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Tigecycline antibacterial activity, clinical effectiveness, and mechanisms and epidemiology of resistance: narrative review
European Journal of Clinical Microbiology & Infectious Diseases ( IF 4.5 ) Pub Date : 2021-01-05 , DOI: 10.1007/s10096-020-04121-1
Sajad Yaghoubi 1 , Angelina Olegovna Zekiy 2 , Marcela Krutova 3 , Mehrdad Gholami 4 , Ebrahim Kouhsari 5, 6 , Mohammad Sholeh 7 , Zahra Ghafouri 8 , Farajolah Maleki 9
Affiliation  

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.



中文翻译:

替加环素的抗菌活性、临床疗效、耐药机制和流行病学:叙述性综述

替加环素是一种独特的甘氨酰环素类半合成抗菌剂,用于治疗由多重耐药革兰氏阳性和革兰氏阴性病原体引起的多种微生物感染。替加环素通过在米诺环素的 9 位添加甘环酰胺部分来逃避主要的四环素耐药遗传机制,例如四环素特异性外排泵获取和核糖体保护。替加环素的肠胃外形式的使用被批准用于成人复杂的皮肤和皮肤结构感染(不包括糖尿病足部感染)、复杂的腹腔内感染和社区获得性细菌性肺炎。新证据还表明替加环素治疗严重艰难梭菌的有效性感染。替加环素在体外对柯克氏菌属立克次氏菌属和耐多药淋病奈瑟菌菌株显示出敏感性,这表明替加环素可能用于治疗由这些病原体引起的感染。除了在某些革兰氏阴性菌中固有的或经常报道的耐药性外,替加环素对广泛的多药耐药医院病原体有效。在此,我们总结了目前可用的关于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及其临床有效性的数据。

更新日期:2021-01-06
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