Van Bambeke F, Michot J-M, Van Eldere J, Tulkens P M
Unit of Cellular and Molecular Pharmacology, Catholic University of Louvain, Brussels.
Clin Microbiol Infect. 2005 Apr;11(4):256-80. doi: 10.1111/j.1469-0691.2005.01131.x.
Quinolones are one of the largest classes of antimicrobial agents used worldwide. This review considers the quinolones that are available currently and used widely in Europe (norfoxacin, ciprofloxacin, ofloxacin, levofloxacin and moxifloxacin) within their historical perspective, while trying to position them in the context of recent and possible future advances based on an understanding of: (1) their chemical structures and how these impact on activity and toxicity; (2) resistance mechanisms (mutations in target genes, efflux pumps); (3) their pharmacodynamic properties (AUC/MIC and Cmax/MIC ratios; mutant prevention concentration and mutant selection window); and (4) epidemiological considerations (risk of emergence of resistance, clonal spread). Their main indications are examined in relation to their advantages and drawbacks. Overall, it is concluded that these important agents should be used in an educated fashion, based on a careful balance between their ease of use and efficacy vs. the risk of emerging resistance and toxicity. However, there is now substantial evidence to support use of the most potent drug at the appropriate dose whenever this is required.
喹诺酮类是全球使用的最大类抗菌药物之一。本综述从历史角度审视了目前在欧洲广泛使用的喹诺酮类药物（诺氟沙星、环丙沙星、氧氟沙星、左氧氟沙星和莫西沙星），同时基于以下理解将它们置于近期及未来可能进展的背景下：（1）它们的化学结构以及这些结构如何影响活性和毒性；（2）耐药机制（靶基因突变、外排泵）；（3）它们的药效学特性（AUC/MIC和Cmax/MIC比值；突变预防浓度和突变选择窗）；以及（4）流行病学考量（耐药性出现风险、克隆传播）。结合其优缺点对它们的主要适应证进行了研究。总体而言，得出的结论是，这些重要药物应以明智的方式使用，基于其易用性和疗效与出现耐药性及毒性风险之间的谨慎权衡。然而，现在有大量证据支持在需要时以适当剂量使用最有效的药物。
