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Pharmacokinetics of chloramphenicol and chloramphenicol succinate in infants and children

R E Kauffman, J N Miceli, L Strebel

    The Journal of Pediatrics
    |February 1, 1981
    PubMed

    Insights

    The metabolism of chloramphenicol-3-monosuccinate in children showed significant variability in elimination, with half-life inversely correlated to age. This variability impacts drug bioavailability and dosing efficacy.

    Area of Science:

    • Pharmacology
    • Pediatric Medicine
    • Drug Metabolism

    Background:

    • Chloramphenicol-3-monosuccinate is an intravenous prodrug of chloramphenicol.
    • Understanding its pharmacokinetics in pediatric populations is crucial for safe and effective use.

    Purpose of the Study:

    • To investigate the metabolism and elimination of chloramphenicol-3-monosuccinate in infants and children.
    • To determine factors contributing to the variability in chloramphenicol pharmacokinetics.

    Main Methods:

    • Intravenous administration of chloramphenicol-3-monosuccinate to 45 pediatric patients (3 days to 16 years).
    • Analysis of serum chloramphenicol concentrations and urinary excretion.
    • Calculation of pharmacokinetic parameters including half-life and renal clearance.

    Main Results:

    • Apparent chloramphenicol half-life was highly variable (1.7–12.0 hours, mean 5.1 hours) and inversely correlated with age.
    • Chloramphenicol-S serum concentrations declined biexponentially with mean half-lives of 0.7 and 2.2 hours.
    • A mean of 33% of the dose was excreted unchanged in urine, indicating poor bioavailability; active tubular secretion was observed.

    Conclusions:

    • Variable hydrolysis and renal elimination of chloramphenicol-3-monosuccinate significantly reduce antibiotic bioavailability.
    • These factors contribute to wide variations in half-life and poor dose-concentration correlation in pediatric patients.
    • Age-dependent pharmacokinetics necessitate careful dosing and monitoring in infants and children.

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