Eliopoulos G M, Gardella A, Moellering R C
Antimicrob Agents Chemother. 1984 Mar;25(3):331-5. doi: 10.1128/AAC.25.3.331.
The in vitro activity of ciprofloxacin (Bay o 9867), a new carboxyquinoline antimicrobial agent, was compared with those of norfloxacin, nalidixic acid, and several other oral and parenteral antimicrobial agents. Ciprofloxacin was substantially more active than nalidixic acid or cinoxacin against all gram-negative bacteria tested. Virtually all strains of Enterobacteriaceae were inhibited by the new drug at concentrations of less than or equal to 0.125 micrograms/ml. Ciprofloxacin was more active than norfloxacin against Klebsiella sp., Enterobacter sp., and Serratia marcescens, and it was the most active agent against Pseudomonas aeruginosa (MIC90, 0.5 micrograms/ml). The new drug also demonstrated significant activity against gram-positive cocci, inhibiting all strains of staphylococci at concentrations of less than or equal to 1.0 microgram/ml. Ciprofloxacin was bactericidal at concentrations near the MIC against most isolates tested. Although stepwise increases in resistance were seen with Escherichia coli and P. aeruginosa during serial passage on plates containing incremental concentrations of the drug, significant resistance did not emerge during incubation of strains in broth containing concentrations of ciprofloxacin above the MBC.
将新型羧基喹啉抗菌剂环丙沙星(Bay o 9867)的体外活性与诺氟沙星、萘啶酸及其他几种口服和胃肠外抗菌剂的活性进行了比较。环丙沙星对所有测试的革兰氏阴性菌的活性明显高于萘啶酸或西诺沙星。实际上,所有肠杆菌科菌株在浓度小于或等于0.125微克/毫升时均被该新药抑制。环丙沙星对克雷伯菌属、肠杆菌属和粘质沙雷氏菌的活性高于诺氟沙星,且是对铜绿假单胞菌活性最强的药物(MIC90为0.5微克/毫升)。该新药对革兰氏阳性球菌也显示出显著活性,在浓度小于或等于1.0微克/毫升时可抑制所有葡萄球菌菌株。环丙沙星在接近MIC的浓度下对大多数测试分离株具有杀菌作用。尽管在含有递增浓度该药物的平板上连续传代期间,大肠杆菌和铜绿假单胞菌出现了逐步耐药性增加,但在含有高于MBC浓度环丙沙星的肉汤中培养菌株期间,未出现显著耐药性。