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Related Experiment Videos

Acyclovir kinetics after intravenous infusion.

P de Miranda, R J Whitley, M R Blum

    Clinical Pharmacology and Therapeutics
    |December 1, 1979
    PubMed
    Summary
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    This study shows the antiviral drug acyclovir has predictable pharmacokinetics and low toxicity in patients with advanced cancers. Acyclovir is a promising treatment for herpes infections due to its favorable disposition and safety profile.

    Area of Science:

    • Pharmacology
    • Clinical Pharmacology
    • Drug Metabolism

    Background:

    • Acyclovir is a widely used antiviral medication.
    • Understanding its pharmacokinetic and safety profile is crucial for effective therapeutic use.
    • Patients with advanced malignancies may have altered drug metabolism and excretion.

    Purpose of the Study:

    • To evaluate the disposition and safety of acyclovir in subjects with advanced malignancies.
    • To determine acyclovir's pharmacokinetic parameters, including plasma levels, half-life, clearance, and urinary excretion.
    • To identify any potential toxicity associated with acyclovir administration in this patient population.

    Main Methods:

    • Intravenous infusion of acyclovir at escalating doses (0.5 to 5.0 mg/kg) in 14 subjects.

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  • Plasma concentrations measured by radioimmunoassay to determine pharmacokinetic profiles.
  • Urinary excretion and metabolite analysis (9-carboxymethoxymethylguanine) using chromatography.

    • Main Results:

    • Acyclovir exhibited dose-independent pharmacokinetics within the studied range.
    • Plasma half-life ranged from 2.2 to 5 hours, with drug detectable for at least 18 hours.
    • Urinary excretion varied (30-69%), indicating both glomerular filtration and tubular secretion.
    • No clinical or laboratory toxicity was observed.

    Conclusions:

    • Acyclovir demonstrates favorable pharmacokinetic properties and a good safety profile in patients with advanced malignancies.
    • Its predictable disposition and low toxicity support its use in treating various herpes infections.
    • Further research into acyclovir's efficacy in specific herpes infections is warranted.