Forstall G J, Knapp C C, Washington J A
Cleveland Clinic Foundation, Ohio 44195.
Antimicrob Agents Chemother. 1991 Aug;35(8):1679-81. doi: 10.1128/AAC.35.8.1679.
Because of the development of newer fluoroquinolones with improved activity against gram-positive organisms, we elected to compare the inhibitory properties of ofloxacin, temafloxacin, sparfloxacin, PD131628, PD127391, and WIN57273 against 105 ciprofloxacin-resistant staphylococci. Based on comparison of MICs for 90% of the organisms (MIC90s), WIN57273 was the most active agent against oxacillin-resistant Staphylococcus aureus; the MIC90 was 0.5 microgram/ml. Against oxacillin-resistant, coagulase-negative staphylococci, PD127391 and WIN57273 were the most active agents; the MIC90 was 0.5 microgram/ml. Against isolates of staphylococci for which ciprofloxacin MICs were greater than or equal to 32 micrograms/ml, WIN57273 and PD127391 still exhibited high activity, inhibiting 100 and 95% of the isolates, respectively, at 2 micrograms/ml. The spontaneous mutation rates for ciprofloxacin-susceptible staphylococci were lowest for ofloxacin. The frequency of spontaneous mutations of ciprofloxacin-resistant staphylococci was low; however, the MICs of PD127391 and WIN57273 for these mutant isolates were greater than 2 micrograms/ml. WIN57273 and PD127391 are two potent new quinolones with high levels of activity against highly ciprofloxacin-resistant staphylococci. There is, however, a major concern of selection of spontaneous mutants resistant to these newer agents.
由于新型氟喹诺酮类药物对革兰氏阳性菌的活性有所提高,我们选择比较氧氟沙星、替马沙星、司帕沙星、PD131628、PD127391和WIN57273对105株耐环丙沙星葡萄球菌的抑制特性。根据90%菌株的最低抑菌浓度(MIC90)比较,WIN57273是对耐苯唑西林金黄色葡萄球菌活性最强的药物;MIC90为0.5微克/毫升。对于耐苯唑西林的凝固酶阴性葡萄球菌,PD127391和WIN57273是活性最强的药物;MIC90为0.5微克/毫升。对于环丙沙星MIC大于或等于32微克/毫升的葡萄球菌分离株,WIN57273和PD127391仍表现出高活性,在2微克/毫升时分别抑制100%和95%的分离株。对环丙沙星敏感的葡萄球菌的自发突变率,氧氟沙星最低。耐环丙沙星葡萄球菌的自发突变频率较低;然而,PD127391和WIN57273对这些突变分离株的MIC大于2微克/毫升。WIN57273和PD127391是两种对高度耐环丙沙星葡萄球菌具有高活性的强效新型喹诺酮类药物。然而,一个主要问题是会选择出对这些新型药物耐药的自发突变体。