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Digitoxin accumulation

H R Ochs, J Pabst, D J Greenblatt

    British Journal of Clinical Pharmacology
    |August 1, 1982
    PubMed
    Summary
    This summary is machine-generated.

    Digitoxin accumulation is slow, with a half-life of approximately 8 days. Achieving steady-state serum concentrations requires a loading dose about 12 times the daily maintenance dose.

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    Area of Science:

    • Pharmacokinetics
    • Clinical Pharmacology

    Background:

    • Digitoxin is a cardiac glycoside used in treating heart failure.
    • Understanding digitoxin's pharmacokinetic profile is crucial for safe and effective dosing.

    Purpose of the Study:

    • To characterize the pharmacokinetic properties of digitoxin after single intravenous and multiple oral doses.
    • To evaluate digitoxin accumulation and steady-state concentrations in healthy volunteers.

    Main Methods:

    • Single intravenous doses of 1 mg digitoxin were administered to nine healthy volunteers.
    • Multiple oral doses of 0.07 mg digitoxin daily for 28 days were given after a 4-month drug-free interval.
    • Serum digitoxin concentrations were measured over 14 days post-IV dose and during oral dosing and a 21-day washout period.

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    Main Results:

    • The elimination half-life of digitoxin was approximately 8 days after a single IV dose.
    • Digitoxin accumulation during oral maintenance therapy was slow, with a mean half-life of 7.9 days.
    • Observed steady-state serum concentrations closely matched predicted values, but individual correlations were not significant.

    Conclusions:

    • Steady-state serum concentrations of digitoxin are achieved slowly with daily oral maintenance therapy.
    • A loading dose approximately 12 times the maintenance dose is recommended to reach therapeutic levels more rapidly.