Page last updated: 2024-12-04

clonidine

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Description

Clonidine is a centrally acting alpha-2 adrenergic agonist. It was synthesized in 1963 and is primarily used to treat hypertension, ADHD, and opiate withdrawal. Its effects include lowering blood pressure by reducing sympathetic nervous system activity, decreasing anxiety, and producing sedation. Clonidine works by binding to alpha-2 adrenergic receptors in the brainstem, which leads to a decrease in norepinephrine release. This decrease in norepinephrine results in decreased sympathetic outflow and a reduction in blood pressure. Clonidine is also studied for its potential use in treating other conditions, such as Tourette syndrome, migraine headaches, and restless legs syndrome. Due to its ability to modulate neurotransmitter release, it is a valuable tool for research into the mechanisms of various neurological disorders. Its mechanism of action and effectiveness in treating various conditions make it a subject of ongoing research and a significant therapeutic agent.'

Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group. [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 CID2803
CHEMBL ID134
CHEBI ID3757
CHEBI ID46632
CHEBI ID46631
SCHEMBL ID5982
MeSH IDM0004605

Synonyms (214)

Synonym
BIDD:GT0547
STL355995
AB00514634-08
BRD-K98530306-003-05-0
BRD-K98530306-001-02-1
gtpl516
kapvay®
2-imidazoline, 2-(2,6-dichlorophenylamino)-
KBIO1_000774
DIVK1C_000774
CLD ,
2-(2,6-dichlorophenylamino)-2-imidazoline
2-imidazoline, 2-(2,6-dichloroanilino)-
catapres-tts-3
klofenil
catapres-tts-2
catapres-tts-1
clonidina [inn-spanish]
clonidinum [inn-latin]
clofenil
catapres
catapres- tts
einecs 224-119-4
SPECTRUM_001341
BSPBIO_000036
clorpres
combipres
BIO1_001448
NCGC00015268-01
tocris-0690
BIO2_000788
NCGC00024734-01
BIO2_000308
NCGC00015268-02
BIO1_000470
BIO1_000959
lopac-c-7897
NCGC00179680-01
BSPBIO_002055
PRESTWICK3_000248
IDI1_000774
BSPBIO_001588
BPBIO1_000040
PRESTWICK2_000248
IDI1_034058
LOPAC0_000268
2,6-dichloro-n-2-imidazolidinylidenebenzenamide
2-(2,6-dichlorophenylimino)imidazolidine
1h-imidazol-2-amine, n-(2,6-dichlorophenyl)-4,5-dihydro-
catarpres
1h-imidazol-2-amine, n-(2,6-dichlorophenyl)-4,5-dihydro- (9ci)
chlornidinum
2-(2,6-dichloroanilino)-1,3-diazacyclopentene-(2)
hsdb 3040
ccris 7787
catapres-tts
m 5041t
2-((2,6-dichlorophenyl)imino)imidazolidine
m-5041t
skf 34427
clonidine
2-(2,6-dichloroanilino)-2-imidazoline
2-[(2,6-dichlorophenyl)imino]-2-imidazoline
clonidin
st 155bs
4205-90-7
catarpresan
st-155-bs
2-imidazoline, 2-(2,6-dichloroanilino)- (7ci,8ci)
adesipress
734571a
catapressan
benzenamine, 2,6-dichloro-n-2-imidazolidinylidene-
AB00514634
2,6-dichloro-n-imidazolidin-2-ylideneaniline
2,6-dichloro-n-2-imidazolidinylidenebenzenamine
clonidine (imino form)
CHEBI:3757 ,
2-[(2,6-dichlorophenyl)imino]imidazoline
CHEBI:46632 ,
n-(2,6-dichlorophenyl)-4,5-dihydro-1h-imidazol-2-amine
clonidine (amino form)
DB00575
chlofazoline
clonidine (jan/usp/inn)
catarpres-tts (tn)
D00281 ,
NCGC00024734-03
NCGC00024734-04
KBIOSS_000308
KBIO3_000615
KBIO2_001821
KBIO3_001275
KBIOGR_001572
KBIO2_006957
KBIO2_002876
KBIOSS_001821
KBIO2_005444
KBIO2_004389
KBIO3_000616
KBIO2_000308
KBIOGR_000308
SPECTRUM2_001187
SPBIO_002255
SPECTRUM4_000956
NINDS_000774
PRESTWICK0_000248
SPECTRUM3_000358
PRESTWICK1_000248
SPBIO_001233
SPECTRUM5_000759
NCGC00024734-02
NCGC00024734-05
HMS1989P10
HMS2089G11
NCGC00015268-08
CHEMBL134
clonidine extended release
catarpres-tts
st-155bs
L000193
HMS1791P10
HMS1361P10
bdbm50016897
NCGC00015268-05
AKOS001595470
NCGC00179680-03
NCGC00179680-02
(2,6-dichloro-phenyl)-imidazolidin-2-ylidene-amine
cas-4205-90-7
tox21_110118
dtxcid402846
dtxsid6022846 ,
CCG-204363
AKOS015960367
NCGC00015268-04
NCGC00015268-07
NCGC00015268-06
NCGC00015268-03
clonidinum
unii-mn3l5rmn02
clonidina
clonidine [usan:usp:inn:ban]
nexiclon xr
mn3l5rmn02 ,
clonidinhydrochlorid
clonidine [orange book]
clonidine [mart.]
clonidine [mi]
clonidine [usp-rs]
clonidine [jan]
clonidine [hsdb]
clonidine [who-dd]
clonidine [inn]
clonidine [usp monograph]
2-[(2,6-dichlorophenyl)imino]imidazolidine
clonidine [usan]
clonidine [vandf]
BBL025137
[3h]clonidine
bdbm14062
n-(2,6-dichlorophenyl)imidazolidin-2-imine
SCHEMBL5982
tox21_110118_1
NCGC00179680-05
AB00514634-07
2-(2',6'-dichlorophenylamino)-2-imidazoline
(2,6-dichlorophenyl)imidazolidin-2-ylidene amine
2-[(2,6-dichlorophenyl)imino]-imidazolidine
2-(2,6-dichlorophenyl-imino)-imidazolidine
2-(2,6-dichlorophenylimino)-imidazolidine
smr001550184
MLS006011925
clonidine, clonidine hydrochloride
n-(2,6-dichlorophenyl)-4,5-dihydro-1h-imidazol-2-amine #
HMS3402P10
AB00053441_03
AB00514634_09
SR-01000759380-4
3h-clonidine
MRF-0000018
SBI-0050256.P004
clonidine(200 mg)
FT-0741246
BCP07223
Q412221
HY-12721
bdbm50225285
BRD-K98530306-003-07-6
SDCCGSBI-0050256.P005
NCGC00015268-12
nexiclon
CS-0012297
4205-90-7 (free base)
clonidine(200mg)
STARBLD0009556
SY267931
mfcd00055059
F74813
EN300-8686697
n02cx02
clonidine transdermal system usp, 0.1 mg/day
chebi:46631
clonidine (usan:usp:inn:ban)
clonidine transdermal system
clonidina (inn-spanish)
clonidine transdermal system usp, 0.2 mg/day
s01ea04
clonidinum (inn-latin)
clonidine (usp-rs)
clonidine (mart.)
c02ac01
clonidine (usp monograph)
clonidine transdermal system usp, 0.3 mg/day

Research Excerpts

Overview

Clonidine is an anti-hypertensive drug that inhibits the release of norepinephrine from pre-synaptic terminals. Clonidine demonstrated to be a well-tolerated sedation option in pediatric patients submitted to mechanical ventilation.

ExcerptReferenceRelevance
"Clonidine is an alpha-2 adrenoreceptor agonist and is frequently combined with opioids (ie, morphine hydrochloride (HCl)) for the management of chronic pain. "( Evaluation of 30-days stability of morphine hydrochloride and clonidine at high and low concentrations in polypropylene syringes.
Bihin, B; Catry, E; Closset, M; Colsoul, ML; Galanti, L; Hecq, JD; Hubert, J; Jamart, J; Nyssen, C; Soumoy, L, 2023
)
2.59
"Clonidine is a first-generation central antihypertensive that reduces sympathetic nerve activity (SNA). "( Quantitative assessment of the central versus peripheral effect of intravenous clonidine using baroreflex equilibrium diagrams.
Hayama, Y; Kawada, T; Li, M; Miyamoto, T; Nishikawa, T; Saku, K; Sugimachi, M; Uemura, K; Zheng, C, 2021
)
2.29
"Clonidine is a sedative-sparing agent and this can help reduce complications associated with prolonged use of opioids and benzodiazepines."( Use of continuous infusion of clonidine for sedation in critically ill infants and children.
Bourdon, O; Dauger, S; Deho, A; Prot-Labarthe, S; Sadozai, L, 2022
)
1.73
"Clonidine is an anti-hypertensive drug that inhibits the release of norepinephrine from pre-synaptic terminals binding to pre-synaptic α"( Clonidine and Brain Mitochondrial Energy Metabolism: Pharmacodynamic Insights Beyond Receptorial Effects.
Ferrari, F; Gorini, A; Villa, RF, 2022
)
3.61
"Clonidine is a presynaptic alpha-2-adrenergic receptor agonist that has been used for many years to treat hypertension and other conditions, including chronic pain. "( Topical clonidine for neuropathic pain in adults.
Dobrogowski, J; Garlicki, J; Jakowicka-Wordliczek, J; Serednicki, WT; Wordliczek, J; Woron, J; Wrzosek, A; Zajaczkowska, R, 2022
)
2.6
"Clonidine demonstrated to be a well-tolerated sedation option in pediatric patients submitted to mechanical ventilation, without relevant influence in hemodynamic variables."( Continuous clonidine infusion: an alternative for children on mechanical ventilation.
Fiamenghi, VI; Fontela, PS; Neves, CC; Piva, JP, 2022
)
2.55
"Clonidine is a frequently prescribed long-term antihypertensive medication in hemodialysis (HD) patients in the USA, but its safety and efficacy has not been clearly established in the HD population."( The Safety and Efficacy of Clonidine in Hemodialysis Patients: A Systematic Review and Meta-Analysis.
An, R; Ashrafi, SA; Barton, A; Derk, G; Fang, HY; Wilund, K, 2022
)
2.46
"Clonidine is an effective adjunctive agent for the prevention of emergence agitation in children, but evidence in the smallest age groups is sparse We aim to investigate the efficacy and safety of an intraoperative bolus of intravenous clonidine for preventing emergence agitation in children 3-12 months of age."( Clonidine for preventing emergence agitation in infants (PREVENT AGITATION II): Protocol and statistical analysis plan.
Afshari, A; Falcon, L; Garioud, ALB; Mondrup, F; Nielsen, BN, 2023
)
3.07
"Clonidine is an α2-agonist that is commonly used for sedation in the intensive care unit. "( In vivo Elimination of Clonidine by Continuous Venovenous Hemofiltration in Critically Ill Patients.
Arbouw, M; Bles, C; de Meijer, AR; Kruisdijk-Gerritsen, A; Nassikovker, P; van den Oever, HLA; van Steveninck, FAL; Zeeman, M, 2020
)
2.31
"Clonidine is a centrally-acting α-2 agonist used in the treatment of hypertension and attention-deficit/hyperactivity disorder, among other off-label uses. "( Clonidine Compounding Error: Bradycardia and Sedation in a Pediatric Patient.
Barbuto, AF; Burns, MM, 2020
)
3.44
"Clonidine is a central alpha-2 agonist well known to produce a syndrome of bradycardia and hypotension in overdose. "( "Road Rash" and Dizziness: A Case of Hemodynamically Significant Topical Clonidine Toxicity.
Cumpston, KL; Downs, JW, 2021
)
2.3
"Clonidine is a centrally acting alpha-2 selective adrenergic receptor agonist used to treat hypertension and to control or prevent withdrawal in patients with opioid and alcohol use disorders. "( Case Report: Concurrent Clonidine Abuse and Opioid Use Disorder.
Lee, J; Mitchell, BG,
)
1.88
"Apraclonidine hydrochloride is a topical ophthalmic solution with selective alpha-2 and weak alpha-1 receptor agonist activity that has the ability to elevate the eye lid."( Apraclonidine in the treatment of ptosis.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
1.49
"Clonidine is an effective and safe adjuvant to local anaesthetics for spinal anaesthesia for caesarean delivery. "( Intrathecal clonidine as an adjuvant for neuraxial anaesthesia during caesarean delivery: a systematic review and meta-analysis of randomised trials.
Crespo, S; Dangelser, G; Haller, G, 2017
)
2.28
"Clonidine is an imidazoline sympatholytic, acting on both α"( A case report of clonidine induced syncope: a review of central actions of an old cardiovascular drug.
Morrison, CM; Rozich, J; Sandweiss, AJ; Spichler, A, 2018
)
2.26
"Clonidine is an anti-hypertensive medication which acts as an alpha-adrenergic receptor agonist. "( Clonidine modulates the activity of the subthalamic-supplementary motor loop: evidence from a pharmacological study combining deep brain stimulation and electroencephalography recordings in Parkinsonian patients.
Albares, M; Ballanger, B; Boulinguez, P; Broussolle, E; Lau, B; Lio, G; Spay, C; Thobois, S, 2018
)
3.37
"Clonidine is an antihypertensive drug used for analgosedation in the PICU. "( Hemodynamic Tolerance to IV Clonidine Infusion in the PICU.
de Wildt, SN; Kleiber, N; Tibboel, D; van Rosmalen, J, 2018
)
2.22
"Clonidine is an α"( Effects of clonidine on MMN and P3a amplitude in schizophrenia patients on stable medication.
Glenthøj, BY; Kruiper, C; Oranje, B, 2019
)
1.63
"Clonidine is an imidazoline derivative antihypertensive medication that is also used as adjunctive therapy for neuropathic pain disorders via topical administration. "( Dermal exposure to a compounded pain cream resulting in severely elevated clonidine concentration.
Fantz, CR; Gooden, CE; Morgan, BW; Pomerleau, AC, 2014
)
2.08
"Clonidine is a nonnarcotic analgesic historically used as a nasal decongestant and more recently established as an antihypertensive agent in adults. "( Oral clonidine in the management of acquired opioid dependency.
Beaulieu, MJ,
)
2.09
"Clonidine is an alpha-2 adrenergic agonist which has sedative, anxiolytic and analgesic properties."( Clonidine premedication for postoperative analgesia in children.
Cyna, AM; Knight, N; Lambert, P; Middleton, P, 2014
)
2.57
"Clonidine is a useful analgesic-sedative agent; however, few data exist regarding its use in infants after congenital heart disease surgery. "( Enteral absorption and haemodynamic response of clonidine in infants post-cardiac surgery.
Arenas-Lopez, S; Durward, A; Manna, S; Mulla, H; Murdoch, IA; Tibby, SM, 2014
)
2.1
"Clonidine is an α2-adrenergic receptor agonist which, at low doses, inhibits noradrenergic signaling by decreasing norepinephrine release from presynaptic noradrenergic neurons."( The α2-adrenergic receptor agonist, clonidine, reduces alcohol drinking in alcohol-preferring (P) rats.
Alexander, L; Federoff, D; Froehlich, JC; Malone, J; Rasmussen, DD, 2014
)
1.4
"Clonidine is an alternative to midazolam. "( Prospective multicentre randomised, double-blind, equivalence study comparing clonidine and midazolam as intravenous sedative agents in critically ill children: the SLEEPS (Safety profiLe, Efficacy and Equivalence in Paediatric intensive care Sedation) st
Boland, A; Gamble, C; Granville, H; McKay, A; Petrou, S; Spowart, C; Sutherland, A; Wolf, A, 2014
)
2.07
"Clonidine is a presynaptic alpha-2-adrenergic receptor agonist used for many years to treat hypertension and other conditions, including chronic pain. "( Topical clonidine for neuropathic pain.
Dobrogowski, J; Jakowicka-Wordliczek, J; Wordliczek, J; Woron, J; Wrzosek, A, 2015
)
2.29
"As clonidine is a well-known effector of the autonomous system, stimulating vagal tone and decreasing sympathetic activity, we compared the autonomous reactions of children with constitutional growth delay (CGD), growth hormone deficiency (GHD) and former small for gestational age (SGA)."( Modified Clonidine Testing for Growth Hormone Stimulation Reveals α2-Adrenoreceptor Sub Sensitivity in Children with Idiopathic Growth Hormone Deficiency.
Buchhorn, R; Meint, S; Rager, K; Willaschek, C, 2015
)
1.35
"Clonidine is a central alpha(2)-agonist antihypertensive used widely for opioid/alcohol withdrawal, attention deficit hyperactivity disorder and chronic pain management. "( Intrathecal Clonidine Pump Failure Causing Acute Withdrawal Syndrome With 'Stress-Induced' Cardiomyopathy.
Graudins, A; Lee, HM; Ruggoo, V, 2016
)
2.26
"Clonidine is an alpha-2 selective adrenergic agonist that may have a role in optimizing current sedation practices in the pediatric and adult critically ill populations by potentially minimizing exposure to other sedative agents."( Clonidine for sedation in the critically ill: a systematic review and meta-analysis (protocol).
Alhazzani, W; Belley-Coté, E; Burry, L; D'Aragon, F; Duffett, M; Jing Wang, G; Karachi, T; Perri, D; Rochwerg, B; Wunsch, H, 2015
)
2.58
"Clonidine is an antihypertensive agent used for induced hypotension."( Effects of oral clonidine premedication on hemodynamic status in bimaxillary orthognathic surgery: A double-blind randomized clinical trial.
Khakbaz, O; Marashi, M; Mohammadi, F; Tavakoli, I, 2016
)
1.5
"Clonidine is a safe and effective drug to reduce bleeding in trans-sphenoidal microscopic pituitary adenoma surgeries."( Preoperative clonidine use in trans-sphenoidal pituitary adenoma surgeries - a randomized controlled trial.
Bajaj, J; Mittal, RS; Sharma, A, 2017
)
2.27
"Clonidine is an α2-adrenoceptor agonist, which has analgesic properties. "( Clonidine Does Not Reduce Pain or Opioid Consumption After Noncardiac Surgery.
Ali Sakr Esa, W; Babazade, R; Devereaux, PJ; Gilron, I; Honar, H; Hutcherson, MT; Kurz, A; Naylor, AJ; Parlow, J; Salmasi, V; Sessler, DI; Turan, A; Zimmerman, NM, 2016
)
3.32
"Apraclonidine is an alpha-2 adrenergic receptor agonist, which causes contraction of superior tarsal (Müller) muscle which may improve blepharospasm-related eyelid closure."( Treatment of blepharospasm with apraclonidine.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
1.21
"Apraclonidine is a potentially useful medication for short term management of blepharospasm symptoms while awaiting botulinum toxin injection."( Treatment of blepharospasm with apraclonidine.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
1.29
"Clonidine is an alpha2-adrenergic agonist with analgetic properties. "( [Clonidine in the treatment of cancer pain].
Nielsen, JB; Sjøgren, P, 2008
)
2.7
"Clonidine is an alpha(2) adrenoreceptor and imidazoline receptor agonist, which has analgesic, sedative, and minimum alveolar anesthetic concentration-sparing effects. "( The analgesic effect of epidural clonidine after spinal surgery: a randomized placebo-controlled trial.
Farmery, AD; Wilson-MacDonald, J, 2009
)
2.08
"Clonidine is a centrally acting, alpha-2 adrenergic agonist used for the treatment of hypertension during pregnancy. "( CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance.
Claessens, AJ; Easterling, TR; Eyal, S; Hebert, MF; Risler, LJ; Shen, DD, 2010
)
2.08
"Clonidine is an α(2)-adrenoceptor agonist which, by coupling with G-protein, has been proposed as an alternative treatment for refractory ascites of patients with cirrhosis for several years. "( Association of the G-protein and α2-adrenergic receptor gene and plasma norepinephrine level with clonidine improvement of the effects of diuretics in patients with cirrhosis with refractory ascites: a randomised clinical trial.
Chu, CJ; Hou, MC; Jap, JS; Lee, FY; Lee, SD; Lee, WP; Lin, HC; Lin, MW; Yang, YY, 2010
)
2.02
"  Clonidine is a potent sympatholytic drug with central neural effects. "( The effects of clonidine on arterial baroreflex sensitivity and cardiopulmonary baroreflex control of sympathetic nerve activity in patients with left ventricular dysfunction.
Iwasaka, T; Kawamura, A; Murakawa, K; Sugiura, T; Yokoe, H; Yoshida, S; Yuasa, F, 2011
)
1.44
"Apraclonidine seems to be a good alternative to cocaine to confirm Horner's syndrome."( [Acquired Horner's syndrome].
Alstadhaug, KB, 2011
)
0.85
"Clonidine is an agonist at the alpha2-adrenergic receptor that has been in clinical use for over 40 years."( Clonidine: clinical pharmacology and therapeutic use in pain management.
Neil, MJ, 2011
)
2.53
"  Clonidine is an alpha-2 agonist with a nearly 100% bioavailability after oral or rectal administration. "( Severe hypertension following accidental clonidine overdose during the refilling of an implanted intrathecal drug delivery system.
Bovy, M; Buchser, E; Durrer, A; Mustaki, JP; Perruchoud, C; Rosato, M; Rutschmann, B,
)
1.12
"Clonidine is a relative alpha2 agonist that's used as a premedicative drug in anesthesia in recent years. "( Effects of clonidine as premedication on plasma renin activity, serum and urine electrolytes and body fluids in general anesthesia. A randomized double blind placebo controlled clinical trial.
Kazemi, AH; Vahabi, S, 2011
)
2.2
"Clonidine is an α(2)-adrenergic agonist, historically known to treat high blood pressure. "( Clonidine-induced growth hormone and growth-hormone-releasing hormone release is mediated by tachykinin NK2 receptors in sheep.
Guillaume, V; Lemamy, GJ; Mouecoucou, J; Ndéboko, B; Oliver, C; Renard, M, 2012
)
3.26
"Clonidine hydrochloride is an alpha 2-agonist."( [A case of effective treatment with clonidine ointment for herpetic neuralgia after bone marrow transplantation in a child].
Arita, H; Hagihara, R; Hanaoka, K; Meno, A, 2002
)
1.31
"Clonidine is a medication long used to treat hypertension, and it is still used in the treatment of refractory hypertension. "( Clonidine-induced hypertension in a patient with a spinal lesion.
Backo, AL; Clause, SL; Gibbs, KA; Triller, DM, 2002
)
3.2
"Clonidine is an alpha 2 adrenergic agonist with analgesic properties. "( Comparison of morphine alone with morphine plus clonidine for postoperative patient-controlled analgesia.
Hall, JE; Jeffs, SA; Morris, S, 2002
)
2.01
"Clonidine hydrochloride is an alpha(2)-adrenergic agonist commonly prescribed as an antihypertensive agent. "( Intentional clonidine patch ingestion by 3 adults in a detoxification unit.
Rapko, DA; Rastegar, DA, 2003
)
2.14
"Clonidine is an effective spinal analgesic, but it is dose-limited by cardiovascular side effects. "( Continuous intrathecal clonidine and tizanidine in conscious dogs: analgesic and hemodynamic effects.
Ivankovich, AD; Kroin, JS; Lubenow, TJ; McCarthy, RJ; Penn, RD, 2003
)
2.07
"Clonidine is a well established antihypertensive agent that is also used effectively to treat a variety of psychiatric disorders. "( Differential expression of alpha2-adrenoceptor vs. imidazoline binding sites in postmortem orbitofrontal cortex and amygdala of depressed subjects.
Duncan, BJ; Halaris, AE; Klimek, V; May, W; Ordway, GA; Piletz, JE; Rajkowska, G; Swilley, S; Zhu, H,
)
1.57
"Clonidine is an NE alpha-2-receptor agonist, which has been considered to act mainly on the autoreceptors of presynaptic noradrenergic neurons to reduce their release of NE."( Clonidine effects on all-night human sleep: opposite action of low- and medium-dose clonidine on human NREM-REM sleep proportion.
Miyazaki, S; Mukai, J; Nishihara, K; Uchida, S, 2004
)
2.49
"Clonidine is a useful premedicant for pediatric anesthesia. "( Oral clonidine does not change ventilatory response to carbon dioxide in sevoflurane-anesthetized children.
Mikawa, K; Nishina, K; Obara, H; Uesugi, T, 2004
)
2.28
"Apraclonidine is an alpha2-adrenergic agonist, which causes Muller muscles to contract quickly elevating the upper eyelid 1-3 mm."( The use of apraclonidine eyedrops to treat ptosis after the administration of botulinum toxin to the upper face.
Scheinfeld, N, 2005
)
1.16
"Clonidine is an alpha2-adrenoceptor agonist exerting central sympatholytic effects."( [Clonidine in oral medicine. Literature review and our experience].
Grätz, KW; Mutzbauer, TS; Obwegeser, JA, 2005
)
1.96
"Clonidine is a classical sympatholytic drug that is widely used for the treatment of hypertension. "( Clonidine lowers blood pressure by reducing vascular resistance and cardiac output in young, healthy males.
Bührmann, S; Mitchell, A; Nürnberger, J; Opazo Saez, A; Philipp, T; Rushentsova, U; Schäfers, RF, 2005
)
3.21
"Apraclonidine eye drop is an alpha adrenergic agonist derived topical clonidine, used for the treatment of intraocular pressure elevation. "( More than just an ocular solution.
Karakus, G; Pekdemir, M; Yanturali, S, 2005
)
0.89
"clonidine 1 microg/kg is an effective method to prevent shivering in patients undergoing spinal anesthesia for orthopedic surgery."( Intrathecal clonidine does not reduce post-spinal shivering.
Bahk, JH; Do, SH; Jeon, YS; Jeon, YT; Kim, YC; Lim, YJ, 2005
)
1.43
"Clonidine is a mixed alpha (2)-/alpha (1)- adrenoceptor agonist. "( [Efficacy of clonidine in paediatric anaesthesia].
Huber, D; Kretz, FJ, 2005
)
2.14
"Apraclonidine is a safe and readily available alternative to cocaine for the diagnosis of Horner syndrome."( Effect of 0.5% apraclonidine on ptosis in Horner syndrome.
Garibaldi, DC; Grant, MP; Hindman, HB; Iliff, NT; Merbs, SL,
)
0.94
"Clonidine (CL) is a alpha2-adrenergic agonist that produces analgesia in animals and humans by a non-opiate alpha2-adrenergic action in the spinal cord dorsal horn. "( Clinical evaluation of clonidine added to lidocaine solution for subarachnoid analgesia in sheep.
Almeida, RG; DeRossi, R; Frazílio, FO; Medeiros, U; Righetto, FR, 2006
)
2.09
"Clonidine is a good option for managing core behavioral symptoms, especially hyperactivity and impulsivity."( Advances in alternative pharmacotherapy of ADHD.
Pityaratstian, N, 2005
)
1.05
"Clonidine is a preferential alpha-2 agonist drug that has been used for over 35 years to treat hypertension. "( Oral clonidine pretreatment prior to venous cannulation.
Hall, DL; Rezvan, E; Tatakis, DN; Walters, JD, 2006
)
2.29
"Clonidine is a frequently administered alpha2-adrenergic agonist which can decrease heart rate and blood pressure. "( Cardiac arrest in a child with cerebral palsy undergoing sevoflurane induction of anesthesia after preoperative clonidine.
Goldfinger, MM; Tripi, PA, 2007
)
1.99
"Clonidine is an alpha2 adrenoceptor agonist that is frequently used to reduce withdrawal symptoms during opioid detoxification in humans. "( Clonidine attenuates morphine withdrawal and subsequent drug sensitization in rhesus monkeys.
Chen, SQ; Cui, YY; Le Foll, B; Lu, L; Shi, J; Zhai, HF, 2007
)
3.23
"Clonidine test proved to be an excellent test for initial assessment of GHD and may be used as a screening test for short stature in third world countries."( Growth hormone deficiency short stature in a third world adult endocrine clinic: usefulness of clonidine test in its diagnosis.
Al-Ruhaily, AD; Malabu, UH, 2008
)
2.01
"Clonidine is a potent agonist of both types and phentolamine behaves as a non-selective antagonist."( Postsynaptic alpha 1- and alpha 2-adrenoceptors in the circulatory system of the pithed rat: selective stimulation of the alpha 2-type by B-HT 933.
Timmermans, PB; Van Zwieten, PA, 1980
)
0.98
"Clonidine is an alpha 2-receptor agonist which lowers both blood pressure and plasma norepinephrine (NE) levels in man. "( Dose-dependent suppression of norepinephrine appearance rate in plasma by clonidine in man.
Best, JD; Halter, JB; Veith, RC, 1984
)
1.94
"Clonidine is a safe and useful drug to obtain a fall of high blood pressure often complicating AMI, without depressing left ventricular performance, as suggested by no significant changes of CI, WP and LVSWI."( [Hemodynamic effects of intravenous clonidine in patients with acute myocardial infarction].
Foresti, A; Lotto, A; Massari, FM; Moglia, F, 1982
)
1.26
"Clonidine is an important new treatment option for selected opiate addicts and may be the treatment of choice when detoxification using methadone is inappropriate, unsuccessful, or unavailable."( Clonidine in opiate withdrawal: review and appraisal of clinical findings.
Resnick, RB; Washton, AM,
)
2.3
"Clonidine is an effective and safe therapy when used as the sole medication in treating mild-to-moderate hypertension."( Hormonal and hemodynamic effects of short- and long-term clonidine therapy in patients with mild-to-moderate hypertension.
Barrett, JD; Eggena, P; Golub, MS; Sambhi, MP; Thananopavarn, C, 1983
)
1.23
"Clonidine is a symptomatic medication that makes flushing more tolerable and should reduce the number of patients who would otherwise be exposed to the risks of estrogens."( Clonidine (Dixarit) for menopausal flushing.
Chagnon, JP; Edington, RF; Steinberg, WM, 1980
)
2.43
"Clonidine appears to be a reliable, sensitive, and safe out-patient stimulation test of growth hormone reserve in prepubertal children, whereas metoclopramide seems not to be a suitable growth hormone-releasing agent in this age group."( Oral clonidine-an effective growth hormone-releasing agent in prepubertal subjects.
Hurtado, E; Lanes, R, 1982
)
1.5
"Clonidine is an effective emergency treatment for acute opiate withdrawal and in the detoxification of methadone, heroin, and other opiate addictions."( Clonidine: inpatient studies from 1978 to 1981.
Extein, I; Gold, MS; Pottash, AL, 1982
)
2.43
"Clonidine is a safe and inexpensive means of achieving rapid opiate withdrawal."( The use of clonidine for management of opiate abstinence in a chronic pain patient.
Bakris, GL; Cross, PD; Hammarsten, JE, 1982
)
1.38
"Clonidine is an antihypertensive agent with a primary action mediated by alpha adrenergic stimulation in the central nervous system, thus inhibiting sympathetic efferent activity. "( Clonidine attenuation of a cardiogenic hypertensive chemoreflex.
Hageman, GR; James, TN; Swatzell, RH; Urthaler, F,
)
3.02
"Clonidine is a centrally acting antihypertensive drug that also has marked renal effects. "( Effect of prostaglandin synthesis inhibitors on clonidine-induced diuresis in rats.
Barr, JG; Kauker, ML, 1981
)
1.96
"Clonidine is a specific alpha-2-adrenoreceptor agonist that stimulates growth hormone (GH) release in animals and humans. "( Inverse control of growth hormone and prolactin secretion in clonidine-stimulated dairy cattle.
Berrini, A; Borromeo, V; Möller, F; Secchi, C, 1995
)
1.98
"Clonidine is an alpha-adrenergic agent that is used in the treatment of hypertension. "( Clonidine-induced bradycardia.
Blount, BW; Golusinski, LL, 1995
)
3.18
"Clonidine is a poor inhibitor (K0.5 = 200 microM) while cimetidine had no effect on the antiporter up to concentration of 1 mM."( Amiloride and harmaline are potent inhibitors of NhaB, a Na+/H+ antiporter from Escherichia coli.
Padan, E; Pinner, E; Schuldiner, S, 1995
)
1.01
"Clonidine is a useful drug to give preoperatively because it produces anxiolysis, sedation, and hemodynamic stability, and reduces intravenous and volatile anesthetic requirements. "( Clonidine decreases the dose of thiamylal required to induce anesthesia in children.
Maekawa, N; Mikawa, K; Nishina, K; Obara, H; Takao, Y, 1994
)
3.17
"Clonidine is a limited aid in cessation, and drug effects come primarily from women at high risk for treatment failure."( Smoking cessation, clonidine, and vulnerability to nicotine among dependent smokers.
Cooper, TB; Covey, LS; Dalack, GW; Fleiss, J; Glassman, AH; Rivelli, SK; Stetner, F, 1993
)
1.34
"Clonidine seems to be a good alternative to neuroleptics when these are not tolerated."( [Indications for clonidine in child psychiatry].
Dollfus, S,
)
1.19
"Clonidine is an effective preanesthetic medication in children, providing a preoperative sedative effect. "( Oral clonidine premedication reduces postoperative pain in children.
Maekawa, N; Mikawa, K; Nishina, K; Obara, H, 1996
)
2.25
"Clonidine is a rare, but important, atypical drug of abuse."( Atypical drug abuse: a case report involving clonidine.
Dy, EC; Yates, WR, 1996
)
1.28
"Clonidine is an alpha 2-adrenoceptor agonist increasingly used in combination with lignocaine for spinal or epidural anaesthesia because of a prolonged analgesic effect. "( Clonidine and or adrenaline decrease lignocaine plasma peak concentration after epidural injection.
Benhamou, D; Mazoit, JX; Samii, K; Veillette, Y, 1996
)
3.18
"Oral clonidine is a useful component to postoperative balanced analgesia as it decreases PCA morphine requirements and decreases the incidence of nausea and vomiting."( Oral clonidine reduces postoperative PCA morphine requirements.
Beattie, S; Bhola, D; Chu, C; Forrest, J; Kolesar, R; Park, J, 1996
)
1.32
"Clonidine is an alpha-adrenergic agonist which may alleviate emerging symptoms in Tourette syndrome, an observation that has fueled speculation regarding involvement of stress-sensitive central noradrenergic systems in this disorder. "( Predictors of clonidine response in Tourette syndrome: implications and inferences.
Jackson, LA; Lichter, DG, 1996
)
2.1
"Apraclonidine is a alpha 2 adrenergic agonic which is a para-amino derivative of clonidine. "( [Effect and side effects of apraclonidine].
Stewart, WC, 1996
)
1.14
"Clonidine is a centrally acting alpha 2-adrenergic agonist used in many psychiatric studies to assess adrenergic functioning. "( The stability of plasma growth hormone and MHPG responses to repeated clonidine challenge in normal males.
Coccaro, EF; Gabriel, SM; Knott, P; Lawrence, T; Siever, LJ; Trestman, RL, 1994
)
1.97
"Clonidine is a centrally active alpha 2-adrenoceptor agonist that raises concentrations of GH in serum in healthy people and those with pure autonomic failure (with peripheral lesions), but not in those with MSA (with a central autonomic deficit). "( Distinction of idiopathic Parkinson's disease from multiple-system atrophy by stimulation of growth-hormone release with clonidine.
Kimber, JR; Mathias, CJ; Watson, L, 1997
)
1.95
"Clonidine is a centrally acting antihypertensive and has been prescribed widely for more than 20 years. "( Clonidine does not potentiate the antipsychotic effects of neuroleptics in chronically ill patients.
Bigelow, LB; El-Mallakh, RS; Elkashef, A; Hedges, S; Issa, F; Wyatt, RJ, 1998
)
3.19
"Clonidine is an alpha 2-adrenoceptor agonist which has been used for over 20 years to treat hypertension. "( The role of clonidine in anaesthesia.
Eltringham, R; Sanderson, PM, 1998
)
2.12
"Clonidine is a selective alpha 2 adrenergic receptors agonist with a wide spectrum of activity. "( [Use of clonidine for perioperative therapy].
Fidziańska-Długosz, E, 1998
)
2.18
"Clonidine overdose is a potentially serious condition, often requiring intensive care management. "( Clonidine overdose in childhood: implications of increased prescribing.
Hanson, RM; Hutchins, P; Kappagoda, C; Schell, DN, 1998
)
3.19
"Oral clonidine is an effective analgesic and sedative for children undergoing tonsillectomy or adenotonsillectomy."( The effectiveness of clonidine as an analgesic in paediatric adenotonsillectomy.
Dunn, GS; Merrick, PM; Montgomery, CJ; Reimer, EJ; Sanderson, PM; Scheepers, LD, 1998
)
1.13
"Clonidine HCl is an antihypertensive that is also sometimes used to alleviate symptoms of withdrawal during narcotics detoxification. "( Evaluation of the intravenous reinforcing effects of clonidine in baboons.
Griffiths, RR; Weerts, EM, 1999
)
2
"Clonidine also proved to be a better agent for the attenuation of pressor response to laryngoscopy and intubation."( A comparative study of clonidine versus a combination of diazepam and atropine for premedication in orthopaedic patients.
Chaudhari, LS; Chaurasia, SK; Kane, DG,
)
1.16
"Clonidine is a widely prescribed, centrally acting antihypertensive with proposed pharmacologic mechanisms of stimulation of central postsynaptic alpha(2)-adrenergic receptors and agonist activity at presynaptic alpha(2)-adrenergic receptors, interfering with peripheral regulation of norepinephrine and acetylcholine release. "( The effect of chronic clonidine administration on salivary glands and caries in the rat.
Bowen, WH; Pearson, SK; Watson, GE,
)
1.89
"Clonidine is a commonly used alpha-adrenergic agonist. "( Hypertensive crisis and myocardial infarction following massive clonidine overdose.
Frye, CB; Vance, MA, 2000
)
1.99
"Clonidine is a central acting a2-agonist used primarily as an antihypertensive agent. "( Clonidine toxicity in an adolescent patient.
Cox, R; Gitter, MF, 2000
)
3.19
"Clonidine is a partial agonist at brain alpha(2)-adrenoceptors (alpha(2)AR), but also has high affinity (K(D) = 51 nM) in homogenate binding assays for non-adrenergic imidazoline-binding sites (I-sites; imidazoline receptors). "( Autoradiographic comparison of [3H]-clonidine binding to non-adrenergic sites and alpha(2)-adrenergic receptors in human brain.
Duncan, BJ; Halaris, A; Ordway, GA; Piletz, JE; Zhu, H, 2000
)
2.02
"Clonidine is an adrenergic agonist with high affinity for alpha2 adrenoceptors that also has affinity for imidazoline receptors. "( Selective imidazoline I2 ligands do not show antidepressant-like activity in the forced swim test in mice.
Conway, MW; O'Neill, MF; Osborne, DJ; Woodhouse, SM, 2001
)
1.75
"Clonidine usually serves as a tic-suppressing agent in patients with Tourette syndrome. "( Clonidine treatment increases tics in patients with Tourette syndrome: case report.
Kessler, AR, 2001
)
3.2
"Clonidine is a potent antihypertensive drug that suppresses RAAS."( Clonidine provides opioid-sparing effect, stable hemodynamics, and renal integrity during laparoscopic cholecystectomy.
Koivusalo, AM; Laisalmi, M; Lindgren, L; Tikkanen, I; Valta, P, 2001
)
2.47
"Clonidine is a noradrenergic alpha2-receptor agonist which can decrease noradrenergic transmission by stimulating presynaptic alpha2-receptors."( Clonidine injections into the lateral nucleus of the amygdala block acquisition and expression of fear-potentiated startle.
Fendt, M; Schnitzler, HU; Schulz, B, 2002
)
2.48
"Clonidine is a valuable adjunct for conscious sedation and can be used safely for sympathicolysis, even in patients with aortic stenosis."( Difficult airway management in a patient with severe aortic stenosis, coronary artery disease, and heart failure.
Kulka, PJ; Tryba, M; Zenz, M, 2002
)
1.04
"Clonidine is a hypotensive drug acting as an alpha-mimetic agent in the central nervous system and causing cardiovascular depression. "( Clonidine effect on insulin secretion and lipolysis in man.
Martinelli, G; Pozza, G; Saibene, V; Vasconi, F,
)
3.02
"Clonidine hydrochloride is a new antihypertensive agent with a primary site of action in the central nervous system. "( Evaluation of clonidine hydrochloride (Catapres). A new antihypertensive agent.
Kosman, ME, 1975
)
2.06
"Clonidine is a clinically used antihypertensive which has been suggested to produce physiological changes in children after exposure in utero. "( Early postnatal clonidine treatment results in altered regional catecholamine utilisation in adult rat brain.
Boer, GJ; Feenstra, MG; van Galen, H, 1992
)
2.07
"Apraclonidine hydrochloride is a derivative of clonidine hydrochloride, an alpha 2-adrenergic agonist."( New developments in the drug treatment of glaucoma.
Crawford, K; Hurvitz, LM; Kaufman, PL; Robin, AL; Shaw, B; Weinreb, RN, 1991
)
0.76
"Clonidine is felt to be a logical and appropriate drug for the treatment of autonomic dysfunction in severe tetanus."( Management of autonomic dysfunction in severe tetanus: the use of magnesium sulphate and clonidine.
Nielsen, MS; Sutton, DN; Tremlett, MR; Woodcock, TE, 1990
)
1.22
"Clonidine is an antihypertensive agent with central and peripheral alpha-2 adrenergic effects. "( Pediatric clonidine intoxications.
Bamshad, MJ; Wasserman, GS, 1990
)
2.12
"Clonidine is a recommended antihypertensive for use during pregnancy, although little is known of its fetal effects. "( Effects of clonidine on breathing movements and electrocortical activity in the fetal lamb.
Bamford, OS; Blanco, CE; Hawkins, RL, 1990
)
2.11
"Clonidine is a centrally acting alpha 2-agonist whose clinical use has often been limited by the dose dependent side effects of dry mouth and sedation, and the belief that it should be given three times per day."( Comparison of pharmacokinetics and pharmacodynamics of adrenoceptor agonists and antagonists as antihypertensive agents.
Anavekar, SN; Conway, EL; Drummer, OH; Howes, LG; Jarrott, B; Louis, WJ; McNeil, JJ; Workman, B, 1987
)
0.99
"Clonidine, which is an alpha-2-agonist affected mostly the mucous cells, with formation of cytoplasmic vacuoles between the mucous droplets."( Salivary gland morphology after alpha-adrenergic and cholinergic stimulation. An ultrastructural study.
Lundquist, PG; Norberg, LE, 1988
)
1
"Clonidine was found to be a partial agonists producing 55% of the inhibition obtained with lofexidine."( Inhibition of adenylate cyclase in bovine ciliary process and rabbit iris ciliary body to alpha 2-adrenergic agonists.
Elko, EE; Jin, Y; Tran, T; Yorio, T, 1989
)
1
"Thus clonidine is a sensitive, easy to use and safe stimulator of STH secretion."( [The use of klofelin for studying somatotropin secretion in children].
Antoshkina, AN; Benikova, EA; Derevianko, DI; Epshteĭn, EV,
)
0.59
"Clonidine is a potent antihypertensive agent with a relatively low therapeutic index."( In vitro/in vivo functionality of Catapres-TTS.
Enscore, DJ; Osborne, JL; Shaw, JE, 1989
)
1
"Clonidine is an effective tool in the hospital preventive treatment of alcohol withdrawal."( [Use of clonidine in the prevention of alcohol withdrawal syndrome].
Ghiazza, GF; Mondavio, M, 1989
)
1.43
"Clonidine is an alpha-adrenergic agonist. "( Fetal effects of maternally administered clonidine and angiotensin-converting enzyme inhibitors.
Boutroy, MJ, 1989
)
1.99
"Clonidine is a centrally acting antihypertensive drug that acts in vivo at both alpha 1- and alpha 2-adrenoceptor sites, whereas rilmenidine (S 3341) is more selective for alpha 2 adrenoceptors. "( Effects of continuous infusions (10 days) and cessation of infusions of clonidine and rilmenidine (S 3341) on cardiovascular and behavioral parameters of spontaneously hypertensive rats.
Doyle, AE; Jarrott, B; Lewis, SJ; Louis, WJ, 1988
)
1.95
"Clonidine may prove to be a useful therapeutic adjunct in the treatment of spasticity."( Effect of clonidine on motoneuron excitability in spinalized rats.
Bedard, PJ; Tremblay, LE, 1986
)
1.39
"Clonidine is a central alpha adrenergic agonist which can be used to treat the opiate withdrawal syndrome. "( Clonidine and the treatment of the opiate withdrawal syndrome.
Gossop, M, 1988
)
3.16
"Clonidine (CLON), is a widely used antihypertensive agent with a potential for expanded therapeutic application in combating drug withdrawal symptoms in opiate and alcohol addiction. "( Behavioral evaluation of rats prenatally exposed to the adrenergic agonists clonidine and lofexidine.
Ali, SF; Holson, RR; Pizzi, WJ, 1988
)
1.95
"Clonidine is a centrally active antihypertensive agent effective in the treatment of mild, moderate and severe hypertension, alone or in combination with other drugs. "( Clinical pharmacokinetics of clonidine.
Lowenthal, DT; MacGregor, TR; Matzek, KM, 1988
)
2.01
"Clonidine is a centrally acting antihypertensive agent used in the management of essential hypertension. "( Reversal of clonidine toxicity by naloxone.
Getzug, T; Murphy, W; Niemann, JT, 1986
)
2.09
"Clonidine appears to be a safe and efficacious outpatient treatment for opiate withdrawal, although the results were less favorable than those obtained in open or inpatient studies."( Clonidine in outpatient detoxification from methadone maintenance.
Charney, D; Gaspari, J; Hogan, I; Kleber, HD; Kosten, T; O'Connor, C; Riordan, CE; Rounsaville, B, 1985
)
2.43
"Clonidine (Catapres) is a safe and effective agent for detoxification of selected opiate addicts. "( Opiate and cocaine dependencies. Techniques to help counter the rising tide.
Gold, MS; Pottash, AC; Washton, AM, 1985
)
1.71

Effects

Clonidine has a significant peripheral action in enhancing duration of local anesthesia on superficial co-infiltration with lidocaine. Yet Clonidine also has a sedative effect due to alpha (2)-adrenoceptor stimulation in the locus coeruleus.

Clonidine has both analgesic and sedative actions. It has been used in a variety of settings as a sedative, or both. Apraclonidine 1.0% has been shown to reverse the potential intraocular pressure increase in patients with chronic open-angle glaucoma.

ExcerptReferenceRelevance
"Clonidine has a narrow therapeutic index, and toxicity can occur with inadvertent double dosing."( Clonidine exposures in children under 6 (2004-2017): a retrospective study.
Brown, JA; Buckley, NA; Cairns, R, 2019
)
2.68
"Yet Clonidine also has a sedative effect due to alpha (2)-adrenoceptor stimulation in the locus coeruleus and antinociceptive action caused through postjunctional noradrenergic pathways in the brainstem and spinal cord."( [Efficacy of clonidine in paediatric anaesthesia].
Huber, D; Kretz, FJ, 2005
)
1.18
"Clonidine has a significant peripheral action in enhancing duration of local anesthesia on superficial co-infiltration with lidocaine."( Co-injection of clonidine prolongs the anesthetic effect of lidocaine skin infiltration by a peripheral action.
Goroszeniuk, T; Pratap, JN; Shankar, RK, 2007
)
2.13
"Clonidine has a poor intrinsic activity but antagonizes the action of epinephrine."( Adrenergic versus VIPergic control of cyclic AMP in human colonic crypts.
Boige, N; Laburthe, M; Munck, A,
)
0.85
"Clonidine has a contractile effect in the isolated rabbit aorta which can be blocked by alpha-adrenergic antagonist, phentolamine. "( Possible involvement of endogenous histamine in the myotropic effect of clonidine on the isolated rabbit aorta.
Bökesoy, TA; Ercan, ZS; Ersoy, F; Türker, RK; Zengil, H, 1978
)
1.93
"Clonidine has a dual action on naloxone-precipitated morphine withdrawal symptoms in rats: a suppressive action on body shakes and body weight loss and a potentiating action on jumping and aggression. "( Effects of alpha 2-agonists on morphine withdrawal behaviour: potentiation of jumping mediated by alpha 2-receptors.
van der Laan, JW, 1985
)
1.71
"Clonidine has similar pharmacological properties and can be administered both parenterally and orally."( Alpha-2-adrenergic receptor agonists for the prevention of delirium and cognitive decline after open heart surgery (ALPHA2PREVENT): protocol for a multicentre randomised controlled trial.
Busund, R; Haaverstad, R; Helbostad, JL; Landsverk, SA; Martinaityte, I; Neerland, BE; Norum, HM; Ræder, J; Selbaek, G; Simpson, MR; Skaar, E; Skjærvold, NK; Skovlund, E; Slooter, AJ; Svendsen, ØS; Tønnessen, T; Wahba, A; Wyller, TB; Zetterberg, H, 2022
)
1.44
"Clonidine has been clinically used to treat Tourette's syndrome for decades. "( Effects of 24 CYP2D6 variants found in Chinese population on the metabolism of clonidine in vitro.
Cai, JP; Hu, GX; Hu, XX; Li, XY; Yang, F; Yuan, LJ, 2019
)
2.18
"Clonidine dosages that have been assessed for discontinuing dexmedetomidine vary from 0.1 to 0.3 mg orally or enterally every 6 to 8 hours; one study assessed use of transdermal clonidine (100 µg/24 h patch)."( Clonidine as a strategy for discontinuing dexmedetomidine sedation in critically ill patients: A narrative review.
Attridge, RL; Christina Gutierrez, G; Glaess, SS, 2020
)
2.72
"Apraclonidine has been used as a diagnostic test in Horner's syndrome."( Apraclonidine in the treatment of ptosis.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
1.49
"Clonidine has not been systematically assessed for use in neonatal sedation during ventilation."( Clonidine for sedation and analgesia for neonates receiving mechanical ventilation.
Bruschettini, M; Calevo, MG; Norman, E; Romantsik, O, 2017
)
2.62
"Clonidine has been shown to reduce intraoperative haemodynamic instability."( Role of Oral Clonidine Premedication on Intra-operative Haemodynamics and PONV in Laparoscopic Cholecystectomy.
Banik, D; Haque, AK; Jahan, S; Masud, M; Saha, NC; Yeasmeen, S, 2017
)
1.55
"As clonidine has been associated with cardiovascular adverse effects, it should be administered only in cases where blood pressure regulation is mandatory."( Non-Hormonal Replacement Therapy Regimens: Do they have an Effect on Cardiovascular Risk?
Ampatzi, C; Goulis, DG; Mareti, E; Paschou, SA; Voziki, E, 2019
)
1.03
"Clonidine has become increasingly popular for management of paediatric behavioural disorders."( Clonidine exposures in children under 6 (2004-2017): a retrospective study.
Brown, JA; Buckley, NA; Cairns, R, 2019
)
2.68
"Clonidine has antiemetic and analgesic properties and thus may be used as premedication to reduce postoperative vomiting and pain."( Safety and efficacy of clonidine on postoperative vomiting and pain in pediatric ophthalmic surgery: A systematic review and meta-analysis.
Bai, CH; Chen, C; Chu, KC; Hsu, CW; Hsu, YP; Huang, CJ, 2019
)
1.55
"Clonidine has anesthetic-sparing properties and it may reduce the hemodynamic and psychological effects of S+ ketamine. "( Clonidine for reduction of hemodynamic and psychological effects of S+ ketamine anesthesia for dressing changes in patients with major burns: an RCT.
Pretto, G; Silva, E; Westphal, GA, 2014
)
3.29
"Clonidine has been advocated as a valid alternative for premedication in children but one of the few limitations is its association with reduced heart rate (HR), which thus raises the question of the safety of clonidine as premedication in children. "( Incidence of bradycardia at arrival to the operating room after oral or intravenous premedication with clonidine in children.
Eksborg, S; Larsson, PG; Lönnqvist, PA, 2015
)
2.07
"Clonidine has been used as an alternative in pregnant or postpartum women with contraindications to captopril, with satisfactory effect."( Clonidine versus Captopril for Severe Postpartum Hypertension: A Randomized Controlled Trial.
Amorim, MM; Coutinho, IC; Katz, L; Maia, SS; Noronha Neto C, C; Souza, AR, 2017
)
2.62
"Clonidine has been used in anesthesia for its sedative and analgesic properties, and to achieve greater hemodynamic stability with reduction in intra-ocular pressure. "( Preoperative intravenous clonidine in the surgical treatment of cataract: evaluation of the clinical benefits.
de Freitas, JC; Fortis, EA; Homrich, PH; Lemes, ET; Stolz, AP; Van Der Fritz, F,
)
1.88
"Clonidine and ET have been reported to have cardiovascular interactions involving the sympathetic nervous system, but it is not known whether ETA receptor antagonist affects clonidine analgesia."( Involvement of imidazoline and opioid receptors in the enhancement of clonidine-induced analgesia by sulfisoxazole.
Andurkar, SV; Boxwalla, M; Gulati, A; Matwyshyn, G; Puppala, BL, 2010
)
1.32
"Clonidine has proven to be effective in reducing the incidence of post-operative agitation at a higher dose (3 and 2 μg kg⁻¹)."( Efficacy of low-dose caudal clonidine in reduction of sevoflurane-induced agitation in children undergoing urogenital and lower limb surgery: a prospective randomised double-blind study.
Agarwala, RB; Ghosh, SM; Pandey, M; Vajifdar, H, 2011
)
1.38
"Clonidine has the potential to significantly prolong the duration of caudal epidural anesthesia. "( Effect of epidural clonidine on minimum local anesthetic concentration (ED50) of levobupivacaine for caudal block in children.
Alberighi, OD; Disma, N; Frawley, G; Mameli, L; Montobbio, G; Pistorio, A; Tuo, P, 2011
)
2.14
"Clonidine has many beneficial effects in the perioperative period."( Onset time for pharmacologic premedication with clonidine as a nasal aerosol: a double-blind, placebo-controlled, randomized trial.
Eksborg, S; Larsson, P; Lönnqvist, PA, 2012
)
1.36
"Clonidine has been shown to reduce perioperative circulatory instability. "( Oral clonidine premedication preserves heart rate variability for patients undergoing larparoscopic cholecystectomy.
Chan, KH; Hseu, SS; Teng, YH; Yien, HW; Yu, HP, 2003
)
2.28
"Clonidine hydrochloride has been used for pre-anesthetic medication to provide a pre-operative sedation in pediatric surgery. "( Sedation and plasma concentration of clonidine hydrochloride for pre-anesthetic medication in pediatric surgery.
Baba, Y; Homma, M; Inomata, S; Kihara, S; Kohda, Y; Sumiya, K; Toyooka, H; Watanabe, M, 2003
)
2.03
"Clonidine has analgesic properties. "( Transdermal clonidine: does it affect pain after abdominal hysterectomy?
Dimou, P; Fassoulaki, A; Papilas, K; Paraskeva, A, 2003
)
2.14
"Clonidine has cardiac and systemic effects that can modify the potentially lethal cardiovascular effects of local anaesthetics. "( Effects of clonidine pre-treatment on bupivacaine and ropivacaine cardiotoxicity in rats.
Aydin, Y; Gulec, S; Senturk, Y; Uzuner, K; Yelken, B, 2004
)
2.16
"Clonidine has been shown to prolong sensory analgesia when given as an adjunct to peripheral nerve blocks but has not been evaluated when given in conjunction with a femoral-sciatic nerve block. "( The addition of clonidine to bupivacaine in combined femoral-sciatic nerve block for anterior cruciate ligament reconstruction.
Couture, DJ; Cuniff, HM; Maye, JP; Pellegrini, J, 2004
)
2.11
"Clonidine has shown considerable analgesic effect, with minimal adverse effects."( Non-narcotic adjuvants may improve the duration and quality of analgesia after knee arthroscopy: a brief review.
Brill, S; Plaza, M, 2004
)
1.04
"Yet Clonidine also has a sedative effect due to alpha (2)-adrenoceptor stimulation in the locus coeruleus and antinociceptive action caused through postjunctional noradrenergic pathways in the brainstem and spinal cord."( [Efficacy of clonidine in paediatric anaesthesia].
Huber, D; Kretz, FJ, 2005
)
1.18
"Clonidine has contrary to midazolam no effect on respiration."( Clonidine in paediatric anaesthesia: review of the literature and comparison with benzodiazepines for premedication.
Bergendahl, H; Eksborg, S; Lönnqvist, PA, 2006
)
2.5
"Clonidine has been used for many purposes, including reduction of blood pressure in hypertension, reduction in alcohol and drug withdrawal phenomena, reduction in nicotine withdrawal symptoms during smoking cessation, analgesia, reduction in stress response, and now as an anti-ischemic agent to reduce the risk of perioperative myocardial ischemia and perioperative mortality."( Clonidine and modification of perioperative outcome.
Wallace, AW, 2006
)
3.22
"Clonidine has recently been used as a pre-operative medication and sedative/anxiolytic drug. "( Oral clonidine pre-treatment and diazepam/meperidine sedation.
Hall, DL; Rezvan, E; Tatakis, DN; Walters, JD, 2006
)
2.29
"As clonidine has immunomodulating properties via reducing sympathetic activity, this study involved the analysis of T-cell function in the early postoperative period in patients undergoing coronary artery bypass graft surgery."( Clonidine attenuated early proinflammatory response in T-cell subsets after cardiac surgery.
Baehr, N; Braun, JP; Hein, OV; Konertz, W; Moshirzadeh, M; Sander, M; Spies, CD; von Dossow, V; von Heymann, C; Wernecke, KD, 2006
)
2.29
"Clonidine has often been applied in combination with local anaesthetics for spinal or epidural anaesthesia. "( Clonidine reduces the excitability of spinal dorsal horn neurones.
Hempelmann, G; Heugel, P; Mühling, J; Olschewski, A; Scholz, A; Wolff, M, 2007
)
3.23
"Clonidine has a significant peripheral action in enhancing duration of local anesthesia on superficial co-infiltration with lidocaine."( Co-injection of clonidine prolongs the anesthetic effect of lidocaine skin infiltration by a peripheral action.
Goroszeniuk, T; Pratap, JN; Shankar, RK, 2007
)
2.13
"Apraclonidine eye drops have been suggested to diagnose Horner syndrome."( The pupil.
Wilhelm, H, 2008
)
0.83
"Clonidine has a poor intrinsic activity but antagonizes the action of epinephrine."( Adrenergic versus VIPergic control of cyclic AMP in human colonic crypts.
Boige, N; Laburthe, M; Munck, A,
)
0.85
"Clonidine has clearly been shown to be effective in the treatment of all grades of hypertension. "( Clonidine in the treatment of hypertension.
Garrett, BN; Kaplan, NM, 1980
)
3.15
"clonidine has enjoyed an ever-growing popularity in psychoneuroendocrinology research as a central NE agonist."( The use and abuse of clonidine as a psychopharmacological tool.
Flemenbaum, A, 1981
)
1.3
"Clonidine and NE have been reported to decrease or have no effect on chronotropic responses to cardiac nerve stimulation."( Controversial evidence regarding the functional importance of presynaptic alpha receptors.
Robie, NW, 1984
)
0.99
"Clonidine has been reported to adversely affect glucose tolerance in experimental animals and normal man. "( Clonidine in patients with diabetes and mild hypertension.
Guthrie, GP; Koenig, SH; Kotchen, TA; Miller, RE, 1983
)
3.15
"Clonidine has been used successfully in the treatment of opiate dependence. "( Influence of clonidine on the acute dependence response elicited in naive rats by naloxone.
Eisenberg, RM, 1983
)
2.08
"Clonidine has been reported to produce its cardiovascular effects through an interaction with opioid and alpha 2-adrenergic receptors."( Opioidergic receptors in the arcuate nucleus are not involved in the cardiovascular effects of clonidine.
Barber, DA; Tackett, RL, 1994
)
1.23
"Clonidine has been shown to be an effective postoperative analgesia when applied epidurally."( Prevention of phantom pain after major lower limb amputation by epidural infusion of diamorphine, clonidine and bupivacaine.
Bradley, JW; Dark, CH; Jahangiri, M; Jayatunga, AP, 1994
)
1.23
"Clonidine has affinity for both I1 and alpha 2-adrenoceptors; guanabenz represents a useful pharmacological tool, since it activates only the alpha 2-adrenoceptor."( Mediation of the hypotensive action of systemic clonidine in the rat by alpha 2-adrenoceptors.
Hieble, JP; Kolpak, DC, 1993
)
1.26
"Clonidine has been demonstrated to attenuate many of these undesirable effects when used as a premedicant."( Oral clonidine premedication attenuates the haemodynamic effects associated with ketamine anaesthetic induction in humans.
Doak, GJ; Duke, PC, 1993
)
1.52
"Clonidine's efficacy has been equivocal."( Cigarette smoking, nicotine addiction, and its pharmacologic treatment.
D'Alonzo, GE; Lee, EW, 1993
)
1.01
"Clonidine has been suggested as an alternative pharmacotherapy for patients with attention-deficit hyperactivity disorder (ADHD) and comorbid tic disorders. "( Comparison of clonidine response in the treatment of attention-deficit hyperactivity disorder with and without comorbid tic disorders.
Biederman, J; Gonzalez, A; Spencer, T; Steingard, R; Wilens, T, 1993
)
2.09
"Clonidine has been shown to reduce some opiate withdrawal signs in morphine-dependent animals."( [Changes in alpha 2-adrenoceptor binding nature in guinea-pig brain following the development of morphine dependence].
Asano, T; Dohi, S; Niwa, M; Nozaki, M; Ohta, S; Takeda, T, 1997
)
1.02
"Clonidine has sedative and anxiolytic properties and reduces the requirement for inhalation agents."( Oral clonidine premedication reduces minimum alveolar concentration of sevoflurane for tracheal intubation in children.
Maekawa, N; Mikawa, K; Nishina, K; Obara, H; Shiga, M, 1997
)
1.53
"Clonidine has not been adequately examined but seems to have small or uncertain effects."( Antidepressants in the treatment of attention-deficit/hyperactivity disorder.
Popper, CW, 1997
)
1.02
"Clonidine has some appliance during perioperative period."( [Use of clonidine for perioperative therapy].
Fidziańska-Długosz, E, 1998
)
1.46
"Clonidine has both analgesic and sedative actions, and it has been used in a variety of settings as a sedative, or both. "( Oral clonidine for sedation and analgesia in a burn patient.
Asada, A; Kariya, N; Nishi, S; Shindoh, M; Yukioka, H, 1998
)
2.26
"Clonidine has been shown to reduce perioperative circulatory instability."( Cardiac baroreflex during the postoperative period in patients with hypertension: effect of clonidine.
Annat, G; Bégou, G; Bonnet, F; Cottet-Emard, JM; Ghignone, M; Hughson, R; Levron, JC; Parlow, JL; Quintin, L; Sagnard, P; Viale, JP, 1999
)
1.24
"Apraclonidine 1.0% has been shown to reverse the potential intraocular pressure (IOP) increase after pupil dilation IOP increases in patients with chronic open-angle glaucoma. "( Reversal of intraocular pressure increases with 0.5% apraclonidine after dilated fundus examination in patients with chronic open-angle glaucoma.
Chang, FW; Kolin, T; Nishimoto, JH; Tang, IH, 1999
)
1.11
"Clonidine has been added to local anesthetic regimens for various peripheral nerve blocks, resulting in prolonged anesthesia and analgesia. "( Intravenous regional anesthesia using lidocaine and clonidine.
Klatt, JL; Klatt, ML; Reuben, SS; Steinberg, RB, 1999
)
2
"Clonidine premedication has been reported to control blood pressure intra- and postoperatively, as well as to reduce the requirements for hypnotic agents."( Clonidine premedication decreases propofol consumption during bispectral index (BIS) monitored propofol-ketamine technique for office-based surgery.
Friedberg, BL; Sigl, JC, 2000
)
2.47
"Clonidine has previously been shown to reduce immobility in the forced swim test (FST) in mice."( Selective imidazoline I2 ligands do not show antidepressant-like activity in the forced swim test in mice.
Conway, MW; O'Neill, MF; Osborne, DJ; Woodhouse, SM, 2001
)
1.03
"The clonidine test has been proposed as diagnostic biochemical test for patients with clinical suspicion of pheochromocytoma."( [Usefulness of the clonidine test for the diagnosis of pheochromocytoma].
Fernández-Torres, C; Hidalgo Tenorio, C; Jiménez-Alonso, J; León-Ruiz, L; López de la Torre Casares, M; Mediavilla García, JD; Piédrola Maroto, G; Pinel Julián, P, 2001
)
1.2
"Clonidine has been proposed to differentiate multiple system atrophy (MSA) from idiopathic Parkinson's disease (IPD), as it does not increase growth hormone (GH) release in MSA. "( Stimulation of growth hormone release in multiple system atrophy, Parkinson's disease and idiopathic cerebellar ataxia.
Barone, P; Colao, AM; De Michele, G; Faggiano, A; Filla, A; Pellecchia, MT; Pivonello, R; Salvatore, E, 2001
)
1.75
"Both clonidine and ketamine have been found to prolong the action of local anesthetics through a peripheral mechanism. "( Clonidine versus ketamine to prevent tourniquet pain during intravenous regional anesthesia with lidocaine.
Alvanos, DN; Giala, MM; Gorgias, NK; Karakoulas, KA; Kyriakidis, AM; Maidatsi, PG,
)
2.09
"Clonidine has a contractile effect in the isolated rabbit aorta which can be blocked by alpha-adrenergic antagonist, phentolamine. "( Possible involvement of endogenous histamine in the myotropic effect of clonidine on the isolated rabbit aorta.
Bökesoy, TA; Ercan, ZS; Ersoy, F; Türker, RK; Zengil, H, 1978
)
1.93
"Clonidine has no significant effect on the accumulation of cyclic AMP elicited by submaximal concentrations of isoproterenol in cerebellar slices."( Interaction of clonidine with pre- and post-synaptic adrenergic receptors of rat brain: effects on cyclic AMP-generating systems.
Daly, JW; Skolnick, P, 1976
)
1.33
"Clonidine has been reported to possess the ability to block the depressant actions of purine compounds on the firing of rat cerebral cortical neurons. "( Is clonidine an adenosine antagonist?
Kirkpatrick, JR; Phillis, JW, 1979
)
2.32
"Clonidine hydrochloride has been demonstrated to produce vasoconstriction in the anterior segment of the cat eye. "( Clonidine.
Cevario, SJ; Macri, FJ, 1978
)
3.14
"Clonidine has been used to assist opiate detoxification in the past 10 years. "( Two cases of clonidine abuse/dependence in methadone-maintained patients.
Lauzon, P, 1992
)
2.1
"Clonidine tablets have been used in the past for treatment of spasticity with some success. "( Clonidine transdermal system for treatment of spasticity in spinal cord injury.
Belen, JG; Weingarden, SI, 1992
)
3.17
"Clonidine has been reported to be effective as an alpha 2-adrenoceptor agonist. "( [Effect of chronic desipramine treatment on rat brain adrenergic alpha 2-receptor].
Kunimi, Y; Naitoh, H; Nomura, S; Sekiya, Y; Sugita, R, 1991
)
1.72
"Clonidine has previously been shown to lower IOP significantly, but has the potential to produce marked lowering of both systolic and diastolic blood pressures."( New developments in the drug treatment of glaucoma.
Crawford, K; Hurvitz, LM; Kaufman, PL; Robin, AL; Shaw, B; Weinreb, RN, 1991
)
1
"Clonidine has some central component for induction of postural hypotension in addition to the frequency-related peripheral component."( Evaluation of the central and peripheral components for induction of postural hypotension by guanethidine, clonidine, dopamine2 receptor agonists and 5-hydroxytryptamine1A receptor agonists.
Cannon, JG; Long, JP; Park, KH, 1991
)
1.22
"Clonidine has been proposed as a premedication before surgery because of its beneficial effects on hemodynamics, especially in patients with a high cardiovascular risk. "( Ventilatory effects of premedication with clonidine.
Benhamou, D; Ecoffey, C; Narchi, P; Veillette, Y, 1991
)
1.99
"Clonidine has been reported to produce analgesia in man after epidural and intrathecal administration. "( Evaluation of the toxicity of subarachnoid clonidine, guanfacine, and a substance P-antagonist on rat spinal cord and nerve roots: light and electron microscopic observations after chronic intrathecal administration.
Gordh, T; Olsson, Y; Post, C, 1986
)
1.98
"Clonidine hydrochloride has been reported to reduce tobacco withdrawal symptoms and facilitate smoking cessation. "( Randomized, controlled trial of clonidine for smoking cessation in a primary care setting.
Bell, B; Franks, P; Harp, J, 1989
)
2
"Clonidine has been used in the management of hypertension in adults with few cases of cardiac dysrhythmia reported. "( Cardiac dysrhythmia with the use of clonidine in explosive disorder.
Dawson, PM; Tyma, TA; Vander Zanden, JA; Washington, RL; Werkman, SL, 1989
)
1.99
"Clonidine has a dual action on naloxone-precipitated morphine withdrawal symptoms in rats: a suppressive action on body shakes and body weight loss and a potentiating action on jumping and aggression. "( Effects of alpha 2-agonists on morphine withdrawal behaviour: potentiation of jumping mediated by alpha 2-receptors.
van der Laan, JW, 1985
)
1.71
"Clonidine has previously been shown to potentiate HIB in guinea pigs."( Effects of rilmenidine on bronchomotor responses in the guinea pig.
Clerici, C; Harf, A; Macquin-Mavier, I, 1988
)
1
"Clonidine has been reported to produce analgesia in humans in different painful conditions. "( Epidural clonidine for treatment of postoperative pain after thoracotomy. A double-blind placebo-controlled study.
Gordh, T, 1988
)
2.13
"Clonidine has been reported to exert anti-anxiety effects in animals and man similar to those of benzodiazepines. "( The effects of clonidine on the partial reinforcement extinction effect (PREE).
Feldon, J; Halevy, G; Weiner, I, 1986
)
2.07
"Clonidine has been incorporated into a small, pliable adhesive cutaneous delivery device designed to provide therapeutically effective doses of drug at a constant rate for at least 7 days."( Clinical pharmacokinetics of clonidine.
Lowenthal, DT; MacGregor, TR; Matzek, KM, 1988
)
1.29
"Clonidine has been suggested to be effective in Gilles de la Tourette's syndrome (GTS), but no double-blind study has ever evaluated its effects using objective measures. "( Clonidine and Gilles de la Tourette's syndrome: double-blind study using objective rating methods.
Carroll, VS; Como, PG; Goetz, CG; Shannon, KM; Tanner, CM; Wilson, RS, 1987
)
3.16
"Clonidine has provided a nonaddicting solution to an ancient problem, opiate withdrawal without opiates. "( Clonidine.
Gold, MS; Roehrich, H, 1987
)
3.16
"Clonidine has been reported to transiently impair glucose tolerance."( Nephrotic-range proteinuria and hyperglycemia associated with clonidine therapy.
Josselson, J; Sadler, JH, 1986
)
1.23
"Clonidine has dual effects on human platelets, since it can imitate adrenaline and synergize with PAF-acether in some subjects, and can also block aggregation induced by adrenaline alone or in combination with PAF-acether."( Potentiation and inhibition by clonidine of PAF-acether-induced human platelet activation.
Fouque, F; Vargaftig, BB, 1987
)
1.28

Actions

Clonidine did not cause allergic reaction in patients with proven allergy to apraclonidine. Clonidine displayed lower efficacy than S18616, was substantially less potent, and had marked affinity for imidazoline(1) sites and alpha(1)-ARs.

ExcerptReferenceRelevance
"Clonidine resulted in lower mean (SD) area under the curve for systolic blood pressure (fentanyl 106.5 [11.0]; clonidine 95.7mmHg [7.9]) and heart rate (fentanyl 104.9 beats per minute [13.6]; clonidine 85.3 [11.5]; p<0.001)."( Comparison of lumbar epidural bupivacaine with fentanyl or clonidine for postoperative analgesia in children with cerebral palsy after single-event multilevel surgery.
Chalkiadis, GA; Dowden, SJ; Graham, HK; Low, J; Orsini, F; Penrose, S; Pirpiris, M; Sommerfield, D; Tay, M, 2016
)
1.4
"Clonidine-induced increase in basal cortisol levels was blocked by the ADRA2A antagonist yohimbine."( Systematic analysis of G protein-coupled receptor gene expression in adrenocorticotropin-independent macronodular adrenocortical hyperplasia identifies novel targets for pharmacological control of adrenal Cushing's syndrome.
Assie, G; Bertherat, J; Chabre, O; Cherradi, N; Clauser, E; Feige, JJ; Groussin, L; Lefebvre, H; Louiset, E; René-Corail, F; Sturm, N; Thomas, M, 2010
)
1.08
"Clonidine produced an increase in ET(A) receptor expression in the brain and abdominal aorta while ET(B) receptors were not affected."( Endothelin modulates the cardiovascular effects of clonidine in the rat.
Briyal, S; Gulati, A; Lavhale, MS; Parikh, N, 2010
)
1.33
"Apraclonidine 0.5% did not produce a significant effect on pupil diameter."( Pupillometry study of brimonidine tartrate 0.2% and apraclonidine 0.5%.
Besada, E; Hardigan, P; Najman, P; Reed, K; Shechtman, D, 2011
)
1.1
"The clonidine group had lower VPS at rest (2.3 vs 3.7, P<0.001 with 95% confidence interval [CI] of difference of 1.4 [1.1, 1.7]) on POD0."( A prospective survey of patient-controlled epidural analgesia with bupivacaine and clonidine after total hip replacement: a pre- and postchange comparison with bupivacaine and hydromorphone in 1,000 patients.
Bae, JJ; Bieltz, M; Liu, SS; Ma, Y; Wukovits, B, 2011
)
1.08
"Clonidine nasal drops produce a similar sedative effect as after oral administration but do not reduce the onset time."( Onset time for pharmacologic premedication with clonidine as a nasal aerosol: a double-blind, placebo-controlled, randomized trial.
Eksborg, S; Larsson, P; Lönnqvist, PA, 2012
)
1.36
"Clonidine reduced the increase in BUN and serum creatinine concentration in envenomed mice."( Effect of clonidine in mice injected with Tityus discrepans scorpion venom.
Bermúdez, V; García, F; Gutiérrez, L; Rodríguez, A; Ruiz, A; Silva, A; Villasmil, S; Zerpa, H, 2013
)
1.51
"Clonidine and RU-1117 produce opposite effects on platelet aggregation induced by ADP in low concentrations."( Mechanisms underlying combined action of clonidine and local anesthetics.
Anisimova, VA; Dukhanin, AS; Galenko-Yaroshevskii, AP; Ponomarev, VP, 2003
)
1.31
"Clonidine was able to produce an analgesic effect but failed to provide maximal analgesia in all horses; the limited analgesic effect persisted for about 60 minutes."( Clonidine in horses: identification, detection, and clinical pharmacology.
Dirikolu, L; ElkHoly, H; Ely, KJ; Lehner, AF; McFadden, ET; Thompson, K, 2006
)
2.5
"Clonidine did not suppress the capacity of forskolin to augment glucose-induced insulin release."( Inhibitory effect of clonidine upon adenylate cyclase activity, cyclic AMP production, and insulin release in rat pancreatic islets.
Dufrane, SP; Garcia-Morales, P; Malaisse, WJ; Sener, A; Valverde, I, 1984
)
1.31
"Clonidine did not cause any inotropic change in the euthyroid rat atrium."( Changes in the effects of clonidine on left atrium and hindlimb vasculature of rats in various thyroid states. A study of the responsiveness of alpha 2-adrenoceptors in the cardiovascular system.
Nakashima, M; Oguro, K; Ohguchi, S; Sotobata, I, 1984
)
1.29
"Clonidine did not produce any significant effects on PGE1- augmented cAMP levels in jejunal mucosa in vivo."( Alpha-2 adrenergic inhibition of intestinal secretion induced by prostaglandin E1, vasoactive intestinal peptide and dibutyryl cyclic AMP in rat jejunum.
Kato, R; Nakadate, T; Nakaki, T; Yamamoto, S, 1982
)
0.99
"Clonidine produced an increase in plasma cGMP in supine position, immediately prior to bicycling and after 5 min of exercise."( Plasma cyclic nucleotides and plasma catecholamines before and after prolonged treatment with clonidine in hypertensive patients.
Heding, L; Hökfelt, B; Malmquist, J; Manhem, P, 1981
)
1.2
"Clonidine did not inhibit the pancreatic secretion induced by electrical stimulation of the vagus nerves."( Clonidine inhibition of pancreatic secretion in rats: a possible central site of action.
Appia, F; Chariot, J; Pascaud, X; Rozé, C; Vaille, C, 1981
)
2.43
"Clonidine appears to inhibit the Leu-ENK-induced heart rate increase by both a centrally mediated increase in vagal tone and a peripheral presynaptic alpha 2-agonist effect."( Interactions of leucine-enkephalin with alpha-adrenoceptors in the conscious dog.
Giles, TD; Sander, GE, 1983
)
0.99
"Clonidine induced an increase of more than 10 ng/ml in the plasma hGH levels in 10 (4 males, 6 females) of the 13 obese subjects and in all of the healthy controls, with peak levels ranging from 14.3 to 31.0 ng/ml (m +/- SD 21.0 +/- 5.2 ng/ml); the ITT elicited a similar rise in only 6 of the 13 subjects and 3 of the healthy controls, with peak levels ranging from 9.8 to 20.0 ng/ml (m +/- SD 14.4 +/- 4.5 ng/ml)."( Plasma growth hormone response to oral clonidine as compared to insulin hypoglycemia in obese children and adolescents.
Bauman, B; Gil-Ad, I; Josefsberg, Z; Laron, Z; Topper, E, 1984
)
1.26
"Clonidine did not lower plasma catecholamines in patients with a pheochromocytoma in the presence or in the absence of phenoxybenzamine."( Effect of phenoxybenzamine on cardiovascular and plasma catecholamine responses to clonidine.
Gross, M; Sisson, J; Zweifler, A, 1983
)
1.21
"clonidine to suppress post-extradural shivering in parturients."( IV clonidine for post-extradural shivering in parturients: a preliminary study.
Capogna, G; Celleno, D, 1993
)
1.63
"The clonidine-induced increase in the serum corticosterone level was considerably, but not totally, reduced by icv or ip pretreatment with yohimbine, an alpha 2-adrenergic receptor antagonist."( Central histaminergic mechanisms in the corticosterone response to clonidine.
Borycz, J; Bugajski, AJ; Bugajski, J; Gadek-Michalska, A, 1993
)
1
"Thus clonidine can lower blood pressure by different receptor mechanisms, dependent on the route of administration."( Mediation of the hypotensive action of systemic clonidine in the rat by alpha 2-adrenoceptors.
Hieble, JP; Kolpak, DC, 1993
)
1
"The clonidine group had lower SBP on arrival in the operating room, preinduction, and postintubation."( Clonidine premedication for craniotomy: effects on blood pressure and thiopentone dosage.
Gillies, R; Traill, R, 1993
)
2.21
"Clonidine did not increase postoperative sedation or diminish overall consciousness."( The effect of prophylactic clonidine on postoperative shivering. A large prospective double-blind study.
Herijgers, P; Mattheussen, M; Van Aken, H; Vanacker, B; Vandermeersch, E; Vanderstappen, I, 1996
)
1.31
"The clonidine induced increase in fractional fluid and Na(+)-excretion was inhibited by yohimbine and desmopressin only."( Effects of moxonidine and clonidine on renal function and blood pressure in anesthetized rats.
Greven, J; Hohage, H; Schlatter, E, 1997
)
1.08
"clonidine at lower doses (2 and 5 micrograms) but not higher doses (10 and 20 micrograms) was observed."( Age-related decrease in centrally-mediated pressor response to clonidine in conscious rats.
Araki, H; Futagami, K; Gomita, Y; Kawasaki, H, 1998
)
1.26
"I.v. clonidine did not cause significant changes in pial arteries, but it caused significant constriction of small veins."( The vascular effects of topical and intravenous alpha2-adrenoceptor agonist clonidine on canine pial microcirculation.
Dohi, S; Iida, H; Ishiyama, T, 1998
)
0.98
"Clonidine can increase the duration of spinal anesthetics. "( Unusually prolonged duration of spinal anesthesia following 2% mepivacaine.
Bertini, L; Tagariello, V,
)
1.57
"Clonidine did not cause allergic reaction in patients with proven allergy to apraclonidine, indicating that there is no cross-reactivity with apraclonidine. "( Clonidine provides an allergy-free alternative in glaucoma patients with proven allergy to apraclonidine.
Geyer, O; Lazar, M; Neudorfer, M; Pianka, P; Schmidt, KG, 2000
)
3.19
"Clonidine displayed lower efficacy than S18616, was substantially less potent, and had marked affinity for imidazoline(1) sites and alpha(1)-ARs."( S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine.
Audinot, V; Boutin, JA; Cordi, A; Cussac, D; Dekeyne, A; Duqueyroix, D; Girardon, S; Lacoste, JM; Millan, MJ; Milligan, G; Mullot, J; Newman-Tancredi, A; Nicolas, JP; Renouard-Try, A, 2000
)
1.22
"6. Clonidine and congeners activate endothelial alpha(2D)-adrenoceptors coupled to the L-arginine pathway, suggesting that the antihypertensive action of clonidine involves an endothelial vasorelaxation mediated by NO release, in addition to presynaptic mechanisms."( Clonidine-induced nitric oxide-dependent vasorelaxation mediated by endothelial alpha(2)-adrenoceptor activation.
Adler-Graschinsky, E; Boric, MP; Figueroa, XF; Huidobro-Toro, JP; Mendizábal, VE; Poblete, MI, 2001
)
2.27
"clonidine-induced increase in the mechanical threshold, but did not affect the increase in tail-flick latency induced by i.t."( Intrathecal alpha2 adrenoceptor agonist clonidine inhibits mechanical transmission in mouse spinal cord via activation of muscarinic M1 receptors.
Honda, K; Kamiya, HO; Koga, K; Koguchi, M; Moriyama, T; Takano, Y, 2002
)
1.3
"Clonidine is able to increase the threshold for vocalisation during stimulation and the threshold for vocalisation after withdrawal of stimulus (vocalisation afterdischarge). "( Clonidine antinociceptive activity: effects of drugs influencing central monoaminergic and cholinergic mechanisms in the rat.
Paalzow, G; Paalzow, L, 1976
)
3.14
"Clonidine did not increase contractile force in guinea pig left atria."( H2-histaminergic activity of clonidine in the guinea pig heart.
McNeill, JH; Verma, SC, 1977
)
1.27
"Clonidine inhibited the increase in plasma epinephrine at the end of hemorrhage without altering plasma norepinephrine, vasopressin, renin, or atrial natriuretic factor."( Intrathecal clonidine and the response to hemorrhage.
Eisenach, JC; Limauro, D; Tong, C, 1992
)
1.38
"The clonidine-induced increase in submandibular calcium content could not be attributed to any adrenergic receptor activity since it was not blocked by either alpha- or beta-adrenergic antagonists."( Effects of clonidine on the calcium content and morphology of rat salivary glands.
Redman, RS; Yu, JH, 1992
)
1.15
"Clonidine did not increase GH levels significantly over time compared with placebo."( Hormonal responses to clonidine and urinary MHPG in delusional and nondelusional melancholic patients: a placebo-controlled study.
Hatzimanolis, J; Lykouras, L; Malliaras, D; Markianos, M; Stefanis, C, 1991
)
1.32
"The clonidine-induced increase in water absorption is not mediated by the sympathetic nerves innervating the intestine."( Regulation of rat ileal water absorption by central alpha 2 adrenergic receptors.
Dong, WH; Fogel, R; Kong, TH; Michelson, G; Pfeiffer, M, 1990
)
0.76
"Clonidine did not produce excitation (in automated cages) when combined with the selective D1 agonist SKF38393."( Alpha 1 (but not alpha 2)-adrenoceptor agonists in combination with the dopamine D2 agonist quinpirole produce locomotor stimulation in dopamine-depleted mice.
Edis, LE; Eshel, G; Jackson, DM; Kelder, D; Ross, SB, 1990
)
1
"Clonidine induced an increase in height velocity significantly different from that in control children only."( Effectiveness of growth-promoting therapies. Comparison among growth hormone, clonidine, and levodopa.
Bernasconi, S; Ghizzoni, L; Muto, G; Spaggiari, R; Virdis, R; Volta, C, 1991
)
1.23
"Clonidine did produce potent sedative and hypotensive effects."( 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
)
1.3
"Clonidine displays immobility-reducing effects in the mouse swimming model at doses (0.06-16 mg/kg IP) which decrease spontaneous motility. "( [Mechanism of action of clonidine in the forced-swimming test in mice].
Bourin, M; Colombel, MC; Malinge, M,
)
1.88
"Clonidine may inhibit secretion by this same mechanism, and/or by interfering with some intracellular event in the secretory mechanism."( Inhibition of adrenomedullary catecholamine release by propranolol isomers and clonidine involving mechanisms unrelated to adrenoceptors.
Cantó, T; Ceña, V; García, AG; González-García, C; Orellana, C; Orts, A, 1987
)
1.22
"Clonidine evoked an increase in plasma IR-ANF from 16.6 +/- 5.9 pg/ml to 229.5 +/- 60 pg/ml (mean +/- SEM) after 24 hr water deprivation and from 13.6 +/- 7.4 pg/ml to 104.8 +/- 21 pg/ml (mean +/- SEM) after 48 hr water deprivation."( Clonidine stimulates atrial natriuretic factor (ANF) release in water-deprived rats.
Baranowska, B; Gutkowska, J; Tremblay, J, 1988
)
2.44
"Clonidine was chosen because its effect on distal colon motility is similar to thioproperazine, an antipsychotic drug that, despite many adverse effects, possesses powerful anti-UC properties."( Treatment of ulcerative colitis with clonidine.
Arocha, L; Gómez, F; Insausti, CL; Lechin, AE; Lechin, F; Oramas, O; van der Dijs, B; Villa, S, 1985
)
1.26
"Clonidine did not increase cGMP levels in vascular preparations with intact endothelia, in the presence or absence of LY83583."( Evidence that cGMP is the mediator of endothelium-dependent inhibition of contractile responses of rat arteries to alpha-adrenoceptor stimulation.
Diamond, J; Harris, KH; MacLeod, KM; Ng, DD, 1987
)
0.99
"The clonidine-induced increase in JNa could be completely blocked by the amiloride analogue, ethylisopropyl amiloride (EIPA, 10(-5) M)."( Alpha 2 adrenergic agonists stimulate Na+-H+ antiport activity in the rabbit renal proximal tubule.
Hafezi, A; Howard, MJ; Insel, PA; Moradeshagi, P; Nord, EP; Vaystub, S, 1987
)
0.75
"Clonidine can produce symptomatic sinus bradycardia or atrioventricular (AV) block in some patients. "( Electrophysiologic and hemodynamic effects of chronic oral therapy with the alpha 2-agonists clonidine and tiamenidine in hypertensive volunteers.
Nadeau, JH; Primm, RK; Roden, DM, 1988
)
1.94
"Clonidine produced an increase of cGMP content and a decrease of the endogenous type II inhibitor of protein kinase in rat hypothalamic slices. "( Changed sensitivity of alpha 2-adrenoceptors mediating a decrease in protein kinase inhibitor activity in the brain of vasopressin-hypertensive rats.
Starke, K; Szadowska, A; Szmigielska, H; Szmigielski, A, 1986
)
1.71

Treatment

Clonidine treatment significantly enhanced the total antioxidant status (TAS) (P < 0.001) and reduced the thibarbituric acid reactive substances (TBARS) and protein carbonyl content (PCO) Clonidinetreatment attenuated seizure activity, increased the latency to onset of seizure behaviour and reduced seizure-induced changes in heart rate.

