatment of anxiety and other related disorders. "( The solvation structure of alprazolam.
Biggin, PC; Johnston, AJ; McLain, SE; Sridhar, A; Varathan, L, 2016
)
2.17
"Alprazolam is a pharmaceutical compound that it is detected in surface waters. "( Persistence of alprazolam in river water according to forced and non-forced degradation assays: adsorption to sediment and long-term degradation products.
Jiménez, JJ; Muñoz, BE; Pardo, R; Sánchez, MI, 2017
)
2.25
"Alprazolam is a triazolobenzodiazepine derivative used as a tranquilizer."( Effects of Alprazolam, Zolpidem and Zopiclone, and of chronic inflammation on peripheral experimental algesia in Wistar rats.
Antonescu, A; Bogdan, M; Dobjanschi, L; Moş, I; Mureşan, M; Muţiu, G; Zdrîncă, M, 2011
)
1.48
"Alprazolam is a benzodiazepine that, when administered acutely, results in impairments in several aspects of cognition, including attention, learning, and memory. "( A process-based approach to characterizing the effect of acute alprazolam challenge on visual paired associate learning and memory in healthy older adults.
Harel, BT; Lim, YY; Maruff, P; Pietrzak, RH; Scott, JC; Snyder, PJ, 2012
)
2.06
"Alprazolam is a benzodiazepine anxiolytic widely prescribed for treatment of panic-disorder and social phobias, although this medication is also subject to abuse. "( Concentrations of alprazolam in blood from impaired drivers and forensic autopsies were not much different but showed a high prevalence of co-ingested illicit drugs.
Holmgren, A; Jones, AW, 2013
)
2.17
"Alprazolam is a hypnotic/tranquilizer that has been shown to specifically inhibit the platelet-activating factor (PAF)-induced aggregation of human platelets. "( Suppression of monocyte chemoattractant protein 1, but not IL-8, by alprazolam: effect of alprazolam on c-Rel/p65 and c-Rel/p50 binding to the monocyte chemoattractant protein 1 promoter region.
Handa, H; Kasahara, T; Oda, T; Shimizu, N; Ueda, A, 2002
)
1.99
"Alprazolam is a benzodiazepine derivative that is currently used in the treatment of generalized anxiety, panic attacks with or without agoraphobia, and depression. "( Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature.
Verster, JC; Volkerts, ER, 2004
)
2
"Alprazolam-XR is an extended-release formulation of alprazolam designed to deliver sustained therapeutic concentrations for 24 h after once-daily dosing. "( Alprazolam extended-release in panic disorder.
Rickels, K, 2004
)
3.21
"Alprazolam is a commonly prescribed benzodiazepine. "( Alprazolam-related deaths in Palm Beach County.
Flannagan, LM; Lavezzi, WA; Middleberg, RA; Sullivan, LM; Wolf, BC, 2005
)
3.21
"Alprazolam (ALP) is a widely prescribed sedative and antidepressant benzodiazepine group of drugs. "( Alprazolam induced conformational change in hemoglobin.
Chanda, PK; Goswami, S; Karmakar, P; Maitra, S; Mukherjee, A; Saha, B; Santra, CR, 2007
)
3.23
"Alprazolam is a triazolobenzodiazepine, a derivative of the benzodiazepines. "( Alprazolam (Xanax, the Upjohn Company).
Evans, RL, 1981
)
3.15
"Alprazolam is a new type triazolobenzodiazepine anxiolytic agent. "( Alprazolam, a new type anxiolytic in neurotic patients. A pilot study.
Itoh, H; Miura, S; Takahashi, R, 1980
)
3.15
"Alprazolam is a triazolobenzodiazepine which is related to diazepam and other 1,4-benzodiazepines, and has a similar pharmacological profile. "( Alprazolam: a review of its pharmacodynamic properties and efficacy in the treatment of anxiety and depression.
Brogden, RN; Dawson, GW; Jue, SG, 1984
)
3.15
"Alprazolam appears to be an excellent anxiolytic drug, with minor cardiovascular and respiratory side effects."( [Alprazolam as premedication in ophthalmologic surgery].
Juhel, A; Le Callonnec, A; Lucas, MM; Mallédant, Y; Miras-Chatellier, A; Toulemont, PJ; Urvoy, M, 1993
)
1.92
"Alprazolam is a drug that will provide therapeutic relief for some patients with tinnitus. "( Use of alprazolam for relief of tinnitus. A double-blind study.
Brummett, R; Johnson, RM; Schleuning, A, 1993
)
2.18
"Alprazolam (APZ) is a benzodiazepine with unique antidepressant activity for a drug of its class. "( Alprazolam blocks the naloxone-stimulated hypothalamo-pituitary-adrenal axis in man.
Crosbie, GV; Grice, JE; Hockings, GI; Jackson, RV; Torpy, DJ; Walters, MM, 1993
)
3.17
"Alprazolam is a triazolobenzodiazepine that is extensively prescribed in the Western world for the treatment of anxiety and panic disorders. "( Clinical pharmacokinetics of alprazolam. Therapeutic implications.
Greenblatt, DJ; Wright, CE, 1993
)
2.02
"Alprazolam is a triazolobenzodiazepine, with a potent anxiolytic action and a short half-life. "( Antinociceptive interaction between alprazolam and opioids.
Pick, CG, 1997
)
2.01
"As alprazolam is a full agonist for the GABAA receptor complex and alpidem is a partial agonist acting with specificity on omega 1 GABAA receptor subtypes, the results are discussed."( Anticonflict effect of alpidem as compared with the benzodiazepine alprazolam in rats.
Bourin, M; Hascoët, M, 1997
)
1.05
"Alprazolam is a short-acting benzodiazepine commonly prescribed for the treatment of anxiety disorders and a potential comedication in patients with IBS."( Effect of alosetron on the pharmacokinetics of alprazolam.
D'Souza, DL; Koch, KM; Levasseur, LM; Nezamis, J; Robbins, DK; Simms, L, 2001
)
1.29
"Alprazolam is a benzodiazepine anti-anxiety agent that acts at the limbic, thalamic, and hypothalamic level of the CNS and has anxioytic. "( Accidental ingestion of alprazolam in 415 dogs.
Wismer, TA, 2002
)
2.06
"Alprazolam is a short-acting triazolobenzodiazepine with anxiolytic and antidepressant properties. "( Urinary screening for alprazolam and its major metabolites by the Abbott ADx and TDx analyzers with confirmation by GC/MS.
Bryan, W; Fraser, AD; Isner, AF,
)
1.89
"Alprazolam is a widely used antianxiety agent, yet relatively little is known about the relationship between chronic oral doses and steady-state plasma levels. "( The relationship of alprazolam dose to steady-state plasma concentrations.
Antal, EJ; Ciraulo, DA; Goldberg, DA; Greenblatt, DJ; Olson, DR; Phillips, JP; Rand, EH; Raskin, RB; Shader, RI; Smith, RB, 1990
)
2.05
"Alprazolam is a possible exception and may have both antianxiety and antidepressant properties."( Treatment of affective disorders.
Lader, MH, 1985
)
0.99
"Alprazolam (Xanax) is a relatively new triazolobenzodiazepine which is anxiolytic in man and is also prescribed in the treatment of panic attacks. "( Modification of the EMIT tox benzodiazepine assay for screening of alprazolam in serum.
Bryan, W; Fraser, AD; Isner, AF,
)
1.81
"Alprazolam appears to be an effective antidepressant in the treatment of outpatients who have a diagnosis of major depressive disorder. "( Alprazolam as an antidepressant.
Hollister, LE; Peabody, CA; Warner, MD; Whiteford, HA, 1988
)
3.16
"Alprazolam (Xanax) is a fairly new, yet very popular benzodiazepine tranquilizer. "( Detection of alprazolam (Xanax) and its metabolites in urine using dual capillary column, dual nitrogen detector gas chromatography.
Joern, AB; Joern, WA,
)
1.94
"Alprazolam was shown to be a safe treatment when combined with propranolol in these patients."( Alprazolam as an adjunct to propranolol in anxious outpatients with stable angina pectoris.
Blatt, M; Chernoff, RW; Mendels, J, 1986
)
2.44

Effects

Alprazolam has a inhibitory effect on HPA axis either in basal conditions or after central nervous system-mediated stimuli. It is unlikely to produce dependency or abuse. The drug has a role in PMS treatment and offers a therapy limited to the luteal phase.

Alprazolam has shown efficacy for control of PD symptoms, particularly in short-term controlled clinical trials. It is no longer recommended as a first-line pharmacological treatment due to concerns about the risks of developing tolerance, dependence and abuse potential.

ExcerptReferenceRelevance
"Alprazolam has a inhibitory effect on HPA axis either in basal conditions or after central nervous system-mediated stimuli."( The stimulatory effect of canrenoate, a mineralocorticoid antagonist, on the activity of the hypothalamus-pituitary-adrenal axis is abolished by alprazolam, a benzodiazepine, in humans.
Arvat, E; Ghigo, E; Giordano, R; Grottoli, S; Maccagno, B; Pellegrino, M, 2002
)
1.24
"Alprazolam has a fast onset of symptom relief (within the first week); it is unlikely to produce dependency or abuse."( Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature.
Verster, JC; Volkerts, ER, 2004
)
1.28
"For alprazolam, which has a low hepatic clearance and low extraction ratio, cimetidine significantly impaired total metabolic clearance (1.05 versus 1.66 ml/min/kg, P less than 0.005), resulting in significantly prolonged elimination half-life (16.6 versus 12.4 h, P less than 0.005)."( Interaction of cimetidine with the triazolobenzodiazepines alprazolam and triazolam.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Harmatz, JS; Moschitto, LJ; Shader, RI, 1983
)
0.99
"Alprazolam has a role in PMS treatment and offers a therapy limited to the luteal phase. "( A double-blind trial of oral progesterone, alprazolam, and placebo in treatment of severe premenstrual syndrome.
Freeman, EW; Polansky, M; Rickels, K; Sondheimer, SJ, 1995
)
2
"Alprazolam has an average terminal elimination half-life of 12 hours, whereas adinazolam generates a metabolite responsible for its benzodiazepine effects whose half-life is less than 3 hours."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
1.23
"Alprazolam has a shorter half-life, which may lead to more withdrawal symptoms than diazepam."( Alprazolam and diazepam: addiction potential.
Juergens, S, 1991
)
2.45
"Alprazolam has been suggested as a potentially useful agent for treatment of individuals with ET, but its efficacy and safety are uncertain."( Alprazolam for essential tremor.
Bruno, E; Colosimo, C; Filippini, G; Nicoletti, A; Quattrocchi, G; Zappia, M, 2015
)
2.58
"Alprazolam, has been associated with disproportionate harms compared to other benzodiazepines, especially among people in opioid substitution treatment (OST). "( Alprazolam use and related harm among opioid substitution treatment clients - 12 months follow up after regulatory rescheduling.
Cubitt, T; Deacon, RM; Ezard, N; Larance, B; Leung, S; Lintzeris, N; Monds, LA; Nielsen, S; Rivas, G, 2016
)
3.32
"Alprazolam has been demonstrated to have efficacy, safety and good tolerability in the treatment of the acute phase of panic disorder, the sublingual tablets showing some comparative advantages."( Efficacy of alprazolam sublingual tablets in the treatment of the acute phase of panic disorders.
Arenoso, H; Caruso, N; Márquez, M,
)
1.95
"Alprazolam has shown efficacy for control of PD symptoms, particularly in short-term controlled clinical trials, but is no longer recommended as a first-line pharmacological treatment due to concerns about the risks of developing tolerance, dependence and abuse potential. "( The role of alprazolam for the treatment of panic disorder in Australia.
Berk, M; Giorlando, F; Moylan, S; Nordfjærn, T, 2012
)
2.2
"Alprazolam has a inhibitory effect on HPA axis either in basal conditions or after central nervous system-mediated stimuli."( The stimulatory effect of canrenoate, a mineralocorticoid antagonist, on the activity of the hypothalamus-pituitary-adrenal axis is abolished by alprazolam, a benzodiazepine, in humans.
Arvat, E; Ghigo, E; Giordano, R; Grottoli, S; Maccagno, B; Pellegrino, M, 2002
)
1.24
"Alprazolam has a fast onset of symptom relief (within the first week); it is unlikely to produce dependency or abuse."( Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature.
Verster, JC; Volkerts, ER, 2004
)
1.28
"Alprazolam has been used in elderly patients with beneficial results and a low frequency of adverse reactions."( Alprazolam: pharmacokinetics, clinical efficacy, and mechanism of action.
Fawcett, JA; Kravitz, HM,
)
2.3
"For alprazolam, which has a low hepatic clearance and low extraction ratio, cimetidine significantly impaired total metabolic clearance (1.05 versus 1.66 ml/min/kg, P less than 0.005), resulting in significantly prolonged elimination half-life (16.6 versus 12.4 h, P less than 0.005)."( Interaction of cimetidine with the triazolobenzodiazepines alprazolam and triazolam.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Harmatz, JS; Moschitto, LJ; Shader, RI, 1983
)
0.99
"Alprazolam has antidepressant activity and has been shown to be similar in efficacy to imipramine in the treatment of unipolar depression."( Alprazolam: a review of its pharmacodynamic properties and efficacy in the treatment of anxiety and depression.
Brogden, RN; Dawson, GW; Jue, SG, 1984
)
2.43
"Alprazolam has a role in PMS treatment and offers a therapy limited to the luteal phase. "( A double-blind trial of oral progesterone, alprazolam, and placebo in treatment of severe premenstrual syndrome.
Freeman, EW; Polansky, M; Rickels, K; Sondheimer, SJ, 1995
)
2
"Alprazolam has proven efficacy as a treatment for panic disorder, but the place of other benzodiazepines is less well established."( Diazepam versus alprazolam for the treatment of panic disorder.
Burrows, GD; Cook, BL; Garvey, MJ; Judd, FK; Marriott, P; Norman, TR; Noyes, R; Reich, JH, 1996
)
2.08
"Alprazolam has been relatively difficult to confirm."( Detection of alprazolam in three cases of methadone/benzodiazepine overdose.
Brissie, RM; Hall, MA; Robinson, CA; Rogers, WO, 1997
)
1.39
"Alprazolam has been suggested as an adjuvant to neuroleptic drugs in the treatment of schizophrenic patients. "( Acute administration of alprazolam has no effect on plasma homovanillic acid concentration in normal subjects.
Davidson, M; Jaff, S; McQueeney, R; Zemishlany, Z,
)
1.88
"Alprazolam has an average terminal elimination half-life of 12 hours, whereas adinazolam generates a metabolite responsible for its benzodiazepine effects whose half-life is less than 3 hours."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
1.23
"Alprazolam has a shorter half-life, which may lead to more withdrawal symptoms than diazepam."( Alprazolam and diazepam: addiction potential.
Juergens, S, 1991
)
2.45
"Alprazolam has shown competitive antagonism on muscarinic and histamine H1 receptors, and noncompetitive antagonism on histamine H2 receptors."( Blockade of muscarinic, histamine H1 and histamine H2 receptors by antidepressants.
Alvarez, FJ; Palomares, JL; Velasco, A, 1988
)
1

Actions

The alprazolam group had lower higher scores in PSQI than that before treatment, with great statistical significant in difference (P < 0.01) The drug did not produce treatment differences in pregnancy outcomes or in dam-pup interactions.

ExcerptReferenceRelevance
"The alprazolam group had lower higher scores in PSQI than that before treatment, with great statistical significant in difference (P < 0.01)."( [Study on efficacy of zaoren anshen capsules in treating senile insomnia and changes in its hemorheology].
Gan, JG; Qin, GX; Tian, GQ, 2013
)
0.87
"Alprazolam did not produce treatment differences in pregnancy outcomes or in dam-pup interactions. "( Effects from prenatal exposure to alprazolam on the social behavior of mice offspring.
Christensen, HD; Gonzalez, CL; Rayburn, WF, 2003
)
2.04
"Alprazolam appears to produce rapid and specific clinical improvement in patients with severe agoraphobia and panic attacks and deserves further evaluation under double-blind conditions."( Some biochemical correlates of panic attacks with agoraphobia and their response to a new treatment.
Coleman, JH; Greenblatt, DJ; Jones, KJ; Levine, PH; Orsulak, PJ; Peterson, M; Schildkraut, JJ; Sheehan, DV; Uzogara, E; Watkins, D, 1984
)
0.99
"Alprazolam tended to produce earlier impairment and earlier recovery."( Alprazolam and lorazepam effects on memory acquisition and retrieval processes.
Berchou, R; Block, RI, 1984
)
2.43
"Alprazolam resulted in lower anxiety and pain ratings during pain stimulation, supporting the idea that (presumably pain-related) anxiety may increase the experience of pain."( No interactive effects of naltrexone and benzodiazepines on pain during phobic fear.
Arntz, A; Janssen, SA, 1999
)
1.02
"Alprazolam produced an increase in levels of forgetting, especially on day 5."( The effects of repeated doses of clomipramine and alprazolam on physiological, psychomotor and cognitive functions in normal subjects.
Allen, D; Curran, HV; Lader, M, 1991
)
1.26

Treatment

Treatment with alprazolam was found to reverse partially the adverse effects of postinoculation stress, and also to inhibit the beneficial effects of the preinoculations administration of stress on tumor development. Treatment with al prazolamic increased hypothalamic CRF concentrations, which was associated with lower plasma ACTH concentrations.

ExcerptReferenceRelevance
"Alprazolam treatment initiation with packs of more than 50 tablets also increased from 63 of 1127 people (5.6%) before the intervention to 144 of 589 people (24.4%) after the intervention (RD, 18.9% [95% CI, 15.1%-22.6%])."( Comparison of Prescribing Patterns Before and After Implementation of a National Policy to Reduce Inappropriate Alprazolam Prescribing in Australia.
Buckley, NA; Cairns, R; Pearson, S; Schaffer, AL, 2019
)
1.45
"Alprazolam pre-treatment significantly reduced the GH response to ITT (p < 0.003), the peak electromyography (p < 0.0001) and galvanic skin response (GSR, p = 0.04) to acoustic startle, the resting GSR (p = 0.01), and increased appetite following ITT (p < 0.0005)."( Neuroendocrine and sympathetic responses to an orexin receptor antagonist, SB-649868, and alprazolam following insulin-induced hypoglycemia in humans.
Bullmore, ET; Kanakaraj, P; Koch, A; Lawrence, P; Miller, SR; Napolitano, A; Nathan, PJ; Patel, AX, 2014
)
1.34
"Nine alprazolam-treated participants (75%) developed AEs, mainly represented by sedation (50%), constipation (17%) and dry mouth (9%)."( Alprazolam for essential tremor.
Bruno, E; Colosimo, C; Filippini, G; Nicoletti, A; Quattrocchi, G; Zappia, M, 2015
)
2.31
"The alprazolam-treated rats were given 5, 10 or 20 mg/kg (low, medium, high) of alprazolam by intragastric administration each day for 14 days."( Effect of alprazolam on rat serum metabolic profiles.
Cao, G; Cao, Y; Chen, B; Li, Y; Li, Z; Lin, G; Wang, L; Wang, X; Wen, C; Yang, X; Zhang, J, 2017
)
1.34
"Alprazolam treatment for 14 days dose dependently reversed DOX-induced increase in LDH and MDA as well as the morphological alterations induced by DOX in TEM studies."( Effect of alprazolam on anxiety and cardiomyopathy induced by doxorubicin in mice.
Akhtar, M; Anwar, MJ; Khanam, R; Pillai, KK; Vohora, D, 2012
)
1.5
"Alprazolam pretreatment significantly attenuated the discriminative stimulus effects of D-amphetamine, and some of the self-reported drug effects."( Alprazolam attenuates the behavioral effects of d-amphetamine in humans.
Glaser, PE; Hays, LR; Rush, CR; Stoops, WW; Wagner, FP, 2004
)
2.49
"Alprazolam treatment of anxious patients with poorly controlled diabetes may result in decreased anxiety and improved glucose regulation through independent mechanisms."( Effects of alprazolam on glucose regulation in diabetes. Results of double-blind, placebo-controlled trial.
Carney, RM; Clouse, RE; Eisen, SA; Freedland, KE; Griffith, LS; Lustman, PJ; McGill, JB; Rubin, EH, 1995
)
1.4
"Alprazolam treatment did not alter the increase in NK cell numbers but did inhibit the increase in NK activity."( Modulation of the immunologic response to acute stress in humans by beta-blockade or benzodiazepines.
Benschop, RJ; Jacobs, R; Raab, JR; Schedlowski, M; Schmidt, RE; Schürmeyer, TH; Sommer, B, 1996
)
1.02
"Alprazolam treatment is seemed to be available for SAD patients."( [The efficiency of alprazolam for seasonal affective disorder (SAD, autumn/winter type)].
Endo, S; Nakamura, S; Suzuki, H; Yamadera, H, 1997
)
1.35
"Alprazolam pretreatment also markedly attenuated the ACTH response to hypoglycemia whereas the cortisol response was only moderately affected."( Hypoglycemia-induced inhibition of LH and stimulation of ACTH secretion in the rhesus monkey is blocked by alprazolam.
Farley, AE; Reid, RL; Van Vugt, DA; Washburn, DL, 1997
)
1.23
"Both alprazolam treatment groups (6 mg and 2 mg) improved significantly more than did the placebo treatment group on most outcome measures."( A fixed-dose study of alprazolam 2 mg, alprazolam 6 mg, and placebo in panic disorder.
Ballenger, JC; DuPont, R; Laraia, M; Lesser, IM; Lydiard, RB; Rubin, RT, 1992
)
1.05
"Alprazolam pretreatment attenuated the 2DG-related cortisol elevations (P = 0.05) but did not effect 2DG-induced glucose increases."( Alprazolam attenuates metabolic stress-induced neuroendocrine and behavioral effects in humans.
Breier, A; Buchanan, RW; Davis, OR, 1991
)
2.45
"Alprazolam-treated patients most frequently reported central nervous system-related side effects (drowsiness and sedation), while buspirone-treated patients most frequently reported gastrointestinal system-related side effects (appetite disturbances and abdominal complaints)."( Alprazolam versus buspirone in the treatment of outpatients with generalized anxiety disorder.
Enkelmann, R, 1991
)
2.45
"Alprazolam treatment is effective for panic disorder, but its major disadvantages include possible dependence and withdrawal symptoms upon discontinuation. "( Preliminary evidence for the utility of carbamazepine in alprazolam withdrawal.
Klein, E; Post, RM; Uhde, TW, 1986
)
1.96
"Alprazolam treatment led to a complete remission of panic attacks in 85% of the patients; panics ceased within an average of 6 days, at a mean dose of 2.2 mg/day."( Alprazolam treatment for panic disorders.
Alexander, DD; Alexander, PE, 1986
)
2.44
"Alprazolam treatment in eight patients markedly attenuated anxiety increases during rebreathing."( Carbon dioxide sensitivity in panic anxiety. Ventilatory and anxiogenic response to carbon dioxide in healthy subjects and patients with panic anxiety before and after alprazolam treatment.
Charney, DS; Goodman, WK; Heninger, GR; Loke, J; Redmond, DE; Woods, SW, 1986
)
1.19
"All alprazolam treatments resulted in significantly greater sedation than placebo on days 1 and 4."( Influence of dosing regimen on alprazolam and metabolite serum concentrations and tolerance to sedative and psychomotor effects.
Kroboth, PD; Smith, RB, 1987
)
1.04
"The alprazolam treated group had a significantly smaller proportion of infarcted tissue in the ventricular section (2.3%) and in the apical sections (1.8%) than the vehicle injected rats (6.5% and 14.7% respectively)."( Alprazolam decreases isoproterenol induced myocardial damage in the rat.
Berkowitz, K; Conahan, S; Vogel, WH, 1988
)
2.2
"Alprazolam treatment was tapered in 17 panic patients at a rate of 10% of the starting dose every 3 days. "( Discontinuation of alprazolam treatment in panic patients.
Campeas, R; Davies, SO; Fyer, AJ; Goetz, D; Gorman, JM; Klein, DF; Levin, A; Liebowitz, MR, 1987
)
2.04
"Treatment for alprazolam dependence is growing."( Alprazolam-related deaths in Scotland, 2004-2020.
Chiappini, S; Corkery, JM; Guirguis, A; Martinotti, G; Schifano, F, 2022
)
2.51
"The treatment with alprazolam during pregnancy involved cellular and molecular changes in the immature cerebellum."( Prenatal effects of alprazolam treatment on the immature cerebellum of rats.
Botelho, FV; Hirano, LQL; Mascarenhas, FNADP; Menezes-Reis, LT; Ribeiro, DL; Silva, NF; Vieira, LG; Zanon, RG, 2022
)
1.36
"Treatment with alprazolam significantly affected the behavior of the zebrafish, e.g., following alprazolam administration time spent in the zone and time freezing were longer in the green zone than in red."( Effects of alprazolam treatment on anxiety-like behavior induced by color stimulation in adult zebrafish.
Doboszewska, U; Guz, L; Pieróg, M; Poleszak, E; Wlaź, P, 2018
)
1.21
"Pretreatment with alprazolam (2 or 4 mg/kg, ip) or oxazepam (20 or 40 mg/kg, ip) reversed the conditioned reinforcer-induced reinstatement of extinguished cocaine-seeking behavior at doses that did not reliably affect the conditioned reinforcer-induced reinstatement of extinguished food seeking, suggesting that benzodiazepines may not have reduced reinstatement responding due to non-specific reductions in behavior."( Alprazolam and oxazepam block the cue-induced reinstatement of extinguished cocaine seeking in rats.
Clampitt, DM; Goeders, NE; Guerin, GF; Keller, C; Sharma, M, 2009
)
2.12
"Treatment with alprazolam reversed the adverse effects of stress."( Inhibitory effects of alprazolam on the development of acute experimental autoimmune encephalomyelitis in stressed rats.
Almeida-Dias, A; Freire-Garabal, M; Novío, S; Núñez-Iglesias, MJ, 2010
)
1.01
"Treatment with alprazolam partially reverses the adverse effects of stress."( The antioxidant potential of alprazolam on the redox status of peripheral blood leukocytes in restraint-stressed mice.
Amigo, G; Freire-Garabal, M; Novío, S; Núñez, MJ, 2011
)
1
"Pretreatment with alprazolam (0.25 and 0.5 mg/kg, i.p.) significantly reversed immobilization stress-induced anxiety, analgesia and impaired locomotor activity."( Protective effect of alprazolam in acute immobilization stress-induced certain behavioral and biochemical alterations in mice.
Anil, K; Goyal, R,
)
0.77
"Treatment with alprazolam (0.25 and 0.5 mg/kg, ip) significantly improved behavioral alterations."( Protective effect of alprazolam against sleep deprivation-induced behavior alterations and oxidative damage in mice.
Kumar, A; Singh, A, 2008
)
1
"Treatment with alprazolam resulted in a significant reduction of stress-induced increase of virus titters and pulmonary vascular permeability."( Effects of alprazolam on influenza virus infection in stressed mice.
Balboa, JL; Belmonte, A; Fernandez-Rial, JC; Freire-Garabal, M; Núñez, MJ, 1993
)
1.02
"Treatment with alprazolam was found to reverse partially the adverse effects of postinoculation stress, and also to inhibit the beneficial effects of the preinoculation administration of stress on tumor development."( Effects of alprazolam on the development of Moloney sarcoma virus-induced tumors in stressed mice.
Balboa, JL; Fernández-Rial, JC; Freire-Garabal, M; García-Vallejo, L; Núñez-Iglesias, MJ; Rey-Méndez, M, 1996
)
1.02
"Treatment with alprazolam (1 mg/Kg) partially reversed this adverse effect of stress."( Effects of alprazolam on the free-choice ethanol consumption induced by isolation stress in aged rats.
Becerra, MA; De Miguel, S; Freire-Garabal, M; Legazpi, MP; Mayán, JM; Núñez, LA; Núñez, MJ; Quintans, MR; Rey-Méndez, M; Riveiro, P; Varela, M, 1999
)
1.03
"Treatment with alprazolam significantly reversed these adverse effects of stress, showing that, besides the psychopharmacological properties of this anxiolytic drug against stress, it has consequences for Candida infection."( Effects of psychological stress and alprazolam on development of oral candidiasis in rats.
Balboa, J; Freire-Garabal, M; García-Vallejo, LA; Liñares, D; Mañá, P; Núñez, MJ; Rey-Méndez, M; Riveiro, P; Rodríguez-Cobos, A; Suárez-Quintanilla, JA, 2002
)
0.93
"treatment with alprazolam induced clear physical dependence in DBA/2J mice as assessed by precipitation of a withdrawal syndrome with an i.v."( Physical dependence induced in DBA/2J mice by benzodiazepine receptor full agonists, but not by the partial agonist Ro 16-6028.
Haefely, WE; Jenck, F; Martin, JR; Moreau, JL; Pieri, L; Schoch, P, 1990
)
0.62
"Pretreatment with alprazolam but not with clonidine significantly reduced the CO2-induced increase in ratings of anxiety."( Effects of alprazolam and clonidine on carbon dioxide-induced increases in anxiety ratings in healthy human subjects.
Charney, DS; Heninger, GR; Krystal, JH; Woods, SW, 1989
)
0.99
"Treatment with alprazolam or adinazolam increased hypothalamic CRF concentrations, which was associated with lower plasma ACTH concentrations."( Acute effects of alprazolam and adinazolam on the concentrations of corticotropin-releasing factor in the rat brain.
Bissette, G; Nemeroff, CB; Owens, MJ, 1989
)
0.96

Toxicity

The primary purpose of this study was to examine whether alprazolam pretreatment can increase the analgesic potency of morphine without increasing opioid side-effect intensities. Both medications were well tolerated with drowsiness being the most common side effect of alpazolam, and insomnia, dry mouth, and constipation, the complaints most associated with desipramine.

