The Sound of Evolution
Clorazepate
Mechanism of action:
Clorazepate is a benzodiazepine derivative. Clorazepate is a prodrug that is rapidly hydrolyzed after gastrointestinal absorption into its main active metabolite, nordazepam (N-desmethyldiazepam). Nordazepam binds to the benzodiazepine-binding site on the GABA_A receptor, enhances the action of the inhibitory neurotransmitter GABA, and increases the frequency of chloride channel opening. This allows chloride ions to enter neurons, causes membrane hyperpolarization, reduces neuronal action potential generation, and lowers central nervous system excitability.
Reference(s):
1. Committee on the Review of Medicines. (1980). Systematic review of the benzodiazepines: Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Br Med J.
2. McElhatton PR et al. (1994). The effects of benzodiazepine use during pregnancy and lactation. Reprod Toxicol.
3. Ochs HR et al. (1982). Desmethyldiazepam kinetics after intravenous, intramuscular, and oral administration of clorazepate dipotassium. Klin Wochenschr.