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Multiple-dose albuterol kinetics.

M L Powell, M Chung, M Weisberger

    Journal of Clinical Pharmacology
    |November 1, 1986
    PubMed
    Summary
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    This study investigated albuterol pharmacokinetics in healthy males. Steady-state plasma levels were reached by day three, with a small accumulation ratio and a 6.5-hour half-life.

    Area of Science:

    • Pharmacology
    • Clinical Pharmacy
    • Drug Metabolism

    Background:

    • Albuterol is a widely used bronchodilator for respiratory conditions.
    • Understanding its steady-state pharmacokinetics is crucial for optimizing therapeutic use.
    • Previous studies have focused on single-dose kinetics, necessitating further investigation into chronic dosing.

    Purpose of the Study:

    • To evaluate the steady-state pharmacokinetics of oral albuterol.
    • To determine plasma concentration-time profiles during repeated dosing.
    • To assess drug accumulation and elimination half-life after multiple doses.

    Main Methods:

    • 12 healthy male volunteers received oral albuterol 4-mg tablets every six hours for five days.
    • Plasma samples were collected to determine albuterol concentrations over time.

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  • Pharmacokinetic parameters were analyzed using a two-compartment open model with first-order absorption.

    • Main Results:

    • Steady-state plasma levels were predictable and achieved by the third day of dosing (9th-10th dose).
    • A small accumulation ratio of approximately two was observed.
    • The elimination phase half-life was determined to be 6.5 hours.

    Conclusions:

    • Oral albuterol exhibits predictable pharmacokinetics at steady-state.
    • The observed half-life is consistent with single-dose administration findings.
    • These results support the established dosing regimen for albuterol in clinical practice.