ExcerptReferenceRelevance
"The primary purpose of this study was to examine whether alprazolam pretreatment can increase the analgesic potency of morphine without increasing opioid side-effect intensities."( Influence of alprazolam on opioid analgesia and side effects during steady-state morphine infusions.
Coda, BA; Hill, HF; Mackie, A, 1992
)
0.9
"Clinical outcome and adverse effects associated with concurrent alprazolam and imipramine administration were studied in 29 patients with major depressive disorder who completed a 6-week trial in which they served as their own controls."( Clinical outcome and adverse effect profile associated with concurrent administration of alprazolam and imipramine.
Antal, EJ; Ereshefsky, L; Evans, RL; Grimmig, J; Hamann, G; Lobeck, F; Rawls, WN; Smith, RB; Wells, BG, 1988
)
0.74
" Both medications were well tolerated with drowsiness being the most common side effect of alprazolam, and insomnia, dry mouth, and constipation, the complaints most associated with desipramine."( A comparison of the efficacy and safety of alprazolam and desipramine in depressed outpatients.
Buchanan, RA; Fleming, JA; Gibson, RE; Keller, FD; Remick, RA, 1988
)
0.76
" However, five of twenty-nine alprazolam patients had to discontinue therapy because of excessive drowsiness, and two of the alprazolam outpatients had motor vehicle accidents directly related to this adverse event."( A comparison of the safety and efficacy of alprazolam and desipramine in moderately severe depression.
Buchanan, RA; Fleming, JA; Hamilton, P; Keller, FD; Loomer, F; Miles, JE; Remick, RA, 1985
)
0.82
" Reported incidences of adverse events can be viewed as being a combination of psychoactive drug effects, disease state effects and other concomitant effects."( Use of statistics in the analysis of side effect data from clinical trials of psychoactive agents.
Assenzo, JR; Shu, VS, 1982
)
0.26
" The efficacy of alprazolam and placebo in panic disorder with agoraphobia, and the side-effect and adverse effect profiles of both drug groups were measured."( Safety and side-effects of alprazolam. Controlled study in agoraphobia with panic disorder.
Başoğlu, M; Kirby, M; Kuch, K; Marks, IM; Noshirvani, H; O'Sullivan, GH; Swinson, R, 1994
)
0.93
"Alprazolam caused side-effects and adverse effects during treatment but many patients were willing to accept these."( Safety and side-effects of alprazolam. Controlled study in agoraphobia with panic disorder.
Başoğlu, M; Kirby, M; Kuch, K; Marks, IM; Noshirvani, H; O'Sullivan, GH; Swinson, R, 1994
)
2.03
" If a side effect profile is known, it will be easier for a clinician to choose the right drug and the appropriate management by taking into account compliance, safety and efficacy in each patient under treatment."( Adverse effects associated with the short-term treatment of panic disorder with imipramine, alprazolam or placebo.
Benkert, O; Cassano, GB; Curtis, G; Deltito, J; Hippius, H; Klerman, G; Maier, W; Petracca, A; Shera, D; Toni, C, 1994
)
0.51
" The value of the Saskatchewan datafiles in an acute adverse event signalling scheme has been evaluated using two benzodiazepines."( Acute adverse event signalling scheme using the Saskatchewan Administrative health care utilization datafiles: results for two benzodiazepines.
Rawson, MJ; Rawson, NS, 1999
)
0.3
" In addition to its therapeutic effects, alprazolam produces adverse effects, such as drowsiness and sedation."( Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature.
Verster, JC; Volkerts, ER, 2004
)
0.82
"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
"The aim of this study was to determine how often do psychiatric outpatients suffer from adverse effects of benzodiazepines, and which adverse effects do they notice."( Adverse effects of benzodiazepines in psychiatric outpatients.
Arbanas, D; Arbanas, G; Dujam, K, 2009
)
0.35
" All of the women who used benzodiazepines had at least one adverse effect; and 91% of men had adverse effects."( Adverse effects of benzodiazepines in psychiatric outpatients.
Arbanas, D; Arbanas, G; Dujam, K, 2009
)
0.35
" Many of them notice adverse effects, but mainly continue to use the drug."( Adverse effects of benzodiazepines in psychiatric outpatients.
Arbanas, D; Arbanas, G; Dujam, K, 2009
)
0.35
" They are mostly presented in the group of mood stabilizers and antiepileptic drugs, particularly the carbamazepine and lamotrigine, and can be manifested through the Stevens Johnson syndrome, Toxic Epidermal Necrolysis (TEN)/Lyell's syndrome with about 30% lethality."( Exanthema medicamentosum as a side effect of promazine.
Cvitanović, MZ; Hlevnjak, I; Lasić, D; Uglešić, B; Višić, V, 2011
)
0.37
"Lack of a safe and convenient disposal method for expired and unused medications may lead to many problems such as accidental exposure, intentional misuse, and food and water contamination."( Evaluation of an activated carbon disposal system for safe disposal of model prescription sedative medications.
Anderson, C; Banga, AK; Dasht Bozorg, B; Fowler, W; Korey, A, 2020
)
0.56
"The co-abuse of ALZ has amplified the hepato-renal toxic effects of MPH."( Co-abuse of alprazolam augments the hepato-renal toxic effects of methylphenidate.
Chopra, K; Dharavath, RN; Dutt, M; Kaur, N; Kaur, T; Sharma, S,
)
0.51
" The primary outcomes included the adverse effects and anxiety level."( Effectiveness and safety of oral sedation in adult patients undergoing dental procedures: a systematic review.
Araújo, JO; Bergamaschi, CC; de Andrade, NK; Guimarães, CC; Lopes, LC; Motta, RHL; Ramacciato, JC, 2021
)
0.62

Pharmacokinetics

Fluoxetine significantly prolonged alprazolam half-life (20 versus 17 hours) and reduced clearance (48 versus 61 ml/min) After single 1 mg oral doses in humans, typical pharmacokinetic variables for alpazolam are: a peak plasma concentration 12 to 22 micrograms/L.

ExcerptReferenceRelevance
" When the sequence of trials was placebo first and fluoxetine second, fluoxetine coadministration significantly prolonged alprazolam half-life (20 versus 17 hours) and reduced clearance (48 versus 61 ml/min)."( Fluoxetine impairs clearance of alprazolam but not of clonazepam.
Cotreau, MM; Greenblatt, DJ; Harmatz, JS; Horst, WD; Preskorn, SH, 1992
)
0.77
" Pharmacodynamic measures showed that sublingual and oral alprazolam both produced sedation, fatigue, impaired digit symbol substitution, slowing of reaction time, and impairment of the acquisition and recall of information."( The pharmacokinetics and pharmacodynamics of sublingual and oral alprazolam in the post-prandial state.
Friedman, H; Goddard, JE; Greenblatt, DJ; Harmatz, JS; Scavone, JM; Shader, RI, 1992
)
0.77
"Alprazolam, adinazolam, and clonazepam share the typical pharmacological effects of benzodiazepines yet are diverse in their pharmacokinetic properties."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
1.95
"5 mg of alprazolam on Day 1 the mean elimination half-life was 11."( Pharmacokinetics of alprazolam in geriatric patients with neurotic depression.
Agrell, B; Dehlin, O; Kullingsjö, H; Lidén, A; Moser, G; Olsen, I, 1991
)
1.04
" There was also a tendency for a later Tmax and a longer elimination half-life in CAPD patients than in normal subjects or HD patients."( Alprazolam in end-stage renal disease: I. Pharmacokinetics.
Kroboth, PD; Piraino, B; Schmith, VD; Smith, RB, 1991
)
1.72
" Mean values of elimination half-life in humans (11."( Comparative pharmacokinetics of alprazolam and lorazepam in humans and in African Green Monkeys.
Friedman, H; Greenblatt, DJ; Redmond, DE, 1991
)
0.56
" No difference in alprazolam pharmacokinetic parameters was observed during the menstrual cycle phases."( Influence of menstrual cycle and gender on alprazolam pharmacokinetics.
DeVane, CL; Hayes, P; Kirkwood, C; Moore, A; Pelonero, A, 1991
)
0.88
"The pharmacokinetic and pharmacodynamic effects of concomitant administration of alprazolam and fluoxetine were studied in this double-blind parallel study in 80 healthy, male volunteers."( Pharmacokinetic pharmacodynamic evaluation of the combined administration of alprazolam and fluoxetine.
Antal, EJ; Fleishaker, JC; Lasher, TA; Steenwyk, RC, 1991
)
0.74
"Six healthy volunteers participated in a study of the pharmacokinetic and psychomotor effects of a single dose of 2 mg of alprazolam compared to placebo when given at night."( Pharmacokinetic and pharmacodynamic effects of a single nocturnal dose of alprazolam.
Burrows, GD; McIntyre, IM; Norman, TR, 1990
)
0.72
" The authors examined the possibilities of a pharmacokinetic effect of alprazolam on neuroleptic plasma levels and of a clinical effect of alprazolam."( Neuroleptic augmentation with alprazolam: clinical effects and pharmacokinetic correlates.
Angrist, B; Cooper, T; Douyon, R; Peselow, E; Rotrosen, J, 1989
)
0.8
"The ability to estimate population pharmacokinetic parameters of alprazolam from fragmentary clinical data collected during clinical efficacy trials was evaluated in this series of studies."( An evaluation of population pharmacokinetics in therapeutic trials. Part III. Prospective data collection versus retrospective data assembly.
Antal, EJ; Grasela, TH; Smith, RB, 1989
)
0.51
" There were no overall differences observed in the elimination half-life of antipyrine, nor were there significant differences between trials in cumulative urinary excretion or fractional recovery of intact antipyrine, 4-hydroxyantipyrine, norantipyrine, or 3-hydroxymethyl antipyrine."( Lack of effect of influenza vaccine on the pharmacokinetics of antipyrine, alprazolam, paracetamol (acetaminophen) and lorazepam.
Blyden, GT; Greenblatt, DJ; Scavone, JM, 1989
)
0.51
" Mean pharmacokinetic parameters for IV administration were consistent with previous results."( Pharmacokinetics and pharmacodynamics of alprazolam following single and multiple oral doses of a sustained-release formulation.
Eller, MG; Fleishaker, JC; Phillips, JP; Smith, RB, 1989
)
0.54
"The contribution of differential absorption-distribution pharmacokinetics to drug activity can be partially determined by comparing simultaneous estimates of drug serum level with pharmacodynamic effects."( Comparative pharmacokinetics and pharmacodynamics of lorazepam, alprazolam and diazepam.
Bjornsson, TD; Ellinwood, EH; Heatherly, DG; Kilts, C; Nikaido, AM, 1985
)
0.51
" Moreover, for triazolam, the C max was increased and the plasma elimination half-life was prolonged; oral clearance of the two triazolobenzodiazepines was markedly reduced."( Pharmacokinetic consequences of long term coadministration of cimetidine and triazolobenzodiazepines, alprazolam and triazolam, in healthy subjects.
Desager, JP; Harvengt, C; Hulhoven, R; Pourbaix, S; Smith, RB, 1985
)
0.48
" Compared with control, metronidazole significantly prolonged phenytoin half-life (23 versus 16 hours, P less than ."( Metronidazole impairs clearance of phenytoin but not of alprazolam or lorazepam.
Blyden, GT; Greenblatt, DJ; Scavone, JM, 1988
)
0.52
"39 L/kg), elimination half-life (11."( Alprazolam pharmacokinetics in women on low-dose oral contraceptives.
Greenblatt, DJ; Locniskar, A; Scavone, JM; Shader, RI, 1988
)
1.72
" No statistically significant differences in pharmacokinetic parameters were found between groups."( Abuse liability and clinical pharmacokinetics of alprazolam in alcoholic men.
Barnhill, JG; Ciraulo, AM; Ciraulo, DA; Foti, ME; Greenblatt, DJ; Molloy, MA; Shader, RI; Tarmey, MF, 1988
)
0.53
"The use of observational data, collected during the routine clinical care of patients, has been advocated as a means to obtain clinically relevant information regarding the pharmacokinetic parameters of drugs."( An evaluation of population pharmacokinetics in therapeutic trials. Part II. Detection of a drug-drug interaction.
Antal, EJ; Ereshefsky, L; Evans, RL; Grasela, TH; Smith, RB; Wells, BG, 1987
)
0.27
"NONMEM, a computer program that uses the method of extended least-squares analysis, has been advocated as a means of obtaining estimates of population pharmacokinetic parameters when only fragmentary information can be obtained from subjects."( An evaluation of population pharmacokinetics in therapeutic trials. Part I. Comparison of methodologies.
Antal, EJ; Grasela, TH; Smith, RB; Townsend, RJ, 1986
)
0.27
"1 hours and has a serum half-life of 12 to 15 hours."( Alprazolam: pharmacokinetics, clinical efficacy, and mechanism of action.
Fawcett, JA; Kravitz, HM,
)
1.57
" The pharmacokinetic properties of these newer drugs can best be understood by their categorisation according to range of elimination half-life and pathway of metabolism (oxidation versus conjugation)."( Clinical pharmacokinetics of the newer benzodiazepines.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Ochs, HR; Shader, RI,
)
0.13
" However, if given once-daily it still would not accumulate with long term dosing due to its short half-life relative to the interval between doses."( The influence of obesity on the pharmacokinetics of oral alprazolam and triazolam.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI; Smith, RB,
)
0.38
" The pharmacokinetic parameters derived from plasma alprazolam concentrations were compared with data obtained from 17 normal subjects who were matched for age and sex."( Alprazolam pharmacokinetics in alcoholic liver disease.
Dittert, LW; Juhl, RP; Smith, RB; Van Thiel, DH,
)
1.82
"84 l/kg; elimination half-life (t1/2) 11."( Pharmacokinetics and pharmacodynamics of alprazolam after oral and IV administration.
Juhl, RP; Kroboth, PD; Phillips, JP; Smith, RB; Vanderlugt, JT, 1984
)
0.53
" Pharmacokinetic values were calculated, and mean data from the smoking and nonsmoking groups were compared."( Single- and multiple-dose pharmacokinetics of oral alprazolam in healthy smoking and nonsmoking men.
Gwilt, PR; Smith, RB; Wright, CE,
)
0.38
" Pharmacokinetic investigations by radioimmunoassay showed a dose-dependent fast rise of plasma concentrations with a peak at 1 h and a rapid decline thereafter."( Pharmacokinetic and -dynamic studies with a new anxiolytic, suriclone, utilizing EEG mapping and psychometry.
Anderer, P; Chwatal, K; Grünberger, J; Linzmayer, L; Saletu, B; Semlitsch, HV, 1994
)
0.29
"We have assessed the pharmacokinetic and pharmacodynamic interaction between fluvoxamine, a serotonin reuptake inhibitor, and alprazolam, a triazolobenzo-diazepine."( A pharmacokinetic and pharmacodynamic evaluation of the combined administration of alprazolam and fluvoxamine.
Fleishaker, JC; Hulst, LK, 1994
)
0.72
"The steady-state pharmacokinetic interaction between buspirone and alprazolam was evaluated in a parallel study with two groups of 12 male volunteers each."( A study of pharmacokinetic interaction between buspirone and alprazolam at steady state.
Barbhaiya, RH; Buch, AB; Seidehamel, RJ; Van Harken, DR, 1993
)
0.76
"The feasibility of incorporating blood sampling for population pharmacokinetic analysis into postmarketing surveillance was evaluated."( Evaluation of population pharmacokinetics in therapeutic trials. IV. Application to postmarketing surveillance.
Antal, EJ; DeVane, CL; Grasela, TH; Miller, RL, 1993
)
0.29
" The mean terminal half-life in serum was 12."( Pharmacokinetics in lactating women: prediction of alprazolam transfer into milk.
Desai, N; Kuhn, RJ; McNamara, PJ; Oo, CY; Wright, CE, 1995
)
0.54
" Noncompartmental pharmacokinetic analysis showed that at steady state, alprazolam Cmax and AUCtau values significantly increased approximately twofold and 4OH Cmax and AUCtau values significantly decreased by 40 and 26%, respectively, when nefazodone was coadministered with alprazolam."( Coadministration of nefazodone and benzodiazepines: III. A pharmacokinetic interaction study with alprazolam.
Barbhaiya, RH; Dockens, RC; Greene, DS; Kroboth, P; Salazar, DE, 1995
)
0.74
" In all studies, blood samples were also obtained at testing times so that effect/concentration comparisons could be made and so full pharmacokinetic analyses could be done for separate studies."( Coadministration of nefazodone and benzodiazepines: I. Pharmacodynamic assessment.
Barbhaiya, R; Chaikin, PC; Folan, MM; Kroboth, PD; Lush, RM; Salazar, DE; Shukla, UA, 1995
)
0.29
" None of the mean pharmacokinetic parameters was significantly different between the EM and PM phenotype groups."( Effects of genetically determined S-mephenytoin 4-hydroxylation status and cigarette smoking on the single-dose pharmacokinetics of oral alprazolam.
Chiba, K; Hayashi, K; Ishizaki, T; Kaneko, S; Ohkubo, T; Osanai, T; Otani, K; Sugawara, K; Yasui, N, 1997
)
0.5
" Area under the concentration-time curve and peak concentration for alprazolam increased proportionally with each higher dose; clearance did not differ significantly between treatments."( Pharmacokinetics and psychomotor performance of alprazolam: concentration-effect relationship.
Antal, EJ; Fleishaker, JC; Sisson, TL; Wright, CE, 1997
)
0.79
" The sigmoid maximal effect-link pharmacodynamic model indicated that caffeine did not alter the concentration at half of the maximal effect value of alprazolam and suggested that the interaction is not competitive, but independent."( Differential reinforcement of low rate performance, pharmacokinetics and pharmacokinetic-pharmacodynamic modeling: independent interaction of alprazolam and caffeine.
Falk, JL; Lau, CE; Wang, Y, 1997
)
0.7
" The means +/- standard deviation of the peak plasma concentration, the total area under the plasma concentration-time curve and the elimination half-life of alprazolam were 11."( Relationship between single oral dose pharmacokinetics of alprazolam and triazolam.
Furukori, H; Hayashi, K; Kaneko, S; Nagasaki, T; Ohkubo, T; Otani, K; Sugawara, K; Tasaki, H; Yasui, N, 1997
)
0.74
"The effect of sertindole (a new selective antipsychotic compound) on the pharmacokinetic disposition of alprazolam was investigated."( Lack of multiple dosing effect of sertindole on the pharmacokinetics of alprazolam in healthy volunteers.
Granneman, GR; Locke, C; Staser, J; Wong, SL, 1998
)
0.75
"54 ml/min/kg) and shortened the elimination half-life (17."( Effect of carbamazepine on the single oral dose pharmacokinetics of alprazolam.
Furukori, H; Kaneko, S; Kondo, T; Nagasaki, T; Ohkubo, T; Otani, K; Shimoyama, R; Sugawara, K; Yasui, N, 1998
)
0.54
" There were modest increases in alprazolam plasma concentration in the elderly compared to the younger group shortly after drug administration, but there was no evidence of increased sensitivity to the pharmacodynamic effects of alprazolam in the elderly."( Single-dose pharmacokinetics and pharmacodynamics of alprazolam in elderly and young subjects.
Ehrenberg, BL; Goddard, JE; Greenblatt, DJ; Harmatz, JS; Kaplan, GB; Shader, RI, 1998
)
0.83
"Potential pharmacokinetic effects of venlafaxine on alprazolam, a substrate of the cytochrome pigment 450 (CYP) isoenzyme CYP3A4, were investigated in 16 healthy volunteers."( Effect of venlafaxine on the pharmacokinetics of alprazolam.
Albano, D; Amchin, J; Klockowski, PM; Taylor, KP; Zarycranski, W, 1998
)
0.81
" Plasma concentrations and pharmacodynamic parameters were measured after each dose."( Ketoconazole inhibition of triazolam and alprazolam clearance: differential kinetic and dynamic consequences.
Corbett, K; Counihan, M; Ehrenberg, BL; Greenblatt, DJ; Harmatz, JS; Harrel, LM; Shader, RI; Tobias, S; von Moltke, LL; Wright, CE, 1998
)
0.57
"002) and apparent elimination half-life (t1/2) prolonged (59 versus 15 hours; P < ."( Ketoconazole inhibition of triazolam and alprazolam clearance: differential kinetic and dynamic consequences.
Corbett, K; Counihan, M; Ehrenberg, BL; Greenblatt, DJ; Harmatz, JS; Harrel, LM; Shader, RI; Tobias, S; von Moltke, LL; Wright, CE, 1998
)
0.57
"10 ml/min per kg) and prolonged the elimination half-life (15."( Effect of itraconazole on the single oral dose pharmacokinetics and pharmacodynamics of alprazolam.
Furukori, H; Kaneko, S; Kondo, T; Nagasaki, T; Ohkubo, T; Otani, K; Sugawara, K; Yasui, N, 1998
)
0.52
" No pharmacokinetic differences were observed between the two menstrual cycle-phase drug administrations."( Influence of endogenous progesterone on alprazolam pharmacodynamics.
Friedman, CI; McAuley, JW, 1999
)
0.57
" The Medline electronic database from 1966 through 1998 was used to identify clinical studies of the pharmacokinetic effect of drugs on these three benzodiazepines."( Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam, and triazolam.
Balian, JD; Flockhart, DA; Yuan, R, 1999
)
0.52
"A healthy 40-year-old Caucasian male volunteer displayed unusually low clearance and long elimination half-life of alprazolam and trazodone, two CYP3A substrate drugs, following single-dose oral administration in clinical pharmacokinetic studies."( Unusually low clearance of two CYP3A substrates, alprazolam and trazodone, in a volunteer subject with wild-type CYP3A4 promoter region.
Cotreau, MM; Greenblatt, DJ; Tran, TH; von Moltke, LL, 2000
)
0.77
" There were no differences in the pharmacodynamic measures of sedation and cognition or differences in pharmacokinetics between the two groups."( Differences in pharmacodynamics but not pharmacokinetics between subjects with panic disorder and healthy subjects after treatment with a single dose of alprazolam.
Ehrenberg, BL; Goddard, JE; Greenblatt, DJ; Harmatz, JS; Kaplan, GB; Shader, RI, 2000
)
0.51
" Grapefruit juice altered neither the plasma concentrations of alprazolam at any time points, any pharmacokinetic parameters, nor the majority of psychomotor function parameters in subjects."( Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam.
Furukori, H; Kaneko, S; Kondo, T; Ohkubo, T; Osanai, T; Otani, K; Sugawara, K; Uno, T; Yasui, N, 2000
)
0.75
"Mean (+/-SD) values of peak plasma concentration (Cmax), time to Cmax (tmax), area under the plasma concentration-time curve [AUC(0-48)] and elimination half-life (tl/2) of alprazolam were 12."( No correlations between the urinary ratio of 6beta-hydroxycortisol to free cortisol and pharmacokinetics of alprazolam.
Chiba, K; Kaneko, S; Kondo, T; Kubota, T; Nagasaki, T; Ohkubo, T; Otake, H; Otani, K; Sugawara, K; Yasui-Furukori, N, 2001
)
0.72
" Building on the existing in vitro and in vivo evidence that suggest a minimal effect of citalopram on cytochrome P450 3A4, we hypothesized that therapeutic doses of citalopram (20 mg/d), as compared with fluoxetine (20 mg/d), would cause less impairment in the metabolism of the probe drug alprazolam (1 mg) through inhibition of the cytochrome P450 3A4 isozyme as measured by pharmacokinetic and pharmacodynamic parameters in vivo."( Pharmacokinetic and pharmacodynamic evaluation of the inhibition of alprazolam by citalopram and fluoxetine.
Hall, J; Herrmann, N; Naranjo, CA; Sproule, BA, 2003
)
0.73
" 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
"(1) To determine the pharmacokinetic parameters of alprazolam and its two metabolites in plasma from healthy volunteers; (2) to identify a suitable single time point to take a plasma sample for CYP3A phenotyping."( Alprazolam as a probe for CYP3A using a single blood sample: pharmacokinetics of parent drug, and of alpha- and 4-hydroxy metabolites in healthy subjects.
Allqvist, A; Bertilsson, L; Gustafsson, LL; Mirghani, RA; Svensson, JO; Wennerholm, A, 2005
)
2.02
" The ratios of estimated geometric means for AUC(0-infinity) and Cmax between adolescents and adults for both dose levels were 115% (95% CI: [93, 143]) and 111% (95% CI: [95, 129]), respectively."( Pharmacokinetics of an extended release formulation of alprazolam (Xanax XR) in healthy normal adolescent and adult volunteers.
Fang, A; Gandelman, K; Glue, P; Klee, B,
)
0.38
" 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
" 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
"Focusing on the genetic similarity of CYP3A subfamily enzymes (CYP3A4 and CYP3A5) between monkeys and humans, we have attempted to provide a single-species approach to predicting human hepatic clearance (CLh) of CYP3A4 substrates using pharmacokinetic parameters in cynomolgus monkeys following intravenous administrations."( A new approach to predicting human hepatic clearance of CYP3A4 substrates using monkey pharmacokinetic data.
Houjo, T; Ishigai, M; Kato, M; Ogawa, K, 2013
)
0.39
" In vitro half-life for disappearance of each compound was converted to hepatic clearance using the well stirred model, with and without correction for plasma protein binding."( Meeting the challenge of predicting hepatic clearance of compounds slowly metabolized by cytochrome P450 using a novel hepatocyte model, HepatoPac.
Chan, TS; Kehtani, SR; Khetani, SR; Moore, A; Tweedie, D; Yu, H, 2013
)
0.39
"The aim of the study was to assess the magnitude of the CYP3A4 inhibitory effect of 2 dosing regimens of ketoconazole and the influence of the pharmacokinetic properties of the CYP3A4 substrate on the extent of the substrate exposure increase."( CYP3A4-based drug-drug interaction: CYP3A4 substrates' pharmacokinetic properties and ketoconazole dose regimen effect.
Boulenc, X; Donazzolo, Y; Hermabessière, S; Martin, V; Nicolas, O; Ollier, C; Zobouyan, I, 2016
)
0.43
"The objective of this study was to evaluate the pharmacokinetic properties and physiologic effects of a single oral dose of alprazolam in horses."( Pharmacokinetics and physiologic effects of alprazolam after a single oral dose in healthy mares.
Alcott, CJ; Coetzee, JF; Davis, JL; Galow-Kersh, NL; Hepworth-Warren, KL; Rice, S; Wong, DM, 2015
)
0.88
" To validate the pharmacodynamic biomarkers for GABA-ergic anxiolytics, this study determined the pharmacodynamics of two anxiolytics and a nonanxiolytic control, and linked them to their anxiolytic and sedative effects, during an anxiety-challenge study day."( Pharmacodynamic response profiles of anxiolytic and sedative drugs.
Baas, J; Broeyer, F; Chen, X; Cohen, A; de Kam, M; van Gerven, J, 2017
)
0.46
" Thus, the potential influence of anxiety on CNS pharmacodynamic markers could be examined."( Pharmacodynamic response profiles of anxiolytic and sedative drugs.
Baas, J; Broeyer, F; Chen, X; Cohen, A; de Kam, M; van Gerven, J, 2017
)
0.46
" The objective of this study was to develop and evaluate a physiologically based pharmacokinetic (PBPK) model for hyperforin (the constituent of SJW responsible for interactions), which has the potential to provide unique insights into SJW interactions and allow prediction of the likely extent of interactions with SJW compared to published interaction reports."( Physiologically Based Pharmacokinetic Modelling of Hyperforin to Predict Drug Interactions with St John's Wort.
Adiwidjaja, J; Boddy, AV; McLachlan, AJ, 2019
)
0.51
" In this study, the association between NAS and plasma alprazolam concentration was examined using the measured neonatal concentrations in the time series as well as simulated plasma concentrations of pregnant woman and neonate by physiologically based pharmacokinetic (PBPK) modeling."( Pharmacokinetic assessment of alprazolam-induced neonatal abstinence syndrome using physiologically based pharmacokinetic model.
Fujioka, K; Fukushima, S; Hashimoto, M; Iijima, K; Mishima, Y; Yamakawa, K; Yamamoto, K; Yano, I, 2019
)
1.05
" A physiologically based pharmacokinetic (PBPK) model that implements the age-dependent size growth and ontogeny of organ functions can be used to predict the concentration-time profiles of drugs in the pediatric population."( Feasibility of physiologically based pharmacokinetic simulations for assessing pediatric patients after accidental drug ingestion: A case study of a 1.4-year-old girl who ingested alprazolam.
Emoto, C; Shimizu, M; Tanaka, T; Yamazaki, H, 2021
)
0.81
" Twelve male, Sprague-Dawley rats were given a 2 mg/kg subcutaneous dose of alprazolam, flualprazolam and flubromazolam and plasma pharmacokinetic parameters were evaluated."( Designer benzodiazepine rat pharmacokinetics: A comparison of alprazolam, flualprazolam and flubromazolam.
Canfield, JR; Kisor, DF; Sprague, JE, 2023
)
1.38
" This study utilized physiologically based pharmacokinetic (PK) and pharmacodynamic (PD) modelling to further examine the underlying mechanisms of anxiety treatment and addiction."( Physiologically based pharmacokinetic and pharmacodynamic modelling of alprazolam: Implications for anxiety and addiction.
Burkat, PM, 2023
)
1.14
" With repetitive administrations, peak concentration is 59 nM for a 2-mg alprazolam immediate-release dose and 122 nM for a 10-mg extended-release dose."( Physiologically based pharmacokinetic and pharmacodynamic modelling of alprazolam: Implications for anxiety and addiction.
Burkat, PM, 2023
)
1.37

Compound-Compound Interactions

Alprazolam, alone and in combination with ethanol, on psychomotor and cognitive performance were studied in healthy male volunteers. Olanzapine (orally disintegrating tablets) was used successfully to relieve this terminally ill patient's anxiety and tension.

