Dubois J, St-Pierre C
Novabyss Inc., Centre Universitaire de Santé de l'Estrie, 614 rue Bowen Sud, Sherbrooke, Québec J1G 2E9, Canada.
J Antimicrob Chemother. 2000 Apr;45 Suppl 1:41-6. doi: 10.1093/jac/45.suppl_3.41.
The comparative in vitro potency and post-antibiotic effect (PAE) of gemifloxacin (SB-265805), moxifloxacin, trovafloxacin, grepafloxacin, levofloxacin, ofloxacin, ciprofloxacin, azithromycin, clarithromycin, erythromycin and rifampicin were evaluated against Legionella pneumophila serogroups 1-9 and 12 (n = 204) and other Legionella spp. (n = 34). MICs were determined by standard two-fold agar dilution. PAE was determined by exposing the isolates to the test agents at 4 x MIC for 1 h. Trovafloxacin was the most potent agent overall (MIC range < or =0.004-0.016 mg/L, MIC(90) < or =0.008 mg/L). Of the other quinolones tested, gemifloxacin, moxifloxacin, grepafloxacin and levofloxacin were more potent (MIC(90) 0.016 mg/L) against L. pneumophila than ciprofloxacin and ofloxacin (MIC(90) 0. 03 mg/L). Against Legionella spp., the test quinolones were more potent (MIC range < or =0.004-0.06 mg/L) than either erythromycin or azithromycin (MIC(90) 0.5 and 0.25 mg/L, respectively). Gemifloxacin had the longest PAE (4.65 h) of the agents tested against erythromycin-resistant L. pneumophila. Of the quinolones, only gemifloxacin, grepafloxacin, levofloxacin and ofloxacin had PAEs of >3 h against erythromycin-resistant Legionella spp. Azithromycin, erythromycin and clarithromycin had PAEs of <3 h against all erythromycin-resistant strains. Against erythromycin-susceptible L. pneumophila, only gemifloxacin, moxifloxacin, ofloxacin and ciprofloxacin had PAEs of >3 h, and only rifampicin, ofloxacin, gemifloxacin and erythromycin had PAEs of >2 h against erythromycin-susceptible Legionella spp. The superior potency of gemifloxacin compared with erythromycin indicates that it may be of use in the treatment of legionellosis. The significant PAE described here, combined with favourable pharmacokinetics, supports once-daily dosing for gemifloxacin in the treatment of legionella infections.
对吉米沙星（SB - 265805）、莫西沙星、曲伐沙星、格帕沙星、左氧氟沙星、氧氟沙星、环丙沙星、阿奇霉素、克拉霉素、红霉素和利福平进行了体外抗菌效力比较及抗生素后效应（PAE）评估，受试菌株为嗜肺军团菌血清型1 - 9和12（n = 204）以及其他军团菌属（n = 34）。MIC通过标准的两倍琼脂稀释法测定。PAE通过将分离菌株暴露于4倍MIC的受试药物中1小时来测定。总体而言，曲伐沙星是最有效的药物（MIC范围≤0.004 - 0.016mg/L，MIC90≤0.008mg/L）。在所测试的其他喹诺酮类药物中，吉米沙星、莫西沙星、格帕沙星和左氧氟沙星对嗜肺军团菌的抗菌效力强于环丙沙星和氧氟沙星（MIC90为0.03mg/L）。对于军团菌属，受试喹诺酮类药物的抗菌效力更强（MIC范围≤0.004 - 0.06mg/L），强于红霉素或阿奇霉素（MIC90分别为0.5和0.25mg/L）。在针对耐红霉素的嗜肺军团菌测试的药物中，吉米沙星的PAE最长（4.65小时）。在喹诺酮类药物中，只有吉米沙星、格帕沙星、左氧氟沙星和氧氟沙星对耐红霉素的军团菌属的PAE大于3小时。阿奇霉素、红霉素和克拉霉素对所有耐红霉素菌株的PAE均小于3小时。对于对红霉素敏感的嗜肺军团菌，只有吉米沙星、莫西沙星、氧氟沙星和环丙沙星的PAE大于3小时，对于对红霉素敏感的军团菌属，只有利福平、氧氟沙星、吉米沙星和红霉素的PAE大于2小时。吉米沙星相对于红霉素的优越抗菌效力表明它可能可用于治疗军团菌病。此处描述的显著PAE，结合良好的药代动力学，支持吉米沙星在治疗军团菌感染时每日给药一次。
