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Related Experiment Videos

Bioavailability of terfenadine in man.

R A Okerholm, D L Weiner, R H Hook

    Biopharmaceutics & Drug Disposition
    |April 1, 1981
    PubMed
    Summary

    This study investigated terfenadine pharmacokinetics in healthy males. Results show high biotransformation, with minimal unchanged terfenadine excreted, suggesting efficient absorption and metabolism.

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    Area of Science:

    • Pharmacology
    • Drug Metabolism
    • Clinical Pharmacokinetics

    Background:

    • Terfenadine is an antihistamine known for its efficacy.
    • Understanding its absorption, distribution, metabolism, and excretion (ADME) is crucial for safe and effective use.
    • Previous studies suggest significant first-pass metabolism of terfenadine.

    Purpose of the Study:

    • To characterize the pharmacokinetic profile of terfenadine in healthy male subjects.
    • To quantify the extent of terfenadine absorption and biotransformation.
    • To determine the routes of excretion for terfenadine and its metabolites.

    Main Methods:

    • A randomized two-way crossover study design was employed.
    • Subjects received oral doses of terfenadine suspension (60mg and 180mg).

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  • Plasma concentrations and AUC were measured; radiolabeled terfenadine (14C) was used to track absorption and excretion via urine and feces over 12 days.

    • Main Results:

    • Higher doses of terfenadine led to increased peak plasma concentrations and AUC.
    • Approximately 99.5% of absorbed terfenadine-related material underwent biotransformation.
    • Urinary excretion accounted for ~40% of the dose, fecal excretion for ~60%, with minimal unchanged terfenadine detected in feces.

    Conclusions:

    • Terfenadine is extensively absorbed and rapidly biotransformed, with minimal unchanged drug excreted.
    • The high biotransformation rate suggests efficient hepatic metabolism.
    • Excretion primarily occurs via urine and feces, with the latter likely representing metabolites rather than unabsorbed drug.