ExcerptReferenceRelevance
"Effects of alprazolam, alone and in combination with ethanol, on psychomotor and cognitive performance were studied in healthy male volunteers and compared to effects of diazepam."( Effects of single doses of alprazolam and diazepam, alone and in combination with ethanol, on psychomotor and cognitive performance and on autonomic nervous system reactivity in healthy volunteers.
Eckardt, MJ; Granger, A; Lane, E; Linnoila, M; Lister, R; Moss, H; Stapleton, JM, 1990
)
0.97
" Although the simple screen suggests the presence of the drug-drug interaction, limited information regarding pharmacokinetic parameters is available and those parameters that can be estimated are biased."( An evaluation of population pharmacokinetics in therapeutic trials. Part II. Detection of a drug-drug interaction.
Antal, EJ; Ereshefsky, L; Evans, RL; Grasela, TH; Smith, RB; Wells, BG, 1987
)
0.27
"5 mg/70 kg), and placebo, alone and in combination with ethanol (0-0."( Acute participant-rated and behavioral effects of alprazolam and buspirone, alone and in combination with ethanol, in normal volunteers.
Griffiths, RR; Rush, CR, 1997
)
0.55
" In the present study, the effect of gabapentin (GBP) on seizure score and memory is evaluated when it is given alone and in combination with some antidepressants, such as sertraline (SERTR) and alprazolam (ALP)."( Effects of gabapentin and antidepressant drug combinations on convulsions and memory in mice.
Ali, A; Dua, Y; Pal, SN; Pillai, KK; Rizwan, AN,
)
0.32
" Olanzapine (orally disintegrating tablets) in combination with alprazolam was used successfully to relieve this terminally ill patient's anxiety and tension improving his relationship with his physicians and his daily life."( Sublingual use of olanzapine in combination with alprazolam to treat agitation in a terminally ill patient receiving parenteral nutrition.
Douzenis, A; Economopoulos, T; Lykouras, L; Michopoulos, I; Soldatos, CR, 2007
)
0.83

Bioavailability

More than 90% of alprazolam is absorbed after an oral dose. The absorption rate is dose independent. Absolute bioavailability of oral alpazolam averages 80 to 100%.

ExcerptReferenceRelevance
" More than 90% of alprazolam is absorbed after an oral dose; the absorption rate is dose independent."( The pharmacology of alprazolam: a review.
Huybrechts, I,
)
0.79
" The rate of absorption of alprazolam was slower in patients with alcoholic liver disease."( Alprazolam pharmacokinetics in alcoholic liver disease.
Dittert, LW; Juhl, RP; Smith, RB; Van Thiel, DH,
)
1.87
" Absolute bioavailability of oral alprazolam averages 80 to 100%."( Clinical pharmacokinetics of alprazolam. Therapeutic implications.
Greenblatt, DJ; Wright, CE, 1993
)
0.86
"NONMEM was applied to single dose and multiple dose bioavailability data for an immediate release (IR) and a controlled release (CR) dosage form of alprazolam to acquire additional information from the data which are not easily obtainable by traditional means."( Nonlinear mixed effects modeling of single dose and multiple dose data for an immediate release (IR) and a controlled release (CR) dosage form of alprazolam.
Baweja, R; Hossain, M; Ludden, T; Miller, R; Wright, E, 1997
)
0.7
" Including a lag time, two different rates of absorption (KAIR and KACR), and bioavailability for the CR relative to the IR dosage form significantly improved the fit of the model to the data."( Nonlinear mixed effects modeling of single dose and multiple dose data for an immediate release (IR) and a controlled release (CR) dosage form of alprazolam.
Baweja, R; Hossain, M; Ludden, T; Miller, R; Wright, E, 1997
)
0.5
" An absorption model incorporating a delay site is proposed to describe the data, and the absolute oral bioavailability is estimated to be about 30%."( A double-peak phenomenon in the pharmacokinetics of alprazolam after oral administration.
Lau, CE; Roy, A; Sun, L; Wang, Y, 1999
)
0.55
"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
" Absorption of the thermal aerosol is nearly complete, with >80% absolute bioavailability found in both dogs and human normal volunteers."( Ultra-fast absorption of amorphous pure drug aerosols via deep lung inhalation.
Cassella, JV; Cross, S; Damani, R; Lloyd, PM; Munzar, P; Myers, DJ; Quintana, R; Rabinowitz, JD; Soni, P; Spyker, DA, 2006
)
0.33
"To evaluate the effect of a standardized meal on the bioavailability of alprazolam formulated as an immediate-release orally disintegrating tablet (ODT) in healthy volunteers."( Absence of food effect on the extent of alprazolam absorption from an orally disintegrating tablet.
Combs, M; Erdman, K; Pollock, S; Stiles, M; Stypinski, D; Witt, P, 2007
)
0.84
"Oral administration of alprazolam generated the irregular gastric emptying profiles, resulting in multiple peaks in the absorption rate profiles of both drugs."( Appearance of double peaks in plasma concentration-time profile after oral administration depends on gastric emptying profile and weight function.
Higaki, K; Kimura, T; Metsugi, Y; Miyaji, Y; Ogawara, K, 2008
)
0.66
"Analysis of human EEG constitutes a useful instrument for the evaluation of drug bioavailability at the brain."( Connectivity analysis of EEG under drug therapy.
Alonso, JF; Barbanoj, MJ; Hoyer, D; Mañanas, MA; Riba, J; Romero, S, 2007
)
0.34
"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
"Quantitative analysis of electroencephalographic signals (EEG) and their interpretation constitute a helpful tool in the assessment of the bioavailability of psychoactive drugs in the brain."( Cross-conditional entropy and coherence analysis of pharmaco-EEG changes induced by alprazolam.
Alonso, JF; Mañanas, MA; Riba, J; Rojas-Martínez, M; Romero, S, 2012
)
0.6
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
"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

Dosage Studied

Seven adult female horses received an oral administration of alprazolam at a dosage of 0.5 mg. No significant effects of the low and middle doses of suriclone on N1 amplitude were observed. The highest dosage reduced N1 amplitudes to an even greater extent.

ExcerptRelevanceReference
"Ninety-six patients with panic disorder and agoraphobia were treated at three sites in a 6-week, fixed-dose, double-blind, placebo-controlled, dose-response study of 2 mg/day or 6 mg/day of alprazolam."( Alprazolam plasma concentrations and treatment response in panic disorder and agoraphobia.
Antal, E; Ballenger, JC; DuPont, R; Lesser, IM; Lydiard, RB; Rubin, RT, 1992
)
1.92
" The majority (67%) of patients interviewed discontinued alprazolam for a period of at least 3 days after a gradual dosage reduction schedule over a 4-week period at the end of the long-term treatment study."( Discontinuation of alprazolam after long-term treatment of panic-related disorders.
Ballenger, JC; Burrows, GD; DuPont, RL; Noyes, R; Pecknold, JC; Rifkin, A; Rubin, RT; Swinson, RP, 1992
)
0.86
" Peak plasma concentrations were reached later after sublingual than oral dosage (2."( The pharmacokinetics and pharmacodynamics of sublingual and oral alprazolam in the post-prandial state.
Friedman, H; Goddard, JE; Greenblatt, DJ; Harmatz, JS; Scavone, JM; Shader, RI, 1992
)
0.52
" The results suggest that studies employing other benzodiazepines or other ALP dosage or taper schedules would be required to demonstrate any benefit for the IMI plus early benzodiazepine cotreatment strategy over IMI alone in the routine pharmacologic management of panic disorder."( Controlled trial of alprazolam supplementation during imipramine treatment of panic disorder.
Charney, DS; Heninger, GR; Koleszar, AS; Krystal, JH; Nagy, LM; Woods, SW, 1992
)
0.61
" Flexible dosage at therapeutic levels resulted in increased heart rate and blood pressure and in decreased cardiac vagal control in patients receiving imipramine but not alprazolam or placebo."( Effects of alprazolam and imipramine on parasympathetic cardiac control in patients with generalized anxiety disorder.
Hoehn-Saric, R; McLeod, DR; Porges, SW; Zimmerli, WD, 1992
)
0.87
" Comparison of the dose-response curves demonstrated a difference in the intensity of the stimulus effects."( The discriminative stimulus effects of diazepam in rats at two training doses.
Franklin, SR; Tang, AH, 1991
)
0.28
" Use of dosage ratios analogous to those used in humans may lead to results that cannot be extrapolated to humans."( Comparative pharmacokinetics of alprazolam and lorazepam in humans and in African Green Monkeys.
Friedman, H; Greenblatt, DJ; Redmond, DE, 1991
)
0.56
" Clonazepam, with its relatively long half-life, permits less frequent dosing than possible with benzodiazepines with shorter half-lives and more continuous control of anxiety, although around 20% of patients experience unacceptable sedative effects or no reduction in anxiety."( High-potency benzodiazepines for short-term management of panic disorder: the U.S. experience.
Tesar, GE, 1990
)
0.28
" Steady-state alprazolam clearance during multiple dosing with lithium was not different from that with the single dose of alprazolam."( Evaluation of the interaction of lithium and alprazolam.
Evans, RL; Hornstra, RK; Melethil, S; Nelson, MV; Smith, RB; Townsend, R, 1990
)
0.9
" A 1 mg dosage increment produced, on the average, a corresponding 10 ng/ml increase in steady state level of the parent drug."( The relationship of alprazolam dose to steady-state plasma concentrations.
Antal, EJ; Ciraulo, DA; Goldberg, DA; Greenblatt, DJ; Olson, DR; Phillips, JP; Rand, EH; Raskin, RB; Shader, RI; Smith, RB, 1990
)
0.6
" In explanted rat hypothalami maintained viable in vitro, PAF stimulated immunoreactive CRH secretion in a bell-shaped dose-response fashion."( The alkyl-ether phospholipid platelet-activating factor is a stimulator of the hypothalamic-pituitary-adrenal axis in the rat.
Bernardini, R; Brucke, T; Calogero, AE; Chrousos, GP; Ehrlich, YH; Gold, PW, 1989
)
0.28
" To determine the effects of chronic dosage in mice, alprazolam (2 mg/kg/day) was administered via osmotic pumps for 1-14 days, and open-field activity, plasma and brain concentrations, benzodiazepine receptor binding in vivo and in vitro, [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding, and muscimol-stimulated chloride uptake were determined."( Chronic benzodiazepine administration. IV. Rapid development of tolerance and receptor downregulation associated with alprazolam administration.
Greenblatt, DJ; Lopez, F; Miller, LG; Roy, RB; Shader, RI; Woolverton, S, 1989
)
0.74
" In the first study modifications to the protocol and case report forms were employed to allow for the prospective collection of accurate dosing and blood sampling time data."( An evaluation of population pharmacokinetics in therapeutic trials. Part III. Prospective data collection versus retrospective data assembly.
Antal, EJ; Grasela, TH; Smith, RB, 1989
)
0.28
" It appeared, however, as if tolerance was more pronounced to the ataxic/sedative effects (approximately a four-fold rightward shift of the dose-response curve) than to the anticonflict effect (approximately a two-fold shift) of APZ, whereas tolerance developed to about the same extent to the two effects of DIZ (approximately two-fold shifts)."( Anticonflict and rotarod impairing effects of alprazolam and diazepam in rat after acute and subchronic administration.
Engel, JA; Eriksson, E; Söderpalm, B, 1989
)
0.54
" Pharmacokinetic parameters for the SR doses were consistent with linear kinetics over the dosage range studied."( Pharmacokinetics and pharmacodynamics of alprazolam following single and multiple oral doses of a sustained-release formulation.
Eller, MG; Fleishaker, JC; Phillips, JP; Smith, RB, 1989
)
0.54
" Treatment failures most often result from an inadequate medication trial (ie, trial too brief or dosage inadequate); with adequate treatment most patients with panic disorder can be helped."( Panic disorder: diagnosis and treatment.
O'Boyle, M, 1989
)
0.28
" All antagonists produced a shift to the right in the dose-response curve to Paf (0."( Antagonism of platelet activating factor-induced chemiluminescence in guinea-pig peritoneal macrophages in differing states of activation.
Bittner, C; Lambrecht, G; Parnham, MJ, 1989
)
0.28
"A case is presented in which a 68-year-old man became delirious after being withdrawn from a low dosage of alprazolam."( Alprazolam withdrawal delirium unresponsive to diazepam: case report.
Baker, RW; Zimmer, B; Zipursky, RB, 1985
)
1.93
" It is suggested that the combined treatment cimetidine-alprazolam requires a reduced daily dosage (one third) of alprazolam or increased dosage intervals (b."( Pharmacokinetic consequences of long term coadministration of cimetidine and triazolobenzodiazepines, alprazolam and triazolam, in healthy subjects.
Desager, JP; Harvengt, C; Hulhoven, R; Pourbaix, S; Smith, RB, 1985
)
0.73
" Careful diagnostic inquiry, individual titration of doses, and use of conservative dosage schedules (with interrupted periods of treatment) will permit pharmacotherapy with maximum benefit and a minimum of adverse consequences."( Pharmacotherapeutic considerations in anxiety disorders.
Hollister, LE, 1986
)
0.27
" The inhibition was shown to be specific and competitive with PAF on its receptor by the following observations: parallel shift of the dose-response curve; crossing of double reciprocal plots on the intersection of the ordinate; and no inhibition on other autacoids such as bradykinin, histamine, 5-hydroxytryptamine and LTC4."( Characterization of the activity of a platelet activating factor antagonist, CV-3988.
Hayashi, M; Kimura, J; Nomura, H; Oh-Ishi, S; Tsushima, S, 1987
)
0.27
" Eighty-two percent (39) of the patients rated clonazepam as being "better" than alprazolam due to decreased dosing frequency and lack of interdose anxiety."( Rebound anxiety in panic disorder patients treated with shorter-acting benzodiazepines.
Brotman, AW; Herman, JB; Rosenbaum, JF, 1987
)
0.5
" In a 6-week, double-blind, parallel-design study with flexible dosage scheduling, the authors compared the effects of alprazolam with those of imipramine in 60 patients who had generalized anxiety disorder."( Differential effects of alprazolam and imipramine in generalized anxiety disorder: somatic versus psychic symptoms.
Hoehn-Saric, R; McLeod, DR; Zimmerli, WD, 1988
)
0.79
" Since tolerance develops to these effects, the advantage of more frequent dosing regimen dissipates by the 4th day."( Influence of dosing regimen on alprazolam and metabolite serum concentrations and tolerance to sedative and psychomotor effects.
Kroboth, PD; Smith, RB, 1987
)
0.56
"25 mg or placebo was administered three times daily from cycle day 20 until the second day of menstruation, at which time the dosage was tapered by one tablet per day to minimize withdrawal effects."( Treatment of premenstrual syndrome with alprazolam: results of a double-blind, placebo-controlled, randomized crossover clinical trial.
Rinehart, JS; Ruddock, VE; Schiff, I; Smith, S, 1987
)
0.54
" The possibility of fading of therapeutic effects of alprazolam (defined as a progressive decrease of therapeutic effects refractory to dosage increase, after non-immediate symptomatic improvement) in such cases is discussed."( Fading of therapeutic effects of alprazolam in agoraphobia. Case reports.
Fava, GA, 1988
)
0.81
" Despite tapering of the daily dosage according to manufacturer guidelines, a withdrawal syndrome was precipitated in three of the cases."( A review of alprazolam withdrawal.
Browne, JL; Hauge, KJ, 1986
)
0.65
" Results suggest that individuals who take benzodiazepines will perform less well on an anterograde memory delayed recall task completed after dosing on the sixth day of treatment, but no similar difference will be found in performance on a similar task completed just before dosing on the sixth day."( Anxiolytics and memory: a comparison of lorazepam and alprazolam.
Gabrielli, WF; Goodwin, DW; Kumar, R; Mac, DS, 1987
)
0.52
" The peak plasma concentration after sublingual dosage was higher than after oral administration (17."( Alprazolam kinetics following sublingual and oral administration.
Greenblatt, DJ; Scavone, JM; Shader, RI, 1987
)
1.72
" Subsequent administration of an equivalent dosage of lorazepam did not induce manic symptoms."( A case of alprazolam, but not lorazepam, inducing manic symptoms.
Charney, DS; Goodman, WK, 1987
)
0.68
" The daily dosage ceiling was increased to 10 mg."( Some biochemical correlates of panic attacks with agoraphobia and their response to a new treatment.
Coleman, JH; Greenblatt, DJ; Jones, KJ; Levine, PH; Orsulak, PJ; Peterson, M; Schildkraut, JJ; Sheehan, DV; Uzogara, E; Watkins, D, 1984
)
0.27
" During long term administration alprazolam should therefore take longer to reach steady-state concentrations in obese patients but the final levels achieved should be no different than for patients of normal bodyweight, provided dosage is adjusted for ideal rather than total bodyweight."( The influence of obesity on the pharmacokinetics of oral alprazolam and triazolam.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI; Smith, RB,
)
0.66
" Alprazolam plasma concentration in multiple samples during 36 h after dosing was determined by electron-capture gas-liquid chromatography."( Pharmacokinetics and pharmacodynamics of alprazolam after oral and IV administration.
Juhl, RP; Kroboth, PD; Phillips, JP; Smith, RB; Vanderlugt, JT, 1984
)
1.44
" From dose-response studies, it can be estimated that IDRA 21 is approximately 10-fold more potent than aniracetam in antagonizing alprazolam-induced learning deficit."( 7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide (IDRA 21), a congener of aniracetam, potently abates pharmacologically induced cognitive impairments in patas monkeys.
Costa, E; DiBella, M; Guidotti, A; Thompson, DM, 1995
)
0.5
"Randomized, double-blind, placebo-controlled 3-month parallel treatment arms with flexible dosage and with the length of clinical contact randomized within each treatment group."( A double-blind trial of oral progesterone, alprazolam, and placebo in treatment of severe premenstrual syndrome.
Freeman, EW; Polansky, M; Rickels, K; Sondheimer, SJ, 1995
)
0.55
" The aim of the XR preparation is to offer less frequent dosing and to reduce interdose anxiety."( A double-blind, placebo-controlled, multicenter study with alprazolam and extended-release alprazolam in the treatment of panic disorder.
Alexander, P; Luthe, L; Munjack, D; Pecknold, J, 1994
)
0.53
" No dose-response relationships were evident for plasma ACTH and norepinephrine."( Dose-dependent effects of intravenous alprazolam on neuroendocrine, biochemical, cardiovascular, and behavioral parameters in humans.
Hsiao, JK; Osman, OT; Potter, WZ, 1993
)
0.56
" Important issues such as selection of an appropriate comparison drug, selection of an appropriate population, dosing regimen and test doses need to be considered in future studies."( Abuse liability of alprazolam relative to other commonly used benzodiazepines: a review.
Bickel, WK; Higgins, ST; Hughes, JR; Rush, CR, 1993
)
0.61
" The dosage of alprazolam should be reduced during co-administration with fluvoxamine."( A pharmacokinetic and pharmacodynamic evaluation of the combined administration of alprazolam and fluvoxamine.
Fleishaker, JC; Hulst, LK, 1994
)
0.87
" In each dosage group, three patients were older than and three were younger than 65 years of age."( Age-related digoxin-alprazolam interaction.
Cavdar, C; Fowler, J; Guneri, S; Guven, H; Tuncok, Y, 1993
)
0.61
" Regulation of the prescribed dosage of alprazolam is important since individuals differ considerably in sensitivity to this medication."( Use of alprazolam for relief of tinnitus. A double-blind study.
Brummett, R; Johnson, RM; Schleuning, A, 1993
)
1.01
"5 years, 78% of patients remained on medication and the mean dosage of alprazolam and clonazepam did not increase."( Long-term outcome after acute treatment with alprazolam or clonazepam for panic disorder.
Cohen, LS; Meltzer-Brody, S; Otto, MW; Pollack, MH; Rosenbaum, JF; Tesar, GE, 1993
)
0.78
" On average, mean steady-state plasma alprazolam concentrations change by 10 to 12 micrograms/L for each daily dosage change of 1 mg/day."( Clinical pharmacokinetics of alprazolam. Therapeutic implications.
Greenblatt, DJ; Wright, CE, 1993
)
0.85
"Long-term, nightly benzodiazepine treatment of injurious parasomnias and other disorders of disrupted nocturnal sleep resulted in sustained efficacy in most cases, with low risk of dosage tolerance, adverse effects, or abuse."( Long-term, nightly benzodiazepine treatment of injurious parasomnias and other disorders of disrupted nocturnal sleep in 170 adults.
Mahowald, MW; Schenck, CH, 1996
)
0.29
" Compared to placebo, no significant effects of the low and middle doses of suriclone on N1 amplitude were observed; the highest dosage reduced N1 amplitude, as did 1 mg alprazolam to an even greater extent."( Acute effects of the anxiolytics suriclone and alprazolam on cognitive information processing utilizing topographic mapping of event-related brain potentials (P300) in healthy subjects.
Anderer, P; Saletu, B; Semlitsch, HV, 1995
)
0.74
" Serial blood samples were collected after dosing on day 1 and day 7 and before the morning dose on days 4, 5, and 6 for the determination of alprazolam and its metabolites alpha-hydroxyalprazolam (AOH) and 4-hydroxyalprazolam (4OH) and nefazodone and its metabolites hydroxynefazodone (HO-nefazodone), m-chlorophenylpiperazine (mCPP), and a triazole dione metabolite (dione) by validated high-performance liquid chromatography methods."( Coadministration of nefazodone and benzodiazepines: III. A pharmacokinetic interaction study with alprazolam.
Barbhaiya, RH; Dockens, RC; Greene, DS; Kroboth, P; Salazar, DE, 1995
)
0.71
" Chronic oral dosing (every 2nd day) with triazolam (0."( Tolerance to the anxiolytic effects of the triazolobenzodiazepines triazolam and alprazolam, as measured by the ingestion of a hypertonic sodium chloride solution in rats.
Barbarito, EJ; Falk, JL; Lau, CE, 1996
)
0.52
" Data from 6 of 12 subjects in this study were evaluable because of a dosing error in the other 6 subjects."( Coadministration of nefazodone and benzodiazepines: I. Pharmacodynamic assessment.
Barbhaiya, R; Chaikin, PC; Folan, MM; Kroboth, PD; Lush, RM; Salazar, DE; Shukla, UA, 1995
)
0.29
" The dose-response curve (DRC) method of Pöch permitted an extensive evaluation of the kind (additivity or independence) of interactions occurring in combined drug effects."( Alprazolam, caffeine and their interaction: relating DRL performance to pharmacokinetics.
Lau, CE; Wang, J, 1996
)
1.74
" Intrathecally administered alprazolam produced a dose-response increase in the tailflick latency with an ED50 of 34 microg (19."( Antinociceptive interaction between alprazolam and opioids.
Pick, CG, 1997
)
0.87
"NONMEM was applied to single dose and multiple dose bioavailability data for an immediate release (IR) and a controlled release (CR) dosage form of alprazolam to acquire additional information from the data which are not easily obtainable by traditional means."( Nonlinear mixed effects modeling of single dose and multiple dose data for an immediate release (IR) and a controlled release (CR) dosage form of alprazolam.
Baweja, R; Hossain, M; Ludden, T; Miller, R; Wright, E, 1997
)
0.7
" Including a lag time, two different rates of absorption (KAIR and KACR), and bioavailability for the CR relative to the IR dosage form significantly improved the fit of the model to the data."( Nonlinear mixed effects modeling of single dose and multiple dose data for an immediate release (IR) and a controlled release (CR) dosage form of alprazolam.
Baweja, R; Hossain, M; Ludden, T; Miller, R; Wright, E, 1997
)
0.5
" The dissimilarity in dose-response curve of WAY-100635 on punished and unpunished behaviour poses questions about the mediation of these effects."( Effects of 5-HT1A receptor ligands in a modified Geller-Seifter conflict model in the rat.
Gommans, J; Hijzen, TH; Joordens, RJ; King, CM; Maes, RA; Olivier, B, 1997
)
0.3
" The interaction was PK linked and mainly not distinguishable from independence as indicated by the Poch dose-response curve method and the integration of PK and pharmacodynamics."( Differential reinforcement of low rate performance, pharmacokinetics and pharmacokinetic-pharmacodynamic modeling: independent interaction of alprazolam and caffeine.
Falk, JL; Lau, CE; Wang, Y, 1997
)
0.5
" Blood samplings were performed up to 48 h after alprazolam dosing and up to 12 h after triazolam dosing."( Relationship between single oral dose pharmacokinetics of alprazolam and triazolam.
Furukori, H; Hayashi, K; Kaneko, S; Nagasaki, T; Ohkubo, T; Otani, K; Sugawara, K; Tasaki, H; Yasui, N, 1997
)
0.8
" Acute alprazolam and caffeine dose-response curves (DRCs) were characterized and were then used to determine the maintenance dose for the respective chronic dose regimens."( Independent interaction of alprazolam and caffeine under chronic dose regimens on differential reinforcement of low-rate (DRL 45-s) performance.
Falk, JL; Lau, CE; Wang, Y, 1997
)
1.05
" During the second 2 weeks, they all took the same dosage of the extended release formulation."( Medication side effects in anxious patients: negative placebo responses?
Alexander, PE; Coleman, BS; Dempsey, GM; Jones, W; Swiontek, AM; Uhlenhuth, EH, 1998
)
0.3
" The percentage of reduction of benzodiazepine daily dosage at all time points in the treatment trial was similar for the ondansetron and placebo groups."( A controlled trial of ondansetron, a 5-HT3 antagonist, in benzodiazepine discontinuation.
Busto, UE; Kaplan, HL; Romach, MK; Sellers, EM; Somer, G, 1998
)
0.3
"The stability of five drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied."( Stability of alprazolam, chloroquine phosphate, cisapride, enalapril maleate, and hydralazine hydrochloride in extemporaneously compounded oral liquids.
Allen, LV; Erickson, MA, 1998
)
0.67
" A secondary goal was to determine the accuracy of Drug Recognition Examiners (DREs) in detecting if subjects were dosed with these drugs."( Laboratory validation study of drug evaluation and classification program: alprazolam, d-amphetamine, codeine, and marijuana.
Crouch, DJ; Heishman, SJ; Singleton, EG, 1998
)
0.53
" In each of the 4 control visits, efficacy (HAMA, GCI, GCI improvement) and tolerability (adverse events) were assessed, as well as the dose, dosage pattern and need of change of the medication."( [Clinical use of sustained release of alprazolam: A naturalistic study].
De La Gándara Martín, JJ; Sanz Granado, O; Such, P; Varona Martínez, A,
)
0.4
" Fifty-eight percent (58%) of the patients needed a change in the dosage regimen (dose, number of daily doses), mostly due to clinical dose adjustment."( [Clinical use of sustained release of alprazolam: A naturalistic study].
De La Gándara Martín, JJ; Sanz Granado, O; Such, P; Varona Martínez, A,
)
0.4
" All three benzodiazepines were susceptible to drug interactions, but oral dosing of midazolam and triazolam resulted in greater alterations in the pharmacokinetic parameters than alprazolam due to their larger presystemic extraction."( Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam, and triazolam.
Balian, JD; Flockhart, DA; Yuan, R, 1999
)
0.72
" Plasma drug concentrations were monitored up to 48 h after alprazolam dosing together with evaluation of psychomotor function."( Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam.
Furukori, H; Kaneko, S; Kondo, T; Ohkubo, T; Osanai, T; Otani, K; Sugawara, K; Uno, T; Yasui, N, 2000
)
0.75
" For example, human terfenadine hepatic extraction goes from 95% in the absence of a competitive inhibitor to 35% in the presence of one (ketoconazole, 200 mg po Q 12 h dosed to steady-state)."( Cytochrome P450 3A4 in vivo ketoconazole competitive inhibition: determination of Ki and dangers associated with high clearance drugs in general.
Boxenbaum, H,
)
0.13
" These findings may also be of value in determining dosing routes for other benzodiazepines or psychotropic drugs."( A comparison of plasma alprazolam concentrations following different routes of chronic administration in the Sprague-Dawley rat: implications for psychotropic drug research.
Nemeroff, CB; Owens, MJ; Skelton, KH, 2000
)
0.62
" Additionally, ethanol caused less than a 2-fold shift to the left in the dose-response function of Co 2-6749 in the rotorod procedure in rats."( Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors.
Barrett, JE; Belluzzi, JD; Carter, RB; Hawkinson, JE; Lan, NC; Rosenzweig-Lipson, S; Stein, L; Vanover, KE; Wood, PL, 2000
)
0.31
" Neuropsychologic function after 6 weeks of therapy at the target dosage was compared with baseline assessments in each group."( Absence of neuropsychologic deficits in patients receiving long-term treatment with alprazolam-XR for panic disorder.
Auerbach, M; Gladsjo, JA; Hahn, T; Haze, A; Judd, LL; McKinney, R; Oliver, T; Rabin, A; Rapaport, MH, 2001
)
0.54
" Therefore, alprazolam may be safely coadministered with alosetron without the need for dosage adjustment."( Effect of alosetron on the pharmacokinetics of alprazolam.
D'Souza, DL; Koch, KM; Levasseur, LM; Nezamis, J; Robbins, DK; Simms, L, 2001
)
0.95
" Results demonstrated that alprazolam produced a leftward shift of the heroin dose-response curve in the conditioned place preference test."( Benzodiazepine modulation of opiate reward.
Ettenberg, A; Walker, BM, 2001
)
0.61
"Dogs received clomipramine at a dosage of 2 mg/kg (0."( Use of clomipramine, alprazolam, and behavior modification for treatment of storm phobia in dogs.
Crowell-Davis, SL; Curtis, TM; Parthasarathy, V; Seibert, LM; Sung, W, 2003
)
0.64
" The combination of alprazolam and varying doses of intravenous heroin resulted in a leftward shift of the heroin dose-response curve."( The effects of alprazolam on conditioned place preferences produced by intravenous heroin.
Ettenberg, A; Walker, BM, 2003
)
1
" After 14 days of St John's wort administration, participants were given the probe drugs along with 1 St John's wort tablet to establish postadministration CYP activity; the St John's wort dosing regimen was continued for 48 hours."( Effect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme.
Chavin, KD; DeVane, CL; Donovan, JL; Markowitz, JS; Ruan, Y; Taylor, RM; Wang, JS, 2003
)
0.32
" This suggests that long-term administration of St John's wort may result in diminished clinical effectiveness or increased dosage requirements for all CYP 3A4 substrates, which represent at least 50% of all marketed medications."( Effect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme.
Chavin, KD; DeVane, CL; Donovan, JL; Markowitz, JS; Ruan, Y; Taylor, RM; Wang, JS, 2003
)
0.32
" In addition, the once-daily dosing (as opposed to three or four times per day) reduces clock-watching, increases compliance and it eliminates the penalty of breakthrough anxiety and panic that many patients experience if they inadvertently miss a dose."( Alprazolam extended-release in panic disorder.
Rickels, K, 2004
)
1.77
"The present study was designed to demonstrate a dose-response relationship between acute alprazolam administration and human risk taking."( Acute effects of alprazolam on risky decision making in humans.
Cherek, DR; Lane, SD; Lieving, LM; Nouvion, S; Tcheremissine, OV, 2005
)
0.89
" They represent an improvement compared with transdermal delivery by patches because they offer more dosage flexibility, less irritation potential and a better cosmetic appearance."( Pharmaceutical development and clinical effectiveness of a novel gel technology for transdermal drug delivery.
Alberti, I; Carrara, DN; Grenier, A; Kraus, H, 2005
)
0.33
" Sprague-Dawley rats were implanted with guide cannula targeting the VTA, after which a heroin-induced CPP dose-response curve was determined (2."( Intra-ventral tegmental area heroin-induced place preferences in rats are potentiated by peripherally administered alprazolam.
Ettenberg, A; Walker, BM, 2005
)
0.54
" Based on the similar pharmacokinetic profiles, dosing of Xanax XR should be similar in adolescents and adults."( Pharmacokinetics of an extended release formulation of alprazolam (Xanax XR) in healthy normal adolescent and adult volunteers.
Fang, A; Gandelman, K; Glue, P; Klee, B,
)
0.38
"The objective of the current study was to develop a validated stability-indicating high-performance liquid chromatographic method for alprazolam and sertraline in combined dosage forms."( Development of a stability-indicating high-performance liquid chromatographic method for the simultaneous determination of alprazolam and sertraline in combined dosage forms.
Pathak, A; Rajput, SJ,
)
0.54
" A dose-response effect was evident for PGB that reached a plateau at a dose of 300 mg/d."( Comparative efficacy of pregabalin and benzodiazepines in treating the psychic and somatic symptoms of generalized anxiety disorder.
Feltner, DE; Herman, B; Lydiard, RB; Rickels, K, 2010
)
0.36
"Many different types of benzodiazepine medications exist to treat a wide array of psychological and physical diseases based on dosage and implications."( Cytogenetic activity of newly synthesized 1,5-benzodiazepines in normal human lymphocyte cultures.
Argyraki, M; Ekonomopoulou, MT; Iakovidou-Kritsi, Z; Polatoglou, E; Stephanidou-Stephanatou, J; Tsoleridis, CA, 2010
)
0.36
" If confirmed, this could have major implications for drug dosing in persistently inflamed patients."( Metabolism of alprazolam (a marker of CYP3A4) in hemodialysis patients with persistent inflammation.
Bertilsson, L; Carrero, JJ; Diczfalusy, U; Heimbürger, O; Lindholm, B; Molanaei, H; Odar-Cederlöf, I; Qureshi, AR; Stenvinkel, P, 2012
)
0.74
" Small sample sizes in many panic provocation studies, lack of dose-response aspects, and still-insufficient knowledge about the biological underpinning of experimental and spontaneous panic limit the interpretation of existing findings and should inspire further research."( Experimental panic provocation in healthy man-a translational role in anti-panic drug development?
Kellner, M, 2011
)
0.37
" Efficacy has been reported with both continuous dosing (all cycle) and intermittent or luteal phase dosing (from ovulation to menses)."( Psychotropic medications and other non-hormonal treatments for premenstrual disorders.
Pearlstein, T, 2012
)
0.38
"The present results support the continued evaluation of an opioid receptor antagonist combined with a GABAA-positive modulator using more clinically relevant experimental conditions like examining the effect of chronic dosing with these drugs on methamphetamine self-administration."( Separate and combined impact of acute naltrexone and alprazolam on subjective and physiological effects of oral d-amphetamine in stimulant users.
Lile, JA; Marks, KR; Rush, CR; Stoops, WW, 2014
)
0.65
" Their socio-demographic characteristics, family function characteristics, dosage of prescribed alprazolam, duration of alprazolam use, alcohol use pattern, pain reliever and cigarette use pattern, severity of depressive symptoms, psychiatric diagnosis, and belief toward alprazolam use were investigated."( Severity of alprazolam dependence and associated features among long-term alprazolam users from psychiatric outpatient clinics in Taiwan.
Chen, ST; Chen, TT; Hwang, TJ; Ko, CH; Lin, JJ; Su, PW; Yen, CF; Yen, CN, 2015
)
1.01
", liking and good effects), inhaled alprazolam was more potent, as evidenced by a leftward shift in the dose-response curve."( Inhaled vs. oral alprazolam: subjective, behavioral and cognitive effects, and modestly increased abuse potential.
Carter, LP; Griffiths, RR; Harrison, JA; Reissig, CJ, 2015
)
1.03
" The patient's clinical condition improved rapidly and the dosage of alpha- and beta-blockers could be decreased."( Pseudopheochromocytoma induced by anxiolytic withdrawal.
Barna, S; Becs, G; Czifra, A; Erdei, A; Kovács, P; Páll, A; Páll, D; Paragh, G; Pfliegler, G; Sira, L; Szabó, Z, 2014
)
0.4
"The aim of the study was to assess the magnitude of the CYP3A4 inhibitory effect of 2 dosing regimens of ketoconazole and the influence of the pharmacokinetic properties of the CYP3A4 substrate on the extent of the substrate exposure increase."( CYP3A4-based drug-drug interaction: CYP3A4 substrates' pharmacokinetic properties and ketoconazole dose regimen effect.
Boulenc, X; Donazzolo, Y; Hermabessière, S; Martin, V; Nicolas, O; Ollier, C; Zobouyan, I, 2016
)
0.43
" On most secondary measures, the dose-response relationship was relatively flat or showed saturation at higher ESL doses."( Abuse liability assessment of eslicarbazepine acetate in healthy male and female recreational sedative users: A Phase I randomized controlled trial.
Blum, D; Chakraborty, B; Cheng, H; Levy-Cooperman, N; Schoedel, KA, 2016
)
0.43
"12mg/kg/infusion) were tested, producing an inverted U-shaped dose-response curve."( The differential effects of alprazolam and oxazepam on methamphetamine self-administration in rats.
Goeders, NE; Guerin, GF; Spence, AL, 2016
)
0.73
"Oxazepam significantly reduced methamphetamine self-administration as demonstrated by a downward shift of the dose-response curve."( The differential effects of alprazolam and oxazepam on methamphetamine self-administration in rats.
Goeders, NE; Guerin, GF; Spence, AL, 2016
)
0.73
"According to the United States pharmacopeia (USP), Gold standard technique for Alprazolam determination in dosage forms is HPLC, an expensive and time-consuming method that is not easy to approach."( PLS-LS-SVM based modeling of ATR-IR as a robust method in detection and qualification of alprazolam.
Ahmadi, F; Ghazali, M; Parhizkar, E; Sakhteman, A, 2017
)
0.9
" This cannot be determined directly, but methods should be able to at least detect the effects of a positive control in dosage known to be clearly associated with increased risk."( Evaluation of simulated driving in comparison to laboratory-based tests to assess the pharmacodynamics of alprazolam and alcohol.
Cohen, AF; de Kam, ML; Huizinga, CR; Kuipers, J; Mejia, Y; van Gerven, JM; Ziagkos, D; Zuiker, RG, 2019
)
0.73
" Data extracted included information about study design, country of origin, number of participants and demographic details, type of surgery, type of anaesthesia, intervention and dosing regimens, preoperative anxiety outcome measures, and postoperative anxiety outcome measures."( Melatonin for preoperative and postoperative anxiety in adults.
Madsen, BK; Møller, AM; Rosenberg, J; Zetner, D, 2020
)
0.56
"The identification of a range of different drugs within counterfeit benzodiazepine tablets has been widely reported; however, limited information is available on the dosage of these products."( What's in fake 'Xanax'?: A dosage survey of designer benzodiazepines in counterfeit pharmaceutical tablets.
Blakey, K; Griffiths, A; Matheson, A; Thompson, A, 2022
)
0.72
" Alp-SLNs are a promising candidate to achieve sustained release of the short-acting drug Alp, thereby reducing its dosing frequency and enhancing patient compliance."( Compritol-Based Alprazolam Solid Lipid Nanoparticles for Sustained Release of Alprazolam: Preparation by Hot Melt Encapsulation.
Ahmad, I; Ahmad, S; Ahmed, M; Ghazwani, M; Hani, U; Khan, KUR; Madni, A; Rai, N; Rao, H; Rao, I; Umair, M, 2022
)
1.07
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (6)

