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Related Experiment Videos

Clazepam: pharmacokinetics and effects on performance.

J F Giudicelli, A Berdeaux, N Idrissi

    British Journal of Clinical Pharmacology
    |January 1, 1978
    PubMed
    Summary

    Clazepam, a new benzodiazepine, showed moderate effects on performance and anxiety in healthy volunteers. Its activity appears linked to the metabolite desmethyldiazepam, though at low plasma levels.

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    Area of Science:

    • Pharmacology
    • Clinical Trials
    • Neuroscience

    Background:

    • Benzodiazepines are commonly prescribed for anxiety and performance enhancement.
    • Understanding the pharmacokinetic and pharmacodynamic profiles of new benzodiazepines is crucial for clinical application.

    Purpose of the Study:

    • To evaluate the effects of clazepam on performance and cardiovascular system compared to chlordiazepoxide and placebo.
    • To investigate the pharmacokinetics of clazepam and its metabolites in healthy volunteers.

    Main Methods:

    • A double-blind trial involving six healthy volunteers.
    • Oral administration of clazepam (30 mg), chlordiazepoxide (30 mg), and placebo.
    • Assessment of performance tests, cardiovascular parameters, and plasma/urine metabolite analysis.

    Main Results:

    • Clazepam was not detected in plasma or urine, but produced two metabolites: an alcoholic derivative and desmethyldiazepam.
    • Desmethyldiazepam has a long half-life, and both metabolites plus oxazepam accounted for 73% of the dose excreted in 24 hours.
    • Clazepam slightly improved performance and reduced anxiety seven hours post-administration, suggesting action via desmethyldiazepam, but with moderate overall activity due to low metabolite levels.

    Conclusions:

    • Clazepam's effects are likely mediated by its metabolite, desmethyldiazepam.
    • The observed moderate activity of clazepam is attributed to low circulating levels of desmethyldiazepam.
    • Further research may be warranted to optimize clazepam's therapeutic potential.

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