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clorazepate (Tranxene)
Tradename: Tranxene. DEA-controlled substance: class 4.
Indications:
1) generalized anxiety
2) management of alcohol withdrawal
3) adjunct anticonvulsant in management of partial seizures
Contraindications:
1) hypersensitivity; cross-sensitivity with other benzodiazepines may exist
2) avoid using in patients with pre-existing CNS depression
3) narrow-angle glaucoma 7.5-15 mg PO QHS/BID [1]. 7.5-60 mg/24 hours QD/BID/TID/QID [2]. Alcohol withdrawal:
- 30 mg initially, then 15 mg BID-QID with taper
Tabs: 3.75, 7.5, 15 mg.
Pharmacokinetics:
1) prodrug for desmethyldiazepam, an active metabolite (also metabolite of diazepam)
2) normal gastric acidity necessary for hydrolysis to desmethyldiazepam
Adverse effects:
1) 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
2) less common (1-10%)
- confusion, nervousness, syncope, dizziness, akathesia, increased salivation, hypotension, rigidity, tremor, dermatitis, nasal congestion, weight gain or weight loss, hyperventilation, tinnitus, muscle cramps
3) uncommon (< 1%)
- menstrual irregularities, blood dyscrasias, reflex slowing, drug dependence
4) long term use
- renal injury, hepatic injury, anemia
Drug interactions:
1) cimetidine, estrogens, disulfiram & erythromycin may inhibit hepatic metabolism
2) CNS depressants may enhance CNS effects of clorazepate
a) alcohol
b) antidepressants
c) antipsychotics
d) sedatives/hypnotics
e) MAO inhibitors
3) antacids decrease activation
4) carbamazepine may increase hepatic metabolism
Laboratory:
1) specimen: serum, plasma (EDTA)
2) methods: HPLC, GC
Interactions
drug interactions
drug adverse effects (more general classes)
General
benzodiazepine
Properties
MISC-INFO: elimination route LIVER
1/2life 30-100 HOURS
therapeutic-range 0.12-1.0 UG/ML
protein-binding 97%
pregnancy-category D
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- 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