RoleDescription
anxiolytic drugAnxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions.
anticonvulsantA drug used to prevent seizures or reduce their severity.
muscle relaxantA drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.
sedativeA central nervous system depressant used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
GABA agonistA drug that binds to and activates gamma-aminobutyric acid receptors.
xenobioticA xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
[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 (2)

ClassDescription
triazolobenzodiazepineAny organic heterotricyclic compound that is any benzodiazepine which is ortho-fused with a triazole.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[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 (38)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency4.94020.000221.22318,912.5098AID743035; AID743042; AID743054; AID743063
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.00700.000214.376460.0339AID720692
pregnane X nuclear receptorHomo sapiens (human)Potency14.12540.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.56180.000229.305416,493.5996AID743069; AID743078; AID743079; AID743080; AID743091
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.83250.001019.414170.9645AID743094
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency3.75780.001723.839378.1014AID743083
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency15.84890.001815.663839.8107AID894
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.60320.000323.4451159.6830AID743065; AID743067
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency2.25360.00798.23321,122.0200AID2551
lamin isoform A-delta10Homo sapiens (human)Potency0.01260.891312.067628.1838AID1487
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency16.83470.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency13.33320.011912.222168.7989AID651632
[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)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.00080.00000.21085.6234AID1889906
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.00110.00000.18819.0000AID1889906; AID1889907; AID1889908; AID1889909
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.00330.00020.561410.0000AID187152
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.00330.00020.635210.0000AID187152
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.00330.00020.621710.0000AID187152
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.00330.00020.675810.0000AID187152
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.00330.00020.646910.0000AID187152
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.00330.00020.671210.0000AID187152
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)64.00000.00000.43624.3000AID52421
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.00150.00010.24425.6234AID1889909
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.00140.00010.25155.6234AID1889908
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.00060.00010.24015.6234AID1889907
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.00110.00000.28325.6234AID1889906; AID1889907; AID1889908; AID1889909
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.00330.00020.557710.0000AID187152
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.00330.00020.640310.0000AID187152
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.00330.00020.570810.0000AID187152
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC50 (µMol)64.00000.00041.13803.5000AID52421
GABA theta subunitRattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.00330.00020.656110.0000AID187152
[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)
Bromodomain-containing protein 4Homo sapiens (human)Kd2.46000.00100.36918.9300AID648853
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC50 (µMol)0.03700.00112.000910.0000AID221774
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC50 (µMol)0.01000.00301.58219.8000AID71247
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC50 (µMol)0.06900.01001.20095.6234AID71238
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC50 (µMol)0.01200.01201.17515.2000AID71233
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
behavioral fear responseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
associative learningGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signaling receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleoplasmGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cytosolGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuronal cell body membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (218)

Assay IDTitleYearJournalArticle
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.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
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.
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.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
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.
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
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).
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.
AID1150961Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as decrease in traction reflex1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
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.
AID1552590Permeability of compound at 25 ug/ml at pH 7.4 incubated for 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease.
AID1150967Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of pentylenetetrazole-induced clonic convulsions1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
AID129148Anticonvulsant activity was determined as the degree of protection against convulsions induced by pentylenetetrazole in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
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.
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.
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).
AID117408Anxiolytic activity (latency to fight) in mice after administration (3.0 mg/kg) using shock-induced aggression assay2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.
AID1889909Displacement of [3H]flunitrazepam from human recombinant alpha5beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay2022Bioorganic & medicinal chemistry letters, 04-15, Volume: 62Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID648850Binding affinity to PB1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
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.
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).
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.
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.
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.
AID1150969Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of electroshock-induced convulsions1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
AID1136393Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of thiosemicarbazide-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID648858Binding affinity to BRD3-BD2 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID224180Concentration required to inhibit PAF (5*10e-8 M) induced platelet aggregation in rabbit platelet rich plasma(PRP) by 50%1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Analogues of platelet activating factor. 7. Bis-aryl amide and bis-aryl urea receptor antagonists of PAF.
AID1209593Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1847942Antiproliferative activity against human CD8-positive T cells at 33 uM measured after 96 hrs by flow cytometry analysis relative to control2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.
AID113894Loss of righting reflex (LORR) was evaluated in CF1 mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4.
AID1533611Effective permeability of the compound by PAMPA2019European journal of medicinal chemistry, Feb-01, Volume: 163Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory.
AID1847948Antiproliferative activity against mouse CD4+ve Th cells at 100 uM measured after 48 hrs by flow cytometry analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.
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]
AID113666Effect on bicuculline-induced tonic-extensor convulsions (B) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID1150963Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of nicotine-induced tonic extensor convulsions1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
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]
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.
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).
AID648853Binding affinity to BRD4-BD1 by isothermal titration calorimetry2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID648851Binding affinity to PCAF assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID26380Dissociation 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.
AID603953In-vivo plasma to lung partition coefficients of the compound, logP(lung) in rat2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs.
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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1150966Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of strychnine-induced lethality1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
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.
AID71247Effective concentration against Gamma-aminobutyric acid A receptor, alpha 52002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID648849Binding affinity to LOC93349 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
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.
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.
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.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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).
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID221774Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 12002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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).
AID1136395Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of maximal electric shock-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
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).
AID187152Binding affinity was determined by displacement of [3H]flumazenil from rat cortex homogenates2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID648846Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID648843Binding affinity to BRD2-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
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]
AID1847947Antiproliferative activity against mouse CD8-positive T cells at 100 uM measured after 48 hrs by flow cytometry analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID167798Concentration needed to inhibit PAF-induced platelet aggregation in rabbit PRP by 50%1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Analogues of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor.
AID113679Effect on pentylenetetrazole-induced clonic convulsions (P) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID131573Sedative activity was determined by measuring the loss of the righting reflux induced by thiopental sodium in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID1383661Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease.
AID1137413Anticonvulsant activity in ip dosed albino CF1 mouse assessed as inhibition of bicucullin-induced tonic extensor convulsions1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID1137415Reduction of hypoxic stress in ip dosed albino CF1 mouse assessed as prolongation of hypoxic survival time1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID648844Binding affinity to BRD3-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID1137417Potentiation of yohimbine toxicity in ip dosed aggregated albino CF1 mouse1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID539468Solubility of the compound in water at pH 72010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1889906Displacement of [3H]flunitrazepam from human recombinant alpha1beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay2022Bioorganic & medicinal chemistry letters, 04-15, Volume: 62Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
AID648847Binding affinity to BAZ2B assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
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
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.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID648859Binding affinity to BRD4-BD2 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1533612Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory.
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]
AID1150968Potentiation of ethanol-induced anxiolytic activity in ip dosed male albino CF-1 mouse1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
AID113678Effect on loss of traction (Tr) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID113321Ex vivo inhibition of [3H]flunitrazepam binding to mouse GABA-A benzodiazepine receptor1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Sequentially labile water-soluble prodrugs of alprazolam.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1137419Potentiation of apomorphine-induced gnawing in ip dosed albino CF1 mouse1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID1150964Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of nicotine-induced death1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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.
AID1890739Permeability of the compound across blood brain barrier incubated for 18 hrs by UV plate reader based PAMPA assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID131572Sedative activity was determined by measuring the loss of the righting reflux induced by chlorprothixene in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID1137412Inhibition of apomorphine-induced cage climbing in ip dosed albino CF1 mouse compound administered prior to challenge measured for 5 mins after 5 mins of challenge1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID1136388Effect on motor activity in ip dosed albino CF-1 mouse by chimney test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
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).
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.
AID648852Binding affinity to BRD4-BD1 assessed as change in melting temperature by isothermal titration calorimetry2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID648857Binding affinity to BRD2-BD2 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
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.
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.
AID648845Binding affinity to BRD4-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID648848Binding affinity to CREBBP assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID131236Muscle relaxation was determined by using rotatory drum (rotarod) in mice, activity is expressed as ED50 values1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID1137416Inhibition of amphetamine aggregation toxicity in ip dosed albino CF1 mouse compound administered 1 hr prior to challenge measured after 2 hrs1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
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).
AID113820Effect on potentiation of gamma-butyrolactone-induced sleep (gamma-B) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID71238Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 32002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1136389Effect on motor activity in ip dosed albino CF-1 mouse by dish test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1660982Inhibition of Escherichia coli Stx2 in human HeLa cells assessed as stimulation of protein synthesis by measuring increase in [14C]-leucine incorporation at 30 uM incubated with cells for 4 hrs prior to Stx2 addition and further incubated for 20 hrs and s2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin.
AID1136392Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of pentylenetetrazole-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID131571Sedative activity was determined by measuring the inhibition of spontaneous motor activity1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID1917372Permeability of compound by PAMPA-BBB assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis, in-vitro, in-vivo and ex-vivo pharmacology of thiazolidine-2,4-dione derivatives as selective and reversible monoamine oxidase-B inhibitors.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID221773Maximum percent potentiation against gamma-aminobutyric acid (GABA) A receptor, alpha 12002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID76083Displacement of [125I]gastrin from guinea pig gastric glands1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
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).
AID1137410Anticonvulsant activity in ip dosed albino CF1 mouse assessed as protection against pentylenetetrazole-induced clonic convulsions1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID1889908Displacement of [3H]flunitrazepam from human recombinant alpha3beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay2022Bioorganic & medicinal chemistry letters, 04-15, Volume: 62Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
AID1847943Antiproliferative activity against human CD4+ve T cells at 33 uM measured after 96 hrs by flow cytometry analysis relative to control2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID71233Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 22002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
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.
AID224348Inhibition of PAF-induced platelet aggregation in rabbit platelet rich plasma1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Analogues of platelet activating factor. 8. Antagonists of PAF containing an aromatic ring linked to a pyridinium ring.
AID1150965Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of thiosemicarbazide -induced lethality1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
AID1150962Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as decrease in dish reflex1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.
AID113664Effect on antagonism of nicotine-induced tonic-extensor convulsions (TE) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1137418Inhibition of oxotremorine-induced hypothermia in ip dosed albino CF1 mouse1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID384956Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID52403Displacement of [125I]CCK from Cholecystokinin receptor of guinea pig brain1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
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).
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).
AID112334Evaluated for antagonistic activity on nicotine-induced tonic-extensor convulsions (TE) in CF1 mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4.
AID188129Rat behavioral spontaneous Locomotor Activity2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
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).
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID112343Evaluated for the antagonism of nicotine induced death (D) in CF1 mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID71246Maximum percent potentiation against gamma-aminobutyric acid (GABA) A receptor, alpha 52002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID1136391Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of nicotine-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID117411Ataxia (time on rotaing rod) in mice after administration (3 mg/kg) using standard Rotarod assay2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.
AID1137411Hypothermic activity in ip dosed albino CF1 mouse assessed as effect on body temperature measured after 45 mins1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID128826Antianxiety activity was determined by measuring the antagonism of foot shock induced fighting (taming) in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID1137414Antidepressant activity in ip dosed albino CF1 mouse assessed as potentiation of gamma-butyrolactone-induced sleep1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity.
AID1136397Anxiolytic activity in ip dosed albino CF-1 mouse under hypoxic stress1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1727019Half life in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID1136387Effect on motor activity in ip dosed albino CF-1 mouse by traction test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
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.
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.
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1148194CNS activity in po dosed mouse assessed as antagonism against pentylenetetrazole-induced response1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1148192CNS activity in po dosed mouse by inclined screen test1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
AID71232Maximum percent potentiation against gamma-aminobutyric acid (GABA) A receptor, alpha 22002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1148193CNS activity in po dosed mouse assessed as antifighting activity by foot shock test1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
AID71237Maximum percent potentiation against gamma-aminobutyric acid (GABA) A receptor, alpha 32002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
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.
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
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]
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1136396Antidepressant activity in ip dosed albino CF-1 mouse assessed as inhibition of ethanol-induced response1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1136120Retention time of the compound by GLC-electron capture detection analysis1978Journal of medicinal chemistry, Jun, Volume: 21, Issue:6
Novel anxiolytic agents derived from alpha-amino-alpha-phenyl-o-tolyl-4H-triazoles and -imidazoles.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID113663Effect on antagonism of nicotine-induced death (D) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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.
AID52421Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreas1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
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.
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).
AID117406Anxiolytic activity (latency to fight) in mice after administration (0.3 mg/kg) using shock-induced aggression assay2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.
AID1136394Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of strychnine-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID112344Evaluated for the pentylene induced clonic convulsions (P) in CF1 mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4.
AID113823Effect on prolongation of hypoxic survival time (HS) in Carworth farms male albino mice1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
AID113898Loss of traction (TR) was evaluated in mice1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4.
AID117410Ataxia (time on rotaing rod) in mice after administration (0.3 mg/kg) using standard Rotarod assay2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.
AID1889907Displacement of [3H]flunitrazepam from human recombinant alpha2beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay2022Bioorganic & medicinal chemistry letters, 04-15, Volume: 62Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
AID1136390Effect on motor activity in ip dosed albino CF-1 mouse by pedestal test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
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.
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.
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.
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.
AID1346504Human GABAA receptor alpha2 subunit (GABAA receptors)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID1346513Human GABAA receptor alpha5 subunit (GABAA receptors)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID1346496Human GABAA receptor alpha3 subunit (GABAA receptors)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
AID1346520Human GABAA receptor alpha1 subunit (GABAA receptors)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,782)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990447 (25.08)18.7374
1990's633 (35.52)18.2507
2000's318 (17.85)29.6817
2010's280 (15.71)24.3611
2020's104 (5.84)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 137.73

