Clorazepate
- Atc Codes:N05BA05
- CAS Codes:57109-90-7#20432-69-3
- PHARMGKB ID:57109-90-7#20432-69-3
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Tranxilium; Belgium: Tranxene; Cyprus: Clorazepate, Tranxene; France: Tranxene; Germany: Tranxilium; Italy: Transene; Lithuania: Tranxene; Luxembourg: Uni-Tranxene; Netherlands: Clorazepatum, Tranxene, Tranxilium; Poland: Cloranxen, Tranxene; Portugal: Medipax, Tranxene; Romania: Tranxene; Spain: Tranxilium.
North America
Canada: Clorazepate, Novo-Clopate; USA: Gen-Xene, Tranxene.
Latin America
Argentina: Justum, Tencilan, Tranxilium; Brazil: Tranxilene; Mexico: Tranxene.
Asia
Japan: Mendon.
Drug combinations
Clorazepate and Sulpiride
Chemistry
Clorazepate Dipotassium: C~16~H~11~ClK~2~N~2~O~4~. Mw:408.92. (1) 1H-1,4-Benzodiazepine-3-carboxylic acid, 7-chloro-2,3-dihydro-2-oxo-5-phenyl-, potassium salt compound with potassium hydroxide (1:1); (2) Potassium 7-chloro-2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-carboxylate compound with potassium hydroxide (1:1). CAS-57109-90-7; CAS-20432-69-3 (clorazepic acid)(1969).
Pharmacologic Category
Anticonvulsants; Benzodiazepines. Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05BA05).
Mechanism of action
Depresses all levels of the CNS, including the limbic and reticular formation, by binding to the benzodiazepine site on the γ-aminobutyric acid (GABA) receptor complex and modulating GABA, resulting in an increased neuronal membrane permeability to chloride ions which produces a hyperpolarization and stabilization.
Therapeutic use
Generalized anxiety disorder. Ethanol withdrawal. Adjunct anticonvulsant in management of partial seizures.
Pregnancy and lactiation implications
Not recommended during pregnancy or lactation.
Unlabeled use
Contraindications
Hypersensitivity to clorazepate or any component of the formulation. Narrow-angle glaucoma. Pregnancy.
Warnings and precautions
Benzodiazepines have been associated with anterograde amnesia. May cause CNS depression. Paradoxical reactions, including hyperactive or aggressive behavior, reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Use caution in depression (particularly if suicidal risk). Use with caution in history of drug abuse or acute alcoholism (potential for drug dependency; tolerance, psychological and physical dependence). Caution in hepatic/renal impairment. Caution in impaired gag reflux/respiratory disease. Use with caution in debilitated patients. Benzodiazepines have been associated with falls and traumatic injury (caution in elderly patients). Active metabolites with extended half-lives may lead to delayed accumulation and adverse effects. Does not have analgesic, antidepressant, or antipsychotic properties. Rebound or withdrawal symptoms may occur following abrupt discontinuation or large decreases in dose. May cause decreased hematocrit, and abnormal liver and renal function tests.