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Pharmacokinetics of chlorazepate after intravenous and intramuscular administration

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Dichlorazepate (DPC) was given to eight healthy volunteers aged 22–38 years (five males and three females). The dose was 20 mg (48.9 μmol) given either as an IV or an IM injection. The interval between the injections was at least 1 week. Plasma samples were analysed for desmethyldiazepam (DMD) by HPLC before and after acid hydrolysis. The kinetics after both IV and IM administration could be explained by a one or two compartment open model. By comparing values before and after hydrolysis an estimate of di- and/or monopotassiumchlorazepate (MPC) could be made. The bioavailability was almost 100% after IM administration. The plasma half lives of DPC and DMD were independent of the form of administration (2.42 and 46.0 h respectively after IV and 2.29 and 45.1 h respectively after IM injection).

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Correspondence to Harry Malmgren.

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Bertler, Å., Lindgren, S., Magnusson, J. et al. Pharmacokinetics of chlorazepate after intravenous and intramuscular administration. Psychopharmacology 80, 236–239 (1983). https://doi.org/10.1007/BF00436160

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Key words

  • Benzodiazepines
  • Dipotassium chlorazepate
  • N-Desmethyldiazepam
  • Pharmacokinetics after intravenous and intramuscular administration