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Piperacillin kinetics.

V K Batra, J A Morrison, K C Lasseter

    Clinical Pharmacology and Therapeutics
    |July 1, 1979
    PubMed
    Summary
    This summary is machine-generated.

    This study investigated piperacillin pharmacokinetics in healthy volunteers. Higher daily doses of piperacillin showed increased peak serum levels and altered clearance over time, suggesting tubular secretion saturation.

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    Area of Science:

    • Pharmacology
    • Clinical Pharmacy
    • Drug Metabolism

    Background:

    • Piperacillin is a broad-spectrum penicillin antibiotic.
    • Understanding piperacillin pharmacokinetics is crucial for optimizing treatment regimens.
    • Intravenous administration is a common route for piperacillin delivery.

    Purpose of the Study:

    • To evaluate the pharmacokinetic profile of piperacillin in healthy volunteers.
    • To assess the impact of different daily dosage regimens on piperacillin serum levels and clearance.
    • To investigate potential saturation of renal tubular secretion at higher piperacillin concentrations.

    Main Methods:

    • Intravenous infusion of piperacillin at 12 gm/day and 24 gm/day for 5 consecutive days.
    • Measurement of mean peak serum levels and pharmacokinetic parameters including half-life, volume of distribution, body clearance, and renal clearance.

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  • Analysis of pharmacokinetic data on day 1 and day 4 of the treatment period.

    • Main Results:

    • Mean peak serum levels of 244 mcg/ml (12 gm/day) and 353 mcg/ml (24 gm/day) were observed.
    • Serum levels declined monoexponentially post-infusion.
    • On day 4, a decreased volume of distribution was noted for the 12 gm/day regimen.
    • For the 24 gm/day regimen, significantly lower body and renal clearance were observed on day 4 compared to day 1.
    • Evidence of tubular secretion process saturation at high piperacillin serum concentrations was suggested by renal clearance patterns.

    Conclusions:

    • Piperacillin pharmacokinetics are dose-dependent and change over consecutive days of administration.
    • The 24 gm/day regimen demonstrated potential saturation of renal tubular secretion.
    • These findings have implications for piperacillin dosing strategies and therapeutic drug monitoring.