Spangler S K, Jacobs M R, Appelbaum P C
Department of Pathology (Clinical Microbiology), Hershey Medical Center, Pennsylvania 17033.
Antimicrob Agents Chemother. 1992 Apr;36(4):856-9. doi: 10.1128/AAC.36.4.856.
The MICs of four new quinolones, sparfloxacin (AT-4140, CI-978), PD 131628 (the active form of the prodrug CI-990), temafloxacin, and Win 57273, compared with those of ciprofloxacin and ofloxacin were tested against 53 penicillin-susceptible, 35 penicillin intermediate-resistant, and 51 penicillin-resistant pneumococci. Susceptibility to RP 59500, a new streptogramin, was also tested and compared with those to the quinolones, erythromycin, and vancomycin. All MICs were determined by a standardized agar dilution method by using Mueller-Hinton agar supplemented with sheep blood. Quinolone, vancomycin, and RP 59500 susceptibilities were not affected by susceptibility or resistance to penicillin. For Win 57273, the MICs for 50% (MIC50) and 90% (MIC90) of strains tested were 0.015 and 0.03 micrograms/ml, respectively. MIC50S of both sparfloxacin and PD 131628 were 0.25 micrograms/ml, and MIC90S were 0.5 micrograms/ml. The MIC50 of temafloxacin was 0.5 micrograms/ml, and the MIC90 was 1.0 micrograms/ml. By comparison, ofloxacin and ciprofloxacin both yielded MIC50S of 1.0 micrograms/ml and MIC90s of 2.0 micrograms/ml. RP 59500 yielded an MIC50 of 0.5 microgram/ml and an MIC90 of 1.0 microgram/ml and was only 1 doubling dilution less active against 17 erythromycin-resistant strains. Vancomycin was active against all strains (MIC50, 0.25 microgram/ml; MIC90, 0.5 microgram/ml). All four experimental quinolones as well as RP 59500 show promise for therapy of infections with penicillin-resistant and -susceptible pneumococci.
将四种新喹诺酮类药物,即司帕沙星(AT - 4140,CI - 978)、PD 131628(前体药物CI - 990的活性形式)、替马沙星和Win 57273,与环丙沙星和氧氟沙星的最低抑菌浓度(MIC)进行了比较,测试对象为53株对青霉素敏感、35株对青霉素中度耐药和51株对青霉素耐药的肺炎球菌。还测试了对新型链阳菌素RP 59500的敏感性,并与对喹诺酮类药物、红霉素和万古霉素的敏感性进行了比较。所有MIC均采用标准化琼脂稀释法,使用添加了羊血的Mueller - Hinton琼脂进行测定。喹诺酮类药物、万古霉素和RP 59500的敏感性不受对青霉素敏感或耐药的影响。对于Win 57273,所测试菌株的50%(MIC50)和90%(MIC90)的MIC分别为0.015和0.03微克/毫升。司帕沙星和PD 131628的MIC50均为0.25微克/毫升,MIC90均为0.5微克/毫升。替马沙星的MIC50为0.5微克/毫升,MIC90为1.0微克/毫升。相比之下,氧氟沙星和环丙沙星的MIC50均为1.0微克/毫升,MIC90均为2.0微克/毫升。RP 59500的MIC50为0.5微克/毫升,MIC90为1.0微克/毫升,对17株红霉素耐药菌株的活性仅低1倍稀释度。万古霉素对所有菌株均有活性(MIC50,0.25微克/毫升;MIC90,0.5微克/毫升)。所有四种实验性喹诺酮类药物以及RP 59500在治疗对青霉素耐药和敏感的肺炎球菌感染方面均显示出前景。