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[Basic and clinical studies on S-1108 in pediatric field]

T Motohiro1, S Handa, S Yamada

  • 1Department of Pediatrics, School of Medicine, Kurume University.

The Japanese Journal of Antibiotics
|December 1, 1993
PubMed
Summary

S-1108, an oral cephem antibiotic, demonstrates broad-spectrum activity against Gram-positive and Gram-negative bacteria. Laboratory and clinical pediatric evaluations show high efficacy and favorable pharmacokinetic profiles for S-1108.

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Area of Science:

  • Microbiology
  • Pharmacology
  • Pediatrics

Background:

  • S-1108 is a novel oral esterified cephem antibiotic with broad-spectrum activity.
  • Its active metabolite, S-1006, exhibits stability against beta-lactamases, with few exceptions.
  • This study focuses on the laboratory and clinical evaluation of S-1108 granules in pediatric patients.

Purpose of the Study:

  • To evaluate the in vitro antimicrobial activity of S-1108 against common pediatric pathogens.
  • To assess the pharmacokinetic and pharmacodynamic properties of S-1108 in children.
  • To determine the clinical efficacy of S-1108 in pediatric infections.

Main Methods:

  • In vitro drug sensitivity testing using minimum inhibitory concentration (MIC) for clinical isolates of Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, and Haemophilus influenzae.

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  • Administration of S-1108 granules at 4.0 mg/kg and 6.0 mg/kg to pediatric patients to measure peak plasma concentration, plasma half-life, and area under the curve (AUC).
  • Monitoring of urinary concentration and recovery rates, alongside assessment of clinical effects in pediatric patients.

    • Main Results:

    • S-1108 showed potent activity against Staphylococcus aureus (MIC80: 6.25 µg/ml) and Streptococcus species (MIC: ≤0.025 µg/ml), comparable to existing antibiotics.
    • Pharmacokinetic studies revealed dose-dependent peak plasma concentrations (1.25-2.43 µg/ml) and half-lives (1.11-1.28 hours) after administration.
    • Clinical evaluation demonstrated a high efficacy rate of 94.6% (88 out of 93 patients) with excellent or good clinical effects.

    Conclusions:

    • S-1108 exhibits significant in vitro activity against key pediatric bacterial pathogens.
    • The drug demonstrates favorable pharmacokinetic properties and a dose-response relationship in pediatric patients.
    • S-1108 is a highly effective oral antibiotic for treating pediatric infections, with a high clinical success rate.