Watanabe N, Hiruma R, Katsu K
Department of Microbiology and Infectious Diseases, Tsukuba Research Laboratories, Eisai Co. Ltd., Ibaraki, Japan.
Antimicrob Agents Chemother. 1992 Mar;36(3):589-97. doi: 10.1128/AAC.36.3.589.
E1077 is a novel parenteral cephalosporin with a wide spectrum of potent antibacterial activity against aerobic and anaerobic gram-positive and gram-negative bacteria. Against methicillin-susceptible Staphylococcus aureus, E1077 was twice as active as cefpirome, with an MIC for 90% of strains tested (MIC90) of 0.78 micrograms/ml. Methicillin-resistant S. aureus was moderately to highly resistant to E1077, but E1077 was at least twice as active as other beta-lactams tested. Against Enterococcus faecalis, E1077 was the most active of the cephalosporins tested (MIC90, 12.5 micrograms/ml) and was at least fourfold more active than cefpirome and ceftazidime. At concentrations of less than or equal to 0.78 micrograms/ml, E1077 inhibited 90% of streptococci and most of the members of the family Enterobacteriaceae tested, with the exceptions of Serratia marcescens and Proteus vulgaris, for which the MIC90s of E1077 were both 3.13 micrograms/ml. Against Pseudomonas aeruginosa, E1077 was two- to fourfold more active than cefpirome and ceftazidime. For the anaerobes, E1077 was as active against Bacteroides fragilis as was cefuzonam, and its activity was fourfold higher than those of cefpirome and ceftazidime. E1077 was at least as resistant as cefpirome to hydrolysis by various beta-lactamases, and these enzymes had a low affinity for E1077.
E1077是一种新型肠胃外使用的头孢菌素，对需氧和厌氧革兰氏阳性及革兰氏阴性菌具有广泛强效抗菌活性。对于对甲氧西林敏感的金黄色葡萄球菌，E1077的活性是头孢匹罗的两倍，90%受试菌株的最低抑菌浓度（MIC90）为0.78微克/毫升。耐甲氧西林金黄色葡萄球菌对E1077有中度至高度耐药性，但E1077的活性至少是其他受试β-内酰胺类药物的两倍。对于粪肠球菌，E1077是受试头孢菌素中活性最强的（MIC90为12.5微克/毫升），其活性至少是头孢匹罗和头孢他啶的四倍。在浓度小于或等于0.78微克/毫升时，E1077抑制了90%的链球菌以及大多数受试肠杆菌科成员，但粘质沙雷氏菌和普通变形杆菌除外，E1077对它们的MIC90均为3.13微克/毫升。对于铜绿假单胞菌，E1077的活性比头孢匹罗和头孢他啶高两至四倍。对于厌氧菌，E1077对脆弱拟杆菌的活性与头孢唑南相当，其活性比头孢匹罗和头孢他啶高四倍。E1077对各种β-内酰胺酶水解的耐药性至少与头孢匹罗相当，并且这些酶对E1077的亲和力较低。
