Del Bene V E, Carek P J, Twitty J A, Burkey L J
Antimicrob Agents Chemother. 1985 May;27(5):817-20. doi: 10.1128/AAC.27.5.817.
Cefbuperazone was compared with other currently available and investigational antibiotics against 278 clinical isolates of anaerobic gram-negative bacilli by an agar dilution method. Cefbuperazone and cefotetan were equally active against Bacteroides fragilis, with 8% of the organisms tested found to be resistant to 32 micrograms of either drug per ml. Cefoperazone, cefotaxime, ceftriaxone, and cefmetazole were less active against these strains; cefoxitin, moxalactam, piperacillin, clindamycin, and metronidazole were more active. None of the agents were consistently active against any of the other anaerobic gram-negative bacilli except imipenem, for which the minimum concentration required to inhibit 90% of all strains tested was 4 micrograms/ml. A 10,000-fold increase in inoculum size caused an increase in the MIC of ceftriaxone, cefotaxime, and cefoperazone but not of cefbuperazone, cefotetan, or cefoxitin. Investigation of the mechanism of resistance to cephalosporin-like agents demonstrated a correlation between the level of resistance and beta-lactamase activity. Cefbuperazone, cefotetan, and cefoxitin were not hydrolyzed, had lower MICs, and were less affected by changes in inoculum size than were cefotaxime, ceftriaxone, and cefoperazone.
采用琼脂稀释法,将头孢布宗与其他目前可用的及正在研究的抗生素针对278株革兰氏阴性厌氧杆菌临床分离株进行了比较。头孢布宗和头孢替坦对脆弱拟杆菌的活性相同,每毫升32微克的这两种药物对8%的受试菌有耐药性。头孢哌酮、头孢噻肟、头孢曲松和头孢美唑对这些菌株的活性较低;头孢西丁、拉氧头孢、哌拉西林、克林霉素和甲硝唑的活性较高。除亚胺培南外,没有一种药物对任何其他革兰氏阴性厌氧杆菌始终具有活性,抑制所有受试菌株90%生长所需的亚胺培南最低浓度为每毫升4微克。接种量增加10000倍会导致头孢曲松、头孢噻肟和头孢哌酮的最低抑菌浓度升高,但不会导致头孢布宗、头孢替坦或头孢西丁的最低抑菌浓度升高。对头孢菌素类药物耐药机制的研究表明,耐药水平与β-内酰胺酶活性之间存在相关性。与头孢噻肟、头孢曲松和头孢哌酮相比,头孢布宗、头孢替坦和头孢西丁不会被水解,最低抑菌浓度较低,且受接种量变化的影响较小。