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[First-past Effect (author's transl)].

G Leopold

    Arzneimittel-Forschung
    |February 1, 1977
    PubMed
    Summary
    This summary is machine-generated.

    The first-pass effect, or drug metabolism before systemic circulation, impacts pharmacokinetics. Its therapeutic relevance depends on dose-effect curves and a drug's therapeutic index.

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    Area of Science:

    • Pharmacology
    • Drug Metabolism
    • Pharmacokinetics

    Context:

    • Enteral drug absorption is subject to presystemic metabolism.
    • The liver is a primary site for drug metabolism.
    • First-pass metabolism significantly impacts drug bioavailability.

    Purpose:

    • To define and explain the concept of first-pass effect.
    • To elucidate the pharmacokinetic implications of first-pass metabolism.
    • To differentiate between pharmacokinetic and therapeutic relevance of first-pass effects.

    Summary:

    • First-pass effect describes drug metabolism before systemic circulation, reducing active drug levels.
    • The extent and rate of hepatic metabolism determine the pharmacokinetic impact.
    • Therapeutic relevance depends on dose-effect relationships and therapeutic index, not just pharmacokinetic changes.

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    Impact:

    • Highlights the importance of considering presystemic metabolism in drug development.
    • Informs dosing strategies for orally administered drugs.
    • Emphasizes the need for comprehensive assessment of drug efficacy and safety.