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 Index137.73 (24.57)
Research Supply Index7.83 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index261.57 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (137.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials591 (30.85%)5.53%
Reviews131 (6.84%)6.00%
Case Studies289 (15.08%)4.05%
Observational3 (0.16%)0.25%
Other902 (47.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (89)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-blind, Placebo- and Active Comparator-controlled, Crossover Trial to Examine the Effect of Multiple Doses of CVL-865 on Panic Symptoms Induced by Carbon Dioxide Inhalation in Healthy Subject [NCT04592536]Phase 156 participants (Actual)Interventional2020-10-06Completed
Licorice Botanical Dietary Supplements - Metabolism and Safety in Women [NCT03948243]Phase 119 participants (Actual)Interventional2019-04-01Completed
A Phase I, Randomized, Double-Blind, Placebo-Controlled, 5-Period, Cross-Over Study Assessing the Effects of Lasmiditan on Simulated Driving Performance in Normal Healthy Volunteers [NCT03012334]Phase 190 participants (Actual)Interventional2017-01-16Completed
Open-label, Randomized, Single-Dose, 2 Way Crossover Bioequivalence Study Comparing A New Alprazolam Sublingual Tablet Formulation To A Reference Alprazolam Immediate Release Tablet [NCT01256151]Phase 128 participants (Actual)Interventional2011-01-31Completed
A Relative Bioavailability Study of 2 mg Alprazolam Oral Disintegrating Tablets Under Non-fasting Conditions [NCT01188057]Phase 140 participants (Actual)Interventional2006-07-31Completed
SAFER-SIM: Opiates and Benzodiazepines on Driving [NCT03447353]Phase 418 participants (Actual)Interventional2016-06-14Completed
A Phase 1 Randomized, Double-Blind, Placebo-Controlled, 3-Way Crossover (Part A) and 2-Arm Parallel Group (Part B) Study to Assess the Pulmonary Safety of Staccato Alprazolam in Healthy Study Participants (Part A) and in Study Participants With Mild Asthm [NCT04802746]Phase 178 participants (Actual)Interventional2021-03-09Completed
Sedative Premedication in Coronary Angiography [NCT03576456]264 participants (Anticipated)Interventional2019-01-01Not yet recruiting
Validation of the Drug Impaired Driving Scenario (DIDS) on the CRCDS-miniSim: Evaluating Sensitivity to the Effects of Cannabis and Alprazolam [NCT04970342]Phase 113 participants (Actual)Interventional2021-07-16Completed
Efficacity of Hypnosis Versus Premedication for the Management of Perioperative Anxiety in Gynecological Surgery [NCT03327506]Phase 4128 participants (Anticipated)Interventional2018-11-27Recruiting
Comparing Efficacy of Oral Midazolam and Sublingual Alprazolam in Reducing Anxiety and Pain/Discomfort Related to Diagnostic Upper Gastrointestinal Endoscopy in Adults [NCT03130842]Phase 2/Phase 3136 participants (Actual)Interventional2016-09-17Completed
Efficacy and Safety Study of a IMSS Developed Phytopharmaceutical for the Treatment of Anxiety. Double Blind and Randomized Clinical Trial Controlled With Alprazolam [NCT03702803]Phase 2122 participants (Anticipated)Interventional2016-03-16Recruiting
A Relative Bioavailability Study of 3 mg Alprazolam Extended Release Tablets Under Non-fasting Conditions [NCT00830024]Phase 136 participants (Actual)Interventional2005-06-30Completed
An Open Label, Randomized, Single Dose, Crossover Pivotal Bioequivalence Study Of Xanax XR Tablet 3 mg (Sourced From Caguas) Versus Xanax XR Tablet 3 mg (Sourced From Barceloneta) In Healthy Subjects [NCT01330472]Phase 116 participants (Actual)Interventional2011-05-31Completed
A Relative Bioavailability Study of 3 mg Alprazolam Extended Release Tablets Under Fasting Conditions [NCT00829426]Phase 132 participants (Actual)Interventional2005-06-30Completed
A Randomized, Double Blind, Active and Placebo Controlled, 5 Way Crossover Study to Determine the Abuse Potential of Orally Administered Gabapentin Enacarbil Immediate Release Capsules in Healthy, Nondependent Recreational Drug Users With Sedative Experie [NCT06097676]Phase 486 participants (Actual)Interventional2021-09-28Completed
A Relative Bioavailability Study of 2 mg Alprazolam Oral Disintegrating Tablets Under Fasting Conditions [NCT01188031]Phase 140 participants (Actual)Interventional2006-06-30Completed
A Randomized, Subject- and Investigator-Blind, Placebo and Active-Controlled Study to Assess the Abuse Potential of Lasmiditan [NCT03286218]Phase 196 participants (Actual)Interventional2017-09-15Completed
Open-Label, Randomized, Single-Dose, 2-Way Crossover Bioequivalence Study Comparing A New Alprazolam Sublingual Tablet Formulation To An Alprazolam Sublingual Tablet [NCT01285505]Phase 10 participants (Actual)Interventional2011-04-30Withdrawn
A Phase IV, Open Label, Randomized, Two-way Crossover, Single Dose Study to Determine Relative Bioavailability of Alprazolam 0,75mg/ml (laboratórios Pfizer Ltda) in the Oral Solution-drops Form, Versus Frontal® 0,25mg (laboratórios Pfizer Ltda), in the Ta [NCT01322867]Phase 430 participants (Actual)Interventional2011-05-31Completed
A Randomized, Double-Blind, Placebo- And Active-Controlled Single-Dose, Crossover Study To Evaluate The Abuse Potential Of Single Doses Of Dimebon (Latrepirdine) In Healthy Recreational Polydrug Users [NCT00975481]Phase 136 participants (Actual)Interventional2009-10-31Completed
MELA Study - Hedonic Study on the Taste of Drugs Crushed in Food: Observational Study Involving 16 Healthy Volunteers [NCT02570581]Phase 116 participants (Actual)Interventional2014-06-30Completed
Open,Two-period, Two-treatment, Two-sequence, Cross-over, Randomized Trial of Single Doses of Two Oral Preparations With 0.25 mg of Alprazolam (Zamoprax® GlaxoSmithKline México, S.A. de C.V. vs. Tafil® 0.25mg, Pharmacia &Upjohn, S.A. de C.V.) in Fasting H [NCT01853956]Phase 128 participants (Actual)Interventional2010-12-02Completed
Bioavailability of Alprazolam Tablets [NCT00913341]Phase 130 participants (Actual)Interventional1991-11-30Completed
Open-Label, Randomized, Single-Dose, 2-Way Crossover Pivotal Bioequivalence Study Comparing Alprazolam Immediate Release (IR) Tablets (Administered Orally) And Alprazolam Sublingual (SL) Tablets (Administered Sublingually) [NCT00860119]Phase 123 participants (Actual)Interventional2009-08-31Completed
A Relative Bioavailability Study of 3 mg Alprazolam Extended Release Tablets Under Non-Fasting Conditions [NCT00865657]Phase 140 participants (Actual)Interventional2005-09-30Completed
A Phase 1, Randomized, Double-blind, Double-dummy, Placebo-controlled, 5-period, Crossover Study Assessing the Effects of Rapastinel Compared to Alprazolam, Ketamine, and Placebo on Simulated Driving Performance in Normal Healthy Participants [NCT03814733]Phase 1107 participants (Actual)Interventional2018-11-05Completed
Abuse Liability Study of Staccato® Alprazolam for Inhalation in Subjects With Histories of Sedative Abuse [NCT00603980]Phase 131 participants (Actual)Interventional2008-01-31Completed
Open-Label, Randomized, Single-Dose, 2-Way Crossover Bioequivalence Study Comparing A New Alprazolam Sublingual Tablet Formulation To A Reference Alprazolam Immediate Release Tablet [NCT01027689]Phase 10 participants (Actual)Interventional2011-04-30Withdrawn
A Randomized, Double-blind, Placebo-controlled Study of Continuation Treatment With Xanax XR in the Treatment of Adolescents With a Primary Diagnosis of Panic Disorder [NCT00635076]Phase 43 participants (Actual)Interventional2004-07-31Terminated(stopped due to Please see Detailed Description for the termination reason.)
An Open-label Study to Assess the Safety and Tolerability of Xanax XR in the Treatment of Adolescents With Panic Disorder or Anxiety With Panic Attacks [NCT00634790]Phase 449 participants (Actual)Interventional2004-05-31Terminated(stopped due to Please see Detailed Description for termination reason.)
Single-Dose Fasting In Vivo Bioequivalence Study of Alprazolam Extended-Release Tablets (3 mg; Mylan) to Xanax XR® Tablets (3 mg; Pharmacia & Upjohn) in Healthy Volunteers [NCT00647634]Phase 121 participants (Actual)Interventional2004-08-31Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Alprazolam Extended-Release Tablets (1 mg; Mylan) to Xanax XR Tablets (1 mg; Pharmacia & Upjohn) in Healthy Volunteers [NCT00647894]Phase 124 participants (Actual)Interventional2005-01-31Completed
A Randomized, Double-blind, Placebo-controlled Study of Xanax XR in the Treatment of Adolescents With a Primary Diagnosis of Panic Disorder [NCT00635531]Phase 416 participants (Actual)Interventional2004-04-30Terminated(stopped due to Please see Detailed Description for termination reason.)
A Cognitive Enhancer May Facilitate Behavioral Exposure Therapy for Veterans With PTSD [NCT00356278]Phase 2/Phase 3156 participants (Actual)Interventional2006-09-30Completed
Open-label, Randomized, Single-dose, 2-way Crossover Bioequivalence Study Comparing A New Alprazolam Sublingual Tablet Formulation To A Reference Alprazolam Sublingual Tablet [NCT00877955]Phase 10 participants (Actual)Interventional2012-09-30Withdrawn
The Effect of Hydroxyzine and Alprazolam Premedication on Preoperative Anxiety and Patient Satisfaction [NCT04184141]Phase 490 participants (Anticipated)Interventional2019-12-01Not yet recruiting
Evaluate The Pharmacokinetics Of Two Alprazolam Formulations (Immediate Release And Extended Release Tablets) And A Clonazepam Tablet In A Healthy Mexican Population [NCT00810316]Phase 124 participants (Actual)Interventional2008-10-31Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel Group, 5-Week Trial To Assess The Efficacy And Safety Of PD 0332334 Compared To Placebo And Alprazolam Extended-Release In Patients With Generalized Anxiety Disorder [NCT00921063]Phase 2222 participants (Actual)Interventional2005-11-30Completed
Randomized, Double-blind, Placebo-controlled Study of a Benzodiazepine vs Placebo on Functional Magnetic Resonance Imaging (fMRI) of the Brain, and on Behavioral/Clinical Measures in Patients With Generalized Anxiety Disorder [NCT00662259]Phase 432 participants (Actual)Interventional2008-04-30Completed
A Relative Bioavailability Study of 3 mg Alprazolam Extended Release Tablets Under Fasting Conditions [NCT00865761]Phase 140 participants (Actual)Interventional2005-09-30Completed
Bioequivalence Study Comparing Two Alprazolam 1 mg Tablets; an Open, Randomised, Single Centre, Single Dose Study With Crossover Design in Healthy Subjects [NCT00878865]Phase 118 participants (Actual)Interventional2009-04-30Completed
A Multicenter, Randomized, Open-label, Parallel Design Trial to Compare Time to Response in the Symptoms of Anxiety to Concomitant Treatment With Niravam™ and an SSRI or SNRI to Treatment With an SSRI or SNRI Alone in Subjects With Generalized Anxiety Dis [NCT00266409]Phase 4418 participants (Actual)Interventional2005-10-31Completed
An Open Label,Crossover,Randomized Study Of Two Periods,Two Treatments,Two Sequences, And A Single Dose Of Two Oral Drug Products Of Alprazolam 2mg (Tafil (r), Product Of Pharmacia& Upjohn S.a De C.v Vs Xanax 2mg, Product Of Pfizer Pharmaceuticals Llc) In [NCT01046162]Phase 10 participants (Actual)Interventional2010-07-15Withdrawn
Comparison Between Sublingual and Oral Alprazolam as Conscious Sedation for Upper Gastrointestinal Endoscopy [NCT01949038]Phase 2/Phase 3220 participants (Actual)Interventional2011-09-30Completed
A Double-Blind, Randomized, Placebo-Controlled, Multicenter, Outpatient, Parallel-Group Study to Assess the Efficacy and Safety of Staccato Alprazolam in Study Participants 12 Years of Age and Older With Stereotypical Prolonged Seizures [NCT05077904]Phase 3250 participants (Anticipated)Interventional2021-12-07Recruiting
An Open-Label, Multicenter, Outpatient Extension Study to Evaluate the Safety and Tolerability of Staccato Alprazolam in Study Participants 12 Years of Age and Older With Stereotypical Prolonged Seizures [NCT05076617]Phase 3300 participants (Anticipated)Interventional2022-02-03Enrolling by invitation
Mechanisms of Hypoglycemia-Associated Autonomic Dysfunction. The Effect of Alprazolam on Exercise Induced Hypoglycemia. [NCT00574639]Early Phase 114 participants (Actual)Interventional2007-07-31Completed
Efficacy of Aerobic Exercise Added to Alprazolam in Panic Disorder Treatment: a Clinical Randomized Trial [NCT00803400]Phase 4150 participants (Actual)Interventional2008-10-01Completed
A 4 Way Placebo And Active Controlled Study To Evaluate The Effects Of Fesoterodine On Cognitive Function In Healthy Elderly Subjects [NCT01161472]Phase 120 participants (Actual)Interventional2010-07-31Completed
A Phase I, Randomized, Placebo Controlled, Parallel Group, Single Dose Study To Evaluate The Effects Of PF-00572778 And Alprazolam On A Naloxone Challenge In Healthy Adult Subjects [NCT00580190]Phase 147 participants (Actual)Interventional2007-09-30Terminated(stopped due to Date of termination was Feb. 7, 2008. Reasons of termination were due to elevation of liver function tests and long elimination half-life of the compound.)
Hypoglycemia Associated Autonomic Failure in Type 1 DM, Question 2 [NCT00592332]56 participants (Anticipated)Interventional2005-06-30Completed
Bioequivalence Study Comparing Two Alprazolam 1 mg Tablets Under Fed Conditions; an Open, Randomised, Single Centre, Single Dose Study With Crossover Design in Healthy Subjects [NCT00878514]Phase 118 participants (Anticipated)Interventional2009-05-31Completed
Single-Dose Food In Vivo Bioequivalence Study of Alprazolam Extended-Release Tablets (3 mg; Mylan) to Xanax XR® Tablets (3 mg; Pharmacia & Upjohn) in Healthy Volunteers [NCT00650299]Phase 121 participants (Actual)Interventional2004-08-31Completed
Bioavailability of Alprazolam Tablets, 2 mg. [NCT00912145]Phase 126 participants (Actual)Interventional1996-02-29Completed
A Phase I/II, 3-Arm, Open Label, Single Centre Study to Investigate the Safety and Effect of Oral GABA Therapy on Beta-Cell Regeneration in Type 1-diabetes Patients [NCT03635437]Phase 1/Phase 235 participants (Actual)Interventional2018-09-05Completed
Safety, Tolerability, and Pharmacokinetics of a Single Dose of StaccatoTM Alprazolam for Inhalation in Normal, Healthy Volunteers [NCT00444522]Phase 150 participants Interventional2005-06-30Completed
Double-blind, Randomized, Placebo and Alprazolam-controlled Three-period Crossover Incomplete Block Design Study to Compare Putative Anxiolytic-like fRMI Activity of GW876008 and GSK561679 After Single-dose Administration in Subjects With Social Anxiety D [NCT00555139]Phase 135 participants (Actual)Interventional2007-03-27Completed
Placebo-Controlled, Randomized, Blinded, Double-Dummy, Crossover Study to Investigate the Attenuation of ACTH Activation Induced by Metyrapone With a Single Dose of GSK561679 or Alprazolam in Healthy Volunteers [NCT00426608]Phase 120 participants (Actual)Interventional2006-10-06Completed
A Comparative Study of Oral Gabapentin, Oral Alprazolam and Intravenous Dexmedetomidine on Perioperative Anxiety and Pain During Posterior Segment Eye Surgery Under Peribulbar Block : a Randomized, Double-blind Study. [NCT04658732]Phase 145 participants (Anticipated)Interventional2020-12-01Recruiting
Effect of Alprazolam on Heart Rate and Acute Inflammatory Marker in Acute Coronary Syndrome Patients [NCT04715269]Phase 1/Phase 248 participants (Anticipated)Interventional2020-12-25Recruiting
A Multicenter, Open-Label, Randomized Crossover Trial to Assess Subject Preference for Alprazolam Orally Disintegrating Tablets Compared to Conventional Alprazolam Tablets in Subjects With Anxiety [NCT00139854]Phase 30 participants Interventional2004-08-31Completed
Spectroscopic Imaging of GABA and Glutamate/Glutamine in Healthy Volunteers at 4T: A Double Blind, Crossover Drug Challenge Study [NCT01577706]7 participants (Actual)Interventional2013-06-30Terminated(stopped due to lack of enrollment)
Effect of Preoperative Alprazolam on the Success of Inferior Alveolar Nerve Block for Teeth With Irreversible Pulpitis [NCT01546090]Phase 460 participants (Actual)Interventional2011-03-31Completed
[NCT01546896]Phase 40 participants (Actual)Interventional2012-03-31Withdrawn
Assessment of Two Modes of Premedication in Surgery - PREMED Study [NCT01549691]Phase 4455 participants (Anticipated)Interventional2012-03-31Completed
A Randomized Double-Blind Comparison of Sertraline With Early Alprazolam XR Co-Administration vs Sertraline/Placebo for Primary Care Panic Disorder Patients [NCT00198094]Phase 4150 participants (Anticipated)Interventional2003-12-31Completed
Investigation of a Single Dose of Staccato™ Alprazolam for Inhalation on Doxapram-Induced Panic Attack in Patients With Panic Disorder [NCT00477451]Phase 249 participants (Actual)Interventional2007-05-31Completed
Assessment of Staccato® Alprazolam on the EEG Photoparoxysmal Response in Patients With Epilepsy [NCT02351115]Phase 25 participants (Actual)Interventional2015-01-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Trial Of The Anxiolytic Efficacy Of Pregabalin And Alprazolam IR In Subjects With Anxiety Prior To Dental Procedure [NCT00245609]Phase 290 participants Interventional2006-01-31Completed
Open, Two Periods, Two Treatments, Two Sequences, Cross-over, Randomized Study With Single Dosage of Two Oral Preparations of Alprazolam 0.5 mg Alprazolam (Zamoprax GlaxoSmithKline México, S.A. de C.V. vs. Tafil 0.5mg, Pharmacia &Upjohn, S.A. de C.V.) in [NCT01745562]Phase 128 participants (Actual)Interventional2010-12-07Completed
Open, Two Periods, Two Treatments, Two Sequences, Cross-over, Randomized Trial With Single Dosageof Two Oral Preparations Containing 2 mg of Alprazolam (Zamoprax GlaxoSmithKline México, S.A. de C.V. vs. Tafil 2.0 mg, Pharmacia &Upjohn, S.A. de C.V.) in Fa [NCT01745575]Phase 126 participants (Actual)Interventional2010-03-28Completed
Imaging the Effects of Zolpidem and Alprazolam in Healthy Volunteers at 3T [NCT01747590]Early Phase 112 participants (Anticipated)Interventional2011-07-31Recruiting
A Phase 1, Randomized, Double-Blind, Double-Dummy, Active- and Placebo-Controlled, 5-Way Crossover Study Evaluating the Abuse Potential of Soticlestat (TAK-935) in Healthy Adult Nondependent Recreational Drug Users With Central Nervous System Depressant E [NCT05602818]Phase 167 participants (Actual)Interventional2022-11-15Completed
A Phase 1 Open-Label, Non-Randomized, Single-Dose, Pharmacokinetic Study Evaluating Staccato® Alprazolam 1 mg Inhaler in Smoker Versus Non-Smoker Healthy Adult Volunteers [NCT03516305]Phase 136 participants (Actual)Interventional2018-04-06Completed
An Open-Label, Randomized, Single-Dose, 2-Way Crossover Study to Evaluate The Relative Bioavailability of Staccato Alprazolam Compared to Oral Alprazolam in Healthy Study Participants [NCT05626439]Phase 121 participants (Actual)Interventional2022-12-28Completed
Benzodiazepine-free Anesthetic for Reduction of Delirium (B-Free): A Two-centre Pilot Study to Determine the Feasibility of a Multi-centre, Randomized, Cluster Crossover Trial [NCT03053869]Phase 1480 participants (Actual)Interventional2017-04-01Completed
PharmacofMRI of Anxiolytic Medications (Alprazolam) [NCT00703885]Phase 416 participants (Actual)Interventional2008-01-31Completed
Alprazolam and Simulated Driving Performance: Next Day Effects [NCT03297944]Phase 415 participants (Actual)Interventional2017-09-15Completed
A Double-Blind, Placebo-Controlled, Inpatient, Dose-Ranging Efficacy Study of Staccato Alprazolam (STAP-001) in Subjects With Epilepsy With a Predictable Seizure Pattern [NCT03478982]Phase 2156 participants (Actual)Interventional2018-03-16Completed
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
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
A Placebo-Controlled, Double-blind, Randomized Study to Assess the Safety, Tolerability, And Pharmacokinetics of Staccato Alprazolam in Healthy Japanese, Chinese, and Caucasian Participants [NCT04782388]Phase 130 participants (Actual)Interventional2021-03-04Completed
[NCT00004373]Phase 280 participants Interventional1997-03-31Completed
Premedication With Melatonin and Alprazolam Combination Versus Alprazolam or Melatonin Alone: a Randomized, Double Blind Placebo Controlled Study [NCT01486615]Phase 480 participants (Actual)Interventional2011-10-31Completed
A Multicenter, Open-Label Study to Evaluate the Pharmacokinetics, Tolerability, and Safety of a Single Dose of Staccato Alprazolam in Adolescent Study Participants With Epilepsy [NCT04857307]Phase 114 participants (Actual)Interventional2021-04-28Completed
Opioid/Benzodiazepine Polydrug Abuse: Integrating Research on Mechanisms, Treatment and Policies - Study 3 [NCT05006079]Phase 224 participants (Anticipated)Interventional2022-06-15Recruiting
Randomized, Double-Blind, Double-Dummy, 5-Way Crossover Study to Evaluate the Abuse Potential of Cenobamate Relative to Alprazolam and Placebo When Administered Orally in Non-Dependent, Recreational Drug Users With Sedative Experience [NCT03509285]Phase 153 participants (Actual)Interventional2017-03-08Completed
A Human Abuse Potential Study to Evaluate the Subjective and Physiological Effects of Cannabidiol (CBD) Compared to Delta-9-Tetrahydrocannabinol (THC) and Alprazolam in an Inpatient Setting [NCT03398083]Phase 142 participants (Actual)Interventional2017-12-04Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 8 Weeks
NCT00266409 (69) [back to overview]Change in Severity of Illness From Baseline Using the Clinical Global Impression Improvement (CGI-I) Score After 2 Weeks
NCT00266409 (69) [back to overview]Change in Severity of Illness From Baseline Using the Clinical Global Impression - Improvement (CGI-I) Score at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Change in Severity of Illness From Baseline Using the Clinical Global Impression - Improvement (CGI-I) Score After 8 Weeks
NCT00266409 (69) [back to overview]Change in Severity of Illness From Baseline Using the Clinical Global Impression - Improvement (CGI-I) Score After 4 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 8 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 7 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 6 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 5 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 4 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 3 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 7 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 6 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 5 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 4 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 3 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 8 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 2 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in the Total HAM-A Score After 1 Week
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 8 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 4 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 7 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 6 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 2 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 1 Week
NCT00266409 (69) [back to overview]Cumulative Percent of Participants Showing a Response in the Symptoms of Anxiety (Decrease in Total Hamilton Anxiety (HAM-A) -Score of >=50%) in the Per Protocol Population (Kaplan-Meier-estimates)
NCT00266409 (69) [back to overview]Cumulative Percent of Participants Showing a Response in the Symptoms of Anxiety (Decrease in Total Hamilton Anxiety (HAM-A) -Score of >=50%) in the Intent-to-treat Population (Kaplan-Meier-estimates)
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 8 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 7 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 6 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 5 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 3 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 2 Weeks
NCT00266409 (69) [back to overview]Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 1 Week
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 3 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 2 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 1 Week
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 7 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 6 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 5 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 5 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 4 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 3 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 2 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-psychic Factors Subscore After 1 Week
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 8 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 7 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-somatic Subscore After 4 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 6 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 5 Weeks
NCT00266409 (69) [back to overview]Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 4 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 3 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 2 Weeks
NCT00266409 (69) [back to overview]Change From Baseline in HAM-A-insomnia Subscore After 1 Week
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score at Endpoint During the 8 Week Treatment Period
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 1 Week
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 2 Weeks
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 3 Weeks
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 4 Weeks
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 5 Weeks
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 6 Weeks
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 7 Weeks
NCT00266409 (69) [back to overview]Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 8 Weeks
NCT00356278 (10) [back to overview]Clinician-Administered PTSD Scale (CAPS)
NCT00356278 (10) [back to overview]PTSD Symptom Scale Self-Report
NCT00356278 (10) [back to overview]PTSD Symptom Scale Self-Report
NCT00356278 (10) [back to overview]PTSD Symptom Scale Self-Report
NCT00356278 (10) [back to overview]PTSD Symptom Scale Self-Report
NCT00356278 (10) [back to overview]Clinician-Administered PTSD Scale (CAPS)
NCT00356278 (10) [back to overview]Clinician-Administered PTSD Scale (CAPS)
NCT00356278 (10) [back to overview]Clinician-Administered PTSD Scale (CAPS)
NCT00356278 (10) [back to overview]Clinician-Administered PTSD Scale (CAPS)
NCT00356278 (10) [back to overview]PTSD Symptom Scale Self-Report
NCT00477451 (3) [back to overview]Number of Participants With Doxapram-induced Panic Attack
NCT00477451 (3) [back to overview]Borg Max Change From Baseline
NCT00477451 (3) [back to overview]Duration of the Doxapram-induced Panic Attack
NCT00603980 (15) [back to overview]"Maximum of DEQ Question 2 Rate Your Liking of the Drug Effect at the 10 Time Points (Predose Through 9 Hours)"
NCT00603980 (15) [back to overview]"EDQ Question Number 7,What Would You be Willing to Pay for Today's Drug?"
NCT00603980 (15) [back to overview]"EDQ Question Number 6 Estimate the Amount of Money You Think the Drug You Took Today Would be Worth on the Street."
NCT00603980 (15) [back to overview]"EDQ Question Number 2 Rate Your Overall Liking of the Drug Effect"
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 6) Maximum of Confusion/Disorientation
NCT00603980 (15) [back to overview]"EDQ Question Number 1, Rate the Overall Strength of the Drug Effect"
NCT00603980 (15) [back to overview]"Maximum of DEQ Question 1 Rate the Strength of the Drug Effect (at the 10 Time Points, Predose Through 9 Hours)"
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 4) Maximum of Muscle Relaxation Posture
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 8) Maximum of Drug Strength
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 7) Maximum of Stimulation/Arousal
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 5) Maximum of Speech
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 3) Maximum of Muscle Relaxation Non-locomotor
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 2) Maximum of Muscle Relaxation Locomotor
NCT00603980 (15) [back to overview]Observer Rated Questionnaire 1) Maximum of Sedation/Sleepiness
NCT00603980 (15) [back to overview]"Response to EDQ Question Number 5, Rate the Degree to Which You Would Like to Take the Drug Again"
NCT00662259 (5) [back to overview]Signal Change in Brain Activity in the Amygdala When Viewing Emotional Faces
NCT00662259 (5) [back to overview]Signal Change in Brain Activity in the Insula When Anticipating the Viewing of Emotional Pictures.
NCT00662259 (5) [back to overview]Score on the Penn State Worry Scale
NCT00662259 (5) [back to overview]Score on the Hamilton Anxiety Scale
NCT00662259 (5) [back to overview]Score on Quick Inventory of Depressive Symptomatology
NCT00803400 (3) [back to overview]Participants´Endpoint Change From Baseline in Clinical Global Impression Severity Scale (CGI-S)
NCT00803400 (3) [back to overview]Participants´Endpoint Change From Baseline in Hamilton Anxiety Rating Scale
NCT00803400 (3) [back to overview]Participants´Endpoint Change From Baseline in Clinical Global Impression Improvement Scale (CGI-I)
NCT00829426 (3) [back to overview]Bioequivalence Based on AUC0-t
NCT00829426 (3) [back to overview]Bioequivalence Based on AUC0-inf
NCT00829426 (3) [back to overview]Bioequivalence Based on Cmax
NCT00830024 (3) [back to overview]Cmax - Maximum Observed Concentration
NCT00830024 (3) [back to overview]AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)
NCT00830024 (3) [back to overview]AUC0-inf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)
NCT00975481 (15) [back to overview]Other Subjective Effects- Drug Similarity
NCT00975481 (15) [back to overview]Balance of Effects- Overall Drug Liking VAS: Peak Effect (Maximum Effect [Emax]) and Minimum Effect (Emin)
NCT00975481 (15) [back to overview]Balance of Effects- Good and Bad Effects VAS: Peak Effect (Maximum Effect [Emax]) and Minimum Effect (Emin)
NCT00975481 (15) [back to overview]Balance of Effects- Drug Liking VAS: Peak Effect (Maximum Effect [Emax]) and Minimum Effect (Emin)
NCT00975481 (15) [back to overview]Sedative Effects- Alertness/Drowsiness: Minimum Effect (Emin)
NCT00975481 (15) [back to overview]Sedative Effects- Addiction Research Center Inventory (ARCI) Pentobarbital Chlorpromazine Group (PCAG): Maximum Effect (Emax)
NCT00975481 (15) [back to overview]Balance of Effects- Subjective Drug Value (SDV): Maximum Effect (Emax)
NCT00975481 (15) [back to overview]Positive Effects- High VAS: Peak Effect (Maximum Effect [Emax])
NCT00975481 (15) [back to overview]Positive Effects- Good Drug Effects: Peak Effect (Maximum Effect [Emax])
NCT00975481 (15) [back to overview]Positive Effects- Addiction Research Center Inventory (ARCI) Morphine Benzedrine Group (MBG): Maximum Effect (Emax)
NCT00975481 (15) [back to overview]Other Subjective Effects- Any Drug Effects: Peak Effect (Maximum Effect [Emax])
NCT00975481 (15) [back to overview]Negative Effects- Bad Drug Effects: Peak Effect (Maximum Effect [Emax])
NCT00975481 (15) [back to overview]Negative Effects- Addiction Research Center Inventory (ARCI) Lysergic Acid Diethylamide (LSD): Maximum Effect (Emax)
NCT00975481 (15) [back to overview]Balance of Effects- Take Drug Again VAS: Peak Effect (Maximum Effect [Emax])
NCT00975481 (15) [back to overview]Other Subjective Effects- Addiction Research Center Inventory (ARCI) Benzedrine Group (BG): Maximum Effect (Emax) and Minimum Effect (Emin)
NCT01161472 (12) [back to overview]Change From Baseline in CogState One Card Learning on Day 6
NCT01161472 (12) [back to overview]Change From Baseline in Computer Based Objective Cognition Testing (CogState) Detection Speed on Day 6
NCT01161472 (12) [back to overview]CogState Continuous Paired Associate Learning (CPAL)
NCT01161472 (12) [back to overview]CogState Groton Maze Learning Task (GMLT)
NCT01161472 (12) [back to overview]Change From Baseline in CogState CPAL on Day 6
NCT01161472 (12) [back to overview]CogState One Card Learning
NCT01161472 (12) [back to overview]Computer Based Objective Cognition Testing (CogState) Detection Speed
NCT01161472 (12) [back to overview]Rey Auditory Verbal Learning Test (RAVLT)
NCT01161472 (12) [back to overview]Rey Auditory Verbal Learning Test (RAVLT) on Day 6
NCT01161472 (12) [back to overview]Change From Baseline in CogState Groton Maze Learning Task on Day 6
NCT01161472 (12) [back to overview]Change From Baseline in CogState Identification Speed on Day 6
NCT01161472 (12) [back to overview]CogState Identification Speed
NCT01486615 (8) [back to overview]Sedation Score at One Hour After Premedication
NCT01486615 (8) [back to overview]Amount of Propofol Consumption
NCT01486615 (8) [back to overview]Change in VAS Anxiety Score Relative to Baseline After Premedication
NCT01486615 (8) [back to overview]Change in VAS Anxiety Score Relative to Baseline at 30 Minutes After Premedication
NCT01486615 (8) [back to overview]Change in VAS Anxiety Score Relative to Baseline at One Hour After Premedication
NCT01486615 (8) [back to overview]Number of Patients With Intact Memory
NCT01486615 (8) [back to overview]Number of Patients With Loss of Memory for Being Transferred to Operating Room.
NCT01486615 (8) [back to overview]Orientation Score
NCT01577706 (7) [back to overview]Right Thalamus: Percent Change in GABA Levels After an Acute Drug Challenge
NCT01577706 (7) [back to overview]Right Temporal: Percent Change in GABA Levels After an Acute Drug Challenge
NCT01577706 (7) [back to overview]Left Basal-Ganglia: Percent Change in GABA Levels After an Acute Drug Challenge
NCT01577706 (7) [back to overview]Left Temporal: Percent Change in GABA Levels After an Acute Drug Challenge
NCT01577706 (7) [back to overview]Left Thalamus: Percent Change in GABA Levels After an Acute Drug Challenge
NCT01577706 (7) [back to overview]Parieto-Occipital: Percent Change in GABA Levels After an Acute Drug Challenge
NCT01577706 (7) [back to overview]Right Basal-Ganglia: Percent Change in GABA Levels After an Acute Drug Challenge
NCT02351115 (6) [back to overview]Correlation of Plasma Concentrations of Alprazolam With Pharmacodynamic Effects on Visual Analog Scale (Sedated-Alert)
NCT02351115 (6) [back to overview]Correlation of Plasma Concentrations of Alprazolam With Pharmacodynamic Effects on Visual Analog Scale (Sleepy-Awake)
NCT02351115 (6) [back to overview]Maximum Observed Change From Pretreatment Baseline in the Standardized Photosensitivity Range (SPR)
NCT02351115 (6) [back to overview]Maximum Sedation Using Visual Analog Scale (Sedated-Alert)
NCT02351115 (6) [back to overview]Maximum Sedation Using Visual Analog Scale (Sleepy-Awake)
NCT02351115 (6) [back to overview]Correlation of Plasma Concentrations of Alprazolam With Pharmacodynamic Effects on Standardized Photosensitivity Range (SPR)
NCT03012334 (8) [back to overview]Driving Performance Using the CRCDS-MiniSim - Lane Exceedance
NCT03012334 (8) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT03012334 (8) [back to overview]Motivational and Self-Appraisal Visual Analog Scale (VAS)
NCT03012334 (8) [back to overview]Simulated Driving Performance in Healthy Participants as Measured by Standard Deviation of Lateral Position (SDLP) Using the Cognitive Research Corporation Driving Simulator-MiniSim (CRCDS-MiniSim)
NCT03012334 (8) [back to overview]Percentage of Participants With Self-Reported Readiness to Drive
NCT03012334 (8) [back to overview]Number of Correct Responses in Driving Performance Using CogScreen Symbol Digit Coding (SDC) Test
NCT03012334 (8) [back to overview]Karolinska Sleepiness Scale (KSS) Score
NCT03012334 (8) [back to overview]Driving Performance Using the CRCDS-MiniSim - Speed Deviation
NCT03286218 (7) [back to overview]PD: Minimum Drug Effects (Emin) Visual Analog Scale (VAS)
NCT03286218 (7) [back to overview]PD: Mean Scores on Drug Similarity VAS Measures
NCT03286218 (7) [back to overview]PK: Area Under the Curve of Lasmiditan From Zero to Infinity (AUC[0-∞])
NCT03286218 (7) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Lasmiditan
NCT03286218 (7) [back to overview]Pharmacodynamics (PD): Maximal Effect Score (Emax) of Bipolar Drug Liking Visual Analog Scale (VAS) Scores
NCT03286218 (7) [back to overview]PD: Maximal Drug Effects (Emax) VAS (Hallucinations)
NCT03286218 (7) [back to overview]PD: Maximal Drug Effects (Emax) Visual Analog Scale (VAS)
NCT03297944 (1) [back to overview]Standard Deviation of Lane Position (SLDP)
NCT03447353 (2) [back to overview]SDLP
NCT03447353 (2) [back to overview]Lane Departures
NCT03478982 (4) [back to overview]Percentage of Participants in Each Treatment Group Achieving Seizure Activity Cessation Within 2 Minutes and no Recurrent Seizure Within 2 Hours
NCT03478982 (4) [back to overview]Percentage of Participants With Secondary Generalization (Evolution to a Complex Partial Seizure and/or a Generalized Tonic-Clonic Seizure)
NCT03478982 (4) [back to overview]Percentage of Participants With Use of Rescue Medication
NCT03478982 (4) [back to overview]Percentage of Participants With Seizure Episode Severity Assessed by Seizure Episode Severity Scale
NCT04970342 (2) [back to overview]Standard Deviation of Lateral Position (SDLP)
NCT04970342 (2) [back to overview]Lane Exceedences

Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 8 Weeks

(NCT00266409)
Timeframe: 8 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI2662
Panic: SSRI/SNRI Alone3255

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Change in Severity of Illness From Baseline Using the Clinical Global Impression Improvement (CGI-I) Score After 2 Weeks

