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口服杀菌剂左氧氟沙星满足耐多药革兰氏阳性菌感染管理中未被满足的需求

Meeting the Unmet Need in the Management of MDR Gram-Positive Infections with Oral Bactericidal Agent Levonadifloxacin.

作者信息

Mehta Yatin, Mishra K C, Paliwal Yashesh, Rangappa Pradeep, Sinha Sharmili, Bhapkar Sandeep

机构信息

Medanta the Medicity, Gurgaon, India.

Yashoda Hospital, Secunderabad, India.

出版信息

Crit Care Res Pract. 2022 Sep 9;2022:2668199. doi: 10.1155/2022/2668199. eCollection 2022.

Abstract

Levonadifloxacin (intravenous) and its oral prodrug alalevonadifloxacin are broad-spectrum antibacterial agents developed for the treatment of difficult-to-treat infections caused by multidrug-resistant Gram-positive bacteria, especially methicillin-resistant , atypical bacteria, anaerobic bacteria, and biodefence pathogens as well as Gram-negative bacteria. Levonadifloxacin has a well-defined mechanism of action involving a strong affinity for DNA gyrase as well as topoisomerase IV. Alalevonadifloxacin with widely differing solubility and oral bioavailability has pharmacokinetic profile identical to levonadifloxacin. Unlike existing MRSA drugs such as vancomycin and linezolid, which cause unfavorable side effects like nephrotoxicity, bone-marrow toxicity, and muscle toxicity, levonadifloxacin/alalevonadifloxacin has demonstrated superior safety and tolerability features with no serious adverse events. Levonadifloxacin/alalevonadifloxacin could be a useful weapon in the battle against infections caused by resistant microorganisms and could be a preferred antibiotic of choice for empirical therapy in the future.

摘要

左氧氟沙星(静脉注射用)及其口服前药阿拉左氧氟沙星是开发用于治疗由多重耐药革兰氏阳性菌引起的难治性感染的广谱抗菌剂,尤其是耐甲氧西林菌、非典型细菌、厌氧菌、生物防御病原体以及革兰氏阴性菌。左氧氟沙星具有明确的作用机制,对DNA旋转酶以及拓扑异构酶IV具有很强的亲和力。溶解度和口服生物利用度差异很大的阿拉左氧氟沙星具有与左氧氟沙星相同的药代动力学特征。与现有耐甲氧西林金黄色葡萄球菌(MRSA)药物如万古霉素和利奈唑胺不同,后者会引起肾毒性、骨髓毒性和肌肉毒性等不良副作用,而左氧氟沙星/阿拉左氧氟沙星已显示出卓越的安全性和耐受性,无严重不良事件。左氧氟沙星/阿拉左氧氟沙星可能是对抗耐药微生物引起的感染的有用武器,并且可能成为未来经验性治疗的首选抗生素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/032e/9922174/9bb94c499357/CCRP2022-2668199.001.jpg

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