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Related Experiment Videos

Amitriptyline disposition in young and elderly normal men.

P Schulz, K Turner-Tamiyasu, G Smith

    Clinical Pharmacology and Therapeutics
    |March 1, 1983
    PubMed
    Summary
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    Amitriptyline disposition in healthy men shows age does not affect clearance or bioavailability. However, older adults experience a longer half-life due to increased volume of distribution, necessitating careful dosing.

    Area of Science:

    • Pharmacokinetics
    • Geriatric Medicine
    • Clinical Pharmacology

    Background:

    • Amitriptyline is a widely used antidepressant.
    • Understanding age-related differences in drug disposition is crucial for safe and effective prescribing.

    Purpose of the Study:

    • To investigate the pharmacokinetic differences of amitriptyline between young and elderly healthy men.
    • To assess the impact of age on amitriptyline's systemic clearance, half-life, volume of distribution, bioavailability, and protein binding.

    Main Methods:

    • A single parenteral or oral dose of amitriptyline was administered to two groups of healthy men: young (mean age 22) and elderly (mean age 71).
    • Pharmacokinetic parameters including systemic clearance, half-life (t 1/2), volume of distribution, bioavailability, and plasma protein binding were measured and compared between groups.

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    Main Results:

    • Systemic clearance and bioavailability of amitriptyline did not significantly differ between young and elderly subjects.
    • The mean half-life (t 1/2) was longer in the elderly group (21.7 hr) compared to the younger group (16.2 hr).
    • This prolonged half-life in the elderly was attributed to an increased volume of distribution (17.1 L/kg vs. 14.1 L/kg).

    Conclusions:

    • Age does not alter amitriptyline's systemic clearance or bioavailability in healthy individuals.
    • Elderly individuals exhibit a longer amitriptyline half-life due to an increased volume of distribution.
    • Single doses of amitriptyline were poorly tolerated in both age groups, highlighting the need for gradual dose titration and close monitoring in elderly patients.