The Clinical Global Impression Improvement (CGI-I) scale is a 7 point ordinal scale that assesses how the patient's illness has improved ranging from 'very much improved' to 'very much worse'(see definition of categories in results table). (NCT00266409)
Timeframe: Baseline and 2 weeks

,,,
InterventionParticipants (Number)
Very much improvedmuch improvedminimally improvedNo changeMinimally worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI425279100
GAD: SSRI/SNRI Alone2102018610
Panic: Niravam+SSRI/SNRI6385317410
Panic: SSRI/SNRI Alone1233540710

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Change in Severity of Illness From Baseline Using the Clinical Global Impression - Improvement (CGI-I) Score at Endpoint During the 8 Week Treatment Period

The Clinical Global Impression Improvement (CGI-I) scale is a 7 point ordinal scale that assesses how the patient's illness has improved ranging from 'very much improved' to 'very much worse'(see definition of categories in results table). Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: Baseline and at endpoint during the 8 week treatment period

,,,
Interventionparticipants (Number)
Very much improvedMuch improvedMinimally improvedNo changeMinimally worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1429128210
GAD: SSRI/SNRI Alone1223165210
Panic: Niravam+SSRI/SNRI3147307610
Panic: SSRI/SNRI Alone27312425231

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Change in Severity of Illness From Baseline Using the Clinical Global Impression - Improvement (CGI-I) Score After 8 Weeks

The Clinical Global Impression Improvement (CGI-I) scale is a 7 point ordinal scale that assesses how the patient's illness has improved ranging from 'very much improved' to 'very much worse'(see definition of categories in results table). (NCT00266409)
Timeframe: Baseline and 8 weeks

,,,
Interventionparticipants (Number)
Very much improvedMuch improvedMinimally improvedNo changeMinimally worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1425115110
GAD: SSRI/SNRI Alone1222134000
Panic: Niravam+SSRI/SNRI2844163200
Panic: SSRI/SNRI Alone27271919121

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Change in Severity of Illness From Baseline Using the Clinical Global Impression - Improvement (CGI-I) Score After 4 Weeks

The Clinical Global Impression Improvement (CGI-I) scale is a 7 point ordinal scale that assesses how the patient's illness has improved ranging from 'very much improved' to 'very much worse'(see definition of categories in results table). (NCT00266409)
Timeframe: Baseline and 4 weeks

,,,
Interventionparticipants (Number)
Very much improvedMuch improvedMinimally improvedNo changeMinimally worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1226137101
GAD: SSRI/SNRI Alone118179100
Panic: Niravam+SSRI/SNRI1840357610
Panic: SSRI/SNRI Alone5402319921

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Change From Baseline in the Total HAM-A Score at Endpoint During the 8 Week Treatment Period

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: Baseline and at endpoint during the 8 week treatment period

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-17.3
Panic: SSRI/SNRI Alone-14.3
GAD : Niravam+SSRI/SNRI-13.6
GAD: SSRI/SNRI Alone-11.5

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Change From Baseline in the Total HAM-A Score After 8 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 8 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-18.5
Panic: SSRI/SNRI Alone-16.6
GAD : Niravam+SSRI/SNRI-13.9
GAD: SSRI/SNRI Alone-12.3

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Change From Baseline in the Total HAM-A Score After 7 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 7 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-17.7
Panic: SSRI/SNRI Alone-15.6
GAD : Niravam+SSRI/SNRI-13.3
GAD: SSRI/SNRI Alone-11.3

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Change From Baseline in the Total HAM-A Score After 6 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 6 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-17.7
Panic: SSRI/SNRI Alone-15.1
GAD : Niravam+SSRI/SNRI-13.4
GAD: SSRI/SNRI Alone-11.0

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Change From Baseline in the Total HAM-A Score After 5 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 5 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-16.7
Panic: SSRI/SNRI Alone-14.4
GAD : Niravam+SSRI/SNRI-13.3
GAD: SSRI/SNRI Alone-10.3

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Change From Baseline in the Total HAM-A Score After 4 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 4 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-15.2
Panic: SSRI/SNRI Alone-13.7
GAD : Niravam+SSRI/SNRI-12.9
GAD: SSRI/SNRI Alone-8.3

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Change From Baseline in the Total HAM-A Score After 3 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 3 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-14.3
Panic: SSRI/SNRI Alone-12.9
GAD : Niravam+SSRI/SNRI-10.9
GAD: SSRI/SNRI Alone-9.5

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 7 Weeks

(NCT00266409)
Timeframe: 7 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI3256
Panic: SSRI/SNRI Alone3154

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 6 Weeks

(NCT00266409)
Timeframe: 6 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI3657
Panic: SSRI/SNRI Alone3351

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 5 Weeks

(NCT00266409)
Timeframe: 5 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI3560
Panic: SSRI/SNRI Alone4044

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 4 Weeks

(NCT00266409)
Timeframe: 4 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI4360
Panic: SSRI/SNRI Alone4350

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 3 Weeks

(NCT00266409)
Timeframe: 3 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI4166
Panic: SSRI/SNRI Alone3758

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Change From Baseline in HAM-A-psychic Factors Subscore After 8 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 8 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-9.9
Panic: SSRI/SNRI Alone-8.9
GAD : Niravam+SSRI/SNRI-8.5
GAD: SSRI/SNRI Alone-8.5

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Change From Baseline in the Total HAM-A Score After 2 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 2 Weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-11.6
Panic: SSRI/SNRI Alone-8.2
GAD : Niravam+SSRI/SNRI-10.0
GAD: SSRI/SNRI Alone-6.1

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Change From Baseline in the Total HAM-A Score After 1 Week

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum HAM-A Score is 56. (NCT00266409)
Timeframe: Baseline and 1 week

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-9.3
Panic: SSRI/SNRI Alone-5.8
GAD : Niravam+SSRI/SNRI-7.8
GAD: SSRI/SNRI Alone-4.6

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Change From Baseline in HAM-A-somatic Subscore at Endpoint During the 8 Week Treatment Period

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: Baseline and at endpoint during the 8 week treatment period

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-8.2
Panic: SSRI/SNRI Alone-6.7
GAD : Niravam+SSRI/SNRI-5.6
GAD: SSRI/SNRI Alone-3.6

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Change From Baseline in HAM-A-somatic Subscore After 8 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 8 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-8.6
Panic: SSRI/SNRI Alone-7.7
GAD : Niravam+SSRI/SNRI-5.5
GAD: SSRI/SNRI Alone-3.8

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 4 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 4 weeks

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI3717
GAD: SSRI/SNRI Alone2523
Panic: Niravam+SSRI/SNRI5839
Panic: SSRI/SNRI Alone5634

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Change From Baseline in HAM-A-somatic Subscore After 7 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 7 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-8.1
Panic: SSRI/SNRI Alone7.2
GAD : Niravam+SSRI/SNRI-5.2
GAD: SSRI/SNRI Alone-3.7

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Change From Baseline in HAM-A-somatic Subscore After 6 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 6 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-8.3
Panic: SSRI/SNRI Alone-6.8
GAD : Niravam+SSRI/SNRI-4.7
GAD: SSRI/SNRI Alone-3.8

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 2 Weeks

(NCT00266409)
Timeframe: 2 weeks

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI6054
Panic: SSRI/SNRI Alone6046

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) After 1 Week

(NCT00266409)
Timeframe: 1 week

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI7642
Panic: SSRI/SNRI Alone6943

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Cumulative Percent of Participants Showing a Response in the Symptoms of Anxiety (Decrease in Total Hamilton Anxiety (HAM-A) -Score of >=50%) in the Per Protocol Population (Kaplan-Meier-estimates)

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Total possible score is 56. Kaplan-Meier-analysis was performed and Kaplan-Meier estimates (cumulative percent of subjects responding) are presented. (NCT00266409)
Timeframe: 10 weeks

,,,
Interventioncumulative percent of responders (Number)
Week 1Week 2Week 3Week 4Week 5Week 6Week 7Week 8Week 9 to 10
GAD : Niravam+SSRI/SNRI1.8933.9652.8358.4967.9271.7077.7079.9386.62
GAD: SSRI/SNRI Alone2.0430.7853.1667.2171.8979.5679.5679.5682.48
Panic: Niravam+SSRI/SNRI1.9235.5851.2363.1875.4577.5979.8380.9586.60
Panic: SSRI/SNRI Alone0.9424.5341.5454.1967.5971.9475.7778.3284.82

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Cumulative Percent of Participants Showing a Response in the Symptoms of Anxiety (Decrease in Total Hamilton Anxiety (HAM-A) -Score of >=50%) in the Intent-to-treat Population (Kaplan-Meier-estimates)

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Thus total possible score is 56. Kaplan-Meier-analysis was performed and Kaplan-Meier estimates (cumulative percent of subjects responding) are presented. (NCT00266409)
Timeframe: 10 weeks

,,,
Interventioncumulative percent of responders (Number)
Week 1Week 2Week 3Week 4Week 5Week 6Week 7Week 8Weeks 9 to 10
GAD : Niravam+SSRI/SNRI1.4932.9351.2257.3266.4769.6674.6676.4783.82
GAD: SSRI/SNRI Alone1.6127.5248.8962.1465.9271.9473.9473.9476.11
Panic: Niravam+SSRI/SNRI1.603.2045.8359.2269.6871.5774.5976.6283.30
Panic: SSRI/SNRI Alone0.8321.7339.4352.4065.9969.7974.1176.2782.20

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) at Endpoint During the 8 Week Treatment Period

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: at endpoint during the 8 week treatment period

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI4420
GAD: SSRI/SNRI Alone4019
Panic: Niravam+SSRI/SNRI7839
Panic: SSRI/SNRI Alone7443

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 8 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 8 weeks

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI3815
GAD: SSRI/SNRI Alone3512
Panic: Niravam+SSRI/SNRI6123
Panic: SSRI/SNRI Alone6222

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 7 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 7 weeks

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI3716
GAD: SSRI/SNRI Alone3415
Panic: Niravam+SSRI/SNRI6023
Panic: SSRI/SNRI Alone5725

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 6 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 6 weeks

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI3116
GAD: SSRI/SNRI Alone3215
Panic: Niravam+SSRI/SNRI6324
Panic: SSRI/SNRI Alone5625

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 5 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 5 weeks

,,,
Interventionparticipants (Number)
ResponseNon Response
GAD : Niravam+SSRI/SNRI3318
GAD: SSRI/SNRI Alone3018
Panic: Niravam+SSRI/SNRI5930
Panic: SSRI/SNRI Alone5130

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 3 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 3 weeks

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI3325
GAD: SSRI/SNRI Alone3121
Panic: Niravam+SSRI/SNRI5645
Panic: SSRI/SNRI Alone5141

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 2 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 2 weeks

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI3031
GAD: SSRI/SNRI Alone2330
Panic: Niravam+SSRI/SNRI4860
Panic: SSRI/SNRI Alone3865

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Clinical Response (Decrease From Baseline in Total HAM-A-score >=50%) After 1 Week

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). (NCT00266409)
Timeframe: 1 week

,,,
Interventionparticipants (Number)
ResponseNo Response
GAD : Niravam+SSRI/SNRI2241
GAD: SSRI/SNRI Alone1641
Panic: Niravam+SSRI/SNRI3973
Panic: SSRI/SNRI Alone2485

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Change From Baseline in HAM-A-somatic Subscore After 3 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 3 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-7.0
Panic: SSRI/SNRI Alone-6.1
GAD : Niravam+SSRI/SNRI-4.5
GAD: SSRI/SNRI Alone-3.4

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Change From Baseline in HAM-A-somatic Subscore After 2 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 2 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-5.6
Panic: SSRI/SNRI Alone-3.7
GAD : Niravam+SSRI/SNRI-4.2
GAD: SSRI/SNRI Alone-2.0

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Change From Baseline in HAM-A-somatic Subscore After 1 Week

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 1 week

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-4.4
Panic: SSRI/SNRI Alone-2.9
GAD : Niravam+SSRI/SNRI-3.3
GAD: SSRI/SNRI Alone-1.4

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Change From Baseline in HAM-A-psychic Factors Subscore at Endpoint During the 8 Week Treatment Period

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: Baseline and at endpoint during the 8 week treatment period

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-9.1
Panic: SSRI/SNRI Alone-7.6
GAD : Niravam+SSRI/SNRI-7.9
GAD: SSRI/SNRI Alone-7.9

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Change From Baseline in HAM-A-psychic Factors Subscore After 7 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 7 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-9.6
Panic: SSRI/SNRI Alone-8.4
GAD : Niravam+SSRI/SNRI-8.1
GAD: SSRI/SNRI Alone-7.6

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Change From Baseline in HAM-A-psychic Factors Subscore After 6 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 6 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-9.4
Panic: SSRI/SNRI Alone-8.3
GAD : Niravam+SSRI/SNRI-8.7
GAD: SSRI/SNRI Alone-7.2

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Change From Baseline in HAM-A-psychic Factors Subscore After 5 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 5 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-8.7
Panic: SSRI/SNRI Alone-7.7
GAD : Niravam+SSRI/SNRI-7.9
GAD: SSRI/SNRI Alone-6.8

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Change From Baseline in HAM-A-somatic Subscore After 5 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 5 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-8.0
Panic: SSRI/SNRI Alone-6.8
GAD : Niravam+SSRI/SNRI-5.4
GAD: SSRI/SNRI Alone-3.4

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Change From Baseline in HAM-A-psychic Factors Subscore After 4 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 4 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-7.7
Panic: SSRI/SNRI Alone-7.4
GAD : Niravam+SSRI/SNRI-7.8
GAD: SSRI/SNRI Alone-5.9

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Change From Baseline in HAM-A-psychic Factors Subscore After 3 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 3 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-7.3
Panic: SSRI/SNRI Alone-6.8
GAD : Niravam+SSRI/SNRI-6.4
GAD: SSRI/SNRI Alone-6.1

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Change From Baseline in HAM-A-psychic Factors Subscore After 2 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 2 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-6.0
Panic: SSRI/SNRI Alone-4.5
GAD : Niravam+SSRI/SNRI-5.8
GAD: SSRI/SNRI Alone-4.1

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Change From Baseline in HAM-A-psychic Factors Subscore After 1 Week

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the psychic factors subscore is 4. (NCT00266409)
Timeframe: Baseline and 1 week

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-4.9
Panic: SSRI/SNRI Alone-2.9
GAD : Niravam+SSRI/SNRI-4.5
GAD: SSRI/SNRI Alone-3.3

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Change From Baseline in HAM-A-insomnia Subscore at Endpoint During the 8 Week Treatment Period

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: Baseline and at endpoint during the 8 week treatment period

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.6
Panic: SSRI/SNRI Alone-1.4
GAD : Niravam+SSRI/SNRI-1.5
GAD: SSRI/SNRI Alone-1.3

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Change From Baseline in HAM-A-insomnia Subscore After 8 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 8 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.6
Panic: SSRI/SNRI Alone-1.6
GAD : Niravam+SSRI/SNRI-1.6
GAD: SSRI/SNRI Alone-1.3

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Change From Baseline in HAM-A-insomnia Subscore After 7 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 7 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.5
Panic: SSRI/SNRI Alone-1.4
GAD : Niravam+SSRI/SNRI-1.6
GAD: SSRI/SNRI Alone-1.2

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Change From Baseline in HAM-A-somatic Subscore After 4 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the somatic subscore is 4. (NCT00266409)
Timeframe: Baseline and 4 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-7.5
Panic: SSRI/SNRI Alone-6.4
GAD : Niravam+SSRI/SNRI-5.1
GAD: SSRI/SNRI Alone-2.3

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Change From Baseline in HAM-A-insomnia Subscore After 6 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 6 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.4
Panic: SSRI/SNRI Alone-1.5
GAD : Niravam+SSRI/SNRI-1.6
GAD: SSRI/SNRI Alone-1.1

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Change From Baseline in HAM-A-insomnia Subscore After 5 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 5 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.3
Panic: SSRI/SNRI Alone-1.4
GAD : Niravam+SSRI/SNRI-1.5
GAD: SSRI/SNRI Alone-1.1

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Presence of Any Panic Attack(s) (for Subjects With Panic Disorder Only) at Endpoint During the 8 Week Treatment Period

Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: at endpoint during the 8 week treatment period

,
Interventionparticipants (Number)
Any panic attackNo panic attack
Panic: Niravam+SSRI/SNRI4776
Panic: SSRI/SNRI Alone5070

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Change From Baseline in HAM-A-insomnia Subscore After 4 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 4 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.3
Panic: SSRI/SNRI Alone-1.4
GAD : Niravam+SSRI/SNRI-1.6
GAD: SSRI/SNRI Alone-1.1

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Change From Baseline in HAM-A-insomnia Subscore After 3 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 3 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.2
Panic: SSRI/SNRI Alone-1.1
GAD : Niravam+SSRI/SNRI-1.4
GAD: SSRI/SNRI Alone-1.2

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Change From Baseline in HAM-A-insomnia Subscore After 2 Weeks

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 2 weeks

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-1.0
Panic: SSRI/SNRI Alone-0.9
GAD : Niravam+SSRI/SNRI-1.2
GAD: SSRI/SNRI Alone-0.6

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Change From Baseline in HAM-A-insomnia Subscore After 1 Week

The Hamilton Anxiety (HAM-A) Rating scale is a test of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe). Maximum score of the insomnia subscore is 4. (NCT00266409)
Timeframe: Baseline and 1 week

InterventionUnits on a scale (Mean)
Panic: Niravam+SSRI/SNRI-0.9
Panic: SSRI/SNRI Alone-0.6
GAD : Niravam+SSRI/SNRI-1.0
GAD: SSRI/SNRI Alone-0.5

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score at Endpoint During the 8 Week Treatment Period

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). Endpoint is last observed value during the 8 week treatment period. (NCT00266409)
Timeframe: at endpoint during the 8 week treatment period

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI21141712110
GAD: SSRI/SNRI Alone14151411132
Panic: Niravam+SSRI/SNRI34362720330
Panic: SSRI/SNRI Alone25273030061

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 1 Week

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 1 week

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI3102720100
GAD: SSRI/SNRI Alone07931321
Panic: Niravam+SSRI/SNRI7243539211
Panic: SSRI/SNRI Alone054046650

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 2 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect. (NCT00266409)
Timeframe: 2 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI5212113011
GAD: SSRI/SNRI Alone472017321
Panic: Niravam+SSRI/SNRI10303429340
Panic: SSRI/SNRI Alone2163837353

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 3 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 3 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI10211612110
GAD: SSRI/SNRI Alone2142213011
Panic: Niravam+SSRI/SNRI22233324212
Panic: SSRI/SNRI Alone7212831350

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 4 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 4 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1319165220
GAD: SSRI/SNRI Alone614188111
Panic: Niravam+SSRI/SNRI18382614222
Panic: SSRI/SNRI Alone13242028431

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 5 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 5 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1319184000
GAD: SSRI/SNRI Alone5201012101
Panic: Niravam+SSRI/SNRI21321616360
Panic: SSRI/SNRI Alone10271919261

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 6 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 6 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1520114000
GAD: SSRI/SNRI Alone615168201
Panic: Niravam+SSRI/SNRI22292316210
Panic: SSRI/SNRI Alone16241718252

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 7 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 7 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI1223118200
GAD: SSRI/SNRI Alone82379111
Panic: Niravam+SSRI/SNRI23281715320
Panic: SSRI/SNRI Alone21241718112

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Subject's Assessment of Treatment Effect as Measured by the Patient Global Impression (PGI) Score After 8 Weeks

The Patient Global Impression (PGI) scale is a 7 point ordinal scale that rates subject's assessment of treatment effect ranging from 'very much better' to 'very much worse' (see categories in results tables). (NCT00266409)
Timeframe: 8 weeks

,,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterUnchangedA little worseMuch worseVery much worse
GAD : Niravam+SSRI/SNRI2014138100
GAD: SSRI/SNRI Alone1313127111
Panic: Niravam+SSRI/SNRI28281713200
Panic: SSRI/SNRI Alone23222116031

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Clinician-Administered PTSD Scale (CAPS)

Scores may range from 0 (no symptoms) to 136 (severe symptoms). The score is based on the first 17 CAPS items administered. (NCT00356278)
Timeframe: Baseline

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine85.3
VRE Therapy and Alprazolam88
VRE Therapy and Placebo82.6

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PTSD Symptom Scale Self-Report

PTSD Symptom Scale - Self-Report Version (PSS-SR) is a 17-item self-reported questionnaire to assess symptoms of PTSD. Each of the 17 items describe PTSD symptoms which respondents rate in terms of their frequency or severity using a Likert-type scale ranging from 0 (not at all or only one time) to 3 (almost always or five or more times per week). Ratings on items are summed to create three subscales, including re-experiencing, avoidance, and arousal, as well as a total score (that ranges from 0 to 51). The total score higher than 13 indicates on likelihood of PTSD. (NCT00356278)
Timeframe: Month 12

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine22.6
VRE Therapy and Alprazolam24.2
VRE Therapy and Placebo21.7

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PTSD Symptom Scale Self-Report

PTSD Symptom Scale - Self-Report Version (PSS-SR) is a 17-item self-reported questionnaire to assess symptoms of PTSD. Each of the 17 items describe PTSD symptoms which respondents rate in terms of their frequency or severity using a Likert-type scale ranging from 0 (not at all or only one time) to 3 (almost always or five or more times per week). Ratings on items are summed to create three subscales, including re-experiencing, avoidance, and arousal, as well as a total score (that ranges from 0 to 51). The total score higher than 13 indicates on likelihood of PTSD. (NCT00356278)
Timeframe: Month 3

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine25.2
VRE Therapy and Alprazolam26.1
VRE Therapy and Placebo21.4

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PTSD Symptom Scale Self-Report

PTSD Symptom Scale - Self-Report Version (PSS-SR) is a 17-item self-reported questionnaire to assess symptoms of PTSD. Each of the 17 items describe PTSD symptoms which respondents rate in terms of their frequency or severity using a Likert-type scale ranging from 0 (not at all or only one time) to 3 (almost always or five or more times per week). Ratings on items are summed to create three subscales, including re-experiencing, avoidance, and arousal, as well as a total score (that ranges from 0 to 51). The total score higher than 13 indicates on likelihood of PTSD. (NCT00356278)
Timeframe: Month 6

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine24.1
VRE Therapy and Alprazolam26.3
VRE Therapy and Placebo20.0

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PTSD Symptom Scale Self-Report

PTSD Symptom Scale - Self-Report Version (PSS-SR) is a 17-item self-reported questionnaire to assess symptoms of PTSD. Each of the 17 items describe PTSD symptoms which respondents rate in terms of their frequency or severity using a Likert-type scale ranging from 0 (not at all or only one time) to 3 (almost always or five or more times per week). Ratings on items are summed to create three subscales, including re-experiencing, avoidance, and arousal, as well as a total score (that ranges from 0 to 51). The total score higher than 13 indicates on likelihood of PTSD. (NCT00356278)
Timeframe: Posttreatment, 8 weeks

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine27.1
VRE Therapy and Alprazolam25.6
VRE Therapy and Placebo24.2

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Clinician-Administered PTSD Scale (CAPS)

Scores may range from 0 (no symptoms) to 136 (severe symptoms). The score is based on the first 17 CAPS items administered. (NCT00356278)
Timeframe: Month 12

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine48.0
VRE Therapy and Alprazolam57.2
VRE Therapy and Placebo48.4

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Clinician-Administered PTSD Scale (CAPS)

Scores may range from 0 (no symptoms) to 136 (severe symptoms). The score is based on the first 17 CAPS items administered. (NCT00356278)
Timeframe: Month 3

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine60.3
VRE Therapy and Alprazolam66.8
VRE Therapy and Placebo51.5

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Clinician-Administered PTSD Scale (CAPS)

Scores may range from 0 (no symptoms) to 136 (severe symptoms). The score is based on the first 17 CAPS items administered. (NCT00356278)
Timeframe: Month 6

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine56.0
VRE Therapy and Alprazolam63.4
VRE Therapy and Placebo46.9

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Clinician-Administered PTSD Scale (CAPS)

Scores may range from 0 (no symptoms) to 136 (severe symptoms). The score is based on the first 17 CAPS items administered. (NCT00356278)
Timeframe: Posttreatment, 8 weeks

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine65.9
VRE Therapy and Alprazolam69.6
VRE Therapy and Placebo63.8

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PTSD Symptom Scale Self-Report

PTSD Symptom Scale - Self-Report Version (PSS-SR) is a 17-item self-reported questionnaire to assess symptoms of PTSD. Each of the 17 items describe PTSD symptoms which respondents rate in terms of their frequency or severity using a Likert-type scale ranging from 0 (not at all or only one time) to 3 (almost always or five or more times per week). Ratings on items are summed to create three subscales, including re-experiencing, avoidance, and arousal, as well as a total score (that ranges from 0 to 51). The total score higher than 13 indicates on likelihood of PTSD. (NCT00356278)
Timeframe: Baseline

Interventionunits on a scale (Mean)
VRE Therapy and D-cycloserine32.9
VRE Therapy and Alprazolam32.4
VRE Therapy and Placebo32.4

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Number of Participants With Doxapram-induced Panic Attack

doxapram-induced panic attack of sufficient intensity (DIPASI) defined as a 10 or greater increase from baseline in the acute panic inventory (API) (NCT00477451)
Timeframe: 0 to 2 hours

InterventionParticipants (Count of Participants)
RCT Placebo14
RCT Alprazolam 1 mg9

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Borg Max Change From Baseline

"Subjects asked to Point to the number (0 to 10) which matches how breathless you feel now where 0=nothing at all to 10=very, very strong" (NCT00477451)
Timeframe: 45 minutes

Interventionunits on a scale (Mean)
RCT Placebo5.73
RCT Alprazolam 1 mg4.63

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Duration of the Doxapram-induced Panic Attack

Length of time from the doxapram injection to the time at which the acute panic inventory (API) value returns to within 10 points of the baseline API value. 0=never exceeded 0, 61=exceeded by more than 10 points still at end of assessment of 60 minutes. Thus each would have a duration whether or not they had a panic attack (DIPASI) (NCT00477451)
Timeframe: 1 hr post-dose

Interventionminutes (Mean)
RCT Placebo12.2
RCT Alprazolam 1 mg9.25

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"Maximum of DEQ Question 2 Rate Your Liking of the Drug Effect at the 10 Time Points (Predose Through 9 Hours)"

"The within patient rank (1-7) of maximum of the Rate your LIKING of the drug effect you are feeling RIGHT NOW; response options range from -4 to +4:~Dislike very much=-4, Dislike quite a bit=-3, Dislike somewhat=-2, Dislike, but not very much=-1, NEUTRAL OR NO EFFECT=0, Like, but not very much=1, Like somewhat=2, Like quite a bit=3, Like very much=4 Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: DEQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo1.607
Oral Alprazolam 1 mg3.500
Oral Alprazolam 2 mg4.536
Oral Alprazolam 4 mg5.536
Inhaled Alprazolam 0.5 mg2.893
Inhaled Alprazolam 1 mg4.250
Inhaled Alprazolam 2 mg5.679

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"EDQ Question Number 7,What Would You be Willing to Pay for Today's Drug?"

"EDQ question number 7, What would you be willing to pay for today's drug?" (NCT00603980)
Timeframe: End of day for each of the 7 crossover treatments

InterventionDollars ($) (Least Squares Mean)
Placebo1.607
Oral Alprazolam 1 mg3.821
Oral Alprazolam 2 mg4.571
Oral Alprazolam 4 mg5.179
Inhaled Alprazolam 0.5 mg2.964
Inhaled Alprazolam 1 mg4.107
Inhaled Alprazolam 2 mg5.750

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"EDQ Question Number 6 Estimate the Amount of Money You Think the Drug You Took Today Would be Worth on the Street."

