Rolfe R D, Finegold S M
Antimicrob Agents Chemother. 1981 Nov;20(5):600-9. doi: 10.1128/AAC.20.5.600.
Several new beta-lactam antimicrobial agents have been introduced in the last few years. In this investigation, the in vitro activities of several recently introduced cephalosporins (cefoperazone, cefotaxime, ceftazidime, and ceftizoxime), moxalactam, and N-formimidoyl thienamycin were compared with those of cefoxitin, clindamycin, and metronidazole against 203 strains of anaerobic bacteria. At achievable serum levels, all of the antimicrobial agents were active against essentially 100% of the strains of anaerobic gram-positive cocci, Clostridium perfringens, Leptotrichia buccalis, and species of Selenomonas, Veillonella, and Eubacterium. Clindamycin, metronidazole, and N-formimidoyl thienamycin were the most active agents against the Bacteroides fragilis group, inhibiting all strains at concentrations which can be achieved in serum. Of the remaining agents tested against the B. fragilis group, cefoxitin (which required 64 mug/ml to inhibit 90% of the strains) was the most active, followed by cefoperazone (128 mug/ml), cefotaxime (128 mug/ml), moxalactam (128 mug/ml), ceftizoxime (256 mug/ml), and ceftazidime (>256 mug/ml). Important differences in cephalosporin susceptibility among species of the B. fragilis group were observed. Metronidazole and N-formimidoyl thienamycin were the most active drugs against species of clostridia other than C. perfringens; the other antibiotics displayed poor activity, although this is partly due to inclusion of a relatively large number of strains of Clostridium difficile which were very resistant to several of the cephalosporins. Only metronidazole was active against all species of Fusobacterium. Clindamycin and N-formimidoyl thienamycin displayed excellent activity against gram-positive, non-spore-forming bacilli, requiring </=8 mug/ml to inhibit 100% of the strains. Ceftazidime, cefoperazone, and moxalactam were bactericidal for 25 strains of B. fragilis at concentrations equal or close to those required for inhibition. On the basis of its activity in vitro, N-formimidoyl thienamycin appears to be the most promising of the new beta-lactam antibiotics for the treatment of infections involving anaerobic bacteria.
在过去几年中引入了几种新型β-内酰胺类抗菌剂。在本研究中,将几种最近引入的头孢菌素(头孢哌酮、头孢噻肟、头孢他啶和头孢唑肟)、莫西沙星和N-甲酰亚胺基硫霉素的体外活性与头孢西丁、克林霉素和甲硝唑对203株厌氧菌的活性进行了比较。在可达到的血清水平下,所有抗菌剂对基本上100%的厌氧革兰氏阳性球菌、产气荚膜梭菌、颊纤毛菌以及月形单胞菌属、韦荣球菌属和真杆菌属的菌株均有活性。克林霉素、甲硝唑和N-甲酰亚胺基硫霉素是对脆弱拟杆菌属最具活性的药物,在血清中可达到的浓度下抑制所有菌株。在针对脆弱拟杆菌属测试的其余药物中,头孢西丁(抑制90%的菌株需要64μg/ml)活性最高,其次是头孢哌酮(128μg/ml)、头孢噻肟(128μg/ml)、莫西沙星(128μg/ml)、头孢唑肟(256μg/ml)和头孢他啶(>256μg/ml)。观察到脆弱拟杆菌属不同种之间头孢菌素敏感性存在重要差异。甲硝唑和N-甲酰亚胺基硫霉素是对除产气荚膜梭菌外的梭菌属最具活性的药物;其他抗生素活性较差,尽管这部分是由于纳入了相对大量对几种头孢菌素耐药性很强的艰难梭菌菌株。只有甲硝唑对所有梭杆菌属物种有活性。克林霉素和N-甲酰亚胺基硫霉素对革兰氏阳性、无芽孢杆菌显示出优异的活性,抑制100%的菌株需要≤8μg/ml。头孢他啶、头孢哌酮和莫西沙星在等于或接近抑制所需浓度时对25株脆弱拟杆菌具有杀菌作用。基于其体外活性,N-甲酰亚胺基硫霉素似乎是用于治疗涉及厌氧菌感染的新型β-内酰胺类抗生素中最有前景的。