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Temporal changes in bupivacaine kinetics.

B Bruguerolle, M Prat

    The Journal of Pharmacy and Pharmacology
    |February 1, 1987
    PubMed
    Summary
    This summary is machine-generated.

    Bupivacaine

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    Area of Science:

    • Pharmacology
    • Pharmacokinetics
    • Chronopharmacology

    Background:

    • Bupivacaine is a widely used local anesthetic.
    • Understanding its pharmacokinetic profile is crucial for safe and effective use.
    • Circadian rhythms can influence drug metabolism and effects.

    Purpose of the Study:

    • To investigate the chronokinetics of bupivacaine in mice.
    • To determine if the time of administration affects bupivacaine's pharmacokinetic parameters.
    • To explore potential circadian variations in bupivacaine efficacy and toxicity.

    Main Methods:

    • Adult male NMRI mice received intraperitoneal injections of bupivacaine (20 mg/kg) at four different times (10:00, 16:00, 22:00, 04:00).
    • Blood samples were collected at various time points post-injection (0.25 to 6 hours).

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  • Serum bupivacaine levels were quantified using gas-liquid chromatography with a flame ionization detector.

    • Main Results:

    • Significant temporal variations were observed in Cmax (maximum concentration), Cmax/Tmax ratio, and beta elimination half-life (T1/2 beta).
    • The highest values for these parameters were recorded when bupivacaine was administered at 22:00.
    • Area under the concentration-time curve (AUC) did not show significant differences across administration times.

    Conclusions:

    • Bupivacaine exhibits statistically significant circadian rhythm in its pharmacokinetic parameters in mice.
    • The time of administration, particularly around 22:00, influences bupivacaine's peak concentration, rate of absorption, and elimination half-life.
    • These findings suggest potential time-dependent differences in bupivacaine's efficacy and toxicity, warranting further investigation.