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Methapyrilene kinetics and dynamics

E P Calandre, N Alferez, K Hassanein

    Clinical Pharmacology and Therapeutics
    |April 1, 1981
    PubMed
    Summary
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    Methapyrilene shows moderate antihistamine effects and mild, short-lived sedation. Its pharmacokinetic profile in humans reveals low bioavailability and rapid elimination, indicating limited systemic exposure.

    Area of Science:

    • Pharmacology
    • Clinical Pharmacokinetics

    Background:

    • Methapyrilene is an H1 receptor antagonist with known central nervous system effects.
    • Understanding its pharmacokinetic properties is crucial for assessing its therapeutic and adverse effects.

    Purpose of the Study:

    • To characterize the H1 receptor blockade of methapyrilene.
    • To evaluate its central nervous system depressant properties.
    • To determine the kinetic parameters of methapyrilene in humans.

    Main Methods:

    • Eight healthy subjects participated in a randomized, crossover study.
    • Administered placebo, intravenous methapyrilene (20 mg), and oral methapyrilene (25 mg and 50 mg).
    • Assessed antihistaminic effect via histamine-provoked skin wheals and monitored for sedation.

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    Main Results:

    • Methapyrilene demonstrated moderate H1 receptor blockade, reducing histamine-induced wheals.
    • Sedation and drowsiness were observed transiently after intravenous administration.
    • Pharmacokinetic parameters included a plasma half-life of 1.1–2.1 hr, volume of distribution of 2.14–6.61 L/kg, and clearance of 0.013–0.048 L/min/kg.
    • Systemic bioavailability was low (4–46%) with significant interindividual variability.
    • Urinary recovery of unchanged methapyrilene was minimal (<2%).

    Conclusions:

    • Methapyrilene possesses moderate antihistaminic activity.
    • Central nervous system depressant effects are transient, primarily with intravenous administration.
    • Low and variable bioavailability, coupled with rapid elimination, suggests limited systemic exposure and potential for dose adjustments.