Sato K, Inoue Y, Fujii T, Aoyama H, Mitsuhashi S
Infection. 1986;14 Suppl 4:S226-30. doi: 10.1007/BF01661277.
The antibacterial activity of ofloxacin against Enterobacteriaceae, Pseudomonas aeruginosa, Haemophilus influenzae, Branhamella catarrhalis, and Neisseria gonorrhoeae was comparable to norfloxacin and enoxacin, and far exceeded the activity of pipemidic acid and nalidixic acid. The activity of ofloxacin was two to eight times less than that of ciprofloxacin. Ofloxacin was more active against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Acinetobacter spp., Legionella spp., and Bacteroides fragilis, than norfloxacin, enoxacin, pipemidic acid and nalidixic acid, and the activity of ofloxacin was comparable to that of ciprofloxacin. Ofloxacin was two to seven times more effective than norfloxacin in systemic infections in mice with S. aureus, Escherichia coli, Serratia marcescens and P. aeruginosa. Ofloxacin strongly inhibited DNA supercoiling activity of DNA gyrase purified from E. coli KL-16. There is a parallel relationship between antibacterial activity of ofloxacin and its inhibitory action against DNA gyrases from ofloxacin-susceptible and ofloxacin-resistant clinical isolates of E. coli. These results indicate that the high bactericidal action of ofloxacin and the related new quinolone agents can be explained by their potent inhibitory activities against DNA gyrase in bacterial cells.
氧氟沙星对肠杆菌科细菌、铜绿假单胞菌、流感嗜血杆菌、卡他布兰汉菌和淋病奈瑟菌的抗菌活性与诺氟沙星和依诺沙星相当，且远远超过吡哌酸和萘啶酸的活性。氧氟沙星的活性比环丙沙星低2至8倍。与诺氟沙星、依诺沙星、吡哌酸和萘啶酸相比，氧氟沙星对金黄色葡萄球菌、表皮葡萄球菌、肺炎链球菌、不动杆菌属、军团菌属和脆弱拟杆菌更具活性，且氧氟沙星的活性与环丙沙星相当。在患有金黄色葡萄球菌、大肠杆菌、粘质沙雷氏菌和铜绿假单胞菌的小鼠全身性感染中，氧氟沙星的疗效比诺氟沙星高2至7倍。氧氟沙星强烈抑制从大肠杆菌KL-16纯化的DNA旋转酶的DNA超螺旋活性。氧氟沙星的抗菌活性与其对氧氟沙星敏感和耐药的大肠杆菌临床分离株的DNA旋转酶的抑制作用之间存在平行关系。这些结果表明，氧氟沙星及相关新喹诺酮类药物的高杀菌作用可通过它们对细菌细胞中DNA旋转酶的有效抑制活性来解释。
