Summary
Six healthy, fasting volunteers were given single doses of chlordesmethyldiazepam by 1 mg i. v., or as drops or tablets. Chlordesmethyldiazepam and its metabolite, lorazepam, in multiple plasma samples and in urine collected for 120 h after each dose were determined by electron-capture GLC.
Mean kinetic variables for intravenous chlordesmethyldiazepam were: volume of distribution, 1.71 l · kg−1; elimination half-life, 113 h; total clearance, 0.21 ml · min−1 · kg−1; cumulative excretion of lorazepam glucuronide 24.2% of the dose.
Following a lag time of 15.5 min (tablets) and 4.2 min (drops), which were significantly different, the absorption of oral chlordesmethyldiazepam was a first order process, with apparent absorption half-life values averaging 1.5 h (tablets) and 1.1 h (drops). Bioavailability was 77% for tablets and 79% for drops.
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Bareggi, S.R., Truci, G., Leva, S. et al. Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans. Eur J Clin Pharmacol 34, 109–112 (1988). https://doi.org/10.1007/BF01061430
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DOI: https://doi.org/10.1007/BF01061430