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Dose-dependent bioavailability of propranolol.

Z Kopitar, B Vrhova, A Lenardic

    International Journal of Clinical Pharmacology, Therapy, and Toxicology
    |June 1, 1986
    PubMed
    Summary
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    This study investigated the pharmacokinetics of propranolol in healthy volunteers. Propranolol showed dose-dependent kinetics, with linearity observed only at higher doses (40-160 mg).

    Area of Science:

    • Pharmacology
    • Clinical Pharmacy
    • Drug Metabolism

    Background:

    • Understanding the pharmacokinetic profile of propranolol is crucial for optimizing therapeutic outcomes.
    • Propranolol is a widely prescribed beta-blocker with known variability in patient response.
    • The metabolism of propranolol, including its active metabolite 4-OH propranolol, influences its efficacy and safety.

    Purpose of the Study:

    • To characterize the dose-dependent pharmacokinetics of orally administered propranolol.
    • To simultaneously quantify propranolol and its metabolite 4-OH propranolol in plasma.
    • To evaluate the linearity of propranolol pharmacokinetics across a range of doses.

    Main Methods:

    • A cross-over trial involving eight healthy volunteers.

    Related Experiment Videos

  • Administration of propranolol at four different oral doses: 10, 40, 80, and 160 mg.
  • A validated analytical method for parallel determination of propranolol and 4-OH propranolol in plasma.

    • Main Results:

    • Demonstrated dose-dependent pharmacokinetics for orally administered propranolol.
    • Established linear dependence within the dosage range of 40 mg to 160 mg.
    • Observed a tendency towards non-linearity for both propranolol and 4-OH propranolol at lower doses (10-40 mg).

    Conclusions:

    • Oral propranolol exhibits dose-dependent pharmacokinetic behavior in healthy individuals.
    • Linear pharmacokinetics are primarily evident at higher propranolol doses.
    • Non-linear kinetics may be significant at lower propranolol doses, impacting drug exposure.