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替加环素的抗菌活性、临床疗效以及耐药机制和流行病学:叙述性综述。

Tigecycline antibacterial activity, clinical effectiveness, and mechanisms and epidemiology of resistance: narrative review.

机构信息

Department of Clinical Microbiology, Iranshahr University of Medical Sciences, Iranshahr, Iran.

Department of Prosthetic Dentistry, Sechenov First Moscow State Medical University, Russian Federation, Trubetskaya st., 8-2, 119991, Moscow, Russia.

出版信息

Eur J Clin Microbiol Infect Dis. 2022 Jul;41(7):1003-1022. doi: 10.1007/s10096-020-04121-1. Epub 2021 Jan 5.

Abstract

Tigecycline is unique glycylcycline class of semisynthetic antimicrobial agents developed for the treatment of polymicrobial infections caused by multidrug-resistant Gram-positive and Gram-negative pathogens. Tigecycline evades the main tetracycline resistance genetic mechanisms, such as tetracycline-specific efflux pump acquisition and ribosomal protection, via the addition of a glycyclamide moiety to the 9-position of minocycline. The use of the parenteral form of tigecycline is approved for complicated skin and skin structure infections (excluding diabetes foot infection), complicated intra-abdominal infections, and community-acquired bacterial pneumonia in adults. New evidence also suggests the effectiveness of tigecycline for the treatment of severe Clostridioides difficile infections. Tigecycline showed in vitro susceptibility to Coxiella spp., Rickettsia spp., and multidrug-resistant Neisseria gonnorrhoeae strains which indicate the possible use of tigecycline in the treatment of infections caused by these pathogens. Except for intrinsic, or often reported resistance in some Gram-negatives, tigecycline is effective against a wide range of multidrug-resistant nosocomial pathogens. Herein, we summarize the currently available data on tigecycline pharmacokinetics and pharmacodynamics, its mechanism of action, the epidemiology of tigecycline resistance, and its clinical effectiveness.

摘要

替加环素是一种独特的甘氨酰环素类半合成抗菌药物,用于治疗由多药耐药革兰阳性和革兰阴性病原体引起的混合感染。替加环素通过在米诺环素的 9 位添加甘氨酰环酰胺部分,规避了主要的四环素耐药遗传机制,如四环素特异性外排泵的获得和核糖体保护。替加环素的注射剂型被批准用于治疗复杂性皮肤和皮肤结构感染(不包括糖尿病足感染)、复杂性腹腔内感染和成人获得性细菌性肺炎。新的证据还表明替加环素在治疗严重艰难梭菌感染方面的有效性。替加环素在体外对柯克斯体、立克次体和多药耐药淋病奈瑟菌菌株具有敏感性,这表明替加环素可能用于治疗这些病原体引起的感染。除了某些革兰氏阴性菌中固有或经常报道的耐药性外,替加环素对多种多药耐药医院获得性病原体均有效。本文总结了替加环素药代动力学和药效学、作用机制、替加环素耐药的流行病学以及临床疗效方面的现有数据。

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