ExcerptReferenceRelevance
"Clonidine treatment was very well tolerated."( Clonidine augmentation in patients with schizophrenia: A double-blind, randomized placebo-controlled trial.
Bakker, PR; Durston, S; Koster, M; Kruiper, C; Oranje, B; Sommer, IEC, 2023
)
3.07
"Clonidine treatment provided significant protection against SEVO-induced apoptosis."( Clonidine Protects Against Neurotoxicity Induced by Sevoflurane Through NF-κB Signaling Inhibition and Proinflammatory Cytokine Release in Rats.
Chen, Y; Guo, L; Sun, J; Xin, N; Yu, M; Yu, Y, 2018
)
2.64
"Clonidine treatment significantly increased fentanyl-vs.-food choice."( Conjugate vaccine produces long-lasting attenuation of fentanyl vs. food choice and blocks expression of opioid withdrawal-induced increases in fentanyl choice in rats.
Banks, ML; Blake, S; Bremer, PT; Faunce, KE; Hwang, CS; Janda, KD; Natori, Y; Townsend, EA; Zhou, B, 2019
)
1.24
"Clonidine treatment significantly enhanced the total antioxidant status (TAS) (P < 0.001) and reduced the thibarbituric acid reactive substances (TBARS) (P < 0.001) and protein carbonyl content (PCO) (P < 0.05)."( Effect of Clonidine (an antihypertensive drug) treatment on oxidative stress markers in the heart of spontaneously hypertensive rats.
Govindasamy, C; Mustapha, Z; Nik Yusoff, NS; Sirajudeen, KN, 2013
)
1.51
"Clonidine treatment attenuated seizure activity, increased the latency to onset of seizure behaviour and reduced seizure-induced changes in heart rate, QTc interval, and T wave amplitude."( Cardiac electrographic and morphological changes following status epilepticus: effect of clonidine.
Andreianova, AA; Goulton, CS; Harrison, JC; Kerr, DS; Read, MI; Sammut, IA, 2014
)
1.35
"Clonidine treatment prevented the further decline in mean arterial pressure, substantially reduced heart rate and renal sympathetic nerve activity and restored pressor responsiveness to both phenylephrine and angiotensin II toward preseptic levels."( Clonidine Restores Pressor Responsiveness to Phenylephrine and Angiotensin II in Ovine Sepsis.
Bellomo, R; Booth, LC; Evans, RG; Kosaka, J; Lankadeva, YR; May, CN; Quintin, L, 2015
)
2.58
"Clonidine treatment affected neither labellar nor tarsal sensitivity to sucrose."( Clonidine effects on protein and carbohydrate electrophysiological responses of labellar and tarsal sensilla in Phormia regina.
Crnjar, R; Liscia, A; Masala, C; Solari, P; Sollai, G, 2008
)
2.51
"Clonidine treatment significantly reduced noradrenaline and adrenaline plasma levels in spontaneously hypertensive rats and Wistar Kyoto rats."( Effect of clonidine on tyrosine hydroxylase activity in the adrenal medulla and brain of spontaneously hypertensive rats.
Afonso, J; Moura, E; Serrão, MP; Vieira-Coelho, MA, 2009
)
1.48
"Clonidine treatment also reduced arterial pressure and increased functional capillary density in the skin and skeletal muscle of WKY."( Microvascular effects of centrally acting antihypertensive drugs in spontaneously hypertensive rats.
Bousquet, P; Lessa, MA; Nascimento, AR; Sabino, B; Tibiriçá, E, 2010
)
1.08
"Clonidine pre-treatment prior to H/S resulted in a significant reduction of LOOHs and O(2)(-·) production in all vital organs (P < 0.05-0.001), while additionally, clonidine reduced H/S-induced endotoxemia in portal (P < 0.05) and systemic circulation as well (P < 0.01)."( Clonidine pre-treatment prevents hemorrhagic shock-induced endotoxemia and oxidative stress in the gut, liver, and lungs of the rat.
Filos, KS; Fligou, F; Georgiou, C; Panteli, ES; Papamichail, C; Papapostolou, I; Spiliopoulou, I; Zervoudakis, G, 2012
)
3.26
"Clonidine pre-treatment prevents endotoxemia and OS in the gut, liver, and lungs of rats subjected to severe H/S. "( Clonidine pre-treatment prevents hemorrhagic shock-induced endotoxemia and oxidative stress in the gut, liver, and lungs of the rat.
Filos, KS; Fligou, F; Georgiou, C; Panteli, ES; Papamichail, C; Papapostolou, I; Spiliopoulou, I; Zervoudakis, G, 2012
)
3.26
"Clonidine treatment per se induced the expression of a single GMP, similar to a last reflexively evoked one, that was completely blocked by pre-treatment with prazosin (1 microg/animal) indicating that it was due to the alpha(1) properties of clonidine."( Yohimbine reverses the exhaustion of the coital reflex in spinal male rats.
Carro-Juáreza, M; Rodríguez-Manzo, G, 2003
)
1.04
"Only clonidine treatment totally prevented the development of insulin resistance, and high-dose aspirin, known to prevent insulin resistance by inhibition of the activity of IkappaB kinase-beta, decreased the degree of insulin resistance by almost 70%."( Hypertension and insulin resistance are not directly related in obese dogs.
Gokee, A; Rocchini, AP; Yang, JQ, 2004
)
0.78
"Clonidine-treated patients experienced a more pronounced decrease in mean arterial pressure as compared to patients treated without clonidine (25 +/- 10% vs 15 +/- 12%, P < 0.05)."( Intrathecal clonidine prolongs labour analgesia but worsens fetal outcome: a pilot study.
Missant, C; Teunkens, A; Van de Velde, M; Vandermeersch, E,
)
1.23
"Clonidine treatment had no evident effects on caspase-3 mRNA level and DNA fragmentation in the cortex of an 8-day-old rat."( Clonidine increases caspase-3 mRNA level and DNA fragmentation in the developing rat brainstem.
Bannova, AV; Dygalo, NN; Kalinina, TS; Shishkina, GT, 2004
)
2.49
"Clonidine pretreatment suppressed the release of both glutamate and aspartate during NCFI in normo- and hyperglycemic rodents when compared with NCFI-treated normo- and hyperglycemic rats without the drug."( The effect of clonidine on cell survival, glutamate, and aspartate release in normo- and hyperglycemic rats after near complete forebrain ischemia.
Jellish, WS; Kindel, G; Murdoch, J; White, FA; Zhang, X, 2005
)
1.41
"Clonidine is used as a treatment for heroin addiction. "( Role of imidazoline receptors in the anti-aversive properties of clonidine during opiate withdrawal in rats.
Caillé, S; Georges, F; Le Moine, C; Stinus, L; Vouillac, C, 2005
)
2.01
"In clonidine-pretreated group, insulin administration could reverse only 37% of the inhibition produced by clonidine and inhibition of SIT was significant compared with vehicle + insulin-treated group, i.e."( An inherent acceleratory effect of insulin on small intestinal transit and its pharmacological characterization in normal mice.
Dkhar, SA; Naveen, AT; Peddyreddy, MK; Ramaswamy, S; Shewade, DG, 2006
)
0.85
"Oral clonidine pretreatment not only helped control patient anxiety and pain but also provided cardiovascular stability."( Oral clonidine pretreatment prior to venous cannulation.
Hall, DL; Rezvan, E; Tatakis, DN; Walters, JD, 2006
)
1.3
"Clonidine pre-treatment increased and prolonged sedation and amnesia and stabilized vital signs while significantly decreasing diazepam and post-operative analgesic usage."( Oral clonidine pre-treatment and diazepam/meperidine sedation.
Hall, DL; Rezvan, E; Tatakis, DN; Walters, JD, 2006
)
1.57
"Clonidine pretreatment significantly alleviated these drug-induced deficits."( The effects of clonidine on discrete-trial delayed spatial alternation in two rat models of memory loss.
Bardgett, ME; Griffith, MS; Lamontagne, T; McDaniel, T; Points, M; Ramsey-Faulkner, C; Roflow, J; Topmiller, J, 2008
)
1.42
"In Clonidine pretreated hypoxic group, the hypoxia-induced increased expression of pro-apoptotic proteins Bad and Bax was prevented in all the three fractions."( Effect of hypoxia on expression of apoptotic proteins in nuclear, mitochondrial and cytosolic fractions of the cerebral cortex of newborn piglets: the role of nuclear Ca++ -influx.
Ashraf, QM; Delivoria-Papadopoulos, M; Mishra, OP, 2008
)
0.86
"A clonidine treatment had been stopped 129 h earlier."( [Withdrawal syndrome during epidural administration of morphine after stopping treatment with clonidine].
Oksenhendler, G; Petit, J; Ropiquet, S; Winckler, C, 1984
)
1.04
"Clonidine pretreatment (0.3 mg/kg) increased the onset latency to tremor from 5 to 20 min, increased the onset latency to death from 12 to 24 min and increased the percentage of survivors to 50%."( Mechanism of the clonidine-induced protection against acetylcholinesterase inhibitor toxicity.
Buccafusco, JJ, 1982
)
1.33
"Clonidine treatment resulted also in a sedative response."( Differential clonidine effects on EEG following lesions of the dorsal and median raphe nuclei in rats.
Bidzinski, A; Dyr, W; Kostowski, W; Zacharski, B, 1983
)
1.36
"Clonidine-treated eyes had a 2 mmHg decrease in intraocular pressure which was statistically significant."( Effect of clonidine on aqueous humor flow in normal human eyes.
Brubaker, RF; Lee, DA; Topper, JE, 1984
)
1.39
"Clonidine treatment of NNAS remains strictly investigational at this time."( Clonidine treatment of neonatal narcotic abstinence syndrome.
Caruso, KA; Cohen, DJ; Ehrenkranz, RA; Hoder, EL; Kleber, HD; Leckman, JF; Poulsen, J, 1984
)
2.43
"Clonidine-treated hypertension was associated with decreased (0.2 +/- 0.1 ng/ml) and renal insufficiency with increased (0.9 +/- 0.7 ng/ml) maternal plasma norepinephrine concentrations (control group, 0.3 +/- 0.1 ng/ml)."( Amniotic fluid norepinephrine concentration as an indicator of fetal sympathetic nervous activity. Effect of pregnancy complications.
Kauppila, A; Puolakka, J; Vuori, J, 1984
)
0.99
"clonidine-treated) groups."( Pharmacological suppression of REM sleep prior to weaning counteracts the effectiveness of subsequent environmental enrichment on cortical growth in rats.
Corner, MA; Mirmiran, M; Uylings, HB, 1983
)
0.99
"Clonidine-treated patients had significantly fewer symptoms than a comparable group of opioid addicts abruptly withdrawn from methadone."( Clonidine suppresses the opioid abstinence syndrome without clonidine-withdrawal symptoms: a blind inpatient study.
Kleber, HD; Redmond, DE; Uhde, TW, 1980
)
2.43
"Clonidine treatment resulted in fewer, shorter, and thinner hyaline casts."( The effect of clonidine on tubular obstruction in postischemic acute renal failure in the rabbit demonstrated by microradiography and microdissection.
Heptinstall, RH; Ideura, T; Solez, K, 1980
)
1.34
"Clonidine treatment resulted in less outer medullary microvascular damage (demonstrated by colloidal carbon staining), higher outer medullary blood flow 1 to 2 hours after unclamping, fewer casts, and higher creatinine clearance and free water clearance/creatinine clearance 4 to 6 hours after unclamping compared with controls."( Clonidine after renal ischemia to lessen acute renal failure and microvascular damage.
Hamilton, B; Ideura, T; Saito, H; Silvia, CB; Solez, K, 1980
)
2.43
"Clonidine pretreatment also caused a more moderate reduction (by 45%) in the number of Fos-positive cells in the nucleus of the solitary tract, but had no effect on Fos expression in the parabrachial nucleus."( Clonidine and rilmenidine suppress hypotension-induced Fos expression in the lower brainstem of the conscious rabbit.
Dampney, RA; Li, YW, 1995
)
2.46
"Clonidine pretreatment (1 mg/kg, i.p.) reduced the number of withdrawal-activated Fos-LIR cells in LC by 81%."( Effects of morphine and morphine withdrawal on adrenergic neurons of the rat rostral ventrolateral medulla.
Baraban, SC; Guyenet, PG; Stornetta, RL, 1995
)
1.01
"Apraclonidine treatment resulted in significantly more patients attaining an additional 20% reduction or more in intraocular pressure from baseline and an intraocular pressure less than or equal to 20 mm Hg (P < .05)."( Short-term efficacy of apraclonidine hydrochloride added to maximum-tolerated medical therapy for glaucoma. Apraclonidine Maximum-Tolerated Medical Therapy Study Group.
Lehmann, RP; Mundorf, T; Ritch, R; Robin, AL; Shin, DH; Smythe, B, 1995
)
1.07
"Clonidine-treated infants (0.05; 0.1; 0.2 mg/kg) also failed to apprehend and attach to the anaesthetized mother's nipple."( Effect of clonidine on the responsiveness of infant rats to maternal stimuli.
Hansen, S, 1993
)
1.41
"Clonidine treatment, at all doses tested, resulted in hyperglycaemia and behavioural effects.(ABSTRACT TRUNCATED AT 250 WORDS)"( Evidence for a primary involvement of somatostatin in clonidine-induced growth hormone release in conscious rats.
Gurd, W; Lanzi, R; Lapointe, M; Tannenbaum, GS, 1994
)
1.26
"Clonidine pretreatment reversed the soman-induced mAChR downregulation in cortex and hindbrain produced by acute soman administration."( Regulation of central muscarinic receptors after cholinesterase inhibition: effect of clonidine.
Buccafusco, JJ; Erwin, L; Li, W; Yang, XH, 1993
)
1.23
"Clonidine treatment resulted in no significant improvement over placebo on any of the cognitive measures employed."( Korsakoff's syndrome, cognition and clonidine.
Ebmeier, KP; Goodwin, GM; Moffoot, A; Murray, C; O'Carroll, RE, 1993
)
1.28
"Clonidine treatment significantly increased the percentage of patients who required pacing after CPB (P < 0.05)."( Clonidine improves perioperative myocardial ischemia, reduces anesthetic requirement, and alters hemodynamic parameters in patients undergoing coronary artery bypass surgery.
Dorman, BH; Gartman, DM; Slachman, FN; Verrier, ED; Zucker, JR, 1993
)
2.45
"Clonidine treatment resulted in improvement in both the ADHD (39/54; 72%) and tic symptoms (18/24; 75%) groups. "( Comparison of clonidine response in the treatment of attention-deficit hyperactivity disorder with and without comorbid tic disorders.
Biederman, J; Gonzalez, A; Spencer, T; Steingard, R; Wilens, T, 1993
)
2.09
"Apraclonidine-treated eyes showed mydriasis and blanching of the conjunctiva."( Apraclonidine protection of the blood-aqueous barrier from traumatic break-down.
Bellucci, R; Bonomi, L; Pagliarusco, A; Stefani, L, 1995
)
1.33
"Apraclonidine treatment resulted in significantly more patients achieving either an additional > or = 20% reduction in IOP from baseline (resulting in an IOP < or = 20 mm Hg) (P < 0.05)."( Topical apraclonidine hydrochloride in eyes with poorly controlled glaucoma. The Apraclonidine Maximum Tolerated Medical Therapy Study Group.
Lehmann, RP; Mundorf, T; Ritch, R; Robin, AL; Shin, D; Smythe, B, 1995
)
1.15
"Clonidine pretreatment modified the local anaesthetic activity of bupivacaine dose-dependently."( Effects of clonidine pretreatment on the local anaesthetic activity of bupivacaine in mice.
Attolini, L; Bruguerolle, B; Gantenbein, M; Grignon, S, 1995
)
1.4
"Clonidine-pretreated mice were tolerant to clonidine, but not cross-tolerant to morphine."( Alteration of spinal protein kinase C expression and kinetics in morphine, but not clonidine, tolerance.
Li, Y; Roerig, SC, 1999
)
1.25
"Clonidine pretreatment similarly and significantly decreased NA levels in all women and, compared to the control test, marginally influenced the ACTH response to CRH + AVP."( alpha2-adrenoceptor regulation of the hypothalamic-pituitary-adrenocortical axis in obesity.
Calzoni, F; Ceroni, L; Cortelli, P; Gambineri, A; Gnudi, U; Menozzi, R; Pasquali, R; Rio, GD; Sinisi, R; Vicennati, V, 2000
)
1.03
"Clonidine pretreatment (0.1 mg/kg, 30 min prior to FG7142) partially reversed the FG7142-induced impairment while guanfacine pretreatment (0.11 mg/kg) completely blocked the FG7142-induced impairment."( Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats.
Arnsten, AF; Birnbaum, SG; Podell, DM, 2000
)
1.03
"Four clonidine-treated patients required urapidil to achieve satisfactory hypotension as compared with 11 controls (P<0.05)."( Clonidine decreases intraoperative bleeding in middle ear microsurgery.
Delgado-Martinez, AD; Gómez-Luque, A; Marchal, JM; Martínez-López, MC; Martos-Crespo, F; Sánchez De La Cuesta, F, 2001
)
2.21
"Clonidine 0.2 mg pretreatment decreased TNF-alpha concentrations both in plasma and CSF."( Clonidine suppresses plasma and cerebrospinal fluid concentrations of TNF-alpha during the perioperative period.
Ignatowski, TA; Knight, PR; Kurek, CJ; Nader, ND; Spengler, RN, 2001
)
2.47
"Clonidine treatment (continuous i.v."( Sympathetic nervous activation following subarachnoid hemorrhage: Influence of intravenous clonidine.
Edén, E; Friberg, P; Lambert, G; Naredi, S; Rydenhag, B, 2002
)
1.26
"The clonidine treatment showed a significant difference from placebo treatment on three subscales of the Ritvo-Freeman Real Life Rating Scale (i.e., social relationship to people, affectual responses, and sensory responses). "( A double-blind, placebo-controlled study of the efficacy of transdermal clonidine in autism.
Fankhauser, MP; German, ML; Karumanchi, SD; Karumanchi, VC; Yates, A, 1992
)
1.07
"Clonidine treatment did not potentiate alfentanil-induced respiratory depression."( Ventilatory effects of clonidine alone and in the presence of alfentanil, in human volunteers.
Duncan, SR; Jarvis, DA; Maze, M; Segal, IS, 1992
)
1.32
"Clonidine-treated rats, lesioned or not, had an acquisition profile indistinguishable from that of sham-operated saline-injected rats, in spite of their increased run time."( Clonidine reverses spatial learning deficits and reinstates theta frequencies in rats with partial fornix section.
Ammassari-Teule, M; Maho, C; Sara, SJ, 1991
)
2.45
"Clonidine treatment also significantly attenuated lactate-panic symptoms, as reflected by time to panic and API comparison between trials."( Noradrenergic function in panic disorder. Effects of intravenous clonidine pretreatment on lactate induced panic.
Campeas, RB; Coplan, JD; Davies, SO; Dillon, DJ; Fyer, AJ; Gorman, JM; Klein, DF; Liebowitz, MR; Martinez, J, 1992
)
1.24
"Clonidine treatment led to a decrease in mean arterial blood pressure (MABP), heart rate (HR), and plasma cortisol and aldosterone concentrations throughout the study, compared with placebo (P less than 0.05)."( Cardiovascular and endocrine effects of clonidine premedication in neurosurgical patients.
Fathi, M; Gaumann, DM; Reverdin, AF; Rivest, RW; Tassonyi, E, 1991
)
1.27
"In clonidine treated eyes, the IOP fell from a mean of 11.9 +/- 3.4 to 9 +/- 3.3 mmHg 2 h postoperatively."( Prevention of the rise in intraocular pressure following neodymium-YAG posterior capsulotomy using topical clonidine.
Geyer, O; Lazar, M; Loewenstein, A; Varssano, D, 1991
)
1.01
"Clonidine pretreatment (200 micrograms/kg, i.p.) eliminated both the withdrawal symptoms and the DA decrease."( Dopamine microdialysis in the nucleus accumbens during acute and chronic morphine, naloxone-precipitated withdrawal and clonidine treatment.
Hoebel, BG; Mark, GP; Pothos, E; Rada, P, 1991
)
1.21
"Clonidine treatment significantly increased the weight gain, but did not affect plasma glucose, insulin, glucagon and norepinephrine in the diabetic animals."( Central adrenergic suppression augments the insulin and glucagon secretory, and the glycogenolytic responses in streptozotocin-diabetic rats.
Colemen, ER; Dunbar, JC; Marzouq, L; Shaffer, LR, 1991
)
1
"Clonidine pretreatment at a dose that did not induce any tolerance slightly enhanced the antagonistic effects of yohimbine and naloxone against morphine."( Interaction between the inhibitory effects of morphine and clonidine on intestinal transit in mice.
Wong, CL, 1991
)
1.25
"Clonidine-treated rats received fentanyl/N2O and 10 micrograms/kg of intravenous clonidine 10 min before ischemia, which was produced by right carotid ligation combined with hemorrhagic hypotension to 35 mm Hg for 30 min."( Clonidine decreases plasma catecholamines and improves outcome from incomplete ischemia in the rat.
Albrecht, RF; Baughman, VL; Cheng, MA; Hoffman, WE; Thomas, C, 1991
)
2.45
"Clonidine-treated patients reported less diarrhea, dizziness, headache and fatigue, and the chlordiazepoxide-treated patients reported less nausea and vomiting."( Transdermal clonidine versus chlordiazepoxide in alcohol withdrawal: a randomized, controlled clinical trial.
Baumgartner, GR; Rowen, RC, 1991
)
1.38
"Clonidine treatment decreased binding in hindbrain while guanabenz treatment decreased binding in both fore- and hindbrain."( Desensitization and down-regulation of brain alpha 2-adrenoceptors by centrally acting antihypertensive drugs.
Hamilton, CA; Howie, CA; Jardine, E; Reid, JL; Yakubu, MA, 1990
)
1
"Clonidine pretreatment did not significantly alter the effect of baclofen alone, but reversed the potentiation of the action of baclofen produced by both theophylline and isobutylmethylxanthine."( Clonidine reverses methylxanthine-induced potentiation of baclofen antinociception.
Sawynok, J; Steardo, L, 1985
)
2.43
"Clonidine reduced pretreatment BP and CSF NE levels by 27% (p less than 0.05) and 39% (p less than 0.01), respectively."( Cerebrospinal fluid norepinephrine levels in essential hypertension: effects of drug treatment and withdrawal.
Cubeddu, LX; Hoffman, IS, 1987
)
0.99
"With clonidine treatment, the antihypertensive effect during exercise was smaller and was observed only at low and moderate workloads."( Comparative effects of transdermal clonidine and oral atenolol on acute exercise performance and response to aerobic conditioning in subjects with hypertension.
Davidman, M; Davies, SF; Graif, JL; Husebye, DG; Iber, C; Maddy, MM; McArthur, CD; O'Connell, MB; Path, MJ, 1989
)
1.01
"Clonidine pretreatment resulted in a significant degree of protection from the lethal effects of soman in the rat."( Protection afforded by clonidine from the acute and chronic behavioral toxicity produced by the cholinesterase inhibitor soman.
Aronstam, RS; Buccafusco, JJ; Graham, JH; VanLingen, J,
)
1.16
"Clonidine treatment produced a dosage related increase in amplitude of both components similar to that produced by chlordimeform (W.K."( An alpha 2-adrenergic mode of action of chlordimeform on rat visual function.
Boyes, WK; Moser, VC, 1988
)
1
"Clonidine treatment evoked a significant dose-dependent increase in urine output."( Is clonidine-induced diuresis mediated by atrial natriuretic factor?
Gutkowska, J; Pan, L, 1988
)
1.62
"Clonidine pretreatment "in vivo" (2 mg/kg), did not counteract the effect of DSP4 (25 mg/kg), suggesting that the enhanced release of NA induced by K+ does not play an important role in the depletion caused by DSP4."( [N-2-chloroethyl-N-ethyl-2-bromobenzylamine (DSP4) increases the liberation of 3H-noradrenaline produced by depolarization of the nerve ending].
Jaim-Etcheverry, G; Landa, ME; Rubio, MC, 1988
)
1
"Clonidine pretreatment blunted the maximal increase in plasma catecholamines by more than 60% of the control response (p less than 0.01), without significantly altering the rise of plasma cortisol or ACTH."( Clonidine and the hormonal responses to graded exercise in healthy subjects.
Baker, SG; Edelstein, D; Haitas, B; Joffe, BI; Lamprey, JM; Panz, V; Seftel, HC, 1986
)
2.44
"Clonidine treatment for 10-14 days in the drinking water did not decrease the cyclic GMP response to clonidine indicating that no tolerance develops to the effect of clonidine on plasma cyclic GMP."( Effects of clonidine and yohimbine on plasma cyclic nucleotide levels in clonidine-naive and clonidine-treated mice.
Ishii, K; Kato, R; Muraki, T, 1986
)
1.38
"Clonidine pretreatment resulted in a significant degree of protection from the lethal effects of soman in the mouse."( Role of central biogenic amines on the protection afforded by clonidine against the toxicity of soman, an irreversible cholinesterase inhibitor.
Aronstam, RS; Buccafusco, JJ; Graham, JH, 1988
)
1.24
"The clonidine-treated group evidenced larger decreases in both systolic and diastolic blood pressures."( Transdermal clonidine in mild hypertension. A randomized, double-blind, placebo-controlled trial.
Daugirdas, JT; Hano, JE; Hockenberry, B; Ing, TS; Neubauer, JA; Popli, S, 1986
)
1.13
"Clonidine treatment was associated with an increase in the levels of NPY-LI in the right atrium in a time- and dose-dependent manner."( Differential effects of clonidine and reserpine treatment on neuropeptide Y content in some sympathetically innervated tissues of the guinea-pig.
Franco-Cereceda, A; Lundberg, JM; Nagata, M; Svensson, TH, 1987
)
1.3
"In clonidine-treated castrated male rats, however, l-adrenaline administration induced a decrease in blood pressure."( [Sexual dimorphism in the pressor response to l-adrenaline in rats].
Fujii, T; Tomori, M, 1986
)
0.78
"Clonidine-naltrexone treatment should succeed with patients receiving methadone doses up to 50 mg/day, facilitate naltrexone maintenance, and apply to many clinical settings."( The combined use of clonidine and naltrexone as a rapid, safe, and effective treatment of abrupt withdrawal from methadone.
Charney, DS; Heninger, GR; Kleber, HD, 1986
)
1.32
"Clonidine treatment was carried out for 10 days by dissolving the drug into drinking water at a concentration of 10 micrograms/ml."( Increase in insulin response to glucose in the rat chronically treated with clonidine.
Ishii, K; Kato, R; Yamamoto, S, 1985
)
1.22
"Clonidine-treated animals showed significant weight loss and decrease in temperature, and those treated with high doses showed marked hypothermia and hind-limb flaccidity."( Intrathecal clonidine: analgesia and effect on opiate withdrawal in the rat.
Cervenko, FW; Jhamandas, K; Milne, B; Sutak, M, 1985
)
1.37
"In clonidine-treated mice which were warmed to reverse drug-induced hypothermia, plasma and liver BSP levels were raised as compared to saline-treated mice."( Clonidine effects on sulfobromophthalein disposition in mice.
Ben-Zvi, Z; Hurwitz, A, 1985
)
2.23
"Pretreatment with clonidine (0.1 and 0.5 mg/kg) significantly reversed the anticonvulsant effect of ACEA (2 mg/kg)."( The role of α₂-adrenoceptors in the anti-convulsant effects of cannabinoids on pentylenetetrazole-induced seizure threshold in mice.
Bahremand, A; Dehpour, AR; Moezi, L; Shafaroodi, H, 2013
)
0.71
"Treatment with clonidine significantly reduced mean arterial blood pressure in spontaneously hypertensive rats to values similar to normotensive Wistar Kyoto rats."( Effect of clonidine on tyrosine hydroxylase activity in the adrenal medulla and brain of spontaneously hypertensive rats.
Afonso, J; Moura, E; Serrão, MP; Vieira-Coelho, MA, 2009
)
1.1
"Treatment with clonidine, but not levetiracetam, resulted in a small reduction in Total Tic Score, with an effect size of 0.57."( Double-blind, crossover study of clonidine and levetiracetam in Tourette syndrome.
Hedderick, EF; Morris, CM; Singer, HS, 2009
)
0.97
"Pretreatment with clonidine or yohimbine failed to affect basal plasma corticosterone and ACTH concentrations, but abolished diazepam-induced inhibition of the HPA axis activity."( The involvement of noradrenergic mechanisms in the suppressive effects of diazepam on the hypothalamic-pituitary-adrenal axis activity in female rats.
Muck-Šeler, D; Pivac, N; Švob Štrac, D, 2012
)
0.7
"Pretreatment with clonidine (0.001-0.1 mg/kg) inhibited the anticonvulsant effect of morphine, while potentiating its proconvulsant effect."( The role of alpha2-adrenoceptors in the modulatory effects of morphine on seizure susceptibility in mice.
Dehpour, AR; Homayoun, H; Khavandgar, S, 2002
)
0.64
"Pre-treatment with clonidine (10 microg/animal) completely prevented the yohimbine-induced GMP, implying that its effect was exerted upon alpha(2)-adrenoceptors."( Yohimbine reverses the exhaustion of the coital reflex in spinal male rats.
Carro-Juáreza, M; Rodríguez-Manzo, G, 2003
)
0.64
"Pretreatment with clonidine inhibited synaptic transmission and abolished PTD while yohimbine did not affect it."( Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia.
Love, JA; Yi, E, 2005
)
0.65
"Treatment for clonidine-induced delirium involves cessation of the medication and patient observation."( Clonidine-induced delirium.
Delaney, J; Doddamani, S; Ostfeld, R; Spevack, D, 2006
)
2.12
"Pretreatment with clonidine (50 micrograms/kg, IP) significantly decreased the incidence of 11 out of 16 withdrawal signs."( Clonidine suppresses methylxanthine induced quasi-morphine withdrawal syndrome.
Grant, SJ; Redmond, DE, 1982
)
2.03
"Pretreatment with clonidine hydrochloride and propranolol hydrochloride, both of which have been reported to have anxiolytic actions in man, attenuated only selective aspects of the response to beta-CCE."( A benzodiazepine receptor-mediated model of anxiety. Studies in nonhuman primates and clinical implications.
Aloi, J; Insel, TR; Jimerson, DC; Ninan, PT; Paul, SM; Skolnick, P, 1984
)
0.59
"Pretreatment with clonidine increased the blood-brain barrier dysfunction in rats given 6-OHDA but not in those given baclofen, probably because the slower rise in pressure facilitates myogenic autoregulation."( Neurogenic modification of the vulnerability of the blood-brain barrier during acute hypertension in conscious rats.
Auer, LM; Johansson, BB, 1983
)
0.59
"In treating PLH, clonidine may serve as an alternative approach to local or surgical treatment."( Clonidine treatment in paroxysmal localized hyperhidrosis.
Bechar, M; Goldhammer, G; Hering, R; Kuritzky, A, 1984
)
2.04
"Pretreatment with clonidine prevented this action of the prostaglandins, but if the animals were first given prostaglandin and allowed to go out of estrus, then clonidine did not restore lordosis."( Prostaglandins, clonidine and sexual receptivity in the guinea pig.
Davis, GA; Goy, RW; Haning, RV; Irving, SM, 1981
)
0.93
"Pretreatment with clonidine, 0.1 mg/kg abolished the increase in MHPG in the striatum and significantly inhibited the rise in HVA."( Evidence that noradrenaline modulates the increase in striatal dopamine metabolism induced by muscarinic receptor stimulation.
Crowley, WR; Jacobowitz, DM; Kopin, IJ; Muth, EA; O'Donohue, TL; Weinstock, M; Zavadil, AP, 1980
)
0.58
"Treatment with clonidine (1 mg/kg, b.i.d., 14 days), hydralazine (10 mg/kg, b.i.d., 14 days) or diuretics (chlorothiazide 100 mg/kg + spironolactone 10 mg/kg, q.d., 21 days) decreased blood pressure of SHRs but did not normalize their body temperatures and heat sensitivity."( Thermoregulation in spontaneously hypertensive rats: effects of antihypertensive treatments.
O'Donnell, A; Volicer, L, 1981
)
0.6
"Treatment with clonidine, as antihypertensive drug that blunts the kidney's response to vasopressin, resulted in significantly higher creatinine clearance and urine flow rate in the first 6 hours after unclamping."( The effect of clonidine on tubular obstruction in postischemic acute renal failure in the rabbit demonstrated by microradiography and microdissection.
Heptinstall, RH; Ideura, T; Solez, K, 1980
)
0.96
"Pretreatment with clonidine (0.01, 0.03, 0.06, and 0.1 mg/kg) led to a dose-dependent decrease in the heart rate response but blood pressure was reduced similarly for all doses."( Blood pressure via telemetry during social confrontations in rats: effects of clonidine.
Meehan, WP; Miczek, KA; Tornatzky, W, 1995
)
0.84
"Treatment with clonidine led to a decrease in both frequency and intensity of the flushing reactions."( Parmesan cheese and vegetable-induced histaminuria in a thermal flusher.
Spencer, DM; Wilkin, JK, 1994
)
0.63
"Pretreatment with clonidine 1 microgram kg-1 i.v."( Comparison of clonidine with fentanyl on phrenic nerve activity and their interaction in anaesthetized rabbits.
Chakrabarti, MK; Knowles, MG; Wang, C; Whitman, JG, 1994
)
0.97
"Pretreatment with clonidine changed neither cumulative convulsant doses (Group 1: 41.8 +/- 2.2, Group 2: 43.8 +/- 2.6, Group 3: 42.3 +/- 2.0 mg.kg-1, respectively) nor plasma concentrations of lidocaine at the onset of convulsions (Group 1: 10.5 +/- 0.3, Group 2: 10.8 +/- 0.3, Group 3: 10.6 +/- 0.3 micrograms.ml-1, respectively)."( Clonidine does not affect lidocaine seizure threshold in rats.
Goto, H; Hirakawa, M; Yokoyama, M, 1993
)
2.05
"Pretreatment with clonidine (100 micrograms/kg, i.p.), which activates alpha 1 receptors under the current experimental conditions, did not enhance the FR in control animals."( 6-Hydroxydopamine treatment of neonatal rats. II. Effects on the development of the hindlimb flexor reflex.
Jones, DJ; Simmons, KE, 1993
)
0.61
"Treatment with clonidine markedly suppressed norepinephrine levels during exercise (matched peak exercise workload: control, 2137 +/- 187 versus clonidine, 1430 +/- 161 pg/mL), increased leg blood flow (control, 1.8 +/- 0.2 versus clonidine, 2.3 +/- 0.4 L/min), reduced systemic oxygen consumption (control, 1002 +/- 70 versus clonidine, 966 +/- 68 mL/min), reduced pulmonary artery lactate concentration (control, 3.2 +/- 0.3 versus clonidine, 2.6 +/- 0.2 mEq/L), and decreased minute ventilation (control, 39.7 +/- 2.1 versus clonidine, 34.9 +/- 2.4 L/min) (all P < .05)."( Effect of sympathoinhibition on exercise performance in patients with heart failure.
Chomsky, DB; Lang, CC; Rayos, GH; Wilson, JR; Wood, AJ, 1997
)
0.64
"Pretreatment with clonidine failed to increase mobility when administered in combination with the 5-HT1B receptor agonist, RU 24969 (1 mg/kg, i.p.) or the 5-HT2A receptor antagonist, ketanserin (8 mg/kg, i.p.)."( Clonidine potentiates the effects of 5-HT1A, 5-HT1B and 5-HT2A/2C antagonists and 8-OH-DPAT in the mouse forced swimming test.
Bourin, M; Redrobe, JP, 1998
)
2.07
"Pretreatment with clonidine, prazosin or ondansetron did not modify the raised ICP-induced inhibition of gastric emptying."( Acute intracranial hypertension-induced inhibition of gastric emptying: evaluation in conscious rats.
Gupta, YK; Kacker, V; Mehta, VS, 1999
)
0.63
"Pre-treatment with clonidine did not affect carbachol-evoked secretion but did reduce catecholamine secretion during electrical stimulation."( Adrenergic regulation of catecholamine secretion from trout (Oncorhynchus mykiss) chromaffin cells.
Montpetit, CJ; Perry, SF, 2002
)
0.63
"Pretreatment with clonidine (20 microgram/kg/day, orally) for 28 days reduced peripherally evoked salivation by 45%."( The effect of clonidine on centrally and peripherally evoked submaxillary salivation.
Green, GJ; Wilson, H; Yates, MS, 1979
)
0.94
"Pre-treatment with clonidine (5-10 micrograms/kg i.v.) or oxymetazoline (5.6-11.2 micrograms/kg i.v.), a peripherally active alpha 2-agonist, inhibited the irregular spiking induced by castor oil and no diarrhoea occurred during the experimental period of 6 h."( Suppression of castor oil-induced diarrhoea by alpha 2-adrenoceptor agonists.
Hellström, PM; Svensson, TH; Thollander, M, 1991
)
0.6
"Pretreatment with clonidine (4 x 0.25 mg kg-1) caused a shift of the clonidine antisecretory dose-response curve to the right, demonstrating tolerance."( Studies to determine whether there is tolerance or cross-tolerance to the antisecretory effect of morphine and clonidine in the rat intestine.
Bentley, GA; Coupar, IM; Margaritis, J, 1991
)
0.82
"Treatment with clonidine reduced both circadian variability of BP and HR and the awakening increase."( Modification of circadian blood pressure and heart rate variability by five different antihypertensive agents in spontaneously hypertensive rats.
Janssen, BJ; Struyker-Boudier, HA; Tyssen, CM, 1991
)
0.62
"Pretreatment with clonidine (200 micrograms/kg, i.p.) reduced these withdrawal symptoms and eliminated the ACh response."( Microdialysis evidence that acetylcholine in the nucleus accumbens is involved in morphine withdrawal and its treatment with clonidine.
Hoebel, BG; Mark, GP; Pothos, E; Rada, P, 1991
)
0.81
"Pretreatment with clonidine clearly changed the pattern of GH release during GRF infusion: the amount of GH secreted was significantly higher, the number of GH peaks significantly increased, and almost all the GH was secreted within them."( Clonidine pretreatment modifies the growth hormone secretory pattern induced by short-term continuous GRF infusion in normal man.
Arce, V; Devesa, J; Diaz, MJ; Lima, L; Tresguerres, JA, 1991
)
2.05
"Pretreatment with clonidine did not augment the peak serum GH response to GHRH but the direction of response was more predictable than when GHRH was administered separately or repeatedly."( The interaction between clonidine and growth hormone releasing hormone in the stimulation of growth hormone secretion in man.
Brain, CE; Brook, CG; Hindmarsh, PC; Pringle, PJ; Suri, D, 1990
)
0.91
"Treatment with clonidine significantly slowed the rate of recovery (Kruskal-Wallis H = 8.755, df = 3; 0.02 less than P less than 0.05)."( Clonidine impairs recovery of beam-walking after a sensorimotor cortex lesion in the rat.
Davis, JN; Goldstein, LB, 1990
)
2.06
"Pretreatment with clonidine had only a slight effect on long-term blockade, but yohimbine was without effect."( Substance P-induced long-term blockade of spinal adrenergic analgesia: reversal by morphine and naloxone.
Nance, PW; Sawynok, J, 1987
)
0.6
"Pretreatment with clonidine (0.05 mg/kg, iv) significantly attenuated the increases to 76 +/- 16% (Ri), and 114 +/- 22% (Re) (p less than 0.05)."( The effects of alpha 2-adrenergic agonism with clonidine on the pulmonary and collateral resistances in the canine lung challenged with histamine.
Chen, HI; Kao, SJ; Shen, CY; Wang, D, 1989
)
0.86
"Treatment with clonidine markedly attenuated the inhibitory effect induced by (-)adrenaline on platelet adenylate cyclase activity."( Alpha 2-adrenoceptor-mediated inhibition of platelet adenylate cyclase activity in heroin addicts in abstinence.
García-Sevilla, JA; Gutierrez, M; Ugedo, L; Ulibarri, I, 1987
)
0.61
"Treatment with clonidine led to significant decreases in receptor densities as well as in functional responses."( Platelet alpha 2-adrenoceptors in heroin addicts during withdrawal and after treatment with clonidine.
Garcia-Sevilla, JA; Gutierrez, M; Ugedo, L; Ulibarri, I, 1985
)
0.83
"Treatment with clonidine resulted in a significant improvement in spatial delayed alteration for experimental as compared to control animals."( Learning impairments after 6-OHDA treatment: a comparison with the effects of thiamine deficiency.
Anderson, CD; Langlais, PJ; Mair, RG; McEntee, WJ, 1986
)
0.61
"Pretreatment with clonidine resulted in a dose-related inhibition of soman-induced cardiovascular changes and enhanced the time of survival as well as the number of animals surviving 24 hr after soman injection."( Protection by clonidine from the cardiovascular changes and lethality following soman administration in the rat: role of brain acetylcholine.
Aronstam, RS; Buccafusco, JJ; Magrí, V, 1988
)
0.96
"Treatment with clonidine (100 micrograms/kg s.c."( Changes in locomotor-activity patterns as a measure of spontaneous morphine withdrawal: no effect of clonidine.
de Groot, G; van der Laan, JW, 1988
)
0.83
"Treatment with clonidine for 14 days normalized low beta-endorphin, high plasma noradrenaline and high blood pressure in essential hypertensives at rest, but had no effect in controls."( Reduced beta-endorphin secretion in young patients with mild essential hypertension at rest and during exercise.
Behrendt, M; Kolloch, R; Kraft, KS; Stumpe, KO, 1988
)
0.61
"A pretreatment of clonidine (1 mg/kg) substantially potentiated the antinociceptive efficacy of the two latter doses, but failed to further augment the pain-suppressive action of guanabenz at 5 mg/kg."( Interactions between guanabenz and clonidine in their antinociceptive effects in the rat.
Chan, JY; Chan, SH, 1987
)
0.87
"Treatment with clonidine reduced the area of wheal-and-flare reaction induced by allergen without significantly changing the blood pressure or the plasma cortisol level."( Inhibitory effects of clonidine on the allergen-induced wheal-and-flare reactions in patients with extrinsic asthma.
Andersson, RG; Brundin, A; Lindgren, BR, 1987
)
0.93
"Rats treated with clonidine (300 micrograms/Kg, i.p.) or yohimbine (10 mg/Kg, i.p.) showed brain concentrations of total MHPG of 68 +/- 22 ng/g and 299 +/- 85 ng/g, respectively."( Quantitation of total MHPG in the rat brain using a non enzymatic hydrolysis procedure. Effects of drugs.
Adell, A; Artigas, F; Gelpí, E; Sarrias, MJ, 1986
)
0.59
"Pretreatment with clonidine protected against several toxic manifestations of soman, but had little effect on echothiophate toxicity."( Clonidine protection from soman and echothiophate toxicity in mice.
Aronstam, RS; Buccafusco, JJ; Smith, MD, 1986
)
2.04

Toxicity

No adverse maternal or fetal effects were noted with serum clonidine concentrations less than 1. Lofexidine significantly reduced opiate withdrawal symptoms without the adverse sedative and hypotensive effects that limit the safety and usefulness ofClonidine.

ExcerptReferenceRelevance
" However, pharmacological agents that enhance central cholinergic and noradrenergic neurotransmission, like physostigmine and clonidine, might have serious adverse effects."( Combined administration of physostigmine and clonidine to patients with dementia of the Alzheimer type: a pilot safety study.
Bierer, LM; Davidson, M; Davis, KL; Kaminsky, R; Ryan, TM, 1989
)
0.74
" While clonidine pretreatment resulted in a similar degree of protection as atropine pretreatment against the acute phase of soman toxicity, only clonidine was effective in preventing the expression of chronic behavioral toxic manifestations to soman."( Protection afforded by clonidine from the acute and chronic behavioral toxicity produced by the cholinesterase inhibitor soman.
Aronstam, RS; Buccafusco, JJ; Graham, JH; VanLingen, J,
)
0.9
" No serious drug-related adverse events or abnormal biochemistry or haematology were observed in either group."( A multicentre placebo-controlled study in general practice to evaluate the efficacy and safety of tizanidine in acute low-back pain.
Berry, H; Hutchinson, DR,
)
0.13
" Experiments were designed to determine whether central catecholaminergic systems are implicated in the toxic and lethal manifestations of soman toxicity and whether the protection afforded by clonidine involves such pathways."( Role of central biogenic amines on the protection afforded by clonidine against the toxicity of soman, an irreversible cholinesterase inhibitor.
Aronstam, RS; Buccafusco, JJ; Graham, JH, 1988
)
0.71
" A single, mild side effect was associated with as much additional pain relief as multiple, severe side effects."( Association of pain relief with drug side effects in postherpetic neuralgia: a single-dose study of clonidine, codeine, ibuprofen, and placebo.
Culnane, M; Dubner, R; Gracely, RH; Max, MB; Schafer, SC, 1988
)
0.49
" Terminations because of adverse effects were relatively low."( Comparison of guanfacine versus clonidine for efficacy, safety and occurrence of withdrawal syndrome in step-2 treatment of mild to moderate essential hypertension.
Bedsole, G; Fillingim, J; Hall, D; Haring, O; Jagger, P; Lewin, A; McMahon, FG; Roginsky, M; Stepansky, W; Wilson, MF, 1986
)
0.55
"Mice pretreated with the centrally active alpha-2 adrenergic agonist, clonidine, were protected from several of the toxic manifestations of soman, an organophosphate acetylcholinesterase inhibitor."( Clonidine protection from the toxicity of soman, an organophosphate acetylcholinesterase inhibitor, in the mouse.
Aronstam, RS; Buccafusco, JJ, 1986
)
1.95
" Pretreatment with clonidine protected against several toxic manifestations of soman, but had little effect on echothiophate toxicity."( Clonidine protection from soman and echothiophate toxicity in mice.
Aronstam, RS; Buccafusco, JJ; Smith, MD, 1986
)
2.04
" Clonidine hydrochloride, like methyldopa, appears to be a safe antihypertensive agent in pregnancy."( Clonidine hydrochloride--a safe and effective antihypertensive agent in pregnancy.
Child, A; Henderson-Smart, DJ; Horvath, JS; Korda, A; Phippard, A; Tiller, DJ, 1985
)
2.62
" A discussion on the pharmacological basis of the side effects of the centrally acting antihypertensives has been limited to those adverse reactions that are somehow related to alpha-adrenergic receptors."( The hypotensive activity and side effects of methyldopa, clonidine, and guanfacine.
Thoolen, MJ; Timmermans, PB; van Zwieten, PA,
)
0.38
" Other reported effects are toxic confusional states and psychotic reactions."( Psychiatric side effects of antihypertensive drugs other than reserpine.
Fleminger, R; Paykel, ES; Watson, JP, 1982
)
0.26
" Lofexidine significantly reduced opiate withdrawal symptoms without the adverse sedative and hypotensive effects that limit the safety and usefulness of clonidine."( Opiate withdrawal using lofexidine, a clonidine analogue with fewer side effects.
Geyer, G; Resnick, RB; Washton, AM, 1983
)
0.73
" Clonidine caused adverse effects more frequently than did lofexidine."( Comparative efficacy and safety of lofexidine and clonidine in mild to moderately severe systemic hypertension.
Lopez, LM; Mehta, JL, 1984
)
1.43
" The results obtained from these experiments showed that there was no adverse effect and the diuretic and saluretic effects of hydrochlorothiazide were not impaired."( Animal experiments on the safety pharmacology of lofexidine.
Graf, E; Sieck, A; Wenzl, H; Winkelmann, J, 1982
)
0.26
" The oral LD50 values for these species were similar."( Acute, subacute and chronic toxicity/Carcinogenicity of lofexidine.
Beitman, RE; Fontaine, R; Friehe, H; Gibson, JP; Larson, EJ; Tsai, TH, 1982
)
0.26
" Observed on four drug-induced behavior categories, it was found that both clonidine and propranolol attenuated the toxic effects of relatively low dose levels of digitoxin, while at higher digitoxin dose levels only propranolol was able to reduce significantly the ED50 and the LD50."( Effect of age, clonidine or propranolol on behavioral toxicity induced with digitoxin in mice.
Felleman, VH; Palfai, T, 1982
)
0.85
" In all patients studied, clonidine was a safe and effective nonopiate treatment of opiate withdrawal that suppressed the affect, signs, and symptoms of opiate withdrawal."( Opiate withdrawal using clonidine. A safe, effective, and rapid nonopiate treatment.
Gold, MS; Kleber, HD; Pottash, AC; Sweeney, DR, 1980
)
0.87
" The most common adverse events during tizanidine treatment were somnolence, xerostomia, and fatigue."( Efficacy and safety of tizanidine in the treatment of spasticity in patients with spinal cord injury. North American Tizanidine Study Group.
Bugaresti, J; Martinez-Arizala, A; Nance, PW; Shellenberger, K; Sheremata, W, 1994
)
0.29
" The current study, using a rodent animal model, evaluated the influence of clonidine pretreatment on the systemic toxic effects of bupivacaine overdose induced by a constant intravenous infusion."( Clonidine pretreatment reduces the systemic toxicity of intravenous bupivacaine in rats.
De Kock, M; Henin, D; Le Polain, B; Scholtes, JL; Vandewalle, F, 1993
)
1.96
" The time of occurrence of the bupivacaine-induced toxic events was recorded and the doses were calculated."( Clonidine pretreatment reduces the systemic toxicity of intravenous bupivacaine in rats.
De Kock, M; Henin, D; Le Polain, B; Scholtes, JL; Vandewalle, F, 1993
)
1.73
"In this model, clonidine given prophylactically delays the toxic manifestations of bupivacaine overdose and does not accentuate the subsequent hypotension."( Clonidine pretreatment reduces the systemic toxicity of intravenous bupivacaine in rats.
De Kock, M; Henin, D; Le Polain, B; Scholtes, JL; Vandewalle, F, 1993
)
2.08
" Apraclonidine is well tolerated systemically with no serious adverse event attributed previously to this medicine."( [Effect and side effects of apraclonidine].
Stewart, WC, 1996
)
1.09
" In dealing with drug toxic states in which the differential diagnosis includes drugs available as transdermal delivery systems, the evaluation should include questions regarding possible dermal exposure and a thorough skin examination."( "Cloniderm" toxicity: another manifestation of clonidine overdose.
Killian, CA; Krenzelok, EP; Roberge, RJ; Stonage, CL, 1997
)
0.55
"Concern based on the reported short-term adverse effects of antihypertensive agents on plasma lipid and lipoprotein profiles (PLPPs) has complicated the therapy for hypertension."( Diuretics and beta-blockers do not have adverse effects at 1 year on plasma lipid and lipoprotein profiles in men with hypertension. Department of Veterans Affairs Cooperative Study Group on Antihypertensive Agents.
Cushman, WC; Freis, ED; Lakshman, MR; Materson, BJ; Reda, DJ, 1999
)
0.3
" Patients achieving positive DBP control using hydrochlorothiazide (responders) showed no adverse changes in PLPPs, whereas nonresponders exhibited increases in triglycerides, total cholesterol, and low-density lipoprotein cholesterol levels."( Diuretics and beta-blockers do not have adverse effects at 1 year on plasma lipid and lipoprotein profiles in men with hypertension. Department of Veterans Affairs Cooperative Study Group on Antihypertensive Agents.
Cushman, WC; Freis, ED; Lakshman, MR; Materson, BJ; Reda, DJ, 1999
)
0.3
"None of these 6 antihypertensive drugs has any long-term adverse effects on PLPPs and, therefore, may be safely prescribed."( Diuretics and beta-blockers do not have adverse effects at 1 year on plasma lipid and lipoprotein profiles in men with hypertension. Department of Veterans Affairs Cooperative Study Group on Antihypertensive Agents.
Cushman, WC; Freis, ED; Lakshman, MR; Materson, BJ; Reda, DJ, 1999
)
0.3
" Young children are very sensitive to the toxic effects of clonidine."( Clonidine toxicity in an adolescent patient.
Cox, R; Gitter, MF, 2000
)
1.99
" No serious adverse events were considered to be drug related."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.31
"Overall, the data suggest that tizanidine is safe and efficacious in the treatment of stroke-related spasticity, preserving muscle strength while reducing muscle tone and painful spasms in affected patients."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.31
"To analyze the trends, demographics, and toxic effects associated with pediatric clonidine hydrochloride exposures reported to poison centers."( Trends and toxic effects from pediatric clonidine exposures.
Klein-Schwartz, W, 2002
)
0.81
"While most of the clonidine exposures resulted in minimal toxic effects, serious toxic effects and death can occur."( Trends and toxic effects from pediatric clonidine exposures.
Klein-Schwartz, W, 2002
)
0.92
"25% drops in twice daily dosage and does not result in any significant ocular and systemic adverse effects."( A prospective, long-term, randomized study of the efficacy and safety of the drug combination pilocarpine 1% with clonidine 0.06% or clonidine 0.125% versus timolol 0.25%.
Agarwal, H; Rajashekhar, YL; Sihota, R; Venkatesh, P, 2002
)
0.53
" A recent group of placebo-controlled, double-blinded clinical trials have consistently shown that certain stimulants, particularly methylphenidate and dextroamphetamine, are effective, well tolerated, and safe when administered to treat ADHD in children with tics."( Tourette's syndrome: are stimulants safe?
Kurlan, R, 2003
)
0.32
" This review focuses on the tolerability, occurrence of adverse events, precautions required to prevent severe adverse events, and essential pharmacological interaction in the treatment of ADHD symptoms by non-stimulants."( The safety of non-stimulant agents for the treatment of attention-deficit hyperactivity disorder.
Banaschewski, T; Heise, CA; Himpel, S; Rothenberger, A, 2005
)
0.33
"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
"(3,4) We report adverse effects of topical apraclonidine when used in the diagnosis of Horner syndrome in infants."( Adverse effects of apraclonidine used in the diagnosis of Horner syndrome in infants.
Lim, MK; Satterfield, D; Watts, P, 2007
)
0.91
"In adolescents, clonidine 1 microg/kg prolonged the duration of sensory block achieved with bupivacaine by 30 min and postoperative analgesia by 120 min without severe adverse events."( Clonidine 1 microg/kg is a safe and effective adjuvant to plain bupivacaine in spinal anesthesia in adolescents.
Abdelaziz, AB; Chattaoui, O; Kaabachi, O; Kokki, H; Ouezini, R; Zarghouni, A, 2007
)
2.13
" Groups were compared regarding adverse events and changes from baseline to week 16 in electrocardiograms and vital signs."( Clonidine for attention-deficit/hyperactivity disorder: II. ECG changes and adverse events analysis.
Bukstein, OG; Daviss, WB; Harris, P; McDERMOTT, MP; Palumbo, D; Patel, NC; Pelham, WE; Robb, AS; Sallee, FR, 2008
)
1.79
" Moderate or severe adverse events were more common in subjects on clonidine (79."( Clonidine for attention-deficit/hyperactivity disorder: II. ECG changes and adverse events analysis.
Bukstein, OG; Daviss, WB; Harris, P; McDERMOTT, MP; Palumbo, D; Patel, NC; Pelham, WE; Robb, AS; Sallee, FR, 2008
)
2.02
"Clonidine, used alone or with methylphenidate, appears safe and well tolerated in childhood ADHD."( Clonidine for attention-deficit/hyperactivity disorder: II. ECG changes and adverse events analysis.
Bukstein, OG; Daviss, WB; Harris, P; McDERMOTT, MP; Palumbo, D; Patel, NC; Pelham, WE; Robb, AS; Sallee, FR, 2008
)
3.23
" The most common adverse events and pharmacodynamic effects are related to plasma concentrations."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.35
" At the 1st and 2nd dosing level there were no reported adverse drug reactions."( A phase II clinical trial to assess the safety of clonidine in acute organophosphorus pesticide poisoning.
Abeysinghe, C; Buckley, NA; Dawson, AH; Hettiarachchi, R; Jayamanna, SF; Karunatilake, H; Perera, PM, 2009
)
0.61
" We compared spontaneous adverse event reports in the Acorda Therapeutics worldwide clinical adverse event database for children (< or = 16 years; n = 99) and adults (>16 years; n = 1153) who had received tizanidine and for whom at least one adverse event was reported, and performed a retrospective chart review of the safety of tizanidine in children (< or = 16 years; n = 76) at a large US pediatric neurology practice."( Pediatric safety of tizanidine: clinical adverse event database and retrospective chart assessment.
Chez, M; Henney, HR, 2009
)
0.35
"The overall safety of tizanidine in the pediatric group appeared good; however, the adverse event profile differed from that in adults."( Pediatric safety of tizanidine: clinical adverse event database and retrospective chart assessment.
Chez, M; Henney, HR, 2009
)
0.35
"There is considerable evidence that caudally administered clonidine in addition to local anesthetics provides extended duration of analgesia with a decreased incidence for analgesic rescue requirement and little adverse effects compared to caudal local anesthetics alone."( Efficacy and safety of clonidine as additive for caudal regional anesthesia: a quantitative systematic review of randomized controlled trials.
Poepping, DM; Pogatzki-Zahn, EM; Schnabel, A; Zahn, PK, 2011
)
0.92
" It is necessary to seek strategies that avoid the possible adverse effects after anaesthesia."( Clonidine abolishes the adverse effects on apoptosis and behaviour after neonatal ketamine exposure in mice.
Eriksson, P; Fredriksson, A; Gordh, T; Pontén, E; Viberg, H, 2012
)
1.82
"The administration of clonidine eliminated the adverse effects of ketamine in this mouse model, suggesting a possible strategy for protection."( Clonidine abolishes the adverse effects on apoptosis and behaviour after neonatal ketamine exposure in mice.
Eriksson, P; Fredriksson, A; Gordh, T; Pontén, E; Viberg, H, 2012
)
2.14
"Caudal block is a safe procedure commonly used for pediatric perioperative analgesia."( [Pediatric caudal anesthesia : importance and aspects of safety concerns].
Mauch, J; Weiss, M, 2012
)
0.38
" In this patient, this rare side effect decisively impaired life quality, subjectively outweighing the considerable pain relief which could be achieved after formerly inefficacious treatment."( Erectile dysfunction as rare side effect in the simultaneous intrathecal application of morphine and clonidine.
Alfieri, A; Koman, G; Rachingter, J; Scheller, C; Strauss, C,
)
0.35
"Caudal block is a safe procedure commonly used for pediatric perioperative analgesia."( [Pediatric caudal anesthesia: importance and aspects of safety concerns].
Mauch, J; Weiss, M, 2012
)
0.38
" While medications for ADHD are generally well-tolerated, there are common, although less severe, as well as rare but severe adverse events AEs during treatment with ADHD drugs."( Practitioner review: current best practice in the management of adverse events during treatment with ADHD medications in children and adolescents.
Banaschewski, T; Buitelaar, J; Coghill, D; Cortese, S; Danckaerts, M; Dittmann, RW; Graham, J; Holtmann, M; Sergeant, J; Taylor, E, 2013
)
0.39
" Tizanidine-induced adverse effects were examined in 100 patients treated with coadministration of tizanidine and 8 CYP1A2 inhibitors."( [Clinical survey of tizanidine-induced adverse effects--impact of concomitant drugs providing cytochrome P450 1A2 modification--].
Homma, M; Kohda, Y; Matsumoto, S; Momo, K; Sasaki, T, 2013
)
0.39
" We aimed to quantify co-administration of MQAB with interacting drugs and associated adverse drug reactions."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Electrocardiographic (ECG) monitoring and associated adverse events were validated in medical records."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Forty-four MQAB users had contraindicated co-administrations of simvastatin, atorvastatin, or tizanidine and three of those related adverse drug reactions."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" However, adverse drug reactions were rarely found, and costs vs."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
" Withdrawals due to all-cause, adverse effects and lack of efficacy were defined as primary outcomes evaluating the safety of such medications."( An Evaluation on the Efficacy and Safety of Treatments for Attention Deficit Hyperactivity Disorder in Children and Adolescents: a Comparison of Multiple Treatments.
Gao, J; He, S; Li, Y; Wang, Q; Zhang, Y, 2017
)
0.46
" Clonidine, melatonin, L-theanine, eszopiclone and guanfacine were well tolerated with mild to moderate adverse events; zolpidem was associated with neuropsychiatric adverse effects."( Safety, Tolerability and Efficacy of Drugs for Treating Behavioural Insomnia in Children with Attention-Deficit/Hyperactivity Disorder: A Systematic Review with Methodological Quality Assessment.
Anand, S; Besag, FMC; Chan, EW; Cortese, S; Tong, H; Wong, ICK, 2017
)
1.37
" This review demonstrates that neuraxial clonidine enhances postoperative analgesia in women having Caesarean section with neuraxial anaesthesia, but this has to be balanced against increased maternal adverse effects."( The impact of neuraxial clonidine on postoperative analgesia and perioperative adverse effects in women having elective Caesarean section-a systematic review and meta-analysis.
Allen, TK; Habib, AS; Klinger, RY; Mishriky, BM, 2018
)
1.05
"We aimed to determine if naloxone administration reversed the effects of clonidine or caused any adverse effects."( Naloxone reversal of clonidine toxicity: dose, dose, dose.
Loden, JK; Seger, DL, 2018
)
1.03
" There were no adverse events following the administration of any dose of naloxone."( Naloxone reversal of clonidine toxicity: dose, dose, dose.
Loden, JK; Seger, DL, 2018
)
0.8
" No adverse effects occurred in any patient including the 21 patients who received 10 mg naloxone."( Naloxone reversal of clonidine toxicity: dose, dose, dose.
Loden, JK; Seger, DL, 2018
)
0.8
" Percentages of improved patients' spasticity scale, mild adverse effect and severe adverse effect were extracted as outcomes."( A mixed treatment comparison on efficacy and safety of treatments for spasticity caused by multiple sclerosis: a systematic review and network meta-analysis.
Fu, X; Li, J; Li, M; Ma, Q; Wang, C; Wang, Y; Wu, H; Yang, W, 2018
)
0.48
" Cannabinoids, tizanidine and diazepam had significantly more mild adverse effect reports than placebo."( A mixed treatment comparison on efficacy and safety of treatments for spasticity caused by multiple sclerosis: a systematic review and network meta-analysis.
Fu, X; Li, J; Li, M; Ma, Q; Wang, C; Wang, Y; Wu, H; Yang, W, 2018
)
0.48
" Overall adverse event (AE) rates were similar across groups."( Safety and Efficacy of Lofexidine for Medically Managed Opioid Withdrawal: A Randomized Controlled Clinical Trial.
Alam, D; Clinch, T; Fishman, M; Gorodetzky, CW; Gullo, K; Tirado, C,
)
0.13
" Data suggest that lofexidine is a generally safe and effective nonopioid treatment for opioid withdrawal."( Safety and Efficacy of Lofexidine for Medically Managed Opioid Withdrawal: A Randomized Controlled Clinical Trial.
Alam, D; Clinch, T; Fishman, M; Gorodetzky, CW; Gullo, K; Tirado, C,
)
0.13
" The use of clonidine premedication was not associated with adverse hemodynamic events."( Safety and efficacy of clonidine on postoperative vomiting and pain in pediatric ophthalmic surgery: A systematic review and meta-analysis.
Bai, CH; Chen, C; Chu, KC; Hsu, CW; Hsu, YP; Huang, CJ, 2019
)
1.2
"We performed a systematic review focusing on adverse events."( Perioperative adverse events attributed to α2-adrenoceptor agonists in patients not at risk of cardiovascular events: systematic review and meta-analysis.
Antunes, T; Demiri, M; Fletcher, D; Martinez, V, 2019
)
0.51
"Pooled data for the incidence of adverse events associated with use of α2-adrenoceptor agonists in various perioperative contexts provide high-confidence evidence for a risk of hypotension and bradycardia, and protective effects against hypertension and tachycardia."( Perioperative adverse events attributed to α2-adrenoceptor agonists in patients not at risk of cardiovascular events: systematic review and meta-analysis.
Antunes, T; Demiri, M; Fletcher, D; Martinez, V, 2019
)
0.51
" The existing side effect prediction methods mainly focus on the chemical and biological properties of drugs."( Prediction of Side Effects Using Comprehensive Similarity Measures.
Kim, MH; Lee, T; Seo, S; Yoon, Y, 2020
)
0.56
" We reviewed adverse effects of clonidine occurring in this indication."( Safety of clonidine used for long-term sedation in paediatric intensive care: A systematic review.
Ahne, G; Eberl, S; Neubert, A; Standing, J; Toni, I, 2021
)
1.31
" However, concomitant use of tizanidine with ciprofloxacin, a strong inhibitor of the P450-CYP1A2 cytochrome metabolic pathway of tizanidine, can result in increased tizanidine plasma levels and associated adverse outcomes, particularly hypotension."( Risk of tizanidine-induced adverse events after concomitant exposure to ciprofloxacin: A cohort study in the U.S.
Giannouchos, TV; Gómez-Lumbreras, A; Malone, DC, 2022
)
0.72
" The prevalence of co-administration of drugs with a documented interaction highlights the need for continuous education across providers to avoid the incidence of DDI related adverse events and further complications and to improve patient outcomes."( Risk of tizanidine-induced adverse events after concomitant exposure to ciprofloxacin: A cohort study in the U.S.
Giannouchos, TV; Gómez-Lumbreras, A; Malone, DC, 2022
)
0.72
" Cases were separated into two groups depending on whether or not they received clonidine, and subsequently analysed according to pre- and post-intervention opioid requirements, clonidine dose administered and adverse effects."( Use of clonidine in the treatment of Irukandji syndrome: A 4-year retrospective cohort study on safety, efficacy and clinical utility.
Isman, A; Little, M; Seymour, J, 2022
)
1.4
" Clonidine was safe to administer and should be considered early when treating IS."( Use of clonidine in the treatment of Irukandji syndrome: A 4-year retrospective cohort study on safety, efficacy and clinical utility.
Isman, A; Little, M; Seymour, J, 2022
)
2.09
"Tizanidine is primarily metabolized via cytochrome P450 (CYP) 1A2 and therefore medications that inhibit the enzyme will affect the clearance of tizanidine, leading to increased plasma concentrations of tizanidine and potentially serious adverse events."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
0.72
"Our aim was to study the occurrence of adverse events reported in the FDA Adverse Event Reporting System (FAERS) involving the combination of tizanidine and drugs that inhibit the metabolic activity of CYP1A2."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
0.72
"A disproportionality analysis of FAERS reports from 2004 quarter 1 through 2020 quarter 3 was conducted to calculate the reporting odds ratio (ROR) of reports mentioning tizanidine in a suspect or interacting role or having any role, a CYP1A2 inhibitor, and the following adverse events: hypotension, bradycardia, syncope, shock, cardiorespiratory arrest, and fall or fracture."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
0.72
"A total of 89 reports were identified mentioning tizanidine, at least one CYP1A2 inhibitor, and one of the adverse events of interest."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
0.72
" Significant adverse effects reported included hypotension, light-headedness, drowsiness, dry mouth, rebound hypertension, and contact dermatitis from patch application."( The Safety and Efficacy of Clonidine in Hemodialysis Patients: A Systematic Review and Meta-Analysis.
An, R; Ashrafi, SA; Barton, A; Derk, G; Fang, HY; Wilund, K, 2022
)
1.02
"There is no evidence supporting the long-term use of clonidine in the HD population and a significant side-effect profile."( The Safety and Efficacy of Clonidine in Hemodialysis Patients: A Systematic Review and Meta-Analysis.
An, R; Ashrafi, SA; Barton, A; Derk, G; Fang, HY; Wilund, K, 2022
)
1.27
"Epidural clonidine improves analgesia but may induce adverse effects in labor."( Efficacy and safety of epidural clonidine by continuous infusion or patient-controlled analgesia in labor: A meta-analysis of randomized controlled trials.
Chang, XY; Wang, LZ; Xia, F; Zhang, YF, 2023
)
1.61
"A random effects model was used to pool the data on analgesia and adverse effects."( Efficacy and safety of epidural clonidine by continuous infusion or patient-controlled analgesia in labor: A meta-analysis of randomized controlled trials.
Chang, XY; Wang, LZ; Xia, F; Zhang, YF, 2023
)
1.19
"Epidural clonidine by continuous infusion or PCEA does not increase significant adverse effects and offers similar analgesia to opioids in labor."( Efficacy and safety of epidural clonidine by continuous infusion or patient-controlled analgesia in labor: A meta-analysis of randomized controlled trials.
Chang, XY; Wang, LZ; Xia, F; Zhang, YF, 2023
)
1.61
"Pharmacotherapeutic options for the treatment of opioid withdrawal are limited by abuse potential, adverse effects, and lack of availability of existing drugs."( Efficacy and safety of tramadol in the treatment of opioid withdrawal: A meta-analysis of randomized controlled trials.
Maiti, R; Mishra, BR; Mohapatra, D; Padhan, M, 2023
)
0.91

Pharmacokinetics

The pharmacokinetic as well as pharmacodynamic properties of a transdermal clonidine, M-5041T (M) and its safety were compared with those of oral Clonidine. Study of the influence of ZJAHC on the pharmacokinetics behaviors ofClonidine seems essential.

ExcerptReferenceRelevance
" Pharmacokinetic variables have been determined that allow: (1) derivation of the loading dose necessary to achieve rapid control of blood pressure with propranolol hydrochloride, guanethidine, minoxidil and clonidine hydrochloride; (2) reduced frequency of dosing with methyldopa, hydralazine hydrochloride, prazosin hydrochloride, propranolol and clonidine; and (3) alteration of propranolol and hydralazine dosage based on physiologic factors (e."( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs.
Schumacher, GE, 1979
)
0.45
"To investigate the pharmacokinetic behavior of clonidine, rats were given clonidine intravenously at 125, 250, and 500 micrograms/kg and blood clonidine concentrations were followed for 6 hr."( Pharmacokinetics of clonidine in the rat and cat.
Edlund, PO; Paalzow, LK, 1979
)
0.84
"28 ng/ml) and plasma half-life (10."( Pharmacokinetic and concentration-effect relationships of clonidine in essential hypertension.
Davies, DS; Dollery, CT; Neill, EA; Reid, JL; Tippett, P; Wing, LM, 1977
)
0.5
"52 ng/ml (SD) at 90 min and fell with a mean half-life of 12."( Clinical pharmacology and pharmacokinetics of clonidine.
Clare, RA; Dargie, HJ; Davies, DS; Dean, CR; Dollery, CT; Draffan, GH; Murray, S; Reid, JL, 1976
)
0.51
"The pharmacokinetic characteristics of a slow-release formulation of clonidine (150 micrograms) were compared with those of a conventional formulation (75 micrograms) after acute and chronic (2 week) administration to 12 hypertensive subjects."( Pharmacokinetic comparison of a slow-release clonidine with a conventional formulation after acute and chronic administration in hypertensives.
Anavekar, SN; Conway, EL; Howes, LG; Louis, WJ, 1992
)
0.78
" Plasma elimination half-life was 829 +/- 157 min and plasma clearance was 177 +/- 28 ml min-1."( Pharmacokinetics of clonidine after epidural administration in surgical patients. Lack of correlation between plasma concentration and analgesia and blood pressure changes.
Bovill, JG; Houben, JJ; Ploeger, EJ; van Essen, EJ, 1992
)
0.61
" A combined pharmacokinetic (first order absorption - 1 compartment) - pharmacodynamic (linear) model, including a hypothetical effect compartment with and without tolerance, were fitted to the data."( Pharmacokinetic-pharmacodynamic modeling of the effects of clonidine on pain threshold, blood pressure, and salivary flow.
Dayer, P; Piletta, P; Porchet, HC, 1992
)
0.53
" Peak plasma fentanyl concentrations (Fmax) and the time to reach Cmax (Tmax) were comparable in the two groups (0."( Effect of epidural clonidine on analgesia and pharmacokinetics of epidural fentanyl in postoperative patients.
Bonnet, F; Levron, JC; Pluskwa, F; Rostaing, S; Saada, M; Vodinh, J, 1991
)
0.61
" However, recent studies have shown that it has substantial antihypertensive efficacy with minimal side effects at low doses, and that half-life is long enough to allow twice daily administration."( Comparison of pharmacokinetics and pharmacodynamics of adrenoceptor agonists and antagonists as antihypertensive agents.
Anavekar, SN; Conway, EL; Drummer, OH; Howes, LG; Jarrott, B; Louis, WJ; McNeil, JJ; Workman, B, 1987
)
0.27
"The efficiency and duration of action of a single oral dose (8 mg) of tizanidine in patients with spinal cord injuries were determined by studying its antispastic, cardiovascular and sedative effects along with its pharmacokinetic profile in five tetraplegic and five paraplegic patients."( Pharmacodynamics and pharmacokinetics of the oral antispastic agent tizanidine in patients with spinal cord injury.
Baker, H; Desai, P; el Masri, W; Frankel, HL; Luckitt, J; Mathias, CJ, 1989
)
0.28
"Using a sensitive and specific radioimmunoassay the pharmacokinetic disposition of clonidine was determined in hypertensive patients after a single dose and then after 5, 28 and 56 days of chronic dosing with 75 micrograms bd."( Pharmacokinetics and antihypertensive effects of low dose clonidine during chronic therapy.
Anavekar, SN; Conway, EL; Howes, LG; Jarrott, B; Louis, WJ; Syrjanen, M, 1989
)
0.75
" Systemic absorption of epidurally administered clonidine occurred rapidly: Tmax in plasma was 34 +/- 6 min and plasma concentrations were similar to those following iv injection at all time points beyond 20 min."( Pharmacokinetics and dynamics of intravenous, intrathecal, and epidural clonidine in sheep.
Castro, MI; Eisenach, JC, 1989
)
0.76
" The lack of dose dependency in half-life and renal clearance estimates emphasise that the transdermal absorption of clonidine is linear."( Clinical pharmacokinetics of clonidine.
Lowenthal, DT; MacGregor, TR; Matzek, KM, 1988
)
0.78
" Repeated administration of [14C]tizanidine resulted in no apparent change in pharmacokinetic characteristics."( Pharmacokinetics of orally administered tizanidine in healthy volunteers.
Bhuta, S; Jaffe, JM; Tse, FL, 1987
)
0.27
" Statistical moment theory is also applied to the topical infusion data to determine ocular pharmacokinetic parameters for clonidine."( Ocular pharmacokinetic models of clonidine-3H hydrochloride.
Chiang, CH; Schoenwald, RD, 1986
)
0.76
"We detail a series of pharmacokinetic investigations to determine the dose linearity, the effect of site of application, the duration of steady-state plasma concentrations, and the effect of chronic application when clonidine is administered transdermally."( Pharmacokinetics of transdermally delivered clonidine.
Keirns, JJ; MacGregor, TR; Matzek, KM; van den Ende, A; van Tol, RG; van Wayjen, RG, 1985
)
0.72
" The assessment of TCA actions that may be additive, synergistic, or antagonistic requires precise knowledge of pharmacodynamic potency and control of pharmacokinetic behavior."( Active metabolites of antidepressants: pharmacodynamics and relevant pharmacokinetics.
Lane, EA; Potter, WZ; Rudorfer, MV, 1984
)
0.27
" The complete bioavailability of clonidine and its elimination half-life (20 to 25."( New aspects of the pharmacokinetics and pharmacodynamics of clonidine in man.
Arndts, D; Doevendans, J; Heintz, B; Kirsten, R, 1983
)
0.79
" 2 After acute oral administration the following values were obtained; Cmax -- 166."( Alinidine pharmacokinetics following acute and chronic dosing.
Arndts, D; Harron, DW; Shanks, RG, 1982
)
0.26
" Sampling over 48 h was necessary for accurate estimation of pharmacokinetic parameters."( Pharmacokinetic and pharmacodynamic studies of oral clonidine in normotensive subjects.
Anavekar, SN; Jarrott, B; Louis, WJ; Toscano, M, 1982
)
0.51
" From pharmacokinetic aspects therefore a fixed combination of two synergistic antihypertensive agents can be considered as useful."( [Pharmacokinetics of clonidine and chlorthalidone following subacute administration of a fixed combination compared with a sustained release formulation of clonidine alone (author's transl)].
Arendt, G; Arndts, D; Doevendans, J; Rippen, G, 1981
)
0.58
" Independent of the route of administration and of the doses given, similar pharmacokinetic parameters were calculated for each group and each trial."( Proof of the linearity of the pharmacokinetics of alinidine in man.
Arndts, D; Justus, H; Rominger, KL; Warnkross, H, 1981
)
0.26
" 5 The pharmacodynamic properties of the drug could explain the changes in pharmacokinetics with increased dose and during multiple doses."( Clonidine kinetics in man--evidence for dose dependency and changed pharmacokinetics during chronic therapy.
Edlund, PO; Frisk-Holmberg, M; Paalzow, L, 1981
)
1.71
" Furthermore, the pharmacodynamic action of alpha-2 adrenergic agonists, like many other sedative hypnotics (e."( Alpha-2 adrenergic modulation of sleep: time-of-day-dependent pharmacodynamic profiles of dexmedetomidine and clonidine in the rat.
Dement, WC; Edgar, DM; Maze, M; Seidel, WF, 1995
)
0.5
" Values of clearance, volume of distribution and elimination half-life were 71."( A pharmacokinetic-pharmacodynamic linking model for the alpha 2-adrenergic antagonism of idazoxan on clonidine-induced mydriasis in the rat.
Jane, F; Menargues, A; Obach, R; Pruñonosa, J; Valles, J, 1995
)
0.51
" There were no significant changes in the half-life (8."( Hormonal and metabolic effects and pharmacokinetics of recombinant insulin-like growth factor-I in growth hormone receptor deficiency/Laron syndrome.
Cohen, P; Diamond, FB; Fielder, PJ; Gargosky, S; Guevara-Aguirre, J; Rosenbloom, AL; Rosenfeld, RG; Vaccarello, MA; Wilson, K, 1993
)
0.29
"88), time to maximum plasma concentration 51 min (29-70), terminal half-life 12."( Pharmacokinetics of clonidine after rectal administration in children.
Bergendahl, HT; Eksborg, S; Lönnqvist, PA, 1994
)
0.61
"To compare the pharmacokinetic and pharmacodynamic profile of orally versus sublingually administered clonidine."( Comparative pharmacokinetics of oral versus sublingual clonidine.
Baughman, VL; Cunningham, FE; Laurito, CE; Peters, J,
)
0.59
"Both routes of administration resulted in similar pharmacokinetic and pharmacodynamic profiles."( Comparative pharmacokinetics of oral versus sublingual clonidine.
Baughman, VL; Cunningham, FE; Laurito, CE; Peters, J,
)
0.38
"The pharmacokinetic as well as pharmacodynamic properties of a transdermal clonidine, M-5041T (M) and its safety were compared with those of oral clonidine, Catapres (Nippon Boehringer Ingelheim, Hyogo, Japan)."( Comparison of the pharmacokinetics, pharmacodynamics, and safety of oral (Catapres) and transdermal (M-5041T) clonidine in healthy subjects.
Ebihara, A; Fujimura, A; Kotegawa, T; Kumagai, Y; Nakashima, H; Ohashi, K; Shiga, T, 1994
)
0.73
"The pharmacokinetic as well as the pharmacodynamic properties of a new transdermal clonidine, M-5041T (M), and its safety were evaluated after single and repeated applications."( Pharmacokinetics and pharmacodynamics of a new transdermal clonidine, M-5041T, in healthy subjects.
Ebihara, A; Fujimura, A; Kotegawa, T; Kumagai, Y; Nakashima, H; Ohashi, K; Shiga, T, 1993
)
0.75
"37) mg per day of clonidine the mean terminal half-life was 15."( The pharmacokinetics of clonidine in high dosage.
Fauler, J; Verner, L, 1993
)
0.93
" Life adrenaline, it may decrease lignocaine peak concentration (Cmax), thus leading to decreased toxicity."( Clonidine and or adrenaline decrease lignocaine plasma peak concentration after epidural injection.
Benhamou, D; Mazoit, JX; Samii, K; Veillette, Y, 1996
)
1.74
" All of the calculated steady-state pharmacokinetic parameter changes for baclofen, tizanidine, and its major metabolites were within the 30% criterion."( A controlled pharmacokinetic evaluation of tizanidine and baclofen at steady state.
Groves, L; Novack, GD; Shah, J; Shellenberger, MK, 1999
)
0.3
" Whether clonidine prolongs local anesthetic block by a pharmacokinetic effect or a pharmacodynamic effect is unclear."( Effect of clonidine on lidocaine clearance in vivo: a microdialysis study in humans.
Bernards, CM; Kopacz, DJ, 2001
)
1.13
" The pharmacokinetic data suggest that the mechanism of prolongation is at least in part pharmacokinetic."( Effect of clonidine on lidocaine clearance in vivo: a microdialysis study in humans.
Bernards, CM; Kopacz, DJ, 2001
)
0.71
" 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
" Blood samples were collected to determine plasma tizanidine pharmacokinetic profiles, and computerized cognitive function tests were performed that yielded a validated composite score, Power of Attention, an index of sedation."( Effects of food on the single-dose pharmacokinetics/pharmacodynamics of tizanidine capsules and tablets in healthy volunteers.
Henney, HR; Kovelesky, RA; Shah, J; Wesnes, KA, 2006
)
0.33
" A pharmacokinetic mechanism for the cranberry juice-warfarin interaction seems unlikely."( Effects of daily ingestion of cranberry juice on the pharmacokinetics of warfarin, tizanidine, and midazolam--probes of CYP2C9, CYP1A2, and CYP3A4.
Backman, JT; Lilja, JJ; Neuvonen, PJ, 2007
)
0.34
"The evaluation of drug disposition properties of chemical entities in drug discovery research typically involves the conduct of pharmacokinetic studies in rodents that requires blood sampling over several time points, preferably without disrupting the physiological status of the animals."( Pharmacokinetic comparisons of tail-bleeding with cannula- or retro-orbital bleeding techniques in rats using six marketed drugs.
Bina, H; Chiang, A; Ebbert, L; Huang, NH; Hui, YH; Kern, T; Maples, C; Patel, N; Pritt, M,
)
0.13
"Among nonsmokers, the peak concentration (C(max)) and area under concentration-time curve from 0 to infinity [AUC(0-infinity)] of tizanidine did not differ significantly between females and males."( Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine.
Backman, JT; Neuvonen, PJ; Schröder, MT, 2008
)
0.35
" The most common adverse events and pharmacodynamic effects are related to plasma concentrations."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.35
"The objective of this study was to characterize the clinical pharmacokinetic profile of lofexidine after oral delivery."( Pharmacokinetics of lofexidine hydrochloride in healthy volunteers.
Al-Ghananeem, AM, 2009
)
0.35
" 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
"The objective of this investigation was to characterize the pharmacokinetic profile of lofexidine."( Clinical pharmacokinetics of lofexidine, the alpha 2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis.
Akerele, E; Al-Ghananeem, AM; Elkashef, A; Fischman, MW; Herman, BH; Kleber, H; Ling, W; Miotto, K; O'Brien, CP; Yu, E, 2008
)
0.35
"During the detoxification period of a phase 3 placebo-controlled, randomized, double-blind trial, six subjects were entered in this preliminary pharmacokinetic study."( Clinical pharmacokinetics of lofexidine, the alpha 2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis.
Akerele, E; Al-Ghananeem, AM; Elkashef, A; Fischman, MW; Herman, BH; Kleber, H; Ling, W; Miotto, K; O'Brien, CP; Yu, E, 2008
)
0.35
"The objective of this study was to determine the pharmacokinetic parameters of clonidine during pregnancy compared with previously published data in nonpregnant subjects."( Clonidine pharmacokinetics in pregnancy.
Buchanan, ML; Carr, DB; Easterling, TR; Hebert, MF; Mattison, DR; Nelson, WL; Risler, LJ; Shen, DD, 2009
)
2.02
"The average half-life obtained from all profiles was 12."( Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients.
Abbassi, M; Al Ghananeem, AM; Herman, BH; Ling, W; Miotto, K; Montgomery, A; O'Brien, CP; Walsh, R; Yu, E, 2009
)
0.35
"5 ng x h/mL), and the half-life (1."( Effects of mexiletine, a CYP1A2 inhibitor, on tizanidine pharmacokinetics and pharmacodynamics.
Homma, M; Inomata, S; Kohda, Y; Momo, K; Osaka, Y; Tanaka, M, 2010
)
0.36
"The population pharmacokinetic (PK) profile of oral clonidine was characterized in newborns with neonatal abstinence syndrome, and significant covariates affecting its PK parameters were identified."( Clonidine clearance matures rapidly during the early postnatal period: a population pharmacokinetic analysis in newborns with neonatal abstinence syndrome.
Agthe, AG; Cao, YJ; Gauda, EB; Hendrix, CW; Lee, H; Xie, HG, 2011
)
2.06
" We sought to describe the pharmacodynamic effects of clonidine in pregnancy and the associated impact on fetal growth."( Pharmacodynamics of clonidine therapy in pregnancy: a heterogeneous maternal response impacts fetal growth.
Brateng, D; Carr, D; Easterling, TR; Hebert, M; Rothberger, S, 2010
)
0.93
"Conducting pharmacokinetic (PK) studies in pregnant women is challenging."( A physiologically based pharmacokinetic model to predict disposition of CYP2D6 and CYP1A2 metabolized drugs in pregnant women.
Isoherranen, N; Ke, AB; Nallani, SC; Rostami-Hodjegan, A; Unadkat, JD; Zhao, P, 2013
)
0.39
"Based on the pharmacokinetic and statistical results, it was concluded that; Tizanidine PIC® 4 mg tablets is bioequivalent to Sirdalud® 4 mg tablets of Novartis and smoking decreases Cmax and AUC of tizanidine."( Pharmacokinetic comparison of two 4 mg tablet formulations of tizanidine.
Al-Ghazawi, M; Alzoubi, M; Faidi, B, 2013
)
0.39
" The objective of this study was to evaluate the pharmacokinetic profile of tizanidine nasal spray and compare it to the profile of tizanidine oral tablets."( Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm.
Cardì, F; Drago, F; Piazza, C; Salomone, S; Sinagra, T; Urso, V; Vitale, DC, 2013
)
0.39
" The pharmacokinetic parameters of tizanidine in 9 healthy male Japanese subjects were compared with those of Caucasians in previous studies."( Lower metabolic clearance of tizanidine in Japanese subjects.
Homma, M; Kohda, Y; Momo, K, 2013
)
0.39
" The population pharmacokinetic modeling was done with NONMEM."( Melatonin and clonidine premedication has similar impact on the pharmacokinetics and pharmacodynamics of propofol target controlled-infusions.
Bienert, A; Grześkowiak, E; Józefowicz, M; Kokot, ZJ; Kusza, K; Matysiak, J; Pachutko, A; Przybyłowski, K; Wawrzyniak, K; Wiczling, P, 2015
)
0.78
" Hence, study of the influence of ZJAHC on the pharmacokinetic behaviors of clonidine seems essential."( Development of an LC-MS/MS method for determining the pharmacokinetics of clonidine following oral administration of Zhenju antihypertensive compound.
Chen, J; Han, L; Li, Y; Qin, J; Shen, T; Wang, J; Wang, L; Wu, L, 2015
)
0.88
" The mini-tablet combination released the two drugs over 24h in vivo with a steady plasma concentration, a markedly lower Cmax, extended Tmax and better bioavailability."( Mini-tablet combination for sustained release of clonidine hydrochloride and hydrochlorothiazide: Preparation and pharmacokinetics in beagle dogs.
Wang, Y; Xu, B; Zhu, H, 2016
)
0.69
" The pharmacokinetic analysis was conducted by nonlinear mixed effect modelling, which enables to establish the separate influences of determinants on drug blood level and to provide individualized dosing."( Population pharmacokinetics of intravenous clonidine for sedation during paediatric extracorporeal membrane oxygenation and continuous venovenous hemofiltration.
Ahsman, MJ; de Wildt, SN; Kleiber, N; Mathôt, RAA; Tibboel, D; Wildschut, ED, 2017
)
0.72
" Combining epidemiological studies with pharmacokinetic modeling, we detected and evaluated high-dimensional DDIs among 30 frequent drugs."( Translational High-Dimensional Drug Interaction Discovery and Validation Using Health Record Databases and Pharmacokinetics Models.
Chiang, CW; Li, L; Ning, X; Quinney, SK; Shen, L; Wang, L; Wang, X; Zhang, P; Zhang, S, 2018
)
0.48
" Simulations of clonidine plasma concentrations based on known population pharmacokinetic parameters suggest a loading dose followed by higher than current practice maintenance dose infusion is required to achieve adequate steady-state concentrations early in treatment."( Optimizing clonidine dosage for sedation in mechanically ventilated children: A pharmacokinetic simulation study.
Bardol, M; Breatnach, CV; Cousins, G; Dawkins, I; Doherty, DR; Gallagher, PJ; Hayden, JC; Healy, M; Standing, JF, 2019
)
1.25
"Clonidine is used off-label in children but only limited pediatric pharmacokinetic data are available for intravenously administered clonidine."( Pharmacokinetics of an intravenous bolus dose of clonidine in children undergoing surgery.
Afshari, A; Anderson, BJ; Falcon, L; Henneberg, SW; Lauritsen, T; Lomstein, E; Nielsen, BN; Ydemann, M, 2020
)
2.26
"To determine pharmacokinetic parameter estimates of clonidine in healthy children undergoing surgery and to investigate age-related differences."( Pharmacokinetics of an intravenous bolus dose of clonidine in children undergoing surgery.
Afshari, A; Anderson, BJ; Falcon, L; Henneberg, SW; Lauritsen, T; Lomstein, E; Nielsen, BN; Ydemann, M, 2020
)
1.06
"In a randomized placebo-controlled trial (The PREVENT AGITATION trial), blood samples for clonidine pharmacokinetic analysis were collected in a proportion of the enrolled patients."( Pharmacokinetics of an intravenous bolus dose of clonidine in children undergoing surgery.
Afshari, A; Anderson, BJ; Falcon, L; Henneberg, SW; Lauritsen, T; Lomstein, E; Nielsen, BN; Ydemann, M, 2020
)
1.03
" These results indicated that no dose reduction is needed in children aged 1 to <2 years compared with those 2-5 years, which was supported by pharmacodynamic observations."( Pharmacokinetics of an intravenous bolus dose of clonidine in children undergoing surgery.
Afshari, A; Anderson, BJ; Falcon, L; Henneberg, SW; Lauritsen, T; Lomstein, E; Nielsen, BN; Ydemann, M, 2020
)
0.81
" The physiologically based pharmacokinetic (PBPK) modeling platform Simcyp® was used to evaluate the impact of CYP1A2 modulation on tizanidine exposure through drug-drug interactions (DDIs) and host-dependent habits (cigarette smoking)."( Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: Impact of drug-drug interactions and cigarette consumption.
Heimbach, T; Jogiraju, VK; Taft, DR; Toderika, Y, 2021
)
0.62
" Physiologically based pharmacokinetic models were developed for tizanidine, incorporating the PerMCL model and the WSM, respectively, to simulate the interaction of tizanidine with a range of CYP1A2 inhibitors and inducers."( Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population Based Physiologically Based Pharmacokinetic Framework.
Bois, FY; Fisher, C; Gardner, I; Jamei, M; Kilford, P; Pan, X; Zhang, M, 2022
)
0.72

Compound-Compound Interactions

The purpose of this study was to evaluate comparatively the effectiveness of hyperbaric bupivacaine combined with 3 different adjuvants. Premedication with the alpha(2)-adrenoceptor agonist clonidine is as good as with benzodiazepines in combination with TCI.

