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奥昔沙星:临床前和临床疗效评价。

Ozenoxacin: a review of preclinical and clinical efficacy.

机构信息

a Red Española de Investigación en Patología Infecciosa (REIPI) , Madrid , Spain.

b Servei de Microbiología , Centre de Diagnòstic Biomèdic, Hospital Clinic , Barcelona , Spain.

出版信息

Expert Rev Anti Infect Ther. 2019 Mar;17(3):159-168. doi: 10.1080/14787210.2019.1573671. Epub 2019 Feb 11.

DOI:10.1080/14787210.2019.1573671
PMID:30686133
Abstract

Impetigo is the most common bacterial skin infection in children. Treatment is becoming complicated due to the development of antimicrobial resistance, especially in the main pathogen, Staphylococcus aureus. Ozenoxacin, a novel non-fluorinated topical quinolone antimicrobial, has demonstrated efficacy in impetigo. Areas covered: This article reviews the microbiology, pharmacodynamic and pharmacokinetic properties of ozenoxacin, and its clinical and microbiological efficacy in impetigo. Expert opinion: In an environment of increasing antimicrobial resistance and concurrent slowdown in antimicrobial development, the introduction of a new agent is a major event. Ozenoxacin is characterized by simultaneous affinity for DNA gyrase and topoisomerase IV, appears to be impervious to certain efflux pumps that confer bacterial resistance to other quinolones, shows low selection of resistant mutants, and has a mutant prevention concentration below its concentration in skin. These mechanisms protect ozenoxacin against development of resistance, while the absence of a fluorine atom in its structure confers a better safety profile versus fluoroquinolones. In vitro studies have demonstrated high potency of ozenoxacin against staphylococci and streptococci including resistant strains of S. aureus. Clinical trials of ozenoxacin in patients with impetigo reported high clinical and microbiological success rates. Preserving the activity and availability of ozenoxacin through antimicrobial stewardship is paramount.

摘要

脓疱疮是儿童中最常见的细菌性皮肤感染。由于抗菌药物耐药性的发展,特别是主要病原体金黄色葡萄球菌的耐药性发展,治疗变得复杂。噁嗪酮是一种新型非氟喹诺酮类局部抗菌药物,已证明在脓疱疮中具有疗效。

涵盖领域

本文综述了噁嗪酮的微生物学、药效学和药代动力学特性,以及其在脓疱疮中的临床和微生物学疗效。

专家意见

在抗菌药物耐药性不断增加和抗菌药物开发同时放缓的环境下,引入新的药物是一件大事。噁嗪酮的特点是同时与 DNA 回旋酶和拓扑异构酶 IV 结合,似乎不易受到某些外排泵的影响,这些外排泵使其他喹诺酮类药物产生细菌耐药性,显示出低耐药突变选择率,且突变预防浓度低于其在皮肤中的浓度。这些机制使噁嗪酮能够防止耐药性的发展,而其结构中不含氟原子则使其与氟喹诺酮类药物相比具有更好的安全性。体外研究表明,噁嗪酮对葡萄球菌和链球菌具有很高的活性,包括金黄色葡萄球菌的耐药菌株。在脓疱疮患者中进行的噁嗪酮临床试验报告了很高的临床和微生物学治愈率。通过抗菌药物管理来保持噁嗪酮的活性和可用性至关重要。

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