Kaatz G W, Seo S M, Lamp K C, Bailey E M, Rybak M J
Department of Internal Medicine, Wayne State University School of Medicine, Detroit, Michigan.
Antimicrob Agents Chemother. 1992 Jun;36(6):1192-7. doi: 10.1128/AAC.36.6.1192.
CI-960 is a new fluoroquinolone with enhanced in vitro activity against gram-positive pathogens. The efficacy of the drug was compared with that of vancomycin by using the rabbit model of nafcillin- and ciprofloxacin-susceptible and -resistant Staphylococcus aureus endocarditis. Animals received intravenous therapy with CI-960, 20 mg/kg of body weight every 8 h, or vancomycin, 17.5 mg/kg every 6 h, for 4 days. In a comparison with the effects on untreated controls, both antimicrobial agents effectively cleared bacteremia and significantly reduced bacterial counts in vegetations and tissues of animals infected with any of the test strains. In some cases, the efficacy of CI-960 was superior to that of vancomycin. The therapeutic activity of CI-960 was reduced, but still very good, against ciprofloxacin-resistant strains. One rabbit infected with such a strain and treated with CI-960 was found to harbor a small number of vegetation-associated organisms resistant to the drug at fivefold its original MIC; this was associated with a microbiological, but not a clinical, failure of therapy. We conclude that CI-960 is as effective as vancomycin is in this model of a serious systemic S. aureus infection, including that caused by strains resistant to ciprofloxacin. Increases in CI-960 MICs may develop during therapy of infections caused by strains highly resistant to ciprofloxacin, but they appear unlikely to occur in ciprofloxacin-susceptible strains.
CI-960是一种新型氟喹诺酮类药物,对革兰氏阳性病原体具有增强的体外活性。通过使用对萘夫西林和环丙沙星敏感及耐药的金黄色葡萄球菌心内膜炎兔模型,将该药物的疗效与万古霉素进行了比较。动物接受静脉治疗,CI-960为每8小时20mg/kg体重,万古霉素为每6小时17.5mg/kg,持续4天。与对未治疗对照的影响相比,两种抗菌药物均有效清除菌血症,并显著降低感染任何测试菌株的动物赘生物和组织中的细菌数量。在某些情况下,CI-960的疗效优于万古霉素。CI-960对环丙沙星耐药菌株的治疗活性有所降低,但仍然很好。发现一只感染此类菌株并用CI-960治疗的兔子,其赘生物相关的一小部分生物体对该药物的耐药性是其原始最低抑菌浓度的五倍;这与治疗的微生物学失败相关,但与临床失败无关。我们得出结论,在这种严重的全身性金黄色葡萄球菌感染模型中,包括由对环丙沙星耐药的菌株引起的感染,CI-960与万古霉素一样有效。在由对环丙沙星高度耐药的菌株引起的感染治疗过程中,CI-960的最低抑菌浓度可能会升高,但在对环丙沙星敏感的菌株中似乎不太可能发生。