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德拉氟沙星治疗急性细菌性皮肤及皮肤结构感染的临床和药代动力学药物评价

Clinical and pharmacokinetic drug evaluation of delafloxacin for the treatment of acute bacterial skin and skin structure infections.

作者信息

Bassetti Matteo, Pecori Davide, Cojutti Piergiorgio, Righi Elda, Pea Federico

机构信息

a Infectious Diseases Clinic, Department of Medicine , University of Udine and Azienda Sanitaria Universitaria Integrata di Udine , Udine , Italy.

b Department of Medicine , Institute of Clinical Pharmacology, 'Santa Maria della Misericordia' University Hospital, ASUIUD , Udine , Italy.

出版信息

Expert Opin Drug Metab Toxicol. 2017 Nov;13(11):1193-1200. doi: 10.1080/17425255.2017.1386654. Epub 2017 Oct 14.

Abstract

In the era of multi-drug resistant pathogens, the adequate treatment of skin and skin structure infections remains a challenge for clinicians. Delafloxacin, with its broad spectrum against Gram-positive, Gram-negative and anaerobic organisms, represents a new therapeutic option in this setting, especially when coverage of methicillin-resistant Staphylococcus aureus is required in the empirical or targeted approach. Areas covered: In this drug evaluation, the Authors have reviewed the pharmacokinetic and pharmacodynamic characteristics of delafloxacin. In addition, recent data on clinical efficacy and safety from clinical trials have been included. Expert opinion: Delafloxacin represents an attractive therapeutic option due to a broad antimicrobial and favorable pharmacokinetic and pharmacodynamic profile. Several in vitro studies have demonstrated the low potential for resistance selection if used in empirical regimens. Delafloxacin is a promising candidate for the treatment of Gram-positive infections, especially if co-infection with other pathogens is suspected. This is because of the very low MIC of the agent for Gram-positive (including MRSA) and anaerobic bacteria and because of the wide spectrum of activity against Gram-negative organisms. For these interesting microbiological and PK/PD characteristics we expect future uses of this drug in other indications such as diabetic foot infection, osteomyelitis, prosthetic joint infections, abdominal infections and central nervous system infections.

摘要

在多重耐药病原体的时代,皮肤及皮肤结构感染的充分治疗对临床医生而言仍是一项挑战。达氟沙星对革兰氏阳性菌、革兰氏阴性菌及厌氧菌具有广谱抗菌活性,在此背景下代表了一种新的治疗选择,尤其是在经验性或靶向性治疗方法中需要覆盖耐甲氧西林金黄色葡萄球菌时。涵盖领域:在本次药物评估中,作者回顾了达氟沙星的药代动力学和药效学特征。此外,还纳入了近期临床试验中有关临床疗效和安全性的数据。专家观点:由于具有广泛的抗菌活性以及良好的药代动力学和药效学特征,达氟沙星是一种有吸引力的治疗选择。多项体外研究表明,若用于经验性治疗方案,其产生耐药性的可能性较低。达氟沙星是治疗革兰氏阳性菌感染的有前景的候选药物,尤其是在怀疑合并其他病原体感染时。这是因为该药物对革兰氏阳性菌(包括耐甲氧西林金黄色葡萄球菌)和厌氧菌的最低抑菌浓度非常低,且对革兰氏阴性菌具有广泛的抗菌活性。鉴于这些有趣的微生物学和药代动力学/药效学特征,我们期待该药物在未来用于其他适应症,如糖尿病足感染、骨髓炎、人工关节感染、腹腔感染和中枢神经系统感染。

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