Sanders C C
Department of Medical Microbiology, Creighton University School of Medicine, Omaha, Nebraska 68178.
Rev Infect Dis. 1988 May-Jun;10(3):516-27. doi: 10.1093/clinids/10.3.516.
Ciprofloxacin is a new fluoroquinolone that is highly active against many diverse microorganisms. At concentrations of less than 1 microgram/mL it is active against most gram-negative bacteria, including Enterobacteriaceae, Haemophilus, Neisseria, and other Pasteurellaceae, Vibrionaceae, and various species of Pseudomonas and Acinetobacter. Most staphylococci, including strains resistant to methicillin, are also susceptible to ciprofloxacin. Streptococci are not highly susceptible to ciprofloxacin, and obligate anaerobes are generally resistant to this and other quinolones. Ciprofloxacin, like other quinolones, inhibits DNA gyrase, but its bactericidal effects are not completely reversible by inhibitors of protein or RNA synthesis. Thus, unlike many other quinolones, ciprofloxacin may have multiple lethal effects. Resistance is less readily selected in vitro by ciprofloxacin than by nalidixic acid, and single-step mutants usually remain susceptible to clinically achievable concentrations. Resistance mediated by mutations in genes altering DNA gyrase and expression of outer membrane proteins has been described for ciprofloxacin and other quinolones. The antimicrobial spectrum and potency of ciprofloxacin, coupled with its rapid bactericidal effects, make this fluoroquinolone a promising new antimicrobial agent.
环丙沙星是一种新型氟喹诺酮类药物，对多种不同微生物具有高度活性。在浓度低于1微克/毫升时，它对大多数革兰氏阴性菌有活性，包括肠杆菌科、嗜血杆菌属、奈瑟菌属以及其他巴斯德菌科、弧菌科，还有各种假单胞菌属和不动杆菌属。大多数葡萄球菌，包括耐甲氧西林菌株，也对环丙沙星敏感。链球菌对环丙沙星不太敏感，专性厌氧菌通常对该药及其他喹诺酮类药物耐药。与其他喹诺酮类药物一样，环丙沙星抑制DNA回旋酶，但其杀菌作用不能被蛋白质或RNA合成抑制剂完全逆转。因此，与许多其他喹诺酮类药物不同，环丙沙星可能有多种致死效应。与萘啶酸相比，环丙沙星在体外较不易选择出耐药性，单步突变体通常对临床可达到的浓度仍敏感。已报道环丙沙星和其他喹诺酮类药物存在由改变DNA回旋酶的基因突变和外膜蛋白表达介导的耐药性。环丙沙星的抗菌谱和效力，加上其快速杀菌作用，使这种氟喹诺酮成为一种有前景的新型抗菌药物。
