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Multiple-dose halazepam kinetics.

M Chung, J M Hilbert, R P Gural

    Clinical Pharmacology and Therapeutics
    |June 1, 1984
    PubMed
    Summary
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    This study evaluated the pharmacokinetics of halazepam and its metabolite N-desalkylhalazepam in healthy men. Steady-state levels were predictable and reached within days, informing anxiety disorder treatment.

    Area of Science:

    • Pharmacology
    • Clinical Pharmacokinetics

    Background:

    • Halazepam is a benzodiazepine prescribed for anxiety disorders.
    • Understanding its steady-state kinetics is crucial for effective therapeutic use.

    Purpose of the Study:

    • To evaluate the steady-state pharmacokinetics of halazepam.
    • To assess the kinetics of its primary active metabolite, N-desalkylhalazepam.

    Main Methods:

    • Eleven healthy male participants received 40 mg of oral halazepam every 8 hours for 14 days.
    • Plasma concentrations of halazepam and N-desalkylhalazepam were quantified using gas chromatography.

    Main Results:

    • Halazepam's kinetics fit a two-compartment open model with first-order absorption.
    • Elimination half-lives were 34.7 hours for halazepam and 57.9 hours for N-desalkylhalazepam.

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  • Steady-state levels were achieved by day 3 for halazepam and day 11 for N-desalkylhalazepam.
  • Conclusions:

    • Steady-state concentrations of halazepam and N-desalkylhalazepam are predictable.
    • Kinetic data supports the dosing regimen for managing anxiety disorders with halazepam.