IN VITRO ANTIBACTERIAL ACTIVITY OF A NEW PARENTERAL PENEM, SULOPENEM

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  • Sulopenem 抗菌活性の基礎的, 細菌学的検討

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Abstract

Eighty percent minimum inhibitory concentrations (MICK) of sulopenem against clinically isolated 12 to 80 strains of each of different bacteria were as follows: methicillin-susceptible Staphylococcus aureus (MSSA): 0.20μg/ml, methicillin-resistant S. aureus (MRSA): 50μg/ml, coagulase-negative staphylococci: 3.13μg/ml, Streptococcus pyogenes:≤0.013μg/ml, Streptococcus pneumoniae:≤0.013μg/ml, β-streptococci: 0.05μg/ml, Enterococcus faecalis: 12.5μg/ml, Enterococcus faecium:>100μg/ml, Escherichia coli CS2(R+): 0.10μg/ml, Klebsiella pneumoniae: 0.05μg/ml, Proteus mirabilis: 0.10μg/ml, Proteus vulgaris: 0.20μg/ml, Morganella morganii: 0.39μg/ml, Providencia rettgeri: 3.13μg/ml, Citrobacter freundii: 0.20μg/ml, Enterobacter cloacae: 0.39μg/ml, Serratia marcescens: 1.56μg/ml, Pseudomonas aeruginosa: 50μg/ml, Pseudomonas cepacia: 3.13μg/ml, Xanthomonas maltophilia: >100μg/ml, Acinetobacter calcoaceticus: 1.56μg/ml, ampicillin-resistant Haemophilus influenzae: 0.39μg/ml and Bacteroides fragilis: 0.20μg/ml, respectively. Sulopenem possesses a stronger activity than flomoxef or cefuzonam against Gram-positive bacteria, the strongest activity among the antibiotics tested against Gram-negative bacteria except P. aeruginosa.<BR>Sulopenem has stronger affinities than imipenem to all fractions of PBPs of S. aureus, E. coli, P. vulgaris, S. marcescens, even of P. aeruginosa. Affinities of sulopenem to PBPs-1 and -3 of S. aureus, PBP-2 of E. coli were much stronger than those of imipenem (IPM).<BR>Sulopenem generally has small Ki values to all types of β-lactamases and also has stronger permanent inactivation effect to Ia and IIb types of β-lactamases than IPM.<BR>No synergistic bactericidal activity of sulopenem was apparent with serum complement. However, synergism of sulopenem with macrophages was prominent in bactericidal activity. The cells of E. coli were well phagocytosed and rapidly digested by cultured macrophages in the presence of a higher than 1/8 MIC of sulopenem.<BR>Moreover, sulopenem was more stable than imipenem against swine and human dehydropeptidase-Is. Sulopenem is one of the antibiotics that do not induce the appearance of subclones resistant to the drug.

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