History of quinolones and their side effects
History of quinolones and their side effects
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DOI：
10.1159/000057838
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发表时间：
2001-01-01
期刊：
影响因子：
3.3
通讯作者：
Rubinstein, E
中科院分区：
文献类型：
--
作者：
Rubinstein, E
本文综述了1985年至今氟喹诺酮类药物的研究进展。依诺沙星、培氟沙星和氟罗沙星的严重药物不良事件均具有光毒性。替马氟沙星与重度溶血性尿毒症综合征相关，洛美沙星引起光毒性和中枢神经系统（CNS）效应，司帕沙星与光毒性和QTc延长相关。妥舒沙星引起重度血小板减少症和肾炎，曲伐沙星报告了肝毒性。格帕沙星因心血管效应而停药，克林沙星与光毒性和低血糖相关。喹诺酮类药物的结构直接关系到其活性和副作用。阐明了喹诺酮类化合物中特定取代基之间的关系。在日本进行的一项为期5年的上市后监测（PMS）研究中，审查了与单种氟喹诺酮类药物相关的特定不良事件的发生率，其中左氧氟沙星的总药物不良反应（ADR）率为1.3%，而帕珠沙星的总ADR率为33%，托舒沙星为3.6%，加替沙星为4.5%，巴洛沙星为5.4%。胃肠道反应是所有氟喹诺酮类药物最常见的不良事件。在列出的药物中，左氧氟沙星的CNS效应和皮肤不良事件发生率最低。版权所有（C）2001 S. Karger AG，巴塞尔。
Fluoroquinolone development from 1985 to the present was reviewed. Severe drug adverse events were noted for enoxacin, pefloxacin and fleroxacin, which were phototoxic. Temafloxacin was associated with severe hemolytic-uremic syndrome, lomefloxacin caused phototoxicity and central nervous system (CNS) effects, and sparfloxacin was associated with phototoxicity and QTc prolongation. Tosufloxacin caused severe thrombocytopenia and nephritis, and hepatotoxicity was reported for trovafloxacin. Grepafloxacin was withdrawn due to cardiovascular effects, and clinafloxacin was associated with phototoxicity and hypoglycaemia. The structure of the quinolones directly relates to both their activity and side-effect profiles. The relationship among specific substituents attached to the quinolone nucleus are clarified. The incidence of specific adverse events associated with individual fluoroquinolones was reviewed in a five-year post-marketing surveillance (PMS) study in Japan, in which a total adverse drug reaction ADR) rate of 1.3% was found for levofloxacin, compared to total ADR rates of 33% for pazufloxacin, 3.6% for tosufloxacin, 4.5% for gatifloxacin and 5.4% for balofloxacin. Gastrointestinal effects were the most common adverse events for all fluoroquinolones. Levofloxacin had the lowest rate of CNS effects and skin adverse events among the agents listed. Copyright (C) 2001 S. Karger AG, Basel.