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Related Experiment Videos

Systemic availability of orally administered meperidine

L E Mather, G T Tucker

    Clinical Pharmacology and Therapeutics
    |November 1, 1976
    PubMed
    Summary

    Meperidine oral administration shows 47-60% bioavailability, avoiding significant first-pass metabolism. Plasma concentration curves after oral dosing revealed irregularities, suggesting gut interactions or recycling.

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    Area of Science:

    • Pharmacokinetics
    • Drug Metabolism
    • Gastrointestinal Physiology

    Background:

    • First-pass metabolism significantly impacts oral drug bioavailability.
    • Understanding meperidine's absorption is crucial for effective pain management.

    Purpose of the Study:

    • To quantify the oral bioavailability of meperidine.
    • To investigate potential reasons for observed irregularities in oral drug absorption.

    Main Methods:

    • Comparison of plasma concentration-time curves after intravenous and oral meperidine administration.
    • Application of the Loo-Riegelman method for drug absorption calculation.

    Main Results:

    • 48% to 56% of the oral meperidine dose avoided first-pass metabolism.
    • Loo-Riegelman method yielded similar bioavailability estimates (47% to 60%).
    • Oral administration showed irregular plasma curves with double peaks.

    Conclusions:

    • Meperidine exhibits moderate oral bioavailability due to limited first-pass metabolism.
    • Observed oral absorption irregularities may indicate enterohepatic circulation or direct gut effects of meperidine.

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