ExcerptReferenceRelevance
"This study investigated antinociceptive effects of intrathecal morphine combined with intrathecal clonidine, noradrenaline, carbachol or midazolam in rats."( Antinociceptive and motor effects of intrathecal morphine combined with intrathecal clonidine, noradrenaline, carbachol or midazolam in rats.
Cmielewski, PL; Cousins, MJ; Gourlay, GK; Owen, H; Plummer, JL, 1992
)
0.73
"Because only limited and controversial data exist concerning the respiratory effects of clonidine in humans, the authors evaluated the respiratory effects of clonidine alone and in combination with morphine, in 12 healthy adult males."( Respiratory effects of clonidine alone and combined with morphine, in humans.
Bailey, PL; East, KA; East, TD; Eldredge, SJ; Johnson, GK; Pace, NL; Sperry, RJ; Stanley, TH, 1991
)
0.81
" Clonidine and the slightly alpha 1-selective agonist ST587, but not ST91, an alpha-agonist which does not readily cross the blood brain barrier, produced marked stimulation when combined with the selective D2 agonist quinpirole."( Alpha 1 (but not alpha 2)-adrenoceptor agonists in combination with the dopamine D2 agonist quinpirole produce locomotor stimulation in dopamine-depleted mice.
Edis, LE; Eshel, G; Jackson, DM; Kelder, D; Ross, SB, 1990
)
1.19
" Clonidine, given alone, had no effect; however, when administered with morphine it blocked the analgesic effect of morphine."( Effects of clonidine and yohimbine, alone and in combination with morphine, on supraspinal analgesia.
Izenwasser, S; Kornetsky, C, 1990
)
1.58
" The jumping elicited by TRH (20 mg/kg IP) in combination with apomorphine (0."( Jumping behavior induced by thyrotropin releasing hormone in combination with apomorphine in mice.
Furukawa, T; Noda, Y; Ushijima, I; Yamada, K, 1982
)
0.26
" Intrathecal carbachol is synergistic when combined with intrathecal morphine or clonidine."( Characteristics of the analgesic effects and drug interactions of intrathecal carbachol in rats.
Abram, SE; O'Connor, TC, 1995
)
0.52
"A double-blind study was conducted to assess the efficacy and the safety of epidural clonidine combined with bupivacaine for analgesia during labor."( Epidural clonidine combined with bupivacaine for analgesia in labor. Effects on mother and neonate.
Bonnet, F; Brohon, E; Cigarini, I; Damas, F; Dutz, F; Hans, P; Kaba, A,
)
0.77
" The ability of intrathecally administered clonidine alone or in combination with morphine, DPDPE, or U50,488H to alter thresholds for the production of the visceromotor response was examined."( Visceral antinociceptive effects of spinal clonidine combined with morphine, [D-Pen2, D-Pen5] enkephalin, or U50,488H.
Collins, JG; Harada, Y; Kishikawa, K; Kitahata, LM; Nishioka, K, 1995
)
0.82
"5 mg combined with adrenaline 25 micrograms and sufentanil 10 micrograms; group B received the same solution with clonidine 30 micrograms."( Clonidine combined with sufentanil and bupivacaine with adrenaline for obstetric analgesia.
De Kock, M; Le Polain, B; Scholtes, JL; Van Lierde, M, 1993
)
1.94
"We have studied the use of clonidine combined with low doses of sufentanil and bupivacaine in 45 parturients requiring extradural analgesia for the first stage of labour, in a double-blind, randomized study."( Extradural clonidine combined with sufentanil and 0.0625% bupivacaine for analgesia in labour.
Boulétreau, P; Chassard, D; Dailler, F; Golfier, F; Mathon, L; Tournadre, JP, 1996
)
0.98
" Epidural clonidine infused at 20 microg/h improves analgesia during coughing when combined with epidural bupivacaine-fentanyl in patients undergoing lower abdominal surgery but is associated with hemodynamic changes and increased vasopressor requirement."( Postoperative epidural infusion: a randomized, double-blind, dose-finding trial of clonidine in combination with bupivacaine and fentanyl.
Evans, SF; Lim, W; Orlikowski, CE; Paech, MJ; Pavy, TJ, 1997
)
0.92
" Because clonidine potentiates the analgesic effects of opioids without increasing their side effects, the authors wanted to determine the efficacy of low doses of intrathecal clonidine (15 and 30 microg) combined with sufentanil."( Intrathecal clonidine combined with sufentanil for labor analgesia.
De Kock, M; Fanard, L; Gautier, PE; Hody, JL; Van Steenberge, A, 1998
)
1.1
"To determine whether a low dose of spinal clonidine either alone or combined with sufentanil would provide effective analgesia following abdominal surgery, as a supplement to bupivacaine spinal anesthesia."( Low-dose intrathecal clonidine combined with sufentanil as analgesic drugs in abdominal gynecological surgery.
Julião, MC; Lauretti, GR, 2000
)
0.89
" Sixty adult patients underwent elective rotator cuff repair using interscalene brachial plexus block combined with general anesthesia and were randomly divided into one of the following three groups."( Clonidine combined with a long acting local anesthetic does not prolong postoperative analgesia after brachial plexus block but does induce hemodynamic changes.
Culebras, X; Gamulin, Z; Hoffmeyer, P; Van Gessel, E, 2001
)
1.75
"The drug-drug interactions discussed in this article have either documented or suspected clinical relevance for patients with cardiovascular disease and the clinician involved in the care of these patients."( Cardiovascular drug-drug interactions.
Anderson, JR; Nawarskas, JJ, 2001
)
0.31
"15 mg/kg) were administered subcutaneously in the rat in combination with KET (50 mg/kg), in the presence or not of YOH (2 mg/kg)."( Corneal toxicity of xylazine and clonidine, in combination with ketamine, in the rat.
Bordi, F; Casini, ML; Corubolo, C; Fehér, J; Fumagalli, E; Guidolin, D; Leone, MG; Mattioli, F; Romanelli, L; Saso, L; Tita, B,
)
0.41
"We previously found that spinal clonidine prolongs labor analgesia when combined with spinal bupivacaine and sufentanil."( Neostigmine combined with bupivacaine, clonidine, and sufentanil for spinal labor analgesia.
D'Angelo, R; Dean, LS; Meister, GC; Nelson, KE, 2001
)
0.86
"This study evaluates the efficacy and side effects of a low dose of epidural morphine combined with clonidine for postoperative pain relief after lumbar disc surgery."( Epidural administration of low-dose morphine combined with clonidine for postoperative analgesia after lumbar disc surgery.
Bonhomme, V; Brichant, JF; Dewandre, PY; Doll, A; Ghassempour, K; Hans, P, 2002
)
0.77
"Spinal anesthesia with supplemental epidural clonidine in combination with incision site subcutaneous bupivacaine was evaluated both intra- and postoperatively and compared with spinal anesthesia alone for lower lumbar spine procedures."( The effect of spinal bupivacaine in combination with either epidural clonidine and/or 0.5% bupivacaine administered at the incision site on postoperative outcome in patients undergoing lumbar laminectomy.
Abodeely, A; Fluder, EM; Jellish, WS; Shea, J, 2003
)
0.81
" We randomized 45 patients to 3 groups receiving intrathecal hyperbaric bupivacaine 6 mg combined with saline (Group B), clonidine 15 micro g (Group BC15), or clonidine 30 micro g (Group BC30); all solutions were diluted with saline to 3 mL."( Clonidine combined with small-dose bupivacaine during spinal anesthesia for inguinal herniorrhaphy: a randomized double-blinded study.
Axelsson, K; Dobrydnjov, I; Gupta, A; Holmström, B; Klockhoff, H; Matthiesen, P; Thörn, SE, 2003
)
1.97
" In this study we examined midazolam and clonidine for premedication in combination with target controlled infusion anaesthesia (TCI) in patients undergoing orthopaedic shoulder surgery and analysed the effects on the peri- and postoperative course."( [Comparison of premedication with clonidine and midazolam combined with TCI for orthopaedic shoulder surgery].
Dietrich, PJ; Grottke, O; Krause, TH; Müller, J; Wappler, F, 2003
)
0.86
"Premedication with the alpha(2)-adrenoceptor agonist clonidine is as good as with benzodiazepines in combination with TCI."( [Comparison of premedication with clonidine and midazolam combined with TCI for orthopaedic shoulder surgery].
Dietrich, PJ; Grottke, O; Krause, TH; Müller, J; Wappler, F, 2003
)
0.85
"The efficiency of bilateral paravertebral blockade combined with general anaesthesia (active) vs."( General anaesthesia combined with bilateral paravertebral blockade (T5-6) vs. general anaesthesia for laparoscopic cholecystectomy: a prospective, randomized clinical trial.
Lönnqvist, PA; Naja, MZ; Ziade, MF, 2004
)
0.32
"We evaluated the efficacy of local or systemic parecoxib combined with lidocaine/clonidine IV regional analgesia in complex regional pain syndrome (CRPS) type 1 in a dominant upper limb."( The antinociceptive effect of local or systemic parecoxib combined with lidocaine/clonidine intravenous regional analgesia for complex regional pain syndrome type I in the arm.
Frade, LP; Lauretti, GR; Lima, ICPR; Pereira, NL, 2005
)
0.78
"Although caudal morphine may result in more sustained initial analgesia, caudal clonidine combined with nurse-controlled analgesia appears to provide comparable analgesia with fewer side effects."( A comparison of single-dose caudal clonidine, morphine, or hydromorphone combined with ropivacaine in pediatric patients undergoing ureteral reimplantation.
Carvallo, D; Johnson, JL; Mazurek, MS; Presson, RG; Vetter, TR, 2007
)
0.84
"To evaluate the quality of sedation and the effects of midazolam and diazepam alone or combined with clonidine on the heart rate (HR) and blood pressure (BP) of patients with suspected coronary artery disease."( Sedative and cardiovascular effects of midazolam and diazepam alone or combined with clonidine in patients undergoing hemodynamic studies for suspected coronary artery disease.
Carvalho, HG; Modolo, NS; Nascimento, Jdos S; Santos, KP; Silva, RC, 2007
)
0.78
"To investigate the clinical effects of epidural clonidine pretreatment in epidural patient-controlled analgesia (PCA) using sufentanil combined with levobupivacaine."( [Effects of epidural clonidine pretreatment in epidural patient-controlled analgesia using sufentanil combined with levobupivacaine].
Ruan, XC; She, SZ; Su, J; Xie, XQ; Xu, LX, 2008
)
0.92
" 4 microg/ml combined with levobupivacaine 2 mg/ml was given for postoperative epidural patient-controlled analgesia."( [Effects of epidural clonidine pretreatment in epidural patient-controlled analgesia using sufentanil combined with levobupivacaine].
Ruan, XC; She, SZ; Su, J; Xie, XQ; Xu, LX, 2008
)
0.66
"Epidural clonidine 2-4 microg/kg pretreatment improves the clinical effects of epidural PCA using sufentanil combined with levobupivacaine."( [Effects of epidural clonidine pretreatment in epidural patient-controlled analgesia using sufentanil combined with levobupivacaine].
Ruan, XC; She, SZ; Su, J; Xie, XQ; Xu, LX, 2008
)
1.08
"The purpose of this study was to evaluate comparatively, in women undergoing caesarean section under spinal anesthesia, the effectiveness of hyperbaric bupivacaine combined with 3 different adjuvants (fentanyl, clonidine, and dexmedtomidine) on quality of blockade and maternal and neonatal repercussions."( A Randomised Controlled Trial to Evaluate the Effectiveness of Intrathecal Bupivacaine Combined with Different Adjuvants (Fentanyl, Clonidine and Dexmedetomidine) in Caesarean Section.
Huang, AJ; Li, AZ; Li, KZ; Li, Z; Qi, J; Shi, CX; Tian, M; Xin, DQ; Zhang, CY, 2015
)
0.81
"Polypharmacy increases the risk of drug-drug interactions (DDIs)."( Translational High-Dimensional Drug Interaction Discovery and Validation Using Health Record Databases and Pharmacokinetics Models.
Chiang, CW; Li, L; Ning, X; Quinney, SK; Shen, L; Wang, L; Wang, X; Zhang, P; Zhang, S, 2018
)
0.48
"Potential drug-drug interactions (pDDIs) are described in various case reports, but few studies have evaluated the impact of specific combinations on a population level."( Analysis of Drug-Drug Interactions in Swiss Claims Data Using Tizanidine and Ciprofloxacin as a Prototypical Contraindicated Combination.
Curkovic, I; Egbring, M; Jödicke, AM; Kullak-Ublick, GA; Neuer, T; Roos, M; Tomka, IT; Zellweger, U, 2018
)
0.48
"Lofexidine (LFX), an α2A adrenergic receptor agonist, known to alleviate opioid withdrawal symptoms, was assessed in combination with oral naltrexone (NTX) for effects on opioid use outcomes and NTX treatment compliance."( Lofexidine in Combination With Oral Naltrexone for Opioid Use Disorder Relapse Prevention: A Pilot Randomized, Double-Blind, Placebo-Controlled Study.
Fogelman, N; Hermes, G; Hyman, SM; Kosten, TR; Sinha, R, 2019
)
0.51
"To compare extracorporeal shock wave therapy combined with oral medication and an exercise program vs sham treatment with medication and exercise for the treatment of chronic low back pain (CLBP)."( Extracorporeal Shock Wave Therapy Combined With Oral Medication and Exercise for Chronic Low Back Pain: A Randomized Controlled Trial.
Khosrawi, S; Ramezani, M; Taheri, P, 2021
)
0.62
"Extracorporeal shock wave therapy combined with oral medication and exercise was safe and effective in the short-term treatment of chronic low back pain."( Extracorporeal Shock Wave Therapy Combined With Oral Medication and Exercise for Chronic Low Back Pain: A Randomized Controlled Trial.
Khosrawi, S; Ramezani, M; Taheri, P, 2021
)
0.62
" The physiologically based pharmacokinetic (PBPK) modeling platform Simcyp® was used to evaluate the impact of CYP1A2 modulation on tizanidine exposure through drug-drug interactions (DDIs) and host-dependent habits (cigarette smoking)."( Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: Impact of drug-drug interactions and cigarette consumption.
Heimbach, T; Jogiraju, VK; Taft, DR; Toderika, Y, 2021
)
0.62
"Paroxysmal localized hyperhidrosis is a rare central autonomic nervous system disorder that can occur in combination with severe headache."( Paroxysmal localized Hyperhidrosis, a case-report: When excessive sweating occurs in combination with severe headaches.
Schoofs, MW; van Coevorden, MH; Venhovens, J, 2021
)
0.62
" The aim of the current study was to compare the performance of a permeability-limited multicompartment liver (PerMCL) model, which operates as an approximation of the dispersion model, and the well stirred model (WSM) for predicting tizanidine drug-drug interactions (DDIs)."( Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population Based Physiologically Based Pharmacokinetic Framework.
Bois, FY; Fisher, C; Gardner, I; Jamei, M; Kilford, P; Pan, X; Zhang, M, 2022
)
0.72
"Methadone and buprenorphine have pharmacologic properties that are concerning for a high risk of drug-drug interactions (DDIs)."( Identifying Clinically Relevant Drug-Drug Interactions With Methadone and Buprenorphine: A Translational Approach to Signal Detection.
Acton, EK; Bilker, WB; Brensinger, CM; Dawwas, GK; Hennessy, S; Leonard, CE; Li, L; Miano, TA; Neuman, M; Nguyen, TPP; Soprano, SE; Wang, L; Woody, G; Yu, E, 2022
)
0.72

Bioavailability

The bioavailability and effect on the systolic and diastolic blood pressure, heart rate, salivary flow, skin temperature, and subjective sedation were studied in nine healthy volunteers. Lofexidine is an orally bioavailable alpha 2-adrenergic receptor agonist analogue of clonidine that acts centrally to suppress opiate withdrawal symptoms.

ExcerptReferenceRelevance
" The bioavailability of oral clonidine in the tablets tested averaged 75."( Pharmacokinetics and concentration-effect relationships of intervenous and oral clonidine.
Davies, DS; Dollery, CT; Neill, DM; Reid, JL; Tippett, P; Wing, AM, 1977
)
0.78
" Alpha-agonist effects are due: 1) to an activation of the post and/or presynaptic alpha 2-adrenoceptors in the substantia gelatinosa of the spinal cord, 2) to a local vasoconstriction by stimulating vascular smooth muscle alpha-receptors which decrease the rate of absorption of local anaesthetics from the subarachnoid or extradural space, 3) to a co-activation of the spinal opioid and alpha-adrenergic receptors at the spinal cord level."( [Intrathecal and epidural administration of alpha adrenergic receptor agonists].
Racle, JP, 1990
)
0.28
"The bioavailability and cardiac depressant activity of 3H-clonidine was studied following intravenous and nasal administration in rodents."( Comparison of intravenous and nasal bioavailability of clonidine in rodents.
Abdullah, ME; Babhair, SA; Tariq, M, 1990
)
0.77
" Sirdalud was well absorbed and almost completely metabolized in the five species."( Biological fate of sirdalud in animals and man.
Hirst, DR; Koch, P; von Wartburg, BR, 1989
)
0.28
" Single- and multiple-dose pharmacokinetic studies in healthy volunteers have shown that the relative bioavailability of the modified release formulation is similar to that of conventional tablets and is unaffected by food."( Modified release tizanidine: a review.
Hutchinson, DR,
)
0.13
" Dural transfer of epidurally administered clonidine was rapid and extensive: time to maximal concentration (Tmax) in CSF was 32 +/- 8 min, bioavailability in CSF was 14 +/- 4% of the administered dose, and maximal CSF concentrations following epidural administration (820 +/- 30 ng/ml) were three orders of magnitude greater than those following iv injection (0."( Pharmacokinetics and dynamics of intravenous, intrathecal, and epidural clonidine in sheep.
Castro, MI; Eisenach, JC, 1989
)
0.77
" Similarly, clinical myotonolytic activity of eperisone would only be expected at high doses unless its functional bioavailability were to be much better in man than in either the mouse or rabbit."( Comparison of the myotonolytic activity of tizanidine, eperisone and afloqualone in mouse and rabbit.
Coward, DM; White, TG,
)
0.13
" In addition, L-654,284 had better (5-6 times) oral bioavailability than RX 781094 or WY 26703."( L-654,284 a new potent and selective alpha 2-adrenoceptor antagonist.
Baldwin, JJ; Clineschmidt, BV; Huff, JR; Lotti, VJ; Martin, GE; Pettibone, DJ; Randall, WC; Vacca, J, 1986
)
0.27
" Compared to the oral route, losses in bioavailability due to first-pass liver metabolism are reduced."( Transdermal delivery of drugs.
Brown, L; Langer, R, 1988
)
0.27
" Tizanidine was rapidly and almost completely absorbed from the gastrointestinal tract, although the estimated bioavailability was only 21% due to extensive first-pass metabolism."( Pharmacokinetics of orally administered tizanidine in healthy volunteers.
Bhuta, S; Jaffe, JM; Tse, FL, 1987
)
0.27
" Evaluation in approximately 2000 patients with mild to moderate hypertension has shown that the bioavailability of transdermal clonidine is comparable to that of oral clonidine and that equivalent blood pressure reductions are achieved."( Efficacy of clonidine as transdermal therapeutic system: the international clinical trial experience.
Bies, C; Cristal, N; Fagan, T; Lowenthal, DT; Paran, E; Saris, S; Sharif, K, 1986
)
0.86
" To understand the implications for retina-optic nerve vascular physiology and pathophysiology, studies of the exact location of the binding sites, the bioavailability of the adrenergic agonists, and the physiological responses to receptor stimulation in both normal and pathological states are required."( Adrenergic alpha 1 and alpha 2 binding sites are present in bovine retinal blood vessels.
Anderson, DR; Ferrari-Dileo, G; Forster, BA, 1987
)
0.27
" Striatal concentrations of 3,4-dihydroxyphenylacetic acid and homovanillic acid were rapidly reduced by N-0500 both after intraperitoneal and oral administration, indicating that this compound is well absorbed from the gastrointestinal tract and passes the blood-brain barrier to activate DA autoreceptors."( Neuropharmacological profile of a new series of dopamine agonists: N-n-propyl-hexahydronaphthoxazines.
De Vries, JB; Dijkstra, D; Hazelhoff, B; Horn, AS; Mulder, TB; Timmermans, PB; Wynberg, H, 1986
)
0.27
"Tablet cores of clonidine (Catapres) showing varying rates of in vitro dissolution were administered in a crossover study with intravenous clonidine to determine the rate of absorption into the systemic circulation in humans."( Pharmacokinetics of oral sustained release clonidine in humans.
Keirns, JJ; MacGregor, TR; Relihan, GL, 1985
)
0.88
" In other experiments, the net absorption rate of the whole gut during steady state total gut perfusion was measured."( Studies of the antidiarrheal action of clonidine. Effects on motility and intestinal absorption.
Fordtran, JS; Morawski, SG; Santa Ana, CA; Schiller, LR, 1985
)
0.54
" The utility of the assay was demonstrated in a bioavailability study of clonidine conducted with 24 healthy subjects."( Radioimmunoassay for clonidine in human plasma and urine using a solid phase second antibody separation.
Chow, CT; Esber, HJ; Farina, PR; Homon, CA; Keirns, JJ; Zavorskas, PA, 1985
)
0.82
" The bioavailability following oral administration was nearly complete (0."( Pharmacokinetic and pharmacodynamic properties of alinidine in man.
Jähnchen, E; Kasper, W; Meinertz, T; Stützle, U; Wiegand, UW,
)
0.13
" Calculated values of clearance and apparent volume of distribution were almost certainly overestimates as it seems probable that the orally-administered drug undergoes significant presystemic elimination (its bioavailability was not determined in the investigation here reported)."( Tizanidine--initial pharmacokinetic studies in patients with spasticity.
Eadie, MJ; Heazlewood, V; Maruff, P; Symoniw, P, 1983
)
0.27
" The complete bioavailability of clonidine and its elimination half-life (20 to 25."( New aspects of the pharmacokinetics and pharmacodynamics of clonidine in man.
Arndts, D; Doevendans, J; Heintz, B; Kirsten, R, 1983
)
0.79
"The bioavailability and effect on the systolic and diastolic blood pressure, heart rate, salivary flow, skin temperature, and subjective sedation of three brands of clonidine were studied in nine healthy volunteers after a single 300-micrograms oral dose."( Bioavailability and clinical effects of three brands of clonidine: the relationship between plasma level and effect.
Allonen, H; Hiltunen, R; Kanto, J; Mäntylä, R; Marvola, M, 1982
)
0.71
" From the accumulated renally-excreted total radioactivities, the enteral absorption of the drug was calculated (91%); the bioavailability of orally administered alinidine was derived from the corresponding areas under the blood plasma concentration curves of the radioimmunologically-evaluated parent compound (72%)."( Development and quality control of a highly sensitive radioimmunoassay for alinidine.
Arndts, D; Stähle, H, 1981
)
0.26
" The bioavailability was 90%."( Clonidine kinetics in man--evidence for dose dependency and changed pharmacokinetics during chronic therapy.
Edlund, PO; Frisk-Holmberg, M; Paalzow, L, 1981
)
1.71
" To estimate the bioavailability of clonidine the results from the current study were compared with data from a previous study in which the same dose of clonidine was given to a similar patient population by the intravenous route."( Pharmacokinetics of clonidine after rectal administration in children.
Bergendahl, HT; Eksborg, S; Lönnqvist, PA, 1994
)
0.89
"5), and bioavailability 95% (73-119) (medians [95% confidence interval])."( Pharmacokinetics of clonidine after rectal administration in children.
Bergendahl, HT; Eksborg, S; Lönnqvist, PA, 1994
)
0.61
"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
" The in vitro release rate of the clonidine from KBD-TTS significantly correlated with the in vivo absorption rate (p<0."( In vitro and in vivo characterization of a newly developed clonidine transdermal patch for treatment of attention deficit hyperactivity disorder in children.
Guo, HY; Ke, GM; Lu, WL; Wang, L; Xue, HY; Zhang, Q; Zhang, X, 2005
)
0.85
"The monoamine theory of depression proposes decreased bioavailability of monoamines, such as norepinephrine (NE), as the underlying cause of depression."( An antidepressant mechanism of desipramine is to decrease tumor necrosis factor-alpha production culminating in increases in noradrenergic neurotransmission.
Ignatowski, TA; Reynolds, JL; Spengler, RN; Sud, R, 2005
)
0.33
" The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic, bioavailability or bioequivalence studies."( Quantification of tizanidine in human plasma by liquid chromatography coupled to tandem mass spectrometry.
Kandikere, VN; Maurya, S; Mudigonda, K; Nirogi, RV; Shukla, M, 2006
)
0.33
" Cannula-bleeding, especially coupled with automated blood-collection techniques, has become the most efficient way for pharmaceutical industry to perform rat bioavailability studies."( Pharmacokinetic comparisons of tail-bleeding with cannula- or retro-orbital bleeding techniques in rats using six marketed drugs.
Bina, H; Chiang, A; Ebbert, L; Huang, NH; Hui, YH; Kern, T; Maples, C; Patel, N; Pritt, M,
)
0.13
" The relative bioavailability of epidural and rectal clonidine was unity (F = 1)."( Clonidine disposition in children; a population analysis.
Anderson, BJ; Eksborg, S; Larsson, P; Lönnqvist, PA; Potts, AL; Warman, G, 2007
)
2.03
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" Lofexidine is an orally bioavailable alpha 2-adrenergic receptor agonist analogue of clonidine that acts centrally to suppress opiate withdrawal symptoms."( Clinical pharmacokinetics of lofexidine, the alpha 2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis.
Akerele, E; Al-Ghananeem, AM; Elkashef, A; Fischman, MW; Herman, BH; Kleber, H; Ling, W; Miotto, K; O'Brien, CP; Yu, E, 2008
)
0.57
" The bioavailability of clonidine given orally in adults is 75-100% but is unknown in children."( Oral bioavailability of clonidine in children.
Almenrader, N; Anderson, BJ; Bergendahl, HT; Eksborg, S; Larsson, P; Lönnqvist, PA; Nordlinder, A, 2011
)
0.98
" The oral bioavailability was 55."( Oral bioavailability of clonidine in children.
Almenrader, N; Anderson, BJ; Bergendahl, HT; Eksborg, S; Larsson, P; Lönnqvist, PA; Nordlinder, A, 2011
)
0.68
" The oral bioavailability was 55."( Oral bioavailability of clonidine in children.
Almenrader, N; Anderson, BJ; Bergendahl, HT; Eksborg, S; Larsson, P; Lönnqvist, PA; Nordlinder, A, 2011
)
0.68
" To show the importance of physicochemical properties, the classic QSAR and CoMFA of neonicotinoids and prediction of bioavailability of pesticides in terms of membrane permeability in comparison with drugs are described."( Importance of physicochemical properties for the design of new pesticides.
Akamatsu, M, 2011
)
0.37
" The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4."( Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.
Chithaluru, K; Kumar, KK; Ramarao, T; Someshwar, K, 2011
)
0.37
"  Clonidine is an alpha-2 agonist with a nearly 100% bioavailability after oral or rectal administration."( Severe hypertension following accidental clonidine overdose during the refilling of an implanted intrathecal drug delivery system.
Bovy, M; Buchser, E; Durrer, A; Mustaki, JP; Perruchoud, C; Rosato, M; Rutschmann, B,
)
1.12
" Addition of clonidine to the formulations decreased the systemic absorption rate of the anesthetics from the patch application site without impacting the coating performance or the rapid onset of anesthesia."( Adjuvants to prolong the local anesthetic effects of coated microneedle products.
Brown, K; Dohmeier, D; Hansen, K; Siebenaler, K; Zhang, Y, 2012
)
0.75
" Therefore, the nasal route of administration, which bypasses portal circulation, may increase the bioavailability of tizanidine and, possibly, reduce the time to peak plasma concentration, thereby shorting the latency of therapeutic effect."( Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm.
Cardì, F; Drago, F; Piazza, C; Salomone, S; Sinagra, T; Urso, V; Vitale, DC, 2013
)
0.39
"The bioavailability of the tizanidine intranasal formulation was higher than that of tizanidine oral tablets."( Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm.
Cardì, F; Drago, F; Piazza, C; Salomone, S; Sinagra, T; Urso, V; Vitale, DC, 2013
)
0.39
" ZJAHC could enhance the bioavailability without greatly increasing peak concentration of clonidine."( Development of an LC-MS/MS method for determining the pharmacokinetics of clonidine following oral administration of Zhenju antihypertensive compound.
Chen, J; Han, L; Li, Y; Qin, J; Shen, T; Wang, J; Wang, L; Wu, L, 2015
)
0.87
"Provided age-appropriate strengths are available, intravenous formulations remain the most predictable in terms of bioavailability and flexible in terms of dose adjustment."( A mini-review of non-parenteral clonidine preparations for paediatric sedation.
Hanning, SM; Neubert, A; Orlu Gul, M; Toni, I; Tuleu, C, 2017
)
0.74
" Compound 12g with MIC values of 5 μg/ml as a representative may possess better oral bioavailability and indicated high permeability by the parallel artificial membrane permeation assay of the blood-brain barrier (PAMPA-BBB)."( Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
An, Q; Deng, Y; Liu, P; Luo, Y; Sang, Z; Tang, Y; Wang, T; Yang, T; Yang, Y; Zhang, T, 2018
)
0.48
"A strong need exists for the development of transdermal patch having improved bioavailability at the site of action with fewer side effects at off-target organs."( Fabrication and characterization of matrix type transdermal patches loaded with tizanidine hydrochloride: potential sustained release delivery system.
Katas, H; Rahman, KU; Razzaq, Z; Shahid, N; Siddique, MI; Waqas, MK, 2018
)
0.48
" It has low oral bioavailability and short halflife."( Optimization of Microemulgel for Tizanidine Hydrochloride.
Brahmane, S; Chabukswar, A; Jagdale, S, 2020
)
0.56
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"The aim of the present investigation was to formulate self-microemulsifying drug delivery system (SMEDDS) tablets to enhance the oral bioavailability of tizanidine hydrochloride."( Development of Solid Self-Microemulsifying System of Tizanidine Hydrochloride for Oral Bioavailability Enhancement: In Vitro and In Vivo Evaluation.
Pramanik, S; Thakkar, H, 2020
)
0.56
" The currently available oral dosage forms exhibit low oral bioavailability due to high first-pass metabolism."( Derma roller mediated transdermal delivery of tizanidine invasomes for the management of skeletal muscle spasms.
Brahmam, B; Chaudhari, P; Dsouza, L; Lewis, SA, 2021
)
0.62
"The main limitations of the therapeutic effectiveness of tizanidine hydrochloride (TNZ) are its low bioavailability due to its tendency to undergo first-pass metabolism and short biological half-life."( Development of Biocompatible Nanoparticles of Tizanidine Hydrochloride in Orodispersible Films:
Dutt, R; Kaushik, D; Mittal, V; Pandey, P; Rahman, MH; Singh, S; Sinha, S; Thapa, S; Verma, R, 2022
)
0.72
" TZN has low oral bioavailability due to extensive first-pass metabolism and is used orally at a dose of 6-24 mg per day."( Chitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine.
Arpa, MD; Cevher, E; Gök, MK; Okur, NÜ; Özgümüş, S, 2023
)
0.91

Dosage Studied

Clonidine showed subsensitivity of alpha2-adrenergic autoreceptors in protein-deprived rats, a phenomenon reversed by fluoxetine treatment. Yohimbine shifted the dose-response curve of the contractile response to the alpha 2-agonist, clonidine, in a dose-dependent manner, causing a 10 fold shift.

