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Protriptyline kinetics.

V E Ziegler, J T Biggs, L T Wylie

    Clinical Pharmacology and Therapeutics
    |May 1, 1978
    PubMed
    Summary
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    Protriptyline exhibits a long half-life (t1/2) of approximately 74.3 hours after oral administration. First-pass metabolism is minimal, and its pharmacokinetics do not correlate with doxepin in subjects.

    Area of Science:

    • Pharmacokinetics
    • Clinical Pharmacology

    Background:

    • Protriptyline is a tricyclic antidepressant.
    • Understanding its pharmacokinetic profile is crucial for therapeutic management.

    Purpose of the Study:

    • To characterize the pharmacokinetic parameters of protriptyline following a single oral dose.
    • To confirm the previously reported long half-life of protriptyline.

    Main Methods:

    • Single oral dose administration of 30 mg protriptyline hydrochloride to 8 healthy subjects.
    • Measurement of plasma protriptyline concentrations over time.
    • Calculation of key pharmacokinetic parameters including half-life and volume of distribution.

    Main Results:

    • Peak plasma protriptyline levels (10.4–22.3 ng/ml) were achieved between 6–12 hours post-dose.

    Related Experiment Videos

  • The mean protriptyline half-life (t1/2) was 74.3 hours (range: 53.6–91.7 hours).
  • Estimated first-pass metabolism was low (10–25%), with a mean volume of distribution of 22.5 L/kg.

    • Conclusions:

    • Protriptyline possesses a notably long elimination half-life.
    • First-pass metabolism of protriptyline is minimal.
    • No correlation was observed between protriptyline and doxepin pharmacokinetics in the studied subjects.