妥舒沙星的体内外抗菌作用研究

测定妥舒沙星的体内外抗菌活性。以同类氟喹诺酮类及其他抗菌药物为对照，测定了６８９株临床分离菌对药物的敏感性，结果显示，妥舒沙星对需氧革兰氏阳性球菌（除ＭＲＳＡ外）均有良好的抗菌作用，对金葡球菌、肺炎球菌和溶血性链球菌的抗菌活性高；妥舒沙星对需氧革兰氏阴性菌具强大的抗菌作用，对肠杆菌科细菌、流感杆菌和淋球菌的抗菌作用尤强；妥舒沙星对脆弱拟杆菌等厌氧菌亦具良好抗菌作用。妥舒沙星对需氧革兰氏阳性球菌及厌氧菌的作用明显优于环丙沙星、氧氟沙星和诺氟沙星，对需氧革兰氏阴性杆菌的作用与其他受试氟喹诺酮类相仿。妥舒沙星对小鼠实验性细菌感染具有明显保护作用，口服或静注妥舒沙星对金葡球菌的体内抗菌作用明显优于环丙沙星；对大肠埃希氏菌的抗菌作用优于或与环丙沙星相似；对铜绿假单胞菌的作用与环丙沙星相似。

In vitro and in vivo activity of tosufloxacin

The in vitro and in vivo activity of tosufloxacin was evaluated and compared with that of ciprofloxacin, ofloxacin, norfloxacin and other antibacterial agents. The in vitro susceptibility of tosufloxacin against 689 clinical isolates was determined. Tosufloxacin was highly active against aerobic gram negative organisms especially Enterobacteriaceae, H.influenzae and N.gonorrhoeae . It also had good activity against aerobics gram positive orgainisms (except methicillin resistant Staphylococcus) and anaerobes, inclucling B.fragilis . The activity of tosufloxacin against aerobic gram positive organisms and anaerobes was superior to that of ciprofloxacin, ofloxacin and norfloxacin. The activity of tosufloxacin against aerobic gram negative bacteria was simmlar to the other fluoroquinolones tested. Tosufloxacin showed excellent therapeutic effect on experimental infections of mice. The in vivo activity of tosufloxacin against Staphylococcus aureus was superior to that of ciprofoxacin; superior or simmilar to that of E.coli and almost equal to that of Pseudomonas aeruginosa .