Jones R N
Clinical Microbiology Institute, Tualatin, Oregon.
Am J Surg. 1988 May 31;155(5A):16-23. doi: 10.1016/s0002-9610(88)80207-1.
Cefotetan (formerly ICI 156834 and YM09330) is a 7-methoxy cephalosporin possessing some advantageous antimicrobial spectrum, safety, and pharmacokinetic characteristics compared with other so-called second-generation cephalosporins. The published literature was reviewed and the cefotetan quantitative susceptibility testing data from nearly 31,000 isolates was tabulated. Against 15,769 enteric bacilli, cefotetan was observed to have a potency and spectrum more closely resembling a third-generation cephalosporin and markedly superior to cefoxitin. The mean of all MIC 90s reported for the Enterobacteriaceae ranged from 0.06 to 13 micrograms/ml except for citrobacter species, E. cloacae, Enterobacter species, and C. freundii. The mean MIC 50 for all 22 recorded species was in the susceptible range. Cefotetan was very effective against B. catarrhalis, H. influenzae, and pathogenic Neisseria species. However, cefotetan and cefoxitin were not active against Pseudomonas species, Acinetobacter species, and some rarely isolated species. Cefotetan was moderately active against the staphylococci (mean MIC 50, 7.6 to 26 micrograms/ml) and streptococci (mean MIC 50, 0.9 to 6.6 micrograms/ml). The coagulase-negative staphylococcus species generally had higher cefotetan and cefoxitin minimum inhibitory concentrations compared with the S. aureus isolates. Oxacillin-resistant staphylococci were resistant to cefotetan. The enterococci, JK group diphtheroids, Corynebacterium species, and L. monocytogenes isolates were resistant. A review of 4,751 strict anaerobes showed cefotetan to have a very comparable activity and spectrum to cefoxitin. The 1,291 B. fragilis strains had a mean MIC 50 and MIC 90 of 5.4 and 23 micrograms/ml, respectively. These values were slightly superior to cefoxitin when tested in parallel. More elevated minimum inhibitory concentrations were observed for other B. fragilis group species for cefoxitin and cefotetan. The mean cefotetan MIC 90 for all other anaerobic bacteria except the Eubacterium species and Lactobacillus species predict favorable clinical efficacy. The beta-lactamase stability of cefotetan is very similar to that of other 7-methoxy cephalosporins. Cefotetan also inhibits Type Ia cephalosporinases with high enzyme affinity and is an inducer of these beta-lactamases, although cefotetan is not rapidly hydrolyzed. Synergy between cefotetan and numerous other antibiotics has been reported, but antagonism has also been occasionally observed.
头孢替坦(曾用名ICI 156834和YM09330)是一种7-甲氧基头孢菌素,与其他所谓的第二代头孢菌素相比,具有一些有利的抗菌谱、安全性和药代动力学特性。对已发表的文献进行了综述,并将近31,000株菌株的头孢替坦定量药敏试验数据制成表格。在15,769株肠道杆菌中,观察到头孢替坦的效力和抗菌谱更类似于第三代头孢菌素,且明显优于头孢西丁。除柠檬酸杆菌属、阴沟肠杆菌、肠杆菌属和弗氏柠檬酸杆菌外,肠杆菌科所有MIC90的平均值范围为0.06至13微克/毫升。所有22种记录菌株的平均MIC50处于敏感范围内。头孢替坦对卡他莫拉菌、流感嗜血杆菌和致病性奈瑟菌属非常有效。然而,头孢替坦和头孢西丁对铜绿假单胞菌属、不动杆菌属和一些罕见分离菌株无活性。头孢替坦对葡萄球菌(平均MIC50为7.6至26微克/毫升)和链球菌(平均MIC50为0.9至6.6微克/毫升)有中度活性。与金黄色葡萄球菌分离株相比,凝固酶阴性葡萄球菌属通常对头孢替坦和头孢西丁的最低抑菌浓度更高。耐苯唑西林的葡萄球菌对头孢替坦耐药。肠球菌、JK组类白喉杆菌、棒状杆菌属和单核细胞增生李斯特菌分离株耐药。对4,751株严格厌氧菌的综述表明,头孢替坦的活性和抗菌谱与头孢西丁非常相似。1,291株脆弱拟杆菌菌株的平均MIC50和MIC90分别为5.4和23微克/毫升。在平行测试时,这些值略优于头孢西丁。对于其他脆弱拟杆菌属菌种,头孢西丁和头孢替坦的最低抑菌浓度更高。除真杆菌属和乳杆菌属外,所有其他厌氧菌的头孢替坦MIC90平均值预示着良好的临床疗效。头孢替坦的β-内酰胺酶稳定性与其他7-甲氧基头孢菌素非常相似。头孢替坦还以高酶亲和力抑制Ia型头孢菌素酶,并且是这些β-内酰胺酶的诱导剂,尽管头孢替坦不会被快速水解。已报道头孢替坦与许多其他抗生素之间存在协同作用,但偶尔也会观察到拮抗作用。