, Volume 11, Issue 3, pp 171-174

Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans

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The pharmacokinetics of chlordemethyldiazepam — a pharmacologically very active new 1,4-benzodiazepine derivative — in healthy subjects after administration of a single oral dose of 2 mg, was studied. Peak concentrations were reached in 1.2 ± 0.2 hours. Plasma levels declined with a biphasic pattern, and the elimination phase had a half-life of 82.9 ± 14.1 hours. The concentrations of the main metabolite of chlordemethyldiazepam, lorazepam, were about 7% of those of the parent compound. In urine only conjugated lorazepam could be found its 96 hour excretion reaching about 15% of the administered dose of parent drug.