ExcerptRelevanceReference
" Dose-response curves for the pre- and postsynaptic effects of eight alpha-receptor agonists were determined on superfused strips of the artery in the presence of cocaine, corticosterone and propranolo."( Relative pre- and postsynaptic potencies of alpha-adrenoceptor agonists in the rabbit pulmonary artery.
Endo, T; Starke, K; Taube, HD, 1975
)
0.25
" Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effects of increasing concentrations of the antagonists on cumulative clonidine dose-response curves on the stimulated vas deferens."( Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.
Doxey, JC; Smith, CF; Walker, JM, 1977
)
0.46
"The influence of the dosage or duration of treatment on the incidence and severity of clonidine withdrawal responses was examined in normotensive rats."( Withdrawal of clonidine: effects of varying dosage or duration of treatment on subsequent blood pressure and heart rate responses.
Monaghan, JC; Oates, HF; Stoker, LM; Stokes, GS, 1978
)
0.84
" The dose-response curve for the chronotropic action of phenylephrine was parallel to that of isoprenaline, whilst the dose-response curve for the inotropic action of phenylephrine was less steep than that of isoprenaline."( Characterization of adrenoceptors mediating positive inotropic responses in the ventricular myocardium of the dog.
Endoh, M; Shimizu, T; Yanagisawa, T, 1978
)
0.26
" 2 In the absence of morphine the inhibitory effects of the presynaptic alpha-adrenoceptor agonists, clonidine and oxymetazoline were much reduced and the dose-response curve was flat."( The inhibitory effects of presynaptic alpha-adrenoceptor agonists on contractions of guinea-pig ileum and mouse vas deferens in the morphine-dependent and withdrawn states produced in vitro.
Gillan, MG; Kosterlitz, HW; Robson, LE; Waterfield, AA, 1979
)
0.48
"2 mg/kg) of apomorphine reduced locomotion in a dose-dependent manner, while the reduction after higher doses was less pronounced, indicating a biphasic dose-response relationship."( Catecholamine receptor agonists: effects on motor activity and rate of tyrosine hydroxylation in mouse brain.
Strömbom, U, 1976
)
0.26
" The increase was blocked by phenoxybenzamine at a dosage level of 20 mg/kg which did not, of itself, reduce flexor reflex amplitude."( A system for measuring the noradrenaline receptor contribution to the flexor reflex.
Austin, JH; Fuxe, K; Nygren, LG, 1976
)
0.26
" This sympathoinhibitory action was characterized by means of a pC30, calculated from dose-response curves."( Central and peripheral alpha-adrenergic effects of some imidazolidines.
Timmermans, PB; Van Zwieten, PA, 1977
)
0.26
"The central hypotensive action of clonidine and 26 structurally related derivatives was quantified by means of an ED30 obtained from dose-response curves following intravenous administration to anesthetized, normotensive rats."( Quantitative structure-activity relationships in centrally acting imidazolidines structurally related to clonidine.
Timmermans, PB; van Zwieten, PA, 1977
)
0.75
" A dose-response curve of the lowering effect on intraocular pressure (IOP) has been made and compared with the dose-response cure obtained after intravenous administration."( The central ocular hypotensive effect of clonidine.
Innemee, HC; van Zwieten, PA, 1979
)
0.53
"Pharmacokinetic methods that have been used to improve antihypertensive drug therapy, including antihypertensive dosage regimens, are reviewed."( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs.
Schumacher, GE, 1979
)
0.26
" Analysis of the dose-response curves demonstrated that the effect of flutonidin was one-fifth to one-twelfth that of clonidine, depending on which variable was considered."( Hypotensive action and side-effects of flutonidin in normal subjects. A double-blind controlled trial.
Chierichetti, SM; Ferrari, P; Sala, P, 1979
)
0.47
"Three dosage combinations of clonidine and cyclothiazide were tested in at least 20 patients each, under clinical (4 weeks) and oupatients (longterm) conditions, in order to find a suitable combination with fewer side effects than the single drugs with at least equal efficacy for the longterm treatment of hypertension."( [Clinical trial of a combination preparation of clonidine and cyclothiazide (author's transl)].
Wimmer, PP, 1977
)
0.8
" The greatest improvement was noted in the perimenopausal group of women whose dosage requirement was 25 microgram three times a day."( Low-dosage clonidine (Dixarit) in menopausal flushing.
Evans, J; Hailes, J, 1979
)
0.65
" In part of the experiments the animals were pretreated with reserpine at a dosage of 2X0."( [Studies on the mechanism of action of clonidine after pretreatment with reserpine (author's transl)].
Dülme, HJ; Tauberger, G; Thoneick, HU, 1978
)
0.53
" During chronic oral dosing there was no evidence of drug accumulation."( Pharmacokinetic and concentration-effect relationships of clonidine in essential hypertension.
Davies, DS; Dollery, CT; Neill, EA; Reid, JL; Tippett, P; Wing, LM, 1977
)
0.5
" (5--20 microgram/kg) and the dose-response curves for hypotension and bradycardia were parallel, although the onset of effects was more rapid via the vertebral route."( Studies on the cardiovascular depressor actions of ST 91--an analogue of clonidine.
Bentley, GA; McLennan, PL, 1978
)
0.49
" The dosage was kept unchanged or increased according to the antihypertensive response."( The use of clonidine and practolol in the treatment of hypertension.
Ala-Laurila, P; Pitkäjärvi, T; Ruosteenoja, R; Torsti, P, 1976
)
0.65
" Excitatory behavioral effects of CL in low dosage may be connected with stimulation of central adrenergic receptors."( Influence of 6-hydroxydopamine on the behavioral effects induced by apomorphine or clonidine in rats.
Brus, R; Drybański, A; Herman, ZS; Slomińska-Zurek, J; Szkilnik, R, 1976
)
0.48
" Since there appeared to be a correlation between the dose and the duration of adequate blood pressure control, administration of clonidine twice a day with a larger dose at bedtime and a smaller dose before noon could limit unwanted drowsiness and combine the convenience of less frequent dosing with superior blood pressure control."( Efficacy and acceptability of different dosage schedules of clonidine.
Jain, AK; McMahon, FG; Ryan, JR; Vargas, R, 1977
)
0.7
" Both the hypotensive and bradycardic effects were quantified by means of equipotent doses, calculated from dose-response characteristics constructed for each derivative."( Hypotensive and bradycardic activities of clonidine and related imidazolidines; structure-activity relationship.
Timmermans, PB; Van Zwieten, PA, 1977
)
0.52
" The antihypertensive and bradycardic activities of clonidine and a number of its derivatives were quantified by means of ED20 values calculated from dose-response curves following intravenous administration to conscious, spontaneously hypertensive rats."( Central hypotensive and antihypertensive activities of imidazolidines, structurally related to clonidine.
Timmermans, PB; Van Zwieten, PA, 1977
)
0.73
" It is concluded that, for the linear part of the dose-response curves for these compounds, the brain concentration is a measure of the hypotensive effect."( Gas-liquid chromatographic determination of clonidine and some analogues in rat brain tissue. Brain concentrations and hypotensive activity.
Brands, A; Timmermans, PB; Van Zwieten, PA, 1977
)
0.52
" The therapeutic cycles were standardized, for each drug, in the way of administration, dosage and total duration of the treatment."( [Therapeutic possibilities in idiopathic headaches. Analysis of about 1000 cases].
Agostoni, A; Brandi, G; Cottino, A; Gai, V; Gastaldi, L; Lisino, F; Nattero, G, 1976
)
0.26
" Small initial dosage and cautious incrementation is needed to avoid patient resistance from side-effects, principally fatigue, dry mouth and constipation, but once satisfactory control is achieved maintenance therapy is relatively trouble free."( A clinical trial of clonidine (Catapres) in private practice.
Bostock, MI, 1975
)
0.58
") shifted the dose-response curve of clonidine (i."( Site and mode of action of clonidine in the central nervous system.
Karppanen, H; Paakkari, I; Paakkari, P, 1976
)
0.83
"In a doubl-blind study, patients receiving a rapidly falling dosage of clonidine recovered about 1 day faster from the symptoms of moderately severe alcohol withdrawal than patients receiving placebo."( Clonidine in alcohol withdrawal.
Björkqvist, SE, 1975
)
1.93
" For the inhibition of the hypotensive action of clonidine by protriptyline a parallel shift of the dose-response curve was obtained, indicating the possibility of a competitive antagonism."( Interaction between centrally acting hypotensive drugs and tricyclic antidepressants.
van Zwieten, PA, 1975
)
0.51
"05) without affecting exogenously applied acetylcholine dose-response curves."( Role of K+ channels in the modulation of cholinergic neural responses in guinea-pig and human airways.
Barnes, PJ; Belvisi, MG; Miura, M; Stretton, CD; Yacoub, MH, 1992
)
0.28
" A beta 1-pattern was seen in both regions when lipolysis dose-response curves were arranged in order of potency."( Mechanisms for differences in lipolysis between human subcutaneous and omental fat cells.
Arner, P; Hellmér, J; Marcus, C; Sonnenfeld, T, 1992
)
0.28
" The alpha 2-blocking agent yohimbine shifted the dose-response curve of the contractile response to the alpha 2-agonist, clonidine, in a dose-dependent manner, 10(-7) M causing a 10 fold shift."( The contribution of alpha-adrenoceptors to neurally-mediated contractions of the rabbit urethral smooth muscle.
Brading, AF; Chen, HI, 1992
)
0.49
" Both depressor and bradycardia responses to intracisternal clonidine were attenuated after 1 day's dosing but only depressor responses were influenced after 6 days."( Do centrally-acting antihypertensive drugs act at non-adrenergic as well as alpha-2 adrenoceptor sites?
Hamilton, CA; Howie, CA; Reid, JL; Yakubu, MA, 1992
)
0.53
"5 to 60 degrees C resulted in right shifts in the dose-response curves for all agents with the magnitude of shift being: 1) greatest on the blood pressure and least on the tail flick, and 2) greatest for ST-91 and CLON and least for DMET."( Suppression by spinal alpha-2 agonists of motor and autonomic responses evoked by low- and high-intensity thermal stimuli.
Saeki, S; Yaksh, TL, 1992
)
0.28
" Included are the drugs' putative mechanisms of action, pharmacology, toxicology, indications for their use, short-term and long-term actions, adverse effects, specific dosing regimens, therapeutic monitoring techniques, alternative medications, and drug interactions."( Pharmacologic treatment of attention deficit hyperactivity disorder.
Greenhill, LL, 1992
)
0.28
" We therefore compared the dose-response curves of three alpha-2 adrenoceptor agonists, clonidine, UK 14,304 and 2,6-DMC."( Opposite rank order of potency for alpha-2 adrenoceptor agonists on water and solute excretion in the rat: two sites and/or receptors?
Blandford, DE; Li, P; Penner, SB; Smyth, DD, 1992
)
0.51
" Dose-response curves show similar sensitivity, but decreased responsiveness in the lean animal."( Food intake of lean and obese Zucker rats following ventricular infusions of adrenergic agonists.
Bray, GA; Tsujii, S, 1992
)
0.28
" CEC treatment had little effect on the pressor dose-response curve of either phenylephrine or BHT 920."( Effect of chlorethylclonidine on arterial blood pressure and heart rate in the conscious rat.
Piascik, MT; Pruitt, TA; Sparks, MS, 1992
)
0.61
" On the other hand, in monkey lingual arteries, diltiazem failed to depress the NE-induced dose-response curve, and the response was attenuated only about 60% in Ca(2+)-free solution."( Pharmacological properties of alpha 1-adrenoceptor-mediated vasoconstrictions in dog and monkey lingual arteries: evidence for subtypes of alpha 1-adrenoceptors.
Chiba, S; Skrbic, R, 1992
)
0.28
" ALO 2145 1% was shown to be effective and well tolerated in the dosage regimen employed in this study."( [Efficacy and tolerability of apraclonidine (ALO 2145, 1%) in the prevention of early ocular hypertonia, after trabeculoretraction using argon laser and posterior capsulotomy using Nd:YAG laser].
Berrod, JP; Raspiller, A, 1992
)
0.56
" The opioid antagonist naloxone and the alpha-2 adrenergic antagonist idazoxan were given as intrathecal pretreatments at doses chosen to shift the dose-response curves of their corresponding agonist (given alone) 4- to 10-fold to the right; this always resulted in a smaller, but significant (2- to 4-fold) shift in the dose-response curve of the other agonist given alone."( Spinal interactions between opioid and noradrenergic agonists in mice: multiplicativity involves delta and alpha-2 receptors.
Hylden, JK; Kitto, K; Lei, S; Roerig, SC; Wilcox, GL, 1992
)
0.28
" Oral administration of 50 mg carvedilol led to a rightward shift in the dose-response curves of angiotensin II, norepinephrine, and PGF2 alpha."( Constriction of human dorsal hand veins in vivo with several vasoconstrictors and the influence of oral administration of carvedilol.
Beermann, C; Belz, GG; Schloos, J, 1992
)
0.28
" Treatment with captopril was found to attenuate pressor responses produced by the administration of either alpha 1- or alpha 2-adrenoceptor agonists, resulting in the displacement to the right of the agonist dose-response curves and significantly increasing the calculated ED50 values."( The interrelationship between the effects of captopril and nifedipine on pressor responses elicited by selective alpha-adrenoceptor agonists in the pithed rat preparation.
Tabrizchi, R; Triggle, CR, 1992
)
0.28
" Because no obvious differences between dose-response relations of plasma NOR (believed to be a presynaptic and peripheral effect), blood pressure (believed to be mainly a central presynaptic and postsynaptic effect), and subjective sedation (believed to be a central and probably postsynaptic effect) were observed, our results do not provide simple parameters to discern the multiple mechanisms of action of CLO."( Cardiovascular, neuroendocrine, and sedative responses to four graded doses of clonidine in a placebo-controlled study.
Boomsma, F; Kruijk, MP; Man in 't Veld, AJ; Moleman, P; Tulen, JH; van de Wetering, BJ; van Steenis, HG; von Saher, RA, 1992
)
0.51
" Whereas castration failed to shift either dose-response curve, ovariectomy mitigated the gender differences in pilocarpine and clonidine analgesia."( Roles of gender and gonadectomy in pilocarpine and clonidine analgesia in rats.
Bodnar, RJ; Kiefel, JM, 1992
)
0.74
" Further studies are needed in a larger autistic population to determine the dose-response relationship of clonidine."( A double-blind, placebo-controlled study of the efficacy of transdermal clonidine in autism.
Fankhauser, MP; German, ML; Karumanchi, SD; Karumanchi, VC; Yates, A, 1992
)
0.73
" Forty-eight patients achieved diastolic blood pressures less than 90 mm Hg on concomitant therapy; 44 patients completed 8 weeks of maintenance dosing with a mean blood pressure of 134/85 mm Hg."( Transdermal clonidine as an adjunct to enalapril: an evaluation of efficacy and patient compliance.
Cook, E; Dillard, D; Lewin, A; Wallin, JD; Weidler, D, 1992
)
0.66
" Addition of morphine caused a left shift in the dose-response curves of all the non-opioid drugs, indicating at least some degree of additive effects."( Antinociceptive and motor effects of intrathecal morphine combined with intrathecal clonidine, noradrenaline, carbachol or midazolam in rats.
Cmielewski, PL; Cousins, MJ; Gourlay, GK; Owen, H; Plummer, JL, 1992
)
0.51
" Thirty minutes later, alinidine was administered as a bolus dosage of 1 mg/kg in five dogs; the other five dogs served as a control group."( Addition of alinidine, a specific bradycardic agent, to dobutamine in a canine model of endotoxic shock.
Moulart, D; Preiser, JC; Vincent, JL, 1992
)
0.28
" Dose-response curves for intrathecally administered agonists with mu- and/or delta-opioid activity were shifted to the left for inflamed hindpaws when compared to contralateral non-inflamed paws."( Spinal opioid analgesic effects are enhanced in a model of unilateral inflammation/hyperalgesia: possible involvement of noradrenergic mechanisms.
Dubner, R; Hylden, JL; Iadarola, MJ; Nahin, RL; Thomas, DA, 1991
)
0.28
" In control aortic rings the dose-response curves for either clonidine or naphazoline were biphasic, consisting of high- and low-affinity components."( Interaction of imidazolines with alkylation-sensitive and -resistant alpha-1 adrenoceptor subtypes.
Piascik, MT; Pruitt, TA; Sparks, MS, 1991
)
0.52
"1-810 nmol) caused a rightward shift of dose-response curve and reduction of maximal effect of alpha-2 agonists used."( Relative efficacy of spinal alpha-2 agonists, dexmedetomidine, clonidine and ST-91, determined in vivo by using N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible antagonist.
Takano, Y; Yaksh, TL, 1991
)
0.52
" Since the behavioural effects of B-HT 920 vary according to the dosage employed, discussion centres on what receptors might conceivably underly these effects and on their preclinical relevance."( Effects of B-HT 920 in the tail-suspension test.
Cassinadri, M; Ferrari, F; Tampieri, A; Tartoni, PL, 1991
)
0.28
" A higher dosage of clonidine (0."( Effects of alpha-noradrenergic substances on the optokinetic and vestibulo-ocular responses in the rabbit: a study with systemic and intrafloccular injections.
Collewijn, H; Pompeiano, O; Tan, HS; van Neerven, J, 1991
)
0.6
"25 mg kg-1) caused a shift of the clonidine antisecretory dose-response curve to the right, demonstrating tolerance."( Studies to determine whether there is tolerance or cross-tolerance to the antisecretory effect of morphine and clonidine in the rat intestine.
Bentley, GA; Coupar, IM; Margaritis, J, 1991
)
0.77
" The ED50 value for the dose-response curves to B-HT 920 and St587 were found to be significantly increased after the administration of staurosporine."( Effects of staurosporine on the pressor responses to alpha-adrenoceptor agonists in pithed rats: a comparison with nifedipine.
Tabrizchi, R; Triggle, CR, 1991
)
0.28
" Further studies are indicated to determine appropriate dosing regimens for oral labetalol in the acute treatment of severe hypertension."( Oral labetalol versus oral clonidine in the emergency treatment of severe hypertension.
Atkin, SH; Beaty, P; Cuffie, C; Jaker, MA; Quadrel, MA; Soto-Greene, ML, 1992
)
0.58
" This preliminary study suggests that reduction of central noradrenergic activity by clonidine, at least at the dosage levels employed in the current study, only partially attenuates panic response to lactate."( Noradrenergic function in panic disorder. Effects of intravenous clonidine pretreatment on lactate induced panic.
Campeas, RB; Coplan, JD; Davies, SO; Dillon, DJ; Fyer, AJ; Gorman, JM; Klein, DF; Liebowitz, MR; Martinez, J, 1992
)
0.75
" The norepinephrine and hemodynamic responses to graded clonidine dosing (1, 2, and 3 micrograms/kg body weight intravenously) indicated that the sympathetic outflow to the hepatomesenteric circulation was more sensitive to pharmacologic suppression with clonidine than was the sympathetic outflow to the systemic circulation."( Increased sympathetic nervous activity and the effects of its inhibition with clonidine in alcoholic cirrhosis.
Colman, J; Crotty, B; Debinski, H; Dudley, F; Esler, M; Jennings, G; Jones, P; Lambert, G; Willett, I, 1992
)
0.76
" Dose-response curves were constructed for phenylephrine (an alpha 1-adrenergic agonist), ST-91 (an alpha 2-adrenergic agonist), angiotensin II, and arginine vasopressin (AVP)."( Does magnesium sulfate alter the maternal cardiovascular response to vasopressor agents in gravid ewes?
Chatterjee, P; Chestnut, DH; Sipes, SL; Thompson, CS; Vincent, RD; Weiner, CP, 1991
)
0.28
" Alinidine (10(-6) M) shifted the dose-response curves of acetylcholine and carbachol to the right, but it did not affect those for isosorbide dinitrate, isoproterenol and adenosine."( Anti-muscarinic effect of alinidine on acetylcholine-induced vasodilation in isolated and perfused dog coronary arteries.
Chiba, S; Furukawa, Y; Nakane, T, 1991
)
0.28
" Indeed, we observed a strong correlation between patient compliance and the administration of agents with longer dosing intervals and improved side effects profiles."( Improving compliance in an inner-city hypertensive patient population.
Batts, JM; Branche, GC; Dowdy, VM; Field, LS; Francis, CK, 1991
)
0.28
" The principal disadvantages of this class of medications are an overlap between the therapeutic dosage and that producing sedation and dry mouth and the potential to cause the discontinuation syndrome and sexual dysfunction."( Use of centrally acting sympatholytic agents in the management of hypertension.
Epstein, M; Oster, JR, 1991
)
0.28
" The plasma concentration of xylose after oral dosing was used as an indicator of groove activation."( The inhibition of the reticular groove reflex in sheep by clonidine.
Belkhiri, M; Nicholson, T, 1991
)
0.53
" These variables were: age, gender, prior utilization of medical services, regimen complexity, and dosage formulation."( Utility of a transdermal delivery system for antihypertensive therapy. Part 1.
Chin, A; Gill, MA; Okamoto, MP; Sclar, DA; Skaer, TL, 1991
)
0.28
" The enhanced attenuation of responses to noxious colorectal distension produced by the coadministration of these drugs is evidenced by significant leftward shifts in the dose-response curves as compared to those of each drug alone and by isobolographic analysis."( Intrathecal coadministration of clonidine with serotonin receptor agonists produces supra-additive visceral antinociception in the rat.
Danzebrink, RM; Gebhart, GF, 1991
)
0.56
" Compliance with the oral twice-daily regimen was variable, with 83% of patients failing to take diltiazem SR at the prescribed dosing intervals 80% to 100% of the time."( Transdermal clonidine as an adjunct to sustained-release diltiazem in the treatment of mild-to-moderate hypertension.
Herron, J; Lueg, MC; Zellner, S,
)
0.51
" Dose-response curves to bolus doses of norepinephrine were shifted markedly to the right by an alpha-1 selective concentration of prazosin (1 nM) and were shifted to the right with depression of maximum by infusions of clonidine (0."( Antagonism of norepinephrine by clonidine in the isolated rat mesenteric vascular bed.
Fleming, WW; Kong, JQ; Taylor, DA, 1991
)
0.75
" Dose-response curves for IT morphine were obtained in the presence of fixed doses (0."( Interaction of intrathecal morphine and ST-91 on antinociception in the rat: dose-response analysis, antagonism and clearance.
Monasky, MS; Stevens, CW; Yaksh, TL; Zinsmeister, AR, 1990
)
0.28
"1-10 nM) shifted the dose-response curves for norepinephrine and phenylephrine to the right."( Agonist interaction with alkylation-sensitive and -resistant alpha-1 adrenoceptor subtypes.
Butler, BT; Kusiak, JW; Piascik, MT; Pruitt, TA, 1990
)
0.28
"In an attempt to maintain stable levels of an alpha 2-adrenergic agonist throughout the perioperative period, two different oral-transdermal clonidine dosage regimens were administered according to a randomized, double-blind, placebo-controlled study in patients undergoing abdominal surgery."( Clinical efficacy of oral-transdermal clonidine combinations during the perioperative period.
Duncan, SR; Jarvis, DJ; Maze, M; Segal, IS; White, PF, 1991
)
0.75
" The dose-response curve to inhibitory effect of clonidine (CLON) on firing rate of locus coeruleus (LC) neurons showed a clear shift to the right."( Time course effects of uncontrollable stress in locus coeruleus neuronal activity.
Pavcovich, LA; Ramirez, OA, 1991
)
0.54
" Alinidine was administered at a dosage of 30 mg 3 times a day."( Alinidine in chronic stable angina: the effect on diastolic perfusion time.
Cinquegrana, G; Condorelli, M; Duilio, C; Ferro, G; Spadafora, M; Spinelli, L, 1990
)
0.28
" A final study evaluated the dose-response relationship of clonidine-induced erectile dysfunction."( Clonidine suppresses copulatory behavior and erectile reflexes in male rats: lack of effect of naloxone pretreatment.
Clark, JT; Smith, ER, 1990
)
1.97
" Continuous administration of a drug should result in better control of the disease with fewer side effects and a marked increase in patient compliance than when traditional dosage forms are used."( Clinical efficacy of current transdermal drug delivery systems: a retrospective evaluation.
Banakar, U; Berba, J, 1990
)
0.28
" The slope of the dopamine dose-response curve was, however, similar to that of the dose-response curve of clonidine."( Inhibitory effects of clonidine and dopamine on adenylate cyclase of rabbit ciliary processes.
Cepelík, J; Hynie, S, 1990
)
0.81
" Clonidine-related side effects are still evident, but the overall tolerance profile for this reduced dosage of the drug appears to be favorable."( Low-dose clonidine administration in the treatment of mild or moderate essential hypertension: results from a double-blind placebo-controlled study (Clobass). The Clobass Study Group.
, 1990
)
1.61
" Clonidine was administered to 16 subjects at two dosage levels (0."( Lack of effect of clonidine and pentoxifylline in short-term therapy of diabetic peripheral neuropathy.
Chomiak, M; Cohen, KL; Lucibello, FE, 1990
)
1.52
" Graded dose-response curves (DRC) were constructed from tail-flick latencies converted to % maximal possible effect (%MPE), and the ED50 calculated."( Spinal antinociceptive synergy between clonidine and morphine, U69593, and DPDPE: isobolographic analysis.
Green, J; Harris, S; Lloyd, P; Lozito, R; Messineo, E; Ossipov, MH, 1990
)
0.55
" These findings were confirmed and extended here with dose-response curves."( Neonatal clonidine treatment results in long-lasting changes in noradrenaline sensitivity and kindling epileptogenesis.
Bos, NP; Gorter, JA; Huisman, E; Kamphuis, W; Mirmiran, M, 1990
)
0.7
" Chloroethylclonidine (1-5 X 10(-5) M) shifted noradrenaline dose-response curve to the right approximately 5000-fold without depressing the maximum."( Chloroethylclonidine unmasks a non-alpha-adrenoceptor noradrenaline binding site in the rat aorta.
Bevan, JA; Oriowo, MA, 1990
)
1.05
"The objective of the study was to determine dose-response relationships of growth hormone, vasopressin, blood pressure, heart rate, and behavioral responses to clonidine."( Dose-response profiles of plasma growth hormone and vasopressin after clonidine challenge in man.
Allen, D; Brown, GM; Cleghorn, JM; Mazurek, M; Szechtman, B, 1990
)
0.71
" Dose-response curves to a variety of additional adrenoceptor stimulants were constructed with the potency rank order for all agonists being: (-)-epinephrine greater than B-HT 920 = (-)-norepinephrine = clonidine much greater than (-)-phenylephrine much greater than B-HT 933 greater than methoxamine."( Characterization of adrenoceptor subtypes in cat cutaneous vasculature.
Koss, MC, 1990
)
0.47
"The purpose of this open, uncontrolled study in a group of confirmed heroin addicts of both sexes was to determine whether clonidine by itself suppresses opiate withdrawal reactions, its maximal effective dosage range, the time of maximal effect, duration of its effectiveness and the extent of cardiovascular side effects."( Evaluation of clonidine suppression of opiate withdrawal reactions: a multidisciplinary approach.
Beroniade, V; Cuthill, JD; Salvatori, VA; Viguié, F, 1990
)
0.85
"A simple and sensitive method for the determination of clonidine in dosage forms is presented."( Spectrophotometric determination of clonidine in dosage forms using bromocresol green.
Agbaba, G; Panić, L; Zivanov-Stakić, D, 1990
)
0.8
" In concentrations greater than 10(-5) M, ouabain caused a parallel shift to the left of the phenylephrine dose-response curve, indicating potentiation."( Effect of ouabain on the responses to vasoconstrictor agents in isolated perfused rat tail arteries.
Armsworth, SJ; Marwood, JF; Stokes, GS,
)
0.13
"In pithed rats two recently-introduced beta-blockers, nipradilol and arotinolol, as well as labetalol shifted the pressor dose-response curve for phenylephrine to the right."( Alpha-blockade and vasodilatation induced by nipradilol, arotinolol and labetalol in pithed rats.
Chin, WP; Imai, S; Nakagawa, Y; Nakahara, H, 1985
)
0.27
" From dose-response curves, near-maximal intracisternal (i."( Differential blood pressure responses to intracisternal clonidine, alpha-methyldopa, and 6-hydroxydopamine in conscious normotensive and spontaneously hypertensive rats.
de Jong, W; Head, GA,
)
0.38
" Detailed analysis revealed a correlation between the dosage and favorable dynamics of mapping parameters."( Intravenous clonidine treatment in acute myocardial infarction (with comparison to a nitroglycerin-treated and control group).
Lada, W; Zochowski, RJ, 1986
)
0.65
" The dosage of clonidine was progressively increased until a normal blood pressure (mean blood pressure less than or equal to 105 mm Hg) was obtained."( Treatment of hypertensive emergencies: classic and newer approaches.
Bisi, G; Gallini, C; Masotti, G; Neri Serneri, GG; Poggesi, L; Scarti, L; Sciagrà, R, 1986
)
0.62
" Bay K 8644 (10(-8) M) markedly potentiated B-HT-958-mediated vasoconstrictor responses with a leftward shift and an increase in the maximum response of the logarithmic dose-response curve."( Sensitivity of alpha-adrenoceptor agonists to the calcium channel activator, Bay K 8644, in canine saphenous vein.
Eskinder, H; Gross, GJ, 1987
)
0.27
"1 mg/kg) enhanced clonidine-induced hypothermia and hypoactivity, chronic dosing (twice daily for 14 days) with desipramine (10 mg/kg) or rolipram (5 mg/kg) antagonized these behavioural effects."( Effect of long-term rolipram administration on the sensitivity of alpha 2-adrenoceptors in rat brain.
Luscombe, DK; Mustafa, MR; Stolz, JF, 1988
)
0.61
" It has been concluded that clonidine reduces sympathoadrenergic activity, but in a low dosage this effect is obviously restricted to a reduction of arteriolar tone."( Hemodynamic and neurohumoral effects of low-dose clonidine in mild to moderate hypertension.
Rüddel, H; Schmieder, R; Schulte, W; von Eiff, AW, 1987
)
0.82
" Twenty-one patients with concentric LVH (thickness of interventricular septum, IVS, and left posterior wall, LPW, above 11 mm) were given a 2D and M-mode echocardiogram before (pre) and 12 and 24 weeks, respectively, after therapy was initiated (mean oral cl dosage 150 micrograms; nf, 30 mg/day)."( Effects of clonidine and nifedipine on left ventricular hypertrophy and muscle mass in hypertensive patients.
Brückner, S; Kleine, P; Meissner, E; von Bruchhausen, V, 1987
)
0.66
" dose-response curves for the effect of the chronic drug given as a bolus."( Potency of infused spinal antinociceptive agents is inversely related to magnitude of tolerance after continuous infusion.
Stevens, CW; Yaksh, TL, 1989
)
0.28
" Antinociception was determined by observing the response to a clamp applied to the tail (Haffner test) in mice and by the tail-flick test in rats; log dose-response curves for antinociception were generated for morphine, clonidine, and each drug combination."( Antinociceptive interactions between alpha 2-adrenergic and opiate agonists at the spinal level in rodents.
Ossipov, MH; Spaulding, TC; Suarez, LJ, 1989
)
0.46
") caused a parallel shift to the right of the dose-response curve for the inhibitory action of the alpha 2-receptor agonist clonidine on LC neurons."( A metabolite of buspirone increases locus coeruleus activity via alpha 2-receptor blockade.
Engberg, G, 1989
)
0.48
" Dose-response curves were generated for epinephrine, and were then repeated in the presence of either prazosin (alpha 1 antagonist), yohimbine (alpha 2 antagonist) or SK&F-86466 (alpha 2 antagonist)."( An in vivo evaluation of alpha adrenergic receptors in canine prostate.
Chernesky, CE; Chou, TC; Felsen, D; Marion, DN; Somers, WJ; Vaughan, ED, 1989
)
0.28
" The drugs induced dose-dependent contractions in all subjects, and dose-response curves were constructed."( Comparative effects of the alpha-adrenoceptor agonists noradrenaline, phenylephrine and clonidine in the human saphenous vein in vivo and in vitro.
Andersson, KE; Norgren, L; Sjöberg, T; Steen, S, 1989
)
0.5
" The absence of a depression of the maximum of the dose-response curve of ST 587 and the very moderate attenuation of the maximal B-HT 920-induced increase in diastolic blood pressure (BP) confirms the lack of major calcium entry blocking properties of R 56865 for alpha-adrenoceptor-activated calcium channels in vitro."( Interaction between R 56865 and alpha-adrenoceptors in the pithed rat.
Fruh, C; Koch, P; Peters, T; Schneider, J; Wilffert, B; Wilhelm, D,
)
0.13
" Clonidine also produced biphasic effects on blood pressure in conscious rats, with the dose-response function shifted upward and to the left of that observed in anesthetized rats."( Pharmacological characterization of alpha adrenoceptors involved in the antinociceptive and cardiovascular effects of intrathecally administered clonidine.
Brody, MJ; Gebhart, GF; Solomon, RE, 1989
)
1.39
" Cumulative dose-response (i."( Evidence that different regional sympathetic outflows vary in their sensitivity to the sympathoinhibitory actions of putative 5-HT1A and alpha 2-adrenoceptor agonists in anaesthetized cats.
Ramage, AG; Wilkinson, SJ, 1989
)
0.28
" Their dose-response curves showed that they had similar IC50's but the maximum inhibition differed among these agonists."( Inhibition of adenylate cyclase in bovine ciliary process and rabbit iris ciliary body to alpha 2-adrenergic agonists.
Elko, EE; Jin, Y; Tran, T; Yorio, T, 1989
)
0.28
" Plasma tizanidine levels rose within half an hour after dosing and peaked at one hour."( Pharmacodynamics and pharmacokinetics of the oral antispastic agent tizanidine in patients with spinal cord injury.
Baker, H; Desai, P; el Masri, W; Frankel, HL; Luckitt, J; Mathias, CJ, 1989
)
0.28
"00007 mg/kg, intravenously) as a component of multicomponent general anesthesia eliminated hemodynamic and endocrine reactions during major abdominal and thoracic surgery in cancer patients, reducing the dosage of calypsol and fentanyl."( [Klofelin as a component of general anesthesia and a means of postoperative analgesia in cancer surgery].
Dolgopolova, TV; Ignatov, IuD; Osipova, NA; Smolina, TA; Vetsheva, MS; Zaĭtsev, AA,
)
0.13
" The dosage was optimized corresponding to the clinical symptoms."( [Comparative double-blind study of the effectiveness and tolerance of baclofen, tetrazepam and tizanidine in spastic movement disorders of the lower extremities].
Paulig, M; Pellkofer, M, 1989
)
0.28
" Although some patients remained normotensive after discontinuation of step II drugs, a greater proportion returned to elevated BP than when step II dosage was unchanged."( Effects of reduction in drugs or dosage after long-term control of systemic hypertension.
Borreson, RE; Fisher, SG; Freis, ED; Hamburger, R; Mezey, KC; Mukherji, B; Neal, WW; Perry, HM; Taguchi, JT; Thomas, JR, 1989
)
0.28
"Using a sensitive and specific radioimmunoassay the pharmacokinetic disposition of clonidine was determined in hypertensive patients after a single dose and then after 5, 28 and 56 days of chronic dosing with 75 micrograms bd."( Pharmacokinetics and antihypertensive effects of low dose clonidine during chronic therapy.
Anavekar, SN; Conway, EL; Howes, LG; Jarrott, B; Louis, WJ; Syrjanen, M, 1989
)
0.75
" In particular, a 3-bromo-5-isoxazolecarbonyl derivative, selected for further in vivo investigation, was provided with as high antihypertensive action as prazosin in spontaneously hypertensive rats (SHR) coupled to a shallow dose-response curve by oral route."( New isoxazole derivatives provided with antihypertensive activity.
Carenzi, A; Chiarino, D; Napoletano, M; Reggiani, A; Sala, A; Sala, R, 1989
)
0.28
" Moreover, small noncontractile doses of STI in this in vitro preparation produced a fivefold leftward shift in the contraction dose-response curve of norepinephrine (P less than ."( Effects of a human-derived sodium transport inhibitor on in vitro vascular reactivity.
Gonick, HC; Prins, BA; Purdy, RE; Weber, MA; Weiler, E, 1989
)
0.28
"This study examined the effects of the alpha 2-adrenergic agonist clonidine on free-running circadian activity rhythms in rats, using a dosing regimen similar to one previously shown to induce behavioral depression in the swim test."( Effects of chronic clonidine administration and withdrawal on free-running circadian activity rhythms.
Rosenwasser, AM, 1989
)
0.84
" DI and VE shifted dose-response curves for phenylephrine and clonidine to the right with suppression of maximal responses."( Effects of calcium antagonists on alpha-adrenoceptor mediated vasoconstrictions of the canine intermediate auricular artery.
Chiba, S; Ito, T, 1987
)
0.51
" Dose-response curves to alpha-MSH were compared in the presence of different calcium concentrations, and Schild regression plots were constructed."( The role of calcium in MSH stimulated melanosome dispersion.
Lucas, AM; Shuster, S; Thody, AJ,
)
0.13
" The inactivation of a small receptor fraction shifted the dose-response curves for isoprenaline and clonidine to the right but did not alter the maximum effect of the agonists (responsiveness)."( Adrenoceptor occupancy in isolated human fat cells and its relationship with lipolysis rate.
Arner, P; Engfeldt, P; Hellmér, J; Ostman, J; Wennlund, A, 1988
)
0.49
" Clonidine treatment produced a dosage related increase in amplitude of both components similar to that produced by chlordimeform (W."( An alpha 2-adrenergic mode of action of chlordimeform on rat visual function.
Boyes, WK; Moser, VC, 1988
)
1.19
" In both models biphasic dose-response curves were obtained; in a narrow low-dose range (6."( Biphasic effects of clonidine on conflict behavior: involvement of different alpha-adrenoceptors.
Engel, JA; Söderpalm, B, 1988
)
0.6
" The dose-response relationship between renal alpha-2 adrenoceptor stimulation (clonidine) and water and electrolyte excretion was evaluated in anesthetized rats."( Dose selective dissociation of water and solute excretion after renal alpha-2 adrenoceptor stimulation.
Blandford, DE; Smyth, DD, 1988
)
0.5
" The dose-response relationships of the alpha 2- and beta-selective agents clonidine and isoproterenol were not appreciably changed by caloric restriction."( Adrenergic regulation of lipolysis in abdominal adipocytes of obese subjects during caloric restriction: reversal of catecholamine action caused by relief of endogenous inhibition.
Fischer, B; Kather, H; Schlierf, G; Wieland, E; Wirth, A, 1985
)
0.5
" Prior saline infusion reduced the hypertensive response to the two higher doses of clonidine by 65 and 70%, and displaced the slope of the dose-response curve downwards, but mannitol had no such effect."( Sodium chloride-induced partial inhibition in vivo of alpha 2-adrenoceptor agonist function.
Biollaz, B; Biollaz, J; Gavras, H; Gavras, I; Kohlmann, O, 1985
)
0.49
" The loss of the righting reflex induced by clonidine in the chicken was prevented by (+/-) and (+) S9871, as shown by a shift of the dose-response curve to clonidine to the right by both agents; on the contrary, (-) S9871 potentiated the sedation induced by clonidine."( Antagonistic effects of S9871 or (imidazolinyl-2)-2-dihydro 2,3 benzofurane and its stereoisomers on some central and peripheral actions of alpha 2-agonists.
Joly, G; Mouillé, P; Schmitt, H, 1985
)
0.53
" Phentolamine, an alpha-adrenergic antagonist, and inhibitors of cyclooxygenase (ibuprofen, indomethacin, and acetylsalicylic acid) caused a shift to the right of the epinephrine dose-response curve, indicating antagonism of the response to epinephrine."( Interaction of epinephrine with isolated rabbit tracheal epithelial cells.
Liedtke, CM, 1986
)
0.27
" Dose-response studies indicated clonidine was 100 times more potent than norepinephrine or cirazoline at inhibiting N-acetyltransferase activity."( Regulation of chicken pineal arylalkylamine-N-acetyl transferase by postsynaptic alpha 2-adrenergic receptors.
Collin, JP; Voisin, P, 1986
)
0.55
"In the present study, the antinociceptive effects of intrathecal injections of the alpha 2-adrenoceptor agonists clonidine and guanfacine in rats was determined to establish their dose-response curves."( Antinociceptive effects and spinal cord tissue concentrations after intrathecal injection of guanfacine or clonidine into rats.
Archer, T; Freedman, J; Gordh, T; Minor, BG; Post, C, 1987
)
0.7
" dose of morphine, show a dose-dependent rightward shift in hot-plate dose-response curves."( Spinal infusion of opiate and alpha-2 agonists in rats: tolerance and cross-tolerance studies.
Monasky, MS; Stevens, CW; Yaksh, TL, 1988
)
0.27
" The antagonism of both receptor types was reversible since washing of the tissues after incubation with DMPEA brought the agonist dose-response curve back to the control value."( Alpha-adrenoceptor occupancy by N,N-dimethyl-2-bromo-2-phenethylamine hydrobromide (DMPEA) in rat vas deferens.
Brasili, L; Cassinelli, A; Giardinà, D; Gulini, U; Melchiorre, C; Quaglia, W, 1988
)
0.27
" IAP pretreatment also caused a marked upward shift in the dose-response curve of vasopressin (10(-10) to 10(-4) M)-induced cAMP accumulation."( Tonic inhibition of renal response to vasopressin by a pertussis toxin substrate.
Fallet, R; Gong, GD; Jeffries, WB; Pettinger, WA; Van Dreal, P, 1988
)
0.27
" The three dose-response curves were compared by analysis of variance."( Comparative effects of rilmenidine and clonidine on bronchial responses to histamine in asthmatic subjects.
Advenier, C; Dinh Xuan, AT; Lockhart, A; Matran, R; Regnard, J; Vitou, P, 1988
)
0.54
" Cumulative dose-response curves were constructed for 8-OH-DPAT, ipsapirone and clonidine."( Evidence that the putative 5-HT1A receptor agonists, 8-OH-DPAT and ipsapirone, have a central hypotensive action that differs from that of clonidine in anaesthetised cats.
Fozard, JR; Ramage, AG, 1987
)
0.7
" Methods also have been developed to determine the skin irritation potential of a drug substance during the preclinical stages of transdermal dosage form development."( Testing of controlled-release transdermal dosage forms. Product development and clinical trials.
Amkraut, AA; Prevo, ME; Shaw, JE, 1987
)
0.27
" Further studies demonstrated a rightward shift in the dose-response curves for the inhibition by norepinephrine of cyclic AMP accumulation following pretreatment with increasing phenoxybenzamine concentration."( Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve.
Ehrlich, YH; Ellis, J; Lenox, RH; Van Riper, D, 1985
)
0.27
" Depletion of CNS monoamines by more than 95% with reserpine (5 mg/kg) and alpha-methyl-para-tyrosine (2 X 300 mg/kg) failed to alter the dose-response relation to clonidine."( Studies on the mechanism of clonidine-induced mydriasis in the rat.
Gherezghiher, T; Hey, JA; Koss, MC, 1985
)
0.76
" Dose-response studies of the effect of epinephrine on adenosine-deaminase or isoproterenol-stimulated fat-cells demonstrate an inhibitory effect of epinephrine on lipolysis promoted by stimulation of alpha 2-adrenoceptors which occurs before the commonly described beta 1-adrenergic effect which promotes stimulation of lipolysis."( Fat cell adrenoceptors: inter- and intraspecific differences and hormone regulation.
Berlan, M; Carpene, C; Lafontan, M, 1985
)
0.27
" Prazosin caused a parallel shift to the right of the dose-response curve to phenylephrine."( Pre- and postjunctional alpha-adrenoceptors at sympathetic neuroeffector junction in bovine mesenteric lymphatics.
Azuma, T; Ohhashi, T, 1986
)
0.27
" The differences observed in the dose-response curves of adenylate cyclase activity to isoproterenol or noradrenaline were prevented in the presence of clonidine (a alpha 2-agonist) or yohimbine (alpha 2-antagonist) respectively."( Occurrence of alpha 2-adrenergic effects on adenylate cyclase activity and (3H)-clonidine specific binding in brown adipose tissue from foetal rats.
Benito, M; Domínguez, MJ; Elliott, K; Fernández, M, 1986
)
0.7
"1% respectively; the dose-response curve for NE inhibitory action is described."( Quantitative evaluation of alpha- and beta-adrenoceptor modulation of [3H]choline release in guinea pig superior cervical ganglia.
Belluzzi, O; Bonifazzi, C; Perri, V; Travagli, RA, 1987
)
0.27
" In the bronchus, functional evidence for such innervation was shown by the following results: a leftward shift in the noradrenaline inhibitory dose-response curve by the neuronal uptake blocker imipramine; the inhibition of uptake of 3H-L-noradrenaline by the neuronal uptake blockers imipramine, cocaine and phenoxybenzamine; and the induced release of noradrenaline and its metabolites by tyramine and electrical field stimulation using nerve-specific parameters; and selective inhibition of field-stimulated contractions by isoprenaline."( Sympathetic innervation of human tracheal and bronchial smooth muscle.
Davis, C; Kannan, MS, 1987
)
0.27
"We performed a double-masked, cross-over, dose-response study of apraclonidine hydrochloride (formerly known as ALO 2145) in 20 patients with elevated intraocular pressure (IOP)."( Apraclonidine. A one-week dose-response study.
Jampel, HD; Pollack, IP; Quigley, HA; Robin, AL, 1988
)
1.07
" The development of supersensitivity, defined as the leftward parallel shift of the dose-response curves for clonidine administered intrathecally, corresponded to the time course of NE depletion following 6-OHDA treatment on the days tested."( Effect of spinal norepinephrine depletion on descending inhibition of the tail flick reflex from the locus coeruleus and lateral reticular nucleus in the rat.
Gebhart, GF; Janss, AJ; Jones, SL, 1987
)
0.49
"Using a dosing paradigm and an automated behavioral testing procedure designed to maximize potential drug efficacy, we evaluated the ability of clonidine to improve performance of aged monkeys on a trial-specific memory task."( Lack of efficacy of clonidine on memory in aged cebus monkeys.
Bartus, RT; Dean, RL,
)
0.66
" We administered propranolol over a wide dosage range to a different group of animals and found that a high dose (20 mg/kg) increased separation-induced coos while decreasing the activity levels."( Effects of clonidine and propranolol on separation-induced distress in infant rhesus monkeys.
Kalin, NH; Shelton, SE, 1988
)
0.66
" The dosage of tizanidine used ranged from 6 to 18 mg/day."( Modified release tizanidine in the treatment of spasticity.
Chantraine, A; Van Ouwenaller, C,
)
0.13
"32 days, despite lower clonidine dosage and significantly lower diazepam dosage on the second day."( Opioid withdrawal and naltrexone induction in 48-72 hours with minimal drop-out, using a modification of the naltrexone-clonidine technique.
Bailey, C; Brewer, C; Rezae, H, 1988
)
0.79
" Dosage was increased progressively, if tolerated, to a maximum of 24 mg tizanidine or 30 mg diazepam per day at the end of 2 weeks."( A multi-centre, double-blind trial of tizanidine, a new antispastic agent, in spasticity associated with hemiplegia.
Bes, A; Eyssette, M; Pierrot-Deseilligny, E; Rohmer, F; Warter, JM, 1988
)
0.27
" Dosing schedule did not affect the objective ratings; scores from clonidine given twice a day were equivalent to those for three times a day."( Clonidine and Gilles de la Tourette's syndrome: double-blind study using objective rating methods.
Carroll, VS; Como, PG; Goetz, CG; Shannon, KM; Tanner, CM; Wilson, RS, 1987
)
1.95
" Its frequency is influenced by length of treatment, daily dosage and degree of hypertension."( [Hypertensive crisis after withdrawal of clonidine and nadolol. Case report and review of the literature].
Fried, M; Schwander, J, 1987
)
0.54
"The study was undertaken to define a dose-response relationship for clonidine in prolonging canine tetracaine spinal anesthesia."( Dose-response relationship of clonidine in tetracaine spinal anesthesia.
Kehler, CH; Kozody, R; Mensink, FJ; Wade, JG, 1987
)
0.8
" It seems probable that the optimal dose of alinidine was not used in this trial and that the dosage could have been higher."( ST 567 (alinidine) in stable angina: a comparison with metoprolol.
Balakumaran, K; Bokslag, M; Fels, PW; Hugenholtz, PG; Jovanovic, A; Lubsen, J; van Es, GA, 1987
)
0.27
" Dosage was held at the minimum effect amount for those who responded."( Clonidine effect on spasticity: a clinical trial.
Carter, RE; Donovan, WH; Rossi, CD; Wilkerson, MA, 1988
)
1.72
" Yohimbine, but not naloxone, antagonized the antinociceptive effects of clonidine, whereas both yohimbine and naloxone altered the dose-response function for the effects of clonidine on blood pressure."( Intrathecal morphine and clonidine: antinociceptive tolerance and cross-tolerance and effects on blood pressure.
Gebhart, GF; Solomon, RE, 1988
)
0.81
" Neither the maximal clinical dosage of tizanidine (3 mg) nor twice that dosage (6 mg) induced any marked somatic or psychic symptoms compared with the placebo."( Effects of tizanidine in healthy volunteers: double-blind study compared with diazepam and a placebo.
Igarashi, S; Yamamura, H; Yanagita, T, 1988
)
0.27
" The dose-response curves were compared by an analysis of variance."( Effects of clonidine on bronchial responses to histamine in normal and asthmatic subjects.
Advenier, C; Dinh Xuan, AT; Lockhart, A; Mantrand, P; Matran, R; Regnard, J, 1988
)
0.66
") or repeated clonidine dosing (0."( Clonidine effects on disposition of xenobiotics in rats: inhibited elimination of flow-limited but not extraction-limited agents.
Ben-Zvi, Z; Hurwitz, A, 1988
)
2.08
" Dose-response experiments indicate that norepinephrine is approximately 10,000 times more potent on a molar basis than carbachol in stimulating antral gastrin release."( Comparison of adrenergic and cholinergic receptor-mediated stimulation of gastrin release from rat antral fragments.
Harty, RF; Maico, DG; McGuigan, JE,
)
0.13
"5 microM), however, the slope of the dose-response curve for EtOH stimulation of AC activity was biphasic."( Effects of ethanol on adenylate cyclase system in the human platelet.
Ishizawa, H; Ozawa, H; Saito, T; Tabakoff, B; Tsuchiya, F, 1987
)
0.27
" We conclude that administration of alinidine in the dosage used does not lead to a significant deterioration even in patients with strongly impaired left ventricular function."( Acute haemodynamic effects of a specific bradycardic agent in patients with coronary heart disease and impaired left ventricular function.
Kreuzer, H; Wiegand, V, 1987
)
0.27
"There is a debate whether the fall in plasma cortisol concentrations after the early morning dosing of clonidine represents drug effect or normal diurnal variation."( Effect of clonidine on plasma cortisol concentrations.
Ellis, NF; MacGillivray, MH; Voorhess, ML, 1986
)
0.89
" The rate at which dose increases were found necessary to maintain adequate blood pressure control over extended periods reflects a low incidence of tolerance to this new once-a-week dosage form of clonidine, and there has been little evidence of rebound hypertension after discontinuation of TTS treatment."( Efficacy of clonidine as transdermal therapeutic system: the international clinical trial experience.
Bies, C; Cristal, N; Fagan, T; Lowenthal, DT; Paran, E; Saris, S; Sharif, K, 1986
)
0.84
" When this preparation was incubated with morphine for 1 h tolerance developed to the inhibitory effect, since dose-response curves were shifted to the right."( Yohimbine reduces morphine tolerance in guinea-pig ileum.
Alamo, C; Alguacil, LF; Cuenca, E; Santos, C, 1987
)
0.27
" After 12 generations of selective breeding, the high antinociceptive response line exhibited about 7 times steeper dose-response curve than did the low antinociceptive response line whereas only small differences were seen with saline alone."( Selective breeding for levorphanol-induced antinociception on the hot-plate assay: commonalities in mechanism of action with morphine, pentazocine, ethylketocyclazocine, U-50488H and clonidine in mice.
Belknap, JK; Danielson, PW; Laursen, SE; Noordewier, B, 1987
)
0.46
" Chronic dosing with morphine or clonidine caused partial tolerance and cross-tolerance to the rise in hepatic BSP caused by an acute challenge with either agonist."( Tolerance to effects of clonidine and morphine on sulfobromophthalein disposition in mice.
Ben-Zvi, Z; Graham, CE; Hurwitz, A, 1987
)
0.86
" These patients are best managed as outpatients with gradual dosage reduction over 4-12 weeks."( Management of benzodiazepine dependence.
Lader, M; Moodley, P, 1986
)
0.27
" In cats, dose-response curves were constructed to noradrenaline and adrenaline given into the perfusion circuit (i."( The effect of clonidine on venous haemodynamics in cats and dogs.
Bentley, GA; Cullen, LK; Reynoldson, JA; Widdop, RE, 1986
)
0.63
" Pretreatment of anaesthetized rabbits with intracisternal CDS (500 units) shifted to the right the dose-response curve obtained with clonidine alone injected the same way."( An endogenous, non-catecholamine clonidine antagonist increases mean arterial blood pressure.
Atlas, D; Bousquet, P; Feldman, J, 1986
)
0.76
" Our data suggest that NIC in the dosage applied shows no clear and pronounced alpha-2-adrenolytic effects and no specific clinical benefits for chronic schizophrenics."( Clinical and biochemical effects of nicergoline in chronic schizophrenic patients.
Ackenheil, M; Albus, M; Botschev, C; Müller-Spahn, F; Münch, U; Naber, D, 1986
)
0.27
" The slope of the dose-response curves was similar in both strains of rat, but the average response to the same concentrations of clonidine was less in the SHR."( Modification of clonidine-induced pressor responses in morphine-dependent and hypophysectomised rats.
Conway, EL, 1986
)
0.82
" When dose-response curves to an alpha adrenergic agonist were obtained in the presence of a threshold concentration of the same or another alpha agonist, the curve was shifted to the left at threshold but converged with the control curve between ED10 and ED70."( Vasoconstrictor threshold synergism and potentiation in the rabbit isolated thoracic aorta.
Murray, DL; Purdy, RE; Stupecky, GL, 1986
)
0.27
" After 2 control runs which had induced regional contractile dysfunction of comparable intensity, alinidine was infused intravenously at a dosage of 1 mg/kg per 5 min."( Effects of alinidine on exercise-induced regional contractile dysfunction in dogs.
Krumpl, G; Mayer, N; Raberger, G; Schneider, W, 1986
)
0.27
" The dose-response curves for noradrenaline, acetylcholine and KCl was not affected by GTX II (2 X 10(-7) to 10(-6) M)."( Presynaptic inhibitory effect of geographutoxin II, a new peptide toxin from Conus geographus venom, in the guinea-pig vas deferens.
Kobayashi, J; Nakamura, H; Ohizumi, Y, 1986
)
0.27
" The similar dose-response relationships for adrenal nerve tone or reflex response in CNS intact and spinalized animals suggest, although not conclusively, that at least some of clonidine's effect in CNS intact animals may be mediated at the spinal level."( The effect of clonidine on adrenal sympathetic nerve responses to mechanical, noxious and innocuous stimulation of the skin in rats.
Kurosawa, M; Minami, M; Saito, H; Togashi, H, 1985
)
0.82
" alpha-Methyldopa and clonidine produced the same hypotensive response at 6 and 8 h after dosing with a similar fall in plasma noradrenaline levels at these times."( The plasma noradrenaline and growth hormone response to alpha-methyldopa and clonidine in hypertensive subjects.
Adams, EF; Brown, MJ; Dollery, CT; Struthers, AD, 1985
)
0.81
" Incorporating combinations of sustained release and immediate release cores into a capsule (Perlonget) gave predictable absorption rates, permitting the formulation scientist to control the plasma levels obtained from oral dosing of clonidine."( Pharmacokinetics of oral sustained release clonidine in humans.
Keirns, JJ; MacGregor, TR; Relihan, GL, 1985
)
0.72
" Independent groups of pups from dams given either 6% or 25% casein diets received one of five doses of clonidine at 5, 10, 15, 20 or 25 days of age and dose-response relationships for motor activity were determined."( Altered development of responsiveness to clonidine in severely malnourished rats.
Goodlett, CR; Morgane, PJ; Resnick, O; Valentino, ML, 1985
)
0.75
" In general, however, no consistent evidence for the development of tolerance or dependence to clonidine were observed under these dosing conditions."( The effects of acute and repeated clonidine administration on fixed-interval performance in rhesus monkeys.
Balster, RL; Wessinger, WD, 1985
)
0.77
" This same dosage and treatment schedule also resulted in a reduction in locomotor activity, but only on the initial day of dosing."( Clonidine-induced alterations in feeding in deprived rats.
Wilson, MC, 1985
)
1.71
" Dose-response curves were constructed correlating decreases in renal blood flow with doses of phenylephrine, clonidine, and guanabenz injected as boluses into renal arteries of anesthetized dogs."( Renal alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in dogs: comparison of phenylephrine, clonidine, and guanabenz.
Buckalew, VM; Strandhoy, JW; Wolff, DW, 1984
)
0.69
" Where pA2 values (-log dose antagonist evoking a twofold shift for the agonist dose-response curve) could be calculated, no significantly different pA2 values against either agonist resulted."( Calcium influx-dependent and -independent alpha 1-adrenoceptor-mediated processes of vasoconstriction in vivo do not operate via different alpha 1-adrenoceptor subtypes.
de Jonge, A; Korstanje, C; Thoolen, MJ; Timmermans, PB; van Zwieten, PA; Wilffert, B,
)
0.13
" The presynaptic alpha-adrenoceptor antagonist activity of the drugs was quantitatively determined by studying the effect of increasing concentrations on the clonidine dose-response curve in the electrically stimulated vas deferens."( Effects of raubasine stereoisomers on pre- and postsynaptic alpha-adrenoceptors in the rat vas deferens.
Demichel, P; Roquebert, J, 1984
)
0.46
" Then prazosin or yohimbine were administered intra-arterially and dose-response curves repeated."( Renal alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in dogs.
Buckalew, VM; Strandhoy, JW; Wolff, DW, 1984
)
0.27
" Since the alpha-adrenoceptor blocking drugs which, at the usual dosage level, antagonize the hypotensive action of clonidine are unknown in man, caution should be exercised for such an association clonidine-alpha-blocker."( [Interaction between clonidine and alpha-blockers (author's transl)].
Chelly, J; Huchet, AM; Schmitt, H, 1980
)
0.79
" The first ionization energies of the pharmacologically active 20-(phenylimino)imidazolidines do not correlate with hypotensive activity based on dosage data after intravenous administration to rats."( Ultraviolet photoelectron spectroscopy of cyclic amidines. 2. Electronic structure of clonidine and some related 2-(phenylimino)imidazolidines with alpha-adrenergic activity.
de Jong, AP; van Dam, H, 1980
)
0.48
"Sixty postmenopausal women with climacteric symptoms were treated with either clonidine hydrochloride or piperazine estrone sulfate in two different dosage strengths."( Effect of estrogen on fasting serum cholesterol and triglyceride levels in postmenopausal women.
Varma, TR,
)
0.36
" Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effect of increasing concentrations of the antagonists on cumulative clonidine dose-response curves on the stimulated vas deferens."( [Comparative study of the pre and post-synaptic alpha blocking activity of thymoxamine and its metabolites in the rat vas deferens (author's transl)].
Canellas, J; Demichel, P; Malek, A; Roquebert, J,
)
0.33
" Clonidine followed by prazosin was added to their regimen on an outpatient basis to establish the dose-response for BP and catecholamines."( Clonidine and prazosin effects in hypernoradrenergic vasodilator-treated and beta-blocker-treated patients.
Mitchell, HC; Pettinger, WA, 1981
)
2.62
" 3 Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effect of increasing antagonist concentrations on cumulative clonidine dose-response curves on the stimulated vas deferens."( Pre- and postsynaptic alpha-adrenoceptor blocking activity of raubasine in the rat vas deferens.
Demichel, P; Gomond, P; Roquebert, J, 1981
)
0.46
" The order of affinity (pA2) for presynaptic alpha-receptors, as assessed from parallel shift of the dose-response curve to clonidine, was: phentolamine greater than yohimbine greater than tolazoline greater than E-643 greater than or equal to prazosin."( Comparison of pre- and postsynaptic alpha-adrenoceptor blocking effects of E-643 in the isolated vas deferens of the rat.
Shoji, T, 1981
)
0.47
" The dose-response curve to guanfacine for increase in blood pressure was shifted in a parallel fashion to the right by 1 mg/kg of yohimbine, an alpha 2-antagonist and by 1 mg/kg of phentolamine, a nonselective alpha 1- and alpha 2-antagonist."( [Effects of guanfacine on pre- and postsynaptic alpha-adrenoceptors studied in comparison with those of clonidine].
Chin, W; Imai, S; Nakagawa, Y, 1982
)
0.48
"3 alpha-Adrenoceptors appear to be involved in the reaction, since noradrenaline showed stereospecificity, and the alpha-adrenoceptor antagonists phentolamine and piperoxan both shifted the dose-response curves of the alpha-adrenoceptor agonist drugs to the right, usually parallel to the control curves."( Studies on the antinociceptive action of alpha-agonist drugs and their interactions with opioid mechanisms.
Bentley, GA; Newton, SH; Starr, J, 1983
)
0.27
"0 mg/kg) resulted in a 3-10-fold shift to the right in the clonidine dose-response curve."( Effects of clonidine on operant behavior and electric shock titration in the squirrel monkey: effects of alpha 2-adrenoreceptor antagonism.
McKearney, JW, 1983
)
0.9
" In contrast, the dose-response curves to tiamenidine and clonidine were flatter and bell-shaped with maxima of 30 and 60 min, respectively."( Sleeping times evoked by alpha adrenoceptor agonists in two-day-old chicks: an experimental model to evaluate full and partial agonists at central alpha-2 adrenoceptors.
Cavero, I; Doxey, JC; Roach, AG; Strachan, DA, 1983
)
0.51
" These alpha 2-agonists also inhibited the uptake of 45Ca evoked by carbachol with similar dose-response curve to inhibition of catecholamine secretion."( Inhibition by alpha 2-adrenoceptor agonists of the secretion of catecholamines from isolated adrenal medullary cells.
Izumi, F; Kobayashi, H; Sakurai, S; Wada, A; Yanagihara, N, 1983
)
0.27
" The dose-response relationships for the effects of alpha 2-adrenoceptor antagonists on retinal TH activity were similar to those for the effects on brain noradrenergic neurons, where alpha 2-adrenoceptors have been shown to be involved in the autoregulation of neuronal activity."( Alpha 2-adrenergic receptors influence tyrosine hydroxylase activity in retinal dopamine neurons.
Iuvone, PM; Rauch, AL, 1983
)
0.27
" Neuroleptic medications are still the mainstay of treatment, but recent studies suggest new approaches to dosage and to the treatment of acute psychosis."( The pharmacologic treatment of schizophrenia: a progress report.
Baldessarini, RJ; Donaldson, SR; Gelenberg, AJ, 1983
)
0.27
" In all these data indicate that in the dog: 1) CLON induces GH release via activation of alpha 2-adrenergic receptors; 2) these receptors are likely located on presynaptic sites [experiments with reserpine (1), DU-18288, mianserin, dose-response curve with CLON 2-32/micrograms/kg iv]; 3) the adrenergic receptors involved in GH release exhibit supersensitivity upon (YOH-induced) chronic pharmacologic denervation."( Presynaptic alpha 2 -adrenergic stimulation leads to growth hormone release in the dog.
Cella, SG; Mantegazza, P; Morgese, M; Müller, EE; Picotti, GB, 1984
)
0.27
" Rauwolscine, RX 781094 and RS 21361 caused rightward parallel displacements of the log dose-response curve to the increase in diastolic pressure of methoxamine (alpha-1 agonist) and B-HT 920 (alpha-2 agonist) as well as to the B-HT 920-induced reduction in stimulation-evoked tachycardia."( A study of the selectivity and potency of rauwolscine, RX 781094 and RS 21361 as antagonists of alpha-1 and alpha-2 adrenoceptors.
Qian, JQ; Ruffolo, RR; Timmermans, PB; van Zwieten, PA, 1984
)
0.27
" Prazosin (10(-8) M-10(-6) M, alpha 1-adrenoceptor antagonist) produced a rightward shift of the phenylephrine and clonidine dose-response curve in both the trigone and urethra."( Alpha 1- and alpha 2-adrenoceptors in the smooth muscle of isolated rabbit urinary bladder and urethra.
Satake, N; Shibata, S; Ueda, S, 1984
)
0.48
" The effects of CU 32-085 and bromocriptine on dose-response curves to sympathomimetic agents (adrenaline, noradrenaline, methoxamine and clonidine), intravenously administered, were also studied."( Hypotensive action and alpha-adrenolytic properties of a new dopaminergic agonist, CU 32-085, in the rat.
Esplugues, J; Morales-Olivas, FJ; Palop, V; Rubio, E, 1984
)
0.47
" A dosage of 100mg twice daily will often be adequate to control mild hypertension and the use of even lower doses has been reported."( Combined alpha- and beta-receptor inhibition in the treatment of hypertension.
Prichard, BN, 1984
)
0.27
" Clonidine also decreased the slope of the ACh dose-response curve and maximal response in denervated mouse diaphragms as well as the carbachol response in the chinck muscle."( Effect of clonidine on neuromuscular transmission and the nicotinic acetylcholine receptor.
Chang, CC; Chiou, LC, 1984
)
1.58
" During chronic oral dosing (3--21 days), tolerance developed and blood pressure returned to base-line pretreatment levels."( Changes in alpha-adrenoceptors during long-term treatment of rabbits with prazosin.
Hamilton, CA; Reid, JL,
)
0.13
" Systolic and diastolic blood pressures and heart rates were assessed for time course, magnitude of change, time-to-peak change, and duration of effect at each dosage level."( Hemodynamic effects of intravenous clonidine in the conscious, normotensive baboon.
Harris, AH; Lukas, SE; Turkkan, JS,
)
0.41
"5 In rats with a sustained tachycardia (100 beats/min produced by electrical stimulation of the spinal cord) both mianserin and phentolamine, in contrast to desipramine, shifted the clonidine heart rate dose-response curve to the right."( Comparison of mianserin with desipramine, maprotiline and phentolamine on cardiac presynaptic and vascular postsynaptic alpha-adrenoceptors and noradrenaline reuptake in pithed normotensive rats.
Cavero, I; Gomeni, R; Lefèvre-Borg, F; Roach, AG, 1980
)
0.45
" Hypotensive potency after intravenous administration to anesthetized, normotensive rats was determined as a measure of central alpha-adrenergic activity and expressed as pC25, obtained from log dose-response curves."( Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
de Jonge, A; Lam, E; Slothorst-Grisdijk, FP; Timmermans, PB; van Meel, JC; van Zwieten, PA, 1981
)
0.26
" There was a shift to the left in pressor dose-response curves to the alpha 1-adrenoreceptor agonist phenylephrine and the mixed alpha 1/alpha 2-adrenoreceptor agonist noradrenaline in 6-hydroxydopamine-pretreated animals."( The effects of intravenous 6-hydroxydopamine on peripheral alpha-adrenoreceptors.
Hamilton, CA; Reid, JL, 1982
)
0.26
" A careful analysis of the dose-response curve showed, however, that the net effect recorded involved the sum of responses from at least two functional systems or receptor sites."( Separate noradrenergic receptors could mediate clonidine-induced antinociception.
Paalzow, GH; Paalzow, LK, 1982
)
0.52
" In the presence of YOH, the ISO dose-response curve therefore completely disappears."( Lipolysis in rat adipose tissue in vitro and its alpha 2 adrenergic control.
Horný, I; Kadrabová, M; Mühlbachová, E; Zámostný, V, 1983
)
0.27
" Higher concentrations of yohimbine (above 2 microM) and phentolamine (above 20 microM) failed to produce a further shift in the dose-response curves of these agonists."( Pharmacological evidence for high affinity and low affinity a2-adrenoceptor binding sites in rat vas deferens.
Mottram, DR, 1983
)
0.27
" Furthermore, the dose-response curves for ACTH and forskolin were clearly shifted to the left in adipocytes from toxin-treated hamsters as compared to control adipocytes."( Effect of pertussis toxin on the hormonal regulation of cyclic AMP levels in hamster fat cells.
García-Sáinz, JA; Martínez-Olmedo, MA, 1983
)
0.27
" Preincubation of rat aortic strips with both derivatives produced non-parallel rightward shifts in the dose-response curves of noradrenaline and significantly depressed the maximum response in a manner characteristic of irreversible receptor antagonists."( Study of two alkylating derivatives: the p-isothiocyanato- and the p-methylisothiocyanato-clonidine.
Decker, N; Leclerc, G; Quennedey, MC; Rouot, B; Schwartz, J, 1983
)
0.49
" Prazosin caused a parallel shift to the right of the dose-response curve to phenylephrine, and not to clonidine in the vessels."( [Characteristics of alpha adrenoceptors of lymphatics and their physiological significance].
Azuma, T; Ohhashi, T, 1983
)
0.48
" All three alpha antagonists employed produced in innervated glands parallel displacements of the dose-response curves to norepinephrine, prazosin being 30 and 100 times more potent than phentolamine and yohimbine, respectively."( Alpha-1 adrenoceptors mediate secretory responses to norepinephrine in innervated and denervated rat submaxillary glands.
Elverdin, JC; Luchelli-Fortis, MA; Perec, CJ; Stefano, FJ, 1984
)
0.27
" ED50 values and dissociation constants for norepinephrine (NE), epinephrine (EPI), isoproterenol (ISO), methoxamine (MET) and clonidine (CLO) were determined by analysis of dose-response data with and without partial inactivation of alpha receptors by phenoxybenzamine."( Characterization of the alpha adrenergic receptor properties of rabbit ear artery and thoracic aorta.
Purdy, RE; Stupecky, GL, 1984
)
0.47
" In rat mesenteric artery, the pA2 value for yohimbine against clonidine was not statistically different from values obtained with the other agonists; however, in the presence of prazosin the dose-response curve to clonidine was biphasic, suggesting that the action of clonidine is mediated through two distinct sites to which prazosin has different affinities."( Pharmacological characterization of the postsynaptic alpha adrenoceptors in vascular smooth muscle from canine and rat mesenteric vascular beds.
Agrawal, DK; Daniel, EE; Triggle, CR, 1984
)
0.51
") evoked dose-dependent shifts to the right of the dose-response curves to B-HT 933 whilst having minimal effects on the methoxamine dose-response curve."( An investigation into the selectivity of a novel series of benzoquinolizines for alpha 2-adrenoceptors in vivo.
Paciorek, PM; Pierce, V; Shepperson, NB; Waterfall, JF, 1984
)
0.27
" Sedation occurred within one hour of dosage and was maximum in the second hour."( Clonidine lowers blood pressure independently of renin suppression in patients with unilateral renal artery stenosis.
Lewis, PS; Mathias, CJ; Peart, WS; Sever, PS; Snell, ME; Wilkinson, A, 1983
)
1.71
" Full PH dose-response curves for standard antihypertensive drugs were explored and were compared to their hypotensive dose-response curves."( Antihypertensive drugs: their postural hypotensive effect and their blood pressure lowering activity in conscious normotensive rats.
Carver, LA; Lee, CH; Strosberg, AM, 1983
)
0.27
" dosing schedules of clonidine on blood pressure, side-effects and plasma concentration of clonidine were studied in a randomized cross-over study."( Clonidine twice daily in hypertension. Effects of two dosage regimens on blood pressure, side-effects and plasma clonidine concentrations.
Huikuri, H; Jounela, AJ; Juustila, HJ; Lilja, M; Paalzow, G, 1983
)
2.03
"We measured the first dosage effect and the long-term effect of lofexidine on blood pressure, heart rate, plasma catecholamines, and their major metabolites in 16 patients with primary hypertension who were receiving 50 mg hydrochlorothiazide twice a day while they were recumbent and upright and during isometric handgrip contraction."( Hemodynamic effect of lofexidine with a diuretic in hypertension.
Alexander, N; Maronde, RF; Velasquez, M; Vlachakis, ND, 1983
)
0.27
" Depot forms of clonidine appear to offer the advantages of once-daily dosing and fewer side effects than standard clonidine preparations."( Comparison of sustained-release and standard preparations of clonidine in essential hypertension.
Fyhrquist, F, 1983
)
0.85
" The ratio of maximum to minimum plasma levels during a dosing interval was 2 for oral Catapres and approximately 1 for Catapres -TTS."( Pharmacokinetics of nitroglycerin and clonidine delivered by the transdermal route.
Shaw, JE, 1984
)
0.54
" For both tissue regions fasting induced a right-ward shift in the dose-response curve for the inhibitory effect of the alpha 2 agonist, clonidine, on theophylline-induced lipolysis, corresponding to a 10-fold decrease in sensitivity."( Influence of fasting on lipolytic response to adrenergic agonists and on adrenergic receptors in subcutaneous adipocytes.
Arner, P; Engfeldt, P; Kimura, H; Ostman, J; Wahrenberg, H, 1984
)
0.47
" Detailed analysis revealed undoubted correlation between the dosage and favourable dynamics of precordial mapping parameters."( Intravenous clonidine in acute myocardial infarction in men.
Lada, W; Zochowski, RJ, 1984
)
0.65
" The beta 1,2 antagonist employed in the test decreased the contrast dosage by 13 per cent, causing the LD50."( Diazepam, alpha and beta neurotransmission modifying drugs and contrast media mortality in mice.
Johansson, G; Luostarinen, M; Virkkunen, P, 1984
)
0.27
" Compound 9d, which lowered arterial blood pressure 37 mmHg in SHR when dosed at 100 mg/kg, was further evaluated in chronic hypertensive dogs because of apparent minimal CNS effects."( N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
Chan, PS; Emma, JE; Meyer, WE; Tomcufcik, AS, 1984
)
0.27
" The dosage of clonidine was progressively increased until a normal BP (mean BP less than or equal to 105 mmHg) was obtained."( Changes in cardiac function after effective treatment of hypertensive emergencies with i.v. clonidine.
Bisi, G; Gallini, C; Masotti, G; Neri Serneri, GG; Poggesi, L; Scarti, L, 1984
)
0.84
" The extent of the activation seems to depend on the dosage of clonidine."( [Activation of the kallikrein-kinin system by clonidine].
Hinkel, GK; Kühne, H; Lehmann, B; Scheuch, DW; Schlagehan, IM, 1984
)
0.77
" No toxic side effects of clonidine were observed at the dosage level used."( Clonidine treatment of neonatal narcotic abstinence syndrome.
Caruso, KA; Cohen, DJ; Ehrenkranz, RA; Hoder, EL; Kleber, HD; Leckman, JF; Poulsen, J, 1984
)
2.01
" Relief of spasticity, from the dosage used, was relatively slight and appeared greatest at the time of peak plasma levels of the drug."( Tizanidine--initial pharmacokinetic studies in patients with spasticity.
Eadie, MJ; Heazlewood, V; Maruff, P; Symoniw, P, 1983
)
0.27
" These results suggest that similar to clonidine, a high dosage of tizanidine influences gastric acid secretion and gastric ulcers, although the activity is lower than that of clonidine."( [Influence of a muscle relaxant, tizanidine, on gastric acid secretion and gastric ulcer in rats].
Kanaoka, R; Maeda-Hagiwara, M; Watanabe, H; Watanabe, K, 1983
)
0.54
" The slopes of the individual dose-response curves were not significantly different which suggested a common mechanism of action."( Central and peripheral anti-inflammatory actions by clonidine and a structurally related imidazoline analog.
Holsapple, MP; Lowy, MT; Malave, A; Yim, GK, 1984
)
0.52
" When a steady state concentration in plasma was reached at each dose level, the blood pressure (BP) and heart rate were measured during a dosage interval."( Relationship between the cardiovascular effects and steady-state kinetics of clonidine in hypertension. Demonstration of a therapeutic window in man.
Frisk-Holmberg, M; Paalzow, L; Wibell, L, 1984
)
0.5
" Prior to study, 2 hours post dosing and coincident with immediate pre-exercise on treadmill, at graded increases of exercise and 2 hours post exercise (approximately 4 hours post dosing), blood was sampled for potassium, renin concentration, aldosterone and catecholamines."( Potassium disposition and neuroendocrine effects of propranolol, methyldopa and clonidine during dynamic exercise.
Affrime, MB; Falkner, B; Hakki, H; Lowenthal, DT; Rosenthal, L; Saris, S, 1982
)
0.49
" We administered both drugs to rats using a dosage schedule which we had shown to produce hypertension and tachycardia when clonidine, but not guanfacine, was stopped after 3 weeks treatment."( Studies on clonidine and guanfacine withdrawal after short term treatment in the rat.
Barber, ND; Reid, JL, 1982
)
0.86
" Long-acting propranolol in a once daily dosage of 160 mg proved to be effective over a 6-week period of treatment with no significant side-effects."( Comparison of sustained-release clonidine and long-acting propranolol in the treatment of hypertension.
Lawson, AA; Rodrigues, E, 1982
)
0.55
" The vasodepressor effect of guanfacine was clearly dose-dependent, and was more marked when the initial level of the blood pressure was high, while that of clonidine was dose-dependent, only within a limited dosage range."( [Antihypertensive effect of guanfacine in rats].
Hamamura, M; Hashimoto, T; Imai, S; Kumada, M; Mitomi, A; Nakagawa, Y; Sakurai, H; Takeda, K, 1981
)
0.46
" Dosage regimens of clonidine must be individualized according to symptoms and side effects and closely supervised because of varying sensitivity to clonidine's sedative, hypotensive, and withdrawal-suppressing effects."( Clonidine in opiate withdrawal: review and appraisal of clinical findings.
Resnick, RB; Washton, AM,
)
1.9
"0 mg/kg) shifted the clonidine dose-response curves to the right, suggesting competitive antagonism."( An analysis of the effects of systemically administered clonidine on the food and water intake of rats.
Sanger, DJ, 1983
)
0.83
"3 mg/kg) or prazosin in high dosage (0."( Bronchopulmonary effects of clonidine on the bronchomotor responses of the guinea-pig.
Advenier, C; Floch, A; Mallard, B, 1983
)
0.56
" In toddlers poisoning is seen after ingestion of a single tablet of 150 micrograms clonidine, whilst in adults poisoning may occur already at a dosage just exceeding the therapeutic limit, which is subject to wide individual variation (1 to 3 tablets)."( [Poisoning with clonidin hydrochloride in children and adults].
Gössinger, H; Haubenstock, A; Hruby, K; Jung, M; Pfister, R, 1983
)
0.49
" Dose-response alteration of VI responding by apomorphine, d-amphetamine, clonidine, and chlordiazepoxide was studied along and in the presence of a dose of acrylamide which, by itself, did not alter VI responding."( The effects of acrylamide on the behavioral suppression produced by psychoactive agents.
Squibb, RE; Tilson, HA, 1982
)
0.5
" In terms of lofexidine, there was no evidence of any adverse interactions with hydrochlorothiazide either following a single, oral administration to rats and mice or following short-term and long-term repeated oral dosing of rats and dogs."( Toxicology of the combination lofexidine/hydrochlorothiazide.
Fontaine, R; Friehe, H; Gibson, JP; Larson, EJ; Sells, DM, 1982
)
0.26
" A dose-response relationship could only be observed in vigilosomnograms, in the tests of self-estimation related to well-being and mood and in the decrease in plasma noradrenaline in the clonidine group."( Differences in psychic performance with guanfacine and clonidine in normotensive subjects.
Brecht, HM; Krauskopf, R; Kugler, J; Raschig, A; Seus, R, 1980
)
0.7
" The daily dosage of propranolol and clonidine was 160 mg and 100 microgram, respectively."( Propranolol (Inderal) and clonidine (Catapressan) in the prophylactic treatment of migraine. A comparative trial.
Kåss, B; Nestvold, K, 1980
)
0.83
" During the following time blood pressure and dosage remained almost unchanged."( [A new antihypertensive agent used in a clinical setting].
Kaiser, HJ; Raschig, A; Wetzels, E, 1980
)
0.26
" The study consisted of 4 parts: I, double-blind cross-over trial at maximal dosage 10 mg/day in 13 patients; II, open trial at maximal dosage 32 mg/day in 10 patients; III, long-term medication at dosage 32 mg/day for 6-15 months in 4 patients; IV, single dose (12 mg) administration in 3 patients."( Antiparetic and antispastic effects induced by tizanidine in patients with spastic paresis.
Gransberg, L; Knutsson, E; Mårtensson, A, 1982
)
0.26
" Before treatment and at the end of each treatment period the patients were hospitalized and their plasma clonidine concentrations (P-CLON) were determined repeatedly during one dosage interval."( Plasma clonidine in relation to blood pressure, catecholamines, and renin activity during long-term treatment of hypertension.
Hökfelt, B; Manhem, P; Paalzow, L, 1982
)
0.93
"1-mg bid doses of C to six normal subjects at rest, 2 hr after dosing and immediately before dynamic physical activity (DPA) on a treadmill, and at peak activity and 2 hr after DPA."( Dynamic and biochemical responses to single and repeated doses of clonidine during dynamic physical activity.
Affrime, MB; Borruso, J; Falkner, B; Gould, AB; Lowenthal, DT; Rosenthal, L, 1982
)
0.5
" Clonidine in the stated dosage had no significant effect on blood pressure and heart rate."( [Treatment of menopausal symptoms with low doses of clonidine (author's transl)].
Lauritzen, C, 1982
)
1.43
"The dose-response effects of clonidine HCl (2."( Differential sensitivity of four central sympathetic pathways to depression by clonidine.
Franz, DN; Madsen, PW, 1982
)
0.78
" Under controlled inpatient conditions established to assess dosage guidelines and to examine specific signs and symptoms of withdrawal, ten (91%) of 11 patients were able to withdraw completely from methadone therapy by the end of a six-day period."( Clonidine and naltrexone. A safe, effective, and rapid treatment of abrupt withdrawal from methadone therapy.
Braverman, P; Charney, DS; Heninger, GR; Kleber, HD; Murburg, M; Redmond, DE; Riordan, CE; Sternberg, DE, 1982
)
1.71
"The effectiveness of clonidine in suppressing the occurrence of postmenopausal hot flashes was examined using a dose-response study design and objective recordings of hot flashes."( Effect of clonidine on hot flashes in postmenopausal women.
Erlik, Y; Judd, HL; Laufer, LR; Meldrum, DR, 1982
)
0.99
" Clonidine, at a low dosage (100 micrograms/kg sc), potentiated the increase in urine flow induced by water overloading but remained ineffective in alcohol--loaded rats (fig."( [Effect of clonidine on polyuria induced by alcohol, water or the lack of vasopressin in the rat].
Guiol, C; Montastruc, JL,
)
1.43
" The effects of the withdrawal of clonidine and 6-(2-chloro-6-fluoro-phenyl)-2,3,6,7-tetrahydro-5H-pyrrolo-(1,2-a)-imidazole hydrobromide (ICI 106270) on the blood pressure and heart rate of chronically dosed beagle dogs has been investigated."( The withdrawal of centrally acting antihypertensives in dogs.
Clough, DP; Keddie, J; Pettinger, SJ, 1981
)
0.54
" The dose-response curve for the LC inhibitory effect of the alpha 2-receptor agonist clonidine was shifted in parallel to the right by pretreatment with SK&F 64139."( Effect of adrenaline synthesis inhibition on brain noradrenaline neurons in locus coeruleus.
Elam, M; Engberg, G; Svensson, TH, 1981
)
0.49
" The dose-response relation between alinidine and frequency is not altered by atropine, and alinidine does not block the positive chronotropic action of isoprenaline."( Pacemaker selectivity: influence on rabbit atria of ionic environment and of alinidine, a possible anion antagonist.
Millar, JS; Williams, EM, 1981
)
0.26
" The age, degree of renal impairment, plasma renin activity, and number and dosage of antihypertensive medicines did not account for these differences in NE."( Effect of antihypertensive therapy on plasma catecholamines in renal failure patients.
Anderson, S; Cronin, R; Henrich, WL; Mitchell, H; Pettinger, WA, 1981
)
0.26
") shifted the dose-response curve for all of the compounds tested to the right."( Analysis of pupillary dilation produced by analogs of clonidine.
Koss, MC, 1981
)
0.51
" Diluted plasma from normal and acromegalic dogs resulted in a dose-response curve parallel to the standard curve."( Radioimmunoassay of canine growth hormone.
Eigenmann, JE; Eigenmann, RY, 1981
)
0.26
" Under controlled inpatient conditions established to assess dosage guidelines and to examine specific signs and symptoms of withdrawal, 20 of 25 (80%) patients were able to withdraw completely from methadone by the end of a two-week period."( The clinical use of clonidine in abrupt withdrawal from methadone. Effects on blood pressure and specific signs and symptoms.
Charney, DS; Heninger, GR; Kleber, HD; Redmond, DE; Sternberg, DE, 1981
)
0.59
"9 micrograms kg-1) twice daily during a dosage interval after 6--12 months monotherapy with clonidine."( Clonidine kinetics in man--evidence for dose dependency and changed pharmacokinetics during chronic therapy.
Edlund, PO; Frisk-Holmberg, M; Paalzow, L, 1981
)
1.93
" The blood pressure reduction in patients with essential hypertension was satisfactory on this regimen and the steady-state plasma concentrations were within the BP-lowering concentration range at the end of a dosage interval."( The effectiveness of clonidine as an antihypertensive in a two-dose regimen.
Frisk-Holmberg, M, 1980
)
0.58
" With the dosage build-up the antidepressants themselves start to exert the hypotensive effect."( [Influence of antidepressants on the hypotensive effect of clofeline in rats].
Mashkovskiĭ, MD; Medvedev, BA,
)
0.13
" Dose-response curves were generated for para-aminoclonidine in the presence of vehicle alone, yohimbine (alpha-2 antagonist), idazoxan (alpha-2/I1/I2 antagonist) and prazosin (alpha-1 antagonist)."( Identification, localization and functional analysis of imidazoline and alpha adrenergic receptors in canine prostate.
Breslin, DS; Ernsberger, P; Felsen, D; Marion, DN; May, M; Nejat, RJ; Nguyen, P; Sutaria, PM; Vaughan, ED, 1994
)
0.54
" NPY decreased LCX flow and increased CVR dose dependently in both groups, and there was no significant difference in the dose-response relation between the two groups."( Influence of inhibition of endothelium-derived nitric oxide formation to effects of vasoconstrictor agents neuropeptide Y, clonidine, and ergonovine on coronary vascular resistance.
Ishizaka, H; Matsunaga, T; Okumura, K; Tsunoda, R; Yasue, H, 1994
)
0.5
" Dose-response curves of the sedative effect of the alpha 2 adrenergic receptor agonist clonidine were established, a sedative effect being defined as a decrease in overall horizontal displacements, rearings and hole visits."( Novelty seeking behavior in the rat is dependent upon the integrity of the noradrenergic system.
Dyon-Laurent, C; Hervé, A; Sara, SJ, 1995
)
0.51
" Neostigmine was injected either 20 or 60 minutes prior to beginning cumulative dosing with the alpha 2-adrenergic agonist."( Subarachnoid neostigmine potentiation of alpha 2-adrenergic agonist analgesia. Dexmedetomidine versus Clonidine.
Bouaziz, H; Eisenach, JC; Hewitt, C,
)
0.35
" Dose-response curves for hot plate and tail immersion tests were established for IT neostigmine, physostigmine, and echothiophate in rats."( Intrathecal acetyl cholinesterase inhibitors produce analgesia that is synergistic with morphine and clonidine in rats.
Abram, SE; Winne, RP, 1995
)
0.51
" Dose-response functions of sufentanil, clonidine and combinations of clonidine plus sufentanil were determined."( Interactions between the lipophilic opioid sufentanil and clonidine in rats after spinal application.
De Kock, M; Meert, TF, 1995
)
0.8
" This effect was noncompetitive as the slopes for the antinociceptive dose-response curves diminished after SP pretreatment."( N-acetyl beta-endorphin-(1-31) and substance P regulate the supraspinal antinociception mediated by mu opioid and alpha-2 adrenoceptors but not by delta opioid receptors in the mouse.
Garzón, J; Sánchez-Blázquez, P, 1993
)
0.29
"The randomized, double-blind, dose-response study was designed to evaluate the effects of the addition of clonidine to epidural morphine on postoperative analgesia and side effects in patients undergoing cesarean delivery."( Addition of clonidine to epidural morphine enhances postoperative analgesia after cesarean delivery.
Capogna, G; Celleno, D; Costantino, P; Foresta, S; Zangrillo, A,
)
0.72
" The dose-response relationship for norepinephrine-induced [Ca2+]i response showed an increase in maximum effect with no change in agonist potency, and the increase in maximum effect was disproportionate to the difference in receptor density."( Effect of receptor density on the receptor-effector coupling: use of cloned and stably expressed alpha 1B-adrenoceptors in CHO cells.
Horie, K; Tsujimoto, G, 1995
)
0.29
" There were no significant differences between the dose-response curves of the diabetic group with normal urinary albumin excretion and the non-diabetic group."( Selective enhancement of alpha 2-adrenoceptor-mediated vasoconstriction in insulin-dependent diabetic patients with microalbuminuria.
Bodmer, CW; De Leeuw, PW; Janssen, M; Schaper, NC; Williams, G, 1995
)
0.29
" However, vasoconstriction due to clonidine post-ENDT even at maximal dosage (10(-3) M), was greatly attenuated in all four branching orders as in group II."( Attenuation of arteriolar alpha 2-adrenoceptor sensitivity during endotoxemia.
Baker, CH; Nessellroth, S; Ortiz-Tweed, M; Price, JM; Sutton, ET, 1994
)
0.57
" The dose-response relationship shifted to the left following REMs deprivation (ED50 values in the group-housed, isolated, and REMs-deprived mice were 250, 200, and 27 micrograms/kg, respectively)."( Monoamine depletion attenuates the REM sleep deprivation-induced increase in clonidine response in the forced swimming test.
Asakura, W; Matsumoto, K; Ohta, H; Watanabe, H, 1994
)
0.52
"This study was designed to evaluate the dose-response effects of different doses of clonidine on the stress response to laryngoscopy and endotracheal intubation."( Dose-response effects of intravenous clonidine on stress response during induction of anesthesia in coronary artery bypass graft patients.
Kulka, PJ; Tryba, M; Zenz, M, 1995
)
0.79
" Taken together, these results indicate a shift to the right in the dose-response function for clonidine in prenatal EtOH-exposed offspring relative to control mice."( Reduced sensitivity to the effects of clonidine on ethanol-stimulated locomotor activity in adult mouse offspring prenatally exposed to ethanol.
Becker, HC; Hale, RL; Weathersby, RT,
)
0.62
" After recovery from catheter implantations (5-7 days), intrathecal dose-response curves were established for the antihyperesthesia effects of clonidine (3, 6, 10, and 20 micrograms) and MK-801 (1, 3, 10, and 20 micrograms) alone to obtain the ED50 for each agent."( Analysis of drug interaction between intrathecal clonidine and MK-801 in peripheral neuropathic pain rat model.
Lee, YW; Yaksh, TL, 1995
)
0.75
" With the fixed-dose analysis, the log dose-response curves showed a left shift that considerably exceeds the theoretical curve made by a simple sum of the effects of clonidine alone and with MK-801 (1 microgram)."( Analysis of drug interaction between intrathecal clonidine and MK-801 in peripheral neuropathic pain rat model.
Lee, YW; Yaksh, TL, 1995
)
0.74
"5% timolol maleate twice daily for at least 4 weeks and who had 8 AM IOPs of at least 22 mm Hg and no greater than 30 mm Hg 12 hours after dosing were eligible for the study."( The efficacy of apraclonidine as an adjunct to timolol therapy. Apraclonidine Adjunctive Therapy Study Group.
Lehmann, RP; Ritch, R; Shin, DH; Shrader, CE; Stewart, WC; van Buskirk, EM, 1995
)
0.61
" The dose-response curves for the hypertensive responses to bradykinin in SD and WKY rats were essentially the same, whereas the hypertensive effect of bradykinin was significantly greater in SHR than in either SD or WKY rats."( Rostral ventrolateral medulla as a site for the central hypertensive action of kinins.
Privitera, PJ; Thibodeaux, H; Yates, P, 1994
)
0.29
" Concentration- or dose-response curves for norepinephrine were obtained from aortic rings, superior mesenteric artery rings or the isolated perfused mesenteric vasculature from male Sprague-Dawley rats."( Functional distribution and role of alpha-1 adrenoceptor subtypes in the mesenteric vasculature of the rat.
Fleming, WW; Kong, JQ; Taylor, DA, 1994
)
0.29
" The dose-response curves for clonidine and NA were shifted to the right by bunazosin (a selective alpha 1-adrenoceptor antagonist), but were not affected by midaglizole (a selective alpha 2-adrenoceptor antagonist)."( Characteristics of the responses of isolated and perfused canine splenic arteries to vasoactive substances and to periarterially electrical stimulation.
Chiba, S; Nakane, T; Ren, LM, 1994
)
0.58
" Liver injury measured by either method was essentially nonexistent for dosages < or = 50 mg/kg in male mice, and was only minimally evident in female mice at the highest dosage testable."( Methylphenidate-induced hepatotoxicity in mice and its potentiation by beta-adrenergic agonist drugs.
Harbison, RD; James, RC; Roberts, SM; Roth, L, 1994
)
0.29
" In the first experiment, sensitivity to the sedative effects of the alpha 2 agonist clonidine was evaluated by determining a dose-response curve to clonidine in a hole board."( Noradrenergic hyperactivity in hippocampus after partial denervation: pharmacological, behavioral, and electrophysiological studies.
Dyon-Laurent, C; Hervé, A; Sara, SJ, 1994
)
0.51
" After the dosage of clonidine was again increased, complete relief of the symptoms was achieved again."( High-dose clonidine in a case of restless legs syndrome.
Wagner, ML; Walters, AS; Zoe, A,
)
0.85
"0123) linear dose-response relation between single doses and antispastic action of tizanidine."( Correlations between dose, plasma concentrations, and antispastic action of tizanidine (Sirdalud).
Emre, M; Leslie, GC; Muir, C; Part, NJ; Pokorny, R; Roberts, RC, 1994
)
0.29
" All efficacy parameters were evaluated by the physician/assessor, and the physician/prescriber was responsible for all dosage adjustments."( Tizanidine treatment of spasticity caused by multiple sclerosis: results of a double-blind, placebo-controlled trial. US Tizanidine Study Group.
Birnbaum, G; Carter, JL; Greenstein, J; Lublin, FD; Smith, C, 1994
)
0.29
" Tizanidine was titrated to an optimized dosage in each patient to a maximum of 36 mg/d."( Efficacy and safety of tizanidine in the treatment of spasticity in patients with spinal cord injury. North American Tizanidine Study Group.
Bugaresti, J; Martinez-Arizala, A; Nance, PW; Shellenberger, K; Sheremata, W, 1994
)
0.29
" Plasma concentration of clonidine increased gradually after application of M and decreased gradually after removal, whereas this parameter increased rapidly during the absorption phase and decreased rapidly in the elimination phase after each dosage of Catapres."( Comparison of the pharmacokinetics, pharmacodynamics, and safety of oral (Catapres) and transdermal (M-5041T) clonidine in healthy subjects.
Ebihara, A; Fujimura, A; Kotegawa, T; Kumagai, Y; Nakashima, H; Ohashi, K; Shiga, T, 1994
)
0.8
" Transient sedation lasting 2 to 3 days occurred after initial administration or dosage increase; otherwise, clonidine was well tolerated."( Clonidine therapy for comorbid attention deficit hyperactivity disorder and conduct disorder: preliminary findings in a children's inpatient unit.
Mandoki, MW; Schvehla, TJ; Sumner, GS, 1994
)
1.94
"5 to 37 fold) to the right of the dose-response curve for clonidine without significant change of maximum inhibitory effect, in a manner compatible with competitive antagonism (ED50B = 29."( Modulation by central postsynaptic alpha 2-adrenoceptors of the jaw-opening reflex induced by orofacial stimulation in rats.
Barturen, F; García-Sevilla, JA; García-Vallejo, P, 1994
)
0.53
"1 mg/kg and with an increase in infusion dosage to 2 micrograms/kg/min."( [Premedication with clonidine in the neurosurgical patient: sedation, anesthetic requirements and hemodynamic perfusion].
Carrera, A; García-Guiral, M; Horno, R; Lora-Tamayo, JI; Luengo, C; Pascual, E; Quintana, B,
)
0.45
" The dose-response relation of NE-induced vasoconstriction was determined and compared for control (n = 5) and trained (n = 6) groups."( Physical conditioning decreases norepinephrine-induced vasoconstriction in rabbits. Possible roles of norepinephrine-evoked endothelium-derived relaxing factor.
Chen, CC; Chen, HI; Li, HT, 1994
)
0.29
" This study was performed to evaluate the dose-response hemodynamic and analgesic profiles of intrathecal clonidine administered after a standard surgical intervention, without perioperative administration of additional analgesics, local anesthetics, or tranquilizers."( Hemodynamic and analgesic profile after intrathecal clonidine in humans. A dose-response study.
Filos, KS; Goudas, LC; Patroni, O; Polyzou, V, 1994
)
0.75
" dose-response curves were obtained with dexmedetomidine, clonidine and ST-91 in groups of rats which had received a 7-day infusion of saline or the equianalgesic concentrations of dexmedetomidine (10 nmol/hr) or ST-91 (30 nmol/hr)."( Chronic spinal infusion of dexmedetomidine, ST-91 and clonidine: spinal alpha 2 adrenoceptor subtypes and intrinsic activity.
Takano, Y; Yaksh, TL, 1993
)
0.78
" Similarly, following chronic dosing with the racemate, RS-15385-196 (3 mg kg-1,p."( Modulation of central noradrenergic function by RS-15385-197.
Brown, CM; Clague, RU; Kilpatrick, AT; MacKinnon, AC; Martin, AB; Redfern, WS; Spedding, M, 1993
)
0.29
" The dose-response curve for the effect of clonidine on NE was shifted to the left in the latter group."( Presynaptic alterations associated with enhancement of evoked release and synthesis of norepinephrine in hippocampus of chronically cold-stressed rats.
Abercrombie, ED; Nisenbaum, LK, 1993
)
0.55
" In the isolated tissue, pretreatment with CEC (10(-5) M, 10 and 30 min) time-dependently shifted to the right the dose-response curve for phenylephrine and decreased the maximal contraction of aortas induced by phenylephrine, but did not shift or decrease those of prostates."( Alpha 1-adrenoceptor subtype in the rat prostate is preferentially the alpha 1A type.
Honda, K; Yazawa, H, 1993
)
0.29
") produced a moderate--but significant--rightward displacement of the dose-response curves to all agonists."( [The alpha-antiadrenergic properties of spiroxatrine, a ligand of serotonergic 5-HT1A receptors].
Hong, E; Ibarra, M; Ransanz, V; Terrón, JA; Villalón, CM,
)
0.13
" Microinjections of medetomidine into the cerebellum or the PAG produced an identical dose-response curve in the tail-flick test as that obtained following microinjection into the RVM."( The rostroventromedial medulla is not involved in alpha 2-adrenoceptor-mediated antinociception in the rat.
Hämäläinen, MM; Pertovaara, A, 1993
)
0.29
" More controlled trials with less aggressive dosing regimens and placebo controls need to be performed to assess the most appropriate treatment for HUs with the fewest adverse effects."( Oral antihypertensives for hypertensive urgencies.
Gales, MA, 1994
)
0.29
" If blood pressure was not adequately controlled (DBP < 90 or 10 mmHg decreased from baseline value) the dosage was increased on a 2 week basis assessment."( One year efficacy and tolerability of clonidine administered by the transdermal route in patients with mild to moderate essential hypertension--a multicentre open label study. The Antihypertensive Patch Italian Study (APIS) Investigators.
, 1993
)
0.56
" The relation between dosage and plasma concentration was linear."( The pharmacokinetics of clonidine in high dosage.
Fauler, J; Verner, L, 1993
)
0.59
" The potentiating action of L-NNA on noradrenaline-induced contractions could also be observed in the presence of yohimbine or rauwolscine, although dose-response curves were shifted to the right."( Involvement of alpha-adrenoceptors in the endothelium-dependent depression of noradrenaline-induced contraction in rat aorta.
Kaneko, K; Sunano, S, 1993
)
0.29
" The dose-response curve for phenylephrine-induced increases in mesenteric or hindlimb vascular resistance was shifted only 2- to 10-fold to the right by CEC."( The regulation of regional hemodynamics by alpha-1 adrenoceptor subtypes in the conscious rat.
Barron, KW; Piascik, MT; Smith, MS; Soltis, EE, 1993
)
0.29
"A statistically significant dose-response effect was found for craving scores (dose-response gradient, -3."( A placebo-controlled study of three clonidine doses for smoking cessation.
Forbes, A; Gourlay, S; Kutin, J; Marriner, T; McNeil, J, 1994
)
0.56
"This study showed a statistically significant dose-response effect of clonidine on tobacco withdrawal craving and a reduction in mean craving scores of 16% during 300 micrograms dosing."( A placebo-controlled study of three clonidine doses for smoking cessation.
Forbes, A; Gourlay, S; Kutin, J; Marriner, T; McNeil, J, 1994
)
0.8
" The chlorhydrate arginine was administered by mouth at a daily dosage of 4 g (1 phial/2) for 6 months."( [Therapy with arginine chlorohydrate in children with short constitutional stature].
Becherucci, P; La Cauza, F; Pittari, AM; Seminara, S,
)
0.13
" Weekly dosing of continuously released antihypertensive agents may result in better blood pressure control than conventional daily dosing."( Use of transdermal clonidine in chronic hemodialysis patients.
Johnson, KL; McConnell, J; Rosansky, SJ, 1993
)
0.61
" When transdermal clonidine was substituted for twice daily dosage of oral clonidine, blood pressure decreases were fully maintained."( The use of transdermal clonidine in the hypertensive patient with chronic renal failure.
Cristal, N; Lowenthal, DT; Paran, E; Saris, SD, 1993
)
0.93
" Pulse rate, blood pressure and dosage of the additional antihypertensive medication as signs of sympathetic disturbance were registered."( Beta-blockade in acute aneurysmal subarachnoid haemorrhage.
Haass, A; Hamann, G; Schimrigk, K, 1993
)
0.29
" Drug was most often given on a fixed dosing schedule with additional medication "as needed" (52% of the programs)."( Alcohol withdrawal: a nationwide survey of inpatient treatment practices.
Friedman, LS; Mayo-Smith, MF; Saitz, R, 1995
)
0.29
" Cold exposure induced elevation of plasma norepinephrine and reduction of the lymphoproliferative response to the suboptimal dosage of PHA."( Central stimulation of hormone release and the proliferative response of lymphocytes in humans.
Jezová, D; Juránková, E; Vigas, M,
)
0.13
" Coadministration of clonidine with LSD produced a leftward shift of the dose-response relationship of LSD without a significant change in the slope of the dose-response line."( Complex stimulus properties of LSD: a drug discrimination study with alpha 2-adrenoceptor agonists and antagonists.
Marona-Lewicka, D; Nichols, DE, 1995
)
0.61
" The dose-response curve was of an inverted U shape since with 10 micrograms of oxymetazoline the plasma GH did not rise."( Hypothalamic alpha 2A-adrenoceptors stimulate growth hormone release in the rat.
Kiem, DT; Makara, GB; Vizi, ES, 1995
)
0.29
"5% timolol 8 hours after dosing on days 1, 30, and 90; and a significant difference (P < ."( A 90-day study of the efficacy and side effects of 0.25% and 0.5% apraclonidine vs 0.5% timolol. Apraclonidine Primary Therapy Study Group.
Horwitz, B; Kottler, M; Laibovitz, R; Ritch, R; Stewart, RH; Stewart, WC, 1996
)
0.53
" This article is a guide to its usage in children and includes discussion of its indications, contraindications, pre-treatment laboratory studies, dosing and drug interactions."( Clonidine: a practical guide for usage in children.
Oesterheld, J; Tervo, R, 1996
)
1.74
" Higher dosage of yohimbine inhibited the baseline expression of bFGF."( Alpha 2-adrenergic agonists induce basic fibroblast growth factor expression in photoreceptors in vivo and ameliorate light damage.
Cao, W; Cheng, T; Li, Y; Steinberg, RH; Wen, R, 1996
)
0.29
"We determined the relative potency of these drugs with respect to their effects on mean arterial pressure and heart rate by performing cumulative intravenous dose-response relationship studies in six conscious rabbits."( Relative importance of central imidazoline receptors for the antihypertensive effects of moxonidine and rilmenidine.
Chan, CK; Head, GA, 1996
)
0.29
" Anesthetic requirements, circulatory variables, interventions, and isoproterenol dose-response curves (pre- and postoperatively) were determined."( Clonidine for major vascular surgery in hypertensive patients: a double-blind, controlled, randomized study.
Bayon, MC; Boucaud, C; Bouilloc, X; Brudon, JR; Butin, E; Danays, T; Frehring, B; Ghignone, M; Levron, JC; Petit, P; Quintin, L; Tassan, H; Tissot, S; Viale, JP, 1996
)
1.74
" Following systemic (intraperitoneal) administration of apomorphine (a dopamine receptor D1/D2 mixed agonist), SKF 38393 (D1 > D3 > D2 agonist), LY 17155 or quinpirole (D3 > D2 and D1) agonist), haloperidol (a DA-D2 antagonist), and clonidine (noradrenaline receptor alpha 2 agonist), the ICSS response rates evoked from LH-MFB and VTA-SN were compared with vehicle or saline-treated animals on the basis of dose-response functions."( Dose-response functions of apomorphine, SKF 38393, LY 171555, haloperidol and clonidine on the self-stimulation evoked from lateral hypothalamus and ventral tegmentum.
Desiraju, T; Raju, TR; Singh, J, 1996
)
0.71
" The parallelism of the dose-response curves indicates activation of a common receptor subtype."( alpha-Adrenoceptor and opioid receptor modulation of clonidine-induced antinociception.
Miranda, HF; Naquira, D; Pinardi, G; Sierralta, F, 1996
)
0.54
" Dose-response curves were obtained for each drug individually; for morphine:clonidine at 1:3, 1:1, and 1:0."( Interaction of morphine and clonidine on gastrointestinal transit in mice.
Pol, O; Puig, MM; Warner, W, 1996
)
0.82
" Dose-response analyses showed that dexmedetomidine, epinephrine, norepinephrine had similar analgesic potencies, but clonidine was significantly less potent."( Spinal administration of adrenergic agents produces analgesia in amphibians.
Brenner, GM; Stevens, CW, 1996
)
0.5
"Twenty eight opiate addicted inpatients who had been stabilised on methadone took part in a double-blind randomised trial of clonidine and lofexidine (14 on each treatment) for opiate detoxification: clonidine or lofexidine dosage was titrated according to symptoms."( Double-blind study of lofexidine and clonidine in the detoxification of opiate addicts in hospital.
Beckford, H; Kahn, A; Mumford, JP; Rogers, GA, 1997
)
0.78
" Dose-response curves were plotted for suppression of paw withdrawal 30 minutes after intrathecal injection of various doses of tizanidine, clonidine, and octreotide."( Effects of intrathecal nonnarcotic analgesics on chronic tactile allodynia in rats: alpha 2-agonists versus somatostatin analog.
Kroin, JS; Ono, N; Paice, JA; Penn, RD, 1997
)
0.5
" Wide interpatient variability in the effective plasma concentrations of tizanidine means that the optimal dosage must be titrated over 2 to 4 weeks for each patient (dosages of 2 to 36 mg/day have been used in clinical trials)."( Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders.
Bryson, HM; Wagstaff, AJ, 1997
)
0.3
" Initial dose-response studies showed that agmatine administered in low doses (0."( Central cardiovascular actions of agmatine, a putative clonidine-displacing substance, in conscious rabbits.
Chan, CK; Godwin, SJ; Head, GA, 1997
)
0.54
" boluses of ST to generate dose-response curves."( Spinal infusion of N-methyl-D-aspartate antagonist MK801 induces hypersensitivity to the spinal alpha-2 agonist ST91 in the rat.
Dunbar, SA; Yaksh, TL, 1997
)
0.3
"A randomized, double-blind, placebo-controlled, dose-response study of tizanidine hydrochloride (8 or 16 mg)."( Relationship of the antispasticity effect of tizanidine to plasma concentration in patients with multiple sclerosis.
Cohen, JA; Francis, GS; Hudson, S; Lindsey, JW; Lynch, SG; Mass, MK; Nance, PW; O'Connor, P; Schapiro, RT; Shellenberger, K; Sheremata, WA; Vollmer, T; Whitham, R, 1997
)
0.3
" Dosage should be individualized, based on withdrawal severity measured by withdrawal scales, comorbid illness, and history of withdrawal seizures."( Pharmacological management of alcohol withdrawal. A meta-analysis and evidence-based practice guideline. American Society of Addiction Medicine Working Group on Pharmacological Management of Alcohol Withdrawal.
Mayo-Smith, MF, 1997
)
0.3
" Dose-response curve data were obtained with fentanyl, clonidine, xylazine, dexmedetomidine, and 40."( Alpha 2-adrenoceptor agonists and stress-induced analgesia in rats: influence of stressors and methods of analysis.
De Kock, M; Meert, TF, 1997
)
0.54
") did not modify the basal activity of the locus coeruleus but shifted to the left the dose-response curve for the clonidine induced inhibition of firing rate and reduced the corresponding ED50 by 77%."( Activation of 5-HT1A receptors potentiates the clonidine inhibitory effect in the locus coeruleus.
Ruiz-Ortega, JA; Ugedo, L, 1997
)
0.76
" Further benefit from lofexidine may be possible with revised dosing regimens."( Double-blind randomised controlled trial of lofexidine versus clonidine in the treatment of heroin withdrawal.
Hu, WH; Lin, SK; Strang, J; Su, LW; Tsai, CJ, 1997
)
0.54
" Clonidine produced steep dose-response lines in all tests."( [Antinociceptive activity of intracisternal clonidine in the mouse].
Izumi, R; Maeda, S; Matsuda, M; Murakawa, K; Noma, K; Tashiro, C; Yoshimura, Y, 1997
)
1.47
" The results obtained show that Adalat in dosage 60 mg daily during 7 days is most effective in cases with concomitant border-line hypertension."( [Premedication with different groups of hypotensive drugs in preparation of patients with concomitant arterial hypertension to planned surgical treatment].
Eliutin, DV; Mil'tsyn, AS; Sadchikov, DV, 1998
)
0.3
" The effects of two different dosage regimens, once before surgery or once before and after surgery, were studied."( The effect of 1% apraclonidine on intraocular pressure after cataract surgery.
Renzenbrink-Bubberman, AC; Sterk, CC; van Best, JA, 1998
)
0.62
"NRT can be delivered through a number of different nicotine-containing dosage forms (e."( Smoking cessation: Part 2--Pharmacologic approaches.
Jack, HM; Popovich, NG; Wongwiwatthananukit, S,
)
0.13
" Pretreatment with yohimbine shifted the dose-response curve for dopamine to the right in femoral veins, but not in arteries."( Dopamine releases endothelium-derived relaxing factor via alpha 2-adrenoceptors in canine vessels: comparisons between femoral arteries and veins.
Fujiwara, H; Inoue, K; Ito, H; Minatoguchi, S; Segawa, T; Wada, H, 1998
)
0.3
" Yohimbine pretreatment resulted in a rightward shift of the dose-response curves (DMET > CLON > UK)."( Pharmacological evidence for different alpha 2-adrenergic receptor sites mediating analgesia and sedation in the rat.
Buerkle, H; Yaksh, TL, 1998
)
0.3
" Concentrations of tizanidine and baclofen were nearly identical during the single and concomitant dosing periods."( A controlled pharmacokinetic evaluation of tizanidine and baclofen at steady state.
Groves, L; Novack, GD; Shah, J; Shellenberger, MK, 1999
)
0.3
" Our results indicated that acute exercise induced the following effects: (1) the dose-response curves of ACh and CLO shifted to the left; (2) the high-affinity M3 binding sites increased in number but not in affinity; (3) the alpha2 binding sites decreased in number but increased in affinity."( Acute exercise enhances receptor-mediated endothelium-dependent vasodilation by receptor upregulation.
Chen, H; Cheng, L; Hsu, L; Jen, CJ; Lin, MT; Yang, C, 1999
)
0.3
" In the presence of the opioid receptor antagonists, naloxone or naltrindole, the resulting nefopam dose-response relationships were shifted to the right."( The involvement of opioidergic and noradrenergic mechanisms in nefopam antinociception.
Gray, AM; Nevinson, MJ; Sewell, RD, 1999
)
0.3
" After the tail-flick latencies returned to baseline levels, dose-response curves were generated to Mor, Clon, and Mor-Clon combinations in tolerant and control mice."( Spinal antinociceptive synergism between morphine and clonidine persists in mice made acutely or chronically tolerant to morphine.
Fairbanks, CA; Wilcox, GL, 1999
)
0.55
" Adequate stable anesthesia was achieved in reduced dosage of conventional anesthesiological agents."( [Use of nonopiate agents for anesthesia in ENT patients at high surgical-anesthesiological risk].
Akopian, RG; Daĭkhes, NA; Davudov, KhSh; Gur'ianov, VA; Kokliaeva, NV; Kuĭian, SM; Nazhmudinov, II; Pogosov, VS; Riazanov, VB; Tiukov, VL, 1998
)
0.3
"Symptoms of the autonomic nervous system were more effectively prevented by GHB as evident in the lower dosage requirement of clonidine."( [Gamma-hydroxybutyrate for treatment of alcohol withdrawal syndrome in intensive care patients. A comparison between with two symptom-oriented therapeutic concepts].
Lenzenhuber, E; Müller, C; Rommelspacher, H; Spies, C, 1999
)
0.51
"Our results show that high doses of epidural clonidine potentiate general anesthetics and provide more efficient postoperative analgesia than the two bupivacaine dosage regimens investigated."( Epidural clonidine or bupivacaine as the sole analgesic agent during and after abdominal surgery: a comparative study.
De Kock, M; Gautier, P; Jonniaux, M; Lavand'homme, P; Pavlopoulou, A, 1999
)
0.98
" The least decrease of BP and minimal need of rescue ephedrine among all patients studied were recorded in the group receiving low dosage of lidocaine with intrathecal clonidine (L40-C100)."( Enhancement of intrathecal lidocaine by addition of local and systemic clonidine.
Dobrydnjov, I; Samarütel, J, 1999
)
0.73
" Dose-response data show dexmedetomidine to be the most potent inhibitor."( Inhibition of water permeability in the rat collecting duct: effect of imidazoline and alpha-2 compounds.
Hébert, CA; Kudo, LH; Rouch, AJ, 1999
)
0.3
" Both drugs, when applied in a once-daily dosage schedule, appear to control hypertension in most patients."( Central I1-imidazoline receptors as targets of centrally acting antihypertensive drugs. Clinical pharmacology of moxonidine and rilmenidine.
Peters, SL; Van Zwieten, PA, 1999
)
0.3
" The authors evaluated the dose-response potency of intrathecally administered clonidine by itself during first stage of labor with respect to analgesia and maternal and fetal side effects."( Analgesic and hemodynamic effects of intrathecal clonidine as the sole analgesic agent during first stage of labor: a dose-response study.
Chiari, A; Eisenach, JC; Germann, P; Kainz, C; Klimscha, W; Krenn, C; Lorber, C; Wildling, E; Zavrsky, A, 1999
)
0.79
"5 mg kg-1) and the time point at which nociceptive responses were recorded (30 min after the administration of the drug) were chosen on the basis of dose-response (0."( Preweanling naltrindole administration differentially affects clonidine induced antinociception and plasma adrenaline levels in male and female neonatal rats.
Aguilar, A; Alberti, I; Alguacil, LF; Caamaño, M; Fernández, B; Romero, EM; Viveros, MP, 1999
)
0.54
" The dose-response studies were performed in vitro analyzing the effect of these compounds on intracellular cAMP production in the presence of pheromone biosynthesis activating neuropeptide (PBAN) at 1 pmol/intersegment."( Three-dimensional quantitative structure-activity studies of octopaminergic agonists responsible for the inhibition of sex-pheromone production in Helicoverpa [correction of Hercoverpa] armigera.
Gileadi, C; Hirashima, A; Kuwano, E; Rafaeli, A, 1999
)
0.3
" Plasma levels of insulin and glucose were measured after a 75-g glucose load, and CC was given at a dosage of 50-250 mg/d for ovulation-induction."( Growth hormone response to clonidine in anovulatory infertile women resistant to clomiphene citrate stimulation.
Garrone, S; Minuto, F; Ragni, N; Rossato, P, 2000
)
0.6
" A similar finding was made in the hot-plate test despite the fact that the dose-response characteristics of the agonists were different in this test."( Synergistic interactions between two alpha(2)-adrenoceptor agonists, dexmedetomidine and ST-91, in two substrains of Sprague-Dawley rats.
Graham, BA; Hammond, DL; Proudfit, HK, 2000
)
0.31
" In the dosage used, urapidil seems to be unable to prevent postanesthetic shivering."( A comparison of urapidil, clonidine, meperidine and placebo in preventing postanesthetic shivering.
Boldt, J; Maleck, WH; Piper, SN; Reich, DG; Schmidt, CC; Suttner, SW, 2000
)
0.61
" In the dosage used, we were unable to show a significant benefit of urapidil."( A comparison of urapidil, clonidine, meperidine and placebo in preventing postanesthetic shivering.
Boldt, J; Maleck, WH; Piper, SN; Reich, DG; Schmidt, CC; Suttner, SW, 2000
)
0.61
" Dose-response curves for morphine and clonidine alone and combined at a 1:1 potency ratio were obtained, and doses producing a 50% and 60% inhibition were calculated (ED50, ED60)."( Intestinal inflammation and morphine tolerance alter the interaction between morphine and clonidine on gastrointestinal transit in mice.
Pol, O; Puig, MM; Warner, W, 2000
)
0.8
"In naive and tolerant mice, the combination induced linear dose-response curves up to the ED60 and then reached a plateau."( Intestinal inflammation and morphine tolerance alter the interaction between morphine and clonidine on gastrointestinal transit in mice.
Pol, O; Puig, MM; Warner, W, 2000
)
0.53
" dosing range and to assess its cardiovascular effects."( Intravenous clonidine infusion in critically ill children: dose-dependent sedative effects and cardiovascular stability.
Ambrose, C; Bevan, C; Howells, R; Jenkins, I; Murphy, P; Sale, S; Weir, P; Wolf, A, 2000
)
0.69
" The lack of any dose-response relationship might be explained by a plateau effect."( The awakening concentration of sevoflurane in children.
Baba, Y; Inomata, S; Kihara, S; Kohda, Y; Toyooka, H; Yaguchi, Y, 2000
)
0.31
" Furthermore, the combinations of moxonidine-morphine and clonidine-morphine resulted in substantial leftward shifts in the dose-response curves compared with those of each agonist administered separately."( Moxonidine, a selective imidazoline-alpha2 -adrenergic receptor agonist, produces spinal synergistic antihyperalgesia with morphine in nerve-injured mice.
Fairbanks, CA; Grocholski, BM; Nguyen, HO; Wilcox, GL, 2000
)
0.55
"Clonidine, dobutamine, and dopexamine at high dosage suppress the gastric mucosal vasodilator response to acid back diffusion, which is an important defense mechanism."( Differential effects of clonidine, dopamine, dobutamine, and dopexamine on basal and acid-stimulated mucosal blood flow in the rat stomach.
Holzer, P; Painsipp, E, 2001
)
2.06
" Dosing was titrated from 2 mg at bedtime to a median daily dose of 14 mg (mean, 13."( An open-label dose-titration study of the efficacy and tolerability of tizanidine hydrochloride tablets in the prophylaxis of chronic daily headache.
Lake, AE; Saper, JR; Winner, PK, 2001
)
0.31
" We investigated the dose-response relationship for epidural clonidine when added to a continuous postoperative epidural infusion of ropivacaine."( The dose-response relationship for clonidine added to a postoperative continuous epidural infusion of ropivacaine in children.
De Negri, P; De Vivo, P; Ivani, G; Lonnqvist, PA; Visconti, C, 2001
)
0.83
" Dose-response curves were obtained for the antinociceptive effect of diclofenac, phenylephrine, clonidine, desipramine, prazosin, and yohimbine administered both systemically and intrathecally, and ED(50)s were calculated."( An isobolographic analysis of the adrenergic modulation of diclofenac antinociception.
Miranda, HF; Pinardi, G; Sierralta, F, 2001
)
0.53
" Ten of 47 patients (21%) were able to reach the maximum daily dosage of 36 mg."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.31
" The average dosage at 4 weeks was 25."( Prospective assessment of tizanidine for spasticity due to acquired brain injury.
Brunner, RM; Guin-Renfroe, S; Johnson, A; Meythaler, JM, 2001
)
0.31
"This placebo-controlled, randomized study evaluated, on separate days, the dose-response relationship for 1 h infusions of clonidine 1, 2 and 4 microg kg(-1) h(-1), in eight healthy volunteers aged 22-30 yr."( Sedative, analgesic and cognitive effects of clonidine infusions in humans.
Ebert, TJ; Hall, JE; Uhrich, TD, 2001
)
0.78
" Dose-response curves were obtained for systemic and intrathecal antinociceptive effects of ketoprofen, phenylephrine, clonidine, desipramine, and prazosin; and ED50 were calculated."( Interaction between the antinociceptive effect of ketoprofen and adrenergic modulatory systems.
Miranda, HF; Pinardi, G; Sierralta, F, 2001
)
0.52
" In addition, dose-response curves for the inhibitory LC activity of clonidine showed a shift to the right in deprived animals indicating a subsensitivity of alpha2-adrenergic autoreceptors."( Increased neuronal activity in locus coeruleus from adult rats undernourished at perinatal age: its reversal by desipramine.
Cuadra, GR; Nasif, FJ; Orsingher, OA; Ramírez, OA, 2001
)
0.55
" We assessed the dose-response relationship of clonidine added to lidocaine in peribulbar block."( A dose response study of clonidine with local anesthetic mixture for peribulbar block: a comparison of three doses.
Bharti, N; Kaul, HL; Khokhar, SK; Madan, R; Shende, D, 2001
)
0.87
" We used the tail-flick test to construct dose-response curves before and 4 days after chronic morphine (75-mg pellets, subcutaneously (s."( Reduced development of tolerance to the analgesic effects of morphine and clonidine in PKC gamma mutant mice.
Basbaum, AI; Gilbert, H; Malmberg, AB; Zeitz, KP, 2001
)
0.54
" Various dosage forms of nicotine replacement therapy increase smoking quit rates relative to placebo, but they generally do not result in 1-year quit rates of over 20%."( Effect of nonnicotine pharmacotherapy on smoking behavior.
Golding, M; Hatsukami, DK; Jamerson, BD; Kotlyar, M, 2001
)
0.31
"3-10 microg) and clonidine (1-30 microg) were administered to obtain the dose-response curves and the 50% effective dose (ED(50)) for each drug."( Intrathecal carbachol and clonidine produce a synergistic antiallodynic effect in rats with a nerve ligation injury.
Han, SM; Hwang, JH; Lee, EJ; Park, JY; Park, PH; Sim, JY, 2002
)
0.95
" These effects are probably mediated via central mechanisms, since there was an approximate 8 fold rightward shift of the dose-response curve in the pithed SHR (indicating a weakened cardiovascular effect)."( Agmatine, an endogenous ligand at imidazoline binding sites, does not antagonize the clonidine-mediated blood pressure reaction.
Dominiak, P; Qadri, F; Raasch, W; Schäfer, U, 2002
)
0.54
" After an acute, 1-day spinalization, there was no change in the antinociceptive dose-response function to clonidine, relative to intact rats."( Spinal transection increases the potency of clonidine on the tail-flick and hindlimb flexion reflexes.
Advokat, C, 2002
)
0.79
" On the other hand, the bolus of intravenous clonidine 2 microg/kg (group C) was less effective in terms of pain relief but with similar side-effects to the 3 microg/kg dosage (group B)."( Clonidine for treatment of postoperative pain: a dose-finding study.
Ciccozzi, A; Di Pietro, A; Donatelli, F; Iovinelli, G; Marinangeli, F; Paladini, A; Rawal, N; Varrassi, G, 2002
)
2.02
" injection of diltiazem (6-48 nmol) inhibited from 50 to 100% the effect of noradrenaline and clonidine in a dose-response manner."( Interaction between brain L-type calcium channels and alpha2-adrenoceptors in the inhibition of sodium appetite.
David, RB; De Luca, LA; Menani, JV; Pereira, DT; Sugawara, AM, 2002
)
0.53
" In fetal, but not adult, MCA, UK-14304 induced a significant decrease in pD(2) for the phenylephrine dose-response relation."( Pre- and postjunctional alpha(2)-adrenergic receptors in fetal and adult ovine cerebral arteries.
Bishai, JM; Buchholz, JN; Gheorghe, CP; Longo, LD; Meulenaar, R; Nijland, R; Penninga, L; Zhang, L; Zhao, Y, 2002
)
0.31
" We conclude that separate dose-response relationships for oral clonidine are present regarding the hypnotic and analgesic effects in children undergoing sevoflurane anesthesia."( The hypnotic and analgesic effects of oral clonidine during sevoflurane anesthesia in children: a dose-response study.
Baba, Y; Inomata, S; Kihara, S; Kohda, Y; Miyabe, M; Sumiya, K; Toyooka, H, 2002
)
0.82
"Separate dose-response relationships for oral clonidine were found regarding the hypnotic and analgesic effects in children undergoing sevoflurane anesthesia."( The hypnotic and analgesic effects of oral clonidine during sevoflurane anesthesia in children: a dose-response study.
Baba, Y; Inomata, S; Kihara, S; Kohda, Y; Miyabe, M; Sumiya, K; Toyooka, H, 2002
)
0.84
" Drugs functionally or structurally related to clonidine, such as oxymetazoline, alpha-methylnorepinephrine and moxonidine, did not have their dose-response curves altered."( Contractile responses of the rat vas deferens after epithelium removal.
Garcez-do-Carmo, L; Jurkiewicz, A; Jurkiewicz, NH; Okpalaugo, EO, 2002
)
0.57
" These include the currently available dosage forms of nicotine replacement therapy (gum, patch, nasal spray, and inhaler) and bupropion."( Managing nicotine addiction.
Hatsukami, DK; Kotlyar, M, 2002
)
0.31
" In combination with either low or high frequency TENS, the dose-response curve shifted to the left and was significantly different from clonidine alone."( Enhanced reduction in hyperalgesia by combined administration of clonidine and TENS.
Chandran, P; Sluka, KA, 2002
)
0.76
" Using a mouse hot-plate test, dose-response relationships were first determined for all compounds individually and then for opioids co-administered with fixed doses of clonidine, ketamine or dextromethorphan."( Interactions of NMDA antagonists and an alpha 2 agonist with mu, delta and kappa opioids in an acute nociception assay.
Baker, AK; Hoffmann, VL; Meert, TF, 2002
)
0.51
" This chapter updates current data on drug dose-response relationships for local anaesthetics and the increasing use of intrathecal adjuncts to improve the anaesthetic and recovery profile for ambulatory spinal anaesthesia."( Spinal anaesthesia: local anaesthetics and adjuncts in the ambulatory setting.
Liu, SS; Salinas, FV, 2002
)
0.31
" Administration of both non-selective and selective alpha-adrenoceptor agonists in doses of 1-40 microg noradrenaline kg(-1) body weight (BW), 1-100 microg clonidine kg(-1) BW, or 100-800 mg methoxamine kg(-1) BW enhanced contractions of the proximal cauda epididymidis in a dose-response manner."( Mediation of contraction in rat cauda epididymidis by alpha-adrenoceptors.
Chaturapanich, G; Maythaarttaphong, S; Pholpramool, C; Verawatnapakul, V, 2002
)
0.51
" The basal firing rate was not modified by either a single dose or repeated doses of MDMA, although the latter produced a shift to the right in the dose-response curve for clonidine-induced inhibition of the firing rate (ED(50) increased by 59%) and a reduction in tyrosine hydroxylase activity (20%) in the hippocampus."( Short-term effects of 3,4-methylenedioximethamphetamine on noradrenergic activity in locus coeruleus and hippocampus of the rat.
Arrue, A; Giralt, MT; Ruiz-Ortega, JA; Ugedo, L, 2003
)
0.51
"25% drops in twice daily dosage and does not result in any significant ocular and systemic adverse effects."( A prospective, long-term, randomized study of the efficacy and safety of the drug combination pilocarpine 1% with clonidine 0.06% or clonidine 0.125% versus timolol 0.25%.
Agarwal, H; Rajashekhar, YL; Sihota, R; Venkatesh, P, 2002
)
0.53
" Dose-response curves for adrenaline were carried out as standard protocol."( Characteristics of histamine tachyphylaxis in rat uterine smooth muscle.
Gil Marqués, M; Martínez-Mir, I; Morales-Olivas, FJ; Rubio-Gomis, E, 2002
)
0.31
" The dosage of the two comparatine groups is given according to Documentation, the method of abserving the treatment protocols and detoxification standard is according to current regulation."( [Clinial study of "qingjunyin" detoxification for the treatment of heroin addicts].
Lan, S; Lu, H; Wang, G; Yuan, D; Zhan, C, 1997
)
0.3
"Morphine dosage [median (25th-75th percentiles)] was less in the first 24 h in the patients who were given intrathecal morphine + clonidine [7 (0-37) mg] than in other patients [40."( Intrathecal morphine and clonidine for coronary artery bypass grafting.
Arnulf, JJ; Balarac, N; Bonnet, F; Lena, P; Teboul, J, 2003
)
0.83
"Evening dosing with guanabenz or clonidine lowered morning BP significantly."( Therapeutic effects of evening administration of guanabenz and clonidine on morning hypertension: evaluation using home-based blood pressure measurements.
Aoki, Y; Araki, T; Chonan, K; Hashimoto, J; Hozawa, A; Imai, Y; Kikuya, M; Matsubara, M; Michimata, M; Nishimura, T; Ohkubo, T; Ugajin, T; Yamaguchi, J, 2003
)
0.84
" Morphine exhibited a bell-shaped dose-response curve in Lewis rats, these animals being more sensitive than F344 at 1 and 5 mg/kg but less sensitive at 10 mg/kg."( The contribution of alpha2-adrenoceptor and opioid receptor mechanisms to antinociception differs in Lewis and Fischer 344 rats.
Alguacil, LF; Herradón, G; Morales, L; Pérez-García, C, 2003
)
0.32
" Similar responses were observed after oral dosing and in lean littermates."( The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat model of metabolic syndrome X.
Ernsberger, P; Velliquette, RA, 2003
)
0.32
" Regarding the dose-response relationship of compounds 1a and 1c, it is evident that the activity of these compounds is in direct proportion to their dose and all compounds show activities comparable to clonidine."( The antinociceptive activities of 1-(4-aryl-2-thiazolyl)-3,5-disubstituted-2 pyrazolines in mouse writhing test.
Abdollahi, M; Bagheri, M; Shafiee, A; Shekarchi, M,
)
0.32
" Methylphenidate and amphetamine-based stimulants are now available in longer-acting, once-daily and shorter-acting divided dosing schedules."( Pharmacological management of attention-deficit hyperactivity disorder.
Reeves, G; Schweitzer, J, 2004
)
0.32
" In this study, we investigated the dose-response characteristics of IT clonidine, and whether a subeffective dose of clonidine could enhance the effect of SCS in nerve-injured rats with tactile hypersensitivity (allodynia)."( Intrathecal clonidine potentiates suppression of tactile hypersensitivity by spinal cord stimulation in a model of neuropathy.
Linderoth, B; Meyerson, BA; Schechtmann, G; Wallin, J, 2004
)
0.93
"We examined the dose-response relationship of intrathecal clonidine at small doses (( Small-dose intrathecal clonidine and isobaric bupivacaine for orthopedic surgery: a dose-response study.
Aeschbach, A; Gurzeler, JA; Kindler, CH; Schneider, MC; Strebel, S, 2004
)
0.88
" The utility of the neuroendocrine response to serotonergic (ipsapirone) and noradrenergic (clonidine) probes as predictors of venlafaxine dosage required for effective treatment was also explored."( Efficacy of open-label venlafaxine in subjects with major depressive disorder: associations with neuroendocrine response to serotonergic and noradrenergic probes.
Goodman, M; Grossman, R; Mitropoulou, V; New, A; Reynolds, D; Schmeidler, J; Siever, LJ; Silverman, J, 2004
)
0.54
" Dose-response curves for the inhibitory effect of clonidine showed subsensitivity of alpha2-adrenergic autoreceptors in protein-deprived rats, a phenomenon reversed by fluoxetine treatment."( Locus coeruleus activity in perinatally protein-deprived rats: effects of fluoxetine administration.
Cuadra, GR; Orsingher, OA; Ramírez, OA; Sodero, AO; Valdomero, A, 2004
)
0.58
" This randomized, double-blind, double-dummy, pilot study compares two buprenorphine sublingual tablet dosing schedules to oral clonidine."( A double-blind, double-dummy, randomized, prospective pilot study of the partial mu opiate agonist, buprenorphine, for acute detoxification from heroin.
Ellis, ML; Knox, PC; Malte, CA; Oreskovich, MR; Reoux, JP; Saxon, AJ, 2005
)
0.53
" Sigmoid dose-response curves for pupillary dilation were produced in pentobarbital anesthetized rats by intravenous administration of increasing doses of agonists (guanabenz for alpha(2)-adrenoceptors, clonidine for both alpha(2)-adrenoceptors and imidazoline I(1) receptors, and rilmenidine for imidazoline I(1) receptors)."( Rat clonidine mydriasis model: imidazoline receptors are not involved.
Koss, MC; Yu, Y, 2005
)
1.07
" The analysis of variance (ANOVA) and Student's t-test were applied to correlate the results of tizanidine and rofecoxib determination in dosage form by means of HPTLC and HPLC method."( Application of HPLC and HPTLC for the simultaneous determination of tizanidine and rofecoxib in pharmaceutical dosage form.
Agrawal, H; Dhaneshwar, SR; Kakad, A; Kaul, N; Patil, B, 2005
)
0.33
" The skin layer may be only a minor rate-limiting barrier after the topical skin layer at the dosing site is saturated with penetrating clonidine in the initial phase (0 to 12 h)."( In vitro and in vivo characterization of a newly developed clonidine transdermal patch for treatment of attention deficit hyperactivity disorder in children.
Guo, HY; Ke, GM; Lu, WL; Wang, L; Xue, HY; Zhang, Q; Zhang, X, 2005
)
0.77
"We performed a prospective case series to seek dosage or clinical parameters to better identify patients who need direct medical evaluation."( Toxic clonidine ingestion in children.
Anderson, DL; Colvin, JM; Johnson, PB; Klein-Schwartz, W; Spiller, HA; Villalobos, D, 2005
)
0.81
" Research needs to be done to establish the utility and dosing of apraclonidine for botulinum toxin-induced ptosis."( The use of apraclonidine eyedrops to treat ptosis after the administration of botulinum toxin to the upper face.
Scheinfeld, N, 2005
)
0.92
"1 mg kg(-1), displaced the dose-response curve approximately six-fold to the right."( Postjunctional alpha1-adrenoceptors in the vasculature of the pithed mouse are of the alpha1A-subtype.
Ibarra, M; López-Guerrero, JJ; Villalobos-Molina, R, 2005
)
0.33
"Baseline (vehicle dosed animals) gastrointestinal transit was significantly greater in fasted versus fed rats."( Effects of fasting on evaluation of gastrointestinal transit with charcoal meal.
Hemenway, CL; Mittelstadt, SW; Spruell, RD,
)
0.13
" Advantages, potential side effects, and dosing for multiple modes of delivery are discussed."( Long-term use of clonidine in a critically-ill infant.
Lowery, R; Polaner, DM; Zuk, J, 2005
)
0.67
" Dose-response curves for the alpha1-adrenoceptor agonist phenylephrine were generated in the absence and presence of fentanyl."( Fentanyl attenuates alpha1B-adrenoceptor-mediated pulmonary artery contraction.
Ding, X; McCune, DF; Murray, PA; Perez, DM; Sohn, JT, 2005
)
0.33
" ITC was delivered locally via catheter to the T2-T4 spinal segments and was dosed to reduce heart rate (HR) by >20% to 25%."( Intrathecal clonidine reduces the incidence of ischemia-provoked ventricular arrhythmias in a canine postinfarction heart failure model.
Groh, WJ; Hildebrand, KR; Issa, ZF; Miller, JM; Rosenberger, J; Ujhelyi, MR; Zhou, X; Zipes, DP, 2005
)
0.71
" This study was designed to determine whether data from the American Association of Poison Control Centers Toxic Exposure Surveillance System (TESS) could be utilized to determine a dose-response relationship for pediatric clonidine exposure."( TESS-based dose-response using pediatric clonidine exposures.
Benson, BE; Spyker, DA; Troutman, WG; Watson, WA, 2006
)
0.78
" Exposures reported as a "taste or lick" (n = 51) were included as a dose of 1/10 of the dosage form involved."( TESS-based dose-response using pediatric clonidine exposures.
Benson, BE; Spyker, DA; Troutman, WG; Watson, WA, 2006
)
0.6
"TESS data can provide the basis for a statistically sound description of dose-response for pediatric clonidine poisoning exposures."( TESS-based dose-response using pediatric clonidine exposures.
Benson, BE; Spyker, DA; Troutman, WG; Watson, WA, 2006
)
0.82
" Dose-response curves were determined for phenylephrine and for several imidazoline ligands, using endothelium denuded, isolated ring segments, of tail arteries from adult male Sprague-Dawley rats."( Centrally acting imidazolines stimulate vascular alpha 1A-adrenergic receptors in Rat-Tail Artery.
Crane, L; Edwards, LP; George, OK; Gonzalez, RR; Kennedy, WB,
)
0.13
" The designed system is able to maintain plasma concentration without the need of frequent dosing and reduce side effects unlike in case of conventional dosage form."( In-vitro studies of tizanidine controlled-release microcapsular matrices.
Dashora, K; Saraf, S, 2006
)
0.33
" Secondary objectives included determining correlations between dosage and age, injury type, location of spasticity, comorbid seizures, or concomitant antispasticity medications."( Oral baclofen and clonidine for treatment of spasticity in children.
Haase, M; Habersang, R; Lubsch, L; Luedtke, S, 2006
)
0.67
" The mean dosage of meperidine used was 76."( The effect of tramadol or clonidine added to intraperitoneal bupivacaine on postoperative pain in total abdominal hysterectomy.
Karamanlioglu, B; Memis, D; Pamukçu, Z; Tükenmez, B; Turan, A,
)
0.43
"Adjuvants are compounds which by themselves have undesirable side-effects or low potency but in combination with opioids allow a reduction of narcotic dosing for postoperative pain control."( Useful adjuvants for postoperative pain management.
Buvanendran, A; Kroin, JS, 2007
)
0.34
" Careful dosing of tizanidine is warranted in small females, whereas male smokers can require higher than average doses."( Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine.
Backman, JT; Neuvonen, PJ; Schröder, MT, 2008
)
0.35
" Cisapride (1, 3 and 10 mg/kg) caused non-significant increases in the indices of gastric emptying, with roughly bell-shaped dose-response curves."( Oral mitemcinal (GM-611), an erythromycin-derived prokinetic, accelerates normal and experimentally delayed gastric emptying in conscious dogs.
Akima, M; Itoh, Z; Kamei, K; Koga, H; Omura, S; Onoma, M; Ozaki, K; Takanashi, H; Yogo, K, 2008
)
0.35
" At 10(-7) M of ST-91, the antagonism was characterized by a rightward shift of isoproterenol dose-response curve (A50=6."( alpha2B-adrenoceptor agonist ST-91 antagonizes beta2-adrenoceptor-mediated relaxation in rat mesenteric artery rings.
Gyires, K; Kató, E; Lipták, L; Mátyus, P; Rónai, AZ; Shujaa, N, 2008
)
0.35
"Tizanidine, an alpha(2)-adrenoceptor agonist, is a short-acting drug with larger interpatient variability, and linear pharmacokinetics that is dosage form-dependent."( A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury.
Henney, HR; Kamen, L; Runyan, JD, 2008
)
0.35
"Tizanidine, one of the few oral antispastic therapies approved for use in the USA, has a narrow therapeutic index that can often make optimal patient dosing difficult."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.35
" Practical advice on tizanidine dosing and/or switching between formulations is provided."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.35
"Scheduled medical uses and dosing of tizanidine in our hospital are shown."( [Protocol for tizanidine use in infantile cerebral palsy].
Arroyo Riaño, O; Benavente Valdepeñas, A; Palazón García, R, 2008
)
0.35
"Treatment with tizanidine was carried out with 1 mg/ day in 18 mo-7 yr old children, 2 mg/day in 7-12 yr old children as initial doses, and for those older than 12 yr similar dosing to that in adults."( [Protocol for tizanidine use in infantile cerebral palsy].
Arroyo Riaño, O; Benavente Valdepeñas, A; Palazón García, R, 2008
)
0.35
" These results provide further evidence that alpha(2)-adrenergic receptor activation shortly after perinatal hypoxia-ischemia can promote neural recovery, but highlight the complex dose-response of exogenous therapy."( Partial neuroprotection with low-dose infusion of the alpha2-adrenergic receptor agonist clonidine after severe hypoxia in preterm fetal sheep.
Bennet, L; Dean, JM; George, S; Gunn, AJ; Mallard, C; Naylor, AS, 2008
)
0.57
" The dosage of PCA drug 0-4 h after operation of the C2 was significantly higher than that of the C4 group."( [Effects of epidural clonidine pretreatment in epidural patient-controlled analgesia using sufentanil combined with levobupivacaine].
Ruan, XC; She, SZ; Su, J; Xie, XQ; Xu, LX, 2008
)
0.66
" When the animals were again tested 48 hours after dosing (no pretreatment), these two patterns of task enhancement were continued and enhanced."( Protracted cognitive effects produced by clonidine in Macaca nemestrina performing a delayed matching task.
Blessing, D; Buccafusco, JJ; Kille, N; Terry, AV; Webster, SJ, 2009
)
0.62
" In the mouse formalin test, DBV injection produced a dramatic leftward shift in the dose-response curve for clonidine-induced analgesia."( Acupoint stimulation with diluted bee venom (apipuncture) potentiates the analgesic effect of intrathecal clonidine in the rodent formalin test and in a neuropathic pain model.
Beitz, AJ; Han, HJ; Kim, HW; Kwon, YB; Lee, HJ; Lee, JH; Roh, DH; Seo, HS; Yoon, SY, 2009
)
0.78
" Serial blood and urine samples were collected in 17 women during mid to late pregnancy over one steady-state dosing interval to determine clonidine noncompartmental pharmacokinetic parameters (n = 17) and creatinine clearance."( Clonidine pharmacokinetics in pregnancy.
Buchanan, ML; Carr, DB; Easterling, TR; Hebert, MF; Mattison, DR; Nelson, WL; Risler, LJ; Shen, DD, 2009
)
2
"The objective of this study was to investigate lofexidine urine and plasma pharmacokinetics using three different dosing regimens in opioid dependent subjects."( Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients.
Abbassi, M; Al Ghananeem, AM; Herman, BH; Ling, W; Miotto, K; Montgomery, A; O'Brien, CP; Walsh, R; Yu, E, 2009
)
0.35
" The dosing regimens of lofexidine hydrochloride were ."( Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients.
Abbassi, M; Al Ghananeem, AM; Herman, BH; Ling, W; Miotto, K; Montgomery, A; O'Brien, CP; Walsh, R; Yu, E, 2009
)
0.35
"8 mg TID dosing regimens did not seem to be different at steady state (day 15)."( Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients.
Abbassi, M; Al Ghananeem, AM; Herman, BH; Ling, W; Miotto, K; Montgomery, A; O'Brien, CP; Walsh, R; Yu, E, 2009
)
0.35
" The amount dispensed was a 30-day supply but the bottle was empty on day 19, leading us to suspect a possible accelerated dosing error."( Toxicity from a clonidine suspension.
Benson, B; Farooqi, M; Johnson, M; Kunkel, S; Seifert, S, 2009
)
0.7
"Compounding and liquid dosing errors are common in children and may result in massive overdoses."( Toxicity from a clonidine suspension.
Benson, B; Farooqi, M; Johnson, M; Kunkel, S; Seifert, S, 2009
)
0.7
" The trial was stopped after completion of the 3rd dosing level."( A phase II clinical trial to assess the safety of clonidine in acute organophosphorus pesticide poisoning.
Abeysinghe, C; Buckley, NA; Dawson, AH; Hettiarachchi, R; Jayamanna, SF; Karunatilake, H; Perera, PM, 2009
)
0.61
" Diagnosis is based on a steady increase in intrathecal morphine dosage after a relatively prolonged period of stability, on the gradual development of neurologic signs and symptoms suggesting radicular or spinal cord compression, and on magnetic resonance images."( [Spinal granuloma in a patient receiving a spinal infusion of morphine and clonidine].
Abejón, D; del Pozo, C; del Saz, JM; Ley, L; Sánchez, MR,
)
0.36
" Dexmethylphenidate XR is a stimulant treatment in a single isomer form, and has an efficacy and tolerability similar to two doses of immediate-release (IR) dexmethylphenidate when taken 4 hours apart, but is dosed at half of the usual d,l-methylphenidate dose."( Attention-deficit hyperactivity disorder: recent advances in paediatric pharmacotherapy.
Kratochvil, CJ; May, DE, 2010
)
0.36
"To review the pharmacology, toxicology, pharmacokinetics, efficacy, adverse effects, drug interactions, and dosage guidelines for lofexidine, an alpha(2)-agonist, for opioid detoxification."( Lofexidine, an {alpha}2-receptor agonist for opioid detoxification.
Gish, EC; Honey, BL; Johnson, PN; Miller, JL, 2010
)
0.36
" Further large-scale controlled studies are needed to identify the safest, most effective dosage regimen required to achieve opioid detoxification."( Lofexidine, an {alpha}2-receptor agonist for opioid detoxification.
Gish, EC; Honey, BL; Johnson, PN; Miller, JL, 2010
)
0.36
"The objective of this study was to formulate stable and controlled release microparticles for simultaneous delivery and UV spectrophotometric detection in combined dosage of an non-steroidal anti-inflammatory drug (NSAID) (nimesulide, NMS) and a spasmolytic agent (tizanidine, TZN) to maintain plasma concentration that may increase patients compliance, improved therapeutic efficacy, The aim was also to reduce severity of upper GI side effects of NMS because of alteration in delivery pattern via slow release of drug from microparticles and to increase the benefits of spasticity and disability for spastic patients by administering TZN in a modified release formulation as these two drugs are often prescribed in combination for the management of pain associated with muscles spasm."( Formulation of two-drug controlled release non-biodegradable microparticles for potential treatment of muscles pain and spasm and their simultaneous spectrophotometeric estimation.
Aamir, MN; Ahmad, M; Akhtar, N; Khan, SA; Kousar, R; Murtaza, G,
)
0.13
" Undisturbed telemetry BP data were continuously collected for at least 24h following dosing and analyzed."( Evaluation of blood pressure measurement using a miniature blood pressure transmitter with jacketed external telemetry in cynomolgus monkeys.
Jenkins, AC; Klein, JL; McMahon, C; Mitchell, AZ; Sarazan, RD,
)
0.13
" These findings may have implications for dosing of local anesthetics in diabetic patients undergoing regional analgesia with nerve blocks."( Local anesthetic sciatic nerve block and nerve fiber damage in diabetic rats.
Buvanendran, A; Kerns, JM; Kroin, JS; Moric, M; Tuman, KJ; Wagenaar, B; Williams, DK,
)
0.13
" After confirmation of the established allodynia, gabapentin at 10, 30, 60 and 100μg or clonidine at 5, 15, 30 and 50μg was injected as a monotherapy in conscious rats through the intrathecal catheter to obtain the dose-response curve of %MPE (maximum possible effect) of the antiallodynic effect and its ED(50)."( Intrathecal gabapentin and clonidine synergistically inhibit allodynia in spinal nerve-ligated rats.
Asada, A; Funao, T; Mori, T; Nishikawa, K; Yamama, Y, 2010
)
0.88
" We investigated the effect of the addition of clonidine to the MLAC of levobupivacaine in a randomized controlled dose-response trial."( Effect of epidural clonidine on minimum local anesthetic concentration (ED50) of levobupivacaine for caudal block in children.
Alberighi, OD; Disma, N; Frawley, G; Mameli, L; Montobbio, G; Pistorio, A; Tuo, P, 2011
)
0.95
" To reduce muscle tension, 34 patients of the main group received tizanidine with the modified release of active substance (sirdalud MR) in dosage one capsule (6 mg) per day."( [The use of sirdalud MR in patients with multiple sclerosis].
Batysheva, TT; Boĭko, AN; Kamchatnov, PR; Petrov, SV; Popova, NF; Zaĭtsev, KA, 2010
)
0.36
" A description of the pharmacological action of each adjuvant is given followed by a review of randomised control trials, dosage and notable papers on the subject."( Adjuvants to local anaesthesia in ophthalmic surgery.
Adams, L, 2011
)
0.37
"Administering preoperative oral clonidine in a dosage of 5 μg/kg, 2 h before phacoemulsification, significantly decreases the prevalence and intensity of acute postoperative IOP rise in those undergoing general anesthesia."( Effect of oral clonidine on acute intraocular pressure rise after phacoemulsification: a prospective double-blind, randomized, clinical trial.
Boroojeny, SB; Fard, MM; Ghaffarpasand, F; Hourang, MH; Zakeri, H; Zeraatian, S, 2011
)
1.01
" Single application of tritiated water and [(14) C]-clonidine HCl were dosed at the same time on dermatomed human skin samples collected from 12 donors in a flow through diffusion cell system."( Ability to estimate relative percutaneous penetration via a surrogate maker - trans epidermal water loss?
Chan, H; Elkeeb, R; Hui, X; Maibach, HI, 2012
)
0.63
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" At each daily visit, signs and symptoms were assessed, and medications and dosing instructions were given for the following 24 hours."( A nonopioid procedure for outpatient opioid detoxification.
Baier, AR; Coons, EE; Fingesten, A; Ockert, DM; Volpicelli, JR, 2011
)
0.37
"Many drugs are unavailable in suitable paediatric dosage forms."( Development and validation of a paediatric oral formulation of clonidine hydrochloride.
Boedhram, RR; de Goede, AL; Eckhardt, M; Hanff, LM; Koch, BC; Vermaat, CH; Vermes, A, 2012
)
0.62
" Specifically, we assessed clonidine dosage in relation to a) plasma concentration levels, b) orthostatic cardiovascular responses, and c) possible adverse effects."( Clonidine in the treatment of adolescent chronic fatigue syndrome: a pilot study for the NorCAPITAL trial.
Andersen, AM; Fagermoen, E; Saul, JP; Sulheim, D; Thaulow, E; Vethe, NT; Winger, A; Wyller, VB, 2012
)
2.12
" Therefore, we asked if a physiologically based pharmacokinetic (PBPK) model could be used to evaluate different dosing regimens for pregnant women."( A physiologically based pharmacokinetic model to predict disposition of CYP2D6 and CYP1A2 metabolized drugs in pregnant women.
Isoherranen, N; Ke, AB; Nallani, SC; Rostami-Hodjegan, A; Unadkat, JD; Zhao, P, 2013
)
0.39
" Isobolographic analyses of dose-response curves determined whether interactions were synergistic or additive."( The delta-opioid receptor is sufficient, but not necessary, for spinal opioid-adrenergic analgesic synergy.
Chabot-Doré, AJ; Millecamps, M; Stone, LS, 2013
)
0.39
" Despite heterogeneity between trials, clonidine premedication in an adequate dosage (4 µg/kg) was likely to have a beneficial effect on postoperative pain in children."( Clonidine premedication for postoperative analgesia in children.
Cyna, AM; Knight, N; Lambert, P; Middleton, P, 2014
)
2.11
" Mean pulmonary arterial pressure and dosage of dobutamine and sodium nitroprusside were assessed four times: before intravenous administration of clonidine (2 μg/kg) or placebo (T0), 30 min after tested treatment and before cardiopulmonary bypass (T1), immediately after CPB (T2), 10 min after protamine injection (T3)."( Intravenous clonidine administration and its ability to reduce pulmonary arterial pressure in patients undergoing heart surgery.
Bueno, RM; de Oliveira-Júnior, IS; do Amaral, JL; Falcão, LF; Ferez, D; João, BB; Perez, MV,
)
0.71
"Each of the single topical drugs produced significant dose-dependent antiallodynic effects compared with vehicle in CPIP rats (N = 30), and the antiallodynic dose-response curves of either PA or PDE inhibitors were shifted 5- to 10-fold to the left when combined with nonanalgesic doses of α2A receptor agonists or NO donors (N = 28)."( Topical combinations to treat microvascular dysfunction of chronic postischemia pain.
Abaji, R; Coderre, TJ; Laferrière, A; Ragavendran, JV; Tsai, CY, 2014
)
0.4
" Dose-response curve for inhibitory action of WIN 55,212-2 was shifted to the right after 4-h incubation with clonidine (3 × 10(-10) m) comparing to the untreated tissues (pD2  = 5."( Pretreatment with clonidine caused desensitization to WIN 55,212-2 in guinea pig ileum.
Dehpour, AR; Ejtemaei Mehr, S; Mohaghegh Shalmani, L; Rahimian, R; Rezania, F,
)
0.68
"Oral dosage forms and traditional transdermal patches are inadequate for complex clonidine therapy dosing schemes, because of the variable dose/flux requirement for the treatment of opioid withdrawal symptoms."( Programmable transdermal clonidine delivery through voltage-gated carbon nanotube membranes.
Hammell, D; Hinds, BJ; Paudel, KS; Pinninti, RR; Stinchcomb, A; Strasinger, C; Wu, J, 2014
)
0.93
"This study was conducted to assess the effects of various excipients in 10 different Tizanidine hydrochloride tablet dosage forms that were prepared by direct compression method (DC)."( Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression.
Anjum, F; Ghayas, S; Khan, LG; Razvi, N; Siddiqui, SA, 2014
)
0.4
" The drug should be gradually reduced in dosage under observation by a psychiatrist."( [Tizanidine withdrawal symptoms in stress cardiomyopathy].
Bayer, D; Bengesser, SA; Kapfhammer, HP; Mörkl, S; Schöggl, H, 2015
)
0.42
" 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 regimen, preoperative anxiety outcome measures and postoperative anxiety outcome measures."( Melatonin for pre- and postoperative anxiety in adults.
Gögenur, I; Halladin, NL; Hansen, MV; Møller, AM; Rosenberg, J, 2015
)
0.42
" Following botulinum toxin A treatment, clinical improvement led to the gradual reduction of baclofen or tizanidine dosing to one-third of the former dose."( Comparison of Efficacy and Side Effects of Oral Baclofen Versus Tizanidine Therapy with Adjuvant Botulinum Toxin Type A in Children With Cerebral Palsy and Spastic Equinus Foot Deformity.
Aksoy, SN; Dai, AI; Demiryürek, AT, 2016
)
0.43
" However, it will first be necessary to optimize the timing and dosing required to inhibit xenoantibodies in vivo."( Clonidine inhibits anti-non-Gal IgM xenoantibody elicited in multiple pig-to-primate models.
Cowan, PJ; d'Apice, AJ; Hawthorne, WJ; Kearns-Jonker, M; Nottle, MB; O'Connell, PJ; Salvaris, EJ; Stewart, JM; Tarantal, AF,
)
1.57
" The concurrent administration of SB203580 reduces the dosage requirements for clonidine, thereby alleviating allodynia without producing undesirable motor or cardiovascular effects."( Clonidine, an alpha-2 adrenoceptor agonist relieves mechanical allodynia in oxaliplatin-induced neuropathic mice; potentiation by spinal p38 MAPK inhibition without motor dysfunction and hypotension.
Beitz, AJ; Kim, SJ; Lee, JH; Oh, SB; Roh, DH; Yeo, JH; Yoon, SY, 2016
)
2.1
"Treating animals repeatedly with intermittent and increasing morphine doses has been suggested to allow some withdrawal during each dosing interval, which causes repeated stress."( Spontaneous withdrawal in intermittent morphine administration in rats and mice: effect of clonidine coadministration and sex-related differences.
Allahverdiyev, O; Enginar, N; Nurten, A; Sehirli, I; Türkmen, AZ, 2015
)
0.64
"Male and female rats and mice were administered with increasing doses of morphine twice daily at different dosing intervals."( Spontaneous withdrawal in intermittent morphine administration in rats and mice: effect of clonidine coadministration and sex-related differences.
Allahverdiyev, O; Enginar, N; Nurten, A; Sehirli, I; Türkmen, AZ, 2015
)
0.64
"Male rats and male and female rats displayed manifestations of morphine withdrawal at the end of 14-h and 24-h dosing intervals, respectively."( Spontaneous withdrawal in intermittent morphine administration in rats and mice: effect of clonidine coadministration and sex-related differences.
Allahverdiyev, O; Enginar, N; Nurten, A; Sehirli, I; Türkmen, AZ, 2015
)
0.64
"Mini-tablets are increasingly gaining attention in solid dosage form design as multiple-unit systems combining different active compounds and providing a single or combined pattern of modified release for polypharmacy or combined treatments."( Mini-tablet combination for sustained release of clonidine hydrochloride and hydrochlorothiazide: Preparation and pharmacokinetics in beagle dogs.
Wang, Y; Xu, B; Zhu, H, 2016
)
0.69
" The IR forms, while themselves not FDA approved for ADHD, may, with dosage adjustment, be reasonable alternatives (with considerable cost savings)."( Treating ADHD in Prison: Focus on Alpha-2 Agonists (Clonidine and Guanfacine).
Mattes, JA, 2016
)
0.68
" Planned subgroup analyses include specific alpha-2 agonist agent, study design, clinical diagnosis, dosing regimen, and use of adjunctive agents."( Alpha-2 agonists for sedation in mechanically ventilated neurocritical care patients: a systematic review protocol.
Blinder, H; English, S; Hutton, B; Tran, A, 2016
)
0.43
" Publications were grouped into different dosage forms and assessed for their potential application for sedation of children in intensive care."( A mini-review of non-parenteral clonidine preparations for paediatric sedation.
Hanning, SM; Neubert, A; Orlu Gul, M; Toni, I; Tuleu, C, 2017
)
0.74
"These results demonstrate the safety, efficacy, and tolerability of low-dose naltrexone, in conjunction with single-day buprenorphine dosing and adjunctive nonopioid medications, for initiating adults with opioid dependence to XR-naltrexone."( Long-Acting Injectable Naltrexone Induction: A Randomized Trial of Outpatient Opioid Detoxification With Naltrexone Versus Buprenorphine.
Bisaga, A; Carpenter, KM; Choi, CJ; Dakwar, E; Levin, FR; Mariani, JJ; Mishlen, K; Nunes, EV; Pavlicova, M; Sullivan, M, 2017
)
0.46
" The aim of this study is to describe clonidine PK in a particular ECMO system and propose dosing guidelines for children on this particular ECMO circuit."( Population pharmacokinetics of intravenous clonidine for sedation during paediatric extracorporeal membrane oxygenation and continuous venovenous hemofiltration.
Ahsman, MJ; de Wildt, SN; Kleiber, N; Mathôt, RAA; Tibboel, D; Wildschut, ED, 2017
)
0.99
" The PK parameters on ECMO and the dosing guidelines proposed hold the potential to improve sedation practices on ECMO but need to be repeated with different ECMO systems."( Population pharmacokinetics of intravenous clonidine for sedation during paediatric extracorporeal membrane oxygenation and continuous venovenous hemofiltration.
Ahsman, MJ; de Wildt, SN; Kleiber, N; Mathôt, RAA; Tibboel, D; Wildschut, ED, 2017
)
0.72
" In summary, our findings suggest that clonidine above 1/32 of its clinical therapeutic dosage is cytotoxic to corneal epithelial cells by inducing cell apoptosis both in vitro and in vivo, and its pro-apoptotic effect on HCEP cells is triggered by a Fas/TNFR1 death receptors-mediated, mitochondria-dependent signaling pathway."( Clonidine Induces Apoptosis of Human Corneal Epithelial Cells through Death Receptors-Mediated, Mitochondria-Dependent Signaling Pathway.
Fan, D; Fan, TJ, 2017
)
2.17
"To evaluate the safety, efficacy and effective dosage of clonidine in the outpatient (OP) management of secondary dystonia."( Clonidine use in the outpatient management of severe secondary dystonia.
Kaminska, M; Lin, JP; Lumsden, DE; Sayer, C, 2017
)
2.14
" This is especially important in the case of pediatric patients, and dose-response relationships require studies using pharmacokinetic-pharmacodynamic modeling."( A highly sensitive method for the simultaneous UHPLC-MS/MS analysis of clonidine, morphine, midazolam and their metabolites in blood plasma using HFIP as the eluent additive.
Aro, R; Herodes, K; Kipper, K; Lutsar, I; Metsvaht, T; Standing, JF; Veigure, R, 2017
)
0.69
" As health care professionals, it is prudent to be familiar with their dosing regimens, common adverse effects, and the monitoring required to maximize patient benefits and minimize harms."( Oral Agents for the Management of Agitation and Agitated Delirium in Critically Ill Patients.
Hammond, DA; Smith, MN; Wiley, TL; Yeo, QM,
)
0.13
" The proposed method was validated according to the ICH guidelines and was successfully applied to the analysis of these drugs in their tablet dosage forms with high accuracy."( Simultaneous Determination of Tizanidine, Nimesulide, Aceclofenac and Paracetamol in Tablets and Biological Fluids Using Micellar Liquid Chromatography.
Belal, F; Derayea, S; Hammad, MA; Omar, MA; Saleh, SF; Zayed, S, 2018
)
0.48
" In further studies, different doses should be explored to determine what dosage of clonidine may offer hemodynamic protection as well as decrease sedative drugs needed."( Clonidine as a preoperative sedative.
Challman, SD; Henry, RG; Kouzoukas, DE; Raybould, TP; Romond, K, 2018
)
2.15
" In one study, tics limited further dosage increases of methylphenidate."( Pharmacological treatment for attention deficit hyperactivity disorder (ADHD) in children with comorbid tic disorders.
Osland, ST; Pringsheim, T; Steeves, TD, 2018
)
0.48
" Because of the lack of land suitable for commercial management, pediatric specialties very often need to prepare extemporaneous formulations to improve the dosage and administration of drugs for children."( Physicochemical and microbiological stability of two news oral liquid formulations of clonidine hydrochloride for pediatric patients.
Cameán-Fernández, M; Cañete, C; Dávila-Pousa, MC; Delgado-Valverde, M; García-Palomo, M; López-Rojas, R; Merino-Bohórquez, V; Rodriguez-Marrodán, B; Villaronga, M, 2019
)
0.74
" Secondarily, dosing of opioids and benzodiazepines was examined."( The Effectiveness of α2 Agonists As Sedatives in Pediatric Critical Care: A Propensity Score-Matched Cohort Study.
Breatnach, CV; Cousins, G; Dawkins, I; Doherty, DR; Gallagher, PJ; Hayden, JC; Healy, M; Leacy, FP, 2019
)
0.51
" A variety of dosage regimens have been utilized in clinical practice and in research studies."( Optimizing clonidine dosage for sedation in mechanically ventilated children: A pharmacokinetic simulation study.
Bardol, M; Breatnach, CV; Cousins, G; Dawkins, I; Doherty, DR; Gallagher, PJ; Hayden, JC; Healy, M; Standing, JF, 2019
)
0.9
"This study aims to propose a target plasma concentration and simulate clonidine pharmacokinetics (PK) in a cohort of mechanically ventilated children to evaluate the adequacy of clonidine dosage regimens used in clinical practice and research studies."( Optimizing clonidine dosage for sedation in mechanically ventilated children: A pharmacokinetic simulation study.
Bardol, M; Breatnach, CV; Cousins, G; Dawkins, I; Doherty, DR; Gallagher, PJ; Hayden, JC; Healy, M; Standing, JF, 2019
)
1.14
" Nine dosage regimens (four intravenous boluses, four intravenous infusions, and one nasogastric route boluses) were evaluated ranging from 1 µg/kg eight hourly intravenous boluses to a regimen up to 3 µg/kg/hr continuous intravenous infusion."( Optimizing clonidine dosage for sedation in mechanically ventilated children: A pharmacokinetic simulation study.
Bardol, M; Breatnach, CV; Cousins, G; Dawkins, I; Doherty, DR; Gallagher, PJ; Hayden, JC; Healy, M; Standing, JF, 2019
)
0.9
"The variety of dosage regimens in the previous studies of clonidine along with difficulties in the conduct of interventional studies may have contributed to the lack of efficacy data to support its use."( Optimizing clonidine dosage for sedation in mechanically ventilated children: A pharmacokinetic simulation study.
Bardol, M; Breatnach, CV; Cousins, G; Dawkins, I; Doherty, DR; Gallagher, PJ; Hayden, JC; Healy, M; Standing, JF, 2019
)
1.15
" The presently available oral dosage form has limitations such as high first pass metabolism resulting in low oral bioavailability."( Microneedle-Mediated Transdermal Delivery of Tizanidine Hydrochloride.
Pandya, K; Patel, B; Thakkar, H, 2020
)
0.56
"The aim of this study was to investigate the population pharmacokinetics (PK) of clonidine in intensive care unit (ICU) patients in order to develop a dosing regimen for sedation."( Optimising the dose of clonidine to achieve sedation in intensive care unit patients with population pharmacokinetics.
Arbouw, MEL; Bles, CMA; Cloesmeijer, ME; de Meijer, AR; Kruisdijk-Gerritsen, A; Mathôt, RAA; Nassikovker, P; van den Oever, HLA; van Steveninck, FL; Zeeman, M, 2020
)
1.1
" A dosing regimen of 1200 μg/d provided a target sedation concentration of >1."( Optimising the dose of clonidine to achieve sedation in intensive care unit patients with population pharmacokinetics.
Arbouw, MEL; Bles, CMA; Cloesmeijer, ME; de Meijer, AR; Kruisdijk-Gerritsen, A; Mathôt, RAA; Nassikovker, P; van den Oever, HLA; van Steveninck, FL; Zeeman, M, 2020
)
0.87
" Blood samples were drawn at baseline, 5, 10, 15, 30, 60 minutes after dosing and additionally every hour until discharge from the PACU."( Pharmacokinetics of an intravenous bolus dose of clonidine in children undergoing surgery.
Afshari, A; Anderson, BJ; Falcon, L; Henneberg, SW; Lauritsen, T; Lomstein, E; Nielsen, BN; Ydemann, M, 2020
)
0.81
" Clonidine can be compounded as a liquid formula for patients who are unable to take pills, however, this can add to the risk of dosing errors."( Clonidine Compounding Error: Bradycardia and Sedation in a Pediatric Patient.
Barbuto, AF; Burns, MM, 2020
)
2.91
"To allow for tailored dosing and overcome swallowing difficulties, compounded liquid medication is often required in pediatric patients."( Stability of Azathioprine, Clonidine Hydrochloride, Clopidogrel Bisulfate, Ethambutol Hydrochloride, Griseofulvin, Hydralazine Hydrochloride, Nitrofurantoin, and Thioguanine Oral Suspensions Compounded with SyrSpend SF pH4.
Anagnostou, K; Cunha, CN; da Silva, SL; Dijkers, E; Ferreira, AO; Polonini, H,
)
0.43
" 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 currently available oral dosage forms exhibit low oral bioavailability due to high first-pass metabolism."( Derma roller mediated transdermal delivery of tizanidine invasomes for the management of skeletal muscle spasms.
Brahmam, B; Chaudhari, P; Dsouza, L; Lewis, SA, 2021
)
0.62
" Our objectives were to describe clonidine dosing regimens used for sedation and analgesia in critically ill adults, the associated adverse effects (i."( High-versus low-dose clonidine for sedation and analgesia in critically ill adults: A retrospective cohort study.
Burry, L; Cheung, A; Coleman, B; Guenette, M; Purivatra, E, 2021
)
1.22
"The fast-dissolving film of TNZ HCl was prepared by the solvent-casting method and characterized using scanning electron microscopy, FTIR, and XRD, and evaluated for critical quality attributes for this type of dosage form such as disintegration time, tensile strength, drug content, dissolution, and ex vivo permeability."( Development of Biocompatible Nanoparticles of Tizanidine Hydrochloride in Orodispersible Films:
Dutt, R; Kaushik, D; Mittal, V; Pandey, P; Rahman, MH; Singh, S; Sinha, S; Thapa, S; Verma, R, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
clonidine
clonidine
imidazolineAn imidazoline compound having the double bond at the 2-position.
[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 (59)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency5.01195.623417.292931.6228AID485281
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
acetylcholinesteraseHomo sapiens (human)Potency0.15490.002541.796015,848.9004AID1347398
AR proteinHomo sapiens (human)Potency33.49150.000221.22318,912.5098AID743042
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.58930.00137.762544.6684AID914; AID915
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency2.98490.001022.650876.6163AID1224838
regulator of G-protein signaling 4Homo sapiens (human)Potency21.19230.531815.435837.6858AID504845
cytochrome P450 2D6Homo sapiens (human)Potency17.37680.00108.379861.1304AID1645840
arylsulfatase AHomo sapiens (human)Potency0.04261.069113.955137.9330AID720538
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency19.25130.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency5.01190.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency7.94330.00636.904339.8107AID883
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.53580.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency17.88160.891312.067628.1838AID1487
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.94330.00638.235039.8107AID883
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency3.54810.009610.525035.4813AID1479145
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency31.62281.000010.475628.1838AID901
[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)
Membrane primary amine oxidase Rattus norvegicus (Norway rat)Ki900.000010.000010.000010.0000AID202892
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)20.79000.21005.553710.0000AID1442001; AID386625
Solute carrier family 22 member 1 Homo sapiens (human)Ki0.55000.55004.26507.4600AID681146
Solute carrier family 22 member 3Homo sapiens (human)IC50 (µMol)79.30000.09003.72779.5000AID679482
Solute carrier family 22 member 3Homo sapiens (human)Ki373.00000.12000.12000.1200AID681584
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki3.23590.00010.532610.0000AID682996
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.10100.00001.44217.3470AID35898; AID36188; AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.14370.00010.807410.0000AID1195979; AID1306485; AID35934; AID35946; AID35950; AID625201; AID671634
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.37570.00010.949010.0000AID35271; AID35412; AID35422; AID35430; AID35437; AID37303
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.03530.00001.23808.1590AID35898; AID36188; AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.02450.00020.725710.0000AID1195979; AID625202; AID671635
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01150.00001.47257.8980AID35898; AID36188
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.04660.00030.483410.0000AID1195979; AID36396; AID36404; AID36407; AID671636
DRattus norvegicus (Norway rat)Ki4.00000.00010.610010.0000AID63016
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki4.00000.00010.25675.8000AID63016
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)5.36500.00031.38338.4000AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki3.06600.00010.739610.0000AID625190
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01730.00031.09147.7625AID219808
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.03160.00000.929610.0000AID35187; AID35192; AID36251; AID36373; AID36375; AID37082; AID37381; AID552774
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki0.10000.00192.379710.0000AID223241
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01730.00031.09147.7625AID219808
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.01520.00000.970810.0000AID35187; AID35192; AID37082; AID37381; AID552774
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01730.00031.06917.7625AID219808
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.11620.00000.937510.0000AID35187; AID35192; AID36094; AID36551; AID36555; AID37082; AID37381; AID552774
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.37570.00000.575110.0000AID35271; AID35412; AID35422; AID35430; AID35437; AID37303
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)1.21000.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.40580.00000.360910.0000AID36104; AID36128; AID36251; AID625200
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki4.00000.00020.24622.0000AID63016
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki0.10000.00061.777110.0000AID223241
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)5.36500.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki3.06600.00031.29679.2440AID625190
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki4.00000.00020.18872.0000AID63016
Delta-type opioid receptorMus musculus (house mouse)Ki0.01410.00000.53939.4000AID1195978
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.34280.00000.272610.0000AID36104; AID36128; AID36251
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.34280.00000.471310.0000AID36104; AID36128; AID36251
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.37570.00000.965010.0000AID35271; AID35412; AID35422; AID35430; AID35437; AID37303
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)22.60002.03005.53139.9000AID386625
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki4.00000.00000.437510.0000AID63016
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.01410.00000.27869.0000AID1195978
Alpha-2A adrenergic receptorBos taurus (cattle)IC50 (µMol)0.00200.00200.49073.8430AID35898
NischarinRattus norvegicus (Norway rat)IC50 (µMol)0.36620.36620.36620.3662AID371645; AID552772
NischarinRattus norvegicus (Norway rat)Ki0.14060.00080.13881.2589AID1195978; AID1306516; AID671632
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki1.40000.13002.37856.9000AID681376
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)33.30000.01002.765610.0000AID721754
NischarinHomo sapiens (human)Ki0.03220.00420.21923.8019AID223225; AID223226; AID342861
[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)
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Kd51.45320.00000.53588.3176AID39946; AID39947
Alpha-1B adrenergic receptor Cricetulus griseus (Chinese hamster)EC50 (µMol)0.08300.01000.34440.9430AID1342011
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)EC50 (µMol)0.00830.00830.00830.0083AID536933
Alpha-2A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.02090.00080.37336.7100AID1297521; AID1306486; AID1342005; AID36512; AID536933; AID550035; AID636210
Alpha-2B adrenergic receptorHomo sapiens (human)EC50 (µMol)0.40490.00051.36446.7100AID1297521; AID36512; AID536937
Alpha-1A adrenergic receptorBos taurus (cattle)EC50 (µMol)0.08900.00900.37401.1320AID1342009
Alpha-2C adrenergic receptorHomo sapiens (human)EC50 (µMol)0.03830.00050.55416.7100AID1297521; AID1342007; AID36512; AID536941
Alpha-1D adrenergic receptorHomo sapiens (human)EC50 (µMol)0.29000.00151.72275.6000AID36261
Adenosine receptor A2bRattus norvegicus (Norway rat)EC50 (µMol)0.00440.00190.19330.7200AID36512
Adenosine receptor A2aRattus norvegicus (Norway rat)EC50 (µMol)0.00440.00000.11560.7200AID36512
Alpha-1A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.29000.00010.50987.1000AID36261
Alpha-1B adrenergic receptorHomo sapiens (human)EC50 (µMol)0.29000.00011.30105.6000AID36261
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.25700.00020.51397.5858AID36159
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)Activity0.71000.71005.30179.7000AID681117
Alpha-2B adrenergic receptorMus musculus (house mouse)IC40 (µMol)0.00370.00370.04080.0780AID36357
Alpha-2C adrenergic receptorMus musculus (house mouse)IC40 (µMol)0.00370.00370.04080.0780AID36357
Alpha-2A adrenergic receptorMus musculus (house mouse)IC40 (µMol)0.00370.00370.04080.0780AID36357
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (154)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
histamine metabolic processSolute carrier family 22 member 3Homo sapiens (human)
organic cation transportSolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 3Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 3Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 3Homo sapiens (human)
serotonin transportSolute carrier family 22 member 3Homo sapiens (human)
organic cation transportSolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 3Homo sapiens (human)
organic anion transportSolute carrier family 22 member 3Homo sapiens (human)
monocarboxylic acid transportSolute carrier family 22 member 3Homo sapiens (human)
monoamine transportSolute carrier family 22 member 3Homo sapiens (human)
spermidine transportSolute carrier family 22 member 3Homo sapiens (human)
dopamine transportSolute carrier family 22 member 3Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 3Homo sapiens (human)
regulation of appetiteSolute carrier family 22 member 3Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 3Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 3Homo sapiens (human)
histamine transportSolute carrier family 22 member 3Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 3Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 3Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 3Homo sapiens (human)
epinephrine uptakeSolute carrier family 22 member 3Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 3Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 3Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 3Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 3Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 3Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1A adrenergic receptorBos taurus (cattle)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of cardiac muscle contractionAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2A adrenergic receptorBos taurus (cattle)
regulation of vasoconstrictionAlpha-2A adrenergic receptorBos taurus (cattle)
platelet activationAlpha-2A adrenergic receptorBos taurus (cattle)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (51)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
protein bindingSolute carrier family 22 member 3Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (38)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
nuclear outer membraneSolute carrier family 22 member 3Homo sapiens (human)
plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
endomembrane systemSolute carrier family 22 member 3Homo sapiens (human)
membraneSolute carrier family 22 member 3Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
mitochondrial membraneSolute carrier family 22 member 3Homo sapiens (human)
neuronal cell bodySolute carrier family 22 member 3Homo sapiens (human)
presynapseSolute carrier family 22 member 3Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1A adrenergic receptorBos taurus (cattle)
caveolaAlpha-1A adrenergic receptorBos taurus (cattle)
nuclear membraneAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (522)

