Ｃｅｆｄｉｔｏｒｅｎの臨床分離Ｈａｅｍｏｐｈｉｌｕｓ　ｉｎｆｌｕｅｎｚａｅに対する抗菌力，殺菌力，β‐ラクタマーゼ安定性およびペニシリン結合蛋白質への結合親和性

DOI 被引用文献5件 参考文献16件

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  • Antibacterial activity, bactericidal effect and ,B-lactamase stability of CDTR, and its binding affinity to PBPs against clinical isolate of Haemophilus influenzae.

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The MIC distribution, bactericidal activity and β-lactamase stability of cefditoren (CDTR). the active form of an oral cephalosporin cefditoren pivoxil (CDTR-PI), against a clinical isolate of Haemophilus influenzae, as well as its affnity for penicillin-binding proteins (PBPs) were compared with those of other reference compounds. The results were as follows.<BR>1. The MIC80 value of CDTR against 46 strains of H. influenzae was 0.025μg/ml, which was almost the same as that of cefteram (CFTM) but superior to that of cefdinir (CFDN), cefaclor (CCL), and cefpodoxime (CPDX).<BR>2. The in vitro bactericidal activity of CDTR against H. influenzae PRC 2 was superior to that of CFDN and CCL at concentrations simulating human blood levels after 6 hours. Under these conditions, after 4 hours H. influenzae treated with CDTR in this model simulating the human blood level showed filaments, bulges and bacteriolysis by scanning electron microscopic observation.<BR>3. The affinity of CDTR for PBP 4 and PBP 5 among the PBPs of H. influenzae PRC 2 was higher than that of CFDN and CCL. Its high affinity was paralleled by its strong antibacterial activity.<BR>. The relative rate of hydrolysis of CDTR by β-lactamase was determined. CDTR as well as CFDN was very stable to β-lactamase derived from H. influenzae.

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