Page last updated: 2024-12-08

clorazepate dipotassium

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Clorazepate Dipotassium: A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID167305
CHEMBL ID2096631
CHEBI ID3762
MeSH IDM0004628

Synonyms (44)

Synonym
abbott-35616
bipotassium chlorazepate
ab 35616
potassium 7-chloro-2,3-dihydro-2-oxo-5-phenyl-1h-1,4-benzodiazepine-3-carboxylate koh
1h-1,4-benzodiazepine-3-carboxylic acid, 7-chloro-2,3-dihydro-2-oxo-5-phenyl-, potassium salt compound with potassium hydroxide (1:1)
clorazepate dipotassium
potassium 7-chloro-2,3-dihydro-2-oxo-5-phenyl-1h-1,4-benzodiazepine-3-carboxylate compound with potassium hydroxide (1:1)
tr 19119
4306-cb
cb 4306
dikalii clorazepas
clorazepate dipotassique
dipotassium 7-chloro-2-oxo-5-phenyl-2,3-dihydro-1h-1,4-benzodiazepine-3-carboxylate hydroxide
CHEBI:3762 ,
clorazepate dipotassium civ
CHEMBL2096631
4306cb
clorazepic acid dipotassium salt
cm 4306
63fn7g03xy ,
clorazepate dipotassium [usan]
clorazepate dipotassium [vandf]
dipotassium clorazepate [mart.]
clorazepate dipotassium [who-dd]
dipotassium clorazepate [ep impurity]
23895-00-3
clorazepic acid dipotassium salt [mi]
clorazepate dipotassium [jan]
clorazepate dipotassium [orange book]
clorazepate dipotassium [usp monograph]
clorazepate dipotassium civ [usp-rs]
AKOS030242472
dikaliumclorazepat
dipotassium;7-chloro-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepine-3-carboxylate;hydroxide
Q27106189
clorazepato de dipotasio
clorazepate dipotassium (usp monograph)
dipotassium clorazepate (ep impurity)
1h-1,4-benzodiazepine-3-carboxylic acid, 7-chloro-2,3-dihydro-2-oxo-5-phenyl-, monopotassium salt, compound with potassium hydroxide
monopotassium 7-chloro-2-oxo-5-phenyl-2,3-dihydro-1h-1,4-benzodiazepine-3-carboxylate mono(potassium hydroxide)
clorazepato dipotassico
dipotassium clorazepate (mart.)
clorazepate dipotassium civ (usp-rs)
clorazapate dipotassique

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" These findings and other results of pharmacokinetic research have clinical implications in terms of dosage schedules, drug accumulation during long-term therapy, antianxiety therapy in the elderly, drug interactions, pharmacotherapy in specific disease states, and the influence of route of administration on drug action."( Clinical implications of benzodiazepine pharmacokinetics.
Greenblatt, DJ; Shader, RI, 1977
)
0.26
" The method is applicable to pharmacokinetic studies of clorazepate, a benzodiazepine derivative transformed to desmethyldiazepam prior to absorption."( Determination of desmethyldiazepam in plasma by electron-capture GLC: application to pharmacokinetic studies of clorazepate.
Greenblatt, DJ, 1978
)
0.26
" It is suggested that differences in the effects of closely related benzodiazepines may not be due solely to their plasma pharmacokinetic properties, but may arise from differences in their intrinsic activity."( Behavioural and pharmacokinetic studies in the monkey (Macaca mulatta) with diazepam, nordiazepam and related 1,4-benzodiazepines.
Curry, SH; Nicholson, AN; Whelpton, R; Wright, CM, 1977
)
0.26
" Mean kinetic variables were volume of distribution (Vd), 90 liters; elimination half-life (t1/2), 93 hours; and clearance, 12."( Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam.
Boxenbaum, HG; Divoll, MK; Greenblatt, DJ; Harmatz, JS; Shader, RI; Soong, MH, 1988
)
0.27
"Knowledge of the pharmacokinetic properties of the benzodiazepines is playing an increasingly important role in their use during pregnancy, labour and lactation."( Use of benzodiazepines during pregnancy, labour and lactation, with particular reference to pharmacokinetic considerations.
Kanto, JH, 1982
)
0.26
" In the control state, antipyrine half-life was longer in elderly than in young subjects (16."( Cimetidine impairs clearance of antipyrine and desmethyldiazepam in the elderly.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI, 1982
)
0.26

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of enoxacin, a new quinolone antibacterial agent, and its combination with 4-biphenylacetate (BPA), an active metabolite of the non-steroidal antiinflammatory agent fenbufen, were examined on population spikes induced by electrical stimulation of the stratum radiatum in the CA1 pyramidal cell layer in rat hippocampal slices."( Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices.
Hori, S; Ito, T; Kadokawa, T; Miura, Y; Miyahara, T; Shimada, J, 1991
)
0.28
" The study shows that a combination with promethazine is recommended, because promethazine has a selective deactivating effect."( [Optimizing anesthesiologic premedication with reference to biopsychological theories. Exemplified by the effect of dipotassium clorazepate and zolpidem in combination with promethazine].
Schmucker, P; Schön, J; Uhlig, T, 1997
)
0.3
"The effectiveness of clorazepate dipotassium combined with fluoxetine and a behaviour modification programme for the treatment of anxiety disorders in dogs was investigated."( Fluoxetine combined with clorazepate dipotassium and behaviour modification for treatment of anxiety-related disorders in dogs.
Anzola, B; Ibáñez, M; Olivares, A; Pineda, S, 2014
)
1.02