Assay IDTitleYearJournalArticle
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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Subtype-specific stimulation of [35S]GTPgammaS binding by recombinant alpha2-adrenoceptors.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Subtype-specific stimulation of [35S]GTPgammaS binding by recombinant alpha2-adrenoceptors.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1998Biochemical pharmacology, Apr-01, Volume: 55, Issue:7
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1346502Mouse HCN1 (Cyclic nucleotide-regulated channels)2007Circulation, Feb-20, Volume: 115, Issue:7
Direct inhibition of cardiac hyperpolarization-activated cyclic nucleotide-gated pacemaker channels by clonidine.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1998Biochimica et biophysica acta, Nov-19, Volume: 1448, Issue:1
Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1998Biochemical pharmacology, Apr-01, Volume: 55, Issue:7
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Subtype-specific stimulation of [35S]GTPgammaS binding by recombinant alpha2-adrenoceptors.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1998Biochimica et biophysica acta, Nov-19, Volume: 1448, Issue:1
Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
AID1345062Human Organic cation transporter 1 (Organic cation transporters (OCT))1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID1346511Mouse HCN4 (Cyclic nucleotide-regulated channels)2007Circulation, Feb-20, Volume: 115, Issue:7
Direct inhibition of cardiac hyperpolarization-activated cyclic nucleotide-gated pacemaker channels by clonidine.
AID1346533Mouse HCN2 (Cyclic nucleotide-regulated channels)2007Circulation, Feb-20, Volume: 115, Issue:7
Direct inhibition of cardiac hyperpolarization-activated cyclic nucleotide-gated pacemaker channels by clonidine.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1998Biochimica et biophysica acta, Nov-19, Volume: 1448, Issue:1
Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1998Biochemical pharmacology, Apr-01, Volume: 55, Issue:7
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1345920Rat alpha1D-adrenoceptor (Adrenoceptors)1994Molecular pharmacology, Nov, Volume: 46, Issue:5
Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes.
AID174564Change in systolic blood pressure after 50 ug/kg oral administration in spontaneous hypertensive rats after 4 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones.
AID1297522Agonist activity at human recombinant Alpha-2 adrenergic receptor expressed in CHOK1 cells after 30 mins by [35S]GTPgammaS binding assay relative to noradrenaline2016European journal of medicinal chemistry, Jun-10, Volume: 115Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies.
AID172281Effect on heart rate of spontaneously hypertensive rats, 24 hr after peroral administration of 1 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID234209Therapeutic ratio is oral dose producing sedation/reduction in blood pressure; Range is 0.8-1.71980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID552772Inhibition of Sprague-Dawley rat imidazoline I1 receptor2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
New imidazoline/α(2)-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies.
AID1390042Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID349880Permeability across porcine brain lipid coated polyvinylidene fluoride membrane by PAMPA2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1306516Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID1379031Effective permeability of compound at 50 ug/mL after 16 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease.
AID182611Antisecretory activity determined after (sc) administration in rat using rat cholera toxin secretion assay1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Potential antisecretory antidiarrheals. 2. Alpha 2-adrenergic 2-[(aryloxy)alkyl]imidazolines.
AID32094Inhibitory activity against acetylcholinesterase in rat striatal preparation1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID16331Delta logPoct-cyc1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID35430Binding affinity against alpha-1 adrenergic receptor in rat using [3H]prazosin as radioligand1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.
AID58630Oral dose required to cause 20% fall in sedation; Range is 0.25-0.501980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID288192Partition coefficient, log P of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
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.
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.
AID175554Effect of compound on reflux function in spinal transected rats at 50 ug/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID1444094Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID35946Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
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.
AID174075Antihypertensive activity was measured as decrease in systolic blood pressure in spontaneously hypertensive rats at 75 mg/kg, po 5 hours after dosing1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Flavones. 3. Synthesis, biological activities, and conformational analysis of isoflavone derivatives and related compounds.
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.
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.
AID15976Antidiuretic activity was determined expressed as volume of urine excreted in mL was reported at a dose of 100 mg/Kg1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
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.
AID1324013Permeability of the compound at 100 ug/ml after 16 hrs by PAMPA-BBB method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1330773Effective permeability of the compound by PAMPA2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
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.
AID37303Binding affinity for alpha-1 adrenergic receptor in rat liver using [3H]prazosin.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.
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.
AID36551Binding affinity towards alpha-2D adrenergic receptor2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID371646Displacement of [3H]2BFI from imidazoline I2 receptor in Sprague-Dawley rat brain by liquid scintillation counting2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
New analogues of agmatine with higher affinity to imidazoline receptors.
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.
AID172271Effect on heart rate of spontaneously hypertensive rats, 10 hr after peroral administration of 0.3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID513633Induction of autophagy in Atg deficient mouse MFF expressing EGFP-HDQ74 at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
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).
AID172283Effect on heart rate of spontaneously hypertensive rats, 24 hr after peroral administration of 3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID223358Intrinsic activity expressed as ratio of maximum responses to the compound to the maximum response to clonidine in guinea pig vas deferens.1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
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).
AID1453097Effective permeability of the compound at 100 ug/ml incubated for 18 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
AID202892Inhibitory activity against porcine kidney amine oxidase2001Bioorganic & medicinal chemistry letters, Oct-08, Volume: 11, Issue:19
Combinatorial synthesis of SSAO inhibitors using sonogashira coupling: SAR of aryl propargylic amines.
AID513626Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID681584TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HRPE cells2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
AID681146TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID513631Induction of autophagy in human SK-N-MC cells assessed as increase in LC3-2 level at 1 uM after 24 hrs by immunoblotting analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1694879Permeability of compound after 16 hrs by PAMPA-BBB assay2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1491367Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay2017European journal of medicinal chemistry, Sep-08, Volume: 1372-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
AID1195979Displacement of [3H]RX821002 from human alpha2 adrenoceptor expressed in CHO cell membranes after 60 mins2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
AID172286Effect on heart rate of spontaneously hypertensive rats, 2 hr after peroral administration of 1 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID1625123Permeability of the compound in pH 7.4 PBS at 200 uL after 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1192731Permeability of the compound in PBS/EtOH buffer at 100 ug/ml by PAMPA2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID671636Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID386625Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1091955Dissociation constant, pKa of the compound at pH 7.32011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
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.
AID386232Antagonist activity at mu opioid receptor expressed in HEK293 cells assessed as blockade of secreted alkaline phosphatase activity at 1 uM after 6 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
Hemopressin is an inverse agonist of CB1 cannabinoid receptors.
AID536934Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry relative to (-)noradrenaline2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID23716Partition coefficient (logD7.4)1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID49601Hypotensive activity measured as the 20% decrease in mean arterial blood pressure in anesthetized cat1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Two clonidine-like compounds with substituents at the 2-, 3-, and 6-position of the phenyl ring possessing pronounced hypotensive potencies.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID36159The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
AID1150956Octan-1-ol-aqueous buffer partition coefficient, log P of the compound at 10 to 20 mg at pH 7.4 by UV-spectroscopic analysis1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Clonidine and related analogues. Quantitative correlations.
AID671633Displacement of [3H]idazoxan from imidazoline I2 receptor in New Zealand rabbit renal cortex homogenate after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
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.
AID639368Permeability of the compound by PAMPA assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID193681Maximum rate of rise of the left ventricular isovolumetric pressure in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID536933Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID172273Effect on heart rate of spontaneously hypertensive rats, 10 hr after peroral administration of 1 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
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.
AID681955TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.85 uM, Clonidine: 5000 uM) in Xenopus laevis oocytes1997Molecular pharmacology, Jun, Volume: 51, Issue:6
Cloning and functional expression of a human liver organic cation transporter.
AID35898Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors.
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).
AID234208Therapeutic ratio is oral dose producing sedation/reduction in blood pressure1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID197293Changes in diastolic blood pressure following iv administration at (0.108 umol/kg)anesthetized rats2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N(1)-agmatine and synthetic analogues.
AID243662Percent displacement of radioligand from human 5-hydroxytryptamine 1D receptor at 1000 nM2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.
AID1322298Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex at 50 uM after 60 mins by microbeta scintillation counting method
AID232721Selectivity ratio of alpha1/alpha2d2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID1444095Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID168899Intrinsic activity expressed as ratio of maximum responses to the compound to the maximum response to norepinephrine.1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
AID1534777Effective permeability of the compound at 100 mg/ml incubated for 16 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID1491366Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA2017European journal of medicinal chemistry, Sep-08, Volume: 1372-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
AID371647Displacement of [3H]RX821002 from alpha2 adrenoceptor in Sprague-Dawley rat kidney by liquid scintillation counting2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
New analogues of agmatine with higher affinity to imidazoline receptors.
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID1056992Permeability of the compound by PAMPA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
AID1753998Permeability of the compound in PBS/EtOH buffer (7:3) incubated for 16 hrs by UV plate reader based PAMPA-BBB assay2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
AID342861Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID514306Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as induction of rhodopsin expression at 3 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1167634Blood brain permeability of the compound at donor and acceptor by PAMPA assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1292330Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID427197Membrane permeability dissolved in PBS/EtOH (70:30) mixture by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID175551Effect of compound on reflux function in spinal transected rats at 3.1 ug/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID1713987Effective permeability of the compound at 25 ug/ml after 18 hrs by UV plate reader based PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Multitarget-directed oxoisoaporphine derivatives: Anti-acetylcholinesterase, anti-β-amyloid aggregation and enhanced autophagy activity against Alzheimer's disease.
AID1336731Permeability of compound at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1378333Permeability of the compound in PBS/EtOH at 100 mg/ml after 16 hrs by PAMPA2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-β aggregation for the treatment of Alzheimer's disease.
AID1511119Permeability of the compound at 25 ug/ml by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID1437174Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1677627Hypotensive activtiy in mouse assessed as decrease in heart rate at 10 mg/kg2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents.
AID327870Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal2007The Journal of biological chemistry, Sep-14, Volume: 282, Issue:37
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.
AID1319976Permeability of the compound at 25 ug/ml at 7.4 pH after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID1427528Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
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.
AID19260Logarithm of partition coefficient of the neutral form of compound given for octanol/water solvent system1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID37381In vitro binding affinity was measured as the inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor of rat cortical membranes1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
AID620399Permeability of the compound by PAMPA2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors.
AID1201746Permeability of the compound after 16 hrs by PAMPA2015European journal of medicinal chemistry, May-05, Volume: 95Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1264249Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID35772Compound was evaluated for hypotensive activity mediated by Alpha-2 adrenergic receptor; no data2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.
AID550036Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting relative to noradrenaline2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α(2)-adrenoceptor compared to the imidazoline I(1) receptor.
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.
AID1306486Agonist activity at recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane incubated for 30 mins by [35S]GTPgammaS binding assay2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID514302Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as decrease in EGFP-HDQ74 aggregation at 10 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID172285Effect on heart rate of spontaneously hypertensive rats, 2 hr after peroral administration of 0.3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID427196Membrane permeability by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID170825Tested for the change in systolic blood pressure administered at 0.108 ug/kg intravenously in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID1636268Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Design, synthesis and biological evaluation of N-methyl-N-[(1,2,3-triazol-4-yl)alkyl]propargylamines as novel monoamine oxidase B inhibitors.
AID193688Percent change in heart rate expressed in beats / min in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID1167550Permeability of the compound in 70:30 PBS:EtOH by PAMPA-BBB assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease.
AID1677626Hypotensive activity in mouse assessed as decrease in delayed blood pressure at 10 mg/kg2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents.
AID364880Displacement of [3H]RX821002 from alpha2 adrenoceptor in human prefrontal cortex neural membrane2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Novel synthesis and pharmacological evaluation as alpha2-adrenoceptor ligands of O-phenylisouronium salts.
AID36512Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-2 adrenergic receptor1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID1091958Hydrophobicity, log P of the compound in octanol-water by shaking-flask method2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1297521Agonist activity at human recombinant Alpha-2 adrenergic receptor expressed in CHOK1 cells after 30 mins by [35S]GTPgammaS binding assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies.
AID1322296Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat brain cerebral cortex at 50 uM after 30 mins by microbeta scintillation counting method
AID173921Oral dose required to cause 20% fall in sedation1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID1352675Effective permeability at 25 ug/ml after 18 hrs by PAMPA2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID243661Percent displacement of radioligand from human 5-hydroxytryptamine 1B receptor at 1000 nM2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.
AID36396Binding affinity for human Alpha-2C adrenergic receptor1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.
AID681678TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, Clonidine: 500 uM) in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID33250Central hypotensive activity in anesthetized normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
AID219808Compound was tested for its ability to inhibit specific binding of [3H]-clonidine to alpha-2-adrenoceptor.1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Two stereoisomeric imidazoline derivatives: synthesis and optical and alpha 2-adrenoceptor activities.
AID223225Displacement of [3H]-clonidine from bovine imidazoline receptor I-11996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.
AID1056993Permeability of the compound at 100 mg/mL after 10 hrs by PAMPA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
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.
AID37363Compound was tested for the inhibition of [3H]clonidine binding Alpha-2 adrenergic receptor of crude rat brain membrane1982Journal of medicinal chemistry, Jan, Volume: 25, Issue:1
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.
AID15983Antidiuretic activity was determined in SH rats expressed as K(+) (potassium) excreted in milli euivalents was reported for a duration of 5 hours after administration of a dose of 100 mg/Kg.1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
AID1365649Permeability of the compound at 100 mg/ml after 16 hrs by BBB-PAMPA method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Design, synthesis, and evaluation of salicyladimine derivatives as multitarget-directed ligands against Alzheimer's disease.
AID171641Change in diastolic blood pressure after iv administration of 0.108 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID173527Maximum percent decrease in heart rate of spontaneously hypertensive rats, 6 hours after peroral administration of 3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID33252Peripheral hypertensive activity in pithed normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID36188Inhibition of [3H]p-aminoclonidine (PAC) binding to alpha-2 adrenergic receptor of purified human platelet plasma membranes1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1585851Effective permeability of the compound by PAMPA2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1465314Effective permeability of the compound by PAMPA2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1198140Permeability of the compound in PBS and EtOH by PAMPA method2015European journal of medicinal chemistry, Mar-26, Volume: 93Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
AID1666036Effective permeability by PAMPA-BBB penetration assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor.
AID1150959Peripheral adrenergic activity in iv dosed pithed rat assessed as change in mean blood pressure1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Clonidine and related analogues. Quantitative correlations.
AID180083Antihypertensive activity determined as heart rate in SH rats, was reported at a dose of 25 mg/Kg1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
AID36375in vitro alpha-2B adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID550035Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α(2)-adrenoceptor compared to the imidazoline I(1) receptor.
AID1496041Effective permeability of the compound by PAMPA-BBB assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
AID15974Antidiuretic activity was determined expressed as Na+(sodium) excreted in milli euivalents was reported for a duration of 5 hours after administration of a dose of 100 mg/Kg1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
AID175544Effect of compound on hyperreflexia in spinal transected rats at 3.1 ug/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID172288Effect on heart rate of spontaneously hypertensive rats, 2 hr after peroral administration of 3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID35412In vitro binding affinity was measured as the inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat cortical membranes1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
AID36935The compound was evaluated for the alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs clonidine1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
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.
AID1491365Binding affinity to BACE1 (unknown origin) by SPR method2017European journal of medicinal chemistry, Sep-08, Volume: 1372-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
AID1909448Permeability of the compound by PAMPA-BBB assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID1194507Displacement of [3H]clonidine from rat cerebral cortex alpha-2 adrenergic receptor by liquid scintillation counting analysis2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
AID192741Maximum rate of rise of the left ventricular isovolumetric pressure was measured after iv administration of 0.108 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID1139646Permeability of the compound at 5 mg/mL after 18 hrs by PAMPA2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of (e)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides as novel multifunctional neuroprotective agents.
AID536938Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry relative to (-)noradrenaline2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID1150958Hypotensive activity in rat assessed as change in mean blood pressure relative to control1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Clonidine and related analogues. Quantitative correlations.
AID35568In vitro agonist activity against alpha-1 adrenoceptor in rat anococcygeus1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
AID39947The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
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).
AID288185Permeability coefficient through artificial membrane in presence of stirred water layer2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID174893Oral hypotensive activity in spontaneously hypertensive rats by using tail-cuff method measured as change in systolic BP at the dose of 0.25 mg/kg po.1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
2,3-dihydro-3-(1-pyrryl)spiro[benzofuran-2,4'-piperidine]s and 2,3-dihydro-3-(1-pyrryl)spiro[benzofuran-2,3'-pyrrolidine]s: novel antihypertensive agents.
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.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID36128Binding affinity for human brain Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.
AID1192730Permeability of the compound by PAMPA2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1442006Ratio of Kii for human OCT1-ASP+-inhibitor complex to Kis for human OCT1-inhibitor complex by Lineweaver-Burk plot analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
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).
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.
AID671635Displacement of [3H]RX821001 from human alpha2B adrenoceptor expressed in CHO cells after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID342863Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID503832Partial agonist activity at adrenergic alpha2A receptor expressed in HEK293 cells coexpressing yellow fluorescent and cyan fluorescent protein assessed as effect on kinetics of receptor conformational change by FRET assay2005Nature chemical biology, Jun, Volume: 1, Issue:1
Molecular basis of inverse agonism in a G protein-coupled receptor.
AID170661Tested for the change in diastolic blood pressure administered at 0.108 ug/kg intravenously in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID1150957Dissociation constant, pKa of the compound in water-ethyl alcohol1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Clonidine and related analogues. Quantitative correlations.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1347981Permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID681117TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells2003Molecular pharmacology, Mar, Volume: 63, Issue:3
Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1.
AID636211Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting assay relative to noradrenaline2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines.
AID111995Antagonistic activity against Scopolamine induced behavioral deficits in mice; 0/61996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1517838Permeability of the compound in pH 7.4 PBS/EtOH at 25 ug/ml after 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID25092Ionization constant (pKa)1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Direct prediction of dissociation constants (pKa's) of clonidine-like imidazolines, 2-substituted imidazoles, and 1-methyl-2-substituted-imidazoles from 3D structures using a comparative molecular field analysis (CoMFA) approach.
AID196038Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1306485Displacement of [3H]RS-79948-197 from recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane by scintillation counting method2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID681118TP_TRANSPORTER: transepithelial transport in Caco-2 cells2003International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2
Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.
AID1568812Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml by PAMPA-BBB assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1330750Effective permeability of the compound after 18 hrs by PAMPA2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
AID1390040Effective permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
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]
AID35192Binding affinity towards alpha-2 adrenergic receptor in rat using [3H]rauwolscine as radioligand1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.
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).
AID671634Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
AID1773264Permeability of the compound at 100 ug/ml incubated for 18 hrs by PAMPA2021European journal of medicinal chemistry, Nov-05, Volume: 223Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
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).
AID186204Hypotensive activity by intravenous administration to rats1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Ultraviolet photoelectron spectroscopy of cyclic amidines. 2. Electronic structure of clonidine and some related 2-(phenylimino)imidazolidines with alpha-adrenergic activity.
AID36261Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
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.
AID36407Binding affinity towards alpha-2C adrenergic receptor2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID174420Change in systolic blood pressure after 100 ug/kg oral administration in spontaneous hypertensive rats after 2 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1713986Effective permeability of the compound in PBS/ethanol buffer (9:1) at 25 ug/ml after 10 hrs by UV plate reader based PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Multitarget-directed oxoisoaporphine derivatives: Anti-acetylcholinesterase, anti-β-amyloid aggregation and enhanced autophagy activity against Alzheimer's disease.
AID1677629Modulation of cardiovascular activity in mouse assessed as inhibition of carotid occlusion-induced pressure response at 10 mg/kg2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents.
AID171843Hypotensive activity in the rat as change in blood pressure (mmHg) at 24 hr after of 1 mg/kg oral dose of the compound1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Arylformamidines with antinociceptive properties.
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.
AID179133Compound is measured for oral antihypertensive activity in groups of 6-12 deoxy-corticosterone-sodium hypertensive (DOCA-Na) rats at 0.5 mg/kg1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID174562Change in systolic blood pressure after 50 ug/kg oral administration in spontaneous hypertensive rats after 24 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones.
AID35422Tested for Binding affinity towards alpha-1 adrenergic receptor2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID223241Binding affinity for imidazoline receptor I-21995Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
AID536952Toxicity in CD1 mouse assessed as induction of hypotension by pentobarbital sodium induced sleep time assay2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID173516Maximum percent decrease in heart rate of spontaneously hypertensive rats, 10 hours after peroral administration of 3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID671632Displacement of [3H]paraiodoclonidine from imidazoline I1 receptor in rat PC12 cells after 30 mins by gamma counter2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
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).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1557184Permeability of the compound at 25 ug/ml by PAMPA-BBB assay2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1324014Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID514304Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as decrease in EGFP-HDQ74 aggregation at 3 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID536949Reduction in morphine dependence expression in CD1 mouse assessed as decrease in expression of naloxone-precipitated withdrawal syndrome at 5 mg/kg, ip administered as single dose 15 mins before last morphine dosing on test day post morphine challenge by 2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID36094in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID569431Antihypertensive activity in cat assessed as change in heart rate at 10 mg/kg measured within 5 mins2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Substituted imidazole derivatives as novel cardiovascular agents.
AID175549Effect of compound on reflux function in spinal transected rats at 12.5 ug/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID1264447Permeability of the compound by PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1511118Permeability of the compound measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
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.
AID1392732Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA
AID1279155Permeability of the compound at 25 ug/ml at pH 7.4 after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID636210Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines.
AID1570001Permeability of compound at 100 ug/ml measured after dilution with PBS/EtOH (70:30) at pH 7.4 after 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1623120Effective permeability of the compound by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1161578Permeability of the compound by PAMPA-BBB assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties.
AID1091956Apparent hydrophobicity, log D of the compound in Octanol-buffer2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID19258Logarithm of partition coefficient of the neutral form of compound given for chloroform/water solvent system1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID514303Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as loss of rhodopsin expression at 10 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID141670Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn; Not tested1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1150071Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in mean arterial blood pressure at 0.5 mg/kg, po administered as two dose at 24 hrs interval measured 4 hrs post second dose relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
4-Substituted semicarbazones of mono- and dichlorobenzaldehydes as antihypertensive agents.
AID114183Effective dose against administration in mice1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
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]
AID427198Membrane permeability dissolved in PBS/EtOH (80:20) mixture by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID1677625Hypotensive activity in mouse assessed as decrease in immediate blood pressure at 10 mg/kg2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents.
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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID536950Reduction in morphine tolerance acquisition in CD1 mouse assessed as morphine analgesic effect incidence at 2 mg/kg, ip administered as single dose 15 mins before last morphine dosing on test day post morphine challenge by radiant heat tail flick test2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID536942Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry relative to (-)noradrenaline2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID1485936Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1442001Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
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.
AID1071344Permeability of the compound by BBB-PAMPA2014European journal of medicinal chemistry, Feb-12, Volume: 731,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.
AID36357Inhibition of alpha-2 adrenergic receptor1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Alpha-adrenoreceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoreceptor activity.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID536941Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
AID1463749Effect on electrical threshold for nociceptive flexion reflex in mouse assessed as A-delta current threshold at 0.1 mg/kg, sc measured every 15 min up to 1 hr (Rvb = 0.71 +/- 0.33 mA)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Discovery of non-zwitterionic aryl sulfonamides as Na
AID764760Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Design, synthesis and pharmacological evaluation of (E)-3,4-dihydroxy styryl sulfonamides derivatives as multifunctional neuroprotective agents against oxidative and inflammatory injury.
AID1436079Permeability of compound at 25 ug/ml after 18 hrs by PAMPA2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID36251Binding affinity for rat Alpha-2B adrenergic receptor1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.
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).
AID36373Compound was tested in vitro for binding affinity against Alpha-2B adrenergic receptor from cloned rat RNG receptor transfected into Chinese hamster ovary (CHO) cells1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID371645Displacement of [3H]clonidine from imidazoline I1 receptor in Sprague-Dawley rat kidney by liquid scintillation counting2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
New analogues of agmatine with higher affinity to imidazoline receptors.
AID128510Analgesic activity was determined in mouse writhing test1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Arylformamidines with antinociceptive properties.
AID183611First ionization energy by intravenous administration to rats1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Ultraviolet photoelectron spectroscopy of cyclic amidines. 2. Electronic structure of clonidine and some related 2-(phenylimino)imidazolidines with alpha-adrenergic activity.
AID192796Maximum rate of rise of the left ventricular isovolumetric pressure administered at 0.108 uM/kg iv in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
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.
AID536937Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
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.
AID37078Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]clonidine from rat brain cortical membranes1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
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.
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.
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.
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1534778Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID1568822Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID139799Agonist potency of clonidine in the mouse electrically stimulated vas deferens1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1378334Permeability of the compound by PAMPA2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-β aggregation for the treatment of Alzheimer's disease.
AID35934Binding affinity for human Alpha-2A adrenergic receptor1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.
AID513655Induction of autophagy in human SK-N-SH cells expressing EGFP-HDQ74/m-calpain assessed as inhibition of EGFP-HDQ74 aggregation at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1183278Permeability of the compound by PAMPA2014European journal of medicinal chemistry, Sep-12, Volume: 84Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies.
AID1295107Permeability of the compound at 100 ug/ml by PAMPA-BBB assay2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Design, synthesis and evaluation of novel ferulic acid-memoquin hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID35806Presynaptic Alpha-2 adrenergic receptor agonist activity in isolated tissue of rat or mouse vas deferens1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
AID172280Effect on heart rate of spontaneously hypertensive rats, 24 hr after peroral administration of 0.3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
AID681376TP_TRANSPORTER: inhibition of MPP+ uptake in OCT1-expressing HEK293 cells
AID1625122Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
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.
AID180082Antihypertensive activity determined as heart rate in SH rats, was reported at a dose of 100 mg/Kg1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
AID36161The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
AID35572In vitro antagonistic activity against alpha1 adrenoceptor in rat anococcygeus; Ag means compound was agonist.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID197167Hypotensive activity (25% decrease in arterial pressure) after i.v. administration to anesthetized normotensive rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID680959TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Clonidine: 5000 uM) in OCT3-expressing HRPE cells2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
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.
AID36493Presynaptic alpha-2 adrenergic receptor agonist activity in isolated mouse vas deferens1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Alpha-adrenoreceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoreceptor activity.
AID1311930Permeability of the compound at 50 ug/ml in 70:30 PBS:EtOH by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.
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.
AID36104Compound was tested for binding affinity based on dissociation constant of Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID175542Effect of compound on hyperreflexia in spinal transected rats at 12.5 ug/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID39946The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
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.
AID193760Change in heart rate after iv administration of 0.108 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID536951Toxicity in CD1 mouse assessed as induction of sedation by pentobarbital sodium induced sleep time assay2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID569432Antihypertensive activity in cat assessed as change in heart rate at 10 mg/kg measured after 5 mins2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Substituted imidazole derivatives as novel cardiovascular agents.
AID297456Displacement of [3H]RX821002 from adrenergic alpha2 receptor in human brain frontal cortex2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1150955Retardation factor, deltaRm of the compound at pH 13 by TLC analysis1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Clonidine and related analogues. Quantitative correlations.
AID1334754Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID1392733Permeability of the compound at 100 ug/ml after 10 hrs by PAMPA
AID1485937Permeability of the compound in PBS/EtOH after 16 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID727731Dissociation constant, pKa of the compound at pH 3 to 12 by UV spectroscopy2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
Rapid Determination of Ionization Constants (pK a) by UV Spectroscopy Using 96-Well Microtiter Plates.
AID569428Antihypertensive activity in cat assessed as change in blood pressure at 10 mg/kg measured after 5 mins2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Substituted imidazole derivatives as novel cardiovascular agents.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID197287Change in systolic blood pressure following iv administration at (0.108 umol/kg)anesthetized rats2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N(1)-agmatine and synthetic analogues.
AID569427Antihypertensive activity in cat assessed as change in blood pressure at 10 mg/kg measured within 5 mins2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Substituted imidazole derivatives as novel cardiovascular agents.
AID193699Percent change in systolic blood pressure (mmHg)in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID35187Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
AID186692Assessment of antihypertensive activity at 100 mg/kg administered perorally by measuring mean arterial blood pressure (MABP) in rats1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
5-(1-piperazinyl)-1H-1,2,4-triazol-3-amines as antihypertensive agents.
AID23238Partition coefficient (logP)1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Two clonidine-like compounds with substituents at the 2-, 3-, and 6-position of the phenyl ring possessing pronounced hypotensive potencies.
AID513627Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID172275Effect on heart rate of spontaneously hypertensive rats, 10 hr after peroral administration of 3 mg/kg of compound1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.
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
AID173906Hypotensive response (diastolic blood pressure) was determined at 30 minutes for a dose of 0.1 mg/kg administered and 1 mL of corn oil in rat1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Preliminary studies of mesoionic 3-(substituted-aryl)-psi-oxatriazoles as potential antihypertensive agents.
AID513635Induction of autophagy in Atg positive human SK-N-MC cells expressing EGFP-HDQ74 at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1091957Apparent permeability of the compound by PAMPA2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID513629Cytotoxicity against human SK-N-MC cells expressing EGFP-HDQ74 at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
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).
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1480849Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
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.
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.
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.
AID1374214Effective permeability of the compound in pH 7.4 buffer after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID180829Tested for change in heart rate administered at 0.108 uM/kg iv in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID1480943Permeability of the compound at pH 7.4 at 5 mg/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.
AID1495958Effective permeability of the compound in PBS/ethanol buffer2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
AID1264455Permeability of the compound by high throughput PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1480942Permeability of the compound at pH 7.4 at 1 mg/ml after 4 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.
AID1496040Effective permeability of the compound in PBS/EtOH at 50 ug/mL after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
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.
AID1427527Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID36555In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID1765292Permeability of compound by PAMPA-BBB assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.
AID552774Inhibition of Sprague-Dawley rat alpha-2 adrenergic receptor2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
New imidazoline/α(2)-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies.
AID173920Oral dose required to cause 20% fall in blood pressure1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID26594pKa values were observed1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
AID1677628Modulation of cardiovascular activity in mouse assessed as inhibition of norepinephrine induced pressure response at 10 mg/kg2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents.
AID1317097Selectivity ratio of agonist activity at I1 receptor imidazoline binding site (unknown origin) to agonist activity at alpha2-AR (unknown origin)
AID223226Binding affinity for imidazoline receptor I-11995Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
AID181262tested for antinociceptive activity at a screening dose of 30 mg/kg, po in the rat air-induced abdominal irritant test (RAIT) using acetylcholine as irritant2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID181769Compound is measured for oral antihypertensive activity in groups of 6-12 conscious spontaneously hypertensive rats at 0.5 mg/kg1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
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.
AID126323Oral dose required to cause 20% fall in sedation; Increase in foot shock rate1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID1195978Displacement of [125I] PIC from I1 imidazoline receptor in rat PC12 cells after 45 mins by gamma counting2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
AID1173449Effective permeability of the compound by PAMPA assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
AID171847Hypotensive activity in the rat as change in blood pressure (mmHg) at 4 hr after a 50 mg/kg oral dose of the compound1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Arylformamidines with antinociceptive properties.
AID37082Binding affinity for alpha-2 adrenergic receptor in rat cortex using [3H]rauwolscine.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.
AID225282ED50 value was measured using rat air-induced abdominal irritant test(RAIT)2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID1347980Permeability of the compound in PBS/EtOH at 100 ug/ml after 12 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID35210In vitro antagonistic activity against alpha-2 adrenoceptor in rat vas deferens; Ag means compound was agonist.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
AID552773Inhibition of Sprague-Dawley rat imidazoline I2 receptor2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
New imidazoline/α(2)-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies.
AID133238Tested for antinociceptive activity at a screening dose of 30 mg/kg, po in the mouse abdominal irritant test (MAIT) using acetylcholine as irritant.[95% confidence limit]2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID1319973Permeability of the compound by PAMPA assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID174421Change in systolic blood pressure after 100 ug/kg oral administration in spontaneous hypertensive rats after 4 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones.
AID1866897Permeability for across blood brain barrier by PAMPA2022European journal of medicinal chemistry, Apr-15, Volume: 234Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors.
AID24217Apparent partion coefficient of compound was evaluated in octanol/buffer at pH of 7.4 at 37 degree Centigrade1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID1495957Effective permeability of the compound in PBS/ethanol buffer after 12 hrs by PAMPA2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
AID625277FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
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).
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.
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).
AID368169Displacement of [3H]RX821002 from alpha2 adrenoceptor in human prefrontal cortex neural membrane after 30 mins by liquid scintillation spectrometry2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor ligands: searching for structure-activity relationships.
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).
AID513628Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID288184Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID174563Change in systolic blood pressure after 50 ug/kg oral administration in spontaneous hypertensive rats after 2 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones.
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]
AID35437in vitro alpha-1 adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID35271Compound was tested for the inhibition of [3H]prazosin binding Alpha-1 adrenergic receptor of crude rat brain membrane.1982Journal of medicinal chemistry, Jan, Volume: 25, Issue:1
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.
AID682996Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID1195980Selectivity ratio of Ki for I1 imidazoline receptor in rat PC12 cells to Ki for human alpha2 adrenoceptor expressed in CHO cell membranes2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
AID1693561Effective permeability of compound in PBS/EtOH buffer (7:3) at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
AID223928potential antinociceptive activity initially at a screening dose of 30 mg/kg po in the mouse abdominal irritant test(MAIT) using acetylcholine bromide as irritant2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID3678350% inhibition of specific [3H]clonidine binding (0.4 nM) to Alpha-2 adrenergic receptors in rat isolated brain membranes1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID1322294Displacement of [3H]clonidine from alpha2 adrenergic receptor in rat brain cerebral cortex after 25 mins by microbeta scintillation counting method
AID1705959Effective permeability of compound at 100 ug/ml incubated for 20 hrs by PAMPA-BBB assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID36715Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.4 nM) to rat isolated brain membranes by 50% was reported.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID229655Relative affinities for Alpha1 and alpha-2 adrenergic receptors in rat1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.
AID186358Antihypertensive activity in SH rats, and mean arterial blood pressure was reported at a dose of 25 mg/Kg1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
AID58629Oral dose required to cause 20% fall in blood pressure1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
AID1365650Permeability of the compound at pH 7.4 by BBB-PAMPA2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Design, synthesis, and evaluation of salicyladimine derivatives as multitarget-directed ligands against Alzheimer's disease.
AID1437175Permeability of the compound by PAMPA2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1623078Effective permeability of the compound at 100 ug/ml after 10 hrs by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
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.
AID180235Assessment of antihypertensive activity at 100 mg/kg administered perorally by measuring the heart rate in rats1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
5-(1-piperazinyl)-1H-1,2,4-triazol-3-amines as antihypertensive agents.
AID35207In vitro agonist activity against alpha-2 adrenoceptor in rat vas deferens1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
AID197166Hypotensive activity measured as the 20% decrease in mean arterial blood pressure in anesthetized normotensive rat1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Two clonidine-like compounds with substituents at the 2-, 3-, and 6-position of the phenyl ring possessing pronounced hypotensive potencies.
AID193687Percent change in diastolic blood pressure (mmHg)in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID469403Permeability across PAMPA membrane 2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID36404Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID173907Hypotensive response (systolic blood pressure) was determined at 30 minutes for a dose of 0.1 mg/kg administered and 1 mL of corn oil in rat1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Preliminary studies of mesoionic 3-(substituted-aryl)-psi-oxatriazoles as potential antihypertensive agents.
AID1557178Permeability of the compound at 100 ug/ml measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID1352674Effective permeability at 25 ug/ml after 16 hrs by PAMPA2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1292332Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1517867Permeability of compound by PAMPA-BBB assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1585850Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID36178The compound was tested for alpha-adrenergic activity against alpha-2 adrenergic receptor from guinea pig vas deferens.1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a beta-blocking side chain.
AID342860Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID404330Displacement of [3H]RX821002 from alpha2 adrenergic receptor in human brain prefrontal cortex tissue by liquid scintillation spectrometry2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor antagonists. 2. Exploring alkyl linkers for new antidepressants.
AID1374215Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID680406TP_TRANSPORTER: inhibition of TEA uptake (TEA: 60 uM, Clonidine: 1000 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, May, Volume: 289, Issue:2
Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.
AID141668Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the absence of Zn; Not tested1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1306487Intrinsic activity at recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane incubated for 30 mins by [35S]GTPgammaS binding assay relative to adrenaline2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
AID63016In vitro binding affinity to Dopamine receptors of rat striatal membranes by [3H]spiroperidol displacement.1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
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.
AID1279139Permeability of the compound at 25 ug/ml at pH 7.4 after 16 hrs by PAMPA2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
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).
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID679482TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.2 uM) in OCT3-expressing HEK293 cells2001Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 363, Issue:1
Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters.
AID174419Change in systolic blood pressure after 100 ug/kg oral administration in spontaneous hypertensive rats after 24 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones.
AID1436078Permeability of compound at 100 ug/ml after 18 hrs by PAMPA2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
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.
AID1201747Permeability of the compound by PAMPA2015European journal of medicinal chemistry, May-05, Volume: 95Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
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.
AID648667Permeability of the compound in porcine brain lipid assessed as ratio of compound in acceptor plate to amount of compound in donor plate at 5 mg/ml after 10 hrs by PAMPA assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Novel oxoisoaporphine-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID186357Antihypertensive activity in SH rats, and mean arterial blood pressure was reported at a dose of 100 mg/Kg1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
AID1465293Effective permeability of the compound at 100 ug/ml by PAMPA-BBB assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID171674Change in systolic blood pressure after iv administration of 0.108 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID35950Binding affinity towards Alpha-2A adrenergic receptor2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
AID175547Effect of compound on hyperreflexia in spinal transected rats at 50 ug/Kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID681705TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Clonidine: 2500 uM) in OCTN2-expressing HRPE cells1999The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3
Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.
AID1334753Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12,677)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905595 (44.14)18.7374
1990's3512 (27.70)18.2507
2000's2031 (16.02)29.6817
2010's1276 (10.07)24.3611
2020's263 (2.07)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 112.72

