clorazepate (Tranxene)
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Introduction
Tradename: Tranxene. DEA-controlled substance: class 4.
Indications
- generalized anxiety
- management of alcohol withdrawal
- adjunct anticonvulsant in management of partial seizures
Contraindications
- hypersensitivity; cross-sensitivity with other benzodiazepines may exist
- avoid using in patients with pre-existing CNS depression
- narrow-angle glaucoma 7.5-15 mg PO QHS/BID[1]. 7.5-60 mg/24 hours QD/BID/TID/QID[2]. Alcohol withdrawal:
Tabs: 3.75, 7.5, 15 mg.
Pharmacokinetics
- prodrug for desmethyldiazepam, an active metabolite (also metabolite of diazepam)
- normal gastric acidity necessary for hydrolysis to desmethyldiazepam
elimination via liver
1/2life = 30-100 hours
protein binding = 97 %
Adverse effects
- common (> 10%)
- drowsiness, fatigue, impaired coordination, lightheadedness, memory impairment, insomnia, dysarthria, anxiety, decreased libido, depression, headache, dry mouth, constipation, diarrhea, decreased salivation, nausea/vomiting, tachycardia, chest pain, blurred vision, sweating, rash, increased or decreased appetite
- less common (1-10%)
- uncommon (< 1%)
- menstrual irregularities, blood dyscrasias, reflex slowing, drug dependence
- long term use
- drug adverse effects of benzodiazepines
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- cimetidine, estrogens, disulfiram & erythromycin may inhibit hepatic metabolism
- CNS depressants may enhance CNS effects of clorazepate
- antacids decrease activation
- carbamazepine may increase hepatic metabolism
- drug interaction(s) of methadone in combination with benzodiazepines
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of benzodiazepines with thiazide diuretics
- drug interaction(s) of antipsycotics with benzodiazepines
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of alcoholic beverage with benzodiazepines
- drug interaction(s) of benzodiazepine with opiates
Laboratory
More general terms
References
- ↑ 1.0 1.1 The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- ↑ 2.0 2.1 Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 7
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995