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Pharmacokinetics and bactericidal activity of sultamicillin in infants and children

C M Ginsburg, G H McCracken, K Olsen

    The Journal of Antimicrobial Chemotherapy
    |March 1, 1985
    PubMed

    Insights

    Sultamicillin, a combination of ampicillin and sulbactam, shows improved ampicillin absorption in children compared to ampicillin alone. This enhanced pharmacokinetic profile may improve treatment efficacy against resistant bacteria.

    Area of Science:

    • Pharmacology
    • Pediatric Infectious Diseases
    • Microbiology

    Background:

    • Sultamicillin is a prodrug combining ampicillin and sulbactam.
    • Understanding its pharmacokinetics in pediatric populations is crucial for effective antibiotic therapy.
    • Ampicillin's efficacy can be limited by beta-lactamase producing bacteria.

    Purpose of the Study:

    • To evaluate the pharmacokinetics of sultamicillin and ampicillin suspensions in infants and children.
    • To compare ampicillin plasma concentrations and bactericidal activity following administration of sultamicillin versus ampicillin alone.
    • To assess the impact of food on sultamicillin absorption.

    Main Methods:

    • A pharmacokinetic study involving 20 infants and children aged 8-69 months.
    • Administration of sultamicillin (42.5 mg/kg) and ampicillin (25 mg/kg) in a cross-over design for a subset of participants.
    • Measurement of plasma concentrations of ampicillin and sulbactam.
    • Assessment of plasma bactericidal activity against Haemophilus influenzae strains (beta-lactamase producing and non-producing).

    Main Results:

    • Mean peak plasma concentrations of ampicillin and sulbactam were achieved at 90 minutes post-sultamicillin administration.
    • Sultamicillin administration resulted in higher ampicillin plasma concentrations and a 39% larger area under the curve (AUC) compared to ampicillin alone.
    • Food intake did not significantly alter AUC values, though it tended to increase concentrations.
    • Plasma bactericidal activity against beta-lactamase producing H. influenzae was significantly higher with sultamicillin than with ampicillin alone.

    Conclusions:

    • Sultamicillin demonstrates improved pharmacokinetic properties and enhanced ampicillin bioavailability in pediatric patients compared to ampicillin monotherapy.
    • The enhanced activity against beta-lactamase producing bacteria suggests potential clinical advantages for sultamicillin.
    • Sultamicillin offers a promising therapeutic option for pediatric infections, particularly those caused by ampicillin-resistant pathogens.

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