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 Index112.72 (24.57)
Research Supply Index9.66 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index215.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (112.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2,044 (14.93%)5.53%
Reviews955 (6.97%)6.00%
Case Studies847 (6.19%)4.05%
Observational24 (0.18%)0.25%
Other9,822 (71.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (241)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized Clinical Study to Compare Different Doses of Clonidine to Fentanyl as an Adjuvant to Hyperbaric Bupivacaine 0.5% for Spinal Anesthesia in Patients Undergoing LSCS [NCT01205204]0 participants (Actual)Interventional2010-08-31Withdrawn(stopped due to This study was registered with Clinical Trials.gov by mistake.)
Advantage of Clonidine With Morphine In Patient Controlled Analgesia Pump for the Treatment of Vaso-occlusive Crisis in Sickle Cell Disease Patients [NCT05848531]Phase 440 participants (Anticipated)Interventional2023-04-25Recruiting
Multicenter, Open Label Trial to Investigate the Efficacy and Safety of a Single Oral Dose of 1.0 mg/kg Macimorelin Acetate as Growth Hormone Stimulation Test (GHST) in Pediatric Patients With Suspected Growth Hormone Deficiency (GHD) [NCT04786873]Phase 3100 participants (Anticipated)Interventional2021-11-16Recruiting
The Role of Stress Neuromodulators in Decision Making Under Risk [NCT05318248]82 participants (Actual)Interventional2022-03-01Completed
Effects and Safety of Clonidine Patch on Young and Middle-aged Smokers With Mild Hypertension: a Randomized Controlled Trial (ECLIPSE) [NCT05416840]Phase 480 participants (Anticipated)Interventional2022-08-31Not yet recruiting
Repurposing Low-Dose Clonidine for PTSD in Veterans [NCT04877093]Phase 332 participants (Anticipated)Interventional2023-06-01Recruiting
A Study to Evaluate the Relative Bioavailability of a Test Formulation of Lofexidine Granules for Reconstitution and the Effect of Food on the Bioavailability of the Test Formulation in Healthy Adult Subjects [NCT04188730]Phase 116 participants (Actual)Interventional2021-02-16Completed
A Randomized, Double-Blind, Placebo-Controlled Pilot Study to Evaluate the Safety and Effectiveness of LUCEMYRA in the Treatment of Opioid Withdrawal During an Opioid Taper in Subjects With Chronic Non-Cancer Pain [NCT04070157]Phase 260 participants (Anticipated)Interventional2019-08-02Suspended(stopped due to COVID pandemic and enrollment issues necessitating an adjustment to the study design.)
Ilioinguinal/Iliohypogastric vs. Quadratus Lumborum Nerve Blockade for Elective Open Inguinal Herniorrhaphy [NCT03007966]Phase 260 participants (Actual)Interventional2017-01-30Completed
Paravertebral Block With Versus Without Clonidine for Patients Undergoing Ventral Hernia Repair: A Prospective Double-blinded Randomized Study [NCT02505204]60 participants (Anticipated)Interventional2015-08-01Suspended
Randomized, Placebo-controlled Trial of Erector Spinae Plane Blocks (ESPB) for Perioperative Pain Management for Minimally Invasive (MIS) Lumbar Spine Surgery [NCT05029726]Phase 4125 participants (Anticipated)Interventional2022-02-01Recruiting
Prophylactic Mirtazapine or Clonidine for Post-spinal Anesthesia Shivering in Patients Undergoing Urological Surgeries: a Randomized Controlled Trial [NCT03679052]Phase 4300 participants (Actual)Interventional2018-03-01Completed
A Phase 3, Prospective, Multicenter, Randomized, Double-blind, Sham-controlled Study of the Efficacy and Safety of STX-015 in the Treatment of Pain Associated With Lumbosacral Radiculopathy [NCT05614648]Phase 3340 participants (Anticipated)Interventional2023-06-19Recruiting
Alpha 2 Adrenergic Receptor Agonists for the Prevention of Delirium and Cognitive Decline After Open Heart Surgery (ALPHA2PREVENT): Randomised Controlled Trial. [NCT05029050]Phase 4900 participants (Anticipated)Interventional2022-01-17Recruiting
Role of Co-administered Dexmedetomidine Or Clonidine With Bupivacaine for Transversus Abdominis Plane Block in Patients Undergoing Elective Caesarean Section: A Randomized, Double-blind Controlled Trial [NCT03770013]150 participants (Actual)Interventional2019-01-01Completed
Sacrococcygeal Local Anesthesia With Different Doses of Clonidine for Pilonidal Sinus Surgery: A Prospective Randomized Trial [NCT02539693]60 participants (Anticipated)Interventional2016-10-31Recruiting
A Phase IV, Longitudinal, Observational Study Examining Real-World Outcomes of Non-Hormonal Pharmacotherapies Among Individuals Treated for Bothersome Vasomotor Symptoms [NCT06049797]1,000 participants (Anticipated)Observational2023-11-15Recruiting
The Norwegian Study of Chronic Fatigue Syndrome in Adolescents: Pathophysiology and Intervention Trial [NCT01040429]Phase 2120 participants (Actual)Interventional2010-02-28Completed
A Single-Center, Open-Label, Two-Period, Two-Treatment, Randomized Sequence Study to Determine the Mass Balance and Absolute Bioavailability of a Single Oral Dose of 14C-Labeled Lofexidine Compared to a Single Intravenous Dose of Lofexidine [NCT01310296]Phase 112 participants (Actual)Interventional2011-07-31Completed
Clonidine and the Skeletal Myopathy of Heart Failure [NCT00858845]Phase 411 participants (Actual)Interventional2008-05-31Completed
Use of Intraoperative Clonidine for Prevention of Postoperative Agitation in Pedriatic Anesthesia With Sevoflurane. [NCT02181543]Phase 330 participants (Actual)Interventional2013-08-31Completed
The Use of Propofol/Ketamine Anesthesia With Bispectral Monitoring (PKA-BIS) Versus Inhalational Anesthetics in Rhytidoplasty - A Prospective, Double-blinded, Randomized Comparison Study [NCT02410460]30 participants (Actual)Interventional2013-09-30Completed
Fentanyl and Clonidine for Analgesia During Hypothermia in Term Asphyxiated Infants - a Prospective Pharmacokinetic/Pharmacodynamic/Pharmacogenetic Observational Study. Cohort 1 in The SANNI Project. [NCT03177980]49 participants (Actual)Observational2017-04-24Completed
Treatment of Chronic Itch in Atopic Dermatitis With Oral Clonidine and Oral Naltrexone: Nerve Function [NCT02268448]Phase 18 participants (Actual)Interventional2015-07-31Completed
The Comparison of Stress Response to Rapid Opioid Detoxification Applying Different Methods of Opioid Antagonism With Naltrexone and Sedation [NCT02362256]60 participants (Actual)Interventional2014-05-31Completed
Matão Controlling Hypertension (MatCH Study): Rationale and Design. Project to Reduce Incidence of Arterial Hypertension in City of Matão, Brazil. [NCT03147092]Early Phase 115,000 participants (Anticipated)Interventional2018-02-01Not yet recruiting
The Effect of Protracted Saphenous Nerve and Obturator Nerve Block Versus Saphenous Nerve Block Versus Local Infiltration Analgesia on Opioid Consumption, Pain, Block Duration of Action and Mobilization After Total Knee Arthroplasty. [NCT02067078]Phase 475 participants (Actual)Interventional2014-02-28Completed
An Extended-Release Form of Clonidine as an Anti-Manic Agent: An Add-On, Open-Label Study [NCT03065933]Phase 45 participants (Actual)Interventional2012-01-31Terminated
Prospective Randomized Clinical Trial to Evaluate the Use of Caudal Nerve Blocks in Adult Penile Prosthesis Surgery [NCT02740127]Phase 352 participants (Actual)Interventional2016-06-30Completed
Transdermal Clonidine on Blood Pressure of Chronic Hemodialysis Patients: A Randomized Crossover Clinical Trial [NCT02545530]45 participants (Anticipated)Interventional2015-05-31Recruiting
Intraoperative Clonidine for Postoperative Pain Management in Patients Undergoing Surgical Treatment for Endometriosis: a Prospective, Double-blind, Randomized Controlled Trial [NCT05560230]Phase 4120 participants (Anticipated)Interventional2022-10-03Recruiting
Sensorial and Physiological Mechanism-based Assessments of Perioperative Pain [NCT03537612]Phase 315 participants (Actual)Interventional2018-06-22Terminated(stopped due to Do to our inability to meet recruitment targets - Sponsor stopped funding. Looking for new sponsor and protocol modifications)
Alpha 2 Agonists for Sedation to Produce Better Outcomes From Critical Illness (A2B Trial): A Randomised, Parallel-group, Allocation Concealed, Controlled, Open, Phase 3 Pragmatic Clinical and Cost- Effectiveness Trial With Internal Pilot [NCT03653832]Phase 31,437 participants (Actual)Interventional2018-12-10Active, not recruiting
"Study Protocol OFA: Opioid-Free Anesthesia." [NCT03124082]Phase 464 participants (Anticipated)Interventional2017-01-04Recruiting
Randomized, Double-Blinded, Placebo-controlled Study to Evaluate the Analgesic Efficacy of Oral Clonidine and Gabapentin as Part of a Multi-modal Analgesic Regimen for Preventing Pain After Arthroscopic Shoulder or Knee Surgery [NCT01112878]Phase 40 participants (Actual)Interventional2015-06-30Withdrawn(stopped due to Several studies going on at the same time.)
Neonatal Spinal Anesthesia: Effects of the Addition of Clonidine [NCT01075490]Phase 4120 participants (Anticipated)Interventional2006-11-30Recruiting
Pharmacological Interaction Between Clonidine and 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy) [NCT01136278]Phase 116 participants (Actual)Interventional2010-07-31Completed
4-drug Nerve Block Versus Plain Local Anesthetic for Knee and Hip Arthroplasty Analgesia in Veterans [NCT02891798]Phase 398 participants (Actual)Interventional2016-10-31Completed
Study of Clonidine Efficacy for the Treatment of Impulse Control Disorders in Parkinson's Disease: A Pilot Double Blind Randomized Trial [NCT03552068]Phase 238 participants (Actual)Interventional2019-05-15Completed
Efficacy of Dexmedetomidine Versus Clonidine to Control Delirium in Patients Undergoing Coronary Artery Bypass Grafting [NCT03477994]147 participants (Actual)Interventional2018-12-01Completed
The Effects of Clonidine on Postoperative Analgesia After Single Shot Femoral Nerve Block Following Arthroscopic Knee Surgery in Children [NCT01293149]Phase 20 participants (Actual)Interventional2011-04-30Withdrawn
Labor Analgesia With Ropivacaine Added to Clonidine. A Randomized Clinical Trial [NCT00626977]32 participants (Actual)Observational2000-05-31Completed
An Open-Label, Chronic Exposure Evaluation of the Safety of CLONICEL (Clonidine HCl Sustained Release) in the Treatment of Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD) [NCT00723190]Phase 3303 participants (Actual)Interventional2008-01-31Completed
Pediatric Tonsillectomy Pain Reduction Study, a Randomized, Placebo Controlled, Double-Blind Clinical Trial Using Clonidine and Local Anesthetics [NCT00678379]Phase 3120 participants (Actual)Interventional2008-04-30Completed
[NCT02812368]Phase 20 participants (Actual)Interventional2016-08-31Withdrawn(stopped due to Failure to recruit)
Postoperative Pain and Systemic Inflammatory Stress Response (SIRS) After Preoperative Analgesia With Clonidine or Levobupivacaine [NCT00860899]Phase 442 participants (Actual)Interventional2007-12-31Completed
Pregabalin Plus Lofexidine for the Outpatient Treatment of Opioid Withdrawal [NCT05995535]Phase 2150 participants (Anticipated)Interventional2024-01-01Not yet recruiting
The Effect of Local Anesthetic and Clonidine on the Cutaneous Silent Period During and After Spinal Anesthesia [NCT03121261]Phase 460 participants (Anticipated)Interventional2017-05-01Active, not recruiting
[NCT02404077]712 participants (Actual)Observational2015-04-30Completed
Analgesic Benefit of PECS Blocks for Biceps Tenodesis Shoulder Surgery [NCT02741713]Phase 340 participants (Actual)Interventional2016-04-30Completed
Prospective Analgesic Compound Efficacy (PACE) Study [NCT02403687]300 participants (Actual)Observational [Patient Registry]2015-06-30Completed
Randomized Study of Spinal Anesthesia Compared With Traditional Epidural Anesthesia Concerning Peroperative and Postoperative Pain After Open Nephrectomy in Patients With Renal Cell Carcinoma [NCT02030717]Phase 2/Phase 3120 participants (Actual)Interventional2012-02-29Completed
Lemborexant vs Zopiclone vs Clonidine for Insomnia Treatment in Chronic Pain Patients [NCT05618002]150 participants (Anticipated)Observational2022-11-08Recruiting
Does Perineural Clonidine Prolong the Duration of an Adductor Canal Block When Controlling for a Systemic Effect? - A Randomised Paired Trial in Healthy Volunteers. [NCT02444559]Phase 221 participants (Actual)Interventional2015-05-31Completed
Propranolol Versus Propranolol and Clonidine in Sympathetic Hyperactivity After Moderate Traumatic Brain Injury [NCT04833218]Early Phase 190 participants (Anticipated)Interventional2020-01-31Active, not recruiting
A PROBE (Prospective, Randomised, Open-Label, Blinded Endpoint) Trial to Investigate the Efficacy and Safety of Telmisartan 40-80mg Once Daily Compared With 10-20 mg Enalapril Once Daily Over a Period of 24 Weeks in Elderly Patients With Blood Hypertensio [NCT02177461]Phase 4374 participants (Actual)Interventional2000-04-30Completed
Clonidine for Analgesia to Preterm Infants During Neonatal Intensive Care - a Prospective Pharmacokinetic/Pharmacodynamic/Pharmacogenetic Observational Study. Cohort 2 in The SANNI Project [NCT04928651]40 participants (Actual)Observational2018-04-06Completed
Intraoperative Autonomic Neural Blockade (ANB) Comparison Between Different Local Anesthetic Combinations. A Randomized Clinical Trial Protocol [NCT06137924]Phase 3150 participants (Anticipated)Interventional2023-12-02Not yet recruiting
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
Effect of Dexamethasone or Clonidine When Given as Adjuncts to Ropivacaine for Caudal Analgesia on Duration of Analgesia Compared to Placebo in Children [NCT02773602]Phase 4155 participants (Anticipated)Interventional2011-05-31Recruiting
Association of Different Doses of Clonidine in Caudal Epidural Anesthesia for Hypospadias Surgery [NCT02769390]Phase 280 participants (Actual)Interventional2015-07-31Completed
Sympathetic Regulation of Large Artery Stiffness in Humans With Age-Related Isolated Systolic Hypertension [NCT04423627]Early Phase 178 participants (Anticipated)Interventional2021-06-01Recruiting
Clonidine for Intra-oral Infra-orbital Nerve Block During Pediatric Cleft Lip Revision Surgeries: Randomized Controlled Double-blind Study [NCT05790044]86 participants (Anticipated)Interventional2023-10-01Not yet recruiting
The PREVENT AGITATION Trial II - Children ≤1 Year [NCT05091242]Phase 2/Phase 3336 participants (Anticipated)Interventional2021-10-25Recruiting
Clonidine is Better Than Zopiclone for Insomnia Treatment in Chronic Pain Patients [NCT05277038]150 participants (Actual)Observational [Patient Registry]2022-03-01Completed
A Placebo-Controlled Study of Clonidine for Fecal Incontinence. [NCT00884832]Phase 244 participants (Actual)Interventional2008-10-31Completed
Effects of a Systematic Addition of Clonidine in the Local Anaesthetic and Opiate Solution for Epidural Patient Controlled Analgesia in Labour (Levobupivacaine 0.568 mg.mLl-1 + Sufentanil 0.45 µg.mL-1) [NCT00983125]Phase 4124 participants (Actual)Interventional2009-08-31Completed
Treating Nightmares in Posttraumatic Stress Disorder With the α-adrenergic Agents Clonidine and Doxazosin: A Randomized-Controlled Feasibility Study (ClonDoTrial) [NCT05360953]Phase 2189 participants (Anticipated)Interventional2022-04-06Recruiting
A Phase 2b/3, Multicenter, Randomized, Double-blind, Placebo-controlled Study Comparing the Efficacy and Safety of Clonidine Mucoadhesive Buccal Tablet to Placebo to Prevent Chemoradiotherapy-induced Severe Oral Mucositis in Patients With Oropharyngeal Ca [NCT04648020]Phase 2/Phase 3190 participants (Actual)Interventional2021-02-11Terminated(stopped due to Interim Analysis did not meet the pre-defined threshold for efficacy of a 15% absolute difference in SOM prevention between Validive and placebo.)
Treatment of Orthostatic Intolerance [NCT00262470]Phase 1/Phase 2150 participants (Anticipated)Interventional1997-04-30Active, not recruiting
Influence of the Noradrenergic System on the Formation of Intrusive Memories: An Experimental Approach With a Trauma Film Paradigm [NCT02541071]118 participants (Actual)Interventional2013-11-30Completed
Effects of Clonidine and Midazolam Premedication on Bispectral Index and Recovery After Elective Surgery [NCT00638729]60 participants (Actual)Interventional2005-08-31Completed
A Randomised, Double-blind, Placebo-controlled Study to Assess the effectIveness of Pectoral Nerves Block (PECS) After Breast Surgery on Piritramide Consumption [NCT02655965]Phase 354 participants (Actual)Interventional2016-05-31Completed
Comparison of Clonidine and Morphine Plus Bupivacaine in Caudal Peridural Anesthesia for Postoperative Analgesia After Pediatric Urogenital Surgery [NCT00672347]Phase 1/Phase 280 participants (Actual)Interventional2008-07-31Completed
Monocentric, Prospective Randomized Controlled Clinical Trial Assessing the Effect on the Lower Limb Spinal Motoneuron Excitability, the Efficacy in Term of Morphinic Sparing and Safety of of Early Clonidine Bolus Intravenous Administration During General [NCT02592915]Phase 340 participants (Anticipated)Interventional2015-10-31Recruiting
Pilot Study to Assess the Safety, Tolerability, and Feasibility of Administering Clonidine as a Pharmacological Challenge in Future Imaging Studies of Cerebrospinal Fluid Kinetics [NCT04030572]Early Phase 13 participants (Actual)Interventional2019-12-10Terminated(stopped due to Not logistically feasible during the COVID pandemic)
Pilot Study of Transforaminal Epidural Injection of Clonidine for the Treatment of Acute Lumbosacral Radiculopathy [NCT00588354]26 participants (Actual)Interventional2006-10-31Terminated(stopped due to Targeted enrollment was not reached.)
A Multicenter, Randomized, Double-Blind, Parallel-Group Study Comparing the Efficacy and Safety of Clonidine Topical Gel, 0.1% With Placebo in the Management of Pain Associated With Painful Diabetic Neuropathy [NCT00695565]Phase 2180 participants (Actual)Interventional2008-05-31Completed
Programmed Intermittent Epidural Bolus Versus Continuous Epidural Infusion for Third Trimester Medical Termination of Pregnancy Analgesia : a Randomized Study. [NCT02563821]Phase 337 participants (Actual)Interventional2015-11-05Completed
The Pathophysiology of Orthostatic Hypotension [NCT00748059]Phase 110 participants (Actual)Interventional1996-12-31Completed
The Effects of Alpha-2 Adrenergic Receptor Modulation on Rates of Carbon-11 Butanol Clearance From Ventricular Cerebrospinal Fluid [NCT04032691]Early Phase 10 participants (Actual)Interventional2019-08-27Withdrawn(stopped due to lack of funding)
Diabetic Neuropathic Pain Topical Treatment- Comparative Study [NCT00661063]Phase 3200 participants (Anticipated)Interventional2008-04-30Not yet recruiting
Effectiveness of Ultrasound Guided Adductor Canal Blockade With Levobupivacaine and Clonidine on Chronic Pain in Knee Osteoarthritis [NCT02695654]77 participants (Actual)Observational2015-11-30Completed
A Large, International, Placebo-controlled, Factorial Trial to Assess the Impact of Clonidine and Acetyl-salicylic Acid (ASA) in Patients Undergoing Noncardiac Surgery Who Are at Risk of a Perioperative Cardiovascular Event [NCT01082874]Phase 310,010 participants (Actual)Interventional2010-07-31Completed
Mitigating the Pro-inflammatory Phenotype of Obesity [NCT04934228]Phase 160 participants (Anticipated)Interventional2021-07-01Recruiting
PeriOperative ISchemic Evaluation-2 (POISE-2) Trial: A Pilot [NCT00860925]Phase 490 participants (Actual)Interventional2009-05-31Completed
Effect of Clonidine on High Volume-Low Concentration Caudals [NCT04263064]Early Phase 1129 participants (Actual)Interventional2020-03-06Completed
New Approaches to Pediatric Sedation: Adjunctive Clonidine in the Sedation of Mechanically Ventilated Children (NAPS Pilot Trial) [NCT00959062]Phase 450 participants (Actual)Interventional2010-01-31Completed
[NCT01425658]Phase 1/Phase 290 participants (Actual)Interventional2011-08-31Completed
Status of the Growth Hormone/ Insulin-like Growth Factor-1 (GH/IGF-1) Axis in Relation to Growth Failure, Body Weight and Neuroprotection in Children With Ataxia Telangiectasia [NCT01052623]Phase 424 participants (Anticipated)Interventional2010-01-31Recruiting
Safety and Efficacy of Oral Tizanidine Hydrochloride in Preventing Migraine Attacks in Adult Migraine Patients: a Multicenter, Randomized, Double Blind, Placebo Controlled Clinical Study [NCT05484349]Phase 3189 participants (Anticipated)Interventional2023-08-31Not yet recruiting
Comparison Between Intravenous and Intrathecal Clonidine in Post-cesarean Analgesia [NCT02550444]64 participants (Actual)Interventional2015-04-30Completed
Randomised Single Dose 3 Way Crossover Single Blind Study to Evaluate the Pharmacokinetic Dose Proportionality, Compare the Bioavailability and Safety of Clonidine Mucoadhesive Buccal Tablets (MBT) With Catapres in Normal Healthy Volunteers [NCT02548806]Phase 136 participants (Actual)Interventional2015-09-30Completed
Clonidine for the Treatment of Neurocognitive Sequelae Following Cancer Treatment in Children [NCT00166686]Phase 1/Phase 20 participants (Actual)InterventionalWithdrawn(stopped due to Study was never initiated)
Aggressive Behaviour in Children With Tourette's Syndrome (TS) and Comorbid Attention Deficit Hyperactivity Disorder (ADHD) [NCT00152750]Phase 432 participants Interventional2006-09-30Recruiting
Safety and Efficacy of Cervical Sympathetic Block in Patients With Cerebral Vasospasm Following Aneurysmal Subarachnoid Hemorrhage - Pilot Study [NCT00930072]Phase 27 participants (Actual)Interventional2009-04-30Terminated(stopped due to Poor Enrollment)
A Phase III, Dose-Response Evaluation of the Efficacy and Safety of CLONICEL® (Clonidine HCl Sustained Release) vs. Placebo in the Treatment of Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD) [NCT00556959]Phase 3236 participants (Actual)Interventional2007-10-31Completed
Randomized Double-blind Trial Comparing the Post-operative Analgesic Efficacy of Local Wound Infiltration With Bupivacaine Alone to Bupivacaine With Clonidine in Posterior Spine Surgeries [NCT01902108]Phase 4225 participants (Actual)Interventional2013-01-31Completed
Transversus Abdominis Plane (TAP) Block Versus Intrathecal Morphine for Caesarean Section - Randomised Controlled Trial [NCT01931215]Phase 4180 participants (Actual)Interventional2013-09-30Completed
Kratom Use Disorder Management Using Clonidine and/or Buprenorphine [NCT05883358]50 participants (Anticipated)Observational2018-07-02Recruiting
A Prospective, Multicenter, Randomized, Double-Blinded, Sham-Control Study to Evaluate the Efficacy and Safety of Clonidine Micropellets for the Treatment of Pain Associated With Lumbosacral Radiculopathy in Adults [NCT03727100]Phase 3207 participants (Actual)Interventional2018-10-16Completed
Positron Emission Tomography Study of alpha2-adrenergic Receptors With [11C]Yohimbine [NCT03520543]Phase 116 participants (Actual)Interventional2018-05-21Completed
Assessing a Clinically-meaningful Opioid Withdrawal Phenotype [NCT05027919]Phase 260 participants (Anticipated)Interventional2022-02-01Recruiting
Efficacy of Clonidine and Propranolol Versus Placebo for the Control of Anxiety During Surgical Procedures in Dentistry [NCT01784250]Phase 260 participants (Anticipated)Interventional2012-08-31Recruiting
The Oslo Study of Clonidine in Elderly Patients With Delirium [NCT01956604]Phase 220 participants (Actual)Interventional2014-04-10Terminated(stopped due to The inclusion rate was too low, due to the exclusion criteria.)
Prospective Randomised Double-blind Study to Compare Ropivacaine 10mg/mL Alone Versus Ropivacaine 10mg/mL Associated With Clonidine 1µg/kg for Peribulbar Anesthesia in Posterior Eye Surgery [NCT01963299]Phase 260 participants (Actual)Interventional2013-08-16Completed
Preschool Supplement to Clonidine in ADHD (Kiddie-CAT) [NCT00414921]Phase 230 participants (Actual)Interventional2003-09-30Completed
Non-Opiate Treatment After Prenatal Opiate Exposure to Prevent Postnatal Injury to the Young Brain [NCT03396588]Phase 3120 participants (Actual)Interventional2017-12-07Active, not recruiting
Interest in Clonidine in Association With Levobupivacaine Performing a Pudendal Block in Proctological Surgery: Pilot Study, Prospective [NCT04530903]Phase 430 participants (Anticipated)Interventional2020-09-09Recruiting
Effect of CYP2B6 Genotype and Efavirenz on the Disposition and Pharmacodynamic of Methadone and Tizanidine in Healthy Volunteers [NCT05789173]Early Phase 160 participants (Anticipated)Interventional2023-10-06Recruiting
Intravenous Clonidine Versus Granisetron for Prevention of Post Spinal Anesthesia Shivering in Cesarean Section [NCT06031090]Phase 2186 participants (Anticipated)Interventional2023-03-05Recruiting
Comparison of Clonidine Versus Phenobarbital as an Adjunct Therapy for Neonatal Abstinence Syndrome [NCT01175668]68 participants (Actual)Interventional2010-07-31Terminated(stopped due to Based on the planned interim analysis results at 50% recruitment, after IRB reviewed the results, further enrollment was stopped.)
Clonidine Versus Adenosine to Treat Neuropathic Pain [NCT00349921]Phase 224 participants (Actual)Interventional2004-08-31Completed
Clonidine-Remifentanil. Effect of the Combination on Acute Pain and Respiration in Healthy Volunteers [NCT00730054]Phase 1/Phase 212 participants (Actual)Interventional2005-02-28Completed
Clonidine as Pain Relief During ROP Eye Examinations [NCT04902859]Phase 450 participants (Anticipated)Interventional2022-04-25Recruiting
Phase III Evaluation of the Safety and Efficacy of CLONICEL (Clonidine HCl Sustained Release) as Add-on to Psychostimulant Medication vs. Psychostimulant Medication Alone in Children and Adolescents With ADHD [NCT00641329]Phase 3198 participants (Actual)Interventional2008-02-29Completed
Comparison of Fentanyl-bupivacaine and Clonidine-bupivacaine for Breakthrough Pain in Advanced Labor in Patients With Continuous Epidural Analgesia [NCT00691795]Phase 40 participants (Actual)InterventionalWithdrawn(stopped due to Study was recently terminated due to poor enrollment - never enrolled.)
Analgesic Efficacy of Transversus Abdominis Plane (TAP) Block After Lumbar Spine Surgery Through Anterior Approach (Anterior Lumbar or Direct Lateral Interbody Fusion): a Prospective, Randomized, Double-blind Placebo-controlled Study [NCT02778178]Phase 440 participants (Actual)Interventional2016-05-02Completed
A Proof-of-Concept, Randomized, Double-Blind and Placebo Controlled Clinical Trial With Naltrexone and Clonidine Combination (ATNC05) Compared With Placebo in the Treatment of Chronic Back Pain [NCT01415895]Phase 278 participants (Actual)Interventional2011-07-31Completed
The EPIC (Evaluating Perioperative Ischemia Reduction by Clonidine) Study: A Randomized, Double-blinded Trial of Clonidine for Reducing Cardiac Morbidity and Mortality Following Non-cardiac Surgery. [NCT00335582]Phase 4165 participants (Anticipated)Interventional2006-06-30Active, not recruiting
An International Randomised Controlled Trial to Establish the Effects of Low-dose rtPA and the Effects of Early Intensive Blood Pressure Lowering in Patients With Acute Ischaemic Stroke [NCT01422616]Phase 34,587 participants (Actual)Interventional2012-03-31Completed
The Effect of Magnesium Sulfate in Comparison to Clonidine as Adjuvants to Bupivacaine 0.25% in Supraclavicular Brachial Plexus Block in Pediatric Upper Limb Surgeries. Prospective, Randomized, Double-blind Study [NCT06180941]70 participants (Anticipated)Interventional2023-12-31Not yet recruiting
"The Efficacy of Exparel Versus a Multidrug Cocktail in Soft Tissue Tumors" [NCT05355597]Phase 2140 participants (Anticipated)Interventional2021-01-27Recruiting
Clonidine to Prevent Implantable Cardiovertor Defibrillator Firing [NCT00585871]0 participants (Actual)Interventional2006-05-31Withdrawn(stopped due to could not recruit)
Comparative Randomized Controlled Trial Study of General Balanced Anesthesia Based on Opioid and Opioid Sparing Balanced Anesthesia for Cholecystectomy Surgery Via Laparoscopy: Intraoperative and Postoperative Outcomes [NCT02953210]Phase 440 participants (Anticipated)Interventional2016-11-30Enrolling by invitation
Efficacy of Clonidine in the Treatment of Neonatal Abstinence Syndrome: A Prospective, Double Blind, Randomized Controlled Trial [NCT00510016]Phase 280 participants (Actual)Interventional2002-07-31Completed
[NCT01851486]0 participants (Actual)Interventional2013-01-31Withdrawn(stopped due to Labortory focus was changed and study was not opened at all)
Up Regulation of Alpha-1 Receptors Upon Septic Shock ? [NCT01856517]Phase 2/Phase 340 participants (Anticipated)Interventional2013-08-31Terminated
Impact on Maternal and Fetal Wellbeing and on Labor Curve of Intrathecal Clonidine Addiction for Labor Analgesia. A Randomized Controlled Trial. [NCT03018171]Phase 4268 participants (Anticipated)Interventional2017-01-31Recruiting
Clinical Outcome Following Arthroscopic Knee Surgery (COFAKS)-Addendum [NCT03704376]Phase 4125 participants (Actual)Interventional2016-02-01Completed
Intravenous Clonidine Does Not Reduce Pulmonary Artery Pressure in Patients Subjected to Cardiac [NCT01597427]Phase 229 participants (Actual)Interventional2009-03-31Completed
Anxiety-mediated Impairments in Large Elastic Artery Function and the Autonomic Nervous System [NCT03109795]Phase 430 participants (Actual)Interventional2017-04-10Terminated(stopped due to Funding ended)
A Phase 2, Open-Label, Randomized, Controlled, Ascending Dose Cohort, Pharmacokinetic and Safety Study of Oral Lofexidine in Neonates Experiencing Opioid Withdrawal Due to Intrauterine Exposure to Opioids [NCT06047834]Phase 224 participants (Anticipated)Interventional2023-10-02Recruiting
The Effects of Clonidine on the Diuretic Response in Cirrhotic Patients With Ascites and Activation of Sympathetic Nervous System: a Randomized Double-Blind Placebo Controlled Study. [NCT00356226]64 participants Interventional2000-10-31Completed
[NCT00279253]Phase 412 participants Interventional2004-03-31Completed
Comparison of Epidural Bupivacaine-Clonidine With Intravenous Morphine Versus Intravenous Morphine Alone for Post-Operative Pain Relief in Pediatric Patients Undergoing Lower Extremity or Pelvic Osteotomy. [NCT00287326]Phase 340 participants (Anticipated)Interventional2006-01-31Terminated(stopped due to terminated by PI)
Clonidine as Adjunct to Morphine in the Management of Term and Near Term Infants With Neonatal Abstinence Syndrome [NCT03762317]Phase 410 participants (Actual)Interventional2018-04-30Terminated(stopped due to Study was initially suspended due to IND application and later terminated due to the difficulty of obtaining consent during COVID period)
Effect of Clonidine on Responses to Imagery Scripts [NCT00318760]Phase 192 participants (Actual)Interventional2005-06-14Completed
Prospective Assessment of Intraoperative Intra-articular Morphine and Clonidine Injection in Hip Arthroscopy on Postoperative Pain Management [NCT02530151]Phase 470 participants (Actual)Interventional2015-11-30Completed
Consequences of Co-Administration of Propofol With Clonidine and Ketamine Throughout Colon Cancer Surgery [NCT05536362]Phase 160 participants (Actual)Interventional2021-02-01Completed
Growth Hormone Trial for Children With 18q- and Abnormal Growth [NCT00134420]Phase 320 participants (Actual)Interventional2001-02-28Completed
Randomized Clinical Trial of Pregabalin for Opioid Withdrawal Syndrome [NCT03017430]Phase 4100 participants (Actual)Interventional2014-01-31Completed
Epidural Analgesia During Labour. Impact of Clonidine Addition to Levobupivacaine and Sufentanil [NCT00437996]Phase 385 participants (Actual)Interventional2007-02-28Completed
Determining the Role of Periarticular Multimodal Analgesia in Decreasing Perioperative Pain in Tibial Plateau Fractures [NCT05037812]Early Phase 1150 participants (Anticipated)Interventional2019-03-25Active, not recruiting
Protocolized Initiation of Clonidine to Prevent Dexmedetomidine Withdrawal: A Prospective Cohort Study [NCT05575219]Phase 4300 participants (Anticipated)Interventional2022-10-08Recruiting
Clonidine for Tourniquet-related Pain in Children: A Pilot Study [NCT04564430]Phase 420 participants (Anticipated)Interventional2021-03-01Recruiting
Premedication With Oral Clonidine Versus Intraoperative Intravenous Tranexamic Acid in Reduction of Blood Loss During Elective Cesarean Section in Abakaliki - a Randomized Control Trial [NCT05371574]Phase 1112 participants (Anticipated)Interventional2022-01-03Recruiting
Nephropathy in Type 2 Diabetes: Effects of an Intensive Multifactorial Intervention Trial on Cardio-renal Events. [NCT00535925]Phase 4850 participants (Actual)Interventional2005-10-31Completed
Randomized Controlled Doubleblind Pilot Study Comparing Analgosedation Concepts During Placement of Regional Anaesthesia With Either Fentanyl, Remifentanil, Clonidine, EMLA-Patch or Placebo in Regard of Pain Reduction. [NCT04026074]Phase 450 participants (Actual)Interventional2019-07-26Completed
Clonidine in Attention Deficit Hyperactivity Disorder (ADHD) Treatment (CAT) [NCT00031395]Phase 3122 participants (Actual)Interventional1999-09-30Completed
The Addition of Clonidine to 0.2% Ropivacaine for Wound Instillation After Minor Lower Abdominal Surgery in Children [NCT00130091]Phase 2120 participants (Actual)Interventional2009-09-30Completed
Safety and Efficacy of Bilateral Superficial Cervical Plexus Block in Thyroidectomy - a Double Blind Randomized Controlled Trial [NCT01454609]Phase 260 participants (Actual)Interventional2009-01-31Completed
Effects of Clonidine Added to Lidocaine in Sub-Tenon's and Peribulbar Anesthesia: Assessments of Intraocular Pressure (IOP), Ocular Perfusion Pressure (OPP) and Ocular Pulse Amplitude (OPA) [NCT02733757]Phase 280 participants (Actual)Interventional2013-05-31Completed
Will Decreased Noradrenergic Activity Normalize Information Processing in Patients With Schizophrenia? [NCT00206986]40 participants (Anticipated)Interventional2005-05-31Completed
Treatment Targets for Chronic Hypertension in Pregnancy [NCT00194974]Phase 1/Phase 20 participants (Actual)Interventional2004-07-31Withdrawn(stopped due to Lack of funding)
The Pathophysiology and Treatment of Supine Hypertension in Patients With Autonomic Failure [NCT00223717]Phase 1152 participants (Actual)Interventional2001-01-31Completed
A Randomised Trial to Establish the Effects of Early Intensive Blood Pressure Lowering on Death and Disability in Patients With Stroke Due to Acute Intracerebral Haemorrhage [NCT00226096]404 participants (Actual)Interventional2005-11-30Completed
Exploration électroencéphalographie et Pharmacologique Des Dysfonctionnements exécutifs Induits Par la Stimulation cérébrale Profonde du Noyau Sous-thalamique Dans la Maladie de Parkinson [NCT01796483]37 participants (Actual)Interventional2012-10-31Completed
Peri-articular Injections Containing a Corticosteroid During Total Knee Arthroplasty [NCT00492973]101 participants (Actual)Interventional2006-03-31Completed
Single-Dose, Phase 1b Study to Assess Pharmacokinetics, Safety and Tolerability, and Pharmacodynamics of Tizanidine at 4 Different Oral Dose Levels in Pediatric Subjects With Mild to Moderate Spasticity Due to Cerebral Palsy [NCT01405950]Phase 110 participants (Actual)Interventional2011-05-31Terminated(stopped due to Please see 'Further study details as provided by Acorda Therapeutics' for explanation of why study stopped.)
Premedication by Clonidine Intranasal in Pediatric Surgery [NCT03725930]Phase 390 participants (Anticipated)Interventional2019-03-26Recruiting
The Use of Clonidine in Pain and Anxiety Associated With Acute Burn Injury in Children [NCT00580151]9 participants (Actual)Interventional2004-06-30Terminated(stopped due to Closed due to no response from PI to IRB)
A Comparison of Ropivacaine Alone Versus Ropivacaine With Dexamethasone or Clonidine Versus a Combination of Ropivacaine, Dexamethasone, and Clonidine for Supraclavicular Brachial Plexus Block Using Ultrasound:A Prospective, Observer-blinded, Randomized S [NCT02151487]97 participants (Actual)Observational2014-03-31Completed
Efficacy of Multimodal Perioperative Analgesia Protocol With Periarticular Drug Injection in Total Knee Arthroplasty: A Randomized, Double Blind Study [NCT01042093]160 participants (Actual)Interventional2010-01-31Completed
Does Single Injection Adductor Canal Block Improve Postoperative Analgesia in Patients Receiving Periarticular Local Anesthesia Injections for Total Knee Arthroplasty? [NCT02276495]55 participants (Actual)Interventional2014-09-26Active, not recruiting
Black Education and Treatment of Hypertension (BEAT HTN) [NCT00661895]Phase 499 participants (Actual)Interventional2005-08-31Completed
Clonidine for Relapse Prevention in Buprenorphine-Maintenance Patients [NCT00295308]Phase 1208 participants (Actual)Interventional2005-11-08Completed
A Safe Ketamine-Based Therapy for Treatment Resistant Depression [NCT01179009]20 participants (Actual)Interventional2012-04-30Completed
A Study of Effect of Epidural Clonidine on Postoperative Pain Relief, Hyperalgesia and Chronic Pain in Patients Undergoing Colorectal Surgery [NCT00417443]Phase 30 participants (Actual)Interventional2007-12-31Withdrawn
A Comparison of Compliance Between Clonidine Patch and Methyldopa for the Treatment of Chronic Hypertension in Pregnancy [NCT00329511]0 participants (Actual)Interventional2004-09-30Withdrawn(stopped due to Feasibility of study. PI termination)
The Effect of Clonidine-enhanced Sedation on Delirium in Ventilated Critically Ill Patients CATAPRES (Confusion and Alpha-Two Agonist Prescription Randomised Efficacy Study) [NCT01876355]Phase 3115 participants (Anticipated)Interventional2024-01-31Not yet recruiting
Pilot Study for the NorCAPITAL Trial [NCT01507701]5 participants (Actual)Interventional2010-01-31Completed
The Effect of Clonidine in Glycemia During Coronary Artery Bypass Graft With Cardiopulmonary By-pass. [NCT01619436]Phase 446 participants (Actual)Interventional2011-01-31Completed
The Effects of Different Clonidine Concentrations on Axillary Brachial Plexus Block With 1,5% Lidocaine for Upper Limb Surgery: a Prospective Randomized Study [NCT01620112]Phase 260 participants (Actual)Interventional2009-02-28Completed
Intravenous Clonidine for Sedation in Infants and Children Who Are Mechanically Ventilated - Dosing Finding Study [NCT02249039]Phase 114 participants (Actual)Interventional2015-09-30Completed
Multicenter Study of Patients With Hypertension Resistant to Patient Identification and Standardization of Therapeutic [NCT01643434]Phase 42,000 participants (Anticipated)Interventional2012-08-31Recruiting
A Randomized, Double-Blind, Placebo-Controlled, Multiple Ascending Dose Study to Assess the Safety, Tolerability, and Electrocardiographic Effects of Lofexidine When Administered Orally to Methadone Maintained Adult Subjects [NCT01650649]Phase 127 participants (Actual)Interventional2012-07-31Completed
Efficacy of Intraoperative Injections on Postoperative Pain Control During Total Hip Arthroplasty: A Prospective, Blinded, Randomized Controlled Study [NCT03119038]Phase 40 participants (Actual)Interventional2016-04-30Withdrawn(stopped due to Investigator no longer actively pursuing this study.)
A Phase 3, Open-Label, Safety Study of Lofexidine [NCT02363998]Phase 3286 participants (Actual)Interventional2015-02-28Completed
Phase 3, Randomized, Multicenter, Double-Blind, Placebo-Controlled, Efficacy, Safety, and Dose-Response Study of Lofexidine for Treatment of Opioid Withdrawal (Days 1-7) Followed by Open-Label, Variable Dose Lofexidine Treatment (Days 8-14) [NCT01863186]Phase 3603 participants (Actual)Interventional2013-06-30Completed
To Compare lidocaine2%/Clonidine in Combination With Bupivacaine 0.5 % Alone in Equal Volumes for Combined Sciatic-saphenous Nerve Block in Terms of Selectivity of Blockade [NCT01759524]Phase 430 participants (Actual)Interventional2011-10-31Completed
Randomized Clinical Trial for Effectiveness of Clonidine Versus Captopril for Treatment of Postpartum Very High Blood Pressure [NCT01761916]Phase 490 participants (Actual)Interventional2013-01-31Completed
Interest of a Bi-truncal Nerve Block (Femoral + Sciatic) Extended, Systematically Associated With General Anesthesia, in the Femoropopliteal Bypass: Study of Post-operative Analgesia and Peripheral Circulation Downstream. [NCT01785693]Phase 447 participants (Actual)Interventional2013-01-30Completed
Efficacy of Intrathecal Clonidine Versus Neostigmine as Adjuvants to Bupivacaine on Postoperative Maternal and Fetal Outcomes After Elective Cesarean Section: A Randomized Double Blind Controlled Trial [NCT05943613]Phase 1111 participants (Anticipated)Interventional2023-12-01Not yet recruiting
A Randomized, Double-Blind, Placebo-Controlled, Multiple Ascending Dose Study to Assess the Safety, Tolerability, and Electrocardiographic Effects of Lofexidine When Administered Orally to Buprenorphine-Maintained Adult Subjects [NCT01820442]Phase 130 participants (Actual)Interventional2013-03-31Completed
A Phase II Randomized Study of Solifenacin Compared to Clonidine for Reducing Hot Flashes Among Breast Cancer Patients Receiving Adjuvant Hormonal Therapy [NCT01530373]Phase 26 participants (Actual)Interventional2012-02-29Active, not recruiting
DASH After TBI Study: Decreasing Adrenergic or Sympathetic Hyperactivity After Severe Traumatic Brain Injury, A Pilot Randomized Clinical Trial Using Propranolol and Clonidine [NCT01322048]Phase 248 participants (Actual)Interventional2011-08-31Completed
Pharmacological Treatment of Neonatal Abstinence Syndrome: Opiate Versus Non-Opiate [NCT01734551]Phase 431 participants (Actual)Interventional2011-09-30Completed
Clonidine-induced Spinal Acetylcholine Release: Normal Volunteers vs. Neuropathic Pain [NCT00350532]Phase 243 participants (Actual)Interventional2004-09-30Completed
ROPIVACAINE WITH CLONIDINE FOR PEDIATRIC RECTUS SHEATH BLOCKS- THE MAGIC COMBINATION? - A Double Blinded Prospective Study [NCT02439281]50 participants (Actual)Interventional2015-05-31Terminated(stopped due to The patients were discharged on the day of the surgery.)
Reduction of Hip Arthroscopy Post-operative Pain Using Ultrasound-guided Fascia-iliaca Block [NCT02365961]Phase 484 participants (Actual)Interventional2015-04-30Completed
Novel Medications for Opiate Detoxification [NCT00000279]Phase 20 participants Interventional1994-09-30Completed
The Effect of Buccal Infiltration Administration of Clonidine on the Success Rate of Inferior Alveolar Nerve Block on Mandibular Molars With Symptomatic Irreversible Pulpitis: a Randomized Double-blind Clinical Trial [NCT04186299]Phase 40 participants (Actual)Interventional2021-08-31Withdrawn(stopped due to Study activities never commenced.)
A Phase II, Double-blind, Randomized, Placebo-controlled 4-way Crossover Study to Evaluate the Relative Efficacy and Safety of OC Oral Solution (Oxybutynin and Clonidine) for Sialorrhoea in Patients With Parkinson's Disease [NCT01370811]Phase 224 participants (Actual)Interventional2011-08-31Completed
Effectiveness of Clonidine, Dexmedetomidine, and Fentanyl Adjuncts for Labor Epidural Analgesia: A Randomized Controlled Quadruple Blinded Non-Inferiority Trial (CLASSIER Trial) [NCT05487196]Phase 288 participants (Actual)Interventional2022-09-28Completed
Transversus Abdominis Plane (TAP) Block for Cesarean Section [NCT01015807]90 participants (Actual)Interventional2009-11-30Completed
Italian Study on the Cardiovascular Effects of Systolic Blood Pressure Control - CARDIOSIS Study [NCT00421863]Phase 41,111 participants (Actual)Interventional2005-02-28Completed
Randomised Controlled Pilot Study: Does Intraoperative Clonidine Reduce the Incidence of Post-hospitalisation Negative Behaviour Changes in Children Who Are Distressed During the Induction of General Anaesthesia? [NCT02324413]Phase 345 participants (Actual)Interventional2013-10-31Completed
Medications Development for Drug Abuse Disorders [NCT01188421]Phase 1/Phase 2106 participants (Actual)Interventional2010-10-31Completed
Hemodynamic Effect of Intrathecal Clonidine in Hypertensive Subjects: A Pilot Study to Assess Its Effectiveness in Hypertensive Subjects With Poor Blood Pressure Control (Phase II) [NCT01297335]Phase 210 participants (Actual)Interventional2011-02-28Completed
A 40-Week, Phase 4, Double-Blind, Placebo-Controlled, Multicenter, Randomized-Withdrawal Study to Evaluate the Long-Term Efficacy and Safety of KAPVAY™ (Clonidine Hydrochloride) Extended-Release in Children and Adolescents With ADHD [NCT01439126]Phase 4135 participants (Actual)Interventional2011-08-31Completed
[NCT01813149]128 participants (Actual)Interventional2012-08-31Terminated(stopped due to Study halted prematurely and will not resume; participants are no longer being examined or receiving intervention. There is no data collected)
Effectiveness of Perineural Clonidine as an Adjuvant With Ropivacaine for Popliteal Nerve Block in Patients Undergoing Foot and Ankle Surgery [NCT01986751]Phase 1/Phase 214 participants (Actual)Interventional2014-01-31Terminated(stopped due to failure to enroll)
Effect of Clonidine vs. Dexmedetomidine in Addition to Standard Treatment in Agitated Delirium in Intensive Care Patients: Pilot Study. [NCT04758936]Phase 450 participants (Anticipated)Interventional2021-02-01Recruiting
Efficacy of Clonidine in Reducing Iatrogenic-induced Opioid Dependence in Infants: [NCT01360450]Phase 2/Phase 312 participants (Actual)Interventional2011-07-31Terminated(stopped due to The study was treminated because of low accural)
Prospective, Randomized, Double Blinded Comparison of the Analgesic Efficacy of Epidural Clonidine Versus Corticosteroid for Low Back Pain [NCT02239627]16 participants (Actual)Interventional2014-09-30Terminated(stopped due to based on interim anaylsis)
Assessment of the Effect of Clonidine on Pain, Arterial and Intraocular Pressure and Arrhythmias for Cataract Surgery [NCT01677351]Phase 240 participants (Anticipated)Interventional2011-07-31Recruiting
Vascular Dysfunction in Human Obesity Hypertension: Integrative Role of Sympathetic and Renin-Angiotensin Systems [NCT01983462]Phase 233 participants (Actual)Interventional2013-10-31Terminated(stopped due to Funding expired)
Great Auricular Nerve Block for Children Undergoing Tympanomastoid Surgery: Does the Addition of Clonidine Increase the Duration of Postoperative Analgesia? [NCT01638052]Phase 256 participants (Actual)Interventional2006-02-28Completed
Treatment of Neonatal Abstinence Syndrome With Clonidine Versus Morphine as Primary Therapy [NCT03092011]Phase 490 participants (Anticipated)Interventional2018-02-21Recruiting
A Multicenter, Open-label, Single-arm Study to Evaluate the Long-term Use of Clonidine Hydrochloride Topical Gel, 0.1% in the Treatment of Pain Associated With Painful Diabetic Neuropathy [NCT02355158]Phase 2197 participants (Actual)Interventional2014-06-30Completed
Does Intraoperative Clonidine Reduce Post Operative Agitation in Children Anaesthetised With Sevoflurane? A RCT Including Pharmacokinetic Investigation. [NCT02361476]Phase 4379 participants (Actual)Interventional2015-01-31Completed
A Multicenter Randomized, Double-Blind, Placebo-Controlled, 2-Arm Parallel-Group Study to Determine the Efficacy and Safety of Clonidine Hydrochloride Topical Gel, 0.1% in the Treatment of Pain Associated With Painful Diabetic Neuropathy [NCT02068027]Phase 2260 participants (Actual)Interventional2014-03-31Completed
A Prospective Triple-masked Randomized Controlled Trial Measuring Analgesia Duration of Dexamethasone, Buprenorphine, or Clonidine With Ropivacaine for Interscalene Nerve Block [NCT03117140]Phase 4160 participants (Actual)Interventional2013-12-31Completed
Clonidine Versus Phenobarbital as Adjunctive Therapy for Neonatal Abstinence Syndrome [NCT03670160]Phase 225 participants (Actual)Interventional2018-10-01Completed
A Randomized Double Blinded Placebo Controlled Trial Of Transdermal Clonidine for Adjuvant Sedation in Ventilated Trauma Patients Experiencing Delirium [NCT01139996]Phase 422 participants (Actual)Interventional2010-05-31Terminated(stopped due to Difficulty in enrolling participants)
The CLONEMESI Study: a Randomized Placebo-controlled Study With Transdermal Clonidine in the Treatment of Severe Hyperemesis Gravidarum. [NCT01559012]Phase 313 participants (Actual)Interventional2012-02-29Completed
Addition of Clonidine to Ropivacaine in Adductor Canal Block for Postoperative Pain Relief in Total Knee Arthroplasty: A Prospective Randomized Double Blind Placebo Controlled Trial [NCT03057015]Phase 480 participants (Anticipated)Interventional2017-05-22Recruiting
Combination of Dronabinol and Clonidine for Cannabis Dependence in Patients With Schizophrenia [NCT01598896]Phase 2/Phase 312 participants (Actual)Interventional2012-05-31Terminated(stopped due to low enrollment due to limited resources)
Two-arm, Double-blind Randomized Study Comparing Exparel and Exparel Plus an Adductor Canal Block in Total Knee Arthroplasty [NCT02365727]Phase 40 participants (Actual)Interventional2015-04-30Withdrawn(stopped due to Protocol not feasible as written)
Buprenorphine in the Emergency Department: Buprenorphine Versus Clonidine for Opioid Withdrawal [NCT03174067]Phase 426 participants (Actual)Interventional2013-03-31Completed
A Multicenter, Randomized, Double Blind, Parallel-Group Study Comparing the Efficacy and Safety of Clonidine Hydrochloride Topical Gel, 0.1%, to Clonidine Hydrochloride Gel Comparator in the Management of Painful Diabetic Neuropathy [NCT02643251]Phase 2138 participants (Actual)Interventional2015-12-31Completed
A Placebo Controlled Study of Colesevelam in Fecal Incontinence [NCT02628626]Phase 388 participants (Actual)Interventional2015-11-30Completed
A Phase II, Multi-center, Randomised, Double-blind, Placebo-controlled Study Comparing the Efficacy and Safety of Clonidine Lauriad® 50 μg and 100 μg Mucoadhesive Buccal Tablet (MBT) Applied Once Daily to Those of Placebo in the Prevention and Treatment o [NCT01385748]Phase 2183 participants (Actual)Interventional2010-04-30Completed
An International Randomised Controlled Trial to Establish the Effects of Early Intensive Blood Pressure Lowering in Patients With Intracerebral Haemorrhage. [NCT00716079]2,839 participants (Actual)Interventional2008-09-30Completed
A Double-blind Randomised Controlled Clinical Trial of Lofexidine Versus Diazepam in the Management of the Opioid Withdrawal Syndrome During Inpatient Detoxification in Singapore [NCT01675648]Phase 4112 participants (Actual)Interventional2012-08-31Completed
Improving Treatment Outcomes for Prescription Opioid Dependence [NCT02543944]Phase 2/Phase 3117 participants (Actual)Interventional2016-02-29Completed
An Investigator-Initiated, Double-Blind, Patient-Controlled, Randomized Control Trial Comparing the Effectiveness of Liposomal Bupivacaine to a Solution of Bupivacaine, Epinephrine Clonidine and Dexamethasone in Bilateral, Single Shot, Erector Spinae Plan [NCT04603911]Phase 275 participants (Actual)Interventional2020-12-04Active, not recruiting
A Randomized, Double-blind Study Designed to Assess the Bioequivalence and Adhesion Properties of Transdermal Clonidine-VistanexTM Compared to Transdermal Clonidine-Oppanol® Following Transdermal Administration in Healthy Male and Female Volunteers [NCT02096744]Phase 156 participants (Actual)Interventional2014-03-31Completed
Utility of Olanzapine in the Treatment of Opioid Withdrawal in the Emergency Department [NCT02643355]70 participants (Actual)Interventional2015-11-30Completed
Assessment of the Effect of Naltrexone on Lofexidine Single Dose Pharmacokinetics in Healthy Subjects [NCT02446002]Phase 125 participants (Actual)Interventional2015-05-31Completed
Phase I-II Clinical Trial to Determine the Safety of Clonidine in Infants With Hypoxic Ischemic Encephalopathy During Therapeutic Hypothermia [NCT01862250]Phase 1/Phase 213 participants (Actual)Interventional2013-10-03Completed
Comparison of Keppra and Clonidine in the Treatment of Tics in Children With Tourette Syndrome [NCT00370838]Phase 412 participants (Actual)Interventional2007-02-28Completed
Do Intraoperative Periarticular Injections Improve Postoperative Pain Control in Patients Receiving Duramorph (Preservative Free) During Total Knee Arthroplasty? A Prospective, Double-Blind, Randomized Controlled Trial [NCT02570503]Phase 464 participants (Actual)Interventional2015-10-31Terminated(stopped due to Study's primary aims are no longer clinically impactful, as intrathecal morphine has fallen out of favor and replaced with different agents so that outpatient/23 hr surgery is more predictably achievable.)
Dexmedetomidine Versus Clonidine Adjuvants to Levobupivacaine for Transversus Abdominis Plane Block in Pediatric Laparoscopic Orcheopexy: Randomized Double-blind Study [NCT03155646]Phase 2/Phase 390 participants (Actual)Interventional2017-06-10Completed
Clonidine to Prevent Postictal Delirium After ElectroConvulsive Therapy: a Randomised, Placebo-controlled, Triple-blind, Single-centre Trial. [NCT04828226]Phase 4130 participants (Anticipated)Interventional2021-04-27Recruiting
Comparison of Fentanyl-bupivacaine and Clonidine-bupivacaine for Breakthrough Pain in Advanced Labor in Patients With Continuous Epidural Analgesia [NCT01846221]Phase 4101 participants (Actual)Interventional2014-07-15Completed
Pharmacokinetics and Clinical Effects of Escalating Doses of Clonidine in ICU Patients [NCT02466373]Phase 332 participants (Actual)Interventional2016-12-31Completed
A Double Blind, Randomised, Multicentre, Active Controlled, Parallel-group, Phase III Trial to Evaluate the Efficacy, Safety and Pharmacokinetics of Intravenous Clonidine (Hydrochloride) Compared to Midazolam for Sedation in Children From Birth to Less Th [NCT02509273]Phase 328 participants (Actual)Interventional2016-05-31Terminated(stopped due to lack of recruitment)
Effects of a Triple Adjuvant Combination of Buprenorphine, Clonidine, and Dexamethasone on Duration of Brachial Plexus Blocks for Upper Extremity Surgery, a Prospective, Randomized Clinical Trial [NCT05824832]Phase 4120 participants (Anticipated)Interventional2023-02-28Recruiting
A Prospective, Randomized Clinical Trial of Two Periarticular Multimodal Drug Injections in Total Hip and Knee Arthroplasty [NCT02543801]Phase 4239 participants (Actual)Interventional2016-01-25Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00349921 (1) [back to overview]Number Meeting Success Criterion
NCT00350532 (1) [back to overview]Acetylcholine Concentration in Cerebrospinal Fluid
NCT00370838 (7) [back to overview]Multidimensional Anxiety Scale for Children (MASC):
NCT00370838 (7) [back to overview]Yale Global Tic Severity Scale (YGTSS):
NCT00370838 (7) [back to overview]Total Tic Score
NCT00370838 (7) [back to overview]DuPaul Attention Deficit Hyperactivity Disorder (ADHD) Rating Scale:
NCT00370838 (7) [back to overview]Clinical Global Impression-Improvement (CGI-I):
NCT00370838 (7) [back to overview]Child Yale-Brown Obsessive Compulsive Scale (CY-BOCS):
NCT00370838 (7) [back to overview]Modified Pittsburgh Side Effect Scale
NCT00492973 (5) [back to overview]Length of Hospital Stay
NCT00492973 (5) [back to overview]Knee Society Scores
NCT00492973 (5) [back to overview]Knee Range of Motion
NCT00492973 (5) [back to overview]Complications, Such as Infections, Hospital Readmissions, Manipulations Under Anesthesia, Etc.
NCT00492973 (5) [back to overview]Amount of Pain Medication Taken Per Day
NCT00535925 (2) [back to overview]"Number of Participants Who Achieved of BP, HbA1c and Total, HDL and LDL Cholesterol Goals at the End of Intervention Phase"
NCT00535925 (2) [back to overview]"Number of Participants With Overall Fatal and Non-fatal, Major Adverse Cardiovascular Events (MACEs)"
NCT00580151 (2) [back to overview]Anxiety Reduction
NCT00580151 (2) [back to overview]Pain Reduction
NCT00588354 (8) [back to overview]Pain Score at 4 Weeks as Measured by the Multidimensional Pain Inventory (MPI)
NCT00588354 (8) [back to overview]Pain Disability Score at 2 Weeks as Measured by Oswestry Low Back Pain Disability Questionnaire (ODI)
NCT00588354 (8) [back to overview]Pain Score at 2 Weeks as Measured by the Multidimensional Pain Inventory (MPI)
NCT00588354 (8) [back to overview]Pain Intensity Score at 4 Weeks as Measured by Pain Intensity Numerical Rating Scale (PI-NRS)
NCT00588354 (8) [back to overview]Pain Intensity Score at 2 Weeks as Measured by Pain Intensity Numerical Rating Scale (PI-NRS)
NCT00588354 (8) [back to overview]Pain Disability Score at 4 Weeks as Measured by the Roland-Morris Disability Questionnaire
NCT00588354 (8) [back to overview]Pain Disability Score at 4 Weeks as Measured by Oswestry Low Back Pain Disability Questionnaire
NCT00588354 (8) [back to overview]Pain Disability Score at 2 Weeks as Measured by the Roland-Morris Disability Questionnaire
NCT00661895 (1) [back to overview]Percentage of Subjects Achieving Blood Pressure Goals
NCT00678379 (7) [back to overview]Total Number of Post-operative Doses of Analgesics.
NCT00678379 (7) [back to overview]Total Time Until Discharge From Hospital.
NCT00678379 (7) [back to overview]Number and Percent of Participants Able to Tolerate a Regular Diet
NCT00678379 (7) [back to overview]Number and Percent of Participants Able to Tolerate Only a Soft Diet
NCT00678379 (7) [back to overview]Number and Percent of Participants Able to Tolerate Only Liquids
NCT00678379 (7) [back to overview]Mean Visual Analog Scale Pain Number.
NCT00678379 (7) [back to overview]Median Number of Pain Medication Doses
NCT00695565 (14) [back to overview]Change From Baseline to Week 12 in the McGill Pain Questionnaire (Short Form) Total Score
NCT00695565 (14) [back to overview]Change From Baseline in the Brief Pain Inventory Functional Interference Scale at Week 12; mLOCF Imputation
NCT00695565 (14) [back to overview]Change From Baseline to Week 12 in Overall Quality of Sleep (Chronic Pain Sleep Inventory)
NCT00695565 (14) [back to overview]Change From Baseline to Week 12 in the Anxiety Score of the Hospital Anxiety and Depression Scale (HADS)
NCT00695565 (14) [back to overview]Clinician Global Impression of Change (CGIC) at Week 12
NCT00695565 (14) [back to overview]Change From Baseline to Week 12 in the Average Daily Pain NPRS (Numeric Pain Rating Scale) Score; mLOCF Imputation
NCT00695565 (14) [back to overview]Change From Baseline in Average Daily Pain NPRS Score for Each Week of Treatment; mLOCF Imputation
NCT00695565 (14) [back to overview]Percentage of Subjects Who Experience at Least 50% Reduction in Average Daily Pain From Baseline; mLOCF Imputation
NCT00695565 (14) [back to overview]Percentage of Subjects Who Experience at Least 30% Reduction in Average Daily Pain From Baseline; mLOCF Imputation
NCT00695565 (14) [back to overview]Change in Blood Pressure From Baseline to Week 12
NCT00695565 (14) [back to overview]Patient Global Impression of Change (PGIC) at Week 12
NCT00695565 (14) [back to overview]Change From Baseline to Week 12 in the Depression Score of the Hospital Anxiety and Depression Scale (HADS)
NCT00695565 (14) [back to overview]Change From Baseline in the Brief Pain Inventory (BPI) Severity Scale at Week 12; mLOCF Imputation
NCT00695565 (14) [back to overview]Change From Baseline to Week 12 in the Worst Daily Pain NPRS Score; mLOCF Imputation
NCT00716079 (2) [back to overview]A Composite of Death or Dependency, With Dependency Being Defined by a Score of 3 to 5 on the Modified Rankin Scale (mRS)
NCT00716079 (2) [back to overview]Death at 90 Days
NCT00723190 (12) [back to overview]Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale-fourth Edition (ADHDRS-IV Scale) (18 Items Scored, 0 [Never/Rarely] to 3 [Very Often]; Total Possible Score Range, 0-54) at Months 1, 2, 3, 4, 6, 9, and 12
NCT00723190 (12) [back to overview]Change From Baseline in Clinical Global Impressions-Improvement (CGI-I) at Months 1, 2, 3, 4, 6, 9, and 12
NCT00723190 (12) [back to overview]Change From Baseline in Clinical Global Impressions-Severity (CGI-S) at Months 1, 2, 3, 4, 6, 9, and 12
NCT00723190 (12) [back to overview]Safety Assessment in Terms of Adverse Events (Treatment-emergent [TEAEs] and Serious [SAEs])
NCT00723190 (12) [back to overview]Safety Assessment in Terms of Adverse Events (Treatment-emergent [TEAEs] and Serious [SAEs])
NCT00723190 (12) [back to overview]Change From Baseline in 12-lead Electrocardiogram in Terms of Heart Rate at Week 4
NCT00723190 (12) [back to overview]Change From Baseline in Body Temperature at Week 4
NCT00723190 (12) [back to overview]Change From Baseline in Diastolic Blood Pressure at Week 4
NCT00723190 (12) [back to overview]Change From Baseline in Heart Rate at Week 4
NCT00723190 (12) [back to overview]Change From Baseline in Systolic Blood Pressure at Week 4
NCT00723190 (12) [back to overview]Change From Baseline in 12-lead Electrocardiogram in Terms of QT, QTc Fridericia (QTcF), and QTc Bazett's (QTcB) at Week 4
NCT00723190 (12) [back to overview]Change From Baseline in Body Weight at Weeks 1, 2, 3, 4, and Months 2, 3, 4, 5, 6, 9, and 12
NCT00858845 (3) [back to overview]Change in Muscle Sympathetic Nerve Activity
NCT00858845 (3) [back to overview]Change in Proportion of Type 1 Fibers
NCT00858845 (3) [back to overview]Change in Citrate Synthase Activity as an Estimate of Mitochondrial Activity
NCT00884832 (13) [back to overview]Percentage of Bowel Movements With Semi-formed and Loose Stools Post-treatment Adjusted for Baseline
NCT00884832 (13) [back to overview]Percentage of Days With Fecal Incontinence (FI)
NCT00884832 (13) [back to overview]Percentage of Days With FI Post-treatment Adjusted for Baseline
NCT00884832 (13) [back to overview]Satisfaction With Treatment
NCT00884832 (13) [back to overview]Mean Percentage of Bowel Movements Which Were Incontinent
NCT00884832 (13) [back to overview]Impact of Fecal Incontinence on Baseline Quality of Life
NCT00884832 (13) [back to overview]Impact of Fecal Incontinence on Post-Treatment Quality of Life
NCT00884832 (13) [back to overview]Mean Fecal Incontinence and Constipation Assessment (FICA) Score
NCT00884832 (13) [back to overview]Mean Number of Days With Fecal Incontinence
NCT00884832 (13) [back to overview]Mean Number of Fecal Incontinence Episodes
NCT00884832 (13) [back to overview]Mean Severity of Fecal Incontinence
NCT00884832 (13) [back to overview]Percentage of Bowel Movements Preceded by Rectal Urgency
NCT00884832 (13) [back to overview]Percentage of Bowel Movements With Semi-formed and Loose Stools in Subjects With and Without Diarrhea
NCT01015807 (1) [back to overview]Wound Hyperalgesia Index (WHA) Assessed 48 Hrs After Block Placement in the Different Groups
NCT01042093 (3) [back to overview]Numerical Rating Scale (NRS) Pain Scores During Hospitalization.
NCT01042093 (3) [back to overview]Narcotic Consumption During Hospitalization
NCT01042093 (3) [back to overview]Knee Society Pain Scores at 6 Week Follow-up Appointment
NCT01082874 (1) [back to overview]Composite of All-cause Mortality and Nonfatal MI
NCT01175668 (2) [back to overview]Length of Treatment With Neonatal Morphine Sulfate
NCT01175668 (2) [back to overview]Total Dose of NMS Used
NCT01179009 (1) [back to overview]Montgomery-Asberg Depression Rating Scale (MADRS) Total Score
NCT01188421 (1) [back to overview]Mean Ratings on Clinical Opiate Withdrawal Scale (COWS) Measure of Withdrawal During Double-blind Taper (7-days) and Post-taper (7-days) Period.
NCT01297335 (3) [back to overview]Change in Blood Pressure After Intrathecal Injection of Clonidine.
NCT01297335 (3) [back to overview]Likert Scale Pain Rating
NCT01297335 (3) [back to overview]Changes in Visual Analogue Scale (VAS) Ratings of Sedation and Sensation of Dry Mouth Reported by the Subjects, Pre and 1 Hour Post Injection
NCT01322048 (2) [back to overview]Ventilator-free Days
NCT01322048 (2) [back to overview]Plasma Norepinephrine Levels
NCT01360450 (1) [back to overview]Time to Complete Detoxification
NCT01370811 (3) [back to overview]Saliva Secreted Rate
NCT01370811 (3) [back to overview]Numeric Rating Scale (NRS) Measurements of Subjective Judgment of Excessive Saliva Production
NCT01370811 (3) [back to overview]Evaluation of the Safety and Tolerability of Different Combinations of Oxybutynin and Clonidine (OC Oral Solution) in Patients Suffering From Parkinson's Disease With Excessive Salivation
NCT01385748 (10) [back to overview]At Least One Opioid Use (Class 3 Analgesic)
NCT01385748 (10) [back to overview]Time to Onset of Severe Oral Mucositis
NCT01385748 (10) [back to overview]Salivary Flow Assessment Using the National Cancer Institute-Common Terminology Criteria (NCI-CTC) for Xerostomia: Time to First Grade 2 or Higher
NCT01385748 (10) [back to overview]Overall Survival
NCT01385748 (10) [back to overview]Opioid Use: Minimal Total Cumulative Dose Administered (Median, Range)
NCT01385748 (10) [back to overview]Opioid Use: Minimal Total Cumulative Dose Administered (Mean, Standard Deviation)
NCT01385748 (10) [back to overview]Cumulative Radiation Dose at Which Severe Oral Mucositis (World Health Organization [WHO] Score ≥ 3) Was First Observed
NCT01385748 (10) [back to overview]The Overall Incidence of Grade 3/4 Mucositis During the Active Phase.
NCT01385748 (10) [back to overview]The Maximum Severity of Oral Mucositis
NCT01385748 (10) [back to overview]Overall Treatment Compliance According to the Patient Diary
NCT01405950 (2) [back to overview]Pharmacokinetic (PK) Parameter Cmax (Maximum Observed Drug Concentration in Plasma) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.
NCT01405950 (2) [back to overview]Pharmacokinetic (PK) Parameter AUC0-8 (Area Under the Concentration-time Curve From Time 0 to 8 Hours) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.
NCT01439126 (8) [back to overview]Long-term Maintenance of Efficacy of KAPVAY in Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD) as Measured by the Percentage of Treatment Failures in the KAPVAY vs. Placebo Groups
NCT01439126 (8) [back to overview]Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the Weiss Functional Impairment Rating Scale-Parent (WFIRS-P)
NCT01439126 (8) [back to overview]Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the Epworth Sleepiness Scale for Children (ESS-C)
NCT01439126 (8) [back to overview]Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the Clinical Global Impressions-Severity of Illness Scale (CGI-S)
NCT01439126 (8) [back to overview]Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the ADHD-Rating Scale-4th Edition (ADHD-RS-IV)
NCT01439126 (8) [back to overview]Long-term Safety of KAPVAY in Children and Adolescents With ADHD Based on the Assessment of Adverse Events (AEs), Serious Adverse Events (SAEs), AEs Leading to Study Drug Discontinuation, Clinically Significant Changes or Abnormalities in Vital Signs
NCT01439126 (8) [back to overview]To Evaluate the Long-term Efficacy of KAPVAY in Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD) as Measured by the Time to Treatment Failure From the Start of Randomized-withdrawal Period
NCT01439126 (8) [back to overview]Long-term Safety of KAPVAY in Children and Adolescents With ADHD Based on the Assessment of Changes in the Columbia Suicide Severity Rating Scale (C-SSRS)
NCT01559012 (10) [back to overview]Newborn Outcome Measure: APGAR Score.
NCT01559012 (10) [back to overview]PUQE Score for Assessment of Severity in Hyperemesis Gravidarum
NCT01559012 (10) [back to overview]Diastolic Blood Pressure
NCT01559012 (10) [back to overview]Morning Urine Ketonuria
NCT01559012 (10) [back to overview]Pregnancy Outcome Measures: Birth Weight.
NCT01559012 (10) [back to overview]Number of Days Off i.v. Therapy, the TD System (Clonidine/Placebo) Being Applied Only
NCT01559012 (10) [back to overview]Systolic Blood Pressure
NCT01559012 (10) [back to overview]VAS Score for Assessment of Severity in Hyperemesis Gravidarum
NCT01559012 (10) [back to overview]Number of Patients Choosing Active Treatment for Off-label, Compassionate Use.
NCT01559012 (10) [back to overview]Daily Doses of Standard Antiemetic Drugs Required in the Two Different Periods.
NCT01598896 (4) [back to overview]Change From Baseline in Cannabis Use at 10 Weeks
NCT01598896 (4) [back to overview]Change From Baseline in Cannabis Use at 14 Weeks
NCT01598896 (4) [back to overview]Change in Craving Symptoms From Baseline at 10 Weeks
NCT01598896 (4) [back to overview]Change in Craving Symptoms From Baseline at 14 Weeks
NCT01638052 (3) [back to overview]Average Observer-Rated Patient Pain Scores
NCT01638052 (3) [back to overview]Number of Participants Requiring Use of Rescue Analgesic Medication in the Initial 24 Hours Postoperatively
NCT01638052 (3) [back to overview]Number of Participants With Nausea/Vomiting
NCT01734551 (4) [back to overview]Duration of Treatment
NCT01734551 (4) [back to overview]Bayley Scales of Infant and Toddler Development Third Edition
NCT01734551 (4) [back to overview]Finnegan Neonatal Abstinence Scoring System
NCT01734551 (4) [back to overview]Neurobehavioral Performance Summary Scores From the Neonatal Intensive Care Unit Network Neurobehavioral Scale (NNNS)
NCT01813149 (1) [back to overview]Expression of α1-adrenoceptors (α1-AR) in Dermal Nerve Bundles in the CRPS-affected Limb of Phenylephrine Responders and Non-responders
NCT01846221 (5) [back to overview]Neonatal Apgar Score
NCT01846221 (5) [back to overview]Number of Spontaneous Vaginal Deliveries
NCT01846221 (5) [back to overview]Number of Subjects With Success Rate at 15 Minutes Post-epidural Bolus Injection
NCT01846221 (5) [back to overview]Maternal Heart Rate
NCT01846221 (5) [back to overview]Maternal Systolic Blood Pressure
NCT01862250 (4) [back to overview]Steady State Clonidine Blood Levels During Hypothermia
NCT01862250 (4) [back to overview]Presence of Shivering After Clonidine
NCT01862250 (4) [back to overview]Amount of Morphine Given
NCT01862250 (4) [back to overview]Time to Passive Rewarming
NCT01863186 (2) [back to overview]Completion Status
NCT01863186 (2) [back to overview]Difference Between the Overall Means From Short Opiate Withdrawal Scale of Gossop (SOWS-Gossop) Scores
NCT01983462 (2) [back to overview]Aortic Stiffness
NCT01983462 (2) [back to overview]24 Hour Average Systolic Blood Pressure
NCT02068027 (2) [back to overview]Change From Baseline to Day 84 (Week 12) in Numeric Pain Rating Scale Score
NCT02068027 (2) [back to overview]Mean Daily Worst Pain Intensity Numeric Pain Rating Scale Scores
NCT02096744 (4) [back to overview]AUC0-inf(Area Under the Concentration-time Curve of Clonidine in Plasma Over the Time Interval From 0 to Infinity)
NCT02096744 (4) [back to overview]AUC0-168 (Area Under the Concentration-time Curve of Clonidine in Plasma Over the Time Interval From 0 to 168 h)
NCT02096744 (4) [back to overview]Cavg (Average of Measured Concentrations of Clonidine in Plasma on Days 5, 6, and 7)
NCT02096744 (4) [back to overview]Cmax (Maximum Concentration of Clonidine in Plasma)
NCT02151487 (2) [back to overview]Postoperative Analgesia
NCT02151487 (2) [back to overview]Duration of the Sensorial Supraclavicular Block
NCT02355158 (1) [back to overview]Summary of Neuropathic Pain Symptom Inventory (NPSI)
NCT02361476 (5) [back to overview]Fentanyl and Morphine Requirements
NCT02361476 (5) [back to overview]Adverse Events
NCT02361476 (5) [back to overview]Postoperative Agitation
NCT02361476 (5) [back to overview]First Administration of Fentanyl or Morphine
NCT02361476 (5) [back to overview]Pain Assessment
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Occurrence of Adverse Events (AEs) Not Related to Opioid Withdrawal
NCT02363998 (31) [back to overview]Occurrence of Per Protocol Adverse Events of Special Interest (AESI)
NCT02363998 (31) [back to overview]Overall Treatment Emergent Adverse Events (TEAEs) by Severity
NCT02363998 (31) [back to overview]Safety Electrocardiograms (ECG) Evaluation Shift From Baseline to Post Dose and End of Study
NCT02363998 (31) [back to overview]Overall Occurrence of Serious Treatment Emergent Adverse Events (Serious TEAEs)
NCT02363998 (31) [back to overview]Overall Occurrence of Treatment Emergent Adverse Events (TEAEs)
NCT02363998 (31) [back to overview]Clinical Laboratory Test Change From Baseline: Chemistry
NCT02363998 (31) [back to overview]Clinical Laboratory Test Change From Baseline: Hematology
NCT02363998 (31) [back to overview]Clinical Laboratory Test Change From Baseline: Urinalysis
NCT02363998 (31) [back to overview]Columbia Suicide Severity Rating Scale Questionnaire (C-SSRS): Suicidal Ideation and Behavior Numbers
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Pulse (Bpm): Vital Signs
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Pulse (Bpm): Vital Signs
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Pulse (Bpm): Vital Signs
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Pulse (Bpm): Vital Signs
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Pulse (Bpm): Vital Signs
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Pulse (Bpm): Vital Signs
NCT02363998 (31) [back to overview]Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign
NCT02365961 (5) [back to overview]Visual Analog Scale
NCT02365961 (5) [back to overview]Total Number of Episodes of Nausea and Vomiting
NCT02365961 (5) [back to overview]Time in PACU
NCT02365961 (5) [back to overview]Opioid Consumption
NCT02365961 (5) [back to overview]Hospital Readmission
NCT02439281 (7) [back to overview]Duration of Sensory Block (Paresthesia)
NCT02439281 (7) [back to overview]Complications Rate
NCT02439281 (7) [back to overview]Change in Anxiety Scores
NCT02439281 (7) [back to overview]Average Pain Severity at the Umbilicus Laparoscopic Site
NCT02439281 (7) [back to overview]Satisfaction With Pain Control From Patient
NCT02439281 (7) [back to overview]Duration of Analgesia at Umbilicus Instrument Site-How Many Minutes Passed From the Time When the Blocks Where Performed Until Patient Reported Pain at Umbilicus
NCT02439281 (7) [back to overview]Medication Consumption
NCT02530151 (3) [back to overview]Quality of Recovery (QoR-15) Scores for Patient Reported Recovery Following Surgery
NCT02530151 (3) [back to overview]Visual Analog Scale (VAS) Pain Scores
NCT02530151 (3) [back to overview]Opioid Consumption in the Acute Postoperative Period
NCT02543801 (3) [back to overview]Narcotic Consumption
NCT02543801 (3) [back to overview]Length of Stay
NCT02543801 (3) [back to overview]Pain Score
NCT02543944 (4) [back to overview]Detox Phase Completers
NCT02543944 (4) [back to overview]Vivitrol Injection Receivers
NCT02543944 (4) [back to overview]NTX Transition Initiation
NCT02543944 (4) [back to overview]Detoxification Phase: Changes in Percent of Illicit Opioid-positive Urine Samples Over Time
NCT02570503 (1) [back to overview]Narcotic Use During Hospitalization
NCT02628626 (15) [back to overview]Percent of Incontinent Bowel Movements to be Semi-Formed Stools During Treatment
NCT02628626 (15) [back to overview]Number of Participants to Report a 50% or Greater Reduction in Weekly Fecal Incontinence (FI) Episodes
NCT02628626 (15) [back to overview]Number of Semi-Formed Stools Per Week
NCT02628626 (15) [back to overview]Percent of Incontinent Bowel Movements During Treatment
NCT02628626 (15) [back to overview]Total Fecal Incontinence Episodes
NCT02628626 (15) [back to overview]Daily Stool Frequency
NCT02628626 (15) [back to overview]Delay of Bowel Movement
NCT02628626 (15) [back to overview]Loperamide Tablets Per Week
NCT02628626 (15) [back to overview]Stool Consistency
NCT02628626 (15) [back to overview]Severity of Fecal Incontinence
NCT02628626 (15) [back to overview]Severity of Bowel Symptoms
NCT02628626 (15) [back to overview]Percent of Incontinent Bowel Movements to be Semi-Formed Stools Pre-Treatment
NCT02628626 (15) [back to overview]Percent of Incontinent Bowel Movements Pre-treatment
NCT02628626 (15) [back to overview]Volume of Fecal Incontinence
NCT02628626 (15) [back to overview]Fecal Incontinence Quality of Life (FI-QoL)
NCT02643251 (2) [back to overview]Change From Baseline to Day 84 (Week 12) in Numeric Pain Rating Scale Score
NCT02643251 (2) [back to overview]Mean Daily Worst Pain Intensity Numeric Pain Rating Scale Scores
NCT02643355 (4) [back to overview]Clinical Opiate Withdrawal Scale Score at the Time of Disposition
NCT02643355 (4) [back to overview]Clinical Opiate Withdrawal Scale Score at 1 Hour Post Medication
NCT02643355 (4) [back to overview]Clinical Opiate Withdrawal Scale Score at 2 Hours Post Medication
NCT02643355 (4) [back to overview]Number of Participants That Received Rescue Medication for Withdrawal Symptoms Within 1 Hour
NCT02733757 (1) [back to overview]Intraocular Pressure (IOP)
NCT02740127 (3) [back to overview]Post-operative Pain the First 24hrs
NCT02740127 (3) [back to overview]Post-Operative Pain Medication Usage in Post Anesthesia Care Unit (PACU)
NCT02740127 (3) [back to overview]Length of Hospital Stay
NCT02741713 (5) [back to overview]Post-operative Axillary Pain
NCT02741713 (5) [back to overview]Time From Block Placement to Onset of Axillary Pain
NCT02741713 (5) [back to overview]Total Opioid Usage
NCT02741713 (5) [back to overview]Numerical Rating Scale Pain Scores (0-10) at Rest
NCT02741713 (5) [back to overview]Percentage of Participants With Episodes of Nausea or Vomiting
NCT02891798 (8) [back to overview]Performed-based Physical Function is Assessed Using the Repeated Chair Stand Test.
NCT02891798 (8) [back to overview]Performed-based Physical Function is Assessed Using the Self-Selected Gait Speed Test.
NCT02891798 (8) [back to overview]Performed-based Physical Function is Assessed Using the Standing Balance Test.
NCT02891798 (8) [back to overview]SF-MPQ2 Continuous Pain Subscore Difference From Baseline
NCT02891798 (8) [back to overview]Quality of Recovery 15 Item Scale (QoR-15) Total Score
NCT02891798 (8) [back to overview]Short-Form McGill Pain Questionnaire (Version 2) Total Score Difference From Baseline
NCT02891798 (8) [back to overview]SF-MPQ2 Intermittent Pain Subscore Difference From Baseline
NCT02891798 (8) [back to overview]Quality of Recovery 15 Item Scale (QoR-15) Total Score
NCT03007966 (12) [back to overview]Number of Participants With Presence of Opioid Related Side Effects--Itching
NCT03007966 (12) [back to overview]Number of Participants With Presence of Opioid Related Side Effects--Itching
NCT03007966 (12) [back to overview]Total Opioid Consumption
NCT03007966 (12) [back to overview]Time to First Oral Analgesic
NCT03007966 (12) [back to overview]Post-operative Verbal Pain Score With Movement
NCT03007966 (12) [back to overview]Post-operative Verbal Pain Score With Activity
NCT03007966 (12) [back to overview]Post-operative Verbal Pain Score at Rest
NCT03007966 (12) [back to overview]Post-operative Verbal Pain Score at Rest
NCT03007966 (12) [back to overview]Number of Participants With Presence of Opioid Related Side Effects--Vomiting
NCT03007966 (12) [back to overview]Number of Participants With Presence of Opioid Related Side Effects--Vomiting
NCT03007966 (12) [back to overview]Number of Participants With Presence of Opioid Related Side Effects--Nausea
NCT03007966 (12) [back to overview]Number of Participants With Presence of Opioid Related Side Effects--Nausea
NCT03117140 (15) [back to overview]Number of Patients Reporting Nausea at Home
NCT03117140 (15) [back to overview]Number of Patients Reporting Itching in the PACU
NCT03117140 (15) [back to overview]Number of Patients Reporting Itching at Home
NCT03117140 (15) [back to overview]Motor Duration of Block
NCT03117140 (15) [back to overview]Number of Patient With Blood Pressure Changes in the Second Stage Recovery Area
NCT03117140 (15) [back to overview]Number of Patients Reporting Nausea in the PACU
NCT03117140 (15) [back to overview]Number of Patients Vomiting in the PACU (Post-Anesthesia Care Unit)
NCT03117140 (15) [back to overview]Pain Score Reported by Patients at First Phone Call
NCT03117140 (15) [back to overview]Patient Reporting Vomiting at Home
NCT03117140 (15) [back to overview]Sensory Duration of Block
NCT03117140 (15) [back to overview]Duration of Analgesia
NCT03117140 (15) [back to overview]Surgical Length
NCT03117140 (15) [back to overview]Surgical Position
NCT03117140 (15) [back to overview]Number of Patients With Blood Pressure (BP) Changes in the PACU
NCT03117140 (15) [back to overview]Block Set up Time
NCT03670160 (5) [back to overview]Readmission Rate
NCT03670160 (5) [back to overview]Number of Patients Requiring Triple Therapy
NCT03670160 (5) [back to overview]Time From Initiation of Adjunctive Therapy Until Hospital Discharge
NCT03670160 (5) [back to overview]Length of Stay
NCT03670160 (5) [back to overview]Length of Oral Morphine Sulfate Therapy
NCT03704376 (17) [back to overview]Narcotics Use as Assessed by Morphine Equivalents Consumed
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Number of Successful Repetitions With Straight Leg Raise Test
NCT03704376 (17) [back to overview]Number of Successful Repetitions With Straight Leg Raise Test
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03704376 (17) [back to overview]Quadriceps Muscle Activation as Assessed by Surface Electromyography (sEMG)
NCT03704376 (17) [back to overview]Quadriceps Muscle Activation as Assessed by Surface Electromyography (EMG)
NCT03704376 (17) [back to overview]Quadriceps Muscle Activation as Assessed by Surface Electromyography (EMG)
NCT03704376 (17) [back to overview]Number of Successful Repetitions With Straight Leg Raise Test
NCT03704376 (17) [back to overview]Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale
NCT03762317 (6) [back to overview]Average Daily Dose of Oral Morphine Over Hospital Stay
NCT03762317 (6) [back to overview]Duration of Hospital Stay
NCT03762317 (6) [back to overview]Duration of Pharmacotherapy for NAS
NCT03762317 (6) [back to overview]Maximum Dose of Morphine Used
NCT03762317 (6) [back to overview]Total Number of Episodes of Blood Pressure (mm of Hg) Variability
NCT03762317 (6) [back to overview]Total Number of Episodes of Heart Rate Variability (Heart Beats/Min)
NCT04188730 (7) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Measurable Concentration (AUC0-t)
NCT04188730 (7) [back to overview]Time to Maximum Plasma Concentration (Tmax)
NCT04188730 (7) [back to overview]Occurrence of Adverse Events (AEs)
NCT04188730 (7) [back to overview]Mean Maximum Plasma Concentration (Cmax)
NCT04188730 (7) [back to overview]First-order Terminal Rate Constant (λz)
NCT04188730 (7) [back to overview]First-order Terminal Half-life (T½)
NCT04188730 (7) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to Time Infinity (AUC0-∞)

