European Journal of Clinical Pharmacology

, Volume 34, Issue 1, pp 109–112

Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans

  • S. R. Bareggi
  • G. Truci
  • S. Leva
  • L. Zecca
  • R. Pirola
  • S. Smirne
Short Communications

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.

Key words

chlordesmethyldiazepam lorazepam pharmacokinetics i.v./p.o. administration 

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Copyright information

© Springer-Verlag 1988

Authors and Affiliations

  • S. R. Bareggi
    • 1
  • G. Truci
    • 2
  • S. Leva
  • L. Zecca
    • 1
  • R. Pirola
    • 1
  • S. Smirne
    • 2
  1. 1.Department of Pharmacology, Medical SchoolUniversita' degli StudiMilanoItaly
  2. 2.Department of Neurology, Istituto Scientifico S. Raffaele, Medical SchoolUniversita' degli StudiMilanoItaly
  3. 3.CNR Center for Muscle WORK PhysiologyMilan

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