Ford A S, Baltch A L, Smith R P, Ritz W
Department of Medicine, Stratton VA Medical Center, Albany, New York.
J Antimicrob Chemother. 1993 Apr;31(4):523-32. doi: 10.1093/jac/31.4.523.
The in-vitro activities of two new fluoroquinolones, clinafloxacin (CI-960, PD 127391, AM-1091) and PD 131628 (the active component of the pro-drug CI-990, PD 131112) and nine other antibiotics were tested against 107 clinical isolates of Pseudomonas aeruginosa, 12 isolates of Xanthomonas maltophilia, and 19 isolates of other Pseudomonas spp. Of the 107 P. aeruginosa isolates, 33 were resistant to gentamicin, tobramycin and amikacin, 17 were resistant to only one or two of these aminoglycosides and 24 were aminoglycoside sensitive. Thirty-three were isolates from cystic fibrosis patients. Susceptibility studies were performed using the agar dilution technique and kinetic time kill curves. With the exception of aminoglycoside-sensitive P. aeruginosa isolates where ciprofloxacin had similar activity to clinafloxacin and PD 131628, the two new fluoroquinolones were the most active agents against all isolates tested (MIC90 0.25-2.0 mg/L). Cross-resistance was identified with ciprofloxacin and ofloxacin-resistant strains, but the superior activity of clinafloxacin and PD 131628 resulted in 90% of the isolates having MICs < 2 mg/L. Kinetic kill curves with aminoglycoside-sensitive P. aeruginosa revealed ciprofloxacin to have the most rapid and sustained killing. However, with amino-glycoside-resistant P. aeruginosa isolates, clinafloxacin and PD 131628 were more rapidly bactericidal than ciprofloxacin.
测试了两种新型氟喹诺酮类药物克林沙星(CI-960、PD 127391、AM-1091)和PD 131628(前体药物CI-990、PD 131112的活性成分)以及其他九种抗生素对107株铜绿假单胞菌临床分离株、12株嗜麦芽窄食单胞菌分离株和19株其他假单胞菌属分离株的体外活性。在107株铜绿假单胞菌分离株中,33株对庆大霉素、妥布霉素和阿米卡星耐药,17株仅对其中一两种氨基糖苷类药物耐药,24株对氨基糖苷类药物敏感。33株分离自囊性纤维化患者。采用琼脂稀释技术和动态时间杀菌曲线进行药敏研究。除氨基糖苷类敏感的铜绿假单胞菌分离株外,环丙沙星与克林沙星和PD 131628活性相似,这两种新型氟喹诺酮类药物是对所有测试分离株活性最强的药物(MIC90为0.25 - 2.0 mg/L)。在环丙沙星和氧氟沙星耐药菌株中发现了交叉耐药性,但克林沙星和PD 131628的优越活性导致90%的分离株MICs < 2 mg/L。对氨基糖苷类敏感的铜绿假单胞菌的动态杀菌曲线显示环丙沙星具有最快和最持久的杀菌效果。然而,对于氨基糖苷类耐药的铜绿假单胞菌分离株,克林沙星和PD 131628比环丙沙星杀菌更快。