Number Meeting Success Criterion

Verbal pain report 2 hours post injection compared to baseline verbal pain scores prior to injection (NCT00349921)
Timeframe: baseline and 2 hours

Interventionparticipants meeting success criterion (Number)
Clonidine10
Adenosine5
Placebo0

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Acetylcholine Concentration in Cerebrospinal Fluid

Acetylcholine levels in CSF after administration of intrathecal clonidine measured by High-performance liquid chromatography (HPLC). (NCT00350532)
Timeframe: 60 minutes

Interventionpicograms per milliliter (pg/ml) (Mean)
Neuropathic Pain Subjects406
Healthy Subjects383

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Multidimensional Anxiety Scale for Children (MASC):

"The child's anxiety will be followed using the multidimensional Anxiety Scale for Children (MASC) (Stallings and March, 1995) and is now considered the preferred instrument for rating childhood anxiety. It is a 39-item questionnaire, ranking each item as Never, Rarely, Sometimes, or Often (0, 1, 2, 3). The sum of all responses yeilds a score (maximum MASC score is 117). A score of 0 represents no anxiety, and a score of 117 represents severe anxiety." (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

,
Interventionscores on a scale (Mean)
BaselineFinal
Clonidine25.225
Levetiracetam32.927.5

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Yale Global Tic Severity Scale (YGTSS):

The YGTSS is a semi-structured clinical interview designed to measure current tic severity [Leckman et al., 1989], and consists of separate rating of motor (0-25) and vocal (0-25) tics. Ratings are made along 5 discriminant dimensions, scaled 0-5 for each including number, frequency, intensity, complexity, and interference. Total of these scores (0-50) is a Total Tic Score (TTS). The YGTSS contains an impairment ranking, 0-50 points, based on the impact of the tic disorder on areas such as self esteem, family life, social acceptance, and school. 0=no tics present; 100=most severe tics. (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

,
Interventionscores on a scale (Mean)
BaselineFinal
Clonidine48.743.1
Levetiracetam45.248.8

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Total Tic Score

The TTS is a portion of the YGTSS [Leckman et al., 1989], and consists of separate rating of motor (0-25) and vocal (0-25) tics. Ratings are made along 5 discriminant dimensions, scaled 0-5 for each including number, frequency, intensity, complexity, and interference. Total of these scores (0-50) is a Total Tic Score (TTS). A score of 0 represent no tics present, a score of 50 represents the most severe tics in each category listed. (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

,
Interventionscores on a scale (Mean)
BaselineFinal
Clonidine25.221.8
Levetiracetam22.723.6

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DuPaul Attention Deficit Hyperactivity Disorder (ADHD) Rating Scale:

The presence of Attention Deficit Hyperactivity Disorder (ADHD) symptoms are assessed using the Diagnostic and Statistical Manual of Mental Disorders (DSM-IV) version of the DuPaul ADHD rating scale, which incorporates the symptom items for ADHD from the DSM into a rating scale format that quantifies symptom severity. Each item is rated as not at all, just a little, pretty much, and very much (0, 1, 2, and 3). There are 18 items in total are summed, with a minimum score of 0 (meaning no inattention or hyperactivity) with a maximum score of 54 (severe inattention and hyperactivity). (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

,
Interventionscores on a scale (Mean)
BaselineFinal
Clonidine12.611.9
Levetiracetam12.512.7

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Clinical Global Impression-Improvement (CGI-I):

"Clinical Global Impression-Improvement (CGI-I): The CGI-I is used to compare current severity to baseline. A score of 1 corresponds to very much improved; 2 equals much improved; 3 denotes minimal change; and 4 represents no change. Scores above 4 are used to indicate deterioration, i.e., 5 equals minimally worse; 6 is much worse; and 7 is very much worse." (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

,
Interventionscores on a scale (Mean)
BaselineFinal
Clonidine4.14
Levetiracetam4.14.1

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Child Yale-Brown Obsessive Compulsive Scale (CY-BOCS):

The severity of obsessive-compulsive disorder (OCD) is evaluated using the CY-BOCS [Scahill et al 1997]. Obsessions and compulsions are rated on 5 separate scales yielding three summary scores: Obsessions (0-20), Compulsions (0-20) and Total score (0-40). The CY-BOCS is the most widely used instrument to assess the severity of OCD symptoms in research studies. It includes checklist of specific obsessions and compulsions followed by examiner ratings of time spent, interference, distress, resistance and control over the obsessions and compulsions.0=no obsessions or compulsions; 40=most severe OC (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

,
Interventionscores on a scale (Mean)
BaselineFinal
Clonidine3.13.2
Levetiracetam4.72.2

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Modified Pittsburgh Side Effect Scale

"Side effects will be assessed by an expanded (modified) Pittsburgh Side Effect Scale modified to include side effects of levetiracetam and clonidine. Significant adverse events will be reported to the UCB, JCCI, and FDA within 24 hours. Positive responses are tallied as number of side effects for the responding period." (NCT00370838)
Timeframe: Baseline (Day 8 or Day 64), Final (6 weeks later: Day 50 or Day 106)

InterventionNumber of Side Effects (Mean)
Levetiracetam2.1
Clonidine3.4

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Length of Hospital Stay

(NCT00492973)
Timeframe: days after surgery

Interventiondays (Mean)
Control Group3.5
Corticosteroid2.6

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Knee Society Scores

The Knee Society Score is on a scale of 0 to 100, with 0 being the worst possible score, and 100 being the best possible score. The Knee Society Score takes into account subjective patient reports of pain and functional ability as well as clinical measures of passive knee range of motion. (NCT00492973)
Timeframe: 3 months postoperative

Interventionunits on a scale (Mean)
Control Group87.1
Corticosteroid83.3

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Knee Range of Motion

(NCT00492973)
Timeframe: 3 months

Interventiondegrees (Mean)
Control Group112.5
Corticosteroid112.4

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Complications, Such as Infections, Hospital Readmissions, Manipulations Under Anesthesia, Etc.

(NCT00492973)
Timeframe: any point during the first postoperative year

InterventionNumber of participants with complication (Number)
Control Group0
Corticosteroid3

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Amount of Pain Medication Taken Per Day

(NCT00492973)
Timeframe: Average of 3 days after surgery

Interventionmg/day morphine equivalant (Mean)
Control Group47.8
Corticosteroid46.0

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"Number of Participants Who Achieved of BP, HbA1c and Total, HDL and LDL Cholesterol Goals at the End of Intervention Phase"

Achievement of targets at end of intervention was performed applying generalized estimating equation (GEE) models, further adjusting for baseline values as covariate. (NCT00535925)
Timeframe: 13 years

InterventionParticipants (Count of Participants)
Standard of Care (SoC) Therapy150
Multifactorial Intensified Therapy191

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"Number of Participants With Overall Fatal and Non-fatal, Major Adverse Cardiovascular Events (MACEs)"

number of MACEs in the two groups are reported. In addition, The primary endpoint was analyzed with event curves for the time-to-first event based on Kaplan-Meier analysis. Cox regression model was used to calculate hazard ratio (HR) and 95% Confidence Interval (CI). Due to the cluster randomized study design, a Cox shared-frailty model was fitted. multivariable model was adjusted for selected potential confounders: age, sex, systolic blood pressure (SBP), hemoglobin, estimated glomerular filtration rate (eGFR), albuminuria, HbA1c, total cholesterol and triglycerides (log-scaled) to reduce risk of bias. (NCT00535925)
Timeframe: 4 years (in the case the number of events needed by sample size is not reached at the expected 4-year time frame, primary end point will be assessed after the follow-up phase)

InterventionParticipants (Count of Participants)
Conventional Therapy146
Intensified Therapy116

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Anxiety Reduction

"The Fear Thermometer measures how much fear subject is currently having. (0=None, 1= A little bit, 2= Some, 3= A lot, 4= Very, very much). The average of daily Value for 10 days." (NCT00580151)
Timeframe: Average of the 10 days

Interventionunits on a scale (Mean)
Experimental Group.76

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Pain Reduction

"The scale name is FACES (Faces Pain Rating Scale). Subjects were asked rate your WORST PAIN today (0 = no pain at all, 1-4 = mild pain, 5-6 = moderate pain, 7-9 = severe pain, 10 = excruciating pain). The Faces Pain Rating Scale should be collected every day and then averaged." (NCT00580151)
Timeframe: Average of the 10 days

Interventionunits on a scale (Mean)
Experimental Group.73

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Pain Score at 4 Weeks as Measured by the Multidimensional Pain Inventory (MPI)

The MPI is a comprehensive instrument comprised of 12 scales divided into three parts for assessing a number of dimensions of the chronic pain experience including pain intensity, emotional distress, cognitive and functional adaptation, and social support. Reference: Kearns RO, Turk DC, Rudy TC. The West Haven-Yale Multidimensional Pain Inventory (WHYMPI). Pain 1985; 23:345-356. Subscales were not used; the DOS WHYMPI computer program version 2.1 was used to score the instrument. Scores range from 0 (no pain) to 100 (highest pain). A score of 50 is the mean for patients with chronic pain. (NCT00588354)
Timeframe: 4 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)56.7
2% Lidocaine and Triamcinolone (40 mg)56.9

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Pain Disability Score at 2 Weeks as Measured by Oswestry Low Back Pain Disability Questionnaire (ODI)

This questionnaire measures a patient's permanent functional disability. The questionnaire consists of 10 sections with 6 statements each of increasing point value (from 0 to 5). The score is a percentage of the total, with higher score showing greater disability. Minimum detectable change is 10%, with a 90% CI. Change of less than this may be attributable to error in measurement. (NCT00588354)
Timeframe: 2 weeks

InterventionUnits on a scale (Mean)
2% Lidocaine and Clonidine (200 or 400 ug)27.0
2% Lidocaine and Triamcinolone (40 mg)21.3

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Pain Score at 2 Weeks as Measured by the Multidimensional Pain Inventory (MPI)

The MPI is a comprehensive instrument comprised of 12 scales divided into three parts for assessing a number of dimensions of the chronic pain experience including pain intensity, emotional distress, cognitive and functional adaptation, and social support. Reference: Kearns RO, Turk DC, Rudy TC. The West Haven-Yale Multidimensional Pain Inventory (WHYMPI). Pain 1985; 23:345-356. Subscales were not used; the DOS WHYMPI computer program version 2.1 was used to score the instrument. Scores range from 0 (no pain) to 100 (highest pain). A score of 50 is the mean for patients with chronic pain. (NCT00588354)
Timeframe: 2 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)51.6
2% Lidocaine and Triamcinolone (40 mg)56.0

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Pain Intensity Score at 4 Weeks as Measured by Pain Intensity Numerical Rating Scale (PI-NRS)

11-point ordinal scale measuring patient pain, ranging from 0 (no pain) to 10 (most severe/disabling pain). (NCT00588354)
Timeframe: 4 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)4.1
2% Lidocaine and Triamcinolone (40 mg)2.7

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Pain Intensity Score at 2 Weeks as Measured by Pain Intensity Numerical Rating Scale (PI-NRS)

11-point ordinal scale measuring patient pain, ranging from 0 (no pain) to 10 (most severe/disabling pain). (NCT00588354)
Timeframe: 2 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)4.1
2% Lidocaine and Triamcinolone (40 mg)4.0

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Pain Disability Score at 4 Weeks as Measured by the Roland-Morris Disability Questionnaire

This scale measures functional disability due to back pain. The score of the scale is the total number of items checked, from a minimum of 0 (no disability) to a maximum of 24 (great disability). Roland MO, Morris RW. A study of the natural history of back Pain. Part 1: development of a reliable and sensitive measure of disability in low back pain. Spine 1983; 8:141-144. (NCT00588354)
Timeframe: 4 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)9.4
2% Lidocaine and Triamcinolone (40 mg)3.5

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Pain Disability Score at 4 Weeks as Measured by Oswestry Low Back Pain Disability Questionnaire

This questionnaire measures a patient's permanent functional disability. The questionnaire consists of 10 sections with 6 statements each of increasing point value (from 0 to 5). The score is a percentage of the total, with higher score showing greater disability. Minimum detectable change is 10%, with a 90% CI. Change of less than this may be attributable to error in measurement. (NCT00588354)
Timeframe: 4 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)23.9
2% Lidocaine and Triamcinolone (40 mg)17.0

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Pain Disability Score at 2 Weeks as Measured by the Roland-Morris Disability Questionnaire

This scale measures functional disability due to back pain. The score of the scale is the total number of items checked, from a minimum of 0 (no disability) to a maximum of 24 (great disability). Roland MO, Morris RW. A study of the natural history of back Pain. Part 1: development of a reliable and sensitive measure of disability in low back pain. Spine 1983; 8:141-144. (NCT00588354)
Timeframe: 2 weeks

InterventionUnits on a scale (Mean)
2% Lidociane and Clonidine (200 or 400 ug)9.6
2% Lidocaine and Triamcinolone (40 mg)5.7

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Percentage of Subjects Achieving Blood Pressure Goals

Percentage of subjects who achieved JNC-VII defined blood pressure goals. (NCT00661895)
Timeframe: 3 month intervals

Interventionpercentage of participants (Number)
Intervention81
Control57

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Total Number of Post-operative Doses of Analgesics.

The total number of intravenous fentanyl doses given PACU which will be compared between the three randomized groups (arms) (NCT00678379)
Timeframe: Post-operative thru day 7

Interventionnumber of doses (Median)
Normal Saline12
Lidocaine (1%) + Bupivacaine 0.5%12
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg14

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Total Time Until Discharge From Hospital.

(NCT00678379)
Timeframe: Day of Surgery

Interventionminutes (Median)
Normal Saline122
Lidocaine (1%) + Bupivacaine 0.5%111
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg120

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Number and Percent of Participants Able to Tolerate a Regular Diet

The number and percent of patients whose post-operative diet has to a regular diet on post-operative days 1, 3, 5 & 7 (NCT00678379)
Timeframe: post-operative days 1,3,5 & 7.

,,
InterventionParticipants (Count of Participants)
post-op day 1post-op day 3post op day 5post op day 7
Lidocaine (1%) + Bupivacaine 0.5%481826
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg1121422
Normal Saline7182124

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Number and Percent of Participants Able to Tolerate Only a Soft Diet

The number and percent of patients whose post-operative diet has only advanced to a soft diet on post-operative days 1, 3, 5 & 7 (NCT00678379)
Timeframe: post-operative days 1,3,5 & 7.

,,
InterventionParticipants (Count of Participants)
post-op day 1post-op day 3post op day 5post op day 7
Lidocaine (1%) + Bupivacaine 0.5%22261710
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg26181814
Normal Saline26181313

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Number and Percent of Participants Able to Tolerate Only Liquids

The number and percent of patients whose post-operative diet has advanced to liquids only on post-op days 1, 3, 5 & 7 (NCT00678379)
Timeframe: post-operative days 1,3,5 & 7.

,,
InterventionParticipants (Count of Participants)
post-op day 1post-op day 3post op day 5post op day 7
Lidocaine (1%) + Bupivacaine 0.5%33131011
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg30231910
Normal Saline168136

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Mean Visual Analog Scale Pain Number.

Visual analog pain scale range is 0-10 with 0=no pain and 10 = worst pain ever (NCT00678379)
Timeframe: in recovery room; post-operative days 1,3,5 & 7

,,
Interventionpain score (Mean)
In recovery roomday 1day 3day 5day 7
Lidocaine (1%) + Bupivacaine 0.5%342.522
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg35332
Normal Saline33332.5

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Median Number of Pain Medication Doses

The median number of intravenous fentanyl doses administered in the PACU due to pain (NCT00678379)
Timeframe: in recovery room

Interventionnumber of doses (Median)
Normal Saline3.0
Lidocaine (1%) + Bupivacaine 0.5%3
Lidocaine 1% + Bupivacaine o.5% + Clondine 25mcg3

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Change From Baseline to Week 12 in the McGill Pain Questionnaire (Short Form) Total Score

The McGill Pain Questionnaire asks subjects to rate 15 different kinds of pain, each on a scale of 0 to 3 (0=None, 1=Mild, 2=Moderate, 3=Severe). The total score is a sum of the individual ratings and has a range from 0 to 45, where higher numbers indicate more pain. The 15 types of pain assessed are throbbing, shooting, stabbing, sharp, cramping, gnawing, hot-burning, aching, heavy, tender, splitting, tiring-exhausting, sickening, fearful, and punishing-cruel. This scale was completed at the Baseline and Week 12 clinic visits. The change from Baseline is calculated as the Week 12 total score minus the Baseline total score, so greater negative numbers indicate more improvement (pain relief). (NCT00695565)
Timeframe: Baseline and Week 12

Interventionunits on a scale (Mean)
Placebo Gel-7.3
Clonidine Topical Gel (ARC-4558)-8.7

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Change From Baseline in the Brief Pain Inventory Functional Interference Scale at Week 12; mLOCF Imputation

"The Brief Pain Inventory was completed by the subject at clinic visits. The Functional Interference Scale (of 0 to 70) is a composite score that measures the degree to which pain interferes with mood, walking, work, relationships, sleep, general activity, and enjoyment of life. The composite score is a sum of the seven individual question scores. Each individual question is rated in reference to pain over the past 24 hours on a scale of 0 to 10, where 0 indicates that pain does not interfere and 10 indicates that pain completely interferes with that function, so lower scores represent better outcomes on this scale.~The change in functional interference is represented as Week 12 minus Baseline, so greater negative numbers represent more improvement." (NCT00695565)
Timeframe: Baseline and Week 12

Interventionunits on a scale (Mean)
Placebo Gel-15.1
Clonidine Topical Gel (ARC-4558)-17.3

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Change From Baseline to Week 12 in Overall Quality of Sleep (Chronic Pain Sleep Inventory)

Subjects rated overall quality of sleep over the past week using a 100 mm Visual Analog Scale (VAS) where 100=Excellent and 0=Very Poor. This scale was completed during clinic visits. Change from Baseline is a positive value where quality of sleep improved. (NCT00695565)
Timeframe: Baseline and Week 12

Interventionunits on a scale (Mean)
Placebo Gel17.7
Clonidine Topical Gel (ARC-4558)19.2

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Change From Baseline to Week 12 in the Anxiety Score of the Hospital Anxiety and Depression Scale (HADS)

The HADS was completed at the Baseline and Week 12 clinic visits. The Anxiety Score component of the HADS includes 7 questions, each with 4 possible answer choices (rated 0 to 3). The composite score is created by adding the scores of the 7 individual questions. A score of 0 to 7 is Normal, 8-10 indicates Mild Anxiety, 11-14 indicates Moderate Anxiety, and 15-21 indicates Severe Anxiety. The change from Baseline is calculated as the Week 12 composite score minus the Baseline composite score. (NCT00695565)
Timeframe: Baseline and Week 12

Interventionunits on a scale (Mean)
Placebo Gel-0.6
Clonidine Topical Gel (ARC-4558)-1.1

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Clinician Global Impression of Change (CGIC) at Week 12

At Week 12, the Investigator was asked to independently rate the subject's total improvement relative to Baseline, whether or not, in their judgement, it was due entirely to study drug treatment or not. Answer choices were: (+3) very much improved, (+2) much improved, (+1) minimally improved, (0) no change, (-1) minimally worse, (-2) much worse, (-3) very much worse. (NCT00695565)
Timeframe: Week 12

,
Interventionpercentage of subjects (Number)
Very Much ImprovedMuch ImprovedMinimally ImprovedNo ChangeMinimally WorseVery Much Worse
Clonidine Topical Gel (ARC-4558)16.530.624.727.11.20
Placebo Gel5.838.427.925.62.30

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Change From Baseline to Week 12 in the Average Daily Pain NPRS (Numeric Pain Rating Scale) Score; mLOCF Imputation

"Pain in the feet was scored daily at bedtime by the subject on a 0-10 numeric pain rating scale (NPRS) through Day 84. Subjects were asked to record average pain in the feet over the past 24 hours. A score of 0 indicated no pain and a score of 10 was worst possible pain.~The change in pain is represented as Week 12 minus Baseline, so greater negative numbers represent more improvement (more pain relief)." (NCT00695565)
Timeframe: Baseline (average of Days -7 to -1) and Week 12 (Average of Days 78 to 84)

,
Interventionunits on a scale (Mean)
All subjectsCapsaicin response ≥ 2
Clonidine Topical Gel (ARC-4558)-2.4-2.7
Placebo Gel-1.9-1.5

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Change From Baseline in Average Daily Pain NPRS Score for Each Week of Treatment; mLOCF Imputation

"Pain in the feet was scored daily at bedtime by the subject on a 0-10 numeric pain rating scale (NPRS). Subjects were asked to record average pain in the feet over the past 24 hours. A score of 0 indicated no pain and a score of 10 was worst possible pain. A weekly average was calculated from the daily scores for each week. The change in pain is represented as the average weekly score minus Baseline, so greater negative numbers represent more improvement (more pain relief)." (NCT00695565)
Timeframe: Baseline (average of Days -7 to -1) and Weeks 1 through 12 (weekly averages)

,
Interventionunits on a scale (Mean)
Week 1Week 2Week 3Week 4Week 5Week 6Week 7Week 8Week 9Week 10Week 11Week 12
Clonidine Topical Gel (ARC-4558)-0.7-1.0-1.5-1.6-1.7-1.8-2.1-2.2-2.3-2.4-2.3-2.4
Placebo Gel-0.6-1.0-1.2-1.5-1.7-1.8-1.8-1.9-1.9-1.9-1.9-1.9

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Percentage of Subjects Who Experience at Least 50% Reduction in Average Daily Pain From Baseline; mLOCF Imputation

"Pain in the feet was scored daily at bedtime by the subject on a 0-10 numeric pain rating scale (NPRS). Subjects were asked to record average pain in the feet over the past 24 hours. A score of 0 indicated no pain and a score of 10 was worst possible pain." (NCT00695565)
Timeframe: Baseline (average of Days -7 to -1) and Week 12 (average of Days 78 to 84)

Interventionpercentage of subjects (Number)
Placebo Gel32
Clonidine Topical Gel (ARC-4558)37

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Percentage of Subjects Who Experience at Least 30% Reduction in Average Daily Pain From Baseline; mLOCF Imputation

"Pain in the feet was scored daily at bedtime by the subject on a 0-10 numeric pain rating scale (NPRS). Subjects were asked to record average pain in the feet over the past 24 hours. A score of 0 indicated no pain and a score of 10 was worst possible pain." (NCT00695565)
Timeframe: Baseline (average of Days -7 to -1) and Week 12 (average of Days 78 to 84)

Interventionpercentage of subjects (Number)
Placebo Gel47
Clonidine Topical Gel (ARC-4558)52

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Change in Blood Pressure From Baseline to Week 12

Systolic and Diastolic Blood Pressure were measured at clinic visits. This outcome assesses the change in blood pressure from Baseline to Week 12 of treatment. (NCT00695565)
Timeframe: Baseline and Week 12

,
InterventionmmHg (Mean)
Change in Systolic BPChange in Diastolic BP
Clonidine Topical Gel (ARC-4558)1.01.0
Placebo Gel-0.4-0.2

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Patient Global Impression of Change (PGIC) at Week 12

At Week 12 the subject was asked to rate their total improvement relative to Baseline, whether or not, in their judgement, it was due entirely to study drug treatment or not. Answer choices were: (+3) very much improved, (+2) much improved, (+1) minimally improved, (0) no change, (-1) minimally worse, (-2) much worse, (-3) very much worse. (NCT00695565)
Timeframe: Week 12

,
Interventionpercentage of subjects (Number)
Very Much ImprovedMuch ImprovedMinimally ImprovedNo ChangeMinimally WorseVery Much Worse
Clonidine Topical Gel (ARC-4558)21.227.128.222.41.20
Placebo Gel11.832.931.821.21.21.2

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Change From Baseline to Week 12 in the Depression Score of the Hospital Anxiety and Depression Scale (HADS)

The HADS was completed at the Baseline and Week 12 clinic visits. The Depression Score component of the HADS includes 7 questions, each with 4 possible answer choices (rated 0 to 3). The composite score is created by adding the scores of the 7 individual questions. A score of 0 to 7 is Normal, 8-10 indicates Mild Depression, 11-14 indicates Moderate Depression, and 15-21 indicates Severe Depression. The change from Baseline is calculated as the Week 12 composite score minus the Baseline composite score. (NCT00695565)
Timeframe: Baseline and Week 12

Interventionunits on a scale (Mean)
Placebo Gel-0.4
Clonidine Topical Gel (ARC-4558)-0.9

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Change From Baseline in the Brief Pain Inventory (BPI) Severity Scale at Week 12; mLOCF Imputation

"The Brief Pain Inventory was completed by the subject at clinic visits. The Severity Scale (of 0 to 40) is a composite score, which is the sum of the individual ratings for worst pain, least pain, average pain, and current pain. Each individual question is rated on a scale of 0 to 10, where 0 indicates No Pain and 10 indicates Pain as bad as you can imagine. The change in pain severity is represented as Week 12 minus Baseline, so greater negative numbers represent greater improvement (pain relief)." (NCT00695565)
Timeframe: Baseline and Week 12

Interventionunits on a scale (Mean)
Placebo Gel-7.9
Clonidine Topical Gel (ARC-4558)-9.6

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Change From Baseline to Week 12 in the Worst Daily Pain NPRS Score; mLOCF Imputation

"Pain in the feet was scored daily at bedtime by the subject on a 0-10 numeric pain rating scale. Subjects were asked to record the worst pain in their feet over the past 24 hours. A score of 0 indicated no pain and a score of 10 was worst possible pain. The change in pain is represented as Week 12 minus Baseline, so greater negative numbers represent greater improvement (greater pain relief)." (NCT00695565)
Timeframe: Baseline (average of Days -7 to -1) and Week 12 (average of Days 78 to 84)

Interventionunits on a scale (Mean)
Placebo Gel-2.1
Clonidine Topical Gel (ARC-4558)-2.5

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A Composite of Death or Dependency, With Dependency Being Defined by a Score of 3 to 5 on the Modified Rankin Scale (mRS)

(NCT00716079)
Timeframe: 90 days

Interventionparticipants (Number)
Intensive Blood-Pressure Lowering719
Guideline-Recommended Blood-Pressure Lowering785

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Death at 90 Days

(NCT00716079)
Timeframe: 90 days

Interventionparticipants (Number)
Intensive Blood-Pressure Lowering166
Guideline-Recommended Blood-Pressure Lowering170

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Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale-fourth Edition (ADHDRS-IV Scale) (18 Items Scored, 0 [Never/Rarely] to 3 [Very Often]; Total Possible Score Range, 0-54) at Months 1, 2, 3, 4, 6, 9, and 12

The ADHDRS-IV consists of 18 items designed to reflect symptoms of ADHD. Each item is scored on a scale of 0 (Never or rarely) to 3 (Very Often). The subscales of the ADHDRS-IV included the Inattention and the hyperactivity/Impulsivity subscales (total possible score range, 0-54). The Inattention subscale consists of the sum of 9 items: 1, 3, 5, 7, 9, 11, 13, 15, and 17. The Hyperactivity/Impulsivity subscale consists of the sum of 9 items: 2, 4, 6, 8, 10, 12, 14, 16, and 18 (NCT00723190)
Timeframe: At baseline, months 1, 2, 3, 4, 6, 9, and 12

InterventionUnits on a scale (Mean)
1-month (n = 229)2-month (n = 221)3-month (n = 203)4-month (n = 142)6-month (n = 184)9-month (n = 119)12-month (n = 98)
KAPVAY (CLONICEL)-13.7-14.4-14.8-16.3-14.6-18.1-14.6

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Change From Baseline in Clinical Global Impressions-Improvement (CGI-I) at Months 1, 2, 3, 4, 6, 9, and 12

"CGI-I scale:~1 = Very much improved; 2 = Much improved; 3 = Minimally improved; 4 = No change; 5 = Minimally worse; 6 = Much worse; 7 = Very much worse" (NCT00723190)
Timeframe: At baseline, months 1, 2, 3, 4, 6, 9, and 12

InterventionUnits on a scale (Mean)
1-month (n = 229)2-month (n = 220)3-month (n = 202)4-month (n = 143)6-month (n = 185)9-month (n = 119)12-month (n = 97)
KAPVAY (CLONICEL)2.52.52.52.32.42.12.4

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Change From Baseline in Clinical Global Impressions-Severity (CGI-S) at Months 1, 2, 3, 4, 6, 9, and 12

"CGI-S scale:~1 = Normal, not ill at all; 2 = Borderline ill; 3 = Mildly ill; 4 = Moderately ill; 5 = Markedly ill; 6 = Severely ill; 7 = Among the most extremely ill patients" (NCT00723190)
Timeframe: At baseline, months 1, 2, 3, 4, 6, 9, and 12

InterventionUnits on a scale (Mean)
1-month (n = 229)2-month (n = 220)3-month (n = 202)4-month (n = 143)6-month (n = 185)9-month (n = 119)12-month (n = 97)
KAPVAY (CLONICEL)-1.2-1.3-1.3-1.5-1.4-1.7-1.4

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Safety Assessment in Terms of Adverse Events (Treatment-emergent [TEAEs] and Serious [SAEs])

Safety assessments were performed at each study visit according to the time and events schedule. All safety analyses were based on safety population (NCT00723190)
Timeframe: 1 year

InterventionParticipants (Number)
Total Safety PopulationSubjects with ≥1 TEAEsSubjects with ≥1 related TEAEsSubjects with ≥1 SAEsSubjects with ≥1 TEAEs leading to discontinuation
KAPVAY (CLONICEL)301246178217

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Safety Assessment in Terms of Adverse Events (Treatment-emergent [TEAEs] and Serious [SAEs])

Safety assessments were performed at each study visit according to the time and events schedule. All safety analysis were based on safety population (NCT00723190)
Timeframe: 1 year

InterventionEvents (Number)
Total number of TEAEsTotal number of related TEAEsTotal number of SAEs
KAPVAY (CLONICEL)9544382

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Change From Baseline in 12-lead Electrocardiogram in Terms of Heart Rate at Week 4

(NCT00723190)
Timeframe: At baseline and at Week 4

Interventionbeats per minute (Mean)
KAPVAY (CLONICEL)-10.6

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Change From Baseline in Body Temperature at Week 4

Temperature was measured with the subject in a sitting position and resting for at least 2 minutes prior to taking the measurement (NCT00723190)
Timeframe: At baseline and at Week 4

InterventionFahrenheit (Mean)
KAPVAY (CLONICEL)-0.08

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Change From Baseline in Diastolic Blood Pressure at Week 4

Blood pressure was measured with the subject in a sitting position and resting for at least 2 minutes prior to taking the measurement. The dominant arm was used for the measurement (NCT00723190)
Timeframe: At baseline and at Week 4

InterventionmmHg (Mean)
KAPVAY (CLONICEL)-4.2

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Change From Baseline in Heart Rate at Week 4

Heart rate was measured with the subject in a sitting position and resting for at least 2 minutes prior to taking the measurement (NCT00723190)
Timeframe: At baseline and at Week 4

Interventionbeats per minute (Mean)
KAPVAY (CLONICEL)-7.0

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Change From Baseline in Systolic Blood Pressure at Week 4

Blood pressure was measured with the subject in a sitting position and resting for at least 2 minutes prior to taking the measurement. The dominant arm was used for the measurement (NCT00723190)
Timeframe: At baseline and at Week 4

InterventionmmHg (Mean)
KAPVAY (CLONICEL)-5.0

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Change From Baseline in 12-lead Electrocardiogram in Terms of QT, QTc Fridericia (QTcF), and QTc Bazett's (QTcB) at Week 4

(NCT00723190)
Timeframe: At baseline and at Week 4

Interventionmilliseconds (Mean)
QTQTcFQTcB
KAPVAY (CLONICEL)17.91.4-8.0

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Change From Baseline in Body Weight at Weeks 1, 2, 3, 4, and Months 2, 3, 4, 5, 6, 9, and 12

(NCT00723190)
Timeframe: At baseline and at weeks 1, 2, 3, 4, and months 2, 3, 4, 5, 6, 9, and 12

InterventionKilograms (Mean)
week 1 (n = 283)week 2 (n = 283)week 3 (n = 278)week 4 (n = 269)month 2 (n = 246)month 3 (n = 232)month 4 (n = 212)month 5 (n = 47)month 6 (n = 204)month 9 (n = 123)month 12 (n = 123)
KAPVAY (CLONICEL)0.30.40.60.70.91.21.41.72.13.64.5

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Change in Muscle Sympathetic Nerve Activity

Muscle sympathetic nerve activity was measured as bursts sympathetic nerve activity per minute. (NCT00858845)
Timeframe: Baseline, 3 months

Interventionbursts/min (Mean)
Clonidine Patch-4.3
Placebo4.4

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Change in Proportion of Type 1 Fibers

Fibers were typed as I or II according to presence of myosin heavy chain. (NCT00858845)
Timeframe: Baseline, 3 months

Interventionpercentage of fibers (Mean)
Clonidine Patch-4.6
Placebo-5.6

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Change in Citrate Synthase Activity as an Estimate of Mitochondrial Activity

(NCT00858845)
Timeframe: Baseline, 3 months

Interventionmicromole/min/wet weight (Mean)
Clonidine Patch-0.3
Placebo0.07

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Percentage of Bowel Movements With Semi-formed and Loose Stools Post-treatment Adjusted for Baseline

"The percentage of bowel movements with semi-formed and loose stools was defined as those with a score of 5-7 on the Bristol stool form scale. The adjustment for baseline was an analysis of covariance (ANCOVA) where the covariate was the baseline version of the endpoint." (NCT00884832)
Timeframe: 4 weeks treatment

,
Interventionpercentage of bowel movements (Mean)
Subjects with diarrheaSubjects without diarrhea
Oral Clonidine23.625.4
Oral Placebo38.722.8

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Percentage of Days With Fecal Incontinence (FI)

(NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionpercentage of days (Mean)
4 weeks baseline, subjects without diarrhea4 weeks baseline, subjects with diarrhea4 weeks treatment, subjects without diarrhea4 weeks treatment, subjects with diarrhea
Oral Clonidine28.735.423.224.3
Oral Placebo37.842.118.733.3

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Percentage of Days With FI Post-treatment Adjusted for Baseline

"The adjustment for baseline was an analysis of covariance (ANCOVA) where the covariate was the baseline version of the endpoint." (NCT00884832)
Timeframe: 4 weeks treatment

,
Interventionpercentage of days (Mean)
Subjects without diarrheaSubjects with diarrhea
Oral Clonidine42.5427.79
Oral Placebo31.4239.51

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Satisfaction With Treatment

"This parameter was determined by a 100 mm visual analog scale, with possible scores ranging from 0 = Not satisfied at all (no relief of symptoms) to 100 = Completely satisfied (symptoms resolved). The parameter was computed from weekly diaries. Scores were averaged over the 4 week baseline period and the 4 week treatment periods." (NCT00884832)
Timeframe: 4 weeks baseline, 4 week treatment

,
Interventionunits on a scale (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine2247
Oral Placebo1838

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Mean Percentage of Bowel Movements Which Were Incontinent

Values were averaged over 4 week baseline and 4 week treatment periods. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionpercentage of bowel movements (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine3124
Oral Placebo4027

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Impact of Fecal Incontinence on Baseline Quality of Life

"Scores were computed from a pre-treatment questionnaire, the Fecal Incontinence Quality of Life Scale. This scale is composed of a total of 29 items; these items form four scales: Lifestyle (10 items) Coping/Behavior (9 items), Depression/Self Perception (7 items), and Embarrassment (3 items).~Scales range from 1 to 4; with a 1 indicating a lower functional status of quality of life. Scales scores are the average (mean) response to all items in the scale (that is, add the responses to all questions in a scale together and then divide by the number of items in the scale, adjusting for missing values)." (NCT00884832)
Timeframe: 4 weeks baseline

,
Interventionunits on a scale (Mean)
Lifestyle scoreCoping scoreDepression scoreEmbarrassment score
Oral Clonidine2.81.83.22.2
Oral Placebo2.31.62.92.3

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Impact of Fecal Incontinence on Post-Treatment Quality of Life

"Scores were computed from a post-treatment questionnaire, the Fecal Incontinence Quality of Life Scale. This scale is composed of a total of 29 items; these items form four scales: Lifestyle (10 items) Coping/Behavior (9 items), Depression/Self Perception (7 items), and Embarrassment (3 items).~Scales range from 1 to 4; with a 1 indicating a lower functional status of quality of life. Scales scores are the average (mean) response to all items in the scale (that is, add the responses to all questions in a scale together and then divide by the number of items in the scale, adjusting for missing values)." (NCT00884832)
Timeframe: after 4 weeks treatment

,
Interventionunits on a scale (Mean)
Lifestyle scoreCoping scoreDepression scoreEmbarrassment score
Oral Clonidine3.12.33.52.8
Oral Placebo2.72.13.22.5

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Mean Fecal Incontinence and Constipation Assessment (FICA) Score

The FICA severity scale has 4 items (frequency, type, amount of leakage, and presence of urgency) and is used to rate the severity of fecal incontinence. The parameter was computed from values in the weekly diaries. The FICA score can range from 1 to 13. Symptom severity scores of 1-6, 7-10, and 11-13 are categorized as mild, moderate, and severe, respectively. Scores were averaged over the 4 week baseline period and the 4 week treatment periods. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionunits on a scale (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine8.16.5
Oral Placebo9.17.6

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Mean Number of Days With Fecal Incontinence

Values were averaged over 4 week baseline and 4 week treatment periods. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventiondays (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine138
Oral Placebo1611

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Mean Number of Fecal Incontinence Episodes

Values were averaged over 4 week baseline and 4 week treatment periods. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionnumber of episodes (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine2012
Oral Placebo3119

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Mean Severity of Fecal Incontinence

The Fecal Incontinence Severity Index was used to compute the severity of fecal incontinence (FI). It is a validated 4-item scale used to assess the frequency of 4 different types of FI (gas, mucus, liquid stool, solid stool). The subject responses are weighted and summed for the 4 types of FI. Scores could range from 0 (no symptoms) to 61 (very frequent FI). Values were computed from pre- and post- treatment questionnaires. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionunits on a scale (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine36.229.3
Oral Placebo37.331.2

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Percentage of Bowel Movements Preceded by Rectal Urgency

Rectal urgency is defined as a sudden, irresistible need to have a bowel movement. Scores were averaged over the 4 week baseline period and the 4 week treatment periods. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionpercentage of bowel movements (Mean)
4 weeks baseline4 weeks treatment
Oral Clonidine5546
Oral Placebo5946

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Percentage of Bowel Movements With Semi-formed and Loose Stools in Subjects With and Without Diarrhea

The percentage of bowel movements with semi-formed and loose stools was defined as those with a score of 5-7 on the Bristol stool form scale. (NCT00884832)
Timeframe: 4 weeks baseline, 4 weeks treatment

,
Interventionpercentage of bowel movements (Mean)
4 weeks baseline, subjects without diarrhea4 weeks baseline, subjects with diarrhea4 weeks treatment, subjects without diarrhea4 weeks treatment, subjects with diarrhea
Oral Clonidine19.447.51431.2
Oral Placebo25.551.61649

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Wound Hyperalgesia Index (WHA) Assessed 48 Hrs After Block Placement in the Different Groups

Determine which of three different TAP formulations (Placebo, TAP, Clo-TAP) has the most beneficial effect on the postoperative area of hyperalgesia 48hrs after the start of the cesarean section. The smaller the area of WHA, assessed in cm2, the better the outcome. Area sizes may range from 0 to any size. (NCT01015807)
Timeframe: 48hrs after CS

Interventioncm^2 (Mean)
Placebo1.07
TAP (Bupi)1.27
Clo-TAP (Bupi + Clon)0.74

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Numerical Rating Scale (NRS) Pain Scores During Hospitalization.

Patient pain was assessed during hospitalization using the VAS Pain Scale, a numerical rating scale ranging from 0 (no pain) to 10 (severe pain). A lower score represents a better outcome. Pain was assessed preoperatively, 1 hour postoperatively in the post anesthesia unit, and then every 8 hours on the Orthopedic inpatient unit, for a duration of 2 days. (NCT01042093)
Timeframe: 2 days after surgery

,,,
Interventionscores on a scale 0-10 (Mean)
Vas Pain Scale - 1 Hour Post OpVas Pain Scale - 8 Hour Post OpVas Pain Scale - 16 Hour Post OpVas Pain Scale - 24 Hour Post OpVas Pain Scale - 32 Hour Post OpVas Pain Scale - 40 Hour Post OpVas Pain Scale - 48 Hour Post OpVas Pain Scale Preoperatively
ROP/EPI1.602.822.412.963.132.802.112.13
ROP/EPI/CLO2.673.932.753.633.623.282.562.43
ROP/EPI/TOR1.901.522.222.562.662.351.972.47
ROP/EPI/TOR/CLO1.061.521.852.332.182.542.411.93

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Narcotic Consumption During Hospitalization

A variety of pain medications were used after surgery to keep patients comfortable. Narcotic use was recorded as morphine equivalents. We report the mean narcotic consumption for each group for the day of surgery as well as post operative day 1,2, and 3. (NCT01042093)
Timeframe: 4 days

,,,
Interventionmg (Mean)
Morphine Equivalent Day of SurgeryMorphine Equivalent Post Operative Day 1Morphine Equivalent Post Operative Day 2Morphine Equivalent Post Operative Day 3
ROP/EPI52.5051.0836.7615.54
ROP/EPI/CLO55.2064.6150.0721.97
ROP/EPI/TOR43.0947.9542.6918.72
ROP/EPI/TOR/CLO46.9246.5440.7120.45

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Knee Society Pain Scores at 6 Week Follow-up Appointment

Patients were assessed for pain at their 6 week follow-up appointment using the Knee Society Rating Scale. Using this scale patients are given a pain score ranging from 0 (severe pain) to 50 (No Pain). This is determined as follows: No pain/50 points, Mild or occasional pain/45 points, pain with stairs only/40 points, pain with walking and stairs/30 points, Moderate/occasional pain/ 20 points,continual pain/10 points, severe pain/0 points. We report the mean score for each group. A higher score represents a better outcome. (NCT01042093)
Timeframe: 6 weeks after surgery

InterventionScores on a scale 0-50 (Mean)
ROP/EPI/TOR/CLO45
REP/EPI/TOR43
REP/EPI/CLO45
REP/EPI45

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Composite of All-cause Mortality and Nonfatal MI

(NCT01082874)
Timeframe: 30 days

Interventionparticipants (Number)
Active Clonidine and Active ASA173
Active Clonidine and Placebo ASA194
Placebo Clonidine and Active ASA178
Placebo Clonidine and Placebo ASA161

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Length of Treatment With Neonatal Morphine Sulfate

(NCT01175668)
Timeframe: subjects were followed for the duration of treatment, up to 3 months

Interventiondays (Mean)
NMS/Clonidine18.2
NMS/Phenobarbital13.6

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Total Dose of NMS Used

(NCT01175668)
Timeframe: For the duration of treatment, upto 3 months

Interventionmg/kg (Mean)
NMS/Clonidine5.7
NMS/Phenobarbital4.6

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Montgomery-Asberg Depression Rating Scale (MADRS) Total Score

The Montgomery-Asberg Depression Rating Scale (MADRS) is a 10-item scale that measures the severity of depression, with a higher score indicating a higher level of depression. The range of scores is 0 to 60. (NCT01179009)
Timeframe: 8 weeks

InterventionScores on a scale (Mean)
Ketamine 100-hour Infusion-9.0
Ketamine 40-minute Infusion-6.4

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Mean Ratings on Clinical Opiate Withdrawal Scale (COWS) Measure of Withdrawal During Double-blind Taper (7-days) and Post-taper (7-days) Period.

Outcomes represent mean peak withdrawal as rated on the Clinical Opiate Withdrawal Scale (COWS) total score. Withdrawal was collected 7 times daily and daily peak values were identified for each participant and averaged together as a function of group. Primary outcomes were mean peak results from the 7-day taper period and first 7 days post-taper. The COWS is an 11-item observer-rated measure of opioid withdrawal severity. Items are rated on individual Likert scales and the total score range is 0-47. Higher values indicate more severe withdrawal. (NCT01188421)
Timeframe: 14 days total

,,
Interventionunits on a scale (Mean)
Taper Day 1Taper Day 2Taper Day 3Taper Day 4Taper Day 5Taper Day 6Taper Day 7Post Taper Day 1Post Taper Day 2Post Taper Day 3Post Taper Day 4Post Taper Day 5Post Taper Day 6Post Taper Day 7
Buprenorphine7.796.164.764.214.314.063.514.825.626.235.495.874.914.91
Clonidine8.288.005.854.703.323.573.863.274.093.683.823.272.912.41
Tramadol ER8.416.103.774.253.253.393.693.364.483.283.132.752.572.30

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Change in Blood Pressure After Intrathecal Injection of Clonidine.

"Subjects baseline blood pressure (systolic blood pressure (SBP), and diastolic blood pressure (DBP)), and blood pressures after clonidine injection was compared against baseline to assess efficacy of clonidine in refractory hypertensive subjects. Subject's blood pressure was monitored continuously after intrathecal injection of clonidine until subjects blood pressure nadir and return to pre clonidine injection level. The mean value reported below are the average changes in blood pressure from baseline (pre clonidine injection) in both SBP and DBP during post clonidine injection blood pressure monitoring for 4 hours.~Blood pressure measurements were collected every 10 minutes for first hour after injection, and every 15 minutes after the first hour, up to 4 hours were averaged to report the change from baseline." (NCT01297335)
Timeframe: Baseline, Every 10 Minutes for first hour after clonidine injection, and every 15 minutes after first hour, until 4 hours after clonidine injection

Interventionmm Hg (Mean)
Change in mean SBP after clonidine injectionChange in DBP after clonidine injection
Intrathecal Clonidine7937

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Likert Scale Pain Rating

Likert scale is 11 point digital pain rating system that asks subjects to rate their pain from 0 to 10. Rating of 0 means no pain at all, and in increasing order, 10 would mean worst pain imaginable/ unbearable pain. (NCT01297335)
Timeframe: Pre-dose and 1 hour post injection.

Interventionunits on a scale (Mean)
Pre-injection average Likert scorePost-injection average Likert score
Intrathecal Clonidine6.53.6

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Changes in Visual Analogue Scale (VAS) Ratings of Sedation and Sensation of Dry Mouth Reported by the Subjects, Pre and 1 Hour Post Injection

Subjects were asked to rate severity of two of the most common side effects of clonidine, sedation and sensation of dry mouth, at pre and post (1 hour after) intrathecal administration of clonidine. The mean changes between pre and post injection VAS ratings of sedation and sensation of dry mouth are reported below. The VAS scale ranges from 1 to 10 cm, with higher values indicating higher level of sedation and higher level of dry mouth. (NCT01297335)
Timeframe: Before clonidine injection (Baseline), and at 1 hour after clonidine injection.

Interventioncm (Mean)
Change in level of sedationChange in sensation of dry mouth
Intrathecal Clonidine3.363.47

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Ventilator-free Days

(NCT01322048)
Timeframe: Baseline to day 28

Interventiondays (Median)
Adrenergic Blockade16.2
Placebo18.05

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Plasma Norepinephrine Levels

(NCT01322048)
Timeframe: Post-treatment (t=Day 8)

Interventionpg/mL (Median)
Adrenergic Blockade962
Placebo714

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Time to Complete Detoxification

Time to complete detoxification is defined as 48 hrs off all opioids/benzodiazepines and study drug with acceptable withdrawal scores of <9 (on average we expect the infant to be enrolled in the study for 2-4 weeks). The scale used to assess withdrawal was the Modified Finnegan Neonatal Withdrawal Scale, which ranges from 0-41, 0 represents no withdrawal and 41 represent maximum withdrawal. (NCT01360450)
Timeframe: up to 4 weeks

,
Interventiondays (Mean)
total days on narcoticsduration on study drug in days
Control37.214.2
Treatment89.521

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Saliva Secreted Rate

Change from baseline, negative mean reduce secret rate from baseline, positive mean not reduce secretion. (NCT01370811)
Timeframe: 8 hours post-dose

Interventionpercentage of change from baseline (Mean)
OC Oral Solution Treatment B-6.508
OC Oral Solution Treatment C-34.512
OC Oral Solution Treatment D83.695
OC Oral Solution Treatment A7.414

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Numeric Rating Scale (NRS) Measurements of Subjective Judgment of Excessive Saliva Production

"Evaluation of change from baseline the subjective assessment of saliva production after administration of a single dose of different combinations of oxybutynin and clonidine (OC Oral solution) in patients suffering from Parkinson's disease with excessive salivation. Compare with baseline the number of rate scale was more production with baseline or reduce from baseline.~The min and max of the score is 0 and 10, the total range is 0~10, and higher value is represented more worse outcome." (NCT01370811)
Timeframe: 8 hours post-dose

Interventionscore on a scale (Mean)
OC Oral Solution Treatment A-0.8
OC Oral Solution Treatment B-1.2
OC Oral Solution Treatment C-1.6
OC Oral Solution Treatment D-1.1

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Evaluation of the Safety and Tolerability of Different Combinations of Oxybutynin and Clonidine (OC Oral Solution) in Patients Suffering From Parkinson's Disease With Excessive Salivation

Evaluation of the safety and tolerability of different combinations of oxybutynin and clonidine (OC Oral solution) in patients suffering from Parkinson's disease with excessive salivation. Calculate the treatment Emergent Adverse Events number during the study treatment period and follow up period up to at least 23 days excluding the screening period. (NCT01370811)
Timeframe: during the study treatment period and follow up period at least 23 days excluding the screening period.

InterventionTreatment Emergent Adverse Events (Number)
OC Oral Solution Treatment A6
OC Oral Solution Treatment B6
OC Oral Solution Treatment C5
OC Oral Solution Treatment D4

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At Least One Opioid Use (Class 3 Analgesic)

Opioid use was recorded twice weekly during the active phase (radiotherapy) (NCT01385748)
Timeframe: 8 weeks

,,
Interventionparticipants (Number)
MissingYesNo
Clonidine Lauriad® 100 µg13034
Clonidine Lauriad® 50 µg22331
Placebo Lauriad®03032

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Time to Onset of Severe Oral Mucositis

Time to onset is the duration until first Severe Oral Mucositis. Severe Oral Mucositis was defined as a Grade 3 or Grade 4 score on the World Health Organization (WHO) oral mucositis severity scale. Participants were assessed twice weekly during the active phase (radiotherapy) by a trained radiation oncologist or an ear nose and throat specialist who took into account the field of radiation treatment. WHO score 3 = ulcers, extensive erythema, and the inability of the participant to swallow a solid diet; WHO score 4 = mucositis to the extent that alimentation was not possible. (NCT01385748)
Timeframe: 8 weeks

Interventionweeks (Median)
Clonidine Lauriad® 50 µg6.4
Clonidine Lauriad® 100 µg6
Placebo Lauriad®5.1
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled6.4

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Salivary Flow Assessment Using the National Cancer Institute-Common Terminology Criteria (NCI-CTC) for Xerostomia: Time to First Grade 2 or Higher

Salivary flow was assessed and scored by the investigator weekly using the NCI-CTC scale for xerostomia for up to 8 weeks during the active phase (radiotherapy). Time to appearance of Grade 2 or higher on the following 4-point scoring scale is reported: 0 = normal; 1 = symptomatic (dry or thick saliva) without significant dietary alteration (unstimulated saliva flow greater than 0.2 mL/minute); 2 = symptomatic and significant oral intake alterations (e.g. copious water, other lubricants, diet limited to purees and/or soft, moist foods) (unstimulated saliva 0.1 to 0.2 mL/minute); and 3 = symptoms leading to inability to adequately aliment orally, intravenous fluids, tube feedings, or total parenteral nutrition indicated (unstimulated saliva < 0.1 mL/minute). (NCT01385748)
Timeframe: 8 weeks

Interventionweeks (Median)
Clonidine Lauriad® 50 µg6
Clonidine Lauriad® 100µg7.4
Placebo Lauriad®5.1
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled7.1

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Overall Survival

After the end-of study visit, the investigator center collects OS follow-up data for each patient who has consented to participate in the follow-up data collection. the OS follow-up period was still ongoing at time of the primary analysis and ended in Nov 2016. The analysis was condicted on the ITT population. The overall survival was evaluate every 6 months after last subject completed in patients who has consented to participate . (NCT01385748)
Timeframe: 2 years

Interventionmonths (Median)
Clonidine Lauriad® 50 µg47
Clonidine Lauriad® 100 µg58.8
Placebo Lauriad®41.8
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled58.8

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Opioid Use: Minimal Total Cumulative Dose Administered (Median, Range)

Opioid use was recorded twice weekly for up to 8 weeks during the active phase (radiotherapy). The sum of non-missing total cumulative doses across all class 3 analgesics recorded for the considered participant is reported. (NCT01385748)
Timeframe: 8 weeks

Interventionmorphine dose equivalent (Median)
Clonidine Lauriad® 50 µg183.6
Clonidine Lauriad® 100 µg174
Placebo Lauriad®215
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled178.65

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Opioid Use: Minimal Total Cumulative Dose Administered (Mean, Standard Deviation)

Opioid use was recorded twice weekly for up to 8 weeks during the active phase (radiotherapy). The sum of non-missing total cumulative doses across all class 3 analgesics recorded for the considered participant is reported. (NCT01385748)
Timeframe: 8 weeks

Interventionmorphine dose equivalent (Mean)
Clonidine Lauriad® 50 µg469.31
Clonidine Lauriad® 100 µg415.49
Placebo Lauriad®624.94
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled439.95

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Cumulative Radiation Dose at Which Severe Oral Mucositis (World Health Organization [WHO] Score ≥ 3) Was First Observed

The primary endpoint planned in the protocol was the percentage of participants with an oral mucositis score greater than or equal to 3 using the WHO oral mucositis severity scale at a cumulative radiation dose of 50 Gy. This was modified by protocol amendment to the cumulative radiation dose at which a WHO score greater than or equal to 3 was first observed. This change was made to account for the fact that in real practice most patients receive a cumulative dose between 60 and 70 Gy. The presence of grade 3 or 4 oral mucositis was assessed twice weekly during the active phase (radiotherapy) by a trained radiation oncologist or an ear nose and throat specialist who took into account the field of radiation treatment. WHO score 3 = oral ulcers, liquid diet only; WHO score 4 = oral alimentation impossible. Each assessment was associated with the actual cumulative dose of radiotherapy. (NCT01385748)
Timeframe: 8 weeks

InterventionCumulative radiation dose (Gy) (Median)
Clonidine Lauriad® 50 µg66
Clonidine Lauriad® 100 µg56
Placebo Lauriad®48
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled60

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The Overall Incidence of Grade 3/4 Mucositis During the Active Phase.

The presence of grade 3 or 4 oral mucositis on the World Health Organization (WHO) oral mucositis severity scale was assessed twice weekly during the active phase (radiotherapy) by a trained radiation oncologist or an ear nose and throat specialist who took into account the field of radiation treatment. WHO score 3 = ulcers, extensive erythema, and the inability of the participant to swallow a solid diet; WHO score 4 = mucositis to the extent that alimentation was not possible.The number of participants with at least one Grade 3 or Grade 4 mucositis score during the active phase is reported. (NCT01385748)
Timeframe: 8 weeks

,,,
Interventionparticipants (Number)
MissingNoYes
Clonidine Lauriad® 100 µg23330
Clonidine Lauriad® 50 µg23123
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled46453
Placebo Lauriad®22436

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The Maximum Severity of Oral Mucositis

Participants were assessed using the World Health Organization (WHO) oral mucositis severity scale twice weekly during the active phase (radiotherapy) by a trained radiation oncologist or an ear nose and throat specialist who took into account the field of radiation treatment. The WHO scores were as follows: 0 = None; 1 = oral soreness, erythema; 2 = oral erythema, ulcers, solid diet tolerated; 3 = oral ulcers, liquid diet only; 4 = oral alimentation impossible. The maximum severity was the maximum score reported during the active phase. (NCT01385748)
Timeframe: 8 weeks

,,,
Interventionparticipants (Number)
Grade 0Grade 1Grade 2Grade 3Grade 4No value during the concerned period
Clonidine Lauriad® 100 µg672020102
Clonidine Lauriad® 50 µg79151762
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled13163537164
Placebo Lauriad®49113062

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Overall Treatment Compliance According to the Patient Diary

"All participants complete a daily questionnaire during the active phase (radiotherapy). Compliance = [ number of tablets / (end date of treatment - start date treatment + 1 ) ] * 100. The number of tablets is the number of days with a tablet applied and treatment start and end dates are the first and last dates of the patient diary with a tablet applied." (NCT01385748)
Timeframe: 8 weeks

Interventionpercentage of compliance (Mean)
Clonidine Lauriad® 50 µg94.28
Clonidine Lauriad® 100 µg93.12
Placebo Lauriad®96.12
Clonidine Lauriad® Muco-adhesive Buccal Tablets Pooled93.66

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Pharmacokinetic (PK) Parameter Cmax (Maximum Observed Drug Concentration in Plasma) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.

"Baseline: immediately before the standardized meal (i.e., before administration of tizanidine) on dosing day~0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours after administration of tizanidine~PK parameters will be derived by using WinNonlin Pro (version 5.0.1 or later, Pharsight Corp)." (NCT01405950)
Timeframe: Baseline and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionnanogram/mililiter (Mean)
Dose Level 11.87
Dose Level 25.29

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Pharmacokinetic (PK) Parameter AUC0-8 (Area Under the Concentration-time Curve From Time 0 to 8 Hours) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.

"Baseline: immediately before the standardized meal (i.e., before administration of tizanidine) on dosing day~0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours after administration of tizanidine~PK parameters will be derived by using WinNonlin Pro (version 5.0.1 or later, Pharsight Corp)." (NCT01405950)
Timeframe: Baseline and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionhour*nanogram/mililiter (Mean)
Dose Level 15.60
Dose Level 26.11

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Long-term Maintenance of Efficacy of KAPVAY in Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD) as Measured by the Percentage of Treatment Failures in the KAPVAY vs. Placebo Groups

"Treatment failure a ≥30 percentage increase (worsening)(ADHD-RS-IV, clinician version) total score and a ≥2 point increase (worsening) in Clinical Global Impressions-Severity of Illness Scale (CGI-S) at any two consecutive visits during the randomized-withdrawal period.~The ADHD-RS-IV of 2 subscales: inattention - 9 items and hyperactivity-impulsivity - 9 items. Each gives a score ranging from 0 (none, never or rarely) to 3 (severe, very often), for a total score ranging from 0 to 54 (higher score worse).~The CGI-S is a 7-point scale,1 (Normal, not at all ill) to 7 (extremely ill patients).The CGI-Severity (CGI-S) asks the clinician one question: Considering your total clinical experience with this particular population, how mentally ill is the patient at this time? which is rated on the following seven-point scale: 1=normal, not at all ill; 2=borderline mentally ill; 3=mildly ill; 4=moderately ill; 5=markedly ill; 6=severely ill; 7=among the most extremely ill patients." (NCT01439126)
Timeframe: From randomization to end of the randomized-withdrawal period (26 weeks)

Intervention% of Participants (Number)
Subjects on KAPVAY (Clonidine Hydrochloride)31
Subjects on Placebo42

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Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the Weiss Functional Impairment Rating Scale-Parent (WFIRS-P)

"The WFIRS-P is designed to assess the impact of child's behavior or emotional problems on 7 domains related to function: Family (10 items), School Learning (4 items), School Behavior (6 items), Life Skills (10 items), Child's Self-concept (3 items), Social Activities (7 items), and Risky Activities (10 items). Each item was scored on a scale ranging from 0 (never or not at all) to 3 (very often or very much). Each scale score was calculated as the average for that scale. The total score is the average of all non-missing items. Higher scores are associated with greater impact of disease on functioning." (NCT01439126)
Timeframe: From randomization to end of the randomized-withdrawal period (26 weeks)

Interventionunits on a scale (Mean)
Subjects on KAPVAY (Clonidine Hydrochloride)0.0
Subjects on Placebo0.0

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Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the Epworth Sleepiness Scale for Children (ESS-C)

"Change in the ESS-C scale from randomization to end of randomized-withdrawal period. The ESS-C is a simple eight-tem Likert scale designed to assess daytime sleepiness in children aged 2-18 years. The scale takes less than two minutes to be completed by patient or by parent rating. Sleepiness is a common symptom in both medicated and unmedicated children with ADHD given the predominance of impaired sleep quality. The total score achieved when the chance of dozing in each situation is added up serves as the outcome measure.~The ESS-C comprises 8 items describing various daytime activities. Item scores ranging from 0 (would never doze or sleep) to 3 (high chance of dozing or sleeping). A total score is derived as the sum of the items, with higher total scores indicative of a greater level of sleepiness (worse outcome). Total scores range from 0 to 24." (NCT01439126)
Timeframe: From randomization to end of the randomized-withdrawal period (26 weeks)

Interventionunits on a scale (Mean)
Subjects on KAPVAY (Clonidine Hydrochloride)-0.6
Subjects on Placebo-0.6

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Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the Clinical Global Impressions-Severity of Illness Scale (CGI-S)

"The CGI-S is a clinician rated instrument designed to assess the subject's current illness state. The CGI-Severity (CGI-S) asks the clinician one question: Considering your total clinical experience with this particular population, how mentally ill is the patient at this time? which is rated on the following seven-point scale: 1=normal, not at all ill; 2=borderline mentally ill; 3=mildly ill; 4=moderately ill; 5=markedly ill; 6=severely ill; 7=among the most extremely ill patients.~This rating is based upon observed and reported symptoms, behavior, and function in the past seven days." (NCT01439126)
Timeframe: From randomization to end of the randomized-withdrawal period (26 weeks)

Interventionscores on a scale (Mean)
Subjects on KAPVAY (Clonidine Hydrochloride)0.4
Subjects on Placebo0.9

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Long-term Efficacy of KAPVAY in Children and Adolescents With ADHD as Measured by the Change From Randomization to the End of the Randomized-withdrawal Period on the ADHD-Rating Scale-4th Edition (ADHD-RS-IV)

The ADHD-RS-IV (clinician version), has been widely used as a measure of efficacy in clinical trials of treatments in children and adolescents with ADHD. It is derived from the 18 inattentive and hyperactive/impulsive diagnostic criteria for ADHD from the Diagnostic and Statistical Manual of Mental Disorders, 4th Edition, Text Revision (DSM-IV-TR). The clinician version of the ADHD-RS-IV has a large base of normative data and has demonstrated reliability and discriminant validity in children and adolescents. The ADHD-RS-IV of 2 subscales: inattention - 9 items and hyperactivity-impulsivity - 9 items. Each gives a score ranging from 0 (none, never or rarely) to 3 (severe, very often), for a total score ranging from 0 to 54 (higher score worse and a lower score more favourable). Two subscales are summed. (NCT01439126)
Timeframe: From randomization to end of the randomized-withdrawal period (26 weeks)

Interventionscores on a scale (Mean)
Subjects on KAPVAY (Clonidine Hydrochloride)3.0
Subjects on Placebo7.0

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Long-term Safety of KAPVAY in Children and Adolescents With ADHD Based on the Assessment of Adverse Events (AEs), Serious Adverse Events (SAEs), AEs Leading to Study Drug Discontinuation, Clinically Significant Changes or Abnormalities in Vital Signs

(NCT01439126)
Timeframe: From study start to study end (40 weeks)

,
InterventionParticipants (Number)
No. Subjects with At Least 1 Treatment-Emergent AEAny Severe Treatment-Emergent AE (TEAE)Any SAETreatment Emergent AE leading to discontinuationAny Treatment-Related AEVital Signs Abnormalities
Subjects on KAPVAY (Clonidine Hydrochloride)34202183
Subjects on Placebo31020121

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To Evaluate the Long-term Efficacy of KAPVAY in Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD) as Measured by the Time to Treatment Failure From the Start of Randomized-withdrawal Period

Time to treatment failure was calculated as follows: Treatment failure (not premature termination) = visit date where the failure criteria was met - visit 9 date + 1; Treatment failure (premature termination) = termination date - visit 9 date + 1 (NCT01439126)
Timeframe: Time From randomization to treatment failure (up to 26 weeks)

Interventiondays (Median)
Subjects on KAPVAY (Clonidine Hydrochloride)212
Subjects on Placebo75

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Long-term Safety of KAPVAY in Children and Adolescents With ADHD Based on the Assessment of Changes in the Columbia Suicide Severity Rating Scale (C-SSRS)

"The outcome reported is the number of subjects that responded Yes to the question Do you have a wish to be dead at Visit 20.~C-SSRS is a clinician-rated instrument designed to provide consistent and systematic assessment of both suicidal ideation and behavior within a study, as well as across studies. The scale is a feasible, low burden series of questions that appropriately assess and track all suicidal events, including ideation. Suicidal ideation is assessed according to yes/no responses to 5 questions of increasing severity (from a wish to die to an active thought of killing oneself with plan and intent) as follows:~Wish to be Dead~Non-Specific Active Suicidal Thoughts~Active Suicidal Ideation with Any Methods (Not Plan) without Intent to Act~Active Suicidal Ideation with Some Intent to Act, without Specific Plan~Active Suicidal Ideation with Specific Plan and Intent" (NCT01439126)
Timeframe: Visit 20 (Week 40)

Interventionparticipants (Number)
Subjects on KAPVAY (Clonidine Hydrochloride)0
Subjects on Placebo1

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Newborn Outcome Measure: APGAR Score.

"The APGAR score is the most common indicator of neonatal status immediately after delivery.~The test is done by a doctor, midwife, or nurse. The health care provider will examine the baby's:~Breathing effort Heart rate Muscle tone Reflexes Skin color Each category is scored with 0, 1, or 2, depending on the observed condition. The APGAR rating is based on a total score of 1 to 10. The higher the score, the better the baby is doing after birth." (NCT01559012)
Timeframe: at 1 minute and at 5 minutes after delivery

Interventionunits on a scale (Mean)
APGAR Score at 1'9
APGAR Score at 5'9

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PUQE Score for Assessment of Severity in Hyperemesis Gravidarum

"PUQE in an acronym for Pregnancy Unique Quantification of Emesis, a validated clinical score for assessment of severity of emesis in pregnancy.~It is composed of three items; every item has a score from 1 (best) to 5 (worst).~The sum range varies from 3 (best) to 15 (worst). Participants are followed for the whole duration of hospital stay (10 days) asking them to score their symptoms daily." (NCT01559012)
Timeframe: Mean values of first period of five days are compared with mean values of second period of five days. Change is reported as baseline value - value at day 5 or at day 10.

Interventionunits on a scale (Mean)
Clonidine6.3
Placebo8.5

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Diastolic Blood Pressure

Diastolic BP was recorded every day during clonidine (5 days) and placebo (5 days) cycle (NCT01559012)
Timeframe: 10 days

InterventionmmHg (Mean)
Clonidine58
Placebo61

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Morning Urine Ketonuria

Morning urine ketonuria is a simple direct marker of starving associated to nausea and vomiting (NCT01559012)
Timeframe: participants are followed for the whole duration of hospital stay (10 days) comparing the first period of 5 days with the second period of 5 days

InterventionProportion of person-days (Mean)
Clonidine0.06
Placebo0.36

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Pregnancy Outcome Measures: Birth Weight.

Birth weight adjusted for gestational age at delivery is a measure of pregnancy outcome after treatment of HG. (NCT01559012)
Timeframe: at delivery

Interventiongrams (Mean)
Mean Birth Weight of 12 Patients3312

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Number of Days Off i.v. Therapy, the TD System (Clonidine/Placebo) Being Applied Only

if the symptoms improve the patient and her doctors may decide to stop parenteral drugs continuing the TD system therapy. (NCT01559012)
Timeframe: participants are followed for the whole duration of hospital stay (10 days) comparing the first period of 5 days with the second period of 5 days

InterventionProportion of person-days (Mean)
Clonidine0.40
Placebo0.20

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Systolic Blood Pressure

Systolic BP was measured every day during the clonidine treatment (5 days) and placebo (5 days) (NCT01559012)
Timeframe: 10 days

InterventionmmHg (Mean)
Clonidine91
Placebo97

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VAS Score for Assessment of Severity in Hyperemesis Gravidarum

VAS is a Visual Analogic Scale formulated in 5 items. Every item has a score from 0 (best) to 10 (worst). The sum range swings from 0 (best ) to 50 (worst). Participants are followed for the whole duration of hospital stay (10 days) asking them to score their symptoms daily. (NCT01559012)
Timeframe: Mean values of first period of five days are compared with mean values of second period of five days. Change is reported as baseline value - value at day 5 or at day 10.

Interventionunits on a scale (Mean)
Clonidine22
Placebo29

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Number of Patients Choosing Active Treatment for Off-label, Compassionate Use.

the patients were asked to choose between two transdermal systems (active drug versus placebo) as the most effective (NCT01559012)
Timeframe: at 10 days since start of treatment

Interventionparticipants (Number)
Clonidine9
Placebo3

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Daily Doses of Standard Antiemetic Drugs Required in the Two Different Periods.

