ANTIBACTERIAL ACTIVITY OF SULOPENEM, A NEW PARENTERAL PENEM ANTIBIOTIC

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  • 新規注射用ペネム薬 Sulopenem の細菌学的評価

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Abstract

Sulopenem, a new penem antibiotic, was compared with other antibiotics with regard to in vitro antibacterial and bactericidal activities, stabilization against β-lactamases, and effect on the release of lipopolysaccharide from Gram-negative bacteria. The results are summarized as follows.<BR>1. Sulopenem showed more potent activities than other antibiotics against both Gram-positive and Gram-negative bacteria except Pseudomonas aeruginosa.<BR>2. Sulopenem showed potent bactericidal activities (MIC/MBC) against both Gram-positive and Gram-negative bacteria. Time kill studies against Staphylococcus aureus, Escherichia coli, Enterobacter cloacae and Citrobacter freundii showed potent bactericidal activities of sulopenem.<BR>3. Sulopenem was found to possess a stronger activity than other antibiotics against β-lactamase-producing strains except P. aeruginosa and Stenotrophomonas maltophilia.<BR>4. In particular, sulopenem was found to be more stable to the hydrolysis by various β-lactamases produced by Gram-negative bacteria than any other antibiotics tested. Vmax/Km values of sulopenem were smaller than those of cefotiam for all tested β-lactamases, which reflected a broad antibacterial spectrum of sulopenem.<BR>5. E. coli ML4707 exposed to sulopenem and imipenem released less endotoxin than did controls at all concentration ranges tested. In contrast, the strain exposed to ceftazidime at bacteriostatic concentrations released a large amount of endotoxin.

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