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上世纪90年代上市了10余种喹诺酮类药物,其中有若干品种抗肺炎链球菌和厌氧菌活性显著提高,并基本上保留了环丙沙星等第Ⅲ代喹诺酮类的抗G~-杆菌活性,而且对呼吸道非典型病原体亦具良好活性,因而被称为“呼吸”喹诺酮类,其主要药物有司帕沙星(Sparfloxacin)、格帕沙星(grepafloxacin)、加替沙星(gafifloxacin)、莫西沙星(moxifloxacin)、吉米沙星(gemifloxacin),多数文献将左氧氟沙星(levofloxacin)亦包括在内。但是司帕沙星因光毒性及与茶碱药物的相互作用相当突出、格帕沙星心脏不良反应(Q-T间期延长和心律紊乱)发生率高而被限制应用指征或撤回批文,吉美沙星完成Ⅱ、Ⅲ期临床试验,仍有待批准。因此呼吸喹诺酮目前主要指加替沙星和莫西沙星和左氧氟沙星。
More than 10 quinolones were marketed in the 1990s, with several of them significantly increasing their activity against S. pneumoniae and anaerobic bacteria and basically retaining the third generation quinolone antibacterials such as ciprofloxacin Activity, but also for respiratory atypical pathogens also have good activity, which is called “breathing” quinolones, the main drugs are sparfloxacin, grepafloxacin, gatifloxacin, gafifloxacin, Moxifloxacin, gemifloxacin, most of which also include levofloxacin. However, sparfloxacin is very limited due to phototoxicity and the significant interaction with theophylline drugs and the high incidence of heart adverse reactions (prolongation of QT interval and arrhythmia) of grepafloxacin. Application indications or withdrawal of approval, Star completed Ⅱ, Ⅲ clinical trials, remains to be approved. Therefore respiratory quinolone currently refers mainly to gatifloxacin and moxifloxacin and levofloxacin.