Suppr超能文献

新型β-内酰胺-β-内酰胺酶抑制剂复方制剂:治疗碳青霉烯类耐药革兰氏阴性病原体的期望。

Novel β-lactam-β-lactamase inhibitor combinations: expectations for the treatment of carbapenem-resistant Gram-negative pathogens.

机构信息

a 1st Department of Internal Medicine-Infectious Diseases , Hygeia General Hospital , Athens , Greece.

b 4th Department of Internal Medicine , University General Hospital ATTIKON, National and Kapodistrian University of Athens , Athens , Greece.

出版信息

Expert Opin Drug Metab Toxicol. 2019 Feb;15(2):133-149. doi: 10.1080/17425255.2019.1563071. Epub 2019 Jan 10.

Abstract

The burden of antimicrobial resistance among Gram-negative bacteria is increasing and growing into a major threat of public health. Treatment options for carbapenem-resistant Enterobacteriaceae are limited and resistance rates to existing compounds are mounting. The pipeline includes only a small number of novel anti-infective agents in development or in the market with promising results against multidrug-resistant (MDR) Gram-negative. Areas covered: Herein the authors present the modern available knowledge regarding novel β-lactam-β-lactamase inhibitors, i.e. mechanisms of action, in vitro activity, current PK/PDs, clinical trials and clinical efficacy against MDR and XDR Gram-negatives, as well as toxicity issues. Expert opinion: Ceftazidime-avibactam and meropenem-vaborbactam are promising therapeutic options as both are active against Enterobacteriaceae producing ESBL, AmpC, and KPC, whereas only avibactam inhibits certain class D β-lactamases, mainly OXA-48. New drugs active against Gram-negative MDR isolates including imipenem/cilastatin with relebactam and avibactam combined with aztreonam or ceftaroline are in different stages of development. However, the disadvantage to be seriously considered by the clinician is that β-lactam/β-lactamase inhibitors are ineffective against metallo-β-lactamases (with the exception of aztreonam-avibactam) as well as Acinetobacter baumannii.

摘要

革兰氏阴性菌的抗菌药物耐药负担正在增加,并成为公共卫生的主要威胁。碳青霉烯类耐药肠杆菌科(Carbapenem-Resistant Enterobacteriaceae,CRE)的治疗选择有限,而现有化合物的耐药率正在上升。在开发或市场上,只有少数新型抗感染药物具有针对多药耐药(Multidrug-Resistant,MDR)革兰氏阴性菌的有前途的结果。

涵盖领域

本文作者介绍了新型β-内酰胺-β-内酰胺酶抑制剂的现有知识,包括作用机制、体外活性、当前的药代动力学/药效学(Pharmacokinetic/pharmacodynamic,PK/PD)、临床试验以及针对 MDR 和 XDR 革兰氏阴性菌的临床疗效,以及毒性问题。

专家观点

头孢他啶-阿维巴坦和美罗培南-沃博巴坦是有前途的治疗选择,因为两者对产生 ESBL、AmpC 和 KPC 的肠杆菌科都有效,而只有阿维巴坦抑制某些 D 类β-内酰胺酶,主要是 OXA-48。针对革兰氏阴性 MDR 分离株的新型药物,包括与雷利巴坦联合的亚胺培南/西司他丁和与阿维巴坦联合的氨曲南或头孢洛林,处于不同的开发阶段。然而,临床医生需要认真考虑的一个缺点是,β-内酰胺/β-内酰胺酶抑制剂对金属β-内酰胺酶(除了阿维巴坦-氨曲南)以及鲍曼不动杆菌无效。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验