Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans.
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.
D000284:Administration, Oral; D000328:Adult; D014151:Anti-Anxiety Agents; D001569:Benzodiazepines; D003975:Diazepam / Q000031:analogs & derivatives*; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D008140:Lorazepam / Q000378:metabolism; D008297:Male; D008433:Mathematics; D003708:Nordazepam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism
D014151:Anti-Anxiety Agents; D001569:Benzodiazepines; D003708:Nordazepam; D008140:Lorazepam; C013434:chlordesmethyldiazepam; D003975:Diazepam