"EDQ question number 6 (of primary interest), Estimate the amount of money you think the drug you took today would be worth on the street." (NCT00603980)
Timeframe: End of day for each of the 7 crossover treatments

InterventionDollars ($) (Least Squares Mean)
Placebo1.750
Oral Alprazolam 1 mg3.571
Oral Alprazolam 2 mg7.071
Oral Alprazolam 4 mg8.714
Inhaled Alprazolam 0.5 mg2.857
Inhaled Alprazolam 1 mg4.286
Inhaled Alprazolam 2 mg8.571

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"EDQ Question Number 2 Rate Your Overall Liking of the Drug Effect"

"The within patient rank (1-7) of End of Day question number 2 (of primary interest), Rate your overall liking of the drug effect, response options range from -4 to +4:~4=Dislike very much~3=Dislike quite a bit~2=Dislike somewhat~1=Dislike, but not very much 0=NEUTRAL OR NO EFFECT~1=Like, but not very much~2=Like somewhat~3=Like quite a bit~4=Like very much Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: End of day for each of the 7 crossover treatments

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo1.679
Oral Alprazolam 1 mg4.214
Oral Alprazolam 2 mg4.429
Oral Alprazolam 4 mg4.607
Inhaled Alprazolam 0.5 mg2.571
Inhaled Alprazolam 1 mg4.857
Inhaled Alprazolam 2 mg5.643

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Observer Rated Questionnaire 6) Maximum of Confusion/Disorientation

"The within patient rank (1-7) of maximum of the observer rated the subject on Confusion/Disorientation on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo1.929
Oral Alprazolam 1 mg2.821
Oral Alprazolam 2 mg4.893
Oral Alprazolam 4 mg6.429
Inhaled Alprazolam 0.5 mg3.393
Inhaled Alprazolam 1 mg3.107
Inhaled Alprazolam 2 mg5.429

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"EDQ Question Number 1, Rate the Overall Strength of the Drug Effect"

"The within patient rank (1-7) of End of Day question number 1, Rate the overall strength of the drug effect, response options range from 0-4:~0=No drug effect at all~Possible mild effect, but not sure~Definite mild effect~Moderate strong drug effect~Very strong drug effect Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: End of day for each of the 7 crossover treatments

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo1.429
Oral Alprazolam 1 mg3.536
Oral Alprazolam 2 mg4.821
Oral Alprazolam 4 mg5.429
Inhaled Alprazolam 0.5 mg2.893
Inhaled Alprazolam 1 mg4.143
Inhaled Alprazolam 2 mg5.750

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"Maximum of DEQ Question 1 Rate the Strength of the Drug Effect (at the 10 Time Points, Predose Through 9 Hours)"

"The within patient rank (1-7) of Drug Effect Questionnaire question number 1: Rate the STRENGTH of the drug effect you are feeling RIGHT NOW; response options range for 0 to 4:~No drug effect at all=0, Possible mild effect, but not sure=1, Definite mild effect=2, Moderate strong drug effect=3, Very strong drug effect=4 Maximum of the 10 time points (predose through 9 hours) Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: DEQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo1.571
Oral Alprazolam 1 mg3.143
Oral Alprazolam 2 mg4.714
Oral Alprazolam 4 mg5.536
Inhaled Alprazolam 0.5 mg3.036
Inhaled Alprazolam 1 mg4.250
Inhaled Alprazolam 2 mg5.750

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Observer Rated Questionnaire 4) Maximum of Muscle Relaxation Posture

"The within patient rank (1-7) of maximum of the observer rated the subject on muscle relaxation (posture) on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo2.750
Oral Alprazolam 1 mg2.893
Oral Alprazolam 2 mg3.964
Oral Alprazolam 4 mg6.250
Inhaled Alprazolam 0.5 mg2.929
Inhaled Alprazolam 1 mg2.929
Inhaled Alprazolam 2 mg2.929

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Observer Rated Questionnaire 8) Maximum of Drug Strength

"The within patient rank (1-7) of maximum of the observer rated the subject on Drug Strength on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Oral Alprazolam 1 mg2.786
Placebo1.714
Oral Alprazolam 2 mg4.571
Oral Alprazolam 4 mg6.321
Inhaled Alprazolam 0.5 mg3.000
Inhaled Alprazolam 1 mg3.929
Inhaled Alprazolam 2 mg5.679

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Observer Rated Questionnaire 7) Maximum of Stimulation/Arousal

"The within patient rank (1-7) of maximum of the observer rated the subject on Stimulation/Arousal on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo3.964
Oral Alprazolam 1 mg3.964
Oral Alprazolam 2 mg3.964
Oral Alprazolam 4 mg3.964
Inhaled Alprazolam 0.5 mg3.964
Inhaled Alprazolam 1 mg3.964
Inhaled Alprazolam 2 mg4,214

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Observer Rated Questionnaire 5) Maximum of Speech

"The within patient rank (1-7) of maximum of the observer rated the subject on speech on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo2.214
Oral Alprazolam 1 mg2.893
Oral Alprazolam 2 mg4.786
Oral Alprazolam 4 mg6.393
Inhaled Alprazolam 0.5 mg3.071
Inhaled Alprazolam 1 mg3.071
Inhaled Alprazolam 2 mg5.357

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Observer Rated Questionnaire 3) Maximum of Muscle Relaxation Non-locomotor

"The within patient rank (1-7) of maximum of the observer rated the subject on muscle relaxation (non-locomotor) on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

Interventionunits on a scale (Least Squares Mean)
Placebo2.536
Oral Alprazolam 1 mg3.036
Oral Alprazolam 2 mg4.607
Oral Alprazolam 4 mg6.393
Inhaled Alprazolam 0.5 mg2.714
Inhaled Alprazolam 1 mg3.786
Inhaled Alprazolam 2 mg4.929

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Observer Rated Questionnaire 2) Maximum of Muscle Relaxation Locomotor

"The within patient rank (1-7) of maximum of the observer rated the subject on muscle relaxation (locomotor) on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Maximum of the 10 time points (predose through 9 hours) Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo2.464
Oral Alprazolam 1 mg2.964
Oral Alprazolam 2 mg4.643
Oral Alprazolam 4 mg6.357
Inhaled Alprazolam 0.5 mg2.821
Inhaled Alprazolam 1 mg3.571
Inhaled Alprazolam 2 mg5.179

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Observer Rated Questionnaire 1) Maximum of Sedation/Sleepiness

"The within patient rank (1-7) of Maximum of Observer Rated Questionnaire (ORQ): A trained and blinded staff member completed observer ratings as the subject completed the questionnaires and psychomotor assessment testing at each time point.~The observer rated the subject on sedation/sleepiness, muscle relaxation, impaired posture, impaired speech, confusion/disorientation, stimulation/arousal and strength of drug effect on a five-point scale from 0 (indicating normal or no effect) to 4 (indicating extreme drug effect).~Maximum of the 10 time points (predose through 9 hours) Thus a higher rank means a stronger drug effect and a lower rank a lesser drug effect" (NCT00603980)
Timeframe: ORQ was assessed at the 10 time points (predose through 9 hours)

InterventionRank across the 7 treatments (Least Squares Mean)
Placebo2.250
Oral Alprazolam 1 mg3.679
Oral Alprazolam 2 mg4.607
Oral Alprazolam 4 mg4.714
Inhaled Alprazolam 0.5 mg3.929
Inhaled Alprazolam 1 mg4.000
Inhaled Alprazolam 2 mg4.821

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"Response to EDQ Question Number 5, Rate the Degree to Which You Would Like to Take the Drug Again"

"The End of Day Questionnaire (EDQ) is a 7-question computerized instrument in which subjects rate the overall effect of the drug they received that day. The primary outcome measure for this trial is the categorical response to question number 5, Rate the degree to which you would like to take the drug again, with a numerical value assigned to each of the responses allowed: 0=Not at all, 1=A little, 2=Moderately, 3=Quite a bit, 4=Very much" (NCT00603980)
Timeframe: End of day for each of the 7 crossover treatments

Interventionunits on a scale (Least Squares Mean)
Placebo0
Oral Alprazolam 1 mg1.714
Oral Alprazolam 2 mg2.143
Oral Alprazolam 4 mg2.286
Inhaled Alprazolam 0.5 mg1.00
Inhaled Alprazolam 1 mg1.714
Inhaled Alprazolam 2 mg2.214

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Signal Change in Brain Activity in the Amygdala When Viewing Emotional Faces

Extent of activation a brain signal when matching emotional face expressions as a percentage of the brain signal when matching geometric designs. The brain signal is the blood oxygen level dependent signal measured by functional magnetic resonance imaging. (NCT00662259)
Timeframe: 0,1,28 days

,
InterventionPercent signal change in brain acitivity (Mean)
Day 0 (Baseline)Day 1Day 28
Alprazolam.1489.0119.1230
Placebo.1074.1404.1699

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Signal Change in Brain Activity in the Insula When Anticipating the Viewing of Emotional Pictures.

Extent of activation of a brain signal when anticipating the viewing of an emotional picture as a percentage of brain signal when the viewing of an emotional signal is not anticipated. The brain signal is the blood oxygen level dependent signal as measured by functional magnetic resonance imaging. (NCT00662259)
Timeframe: 0,1,28 days

,
InterventionPercent signal change in brain acitivity (Mean)
Day 0 (Baseline)Day 1Day 28
Alprazolam.0707.0458.0596
Placebo.0724.0645.0461

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Score on the Penn State Worry Scale

Measured participant's extent of worry; range 16 - 80, higher scores worse (NCT00662259)
Timeframe: 0, 7, 28 days

,
Interventionscore on a scale (Mean)
Day 0 (Baseline)Day 7Day 28
Alprazolam64.7450.2648.11
Placebo66.7362.4561.36

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Score on the Hamilton Anxiety Scale

Measured participant's general anxiety; range 0 - 56; higher scores worse (NCT00662259)
Timeframe: 0, 7, 28 days

,
Interventionscore on a scale (Mean)
Day 0 (Baseline)Day 7Day 28
Alprazolam27.7913.5810.85
Placebo28.0022.1820.18

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Score on Quick Inventory of Depressive Symptomatology

Measured the level of a participant's depression; 0 - 48; higher scores worse (NCT00662259)
Timeframe: 0, 7, 28 days

,
Interventionscore on a scale (Mean)
Day 0 (Baseline)Day 7Day 28
Alprazolam12.428.056.42
Placebo12.0910.099.09

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Participants´Endpoint Change From Baseline in Clinical Global Impression Severity Scale (CGI-S)

The Clinical Global Impression Severity scale is a 7 point ordinal scale that rates the severity of the patient's illness, assessing on the severity of a patient's mental illness. It ranges from 1 to 7 (1, normal, not at all ill; 2, borderline mentally ill; 3, mildly ill; 4, moderately ill; 5, markedly ill; 6, severely ill; 7, extremely ill). (NCT00803400)
Timeframe: Baseline and 12 weeks

InterventionUnits on a scale (Mean)
Alprazolam4.05
Alprazolam + Aerobic Exercise4.06

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Participants´Endpoint Change From Baseline in Hamilton Anxiety Rating Scale

"The Hamilton Anxiety Rating Scale is a test that consists of 14 items measuring the severity of anxiety symptoms. Each item is rated on a 5-point ordinal scale, ranging from 0 (not present) to 4 (severe).~Each of the 14 items measure both psychic anxiety (mental agitation and psychological distress) and somatic anxiety (physical complaints related to anxiety)with a total score range of 0-56, where 17 indicates mild severity, 18-24 mild to moderate severity, and 25-30 moderate to severe." (NCT00803400)
Timeframe: 12 weeks

InterventionUnits on a scale (Mean)
Alprazolam22.59
Alprazolam + Aerobic Exercise22.73

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Participants´Endpoint Change From Baseline in Clinical Global Impression Improvement Scale (CGI-I)

The Clinical Global Impression Improvement Scale is a 7 point ordinal scale that assesses how much the patient's illness has improved or worsened relative to a baseline state before the intervention. Rated as: 1, very much improved; 2, much improved; 3, minimally improved; 4, no change; 5, minimally worse; 6, much worse; or 7, very much worse. (NCT00803400)
Timeframe: Baseline and 12 weeks

InterventionScore on a scale (Mean)
Alprazolam2.70
Alprazolam + Aerobic Exercise1.86

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Bioequivalence Based on AUC0-t

AUC0-t - Area under the concentration-time curve from time zero to time of last non-zero concentration (NCT00829426)
Timeframe: Blood samples collected over 72 hour period

Interventionng*h/mL (Mean)
Alprazolam620.40
Xanax®663.08

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Bioequivalence Based on AUC0-inf

AUC0-inf - Area under the concentration-time curve from time zero to infinity (extrapolated) (NCT00829426)
Timeframe: Blood samples collected over 72 hour period

Interventionng*h/mL (Mean)
Alprazolam668.79
Xanax®725.34

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Bioequivalence Based on Cmax

Cmax - Maximum Observed Concentration (NCT00829426)
Timeframe: Blood samples collected over 72 hour period

Interventionng/mL (Mean)
Alprazolam24.33
Xanax®23.62

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Cmax - Maximum Observed Concentration

Bioequivalence based on Cmax (NCT00830024)
Timeframe: Blood samples collected over 72 hour period

Interventionng/mL (Mean)
Alprazolam28.79
Xanax XR®28.95

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AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)

Bioequivalence based on AUC0-t (NCT00830024)
Timeframe: Blood samples collected over 72 hour period

Interventionng*h/mL (Mean)
Alprazolam600.24
Xanax XR®626.54

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AUC0-inf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)

Bioequivalence based on AUC0-inf (NCT00830024)
Timeframe: Blood samples collected over 72 hour period

Interventionng*h/mL (Mean)
Alprazolam650.91
Xanax XR®683.25

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Other Subjective Effects- Drug Similarity

Drug similarity VAS is one of the measures of other subjective effects. It assesses the similarity of the drug recently received by the participant on a 100 mm unipolar VAS, where responses are unidirectional and range from a response of 'none' (score of 0 mm= not at all similar) to 'extremely' (score of 100 mm= very similar). Recently received drugs were compared with placebo, benzodiazepines, codeine/morphine, Tetrahydrocannabinol (THC), pseudoephedrine. (NCT00975481)
Timeframe: 12 hours post-dose

,,,,,
Interventionmm (Mean)
Placebo (n=32, 33, 34, 33, 32, 31)Benzodiazepines (n=23, 23, 25, 24, 22, 22)Codeine/Morphine (n=20, 20, 23, 22, 20, 20)THC (n=32, 33, 34, 33, 32, 31)Pseudoephedrine (n=6, 6, 6, 6, 7, 5)
Alprazolam 1 mg10.288.642.745.621.5
Alprazolam 3 mg4.092.746.348.966.5
Dimebon 20 mg61.433.014.721.931.7
Dimebon 40 mg57.842.624.516.230.7
Dimebon 60 mg55.753.028.225.333.4
Placebo56.351.018.521.221.8

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Balance of Effects- Overall Drug Liking VAS: Peak Effect (Maximum Effect [Emax]) and Minimum Effect (Emin)

"Overall drug liking VAS is one of the measures of balance of effects that assesses the participant's global perception of drug liking (that is, effects over the whole course of the drug experience including any carryover effects). A 100 mm bipolar VAS is used to assess response based on a score ranging from 0 mm to 100 mm (0 mm = strong disliking, 50 mm= neither like nor dislike, and 100 mm= strong liking).~Emax is the largest effect score between 6 to 24 hours post-dose. Emin is the smallest effect score between 6 to 24 hours post-dose." (NCT00975481)
Timeframe: 6, 12, 24 hours post-dose

,,,,,
Interventionmm (Mean)
EmaxEmin
Alprazolam 1 mg74.664.5
Alprazolam 3 mg78.062.6
Dimebon 20 mg56.548.2
Dimebon 40 mg55.452.0
Dimebon 60 mg58.151.1
Placebo57.852.5

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Balance of Effects- Good and Bad Effects VAS: Peak Effect (Maximum Effect [Emax]) and Minimum Effect (Emin)

"Good and Bad effects VAS is one of the measures of balance of effects that assesses the effect experienced by the participant on a 100 mm bipolar VAS, anchored in the center with a neutral anchor of neither good nor bad effects (score of 50 mm), on the left with bad effects(score of 0 mm) and on the right with good effects (score of 100 mm).~Emax is largest effect score between 0.5 to 24 hours post-dose. Emin is smallest effect score between 0.5 to 24 hours post-dose." (NCT00975481)
Timeframe: 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

,,,,,
Interventionmm (Mean)
EmaxEmin
Alprazolam 1 mg80.946.7
Alprazolam 3 mg81.938.6
Dimebon 20 mg57.949.3
Dimebon 40 mg56.648.3
Dimebon 60 mg57.648.9
Placebo56.248.0

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Balance of Effects- Drug Liking VAS: Peak Effect (Maximum Effect [Emax]) and Minimum Effect (Emin)

"Drug liking VAS is one of the measures of balance of effects that assesses the degree that a participant likes a drug effect at the time the question is being asked (that is, at the moment). It is scored using a 100 millimeter (mm) bipolar visual analogue scale (VAS) anchored in the center with a neutral anchor of neither like nor dislike (score of 50 mm), on the left with strong disliking (score of 0 mm) and on the right with strong liking (score of 100 mm).~Emax is largest effect score between 0.5 to 24 hours post-dose. Emin is smallest effect score between 0.5 to 24 hours post-dose." (NCT00975481)
Timeframe: 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

,,,,,
Interventionmm (Mean)
EmaxEmin
Alprazolam 1 mg78.645.4
Alprazolam 3 mg82.237.4
Dimebon 20 mg57.248.4
Dimebon 40 mg55.849.0
Dimebon 60 mg58.546.5
Placebo57.847.0

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Sedative Effects- Alertness/Drowsiness: Minimum Effect (Emin)

"Alertness/Drowsiness VAS is one of the measures of sedative effects. It is scored using a 100 mm bipolar VAS anchored in the center with a neutral anchor of neither drowsy nor alert (score of 50 mm), on the left with very drowsy (score of 0 mm) and on the right with very alert (score of 100 mm). Emin is the smallest effect score between 0 to 24 hours post-dose." (NCT00975481)
Timeframe: 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

Interventionmm (Mean)
Placebo42.1
Alprazolam 1 mg14.4
Alprazolam 3 mg8.6
Dimebon 20 mg42.9
Dimebon 40 mg37.7
Dimebon 60 mg38.5

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Sedative Effects- Addiction Research Center Inventory (ARCI) Pentobarbital Chlorpromazine Group (PCAG): Maximum Effect (Emax)

ARCI (PCAG) is one of the measures of sedative effects. It is a set of 15 questions in which each question contributes to total score. Participants indicate their responses by selecting 'False' or 'True'. One point is given for each response that agrees with the scoring direction on scale i.e, true items receive a score of 1 if answer is 'True', false items receive a score of 1 if answer is 'False'. No points are given when answer is opposite to scoring direction. Score range: 0 to 15, higher score indicated higher sedative effects. Emax: largest effect score between 0 to 24 hours post-dose. (NCT00975481)
Timeframe: 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

InterventionUnits on Scale (Mean)
Placebo4.7
Alprazolam 1 mg9.9
Alprazolam 3 mg11.5
Dimebon 20 mg5.3
Dimebon 40 mg5.5
Dimebon 60 mg5.5

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Balance of Effects- Subjective Drug Value (SDV): Maximum Effect (Emax)

SDV is one of measures of balance of effects. It is a proxy measure of reinforcing efficacy that involves a series of independent, theoretical forced choices between drug administered and different monetary values. Participants were asked to choose between receiving another dose of same drug or an envelope containing specified amount of money, but they did not receive drug or money as described. Possible score range from 0.25 to 50. Higher score range indicates higher SDV. Emax: largest effect score between 6-24 hours post-dose. (NCT00975481)
Timeframe: 6, 12, 24 hrs post-dose

InterventionDollar (Mean)
Placebo4.805
Alprazolam 1 mg19.621
Alprazolam 3 mg25.551
Dimebon 20 mg6.098
Dimebon 40 mg3.836
Dimebon 60 mg4.573

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Positive Effects- High VAS: Peak Effect (Maximum Effect [Emax])

"High VAS is one of the measures of positive effects that assesses the effect experienced by the participant on a 100 mm unipolar VAS, where responses are unidirectional and range from a response of 'none' (score of 0 mm= definitely not) to 'extremely' (score of 100 mm= definitely so).~Emax is largest effect score between 0 to 24 hours." (NCT00975481)
Timeframe: 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

Interventionmm (Mean)
Placebo30.4
Alprazolam 1 mg77.1
Alprazolam 3 mg88.0
Dimebon 20 mg25.9
Dimebon 40 mg29.9
Dimebon 60 mg35.8

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Positive Effects- Good Drug Effects: Peak Effect (Maximum Effect [Emax])

"Good drug effects VAS is one of the measures of positive effects that assesses the effect experienced by the participant on a 100 mm unipolar VAS, where responses are unidirectional and range from a response of 'none' (score of 0 mm= definitely not) to 'extremely' (score of 100 mm= definitely so).~Emax is the largest effect score between 0.5 to 24 hours post-dose." (NCT00975481)
Timeframe: 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

Interventionmm (Mean)
Placebo35.2
Alprazolam 1 mg81.2
Alprazolam 3 mg84.7
Dimebon 20 mg34.4
Dimebon 40 mg32.0
Dimebon 60 mg39.7

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Positive Effects- Addiction Research Center Inventory (ARCI) Morphine Benzedrine Group (MBG): Maximum Effect (Emax)

ARCI (MBG) is one of the measures of positive effects. It is a set of 16 questions in which each question contributes to total score. Participants indicate their responses by selecting 'False' or 'True'. One point is given for each response that agrees with the scoring direction on scale i.e, true items receive a score of 1 if answer is 'True', false items receive a score of 1 if answer is 'False'. No points are given when the answer is opposite to the scoring direction. Score range: 0 to 16, higher score indicated positive effects. Emax: largest effect score between 0 to 24 hours post-dose. (NCT00975481)
Timeframe: 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8 12, 24 hours post-dose

InterventionUnits on scale (Mean)
Placebo3.2
Alprazolam 1 mg6.2
Alprazolam 3 mg8.1
Dimebon 20 mg3.5
Dimebon 40 mg3.6
Dimebon 60 mg3.5

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Other Subjective Effects- Any Drug Effects: Peak Effect (Maximum Effect [Emax])

Any drug effects VAS is one of the measures of other subjective effects. It assesses the effect experienced by the participant on a 100 mm unipolar VAS, where responses are unidirectional and range from a response of 'none' (score of 0 mm= definitely not) to 'extremely' (score of 100 mm= definitely so). Emax is the largest effect score between 0.5 to 24 hours post-dose. (NCT00975481)
Timeframe: 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

Interventionmm (Mean)
Placebo37.2
Alprazolam 1 mg84.0
Alprazolam 3 mg88.7
Dimebon 20 mg37.5
Dimebon 40 mg33.4
Dimebon 60 mg44.4

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Negative Effects- Bad Drug Effects: Peak Effect (Maximum Effect [Emax])

"Bad effects VAS is one of the measures of negative effects that assesses the effect experienced by the participant on a 100 mm unipolar VAS, where responses are unidirectional and range from a response of 'none' (score of 0 mm= definitely not) to 'extremely' (score of 100 mm= definitely so).~Emax is largest effect score between 0.5 to 24 hrs." (NCT00975481)
Timeframe: 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

Interventionmm (Mean)
Placebo17.2
Alprazolam 1 mg33.9
Alprazolam 3 mg44.6
Dimebon 20 mg15.9
Dimebon 40 mg16.8
Dimebon 60 mg19.7

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Negative Effects- Addiction Research Center Inventory (ARCI) Lysergic Acid Diethylamide (LSD): Maximum Effect (Emax)

ARCI (LSD) is one of the measures of negative effects. It is a set of 14 questions in which each question contributes to total score. Participants indicate their responses by selecting 'False' or 'True'. One point is given for each response that agrees with scoring direction on scale i.e, true items receive a score of 1 if answer is 'True', false items receive a score of 1 if answer is 'False'. No points are given when the answer is opposite to scoring direction. Score range: 0 to 14, higher score indicated higher negative effects. Emax: largest effect score between 0 to 24 hours post-dose. (NCT00975481)
Timeframe: 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

InterventionUnits on Scale (Mean)
Placebo3.8
Alprazolam 1 mg4.9
Alprazolam 3 mg7.0
Dimebon 20 mg3.8
Dimebon 40 mg3.8
Dimebon 60 mg3.6

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Balance of Effects- Take Drug Again VAS: Peak Effect (Maximum Effect [Emax])

"Take drug again VAS is one of the measures of balance of effects. It is a subjective assessment of the degree to which a participant would desire to take the drug again if given the opportunity. It is presented on a 100 mm bipolar VAS with score ranging from 0 mm to 100 mm (score of 0 mm = definitely not, 50 mm = do not care, and 100 mm = definitely so).~Emax is largest effect score between 6 hours to 24 hours." (NCT00975481)
Timeframe: 6, 12, 24 hours post-dose

Interventionmm (Mean)
Placebo53.9
Alprazolam 1 mg77.5
Alprazolam 3 mg83.2
Dimebon 20 mg47.6
Dimebon 40 mg50.4
Dimebon 60 mg52.5

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Other Subjective Effects- Addiction Research Center Inventory (ARCI) Benzedrine Group (BG): Maximum Effect (Emax) and Minimum Effect (Emin)

ARCI (BG) is measure of other subjective effects. It is a set of 13 questions in which each question contributes to total score. Participants select 'False' / 'True' for response. One point given for each response that agrees with scoring direction, true items receive score of 1 if answer 'True', false items receive score of 1 if answer 'False'. No points if answer is opposite to scoring direction. Score range: 0 to 13, higher score indicated higher other subjective effects. Emax: largest effect score between 0 - 24 hours post-dose. Emin: smallest effect score between 0 - 24 hours post-dose. (NCT00975481)
Timeframe: 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose

,,,,,
InterventionUnits on Scale (Mean)
EmaxEmin
Alprazolam 1 mg6.62.5
Alprazolam 3 mg7.21.7
Dimebon 20 mg6.54.4
Dimebon 40 mg6.34.7
Dimebon 60 mg6.44.3
Placebo6.34.8

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Change From Baseline in CogState One Card Learning on Day 6

One card learning: a cognitive test which assessed visual learning. Participants were to remember which cards were previously shown in a task. The outcome measure was accuracy of performance; arcsine transformation of the square root (sqrt) of the proportion of correct responses. Higher scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6

InterventionArcsine [(sqrt) proportion correct] (Least Squares Mean)
Fesoterodine 4 mg-0.0094
Fesoterodine 8 mg0.0151
Aplrazolam 1 mg-0.0880
Placebo-0.0058

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Change From Baseline in Computer Based Objective Cognition Testing (CogState) Detection Speed on Day 6

Detection speed: a cognitive test which assessed psychomotor function. A playing card was presented face up in the center of the screen. As soon as this happened, the participant was to press the 'Yes' key. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses [measured in log10 milliseconds (MS)]. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6

InterventionLog10 MS (Least Squares Mean)
Fesoterodine 4 mg-0.0201
Fesoterodine 8 mg-0.0119
Aplrazolam 1 mg0.0684
Placebo0.0084

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CogState Continuous Paired Associate Learning (CPAL)

CPAL: a cognitive test which assessed visual episodic learning. Participant was to learn and remember picture locations on the screen and was to tap the target on the central location to begin. As each picture was revealed, the participant was to remember where the picture was located and tap that location. The outcome measure was the number of errors made in correctly placing each of the 4 patterns in their location 4 times. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline

InterventionErrors (Mean)
Fesoterodine 4 mg96.33
Fesoterodine 8 mg99.83
Aplrazolam 1 mg89.50
Placebo107.44

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CogState Groton Maze Learning Task (GMLT)

GMLT: a cognitive test which assessed executive function. Participant was shown a 10 x 10 grid of tiles on a computer touch screen. A 28-step pathway was hidden among 100 possible locations. The participant was instructed to move 1 step from the start location and then continue 1 tile at a time, toward the end to find the pathway. The outcome measure was total number of errors made in attempting to learn the same hidden pathway on 5 consecutive trials at a single session. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline

InterventionErrors (Mean)
Fesoterodine 4 mg53.72
Fesoterodine 8 mg58.39
Aplrazolam 1 mg56.83
Placebo52.28

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Change From Baseline in CogState CPAL on Day 6

CPAL: a cognitive test which assessed visual episodic learning. Participant was to learn and remember picture locations on the screen and was to tap the target on the central location to begin. As each picture was revealed, the participant was to remember where the picture was located and tap that location. The outcome measure was the number of errors made in correctly placing each of the 4 patterns in their location 4 times. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6

InterventionErrors (Least Squares Mean)
Fesoterodine 4 mg6.7933
Fesoterodine 8 mg-16.7905
Aplrazolam 1 mg58.2002
Placebo3.1304

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CogState One Card Learning

One card learning: a cognitive test which assessed visual learning. Participants were to remember which cards were previously shown in a task. The outcome measure was accuracy of performance; arcsine transformation of the square root (sqrt) of the proportion of correct responses. Higher scores meant a better performance. (NCT01161472)
Timeframe: Baseline

InterventionArcsine [(sqrt) proportion correct] (Mean)
Fesoterodine 4 mg0.9585
Fesoterodine 8 mg0.9421
Aplrazolam 1 mg0.9531
Placebo0.9302

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Computer Based Objective Cognition Testing (CogState) Detection Speed

Detection speed: a cognitive test which assessed psychomotor function. A playing card was presented face up in the center of the screen. As soon as this happened, the participant was to press the 'Yes' key. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses [measured in log10 milliseconds (MS)]. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline

InterventionLog10 MS (Mean)
Fesoterodine 4 mg2.6333
Fesoterodine 8 mg2.5971
Aplrazolam 1 mg2.6103
Placebo2.5842

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Rey Auditory Verbal Learning Test (RAVLT)

RAVLT evaluates a wide diversity of functions: short-term auditory-verbal memory, rate of learning, learning strategies, retroactive, and proactive interference, presence of confabulation of confusion in memory processes, retention of information, and differences between learning and retrieval. Assessment of RAVLT is between 10 to 15 minutes; Performance variable: the sum of the number of words recalled successfully on the delayed recall trial. Higher score meant a better performance. (NCT01161472)
Timeframe: Baseline

InterventionWords Recalled (Mean)
Fesoterodine 4 mg6.50
Fesoterodine 8 mg6.67
Aplrazolam 1 mg7.22
Placebo6.33

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Rey Auditory Verbal Learning Test (RAVLT) on Day 6

RAVLT evaluates a wide diversity of functions: short-term auditory-verbal memory, rate of learning, learning strategies, retroactive, and proactive interference, presence of confabulation of confusion in memory processes, retention of information, and differences between learning and retrieval. Assessment of RAVLT is between 10 to 15 minutes; Performance variable: the sum of the number of words recalled successfully on the delayed recall trial. Higher score meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6

InterventionWords Recalled (Least Squares Mean)
Fesoterodine 4 mg0.1565
Fesoterodine 8 mg-0.1780
Aplrazolam 1 mg-3.9222
Placebo-0.1119

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Change From Baseline in CogState Groton Maze Learning Task on Day 6

GMLT: a cognitive test which assessed executive function. Participant was shown a 10 x 10 grid of tiles on a computer touch screen. A 28-step pathway was hidden among 100 possible locations. The participant was instructed to move 1 step from the start location and then continue 1 tile at a time, toward the end to find the pathway. The outcome measure was total number of errors made in attempting to learn the same hidden pathway on 5 consecutive trials at a single session. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6

InterventionErrors (Least Squares Mean)
Fesoterodine 4 mg-4.1399
Fesoterodine 8 mg-5.7717
Aplrazolam 1 mg24.7115
Placebo-4.1467

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Change From Baseline in CogState Identification Speed on Day 6

Identification speed: a cognitive test which assessed visual attention. A playing card was presented face up in the center of the screen. As soon as this happened, the participant had to decide whether the card was red or not. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses (measured in log10 MS). Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6

InterventionLog10 MS (Least Squares Mean)
Fesoterodine 4 mg0.0105
Fesoterodine 8 mg0.0057
Aplrazolam 1 mg0.0817
Placebo0.0142

