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索利霉素在细菌性社区获得性肺炎管理中的作用。

The role of solithromycin in the management of bacterial community-acquired pneumonia.

机构信息

a Pharmacologie cellulaire et moléculaire , Louvain Drug Research Institute, Université catholique de Louvain , Brussels , Belgium.

出版信息

Expert Rev Anti Infect Ther. 2016;14(3):311-24. doi: 10.1586/14787210.2016.1138857. Epub 2016 Feb 5.

Abstract

The fluoroketolide solithromycin is 2-fold more potent in vitro than telithromycin against pneumococci (including macrolide-resistant strains) and Haemophilus influenzae and very active on pathogens causing atypical pneumonia. In contrast, it is a 30-fold less potent inhibitor of nicotinic receptors incriminated in telithromycin toxicity. In Phase II/III trials, oral solithromycin once-daily (800 mg on day 1; 400 mg on days 2-5) proved effective and safe when compared to respiratory fluoroquinolones for the treatment of community-acquired bacterial pneumonia (CABP). A Phase III intravenous trial vs. moxifloxacin has been recently completed for the same indication. Solithromycin may restore interest in ketolides as a first-line therapy for CAPB. Solithromycin safety should nevertheless be confirmed in larger populations allowing for detection of rare adverse events.

摘要

氟喹诺酮类药物索利霉素在体外对肺炎球菌(包括大环内酯类耐药株)和流感嗜血杆菌的活性比泰利霉素强 2 倍,对引起非典型肺炎的病原体非常有效。相比之下,它对引起泰利霉素毒性的烟碱受体的抑制作用要弱 30 倍。在 II/III 期临床试验中,与呼吸氟喹诺酮类药物相比,口服索利霉素(第 1 天 800mg,第 2-5 天 400mg)每日一次治疗社区获得性细菌性肺炎(CABP)有效且安全。最近已完成一项针对同一适应证的索利霉素与莫西沙星的 III 期静脉试验。索利霉素可能会重新引起人们对酮内酯类药物作为 CAPB 一线治疗的兴趣。然而,应在更大的人群中确认索利霉素的安全性,以便发现罕见的不良事件。

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