Martínez-Beltrán J, Cantón R, Liñares J, García de Lomas J, Gimeno C, Tubau F, Baquero F
Servicio de Microbiología, Hospital Ramón y Cajal, Madrid, Spain.
Eur J Clin Microbiol Infect Dis. 1995 Mar;14(3):244-52. doi: 10.1007/BF02310366.
The in vitro antibacterial activity of FK-037, a new parenteral cephalosporin structurally related to cefpirome and cefepime, was compared with that of cefotaxime, ceftazidime, aztreonam, cefpirome, cefepime, imipenem and meropenem against 1,837 clinical isolates obtained from three Spanish hospitals. FK-037 inhibited 90% of Enterobacteriaceae isolates at < or = 0.25 microgram/ml, with the exception of Enterobacter aerogenes (MIC90 1 microgram/ml), Enterobacter cloacae and Citrobacter freundii (MIC90 8 micrograms/ml). In cefotaxime- and ceftazidime-resistant Klebsiella pneumoniae strains producing SHV-2 and SHV-6 beta-lactamases, the activity of FK-037, cefpirome and cefepime was similar (MIC range 0.25-32 micrograms/ml). In Enterobacteriaceae strains hyper-producing chromosomally inducible beta-lactamases, FK-037 (MIC90 range, 0.25-8 micrograms/ml) was 8- to 16-fold more active than cefotaxime and ceftazidime but two- to eightfold less active than cefpirome and cefepime. FK-037 and cefpirome were twofold more active than ceftazidime and cefepime against Pseudomonas aeruginosa isolates, with MIC90 values of 16 micrograms/ml. The activity of FK-037, cefpirome and cefepime was two- to eightfold lower in ceftazidime-resistant derepressed Pseudomonas aeruginosa mutants. FK-037 (MIC range, 0.12-2 micrograms/ml) and the other beta-lactam agents tested were active against methicillin-susceptible staphylococci; however, only cefpirome and, particularly, FK-037 (MIC90 of 32 micrograms/ml) displayed some activity against methicillin-resistant strains. In penicillin-susceptible, -intermediate and -resistant Streptococcus pneumoniae isolates, the MIC90s of FK-037 were 0.03, 0.5 and 1 microgram/ml, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
将一种与头孢匹罗和头孢吡肟结构相关的新型肠外头孢菌素FK - 037的体外抗菌活性,与头孢噻肟、头孢他啶、氨曲南、头孢匹罗、头孢吡肟、亚胺培南和美罗培南针对从三家西班牙医院获取的1837株临床分离菌的抗菌活性进行了比较。FK - 037在≤0.25微克/毫升时能抑制90%的肠杆菌科分离菌,但产气肠杆菌(MIC90为1微克/毫升)、阴沟肠杆菌和弗氏柠檬酸杆菌(MIC90为8微克/毫升)除外。在产生SHV - 2和SHV - 6β - 内酰胺酶的对头孢噻肟和头孢他啶耐药的肺炎克雷伯菌菌株中,FK - 037、头孢匹罗和头孢吡肟的活性相似(MIC范围为0.25 - 32微克/毫升)。在超产染色体诱导型β - 内酰胺酶的肠杆菌科菌株中,FK - 037(MIC90范围为0.25 - 8微克/毫升)的活性比头孢噻肟和头孢他啶高8至16倍,但比头孢匹罗和头孢吡肟低2至8倍。FK - 037和头孢匹罗对铜绿假单胞菌分离菌的活性比头孢他啶和头孢吡肟高两倍,MIC90值为16微克/毫升。在对头孢他啶耐药的去阻遏铜绿假单胞菌突变体中,FK - 037、头孢匹罗和头孢吡肟的活性降低了2至8倍。FK - 037(MIC范围为0.12 - 2微克/毫升)和其他测试的β - 内酰胺类药物对甲氧西林敏感葡萄球菌有活性;然而,只有头孢匹罗,特别是FK - 037(MIC90为32微克/毫升)对耐甲氧西林菌株有一定活性。在对青霉素敏感、中介和耐药的肺炎链球菌分离菌中,FK - 037的MIC90分别为0.03、0.5和1微克/毫升。(摘要截短于250字)