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CogState Identification Speed

Identification speed: a cognitive test which assessed visual attention. A playing card was presented face up in the center of the screen. As soon as this happened, the participant had to decide whether the card was red or not. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses (measured in log10 MS). Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline

InterventionLog10 MS (Mean)
Fesoterodine 4 mg2.7540
Fesoterodine 8 mg2.7672
Aplrazolam 1 mg2.7577
Placebo2.7457

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Sedation Score at One Hour After Premedication

Sedation level was assessed with a 5 point scale (0=alert, 1=arouses to voice, 2=arouses with gentle tactile stimulation, 3=arouses with vigorous tactile stimulation, 4=lack of responsiveness). Minimum score is 0 and Maximum is 4. The lesser the score, the better the outcome. (NCT01486615)
Timeframe: Sedation score at 1 hour after the premedication

Interventionunits on a scale (Median)
Melatonin0.5
Melatonin and Alprazolam1
Alprazolam1
Placebo0

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Amount of Propofol Consumption

Dose of propofol needed for loss of response to verbal command was noted at the time of induction of general anesthesia. The lesser the propofol needed for the loss of response to verbal command, the better the outcome. (NCT01486615)
Timeframe: 1 - 2 hour after premedication

Interventionmg (Mean)
Melatonin79.2
Melatonin and Alprazolam65.5
Alprazolam59.0
Placebo75.8

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Change in VAS Anxiety Score Relative to Baseline After Premedication

VAS (Visual Analogue Score) Anxiety Scale is a 10 cm long scale with two sides, the patient side (front) and the clinicians side (back). The extremes of the front are colored as white and black with a gradual darkening of color from white to black. The back is marked in centimeter from 0 to 10 and 0 correlates with white color (no anxiety at all) and 10 correlates to black color (anxiety as bad as ever can be) on the front. As anxiety is worsened, the color is darker and score is more. The maximum score is 10 and minimum 0. The patient is asked to point on the scale according to his anxiety level. The anxiety score is the correlating number on the clinicians side. The more the reduction in anxiety from baseline, the better the outcome. (NCT01486615)
Timeframe: Change from baseline in VAS anxiety score at 15 minutes after premedication

InterventionCentimeter (Mean)
Melatonin0.35
Melatonin and Alprazolam0.70
Alprazolam0.65
Placebo0.25

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Change in VAS Anxiety Score Relative to Baseline at 30 Minutes After Premedication

VAS (Visual Analogue Score) Anxiety Scale is a 10 cm long scale with two sides, the patient side (front) and the clinicians side (back). The extremes of the front are colored as white and black with a gradual darkening of color from white to black. The back is marked in centimeter from 0 to 10 and 0 correlates with white color (no anxiety at all) and 10 correlates to black color (anxiety as bad as ever can be) on the front. As anxiety is worsened, the color is darker and score is more. The maximum score is 10 and minimum 0. The patient is asked to point on the scale according to his anxiety level. The anxiety score is the correlating number on the clinicians side. The more the reduction in anxiety from baseline, the better the outcome. (NCT01486615)
Timeframe: Changes from baseline in VAS anxiety score at 30 minutes after premedication

Interventioncentimeter (Mean)
Melatonin1.15
Melatonin and Alprazolam1.72
Alprazolam1.62
Placebo0.82

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Change in VAS Anxiety Score Relative to Baseline at One Hour After Premedication

VAS (Visual Analogue Score) Anxiety Scale is a 10 cm long scale with two sides, the patient side (front) and the clinicians side (back). The extremes of the front are colored as white and black with a gradual darkening of color from white to black. The back is marked in centimeter from 0 to 10 and 0 correlates with white color (no anxiety at all) and 10 correlates to black color (anxiety as bad as ever can be) on the front. As anxiety is worsened, the color is darker and score is more. The maximum score is 10 and minimum 0. The patient is asked to point on the scale according to his anxiety level. The anxiety score is the correlating number on the clinicians side. The more the reduction in anxiety from baseline, the better the outcome. (NCT01486615)
Timeframe: Changes from baseline in VAS anxiety score at one hour after premedication

InterventionCentimeter (Mean)
Melatonin1.80
Melatonin and Alprazolam2.92
Alprazolam2.35
Placebo0.85

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Number of Patients With Intact Memory

Number of patients who recalled or recognized the picture number five shown one hour after premedication. The more the number of patients with intact memory, the better the outcome. (NCT01486615)
Timeframe: 24 hour after surgery

InterventionParticipants (Number)
Melatonin13
Melatonin and Alprazolam4
Alprazolam5
Placebo14

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Number of Patients With Loss of Memory for Being Transferred to Operating Room.

Patients were asked whether they recalled the event of being transferred to the operating room before anaesthesia. The lesser the number of patients with amnesia, the better the outcome. (NCT01486615)
Timeframe: 24 hour after surgery

InterventionParticipants (Number)
Melatonin1
Melatonin and Alprazolam5
Alprazolam4
Placebo0

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Orientation Score

Orientation was assessed with a 3 point scale (0=none, 1=orientation in either time or place, 2=orientation in both). Minimum score is 0 and maximum is 2. The lesser the score, the lesser the effect on patients cognition and the better the outcome. (NCT01486615)
Timeframe: Orientation score at one hour after premedication

Interventionunits on a scale (Median)
Melatonin2
Melatonin and Alprazolam2
Alprazolam2
Placebo2

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Right Thalamus: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam2.7219.204.5416.51-1.7812.12
Dextroamphetamine-3.6114.6330.2314.951.6015.51
Placebo6.557.268.39-7.132.8712.69

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Right Temporal: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam-1.4524.2931.06-4.8623.3419.53
Dextroamphetamine2.09-23.1730.2318.5270.8831.58
Placebo14.9321.2648.95-13.9110.8526.78

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Left Basal-Ganglia: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam43.1743.0944.266.573.53-4.57
Dextroamphetamine5.2817.0614.6813.4020.1922.34
Placebo-2.912.1115.59-0.582.665.10

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Left Temporal: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam4.3813.4458.4914.5532.8119.68
Dextroamphetamine6.361.3418.24-6.707.53-20.20
Placebo-10.24-13.82-8.77-10.553.83-2.03

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Left Thalamus: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam23.5739.2923.3012.72-2.1010.79
Dextroamphetamine-12.518.2613.6317.755.4524.16
Placebo-6.80-2.6310.014.47-6.3215.44

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Parieto-Occipital: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam-0.511.9021.954.6410.7818.83
Dextroamphetamine39.69-10.2922.35-17.3336.387.97
Placebo6.09-1.6024.542.1521.7633.46

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Right Basal-Ganglia: Percent Change in GABA Levels After an Acute Drug Challenge

"The primary goal of this study is to assess the efficacy of an advanced spectroscopic imaging protocol in detecting changes in the levels of brain GABA in response to an acute drug challenge.~GABA levels are expressed as a ratio to total creatinine: GABA/Cr percent change = 100*(later timepoint - earlier timepoint) / earlier timepoint" (NCT01577706)
Timeframe: from 45 minutes post-dose to 102 minutes post-dose in 19-minute intervals (4 time points at t1: 45, t2: 64, t3: 83, t4: 102 minutes post-dose)

,,
Interventionpercent change (Median)
t1 to t2: 45min-64mint1 to t3: 45min-83mint1 to t4: 45min-102mint2 to t3: 64min-83mint3 to t4: 83min-102mint2 to t4: 64min-102min
Alprazolam-9.443.0333.5817.08-0.8235.96
Dextroamphetamine38.7867.4137.9221.02-5.9614.20
Placebo18.63-3.97-1.53-9.8811.4610.15

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Correlation of Plasma Concentrations of Alprazolam With Pharmacodynamic Effects on Visual Analog Scale (Sedated-Alert)

Pearson correlation of all paired plasma concentrations of alprazolam (PK) with pharmacodynamic effect on Sedation (PD) for each alprazolam dose (NCT02351115)
Timeframe: Pretreatment, 2, 10, 30 min, 1, 2, 4, and 6 hr post each study drug administration

Interventioncorrelation coefficient (Mean)
Staccato Alprazolam, 0.5 mg-0.350
Staccato Alprazolam, 1 mg-0.567
Staccato Alprazolam, 2 mg-0.623

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Correlation of Plasma Concentrations of Alprazolam With Pharmacodynamic Effects on Visual Analog Scale (Sleepy-Awake)

Pearson correlation of all paired plasma concentrations of alprazolam (PK) with pharmacodynamic effect on Sleepiness (PD) for each alprazolam dose (NCT02351115)
Timeframe: Pretreatment, 2, 10, 30 min, 1, 2, 4, and 6 hr post each study drug administration

Interventioncorrelation coefficient (Mean)
Staccato Alprazolam, 0.5 mg-0.449
Staccato Alprazolam, 1 mg-0.582
Staccato Alprazolam, 2 mg-0.586

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Maximum Observed Change From Pretreatment Baseline in the Standardized Photosensitivity Range (SPR)

Photosensitivity describes the presentation of an epileptiform EEG response (photoparoxysmal response) from exposure to intermittent photic stimulation (IPS). SPR is the number of frequency steps (2, 5, 8, 10, 13, 15, 18, 20, 23, 25, 30, 40, 50 and 60 Hz). between the upper and lower limits of sensitivity to IPS for that patient at that time, in order not to evoke seizures. Thus a reduction (-change) means the intervention is working (desired effect on sensitivity) (NCT02351115)
Timeframe: SPR was recorded pretreatment, 2, 10, 30 min, 1, 2, 4, and 6 hr post each study drug administration The maximum change from baseline occurred at: 10 min for alprazolam 2 mg, 1 hour for alprazolam 0.5 and 1 mg and placebo

InterventionNumber of frequency steps (Mean)
Inhaled Placebo-0.2
Staccato Alprazolam, 0.5 mg-4.4
Staccato Alprazolam, 1 mg-5.2
Staccato Alprazolam, 2 mg-4.8

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Maximum Sedation Using Visual Analog Scale (Sedated-Alert)

Maximum change (in mm) from pretreatment baseline in level of sedation reported by the patient on a 100 mm line anchored by Sedated (0) and Alert (100) (NCT02351115)
Timeframe: Sedation was recorded pretreatment, 2, 10, 30 min, 1, 2, 4, and 6 hr post each study drug administration The maximum change from baseline occurred at:: 30 min for alprazolam 1 mg, 1 hour for alprazolam 0.5 and 2 mg, and 4 hours for placebo

Interventionunits on a scale (Mean)
Inhaled Placebo-5.3
Staccato Alprazolam, 0.5 mg-58
Staccato Alprazolam, 1 mg-67.4
Staccato Alprazolam, 2 mg-70.6

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Maximum Sedation Using Visual Analog Scale (Sleepy-Awake)

Maximum change (in mm) from pretreatment baseline in level of sedation reported by each subject on a 100 mm line anchored by Sleepy (0) and Awake (100) (NCT02351115)
Timeframe: Sleepiness was recorded pretreatment, 2, 10, 30 min, 1, 2, 4, and 6 hr post each study drug administration The maximum change from baseline occurred: at: 30 min for alprazolam 1 mg, 1 hour for alprazolam 0.5 and 2 mg and placebo

Interventionunits on a scale (Mean)
Inhaled Placebo-9.2
Staccato Alprazolam, 0.5 mg-54
Staccato Alprazolam, 1 mg-58.8
Staccato Alprazolam, 2 mg-58.8

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Correlation of Plasma Concentrations of Alprazolam With Pharmacodynamic Effects on Standardized Photosensitivity Range (SPR)

Pearson correlation of all paired plasma concentrations of alprazolam (PK) with pharmacodynamic effect on SPR (PD) for each alprazolam dose (NCT02351115)
Timeframe: Pretreatment, 2, 10, 30 min, 1, 2, 4, and 6 hr post each study drug administration

Interventioncorrelation coefficient (Mean)
Staccato Alprazolam, 0.5 mg-0.454
Staccato Alprazolam, 1 mg-0.534
Staccato Alprazolam, 2 mg-0.410

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Driving Performance Using the CRCDS-MiniSim - Lane Exceedance

The CRCDS-MiniSim is a PC-based research driving simulator that provides a realistic automotive driving environment. The present study employs the Country Vigilance-Divided Attention (CVDA) driving scenario, a 62.1 mile (100 km), monotonous, two lane highway driving task that includes a secondary visual vigilance task (DA). The monotonous Country Vigilance scenario has been demonstrated to be sensitive to detect the effects of fatigue or sleepiness on driving performance. Lane exceedance is the number of lane exceedances, an indication of lane position control, (i.e., the driver's ability to stay within his/her lane), as measured by the number of times that the front left or right tire of the vehicle crosses over the right or left lane boundary. (NCT03012334)
Timeframe: Approximately 90 minutes post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

InterventionLane Exceedances (Mean)
Placebo2.288
Lasmiditan 50mg3.716
Lasmiditan 100mg4.301
Lasmiditan 200mg4.884
Alprazolam 1mg4.841

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Data presented are the number of participants who experienced 1 or more AEs (all causalities and drug-related) and serious AEs (SAEs). A summary of SAEs and other non-serious AEs, regardless of causality is located in the Reported Adverse Events section of this record. (NCT03012334)
Timeframe: Up To 35 days

,,,,
InterventionParticipants (Count of Participants)
Other AEsSAEs
Alprazolam 1mg710
Lasmiditan 100mg470
Lasmiditan 200mg620
Lasmiditan 50mg340
Placebo81

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Motivational and Self-Appraisal Visual Analog Scale (VAS)

After completing the driving simulation, participants assessed their own performance and their level of motivation to perform at their best during the driving simulation. Participants responded to 2 questions: 1. How well do you think you drove for the last 60 minutes? 2. How motivated did you feel to drive at your best during the last 60 minutes of driving?. Participants recorded their response to each question by writing a vertical line on a 100 millimeters (mm) horizontal, linear visual analog scale indicating their level of performance (Not Satisfactory to Satisfactory) and motivation (Not Motivated to Motivated). Scores on the 100 mm linear scale were measured to the nearest millimeter from the left. Scores ranged from 0-100 mm, with higher scores indicating motivated and satisfactory and lower scores indicating not motivated and not satisfactory. (NCT03012334)
Timeframe: Approximately 2.5 hours post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

,,,,
InterventionMillimeters (mm) (Mean)
VAS MotivationVAS Self-appraisal
Alprazolam 1mg47.624.7
Lasmiditan 100mg53.739.8
Lasmiditan 200mg49.930.8
Lasmiditan 50mg65.651.2
Placebo78.077.2

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Simulated Driving Performance in Healthy Participants as Measured by Standard Deviation of Lateral Position (SDLP) Using the Cognitive Research Corporation Driving Simulator-MiniSim (CRCDS-MiniSim)

The standard deviation of lateral position (SDLP) is the primary parameter used as stable measure of driving performance with high test-retest reliability. It measures the driver's ability to stay in a constant position within the driving lane. Variations in the lateral position are recorded and analyzed. SDLP, was analyzed using a mixed model with fixed effects for sequence, period, and treatment, and a random effect for participant within sequence. A variance component covariance structure and Kenward-Roger degrees of freedom was used. (NCT03012334)
Timeframe: Approximately 90 minutes post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

InterventionCentimeters (cm) (Mean)
Placebo28.77
Lasmiditan 50mg38.52
Lasmiditan 100mg44.03
Lasmiditan 200mg50.24
Alprazolam 1mg51.48

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Percentage of Participants With Self-Reported Readiness to Drive

"On each dosing day participants were asked Right now do you feel safe to drive?. Pair-wise comparisons for readiness to drive were analyzed using McNemar test." (NCT03012334)
Timeframe: Approximately 85 minutes post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

InterventionPercentage of Participants (Number)
Placebo100
Lasmiditan 50mg80
Lasmiditan 100mg67.9
Lasmiditan 200mg55.3
Alprazolam 1mg43.5

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Number of Correct Responses in Driving Performance Using CogScreen Symbol Digit Coding (SDC) Test

The SDC Test, a digit symbol substitution test that is sensitive to changes in information processing speed, provides measures of response speed and accuracy. The test was administered prior to the simulated driving sessions. The principal test score measures the number of correct responses in 120 seconds. SDC was used in this study to measure attention, visual scanning, working memory, and speed of information processing. Scores range from 0 (No correct responses). A higher score indicates greater processing speed. (NCT03012334)
Timeframe: Approximately 85 minutes post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

InterventionResponses (Mean)
Placebo72.8
Lasmiditan 50mg68.1
Lasmiditan 100mg66.0
Lasmiditan 200mg64.1
Alprazolam 1mg61.7

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Karolinska Sleepiness Scale (KSS) Score

The KSS is used to assess subjective level of sleepiness. This is a participant self-report measure of situational sleepiness and provides an assessment of alertness/sleepiness at a particular point in time. It is a 9-point categorical Likert scale on which the participant rates sleepiness from 1 (very alert) to 9 (very sleepy/fighting sleep), with higher scores indicating more sleepiness and lower scores indicating more alertness. (NCT03012334)
Timeframe: Approximately 85 minutes post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

InterventionUnits on a scale (Mean)
Placebo2.8
Lasmiditan 50mg4.4
Lasmiditan 100mg5.1
Lasmiditan 200mg5.7
Alprazolam 1mg6.2

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Driving Performance Using the CRCDS-MiniSim - Speed Deviation

The CRCDS-MiniSim is a PC-based research driving simulator that provides a realistic automotive driving environment. The present study employs the Country Vigilance-Divided Attention (CVDA) driving scenario, a 62.1 mile (100 km), monotonous, two lane highway driving task that includes a secondary visual vigilance task (DA). The monotonous Country Vigilance scenario has been demonstrated to be sensitive to detect the effects of fatigue or sleepiness on driving performance. Speed deviation is a measure of intra-individual variability. Measures that assess an individual's failure to maintain consistent performance are more sensitive to sedation than are measures of absolute performance. (NCT03012334)
Timeframe: Approximately 90 minutes post dose, on Day 1, 7, 14, 21, or 28 depending upon the assigned treatment sequence

Interventionmeter per second (m/sec) (Mean)
Placebo0.635
Lasmiditan 50mg0.814
Lasmiditan 100mg0.935
Lasmiditan 200mg1.013
Alprazolam 1mg1.238

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PD: Minimum Drug Effects (Emin) Visual Analog Scale (VAS)

Drug Effects VAS Battery lists a series of measures that evaluate different effects of the abuse potential of the study drug. The scales included: Alertness/Drowsiness (I am feeling) ranges from 0 very drowsy to 100 very alert. Agitation/Relaxation (my mood is) and ranges from 0 very relaxed to 100 very agitated. Emin is derived across all postdose time points for each participant. LS Mean was calculated using the linear mixed-effects model with period, sequence and treatment as fixed effects and participant as a random effect. (NCT03286218)
Timeframe: Each Phase:Predose, 0.25, 0.5, 1, 1.5, 2, 2.5,3, 3.5, 4, 4.5, 5, 6, 8, 12, 24 Hours Post Dose

,,,,
Interventionmm (Least Squares Mean)
Alertness/drowsinessAgitation/relaxation
Alprazolam - 2 mg12.513.4
Lasmiditan - 100 mg25.624.6
Lasmiditan - 200 mg22.922.4
Lasmiditan - 400 mg17.715.4
Placebo42.544.1

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PD: Mean Scores on Drug Similarity VAS Measures

"Participants marked a point on a 100-mm horizontal line that best represented their response to the given question. The endpoints of each electronic scale were marked with descriptive anchors on a scale from 0 to 100 (Fraser et al. 1961; Bond and Lader 1974; Bigelow 1991; Shram et al. 2010). In the How similar questions, ranges from 0 to 100 and a score of 0 indicates definitely not similar, and a score of 100 indicates definitely similar." (NCT03286218)
Timeframe: Each Phase: 24 Hours Post Dose

,,,,,,
Interventionscore on a scale (Mean)
How similar with cocaine /How similar with caffeineHow similar to MDMA (Ectasy)How similar to amphetamine or methamphetamineHow similar to phencyclidine (PCP)How similar to codeine or morphine useHow similar to (lysergic acid diethylamide (LSD)How similar to nicotineHow similar to cannabisHow similar to benzodiazepineHow similar to mushroomsHow similar to heroin
1 mg Alprazolam - Qualification Phase5.83.210.04.30.541.54.15.139.975.92.717.8
2 mg Alprazolam6.14.420.53.926.750.86.23.851.288.13.7NA
Lasmiditan - 100 mg2.72.210.62.31.330.93.53.329.957.22.1NA
Lasmiditan - 200 mg14.64.417.14.624.037.65.93.637.466.93.8NA
Lasmiditan - 400 mg12.54.118.74.432.345.97.24.341.774.64.9NA
Placebo2.21.51.42.40.08.14.21.48.913.12.1NA
Placebo - Qualification Phase1.32.94.71.522.011.41.22.910.814.40.00.0

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PK: Area Under the Curve of Lasmiditan From Zero to Infinity (AUC[0-∞])

PK defined as the area under the curve of lasmiditan from zero to infinity (AUC[0-∞]) (NCT03286218)
Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours Post Dose

Interventionnanogram*hour/milliliter (ng*h/mL) (Geometric Mean)
Lasmiditan - 100 mg856
Lasmiditan - 200 mg1810
Lasmiditan - 400 mg Dose3920

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Lasmiditan

Pharmacokinetics (PK) defined as the maximum observed drug concentration (Cmax) of lasmiditan (NCT03286218)
Timeframe: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours Post Dose

Interventionnanogram/milliliter (ng/mL) (Geometric Mean)
Lasmiditan - 100 mg132
Lasmiditan - 200 mg299
Lasmiditan - 400 mg689

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Pharmacodynamics (PD): Maximal Effect Score (Emax) of Bipolar Drug Liking Visual Analog Scale (VAS) Scores

The Emax of Bipolar Drug Liking VAS Scores were derived as the maximum at-the-moment Drug Liking VAS score where the time to Emax was the corresponding time point at which the maximum score occurred. The bipolar Drug Liking VAS is consistent with FDA Guidance (January 2017) such that placebo should produce a score between 40 and 60 representing neutral drug-liking (ie, neither like nor dislike); a score ranging from 0 to 100 and a score of 0 indicates strong disliking, and a score of 100 indicates strong liking. Least squares mean (LS mean) was calculated using a linear mixed-effects model, including period, sequence, and treatment as fixed effects, and subject as a random effect, was used to evaluate the hypothesis tests of primary interest (at-the-moment Drug Liking) at the Emax. (NCT03286218)
Timeframe: Each Phase: 24 Hours

Interventionmillimeter (mm) (Least Squares Mean)
Placebo53.0
Alprazolam - 2 mg85.4
Lasmiditan - 100 mg68.6
Lasmiditan - 200 mg73.3
Lasmiditan - 400 mg76.6

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PD: Maximal Drug Effects (Emax) VAS (Hallucinations)

Drug Effects VAS Battery lists a series of measures that evaluate different effects of the abuse potential of the study drug. The hallucinations scale is presented meaning (I am hallucinating) and ranges from 0 not at all to 100 extremely. Emax is derived as the maximum score across all postdose time points for each participant. Median and interquartile range are reported for each treatment group. (NCT03286218)
Timeframe: Each Phase: Predose, 0.25, 0.5, 1, 1.5, 2, 2.5,3, 3.5, 4, 4.5, 5, 6, 8, 12, 24 Hours Post Dose

Interventionmm (Median)
Placebo0
Alprazolam - 2 mg0
Lasmiditan - 100 mg0
Lasmiditan - 200 mg0
Lasmiditan - 400 mg0

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PD: Maximal Drug Effects (Emax) Visual Analog Scale (VAS)

Drug Effects VAS Battery lists a series of measures that evaluate different effects of the abuse potential of the study drug. Scales include: Overall drug liking (overall, my liking for this drug is) and ranges from 0 definitely not to 100 definitely so. Take Drug Again (I would take this drug again) and ranges from 0 definitely not to 100 definitely so. Good effects (I can feel good drug effects) and ranges from 0 definitely not to 100 definitely so. Bad effects (I can feel bad drug effects) and ranges from 0 definitely not to 100 definitely so. High (I am feeling) and ranges from 0 not at all high to 100 extremely high. Emax is derived as the maximum score across all postdose time points for each participant. Least Square (LS) Mean is calculated using the linear mixed-effects model with period, sequence and treatment as fixed effects and participant as a random effect. (NCT03286218)
Timeframe: Each Phase: Predose, 0.25, 0.5, 1, 1.5, 2, 2.5,3, 3.5, 4, 4.5, 5, 6, 8, 12, 24 Hours Post Dose

,,,,
Interventionmm (Least Squares Mean)
Overall Drug LikingTake Drug AgainGood EffectsBad EffectsAny EffectsHigh
Alprazolam - 2 mg86.286.080.522.983.777.2
Lasmiditan - 100 mg71.771.146.47.5153.343.0
Lasmiditan - 200 mg72.272.762.99.7565.156.1
Lasmiditan - 400 mg77.477.363.815.073.267.0
Placebo53.152.010.82.478.358.61

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Standard Deviation of Lane Position (SLDP)

Lane deviation (swerving) on a driving simulator. This is measured as the distance (cm) the driver deviates from the lane. (NCT03297944)
Timeframe: 16 hours

Interventiondistance (cm) (Mean)
2ALP/PLC1ALP/PLC0.5ALP/PLCZOL/PLCPLC/PLCPLC/ALP
All Participants40.0837.2836.0637.6136.3040.72

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SDLP

"Standard Deviation of Lane Position~Standard deviation of lane position was analyzed using the SAS GLM function to identify changes in driver performance. Values represents means across the driving environments studied." (NCT03447353)
Timeframe: over course of each simulator drive, approximately 35 minutes per visit

Interventioncentimeters (Mean)
"Sober or Double Placebo"35.2
Active Xanax, Active Norco49.8
Active Xanax, Placebo Norco50.0
Placebo Xanax, Active Norco33.5

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Lane Departures

"Total number of lane departures per drive~The total number of lane departures across the drive were analyzed using the SAS GLM procedure." (NCT03447353)
Timeframe: over course of each simulator drive, approximately 35 minutes per visit

Interventioncount (Mean)
"Sober or Double Placebo"23.8
Active Xanax, Active Norco72.0
Active Xanax, Placebo Norco64.4
Placebo Xanax, Active Norco22.3

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Percentage of Participants in Each Treatment Group Achieving Seizure Activity Cessation Within 2 Minutes and no Recurrent Seizure Within 2 Hours

Percentage of participants with onset of a predictable seizure through 2 minutes post dosing with study drug and no recurrence of seizure activity within 2 hours were reported for each treatment group based on clinical observation. (NCT03478982)
Timeframe: 2 hours post-dosing on dosing day

Interventionpercentage of participants (Number)
Open-label: Staccato Alprazolam (STAP-001) 1.0 Milligram (mg)62.5
Double-blind: Placebo42.5
Double-blind: Staccato Alprazolam 1.0 mg65.8
Double-blind: Staccato Alprazolam 2.0 mg65.8

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Percentage of Participants With Secondary Generalization (Evolution to a Complex Partial Seizure and/or a Generalized Tonic-Clonic Seizure)

Percentage of participants who had seizures that evolved to a complex partial seizure and/or a generalized tonic-clonic seizure were reported. (NCT03478982)
Timeframe: 24 hours post-dosing on dosing day

Interventionpercentage of participants (Number)
Open-label: Staccato Alprazolam (STAP-001) 1.0 Milligram (mg)12.5
Double-blind: Placebo0.0
Double-blind: Staccato Alprazolam 1.0 mg0.0
Double-blind: Staccato Alprazolam 2.0 mg0.0

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Percentage of Participants With Use of Rescue Medication

Percentage of participants with use of rescue medication to stop a seizure episode at the discretion of the principal investigator were reported. (NCT03478982)
Timeframe: 2 hours post-dosing on dosing day

Interventionpercentage of participants (Number)
Open-label: Staccato Alprazolam (STAP-001) 1.0 Milligram (mg)0
Double-blind: Placebo7.5
Double-blind: Staccato Alprazolam 1.0 mg15.8
Double-blind: Staccato Alprazolam 2.0 mg7.9

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Percentage of Participants With Seizure Episode Severity Assessed by Seizure Episode Severity Scale

Severity of on study seizure episode compared to previously experienced seizures was assessed with Seizure Episode Severity Scale. It is a 5-point scale with range from 1 to 5, where 1 indicates much worse than and 5 indicates much better than. (NCT03478982)
Timeframe: 6 hours post-dosing on dosing day

,,,
Interventionpercentage of participants (Number)
Much worse thanWorse thanSame asBetter thanMuch better thanNot done
Double-blind: Placebo2.55.042.535.07.57.5
Double-blind: Staccato Alprazolam 1.0 mg02.657.918.415.85.3
Double-blind: Staccato Alprazolam 2.0 mg05.355.328.95.35.3
Open-label: Staccato Alprazolam (STAP-001) 1.0 Milligram (mg)0012.550.025.012.5

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Standard Deviation of Lateral Position (SDLP)

The ability to keep the vehicle straight in the lane. Data is presented from the a rural drive with a concurrent divided attention task. (NCT04970342)
Timeframe: over one hour during the course of the simulator drive conducted 45 minutes post-dose at Treatment Visit 1, 2, and 3

Interventioncm (Mean)
"Sober or Double Placebo"25.490
Active Alprazolam (Xanax), Placebo Cannabis37.849
Placebo Alprazolam (Xanax), Active Cannabis33.086

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Lane Exceedences

Count of the number of times the simulated vehicle leaves the driving lane, will be compared across treatments. Data is from a rural drive with a concurrent divided attention task. (NCT04970342)
Timeframe: over one hour during the course of the simulator drive conducted 45 minutes post-dose at Treatment Visit 1, 2, and 3

Interventionnumber of times vehicle departed lane (Mean)
"Sober or Double Placebo"5.750
Active Alprazolam (Xanax), Placebo Cannabis36.500
Placebo Alprazolam (Xanax), Active Cannabis29.875

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