Bioavailability

ExcerptReferenceRelevance
" The assay was used in a comparative bioavailability study of single equimolar oral doses of monopotassium and dipotassium salts of clorazepate in dogs."( GLC determination of plasma drug levels after oral administration of clorazepate potassium salts.
Chun, AH; Hoffman, DJ, 1975
)
0.25
"The pharmacokinetics and bioavailability of desmethyldiazepam (DMDZ), formed from its precursor clorazepate (CZP) dipotassium, were assessed in a series of 17 healthy volunteers aged 21--66 years."( Desmethyldiazepam kinetics after intravenous, intramuscular, and oral administration of clorazepate dipotassium.
Greenblatt, DJ; Knüchel, M; Locniskar, A; Ochs, HR; Steinhaus, E, 1982
)
0.49
" The bioavailability was almost 100% after IM administration."( Pharmacokinetics of chlorazepate after intravenous and intramuscular administration.
Bertler, A; Lindgren, S; Magnusson, JO; Malmgren, H, 1983
)
0.27
" Thus, differences in absorption rate of orally administered benzodiazepines can lead to differences in the intensity of single-dose effects, despite administration of doses that are equivalent in terms of long-term anxiolytic efficacy."( Plasma concentrations and clinical effects after single oral doses of prazepam, clorazepate, and diazepam.
Allison, S; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Pary, RJ; Shader, RI, 1984
)
0.27

Dosage Studied

Clorazepate dipotassium was administered orally to 8 healthy dogs at a dosage of 2 mg/kg of body weight, q 12 h, for 21 days. After oral administration of DMDZ in tablet form (10 mg) and capsule form (15 mg), systemic availability of D MDZ from each of the oral dosage forms was not significantly different from 100%.