"The patients were randomly treated with and without TD clonidine (5mg patch) for 2 consecutive periods of 5 days , other antiemetic drugs (promethazine, prochlorperazine, metoclopramide, ondansetron) and anti reflux drugs (ranitidine, omeprazole) being administered on a scheduled or as-needed basis.~All patients received intravenous hydration and supplementation with thiamine, during both periods. The use of steroids was allowed as a rescue medication in case of further worsening of symptoms." (NCT01559012)
Timeframe: participants are followed for the whole duration of hospital stay (10 days) comparing the first period of 5 days with the second period of 5 days

Interventiondaily doses of antiemetics (Mean)
Clonidine1.5
Placebo2.3

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Change From Baseline in Cannabis Use at 10 Weeks

Subject self-report hits of marijuana per day at week 10 (NCT01598896)
Timeframe: At 10 weeks

Interventionhits/day (Mean)
Dronabinol + Clonidine16.91
Placebo22.35

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Change From Baseline in Cannabis Use at 14 Weeks

Self-report cannabis use at 14 weeks after initiating the study. (NCT01598896)
Timeframe: At 14 weeks

Interventionhits/day (Mean)
Dronabinol + Clonidine18.95
Placebo16.29

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Change in Craving Symptoms From Baseline at 10 Weeks

"Scores on the Marijuana Craving Questionnaire (MCQ) (Heishman et al. 2009) - The 4 Factor Total Score.~Maximum Score = 84 Minimum Score = 12 The higher the score, the more severe marijuana craving symptoms endorsed by the subject." (NCT01598896)
Timeframe: At 10 weeks

Interventionscore on a MCQ 4 Factor Total scale (Mean)
Dronabinol + Clonidine51
Placebo52.33

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Change in Craving Symptoms From Baseline at 14 Weeks

"Scores on the Marijuana Craving Questionnaire (Heishman et al. 2009) - The 4 Factor Total Score~Maximum Score = 84 Minimum Score = 12 The higher the score, the more severe marijuana craving symptoms endorsed by the subject." (NCT01598896)
Timeframe: At 14 weeks

Interventionscore on MCQ Total 4 Factor scale (Mean)
Dronabinol + Clonidine54.33
Placebo56

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Average Observer-Rated Patient Pain Scores

Patients will be observed with behaviors rated at regular time intervals using the CHIPPS (Children and Infants Postoperative Pain Scale) pain survey. The CHIPPS scale values range from a minimum of 0 (no pain, better outcome) to a maximum of 10 (worst pain, worse outcome). (NCT01638052)
Timeframe: 60 minutes

Interventionunits on a scale (Mean)
0.25% Bupivacaine2
0.25% Bupivacaine + Clonidine1.9

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Number of Participants Requiring Use of Rescue Analgesic Medication in the Initial 24 Hours Postoperatively

Count of participants who will require use of rescue analgesic medication in the initial 24 hours postoperatively as recorded in the hospital or by parents at home following discharge. (NCT01638052)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
0.25% Bupivacaine18
0.25% Bupivacaine + Clonidine22

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Number of Participants With Nausea/Vomiting

Incidence of nausea/vomiting during 24 hour observation (NCT01638052)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
0.25% Bupivacaine14
0.25% Bupivacaine + Clonidine10

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Duration of Treatment

Total number days of treatment (NCT01734551)
Timeframe: 120 days

Interventiondays (Median)
Morphine39
Clonidine27

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Bayley Scales of Infant and Toddler Development Third Edition

Scores obtained Bayley Scales of Infant and Toddler Development Third Edition in the developmental domains of motor, cognitive, and language. This tool for measures of motor, cognitive and language development is a series of standardized measurements and for each domain, the standardized scores have a mean of 100 and standard deviation of 15. Scores below 1 standard deviation (= or less than 84) is considered below normal. Scores above 1 standard deviation (over 115) represent higher than normal functioning in each domain The score for each domain (motor, cognitive, and language functioning) represents the full-scale score (NCT01734551)
Timeframe: 1 year of life

,
Interventionscores on a scale (Mean)
Bayley III motorCognitiveLanguage totalLanguage ReceptiveLanguage Expressive
Clonidine95.893.395.895.099.2
Morphine97.692.998.0101.1100.0

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Finnegan Neonatal Abstinence Scoring System

Mean of total Finnegan Scores obtained every 3 hours on days 2, 7, and 14 following start of treatment; A score is a number representing the total score or sum from 21 items or symptoms or manifestations of opiate withdrawal in newborn infants. The total score ranges from 0 to 43. Reference: 1. Finnegan LP, Connaughton JF, Jr., Kron RE, et al. Neonatal abstinence syndrome: assessment and management. Addict Dis 1975;2(1-2):141-58. Although normal newborn may manifest mild symptoms that will give scores in the range of 0 to 7. A score of 8 consecutively obtained times 3 indicate that infant will benefit from treatment, in this study morphine or clonidine. A decrease in scores especially to less than 8 is suggestive of a good response to treatment. (NCT01734551)
Timeframe: 14 days

,
Interventionscores on a scale (Mean)
Finnegan scores day 2 of treatmentFinnegan scores day 7 of treatmentFinnegan scores day 14 of treatment
Clonidine8.55.76.7
Morphine7.56.67.1

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Neurobehavioral Performance Summary Scores From the Neonatal Intensive Care Unit Network Neurobehavioral Scale (NNNS)

The summary scores from the Neonatal Intensive Care Unit Network Neurobehavioral Scale (NNNS) give a measure of infant neurobehavior in the following areas (score range): habituation (1-9), regulation (2.20-7.50), attention (1.29 -8.4), Handling (0 - 1), quality of movement (1.20 - 6.20), Non-optimal reflexes (0-12), Asymmetric reflexes (0-7), arousal (2.43 - 6.67), hypertonicity (0- 8), hypotonicity (0 - 5.0), excitability (0-11), lethargy (0 - 11.0). and stress/abstinence (0. - 0.57). A higher score for each item means a higher level of the construct. For example, a higher score for hypertonicity means the infant is more hypertonic and higher score on hypotonicity means the infant is more hypotonic. No cut-off score published for normal or abnormal behavioral performance. Reference: Lester BM et al. Summary Statistics of Neonatal Intensive Care Unit Network Neurobehavioral Scale Scores From the Maternal Lifestyle Study: A Quasinormative Sample, in Pediatrics 2004; 113,668. (NCT01734551)
Timeframe: 5-10 days after treatment starts

,
Interventionscores on a scale (Mean)
AttentionHandlingQuality of movementRegulationNon-optimal reflexesAsymmetric reflexesStress/abstinenceArousalHypertonicityHypotonicityExcitabilityLethargy
Clonidine4.510.424.925.264.130.000.083.950.250.192.385.13
Morphine5.060.364.775.23.730.200.073.910.400.132.63.6

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Expression of α1-adrenoceptors (α1-AR) in Dermal Nerve Bundles in the CRPS-affected Limb of Phenylephrine Responders and Non-responders

Expression of α1-AR was determined from the skin biopsies using immunohistochemistry. Nerve bundles in the reticular dermis were identified in the affected limb of 25 patients with CRPS [only 22 of these were classified as phenylephrine responders/non-responders], in the contralateral limb of 21 patients with CRPS, and in 12 controls. Samples were processed in batches containing sections from 10 controls and from the affected and contralateral limbs of 10 patients. The α1-AR immunoreactivity (a measure of the expression of receptors) scores were transformed into standard units with a mean of 0 and a SD of 1 (ie, Z-scores). Positive scores represent greater than average α1-AR immunoreactivity (i.e. higher expression of α1-AR) compared with other samples in the run, and negative scores represent less than average α1-AR immunoreactivity. Normalized scores were averaged across multiple runs for each patient or control to obtain a mean α1-AR score. (NCT01813149)
Timeframe: Day 2, after clonidine injection

,
Interventionz-score (Mean)
Nerve bundles identified in reticular dermisNerve bundle not identified in reticular dermis
Phenylephrine Non-responders0.142NA
Phenylephrine Responders1.146NA

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Neonatal Apgar Score

The Apgar score is based on a total score of 1 to 10. The higher the score, the better the baby is doing after birth. A score of 7, 8, or 9 is normal and is a sign that the newborn is in good health. (NCT01846221)
Timeframe: 1 minute and 5 minutes post delivery

,
InterventionApgar score (Mean)
1 Minute5 Minutes
Clonidine8.538.94
Fentanyl8.248.88

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Number of Spontaneous Vaginal Deliveries

Mode of delivery: spontaneous vaginal or instrumental vaginal versus cesarean. (NCT01846221)
Timeframe: Upon delivery (approximately up to 8 hours from baseline)

Interventionspontaneous vaginal deliveries (Number)
Clonidine38
Fentanyl40

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Number of Subjects With Success Rate at 15 Minutes Post-epidural Bolus Injection

Pain Visual Analogue Scale (VAS) was evaluated every 5 min for 15 min. 'Success' is defined as at least a 4-point reduction in VAS at 15 min. (0=no pain, 10= worst pain) (NCT01846221)
Timeframe: Baseline, 15 Minutes post epidural administration

InterventionParticipants (Count of Participants)
Clonidine31
Fentanyl38

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Maternal Heart Rate

Heart rate will be measured at different timepoints. (NCT01846221)
Timeframe: Baseline, 30 Minutes post epidural administration

,
Interventionbeats per minute (BPM) (Mean)
Baseline30 Minutes
Clonidine8784
Fentanyl8485

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Maternal Systolic Blood Pressure

Blood pressure will be measured at different timepoints. (NCT01846221)
Timeframe: Baseline, 30 Minutes post epidural administration

,
Interventionmm Hg (Mean)
Baseline30 Minutes
Clonidine123116
Fentanyl121118

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Steady State Clonidine Blood Levels During Hypothermia

"Trough clonidine blood levels were measured after 4-7 doses of clonidine were given intravenously with a dosing interval of every 8 hrs. Mean and standard deviation (SD) of the number of doses given prior to levels being drawn was 5.3 (mean) and 0.37 (SD).~Time after last dose before measurement was 9hrs (mean) and 2.7hrs (SD)." (NCT01862250)
Timeframe: 3 days

Interventionng/ml (Median)
Clonidine Infants With HIE0.6

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Presence of Shivering After Clonidine

Babies were assessed after administration of clonidine for the presence or absence of shivering. (NCT01862250)
Timeframe: 48hrs

InterventionParticipants (Count of Participants)
Clonidine Infants With HIE0

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Amount of Morphine Given

Intravenous morphine (mg/kg) was given. The standard dose is 0.05 mg/kg per dose (NCT01862250)
Timeframe: Up to 2 days

Interventionmg/kg (Median)
Clonidine Infants With HIE0.02

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Time to Passive Rewarming

Following 2 hours of therapeutic hypothermia, the temperature of the thermo-blanket is adjusted up half degree per hour allowing passive rewarming until 36.5 degrees is reached (NCT01862250)
Timeframe: Beginning at 72 hours up to 12 hours

InterventionHours (Median)
Clonidine Infants With HIE8.7

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Completion Status

The percentage of subjects in each treatment arm who receive at least one dose of study medication on Day 7 and complete the 3.5 hour post-dose SOWS-Gossop assessment on Day 7. (NCT01863186)
Timeframe: Day 7

,,
InterventionParticipants (Count of Participants)
Yes/CompleteNo/Did Not Complete
DB: Lofexidine HCl 2.4mg Dose95134
DB: Lofexidine HCl 3.2mg Dose88134
DB: Placebo42109

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Difference Between the Overall Means From Short Opiate Withdrawal Scale of Gossop (SOWS-Gossop) Scores

"The SOWS-Gossop was completed by the mITT population subject at baseline, once daily at 3.5 hours after the first dose of the study medication on Days 1 to 7. It consists of 10 items that are scored on a 4-point scale; 0=none, 1=mild, 2=moderate, and 3=severe. The overall score is the simple sum of the 10-item scores (minimum overall score of 0, maximum score of 30). Higher individual scores on the scale indicate greater symptom severity. However, as the outcome measure is a difference from placebo, a lower number indicates a better outcome.~mITT population: all randomized subjects who received at least 1 dose of study medication" (NCT01863186)
Timeframe: Days 1 through 7

,,
Interventionscore on a scale (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
DB: Lofexidine HCl 2.4mg Dose7.810.27.65.74.73.62.7
DB: Lofexidine HCl 3.2mg Dose7.69.97.45.54.53.22.3
DB: Placebo9.413.910.99.26.44.42.7

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Aortic Stiffness

Carotid-femoral pulse wave velocity (PWV) (NCT01983462)
Timeframe: 4 weeks

,,
Interventionmeters/sec (Mean)
Baseline4 weeks
Clonidine7.97.3
Hydrochlorothiazide7.07.0
Placebo8.18.0

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24 Hour Average Systolic Blood Pressure

24 hour ambulatory systolic blood pressure (NCT01983462)
Timeframe: 4 weeks

,,
InterventionmmHg (Mean)
Baseline4 weeks
Clonidine133126
Hydrochlorothiazide135131
Placebo133134

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Change From Baseline to Day 84 (Week 12) in Numeric Pain Rating Scale Score

"The Numeric Pain Rating Scale is a single reading that measures the patients interpretation of their pain on a scale from 0, no pain to 10, worst pain imaginable. The change from baseline can range from -10 to 10. The change from Baseline (averaged over Day -14 to Day -8) to End-of-Treatment (averaged over Days 78 to 84 [±3 days]) in the Numeric Pain Rating Scale score assessing the average pain in the past 24 hours in the painful areas of the feet averaged over Days 78 to 84 compared to the 7 days at the Baseline Phase (Days -14 to -8). For the primary efficacy endpoint, the mean change in pain intensity from Baseline to Week 12 was analyzed using an analysis of covariance (ANCOVA) model with the Baseline pain intensity score serving as a covariate. The statistical model also included treatment, site, site by treatment interaction, and strata. If the site by treatment interaction term was not significant at the 0.1 level, then it was excluded from the model." (NCT02068027)
Timeframe: The change from Baseline (averaged over Day -14 to Day -8) to End-of-Treatment (averaged over Days 78 to 84 [±3 days])

Interventionunits on a scale (Mean)
Clonidine Gel 0.1%-1.6
Placebo-1.6

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Mean Daily Worst Pain Intensity Numeric Pain Rating Scale Scores

"The Numeric Pain Rating Scale is a single reading that measures the patients interpretation of their pain on a scale from 0, no pain to 10, worst pain imaginable. The change from baseline can range from -10 to 10. The change from Baseline (worst score from Day -14 to Day -8) to End-of-Treatment (worst score during Days 78 to 84 [±3 days]) in the Numeric Pain Rating Scale score assessing the worst pain in the past 24 hours in the painful areas of the feet from Days 78 to 84 compared to the 7 days at the Baseline Phase (Days -14 to -8). For the endpoint, the change in worst pain intensity from Baseline to Week 12 was analyzed using an analysis of covariance (ANCOVA) model with the Baseline worst pain intensity score serving as a covariate. The statistical model also included treatment, site, site by treatment interaction, and strata. If the site by treatment interaction term was not significant at the 0.1 level, then it was excluded from the model." (NCT02068027)
Timeframe: The change from Baseline (worse over Day -14 to Day -8) to End-of-Treatment (worse over Days 78 to 84 [±3 days])

Interventionunits on a scale (Mean)
Clonidine Gel 0.1%-1.4
Placebo-1.4

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AUC0-inf(Area Under the Concentration-time Curve of Clonidine in Plasma Over the Time Interval From 0 to Infinity)

AUC 0-inf(area under the concentration-time curve of clonidine in plasma over the time interval from 0 to infinity) The values for geometric mean and gCV are actually adjusted geometric means and adjusted intra-individual gCVs, respectively. (NCT02096744)
Timeframe: 1 hour (h) before patch administration and 12h, 24h, 48h, 72h, 96h, 120h, 144h, 168h, 192h, 216h, 240h after patch administration

Interventionpg*h/mL (Geometric Mean)
Catapres®-TTS-3 With Oppanol®119127.55
Catapres-TTS-3 With Vistanex™115903.34

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AUC0-168 (Area Under the Concentration-time Curve of Clonidine in Plasma Over the Time Interval From 0 to 168 h)

AUC0-168 (area under the concentration-time curve of clonidine in plasma over the time interval from 0 to 168 h) The values for geometric mean and geometric coefficient of variation (gCV) are actually adjusted geometric means and adjusted intra-individual gCVs, respectively. (NCT02096744)
Timeframe: 1 hour (h) before patch administration and 12h, 24h, 48h, 72h, 96h, 120h, 144h, 168h after patch administration

Interventionpg*h/mL (Geometric Mean)
Catapres®-TTS-3 With Oppanol®82517.99
Catapres®-TTS-3 With Vistanex™80641.47

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Cavg (Average of Measured Concentrations of Clonidine in Plasma on Days 5, 6, and 7)

Cavg (average of measured concentrations of clonidine in plasma on Days 5, 6, and 7) The values for geometric mean and gCV are actually adjusted geometric means and adjusted intra-individual gCVs, respectively. (NCT02096744)
Timeframe: 1 hour (h) before patch administration and 12h, 24h, 48h, 72h, 96h, 120h, 144h, 168h, 192h, 216h, 240h after patch administration

Interventionpg/mL (Geometric Mean)
Catapres®-TTS-3 With Oppanol®697.327
Catapres®-TTS-3 With Vistanex™668.893

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Cmax (Maximum Concentration of Clonidine in Plasma)

Cmax (maximum concentration of clonidine in plasma) The values for geometric mean and gCV are actually adjusted geometric means and adjusted intra-individual gCVs, respectively. (NCT02096744)
Timeframe: 1 hour (h) before patch administration and 12h, 24h, 48h, 72h, 96h, 120h, 144h, 168h, 192h, 216h, 240h after patch administration

Interventionpg/mL (Geometric Mean)
Catapres®-TTS-3 With Oppanol®813.516
Catapres®-TTS-3 With Vistanex™781.896

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Postoperative Analgesia

Post-operative Visual Analog Pain (VAS) scores on the scale of 10 (0=no pain and 10=worse imaginary pain). (NCT02151487)
Timeframe: within 15 minutes at postanesthesia care unit (PACU) arrival

Interventionscore on a scale of 10 (Median)
Ropivacaine0
Ropivacaine and Dexamethasone0
Ropivacaine and Clonidine0
Ropivacaine, Dexamethasone and Clonidine0

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Duration of the Sensorial Supraclavicular Block

Duration of sensorial block defined as the time interval between subject admitted to the Post-Anesthesia Care Unit and the time the first pain medication taken at home (NCT02151487)
Timeframe: within 24-hr after surgery

Interventionhour (Mean)
Ropivacaine13.4
Ropivacaine and Dexamethasone14
Ropivacaine and Clonidine17.4
Ropivacaine, Dexamethasone and Clonidine18.8

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Summary of Neuropathic Pain Symptom Inventory (NPSI)

The NPSI is a validated, self-administered questionnaire designed to evaluate the different symptoms of neuropathic pain. Each item is quantified on an 11-point (0-10) numeric scale. The NPSI includes 10 descriptors (plus 2 temporal items) that allow discrimination and quantification of 5 distinct clinically relevant dimensions of neuropathic pain syndromes. The Neuropathic Pain Symptom Inventory (NPSI) is a self-questionnaire designed to evaluate the different symptoms of neuropathic pain, which contains a list of descriptors reflecting spontaneous ongoing or paroxysmal pain, evoked pain (i.e., mechanical and thermal allodynia/hyperalgesia) and dysesthesia/paresthesia. Each of these items is quantified on an 11-point (0-10) numerical scale. NPSI total score was calculated and summarized descriptively at month 12 or the subjects last visit. The total score was calculated and summarized. (NCT02355158)
Timeframe: Month 12 or last visit

Interventionunits on a scale (Mean)
Active34.44

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Fentanyl and Morphine Requirements

Amount used (NCT02361476)
Timeframe: Recorded during the stay in the postoperative recovery room

Interventionmg morphine equivalents (Mean)
Intervention0.46
Placebo0.7

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Adverse Events

(NCT02361476)
Timeframe: from intervention to discharge from the recovery room

,
Interventionparticipants (Number)
adverse eventsserious adverse eventsTreated for low blood pressure
Intervention020
Placebo520

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Postoperative Agitation

Measured by Watchae Scale (score 1-4), scores 1-2 = no agitation and scores 3-4 = agitated (NCT02361476)
Timeframe: 1 day

Interventionparticipants with agitation (Number)
Intervention46
Placebo86

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First Administration of Fentanyl or Morphine

Time to administration (NCT02361476)
Timeframe: recovery room

InterventionMEDIAN time (min) to administration (Median)
Intervention105
Placebo60

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Pain Assessment

"Pain score used:~FLACC score = Face, Legs, Activity, Cry, Consolability Score ranges from 0 to 10 (severity increases with increasing score) Pain is FLACC score more than 3" (NCT02361476)
Timeframe: recovery room - hours

InterventionPain Score (Mean)
Intervention1.57
Placebo2.45

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Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

,,,,,
InterventionmmHg (Mean)
Day 1 ObservedDay 1 ChangeDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: 3.5 hr Post 1PM106.7-15.8108.6-14.1107.8-14.8109.7-13.2109.5-13.0109.1-13.8110.1-9.6
Inpatient: 3.5 hr Post 6PM108.7-13.9110.4-12.2110.8-11.9111.7-10.8110.2-12.3110.9-12.0114.6-4.6
Inpatient: 3.5 hr Post 8AM105.7-16.8108.5-14.0108.1-14.4107.9-14.4108.9-13.6108.8-14.0113.9-8.2
Inpatient: Pre 11PM109.0-13.6110.7-11.9110.5-12.2111.1-11.3111.4-11.0112.7-10.0111.6-7.3
Inpatient: Pre 1PM107.9-14.3108.0-14.7109.1-13.5110.9-11.9109.2-13.2110.2-12.6110.1-8.8
Inpatient: Pre 6PM108.2-14.7109.8-13.0110.0-12.6112.4-9.9110.8-11.7110.7-12.3112.7-6.8

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Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 Change
Outpatient: 3.5 hr Postdose113.4-8.8116.1-7.5116.4-5.8116.6-5.8117.6-2.5119.5-0.9121.91.6123.21.8118.4-4.1125.13.5

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Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 ChangeDay 14 ObservedDay 14 Change
Outpatient: Predose116.6-6.1114.6-8.4116.6-5.8118.0-4.6117.8-2.8119.4-0.8122.31.6123.73.0124.32.0122.71.0128.87.8

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Occurrence of Per Protocol Adverse Events of Special Interest (AESI)

(NCT02363998)
Timeframe: Day 1 to Day 14

InterventionParticipants (Count of Participants)
Orthostatic hypotensionOrthostatic bradycardiaSyncope
OL: Lofexidine HCl9601

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Overall Treatment Emergent Adverse Events (TEAEs) by Severity

(NCT02363998)
Timeframe: Days 1-14

InterventionParticipants (Count of Participants)
MildModerateSevere
OL: Lofexidine HCl1041588

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Safety Electrocardiograms (ECG) Evaluation Shift From Baseline to Post Dose and End of Study

For each 12-lead ECG obtained during the study, the investigator made an overall interpretation of the ECG (normal, abnormal NCS, and abnormal CS). Shifts from normal at baseline to abnormal NCS and abnormal CS at the end of study predose and postdose assessments were summarized. (NCT02363998)
Timeframe: Day 1 and Day 14

InterventionParticipants (Count of Participants)
Day 1 Post 8am Dose72274652Day 1 Post 8am Dose72274654Day 1 Post 8am Dose72274655Day 1 Post 8am Dose72274653End of Study Pre Dose72274652End of Study Pre Dose72274653End of Study Pre Dose72274655End of Study Pre Dose72274654End of Study Post Dose72274653End of Study Post Dose72274654End of Study Post Dose72274655End of Study Post Dose72274652
NormalAbnormal (NCS)Abnormal (CS)
Baseline Finding: Normal (OL: Lofexidine HCl)139
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)16
Baseline Finding: Abnormal (CS) (OL: Lofexidine HCl)0
Total (OL: Lofexidine HCl)155
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)87
Total (OL: Lofexidine HCl)128
Baseline Finding: Normal (OL: Lofexidine HCl)0
Total (OL: Lofexidine HCl)0
Baseline Finding: Normal (OL: Lofexidine HCl)83
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)20
Baseline Finding: Normal (OL: Lofexidine HCl)19
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)38
Total (OL: Lofexidine HCl)57
Baseline Finding: Normal (OL: Lofexidine HCl)1
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)0
Total (OL: Lofexidine HCl)1
Baseline Finding: Normal (OL: Lofexidine HCl)77
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)26
Total (OL: Lofexidine HCl)103
Baseline Finding: Normal (OL: Lofexidine HCl)41
Baseline Finding: Abnormal (NCS) (OL: Lofexidine HCl)47
Total (OL: Lofexidine HCl)88
Baseline Finding: Normal (OL: Lofexidine HCl)2
Total (OL: Lofexidine HCl)2

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Overall Occurrence of Serious Treatment Emergent Adverse Events (Serious TEAEs)

(NCT02363998)
Timeframe: Days 1-14

InterventionParticipants (Count of Participants)
OL: Lofexidine HCl2

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Overall Occurrence of Treatment Emergent Adverse Events (TEAEs)

Subjects with at least 1 TEAE occurring on days 1-14. (NCT02363998)
Timeframe: Days 1-14

InterventionParticipants (Count of Participants)
OL: Lofexidine HCl270

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Clinical Laboratory Test Change From Baseline: Chemistry

Chemistry Parameters with Shifts in ≥3% of Subjects from Screening to End of Study (NCT02363998)
Timeframe: Day 1 to Day 14

,,
InterventionParticipants (Count of Participants)
Alanine aminotransferase (U/L) : Below (Baseline)Alanine aminotransferase (U/L) : Normal (Baseline)Alanine aminotransferase (U/L) : Above (Baseline)Aspartate Aminotransferase (U/L) : Below (Baseline)Aspartate Aminotransferase (U/L) : Normal (Baseline)Aspartate Aminotransferase (U/L) : Above (Baseline)Gamma-glutamyl transferase (U/L) : Below (Baseline)Gamma-glutamyl transferase (U/L) : Normal (Baseline)Gamma-glutamyl transferase (U/L) : Above (Baseline)Alkaline phosphatase (U/L) : Below (Baseline)Alkaline phosphatase (U/L) : Normal (Baseline)Alkaline phosphatase (U/L) : Above (Baseline)Lactate dehydrogenase (U/L) : Below (Baseline)Lactate dehydrogenase (U/L) : Normal (Baseline)Lactate dehydrogenase (U/L) : Above (Baseline)Blood urea nitrogen (mg/dL) : Below (Baseline)Blood urea nitrogen (mg/dL) : Normal (Baseline)Blood urea nitrogen (mg/dL) : Above (Baseline)Creatinine (mg/dL) : Below (Baseline)Creatinine (mg/dL) : Normal (Baseline)Creatinine (mg/dL) : Above (Baseline)Cholesterol (mg/dL) : Below (Baseline)Cholesterol (mg/dL) : Normal (Baseline)Cholesterol (mg/dL) : Above (Baseline)Triglycerides (mg/dL) : Below (Baseline)Triglycerides (mg/dL) : Normal (Baseline)Triglycerides (mg/dL) : Above (Baseline)Calcium (mg/dL) : Below (Baseline)Calcium (mg/dL) : Normal (Baseline)Calcium (mg/dL) : Above (Baseline)Sodium (mEq/L) : Below (Baseline)Sodium (mEq/L) : Normal (Baseline)Sodium (mEq/L) : Above (Baseline)Potassium (mEq/L) : Below (Baseline)Potassium (mEq/L) : Normal (Baseline)Potassium (mEq/L) : Above (Baseline)Chloride (mEq/L) : Below (Baseline)Chloride (mEq/L) : Normal (Baseline)Chloride (mEq/L) : Above (Baseline)Carbon dioxide (bicarbonate) (mEq/L) : Below (Baseline)Carbon dioxide (bicarbonate) (mEq/L) : Normal (Baseline)Carbon dioxide (bicarbonate) (mEq/L) : Above (Baseline)Glucose (mg/dL) : Below (Baseline)Glucose (mg/dL) : Normal (Baseline)Glucose (mg/dL) : Above (Baseline)Phosphate (mg/dL) : Below (Baseline)Phosphate (mg/dL) : Normal (Baseline)Phosphate (mg/dL) : Above (Baseline)Protein (g/dL) : Below (Baseline)Protein (g/dL) : Normal (Baseline)Protein (g/dL) : Above (Baseline)Thyroid Stimulating Hormone-3rd Generation (TSH Thyrotropin)(mU/L) : Below (Baseline)Thyroid Stimulating Hormone-3rd Generation (TSH Thyrotropin)(mU/L) : Normal (Baseline)Thyroid Stimulating Hormone-3rd Generation (TSH Thyrotropin)(mU/L) : Above (Baseline)
Above Baseline (End of Study)01722010140112403807915102101820040390300500110051078035140226043031
Below Baseline (End of Study)0000009206902309281298000000017033002003003001016100011160
Normal (End of Study)015312016416131396317050164192812741714700153130107189182261870218365190001345251301941382611906181496

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Clinical Laboratory Test Change From Baseline: Hematology

Hematology Parameters with Shifts in ≥3% of Subjects from Screening to End of Study (NCT02363998)
Timeframe: Day 1 to Day 14

,,
InterventionParticipants (Count of Participants)
Hemoglobin (g/dL) : Below (Baseline)Hemoglobin (g/dL) : Normal (Baseline)Hemoglobin (g/dL) : Above (Baseline)Hematocrit (%) : Below (Baseline)Hematocrit (%) : Normal (Baseline)Hematocrit (%) : Above (Baseline)Platelet count (x10^9/L) : Below (Baseline)Platelet count (x10^9/L) : Normal (Baseline)Platelet count (x10^9/L) : Above (Baseline)Erythrocytes (x10^12/L) : Below (Baseline)Erythrocytes (x10^12/L) : Normal (Baseline)Erythrocytes (x10^12/L) : Above (Baseline)Erythrocytes distribution width (%) : Below (Baseline)Erythrocytes distribution width (%) : Normal (Baseline)Erythrocytes distribution width (%) : Above (Baseline)Mean corpuscular volume (fL) : Below (Baseline)Mean corpuscular volume (fL) : Normal (Baseline)Mean corpuscular volume (fL) : Above (Baseline)Leukocytes (x10^9/L) : Below (Baseline)Leukocytes (x10^9/L) : Normal (Baseline)Leukocytes (x10^9/L) : Above (Baseline)Neutrophils/Leukocytes (%) : Below (Baseline)Neutrophils/Leukocytes (%) : Normal (Baseline)Neutrophils/Leukocytes (%) : Above (Baseline)Neutrophils (x10^9/L) : Below (Baseline)Neutrophils (x10^9/L) : Normal (Baseline)Neutrophils (x10^9/L) : Above (Baseline)Lymphocytes/Leukocytes (%) : Below (Baseline)Lymphocytes/Leukocytes (%) : Normal (Baseline)Lymphocytes/Leukocytes (%) : Above (Baseline)Lymphocytes, absolute (x10^9/L) : Below (Baseline)Lymphocytes, absolute (x10^9/L) : Normal (Baseline)Lymphocytes, absolute (x10^9/L) : Above (Baseline)Monocytes/Leukocytes (%) : Below (Baseline)Monocytes/Leukocytes (%) : Normal (Baseline)Monocytes/Leukocytes (%) : Above (Baseline)Monocytes (x10^9/L) : Below (Baseline)Monocytes (x10^9/L) : Normal (Baseline)Monocytes (x10^9/L) : Above (Baseline)Eosinophils absolute (x10^9/L) : Below (Baseline)Eosinophils absolute (x10^9/L) : Normal (Baseline)Eosinophils absolute (x10^9/L) : Above (Baseline)Eosinophils/Leukocytes (%) : Below (Baseline)Eosinophils/Leukocytes (%) : Normal (Baseline)Eosinophils/Leukocytes (%) : Above (Baseline)Prothrombin time (seconds) : Below (Baseline)Prothrombin time (seconds) : Normal (Baseline)Prothrombin time (seconds) : Above (Baseline)Activated Partial Thromboplastin Time (seconds) : Below (Baseline)Activated Partial Thromboplastin Time (seconds) : Normal (Baseline)Activated Partial Thromboplastin Time (seconds) : Above (Baseline)
Above Baseline (End of Study)0890201201020161102222061302340196013311050210196071097012190201401318
Below Baseline (End of Study)2580116011401411000040002002001023321130010000000000000000
Normal (End of Study)271241231201001664201228015082173421674416380182315103122192101591701922017610014031015417115419

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Clinical Laboratory Test Change From Baseline: Urinalysis

(NCT02363998)
Timeframe: Day 1 to Day 7

,,
InterventionParticipants (Count of Participants)
Erythrocytes (/HPF) : Below (Baseline)Erythrocytes (/HPF) : Normal (Baseline)Erythrocytes (/HPF) : Above (Baseline)Leukocytes (/HPF) : Below (Baseline)Leukocytes (/HPF) : Normal (Baseline)Leukocytes (/HPF) : Above (Baseline)Specific Gravity : Below (Baseline)Specific Gravity : Normal (Baseline)Specific Gravity : Above (Baseline)pH : Below (Baseline)pH : Normal (Baseline)pH : Above (Baseline)
Above Baseline (End of Study)030130154031010
Below Baseline (End of Study)000000000000
Normal (End of Study)01362801751321881302042

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Columbia Suicide Severity Rating Scale Questionnaire (C-SSRS): Suicidal Ideation and Behavior Numbers

The C-SSRS measures both suicidal ideation and suicidal behavior and will be completed to assess lifetime suicidality before first dose of study drug, 3.5 hours after first daily dose of study drug on in-clinic treatment days, and then once a day before dosing during outpatient treatment days. C-SSRS will also be assessed at end of study/discontinuation. (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionParticipants (Count of Participants)
SuicidalitySuicidal ideationSuicidal behaviorEmergence of suicidal ideationEmergence of serious suicidal ideationWorsening of suicidal ideationEmergence of suicidal behavior
OL: Lofexidine HCl3027122020

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Mean Observed and Change From Screening in Seated Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

,,,,,,
InterventionmmHg (Mean)
Day 1 ObservedDay 1 ChangeDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: 3.5 hr Post 1PM70.8-6.373.4-3.873.0-4.174.7-2.672.7-4.272.2-4.670.2-6.9
Inpatient: 3.5 hr Post 6PM73.5-3.775.4-1.873.2-4.074.0-3.173.1-3.772.8-4.073.1-4.5
Inpatient: 3.5 hr Post 8AM69.4-7.872.2-4.973.2-4.071.4-5.771.5-5.469.8-7.074.3-3.5
Inpatient: Pre 11PM72.8-4.374.0-3.373.5-3.873.4-3.672.3-4.772.0-4.969.8-7.5
Inpatient: Pre 1PM69.3-7.972.2-5.071.4-5.870.9-6.471.7-5.170.8-6.071.5-4.8
Inpatient: Pre 6PM71.5-5.773.7-3.472.9-4.373.7-3.371.8-5.072.6-4.370.0-7.6
Inpatient: Pre 8AM78.3NA73.8-3.373.7-3.673.9-3.273.2-3.872.2-4.672.9-3.6

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Mean Observed and Change From Screening in Seated Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 Change
Outpatient: 3.5 hr Postdose71.7-6.172.8-6.076.8-1.471.8-7.673.9-3.574.0-3.575.8-1.276.3-0.476.6-0.577.92.0

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Mean Observed and Change From Screening in Seated Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 ChangeDay 14 ObservedDay 14 Change
Outpatient: Predose75.0-3.072.6-5.674.2-3.976.1-2.673.5-4.175.5-1.774.6-2.475.7-0.977.30.677.21.378.43.5

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Mean Observed and Change From Screening in Seated Pulse (Bpm): Vital Signs

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

,,,,,,
Interventionbeats per minute (bpm) (Mean)
Day 1 ObservedDay 1 ChangeDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: 3.5 hr Post 1PM69.9-4.966.8-8.066.6-8.567.8-7.369.0-5.268.6-5.373.0-3.8
Inpatient: 3.5 hr Post 6PM67.6-7.365.9-9.165.9-9.267.8-6.868.3-6.068.9-5.167.4-9.5
Inpatient: 3.5 hr Post 8AM68.8-6.168.8-5.967.5-7.568.3-6.869.1-5.369.8-4.173.90.0
Inpatient: Pre 11PM67.7-7.066.4-8.667.4-7.869.9-4.570.0-4.471.2-2.869.824
Inpatient: Pre 1PM69.2-5.769.4-5.468.7-6.470.6-4.571.4-2.870.6-3.373.6-3.1
Inpatient: Pre 6PM70.5-4.368.7-6.268.3-6.870.0-5.068.7-5.569.7-4.373.6-3.4
Inpatient: Pre 8AM73.3NA70.2-4.7213-5.070.1-5.070.9-3.470.5-3.673.2-1.1

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Mean Observed and Change From Screening in Seated Pulse (Bpm): Vital Signs

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

Interventionbeats per minute (bpm) (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 Change
Outpatient: 3.5 hr Postdose72.4-3.373.3-3.274.8-1.667.1-7.772.6-3.875.1-1.777.91.174.5-1.472.3-3.675.50.8

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Mean Observed and Change From Screening in Seated Pulse (Bpm): Vital Signs

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

Interventionbeats per minute (bpm) (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 ChangeDay 14 ObservedDay 14 Change
Outpatient: Predose70.6-5.276.3-0.375.2-1.673.6-3.477.71.679.62.880.03.279.33.279.74.076.62.476.42.4

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Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

,,,,,
InterventionmmHg (Mean)
Day 1 ObservedDay 1 ChangeDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: 3.5 hr Post 1PM112.6-9.4115.7-6.2116.9-5.0118.6-3.7116.3-5.6116.8-5.1117.9-3.0
Inpatient: 3.5 hr Post 6PM116.9-5.2119.7-2.1118.2-3.8120.0-1.8117.2-4.8117.5-4.5121.10.2
Inpatient: 3.5 hr Post 8AM109.7-12.2114.8-7.0116.1-5.8113.7-8.1114.8-7.1113.4-8.7116.4-5.4
Inpatient: Pre 11PM116.7-5.3117.9-3.9117.1-4.9117.7-4.0117.0-4.9118.4-3.5118.5-1.7
Inpatient: Pre 1PM111.1-10.8114.5-7.3114.3-7.5114.4-7.7115.2-6.6114.0-8.0114.9-5.1
Inpatient: Pre 6PM114.1-8.0117.4-4.5116.9-5.0118.7-3.0117.1-4.8116.6-5.5117.9-3.0

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Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
ScreeningDay 1 ObservedDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: Pre 8AM121.9122.2116.8-5.0116.0-5.9116.2-6.0115.4-6.3115.2-6.5118.0-4.4

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Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 Change
Outpatient: 3.5 hr Postdose115.7-5.5118.3-4.7122.00.4116.3-5.1122.82.1122.31.4124.33.6125.14.6120.4-1.4123.53.0

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Mean Observed and Change From Screening in Seated Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 ChangeDay 14 ObservedDay 14 Change
Outpatient: Predose117.0-4.7116.7-6.3118.7-3.6120.82.6118.4-2.8124.33.6122.21.2121.20.7126.34.3124.84.0128.07.6

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Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 1 ObservedDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: Pre 8AM79.873.4-6.574.0-6.273.2-7.072.4-7.672.9-7.173.6-6.2

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Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

,,,,,
InterventionmmHg (Mean)
Day 1 ObservedDay 1 ChangeDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: 3.5 hr Post 1PM69.8-10.071.6-8.570.0-10.171.5-8.970.3-9.670.2-9.871.3-9.7
Inpatient: 3.5 hr Post 6PM71.0-8.972.3-7.971.3-8.871.2-9.070.2-9.872.1-7.972.5-8.5
Inpatient: 3.5 hr Post 8AM68.8-11.170.7-9.470.6-9.470.6-9.470.0-10.069.3-10.773.2-7.4
Inpatient: Pre 11PM70.4-9.671.8-8.471.5-8.771.8-8.271.1-9.072.5-7.569.0-11.8
Inpatient: Pre 1PM70.3-9.571.0-9.170.0-10.071.2-9.270.7-9.271.1-8.970.3-9.5
Inpatient: Pre 6PM70.7-9.472.2-7.970.8-9.372.2-8.071.1-8.771.4-8.670.4-10.8

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Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 Change
Outpatient: 3.5 hr Postdose70.1-10.074.5-6.373.2-6.870.8-10.474.5-6.276.5-4.275.9-4.576.0-3.978.7-1.680.81.1

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Mean Observed and Change From Screening in Standing Diastolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 ObservedDay 12 ChangeDay 13 ObservedDay 13 ChangeDay 14 ObservedDay 14 Change
Outpatient: Predose75.7-4.574.8-5.574.1-6.177.1-3.374.6-5.878.4-1.876.9-3.278.1-1.780.00.383.64.584.85.5

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Mean Observed and Change From Screening in Standing Pulse (Bpm): Vital Signs

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

,,,,,,
Interventionbeats per minute (bpm) (Mean)
Day 1 ObservedDay 1 ChangeDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: 3.5 hr Post 1PM81.30.080.5-0.678.1-3.379.9-1.584.74.279.5-0.979.0-4.9
Inpatient: 3.5 hr Post 6PM78.9-2.578.0-3.376.4-5.078.2-2.779.5-1.280.90.475.1-8.6
Inpatient: 3.5 hr Post 8AM79.6-1.880.6-0.579.0-2.680.1-1.381.00.379.9-0.580.30.2
Inpatient: Pre 11PM79.4-1.878.4-3.078.3-3.280.4-0.280.6-0.180.90.474.3-9.7
Inpatient: Pre 1PM80.1-1.381.10.080.0-1.581.50.082.31.681.81.483.4-0.5
Inpatient: Pre 6PM81.2-0.180.8-0.479.1-2.380.8-0.780.2-0.481.51.080.0-3.6
Inpatient: Pre 8AM82.8NA82.41.081.1-0.281.2-0.283.12.481.71.484.53.5

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Mean Observed and Change From Screening in Standing Pulse (Bpm): Vital Signs

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

Interventionbeats per minute (bpm) (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 Observed0Day 12 ChangeDay 13 ObservedDay 13 Change
Outpatient: 3.5 hr Postdose83.32.180.8-1.784.81.676.9-4.380.7-2.982.8-1.185.11.682.0-0.180.0-1.481.41.1

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Mean Observed and Change From Screening in Standing Pulse (Bpm): Vital Signs

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

Interventionbeats per minute (bpm) (Mean)
Day 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 ChangeDay 8 ObservedDay 8 ChangeDay 9 ObservedDay 9 ChangeDay 10 ObservedDay 10 ChangeDay 11 ObservedDay 11 ChangeDay 12 Observed0Day 12 ChangeDay 13 ObservedDay 13 ChangeDay 14 ObservedDay 14 Change
Outpatient: Predose82.00.985.22.886.42.683.2-0.585.32.590.76.888.75.189.36.490.89.286.66.287.07.2

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Mean Observed and Change From Screening in Standing Systolic Blood Pressure (mmHg): Vital Sign

"Baseline vital signs were defined by the assessment value at screening when subjects were not experiencing opioid withdrawal to reduce the potential for variability from the effects of different states of withdrawal that may have been present before dosing on Day 1.~Overall screening values are captured in the column Inpatient: Pre 8AM; these values were recorded at various times for each participant during the screening visit, not necessarily at 8AM.~Serial vital sign assessments required for inpatient visits on days 1-3, either inpatient or outpatient for days 4-7, and outpatient only for days 8-14.~Day 14 only required pre-dose vital signs measurement. Day 1 Change, Pre 8AM was prior to the first dose." (NCT02363998)
Timeframe: Day 1 to Day 14

InterventionmmHg (Mean)
Day 1 ObservedDay 2 ObservedDay 2 ChangeDay 3 ObservedDay 3 ChangeDay 4 ObservedDay 4 ChangeDay 5 ObservedDay 5 ChangeDay 6 ObservedDay 6 ChangeDay 7 ObservedDay 7 Change
Inpatient: Pre 8AM120.4112.4-10.0111.2-11.4112.4-10.3111.3-11.1112.2-10.4113.9-8.7

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Visual Analog Scale

Pain, as measured by Visual Analog Scale (VAS). Scores are ranged from 0-10, 0 is no pain and 10 is worst possible pain. The unit of measure is units on a scale. (NCT02365961)
Timeframe: 3 Months

Interventionunits on a scale (Mean)
FI Block2.65
Local Injection2.50

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Total Number of Episodes of Nausea and Vomiting

Occurrences of periods of nausea and vomiting (NCT02365961)
Timeframe: From end of surgery to discharge from PACU

InterventionNumber of episodes (Number)
FI Block11
Local Injection7

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Time in PACU

Measured time subjects spent in the post anesthesia care unit. (NCT02365961)
Timeframe: Duration of PACU stay in minutes from end of surgery to discharge from PACA

InterventionMinutes (Mean)
FI Block150.04
Local Injection151.59

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Opioid Consumption

Opioid consumption, as measured by narcotic usage (morphine milligram equivalents) (NCT02365961)
Timeframe: 3 Months

Interventionmorphine milligram equivalents (Mean)
FI Block26.87
Local Injection30.32

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Hospital Readmission

Number of participants that were readmitted to the hospital (NCT02365961)
Timeframe: 3 months

InterventionParticipants (Count of Participants)
FI Block1
Local Injection2

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Duration of Sensory Block (Paresthesia)

The investigators hypothesize that rectus sheath injections with ropivacaine and clonidine result in longer duration of sensory block (paresthesia) compared to ropivacaine alone. (NCT02439281)
Timeframe: Indicated by return of normal sensation (expected average of 12 hours after block placement).

Interventionminutes (Median)
Ropivacaine/ Clonidine Group823.5
Ropivacaine Group540

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Complications Rate

The investigators expect no difference in incidence of complications (e.g. oversedation, hypotension, bradycardia episodes, etc.). (NCT02439281)
Timeframe: until study completion

InterventionParticipants (Count of Participants)
Ropivacaine/ Clonidine Group1
Ropivacaine Group1

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Change in Anxiety Scores

The investigators hypothesize that patient postoperative anxiety scores are lower in the Ropivacaine/Clonidine group and postoperative anxiety scores decrease more in Ropivacaine /Clonidine Group, than in Ropivacaine Group. (NCT02439281)
Timeframe: 6 hours after block placement

Interventionunits on a scale (Median)
Ropivacaine Group30
Ropivacaine/ Clonidine Group29

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Average Pain Severity at the Umbilicus Laparoscopic Site

Numeric Rating Pain Scores ( 0-10), will be obtained every 2 hours after PACU discharge up to 18 hours or until hospital discharge, whichever occurs first. The pain score of 0, means no pain, is a good outcome , and a pain score of 10 is excruciating pain, a very bad outcome. The average of these scores will be evaluated.The pain scores will not longer be documented after the numbness went away. (NCT02439281)
Timeframe: Logistic regression of the 4 th pain score assessment

Interventionunits on a scale (Median)
Ropivacaine Group2
Ropivacaine/ Clonidine Group1.5

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Satisfaction With Pain Control From Patient

The investigators hypothesize that rectus sheath injections with ropivacaine/ clonidine would result in better satisfaction with pain control. (NCT02439281)
Timeframe: Prior to hospital discharge (up to 24 hours after surgery)

Interventionunits on a scale (Median)
Ropivacaine/ Clonidine Group9
Ropivacaine Group9

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Duration of Analgesia at Umbilicus Instrument Site-How Many Minutes Passed From the Time When the Blocks Where Performed Until Patient Reported Pain at Umbilicus

The investigators hypothesize that rectus sheath injections with ropivacaine/ clonidine would result in longer duration of analgesia and decreased pain scores compared to ropivacaine alone. (NCT02439281)
Timeframe: indicated by the first request for pain medication at umbilicus site

Interventionminutes (Median)
Ropivacaine/ Clonidine Group230
Ropivacaine Group240

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Medication Consumption

Total intravenous morphine equivalents mg/kg (NCT02439281)
Timeframe: 18 hours after surgery

Interventionmg/kg (Median)
Ropivacaine/ Clonidine Group0.20
Ropivacaine Group0.22

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Quality of Recovery (QoR-15) Scores for Patient Reported Recovery Following Surgery

The Quality of Recovery questionnaire (QoR-15) is a 15 question patient reported outcome measure used to evaluate the quality of recovery following surgical anesthesia concerning pain, physical function, and psychological factors; reported as a summative score with each question graded between 0-10 (Range:0-150) with higher scores indicating improved physical/psychological recovery or infrequent symptoms (NCT02530151)
Timeframe: Preoperative to 24 hrs. post operatively

,
Interventionscore on a scale (Mean)
Preoperative QoR-15 ScoreChange in QoR-15 Score at 24 hrs. Post Op
Morphine With Clonidine123-22
Normal Saline131-20

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Visual Analog Scale (VAS) Pain Scores

Patients will rate their pain (0-10) on the Visual Analog Scale with higher scores for the VAS indicated elevated pain intensity reported by the patient for the indicated time point (NCT02530151)
Timeframe: Immediately preoperative (5-10 minutes before surgery), immediately postoperative (5-10 minutes after surgery), 1 hr post operatively

,
Interventionscore on a scale (Mean)
Preoperative VAS Pain ScoreImmediate Post Op VAS Pain Score1 hr. Post Op VAS Pain Score
Morphine With Clonidine234
Normal Saline245

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Opioid Consumption in the Acute Postoperative Period

The total usage of opioid medication (mEq) for pain relief in the intraoperative period and again through the postoperative recovery period from arrival in the PACU through 7 days post op (NCT02530151)
Timeframe: Recorded intraoperatively, during PACU stay, 6 hours post discharge, 18 hours post discharge, 24 hours post discharge, 48 hours post discharge, and at 7 days post discharge

,
Interventionmilligram morphine equivalents (mEq) (Mean)
IntraoperativePACU6 hours Post Discharge18 hours Post Discharge24 hours Post Discharge48 hours Post Discharge7 days Post Discharge
Morphine With Clonidine57.337.05.514.519.527.750.7
Normal Saline56.040.15.313.820.035.673.8

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Narcotic Consumption

Total amount of narcotics administered as calculated in oral morphine equivalent dose immediate post operatively up to 48 hours. (NCT02543801)
Timeframe: Starting immediately post operatively up to 48 hours

Interventionmorphine equivalents (Mean)
Hip Cohort Liposomal Bupivacaine48.8
Hip Cohort Ropivacaine57.4
Knee Cohort Liposomal Bupivacaine52.2
Knee Cohort Ropivacaine50.0

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Length of Stay

Measured in hours (NCT02543801)
Timeframe: Start of surgery to hospital discharge up to 140 hours

InterventionHours (Mean)
Hip Cohort Liposomal Bupivacaine33.8
Hip Cohort Ropivacaine50.3
Knee Cohort Liposomal Bupivacaine36.0
Knee Cohort Ropivacaine38.4

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Pain Score

"Self-reported pain score 0-10 (0=no pain - 10=worst possible pain experienced) and higher scores indicate a worse outcome~Pain scores, collected every 4 hours per hospital care standards, were averaged (post-operatively up to 48 hours) to obtain individual mean pain scores and a mean score for the group was then calculated." (NCT02543801)
Timeframe: Starting post operatively and then every four hours up to 48 hours

Interventionscore on a scale (Mean)
Hip Cohort Liposomal Bupivacaine3.78
Hip Cohort Ropivacaine3.85
Knee Cohort Liposomal Bupivacaine3.3
Knee Cohort Ropivacaine3.4

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Detox Phase Completers

% of enrolled participants who completed the Detox Phase (NCT02543944)
Timeframe: 3 weeks (week 1-3)

InterventionParticipants (Count of Participants)
Gabapentin41
Placebo34

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Vivitrol Injection Receivers

% of participants starting the NTX transition who received Vivitrol injection (NCT02543944)
Timeframe: 5 days (week 4 day 1 to week 4 day 5)

InterventionParticipants (Count of Participants)
Gabapentin12
Placebo12

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NTX Transition Initiation

% of Participants who completed the detox and started the NTX transition (NCT02543944)
Timeframe: 3 days (wk 4 day 1 - week 4 day 3)

InterventionParticipants (Count of Participants)
Gabapentin33
Placebo29

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Detoxification Phase: Changes in Percent of Illicit Opioid-positive Urine Samples Over Time

Thrice weekly urine samples obtained during weeks 1-3; data include assessments from week 1 day 1 through week 4 day 1 (up to 10 total samples per participant) (NCT02543944)
Timeframe: Week 1 day 1 (study entry) through Week 4 day 1 (first day of NTX transition)

Interventionpercentage of urine positive samples (Mean)
Gabapentin35.0
Placebo41.6

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Narcotic Use During Hospitalization

The amount of narcotic pain medication needed for patient to be comfortable. This is measured in morphine equivalents since there are many pain medications other than morphine. (NCT02570503)
Timeframe: 0-24 hours post surgery period, 24 - 48 hours post surgery period, and Full 48 hours post surgery period

,
Interventionmg morphine equivalents (Mean)
0 to 24 hour post surgery period24 to 48 hour post surgery periodFull 48 hour post surgery period
Placebo72.372.8145.7
ROP/KET/CLON/EPI/SAL58.966.5125.6

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Percent of Incontinent Bowel Movements to be Semi-Formed Stools During Treatment

The percentage of incontinent bowel movements where the Bristol stool score was 5, 6 or 7. (5=soft blobs; 6=mushy, fluffy pieces; 7= watery, no solid pieces) during treatment, per self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

Interventionpercent of semi-formed stools (Mean)
Placebo67
Colesevelam and Clonidine61

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Number of Participants to Report a 50% or Greater Reduction in Weekly Fecal Incontinence (FI) Episodes

The number of participants that report a 50% or greater reduction in weekly incontinent episodes as measured by self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

InterventionParticipants (Count of Participants)
Placebo17
Colesevelam and Clonidine13

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Number of Semi-Formed Stools Per Week

The number of stools per week measured by self-reported bowel diaries where the Bristol stool score was 5, 6, or 7. (5=soft blobs; 6=mushy, fluffy pieces; 7= watery, no solid pieces) (NCT02628626)
Timeframe: 4 weeks

Interventionnumber of stools per week (Mean)
Placebo1.0
Colesevelam and Clonidine1.2

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Percent of Incontinent Bowel Movements During Treatment

The percentage of bowel movements that were incontinent during treatment, per self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

Interventionpercent of incontinent bowel movements (Mean)
Placebo27
Colesevelam and Clonidine28

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Total Fecal Incontinence Episodes

The total number of fecal incontinence episodes per week as measured by self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

Interventionincontinence episodes per week (Mean)
Placebo4.2
Colesevelam and Clonidine4.8

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Daily Stool Frequency

The number of bowel movements daily measured by self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

Interventionbowel movements per day (Mean)
Placebo2.4
Colesevelam and Clonidine2.1

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Delay of Bowel Movement

The time in minutes a bowel movement can be delayed after sense of urgency to defecate as measured by self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

Interventionminutes (Mean)
Placebo2.8
Colesevelam and Clonidine3.6

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Loperamide Tablets Per Week

The number of tablets of loperamide used, per self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

Interventiontablets per week (Mean)
Placebo1.9
Colesevelam and Clonidine6

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Stool Consistency

Stool consistency as measured by self-reported bowel diaries. Expressed in terms of the Bristol Stool Form Scale, where: 1= separate hard lumps; 2= lumpy sausage-shape; 3= cracked sausage; 4= smooth and soft sausage; 5=soft blobs; 6=mushy, fluffy pieces; 7= watery, no solid pieces. (NCT02628626)
Timeframe: 4 weeks

Interventionscore on a scale (Mean)
Placebo4.1
Colesevelam and Clonidine3.2

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Severity of Fecal Incontinence

Measured by the Fecal Incontinence Severity Index (FISI). It is a validated 4-item scale used to assess the frequency (never, 1-3 times a month, once a week, 2 or more times per week but not daily, once a day, 2 or more times per day) of 4 different types of FI (gas, mucus, liquid stool, solid stool). Each of the four types of FI is awarded a number of points, depending on the frequency at which that type of incontinence is experienced. The points are totaled and the scores can range from 0 to 61, where the higher the score, the higher the perceived severity of the fecal incontinence. (NCT02628626)
Timeframe: 4 weeks

Interventionscore on a scale (Mean)
Placebo28
Colesevelam and Clonidine22

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Severity of Bowel Symptoms

The Fecal Incontinence Symptom Severity (FISS) score is based on five questions; (1) the frequency of FI; (2) the type of FI (stool only, liquid or mucus only, both liquid/mucus and stool, or gas only); (3) the amount of stool leaked (small, moderate, or large); (4) the frequency of having to rush to the toilet; and (5) the frequency of having stool leak without warning. Questions 4 & 5 are merged to determine if the participant has passive FI (FI without warning), urge FI, both, or neither. The responses to the questions are assigned physician-derived weights and added together for a total score of 4 to 13. The higher the score the more severe the FI symptoms. (NCT02628626)
Timeframe: 4 weeks

Interventionscore on a scale (Mean)
Placebo6
Colesevelam and Clonidine4.6

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Percent of Incontinent Bowel Movements to be Semi-Formed Stools Pre-Treatment

The percentage of incontinent bowel movements where the Bristol stool score was 5, 6 or 7. (5=soft blobs; 6=mushy, fluffy pieces; 7= watery, no solid pieces), pre-treatment, per self-reported bowel diaries. (NCT02628626)
Timeframe: baseline

Interventionpercent of semi-formed stools (Mean)
Placebo61
Colesevelam and Clonidine76

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Percent of Incontinent Bowel Movements Pre-treatment

The percentage of bowel movements that were incontinent prior to treatment initiation, per self-reported bowel diaries. (NCT02628626)
Timeframe: baseline

Interventionpercent of incontinent bowel movements (Mean)
Placebo45
Colesevelam and Clonidine40

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Volume of Fecal Incontinence

The volume of fecal incontinence measured as the number of incontinent episodes per week as categorized by small (staining only), moderate (requiring change of underwear) or large (requiring change of all clothes) in self-reported bowel diaries. (NCT02628626)
Timeframe: 4 weeks

,
Interventionincontinent episodes per week (Mean)
Small (staining only)Moderate (requires change of underwear)Large (requires complete change of clothes
Colesevelam and Clonidine3.32.02.4
Placebo2.40.91.3

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Fecal Incontinence Quality of Life (FI-QoL)

The Fecal Incontinence Quality of Life questionnaire measures specific quality of life issues expected to affect patients with fecal incontinence. The questions are grouped into four categories: lifestyle (10 questions), coping (9 questions), depression (7 questions), and embarrassment (3 questions). Each category is scored from 1 to 4. The scale scores are calculated by adding the numerical values of all responses in that specific scale and then dividing by its number of items. Higher scores indicate a better quality of life. (NCT02628626)
Timeframe: 4 weeks

,
Interventionscore on a scale (Mean)
Lifestyle scoreCoping scoreDepression ScoreEmbarrassment score
Colesevelam and Clonidine2.72.13.12.5
Placebo2.72.03.12.6

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Change From Baseline to Day 84 (Week 12) in Numeric Pain Rating Scale Score

"The Numeric Pain Rating Scale is a single reading that measures the patients interpretation of their pain on a scale from 0, no pain to 10, worst pain imaginable. The change from baseline can range from -10 to 10. The change from Baseline (averaged over Day -14 to Day -8) to End-of-Treatment (averaged over Days 78 to 84 [±3 days]) in the Numeric Pain Rating Scale score assessing the average pain in the past 24 hours in the painful areas of the feet averaged over Days 78 to 84 compared to the 7 days at the Baseline Phase (Days -14 to -8). For the primary efficacy endpoint, the mean change in pain intensity from Baseline to Week 12 was analyzed using an analysis of covariance (ANCOVA) model with the Baseline pain intensity score serving as a covariate. The statistical model also included treatment, site, site by treatment interaction, and strata. If the site by treatment interaction term was not significant at the 0.1 level, then it was excluded from the model." (NCT02643251)
Timeframe: The change from Baseline (averaged over Day -14 to Day -8) to End-of-Treatment (averaged over Days 78 to 84 [±3 days])

Interventionunits on a scale (Mean)
Clonidine Hydrochloride Topical Gel, 0.1%-1.2
Clonidine Hydrochloride Gel Comparator-1.4

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Mean Daily Worst Pain Intensity Numeric Pain Rating Scale Scores

"The Numeric Pain Rating Scale is a single reading that measures the patients interpretation of their pain on a scale from 0, no pain to 10, worst pain imaginable. The change from baseline can range from -10 to 10. The change from Baseline (worse score from Day -14 to Day -8) to End-of-Treatment (worse score during Days 78 to 84 [±3 days]) in the Numeric Pain Rating Scale score assessing the worse pain in the past 24 hours in the painful areas of the feet from Days 78 to 84 compared to the 7 days at the Baseline Phase (Days -14 to -8). For the primary efficacy endpoint, the mean change in pain intensity from Baseline to Week 12 was analyzed using an analysis of covariance (ANCOVA) model with the Baseline pain intensity score serving as a covariate. The statistical model also included treatment, site, site by treatment interaction, and strata. If the site by treatment interaction term was not significant at the 0.1 level, then it was excluded from the model." (NCT02643251)
Timeframe: The change from Baseline (worse over Day -14 to Day -8) to End-of-Treatment (worse over Days 78 to 84 [±3 days])

Interventionunits on a scale (Mean)
Clonidine Hydrochloride Topical Gel, 0.1%-1.29
Clonidine Hydrochloride Gel Comparator-1.48

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Clinical Opiate Withdrawal Scale Score at the Time of Disposition

"Opiate withdrawal scale score for all patients who received medication by one hour~The Clinical Opiate Withdrawal Scale (COWS) is an 11-item scale, ranging from 0 to 48 (5- 12 = mild; 13-24 = moderate; 25-36 = moderately severe; more than 36 = severe withdrawal).~This tool can be used to reproducibly rate common signs and symptoms of opiate withdrawal and monitor these symptoms over time. The summed score for the complete scale can be used to help clinicians determine the stage or severity of opiate withdrawal and assess the level of physical dependence on opioids. The 11 items on the scale include scores rate the following symptoms: pulse rate, GI upset, sweating, tremor, restlessness, yawning, pupil size, anxiety, bone or joint aches, gooseflesh skin, runny nose." (NCT02643355)
Timeframe: Time of Disposition (on average within 6 hours)

Interventionunits on a scale (Mean)
Olanzapine4.3
Clonidine3.6

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Clinical Opiate Withdrawal Scale Score at 1 Hour Post Medication

"Opiate withdrawal scale score for all patients who received medication by one hour~The Clinical Opiate Withdrawal Scale (COWS) is an 11-item scale, ranging from 0 to 48 (5- 12 = mild; 13-24 = moderate; 25-36 = moderately severe; more than 36 = severe withdrawal).~This tool can be used to reproducibly rate common signs and symptoms of opiate withdrawal and monitor these symptoms over time. The summed score for the complete scale can be used to help clinicians determine the stage or severity of opiate withdrawal and assess the level of physical dependence on opioids. The 11 items on the scale include scores rate the following symptoms: pulse rate, GI upset, sweating, tremor, restlessness, yawning, pupil size, anxiety, bone or joint aches, gooseflesh skin, runny nose." (NCT02643355)
Timeframe: At 1 hour

Interventionunits on a scale (Mean)
Olanzapine5.3
Clonidine6.7

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Clinical Opiate Withdrawal Scale Score at 2 Hours Post Medication

"Opiate withdrawal scale score for all patients who received medication by one hour~The Clinical Opiate Withdrawal Scale (COWS) is an 11-item scale, ranging from 0 to 48 (5- 12 = mild; 13-24 = moderate; 25-36 = moderately severe; more than 36 = severe withdrawal).~This tool can be used to reproducibly rate common signs and symptoms of opiate withdrawal and monitor these symptoms over time. The summed score for the complete scale can be used to help clinicians determine the stage or severity of opiate withdrawal and assess the level of physical dependence on opioids. The 11 items on the scale include scores rate the following symptoms: pulse rate, GI upset, sweating, tremor, restlessness, yawning, pupil size, anxiety, bone or joint aches, gooseflesh skin, runny nose." (NCT02643355)
Timeframe: 2 hours

Interventionunits on a scale (Mean)
Olanzapine4.8
Clonidine3.7

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Number of Participants That Received Rescue Medication for Withdrawal Symptoms Within 1 Hour

Rescue Medication (additional medications given for symptoms) within 1 hour of medication administration (NCT02643355)
Timeframe: 1 Hour

InterventionParticipants (Count of Participants)
Olanzapine9
Clonidine19

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Intraocular Pressure (IOP)

(NCT02733757)
Timeframe: Within 10 minutes before the surgery procedure

InterventionmmHg (Mean)
Sub-Tenon's Group Control18
Sub-Tenon's Group Clonidine16
Peribulbar Group Control19
Peribulbar Group Clonidine16

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Post-operative Pain the First 24hrs

To determine whether the use of a CNB in patients undergoing penile prosthesis surgery results in decreased immediate postoperative pain in the first 24 hours after surgery compared with patients having only general anesthesia as determined by postop pain score. The mean, median and max pain will be assessed using the numeric rating scale (NRS). The NRS is scored by numeric integers, 0 through 10. The NRS will be used verbally. Numerical Rating Scale (NRS), patients are asked to circle the number between 0 and 10 that fits best to their pain intensity. Zero usually represents 'no pain at all' whereas the upper limit represents 'the worst pain ever possible' (NCT02740127)
Timeframe: 24 hours

,
Interventionscore on a scale (Mean)
Min Pain within 24hrsMedian Pain within 24 hrsMax Pain within 24 hrs
General Anesthesia and Caudal Nerve Block1.16673.08336.125
General Anesthesia Only0.92863.71436.7857

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Post-Operative Pain Medication Usage in Post Anesthesia Care Unit (PACU)

Pain evaluated by the amount of intravenous and oral pain medicine administered in the first 24 hours post-operatively. Pain assessed using the numeric rating scale (NRS). The NRS is scored by numeric integers, 0 through 10, where 0 is no pain and 10 is the worst pain. (NCT02740127)
Timeframe: 24 hours

Interventionmg (Mean)
General Anesthesia and Caudal Nerve Block13.0208
General Anesthesia Only15.1786

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Length of Hospital Stay

To determine whether the use of a CNB in patients undergoing penile prosthesis surgery results in a decreased length of hospital stay compared with patients having only general anesthesia. (NCT02740127)
Timeframe: 32 Hours

InterventionHours (Mean)
General Anesthesia and Caudal Nerve Block24.8424
General Anesthesia Only24.9506

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Post-operative Axillary Pain

Post-operative ambulatory surgery subjects will be asked 6 hours after block placement about the presence of axillary pain at rest. Numerical Rating Scale scores (0-10) will be recorded with 0= no pain, 10=most pain possible. Higher scores denotes worse outcome. (NCT02741713)
Timeframe: 6 hours post-block.

Interventionunits on a scale (Median)
Interscalene Block Plus Sham Block3
Interscalene Plus PECS Blocks0

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Time From Block Placement to Onset of Axillary Pain

Time self-reported by patients in the Interscalene Plus PECS Blocks group during data collection phone call at 24 hours post-block. (NCT02741713)
Timeframe: Assessed 24hrs post-block in hours

InterventionHours (Mean)
Interscalene Plus PECS Blocks16.7

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Total Opioid Usage

Recorded in oxycodone equivalents in the first 24 hours post-discharge from the PACU. (NCT02741713)
Timeframe: Assessed 24hrs post-block in mg

Interventionmg (Mean)
Interscalene Block Plus Sham Block31.6
Interscalene Plus PECS Blocks26.9

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Numerical Rating Scale Pain Scores (0-10) at Rest

Subjects were asked about their overall shoulder pain during the followup phone call at 24hrs post-block. Numerical Rating Scale scores (0-10) will be recorded with 0= no pain, 10=most pain possible. Higher scores denotes worse outcome. (NCT02741713)
Timeframe: Assessed 24hrs post-block on a scale from 0-10.

Interventionunits on a scale (Median)
Interscalene Block Plus Sham Block6
Interscalene Plus PECS Blocks6

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Percentage of Participants With Episodes of Nausea or Vomiting

Any episodes during the first 24 hours will be recorded as a yes. (NCT02741713)
Timeframe: Assessed 24hrs post-block (yes/no)

Interventionpercentage of participants (Number)
Interscalene Block Plus Sham Block39
Interscalene Plus PECS Blocks37

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Performed-based Physical Function is Assessed Using the Repeated Chair Stand Test.

"The Repeated Chair Stand Test is a timed test based on the ability of the participant to perform a series of standing exercises.~This test is germane to subjects with total joint replacement that are easily performed in the clinical settings. The test will capture the domains of muscle strength and activation, and balance." (NCT02891798)
Timeframe: 6 weeks post-operation

Interventionseconds (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)12.34
Bupivacaine Only (Control Arm)11.93

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Performed-based Physical Function is Assessed Using the Self-Selected Gait Speed Test.

"The Self-Selected Gait Speed Test is a timed test based on the ability of the participant to walk a 4 meter distance.~This test is germane to subjects with total joint replacement that are easily performed in the clinical settings. The test captures the ability to walk." (NCT02891798)
Timeframe: 6 weeks post-operation

Interventionmeters per second (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)0.88
Bupivacaine Only (Control Arm)0.94

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Performed-based Physical Function is Assessed Using the Standing Balance Test.

"The Standing Balance Test score based on the ability of the participant to perform a series of standing exercises. Scores range from 0 to 4, with 4 indicating a longer time holding the stand (a better outcome).~This test is germane to subjects with total joint replacement that are easily performed in the clinical settings. The test will capture the domains of muscle strength and activation, and balance." (NCT02891798)
Timeframe: 6 weeks post-operation

Interventionscore on a scale (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)3.86
Bupivacaine Only (Control Arm)3.94

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SF-MPQ2 Continuous Pain Subscore Difference From Baseline

Continuous pain subscore difference of Post-Operative Day 1 value minus the Baseline value. Differences can range from -10 to +10. Negative scores indicate a decrease in pain. (NCT02891798)
Timeframe: Baseline, Post-Operative day after surgery (7AM-9AM EST)

Interventionunits on a scale (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)-2.29
Bupivacaine Only (Control Arm)0.33

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Quality of Recovery 15 Item Scale (QoR-15) Total Score

Quality of Recovery 15 Item Scale, total score 0-150, 150 reflecting a perfect score and better recovery. (NCT02891798)
Timeframe: 6 weeks post-operation

Interventionscore on a scale (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)128.89
Bupivacaine Only (Control Arm)130.06

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Short-Form McGill Pain Questionnaire (Version 2) Total Score Difference From Baseline

SF-MPQ version 2 total score difference of Post-Operative Day 1 value minus the Baseline value. Differences can range from -10 to +10. Negative scores indicate a decrease in pain. (NCT02891798)
Timeframe: Baseline, Post-Operative day after surgery (7AM-9AM EST)

Interventionscore on a scale (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)-1.85
Bupivacaine Only (Control Arm)-0.05

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SF-MPQ2 Intermittent Pain Subscore Difference From Baseline

Intermittent pain subscore difference of Post-Operative Day 1 value minus the Baseline value. Differences can range from -10 to +10. Negative scores indicate a decrease in pain. (NCT02891798)
Timeframe: Baseline, Post-Operative day after surgery (7AM-9AM EST)

Interventionunits on a scale (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)-2.79
Bupivacaine Only (Control Arm)-1.14

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Quality of Recovery 15 Item Scale (QoR-15) Total Score

Quality of Recovery 15 Item Scale, total score 0-150, 150 reflecting a perfect score and better recovery. (NCT02891798)
Timeframe: Day after surgery (7AM-9AM EST)

Interventionscore on a scale (Mean)
Bupivacaine + BCD (Buprenorphine, Clonidine, Dexamethasone)106.08
Bupivacaine Only (Control Arm)90.13

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Total Opioid Consumption

Total opioids consumed during the first 24hrs post operatively. Measured as 24hr Oxycodone Equivalent (NCT03007966)
Timeframe: 24 hrs Post Nerve Block

Interventionmilligrams (Mean)
Ilioinguinal / Iliohypogastric Block19.7
Quadratus Lumborum Block25.2

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Time to First Oral Analgesic

When does the patient require their first post operative analgesic dose? (NCT03007966)
Timeframe: 24hrs Post Nerve Block

Interventionminutes (Median)
Ilioinguinal / Iliohypogastric Block141
Quadratus Lumborum Block91

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Post-operative Verbal Pain Score With Movement

Assessed on an 11-point (0-10) numeric analog scale with a higher score denoting a worse outcome. (NCT03007966)
Timeframe: 8 hrs Post Nerve Block

Interventionscore on a scale (Mean)
Ilioinguinal / Iliohypogastric Block5.10
Quadratus Lumborum Block5.03

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Post-operative Verbal Pain Score With Activity

Assessed on an 11 point (0-10) numeric analog scale with a higher score denoting a worse outcome (NCT03007966)
Timeframe: 24hrs Post Nerve Block

Interventionscore on a scale (Mean)
Ilioinguinal / Iliohypogastric Block4.9
Quadratus Lumborum Block5.3

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Post-operative Verbal Pain Score at Rest

Assessed on an 11-point (0-10) numeric analog scale with a higher score denoting a worse outcome (NCT03007966)
Timeframe: 8 hrs Post Nerve Block

Interventionscore on a scale (Mean)
Ilioinguinal / Iliohypogastric Block3.6
Quadratus Lumborum Block3.3

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Post-operative Verbal Pain Score at Rest

Assessed on an 11 point (0-10) numeric analog scale with a higher score denoting a worse outcome (NCT03007966)
Timeframe: 24 hrs Post Nerve Block

Interventionscore on a scale (Mean)
Ilioinguinal / Iliohypogastric Block3
Quadratus Lumborum Block2.7

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Number of Patients Reporting Nausea at Home

Patients are called 1-3 days post-operatively to assess if they had any side effects of the adjuvants such as nausea, vomiting or itching. There blood pressure is looked at pre-op and compared to post-op. Any prolonged PACU (Post Anesthesia Care Unit) stay for sedation is recorded. (NCT03117140)
Timeframe: 1-3 days

InterventionParticipants (Count of Participants)
Plain Ropivacaine4
Ropivacaine + Buprenorphine9
Ropivacaine + Clonidine2
Ropivacaine + Dexamethasone3

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Number of Patients Reporting Itching in the PACU

Patients itching was assessed post-op in the PACU. (NCT03117140)
Timeframe: Post-op day 0 (baseline)

InterventionParticipants (Count of Participants)
Plain Ropivacaine5
Ropivacaine + Buprenorphine2
Ropivacaine + Clonidine6
Ropivacaine + Dexamethasone3

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Number of Patients Reporting Itching at Home

Patients are called 1-3 days post-operatively to assess if they had any side effects of the adjuvants such as nausea, vomiting or itching. There blood pressure is looked at pre-op and compared to post-op. Any prolonged PACU (Post Anesthesia Care Unit) stay for sedation is recorded. (NCT03117140)
Timeframe: 1-3 days

InterventionParticipants (Count of Participants)
Plain Ropivacaine1
Ropivacaine + Buprenorphine2
Ropivacaine + Clonidine2
Ropivacaine + Dexamethasone0

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Motor Duration of Block

Patients are called 1-3 days post-operatively to assess when motor component of their nerve block wore off (NCT03117140)
Timeframe: Day 1-3

Interventionminutes (Median)
Plain Ropivacaine1120
Ropivacaine + Buprenorphine1198
Ropivacaine + Clonidine1090
Ropivacaine + Dexamethasone1143.5

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Number of Patient With Blood Pressure Changes in the Second Stage Recovery Area

Blood pressure changes in Second Stage Recovery Area for patients was looked at (NCT03117140)
Timeframe: Post-op Day 0 (baseline)

InterventionParticipants (Count of Participants)
Plain Ropivacaine5
Ropivacaine + Buprenorphine1
Ropivacaine + Clonidine5
Ropivacaine + Dexamethasone0

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Number of Patients Reporting Nausea in the PACU

PACU (Post-Anesthesia Care Unit) assessment of nausea (NCT03117140)
Timeframe: Post-op day 0 (Baseline)

InterventionParticipants (Count of Participants)
Plain Ropivacaine4
Ropivacaine + Buprenorphine9
Ropivacaine + Clonidine2
Ropivacaine + Dexamethasone9

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Number of Patients Vomiting in the PACU (Post-Anesthesia Care Unit)

Vomiting in PACU (Post-Anesthesia Care Unit) for patients was looked at (NCT03117140)
Timeframe: Post-op Day 0 (Baseline)

InterventionParticipants (Count of Participants)
Plain Ropivacaine0
Ropivacaine + Buprenorphine1
Ropivacaine + Clonidine0
Ropivacaine + Dexamethasone0

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Pain Score Reported by Patients at First Phone Call

Patients are called 1-3 days post-operatively to assess pain. Pain score is 0-10 scale with 0 is no pain and 10 is most severe pain. (NCT03117140)
Timeframe: Day 1-3

Interventionunits on a scale (Median)
Plain Ropivacaine4
Ropivacaine + Buprenorphine3
Ropivacaine + Clonidine4
Ropivacaine + Dexamethasone3

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Patient Reporting Vomiting at Home

Patients are called 1-3 days post-operatively to assess if they had any side effects of the adjuvants such as nausea, vomiting or itching. There blood pressure is looked at pre-op and compared to post-op. Any prolonged PACU (Post Anesthesia Care Unit) stay for sedation is recorded. (NCT03117140)
Timeframe: 1-3 days

InterventionParticipants (Count of Participants)
Plain Ropivacaine0
Ropivacaine + Buprenorphine3
Ropivacaine + Clonidine2
Ropivacaine + Dexamethasone1

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Sensory Duration of Block

Patients are called 1-3 days post-operatively to assess when the sensory component of their nerve block wore off (NCT03117140)
Timeframe: Day 1-3

Interventionminutes (Median)
Plain Ropivacaine923.5
Ropivacaine + Buprenorphine982
Ropivacaine + Clonidine940.5
Ropivacaine + Dexamethasone1066

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Duration of Analgesia

Patients are called 1-3 days post-operatively to assess when the analgesia of their nerve block wore off (NCT03117140)
Timeframe: 1-3 days post-operative

Interventionminutes (Median)
Plain Ropivacaine911
Ropivacaine + Buprenorphine1026.5
Ropivacaine + Clonidine1181
Ropivacaine + Dexamethasone982

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Surgical Length

Surgical length was recorded (NCT03117140)
Timeframe: Post op Day 0 (Baseline)

Interventionminutes (Median)
Plain Ropivacaine68.5
Ropivacaine + Buprenorphine65
Ropivacaine + Clonidine73.5
Ropivacaine + Dexamethasone71

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Surgical Position

Surgical position was recorded (NCT03117140)
Timeframe: Post-op Day 0 (Baseline)

,,,
InterventionParticipants (Count of Participants)
Beach ChairLateralSupine
Plain Ropivacaine3820
Ropivacaine + Buprenorphine3163
Ropivacaine + Clonidine3172
Ropivacaine + Dexamethasone3262

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Number of Patients With Blood Pressure (BP) Changes in the PACU

Blood pressure changes in PACU (Post-Anesthesia Care Unit) for patients was looked at (NCT03117140)
Timeframe: Post-op Day 0 (baseline)

InterventionParticipants (Count of Participants)
Plain Ropivacaine8
Ropivacaine + Buprenorphine3
Ropivacaine + Clonidine7
Ropivacaine + Dexamethasone2

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Block Set up Time

Patients are assessed from needle removal to when they are no longer able to feel cold on the blocked extremity (NCT03117140)
Timeframe: Day one

Interventionminutes (Median)
Plain Ropivacaine6
Ropivacaine + Buprenorphine3
Ropivacaine + Clonidine6
Ropivacaine + Dexamethasone4.5

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Readmission Rate

Number of patients readmitted to the hospital within 30 days of hospital discharge or discontinuation of phenobarbital. (NCT03670160)
Timeframe: From date of randomization until 30 days after hospital discharge or discontinuation of phenobarbital, up to 6 months

InterventionParticipants (Count of Participants)
Phenobarbital0
Clonidine0

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Number of Patients Requiring Triple Therapy

Number of patients requiring a third agent to control withdrawal symptoms (NCT03670160)
Timeframe: From date of randomization until hospital discharge, up to 4 months

Interventionparticipants (Number)
Phenobarbital4
Clonidine10

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Time From Initiation of Adjunctive Therapy Until Hospital Discharge

Number of days from initiation of adjunctive therapy until hospital discharge (NCT03670160)
Timeframe: From date of randomization until hospital discharge, up to 4 months

InterventionDays (Mean)
Phenobarbital20
Clonidine33.8

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Length of Stay

Number of days of hospital admission (NCT03670160)
Timeframe: From date of randomization until hospital discharge, up to 4 months

InterventionDays (Mean)
Phenobarbital31
Clonidine41.78

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Length of Oral Morphine Sulfate Therapy

Number of days of oral morphine sulfate therapy (NCT03670160)
Timeframe: From date of randomization until hospital discharge, up to 4 months

InterventionDays (Mean)
Phenobarbital25.45
Clonidine34.36

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Narcotics Use as Assessed by Morphine Equivalents Consumed

morphine equivalents consumed during the entire post-anesthesia care unit (PACU) visit post surgery will be obtained from the All-scripts electronic medical record (EMR) system. (NCT03704376)
Timeframe: Entire post-anesthesia care unit (PACU) visit post surgery, PACU range 1 hr to 12 hrs post surgery

Interventionmilligrams (mg) (Mean)
Femoral Nerve Blockade14.8
Adductor Canal Blockade16.0

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 4 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.83
Adductor Canal Blockade2.87

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 5 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.97
Adductor Canal Blockade3.06

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 7 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.83
Adductor Canal Blockade2.81

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 8 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.84
Adductor Canal Blockade2.57

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 9 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.91
Adductor Canal Blockade2.41

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 10 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2
Adductor Canal Blockade2.53

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better (NCT03704376)
Timeframe: 3 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.65
Adductor Canal Blockade3.23

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, 0 being the better outcome. (NCT03704376)
Timeframe: 1 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade0.81
Adductor Canal Blockade0.8

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Number of Successful Repetitions With Straight Leg Raise Test

The straight leg raise assessment was performed in a standardized long-sitting position with well-knee flexed to 90 degrees. Patients were asked to complete 30 repetitions of straight leg raises with a small bolster supporting the heel using the following criteria; (1) perform with no visible quad lag (2) reach the height of the opposite tibial tubercle and (3) maintain a controlled rate of 30 hertz for the ascending and descending phases. The examination was only performed on the surgical limb and the absolute number of successful repetitions is reported. (NCT03704376)
Timeframe: Post-operative day 14

Interventionnumber of repetitions (Mean)
Femoral Nerve Blockade23.3
Adductor Canal Blockade24.2

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Number of Successful Repetitions With Straight Leg Raise Test

The straight leg raise assessment was performed in a standardized long-sitting position with well-knee flexed to 90 degrees. Patients were asked to complete 30 repetitions of straight leg raises with a small bolster supporting the heel using the following criteria; (1) perform with no visible quad lag (2) reach the height of the opposite tibial tubercle and (3) maintain a controlled rate of 30 hertz for the ascending and descending phases. The examination was only performed on the surgical limb and the absolute number of successful repetitions is reported. (NCT03704376)
Timeframe: Post-operative day 1

Interventionnumber of repetitions (Mean)
Femoral Nerve Blockade3.2
Adductor Canal Blockade6.2

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 6 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade2.63
Adductor Canal Blockade3.03

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Quadriceps Muscle Activation as Assessed by Surface Electromyography (sEMG)

Quadriceps muscle activation was examined using surface electromyography (sEMG) of the vastus medialis oblique muscle. Peak sEMG activity was recorded in microvolts (uV) on the surgical and contralateral limbs while performing five maximal effort isometric contractions in full knee extension--the reported values are equal to the quadriceps sEMG in uV of the contralateral limb minus the quadriceps sEMG in uV of the surgical limb. (NCT03704376)
Timeframe: Post-operative day 1

Interventionmicrovolts (uV) (Mean)
Femoral Nerve Blockade266.5
Adductor Canal Blockade212.5

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Quadriceps Muscle Activation as Assessed by Surface Electromyography (EMG)

Quadriceps muscle activation was examined using surface electromyography (sEMG) of the vastus medialis oblique muscle. Peak sEMG activity was recorded in microvolts (uV) on the surgical and contralateral limbs while performing five maximal effort isometric contractions in full knee extension--the reported values are equal to the quadriceps sEMG in uV of the contralateral limb minus the quadriceps sEMG in uV of the surgical limb. (NCT03704376)
Timeframe: Post-operative day 14

Interventionmicrovolts (uV) (Mean)
Femoral Nerve Blockade183.2
Adductor Canal Blockade126.5

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Quadriceps Muscle Activation as Assessed by Surface Electromyography (EMG)

Quadriceps muscle activation was examined using surface electromyography (sEMG) of the vastus medialis oblique muscle. Peak sEMG activity was recorded in microvolts (uV) on the surgical and contralateral limbs while performing five maximal effort isometric contractions in full knee extension--the reported values are equal to the quadriceps sEMG in uV of the contralateral limb minus the quadriceps sEMG in uV of the surgical limb. (NCT03704376)
Timeframe: 4 weeks post operative

Interventionmicrovolts (uV) (Mean)
Femoral Nerve Blockade109.1
Adductor Canal Blockade94.1

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Number of Successful Repetitions With Straight Leg Raise Test

The straight leg raise assessment was performed in a standardized long-sitting position with well-knee flexed to 90 degrees. Patients were asked to complete 30 repetitions of straight leg raises with a small bolster supporting the heel using the following criteria; (1) perform with no visible quad lag (2) reach the height of the opposite tibial tubercle and (3) maintain a controlled rate of 30 hertz for the ascending and descending phases. The examination was only performed on the surgical limb and the absolute number of successful repetitions is reported. (NCT03704376)
Timeframe: 4 weeks post operative

Interventionnumber of repetitions (Mean)
Femoral Nerve Blockade29.7
Adductor Canal Blockade30

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Postoperative Pain Control as Assessed by a Numeric Pain Rating Scale

The items are scored on a visual analogical scale from 0-10, with 0 being the better outcome. (NCT03704376)
Timeframe: 2 hr post surgery

Interventionunits on a scale (Mean)
Femoral Nerve Blockade1.78
Adductor Canal Blockade2.13

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Average Daily Dose of Oral Morphine Over Hospital Stay

The average daily dose of morphine used throughout study period in mg/kg/day (NCT03762317)
Timeframe: From beginning of morphine therapy during NICU admission until discharge from the hospital, up to 100 days

Interventionmg/kg/day (Mean)
Clonidine0.4
Placebo0.4

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Duration of Hospital Stay

Number of days spent in the hospital (NCT03762317)
Timeframe: From beginning of morphine therapy during NICU admission until discharge from the hospital, up to 100 days

Interventiondays (Mean)
Clonidine32.4
Placebo31.6

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Duration of Pharmacotherapy for NAS

The length of time in days from the initiation of pharmacotherapy on day 1 until the medication has been stopped (NCT03762317)
Timeframe: From beginning of morphine therapy during NICU admission until discharge from the hospital, up to 100 days

Interventiondays (Mean)
Clonidine30.2
Placebo25.6

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Maximum Dose of Morphine Used

The maximum dose of morphine in mg/kg used for symptom control (NCT03762317)
Timeframe: From beginning of morphine therapy during NICU admission until discharge from the hospital, up to 100 days

Interventionmg/kg (Mean)
Clonidine0.11
Placebo0.10

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Total Number of Episodes of Blood Pressure (mm of Hg) Variability

Number of episodes of hypotension (blood pressure < 5th percentile for age) and hypertension (blood pressure > 95th percentile for age) (NCT03762317)
Timeframe: From beginning of morphine therapy during NICU admission until discharge from the hospital, up to 100 days

Interventionepisodes (Number)
Clonidine0
Placebo0

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Total Number of Episodes of Heart Rate Variability (Heart Beats/Min)

Number of episodes of bradycardia (Heart rate < 60/min for a minimum of 20 seconds and not associated with apnea or signs of reflux such as emesis, regurgitation of milk into the mouth or nose, arching while feeding, number of episodes of tachycardia (Heart rate > 200/min) and not related to pain and/or agitation (NCT03762317)
Timeframe: From beginning of morphine therapy during NICU admission until discharge from the hospital, up to 100 days

Interventionevents (Number)
Clonidine0
Placebo0

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Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Measurable Concentration (AUC0-t)

Areas under the plasma concentration-time curve from time zero to the time of last measurable concentration (AUC0-t) (NCT04188730)
Timeframe: Day 1 through Day 3 for Periods I, II, III.

Interventionh*ng/mL (Mean)
Treatment A: Lofexidine Granules - Fasted Conditions12.1333
Treatment B: LUCEMYRA Tablets - Fasted Conditions12.2450
Treatment C: Lofexidine Granules - Fed Conditions12.4540

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Time to Maximum Plasma Concentration (Tmax)

Time to peak plasma concentration (h) collection time at which Cmax is first observed. (NCT04188730)
Timeframe: Day 1 through Day 3 for Periods I, II, III.

Interventionhours (Mean)
Treatment A: Lofexidine Granules - Fasted Conditions4.2678
Treatment B: LUCEMYRA Tablets - Fasted Conditions4.3367
Treatment C: Lofexidine Granules - Fed Conditions4.5344

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Occurrence of Adverse Events (AEs)

Number of Subjects dosed for each Treatment groups: Treatment A = 15 subjects dosed; Treatment B = 16 subjects dosed; Treatment C = 15 subjects dosed (NCT04188730)
Timeframe: Total from occurrences assessed daily after each dosing for Periods 1-3, as well as end of study (22 days)

Interventionadverse events (Number)
Treatment A: Lofexidine Granules - Fasted Conditions3
Treatment B: LUCEMYRA Tablets - Fasted Conditions13
Treatment C: Lofexidine Granules - Fed Conditions14

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Mean Maximum Plasma Concentration (Cmax)

The peak exposure plasma concentrations (Cmax) of lofexidine were observed and measured. (NCT04188730)
Timeframe: Mean from Day 1 through Day 3 for Periods I, II, III.

Interventionng/mL (Mean)
Treatment A: Lofexidine Granules - Fasted Conditions0.6984
Treatment B: LUCEMYRA Tablets - Fasted Conditions0.7275
Treatment C: Lofexidine Granules - Fed Conditions0.6977

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First-order Terminal Rate Constant (λz)

(NCT04188730)
Timeframe: Mean from Day 1 through Day 3 for Periods I, II, III.

Interventionh^-1 (Mean)
Treatment A: Lofexidine Granules - Fasted Conditions0.0549
Treatment B: LUCEMYRA Tablets - Fasted Conditions0.0524
Treatment C: Lofexidine Granules - Fed Conditions0.0524

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First-order Terminal Half-life (T½)

(NCT04188730)
Timeframe: Mean from Day 1 through Day 3 for Periods I, II, III.

Interventionhours (Mean)
Treatment A: Lofexidine Granules - Fasted Conditions13.5577
Treatment B: LUCEMYRA Tablets - Fasted Conditions13.4681
Treatment C: Lofexidine Granules - Fed Conditions13.5008

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Area Under the Plasma Concentration-time Curve From Time Zero to Time Infinity (AUC0-∞)

(NCT04188730)
Timeframe: Mean from Day 1 through Day 3 for Periods I, II, III.

Interventionh·ng/mL (Mean)
Treatment A: Lofexidine Granules - Fasted Conditions14.9643
Treatment B: LUCEMYRA Tablets - Fasted Conditions14.7229
Treatment C: Lofexidine Granules - Fed Conditions14.9004

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