Heifetz C L, Bien P A, Cohen M A, Dombrowski M E, Griffin T J, Malta T E, Sesnie J C, Shapiro M A, Wold S A
Parke-Davis Pharmaceutical Research Division, Ann Arbor, MI.
J Antimicrob Chemother. 1988 Feb;21 Suppl B:29-42. doi: 10.1093/jac/21.suppl_b.29.
Enoxacin was evaluated in in-vitro tests and in studies of effectiveness and blood concentrations in the mouse. Enoxacin was active against both susceptible and multiresistant hospital isolates of Enterobacteriaceae, Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria gonorrhoeae and staphylococci. Less susceptible were streptococci and anaerobes. Of nine quinolones tested, only norfloxacin was equivalent in vitro. The MBCs of enoxacin were one- to twofold greater than the MICs, and enoxacin was rapidly bactericidal. No single-step resistant mutants could be detected at 10 mg/l against large inocula and six to 11 steps were required for selection of resistant clones. In systemic mouse infections, enoxacin was effective in a single oral or subcutaneous dose against one strain each of Enterobacter cloacae, Escherichia coli, Klebsiella pneumoniae, Providencia rettgeri and Ps. aeruginosa, and two Staphylococcus aureus strains. Single oral and subcutaneous enoxacin doses (50 mg/kg) gave peak mouse blood levels of 4.9 and 9.5 mg/l and an elimination half-life of 1.8 h.
对依诺沙星进行了体外试验以及在小鼠身上的有效性和血药浓度研究。依诺沙星对肠道杆菌科、铜绿假单胞菌、流感嗜血杆菌、淋病奈瑟菌和葡萄球菌的易感及多重耐药医院分离株均有活性。链球菌和厌氧菌的敏感性较低。在所测试的9种喹诺酮类药物中，只有诺氟沙星在体外具有同等效力。依诺沙星的最低杀菌浓度（MBC）比最低抑菌浓度（MIC）高1至2倍，且依诺沙星具有快速杀菌作用。在10mg/l浓度下，针对大量接种菌无法检测到单步耐药突变体，选择耐药克隆需要6至11步。在小鼠全身感染中，依诺沙星单剂量口服或皮下给药对阴沟肠杆菌、大肠埃希菌、肺炎克雷伯菌、雷氏普罗威登斯菌和铜绿假单胞菌各一株以及两株金黄色葡萄球菌均有效。依诺沙星单剂量口服和皮下给药（50mg/kg）时，小鼠血药峰值浓度分别为4.9mg/l和9.5mg/l，消除半衰期为1.8小时。