ExcerptRelevanceReference
"A specially designed tablet dosage form of the benzodiazepine clorazepate dipotassium (Tranxene) was developed for once-a-day administration."( Steady-state bioavailability of two clorazepate dipotassium dosage forms.
Barker, WM; Carrigan, PJ; Chao, GC; Chun, AH; Hoffman, DJ, 1977
)
0.77
" These findings and other results of pharmacokinetic research have clinical implications in terms of dosage schedules, drug accumulation during long-term therapy, antianxiety therapy in the elderly, drug interactions, pharmacotherapy in specific disease states, and the influence of route of administration on drug action."( Clinical implications of benzodiazepine pharmacokinetics.
Greenblatt, DJ; Shader, RI, 1977
)
0.26
" No significant differences were found between the dosage schedules or between the active medication and the placebo."( Comparison studies of chlorazepate administered as a divided daily dose and as a single dose at night.
Dureman, I; Malmgren, H; Norrman, B, 1978
)
0.26
"The effect of a single dosage of 20 mg dipotassium clorazepate (DPC) on reaction times, with and without administration of ethanol (1 g/kg body weight), was studied in 14 male subjects."( Pharmacopsychological investigations concerning the combined effects of dipotassium clorazepate and ethanol.
Nusser, W; Raff, G; Staak, M, 1979
)
0.26
"Pharmacokinetic investigations concerning possible interactions of an orally administered single dosage of 20 mg dipotassium clorazepate and ethanol were conducted with 14 male subjects."( [Pharmacokinetic studies on interactions between dipotassium clorazepate and alcohol after oral application (author's transl)].
Moosmayer, A; Staak, M, 1978
)
0.26
" Bases for selection include: (1) availability of other than oral dosage forms; (2) differences in additive effect with alcohol in producing central nervous system depression; (3) differences in anticonvulsant effect; and (4) differences in duration of effect in the body (ie, half-life)."( Selection among benzodiazepines for alcohol withdrawal.
Keeler, MH; Miller, WC, 1977
)
0.26
" The dose-response relationships showed that the effect of enoxacin was 100 times potentiated in the presence of BPA (10(-5) M)."( Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices.
Hori, S; Ito, T; Kadokawa, T; Miura, Y; Miyahara, T; Shimada, J, 1991
)
0.28
"Clorazepate dipotassium was administered orally to 8 healthy dogs at a dosage of 2 mg/kg of body weight, q 12 h, for 21 days."( Disposition of clorazepate in dogs after single- and multiple-dose oral administration.
Brown, SA; Forrester, SD; Hartsfield, SM; Lees, GE, 1990
)
1.72
" The dosage remained the same for all patients during the 28 days of the experiment."( [Efficacy and kinetics of chlorazepate administered to anxious patients in a single daily dose].
Adamkiewicz, L; Duguay, R; Le Lorier, J; Messier, R; Rochefort, JG; Viguié, F, 1985
)
0.27
" After oral administration of DMDZ in tablet form (10 mg), or of clorazepate dipotassium in capsule form (15 mg), systemic availability of DMDZ from each of the oral dosage forms was not significantly different from 100%."( Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam.
Boxenbaum, HG; Divoll, MK; Greenblatt, DJ; Harmatz, JS; Shader, RI; Soong, MH, 1988
)
0.51
" Dosage was adjusted to fit patient needs."( Effectiveness of bedtime dosing of benzodiazepines: a placebo-controlled comparison of halazepam and clorazepate.
Aden, GC; O'Hair, DE, 1980
)
0.26
"Methodology for the quantitative determination of clorazepate dipotassium and monopotassium in solid dosage forms was developed."( High-performance liquid chromatographic analysis of clorazepate dipotassium and monopotassium in solid dosage forms.
Elrod, L; Shada, DM; Taylor, VE, 1981
)
0.77
" administration of pure ND in two dogs, has shown that ND declines biexponentially with a t1/2 beta similar to the one estimated after CZP dosing in control animals."( Cimetidine interaction with dipotassium clorazepate disposition in the anesthetized dog.
Colin, P; Lelorier, J; Sirois, G, 1984
)
0.27
" Determination of diazepam and desmethyldiazepam plasma concentrations during the dosing period and for a withdrawal period indicated that accumulation half-life for both diazepam (7."( Prolonged accumulation of diazepam in obesity.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI,
)
0.13
" New antiepileptic drugs have improved medical management, and technical and theoretical advances in pharmacokinetics have permitted physicians to design balanced dosing for individual patients."( Recent developments in the diagnosis and therapy of epilepsy.
Crandall, PH; Engel, J; Sterman, MB; Troupin, AS; Wasterlain, CG, 1982
)
0.26
", owing to the higher dosage used in our study (50 mg as against 20 mg)."( [Oral premedication with clorazepate dipotassium. Comparison with oral premedication with flunitrazepam and intramuscular premedication with promethazine, pethidine and atropine in adults].
Gonzales, I; Kretz, FJ; Peidersky, P, 1993
)
0.59
"The present work describes a quantitative thin layer procedure for estimating primidone, clorazepate dipotassium and chlorzoxazone in bulk powders and in dosage forms, each in the presence of its degradation product."( Spectrodensitometric determination of clorazepate dipotassium, primidone and chlorzoxazone each in presence of its degradation product.
Amer, SM; El Bayoumi, AA; Moustafa, NM; Tawakkol, MS, 1999
)
0.8
" It was found that, when opening of the Mendon capsule is necessary to prepare the powdered dosage form, the CM should be stored below 60% RH to avoid the adsorption of water vapor and discoloration."( Stability of the powdered dosage form prepared by unsealing the capsules: water vapor sorption and discoloration of the powdery contents of clorazepate dipotassium capsules.
Hanawa, T; Ikoma, R; Kimura, F; Nakajima, S; Ohta, T; Suzuki, M; Tsuchiya, T; Uchida, T, 2000
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
anticonvulsantA drug used to prevent seizures or reduce their severity.
anxiolytic drugAnxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions.
GABA modulatorA substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor-ionophore complex. GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of gamma-aminobutyric acid-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
potassium saltAny alkali metal salt having potassium(1+) as the cation.
[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]

Research

Studies (293)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990206 (70.31)18.7374
1990's46 (15.70)18.2507
2000's27 (9.22)29.6817
2010's13 (4.44)24.3611
2020's1 (0.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 50.88

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 Index50.88 (24.57)
Research Supply Index6.03 (2.92)
Research Growth Index4.11 (4.65)
Search Engine Demand Index84.32 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (50.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials90 (27.69%)5.53%
Reviews18 (5.54%)6.00%
Case Studies51 (15.69%)4.05%
Observational0 (0.00%)0.25%
Other166 (51.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Continuation Electroconvulsive Therapy Associated With Pharmacotherapy Versus Pharmacotherapy Alone for Relapse Prevention in Major Depression. A Clinical, Controlled, Prospective and Randomized Trial [NCT01305707]Phase 4104 participants (Actual)Interventional2009-07-31Terminated(stopped due to Difficulties in recruiting)
The Objective of This Study Was to Compare the Single-Dose Relative Bioavailability of Ranbaxy and Abbott (Tranxene® T-Tab®) 15 mg Clorazepate Dipotassium Tablets Under Fasting Conditions. [NCT00775996]32 participants (Actual)Interventional2003-08-31Completed
Randomized Double Blinded Monocentric Study Evaluating the Efficacy of CLORazepate for the Treatment of MIGraine Attack in the Emergency Room [NCT04726592]Phase 3420 participants (Anticipated)Interventional2021-07-08Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]