Inoue K, Inoue E, Mitsuhashi S
Episome Institute, Gunma, Japan.
Chemotherapy. 1995 Jul-Aug;41(4):257-66. doi: 10.1159/000239354.
The antibacterial and bactericidal activities and the stability of FK037 to beta-lactamases were investigated and compared with those of cefpirome, flomoxef, ceftazidime, ceftizoxime, and vancomycin. Against clinical isolates of methicillin-sensitive and methicillin-resistant Staphylococcus aureus, FK037 was less active than vancomycin but more potent than the other drugs tested. Among highly methicillin-resistant staphylococci (MIC for methicillin: 200 mg/l or higher), none of the strains were highly resistant to FK037 (MIC > or = 100 mg/l) unlike the other cephalosporins. With the exception of Enterococcus faecalis, FK037 had an activity equipotent to that of cefpirome and far superior to those of flomoxef, ceftazidime and ceftizoxime against other gram-positive clinical isolates. The activity of FK037 against Pseudomonas aeruginosa and Pseudomonas cepacia was equipotent to that of cefpirome but 2- to 4-fold less active than that of ceftazidime. FK037 inhibited 90% of Enterobacter cloacae and Citrobacter freundii growth at a concentration of 6.25 mg/l; it was as active as cefpirome and much more active than ceftazidime. Against the other gram-negative bacteria tested, FK037 was equipotent to cefpirome and ceftazidime and was more effective than flomoxef. FK037, like cefpirome, portrayed a high stability to various beta-lactamases except type II penicillinase and oxyimino-cephalosporinase (CXase). FK037 scored an MIC range of 0.013-6.25 mg/l against numerous beta-lactamase-producing bacterial strains with the exception of some CXase-producing strains and a cephalosporinase-producing C. freundii; and against strains other than P. aeruginosa FK037 was as active as cefpirome and 2- to 32-fold more active than ceftazidime. FK037 displayed highly potent activities against cephalosporinase-producing E. cloacae, C. freundii and Serratia marcescens which were resistant to flomoxef and ceftizoxime. FK037 was highly bactericidal against S. aureus and Escherichia coli at its MIC or higher.
对FK037的抗菌和杀菌活性以及对β-内酰胺酶的稳定性进行了研究,并与头孢匹罗、氟氧头孢、头孢他啶、头孢唑肟和万古霉素进行了比较。针对甲氧西林敏感和耐甲氧西林金黄色葡萄球菌的临床分离株,FK037的活性低于万古霉素,但比其他受试药物更强。在高度耐甲氧西林葡萄球菌(对甲氧西林的MIC:200mg/l或更高)中,与其他头孢菌素不同,没有菌株对FK037高度耐药(MIC≥100mg/l)。除粪肠球菌外,FK037对其他革兰氏阳性临床分离株的活性与头孢匹罗相当,远优于氟氧头孢、头孢他啶和头孢唑肟。FK037对铜绿假单胞菌和洋葱伯克霍尔德菌的活性与头孢匹罗相当,但比头孢他啶低2至4倍。FK037在浓度为6.25mg/l时可抑制90%的阴沟肠杆菌和弗氏柠檬酸杆菌生长;其活性与头孢匹罗相当,比头孢他啶活性高得多。针对其他受试革兰氏阴性菌,FK037与头孢匹罗和头孢他啶相当,比氟氧头孢更有效。FK037与头孢匹罗一样,对除II型青霉素酶和氧亚氨基头孢菌素酶(CX酶)外的各种β-内酰胺酶具有高度稳定性。除了一些产生CX酶的菌株和一株产生头孢菌素酶的弗氏柠檬酸杆菌外,FK037对众多产生β-内酰胺酶的细菌菌株的MIC范围为0.013 - 6.25mg/l;对于除铜绿假单胞菌外的菌株,FK037的活性与头孢匹罗相当,比头孢他啶高2至32倍。FK037对耐氟氧头孢和头孢唑肟的产头孢菌素酶的阴沟肠杆菌、弗氏柠檬酸杆菌和粘质沙雷氏菌具有高效活性。FK037在其MIC或更高浓度时对金黄色葡萄球菌和大肠杆菌具有高度杀菌作用。