头孢吡肟/恩美唑巴坦:微生物学、药代动力学、药效学和临床评估。

Christopher A Darlow, William Hope, Vineet Dubey
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引用次数: 0

摘要

简介头孢吡肟/恩美唑巴坦是一种新型β-内酰胺/β-内酰胺酶抑制剂(BL-BLI)组合,具有广泛的革兰氏阳性和阴性活性。头孢吡肟对 AmpC 的水解具有较强的抵抗力,而恩美唑巴坦对所有 Ambler A 类广谱β-内酰胺酶(ESBLs)均有抑制作用。因此,该组合对许多 ESBLs 的水解具有抗性。重要的广谱缺口包括 MRSA、肠球菌、醋酸杆菌属和厌氧菌。对碳青霉烯类耐药菌没有完全可靠的活性:我们通过对已发表的有关头孢吡肟/头孢美唑巴坦的文献进行回顾,介绍了头孢吡肟/头孢美唑巴坦的化学成分、药效学、药代动力学、毒性、药物间相互作用、临床疗效和目前的监管情况:头孢吡肟/恩美唑巴坦的主要潜在作用是作为一种碳青霉烯类备用药物,用于治疗由产ESBL肠杆菌引起的感染,以避免使用碳青霉烯类药物,并避免非β-内酰胺类替代药物的毒性。鉴于其活性范围和药代动力学特性,头孢吡肟/恩美唑巴坦可能会用于治疗生殖道感染、腹腔感染和新生儿败血症。不过,在这些情况下使用前还需要进行更多的非临床和临床研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Cefepime/Enmetazobactam: a microbiological, pharmacokinetic, pharmacodynamic, and clinical evaluation.

Introduction: Cefepime/enmetazobactam is a novel β-lactam/β-lactamase inhibitor (BL-BLI) combination with broad Gram-positive and -negative activity. Cefepime is relatively resistant to hydrolysis by AmpC, and enmetazobactam inhibits all Ambler Class A extended spectrum β-lactamases (ESBLs). Hence, the combination is resistant to hydrolysis by many ESBLs. Important spectrum gaps are MRSA, enterococci, Acinetobacter spp. and anaerobes. There is no completely reliable activity against carbapenem-resistant organisms.

Areas covered: We describe the chemistry, pharmacodynamics, pharmacokinetics, toxicities, drug-drug interactions, clinical efficacy, and current regulatory position of cefepime/enmetazobactam, following a review of available published literature relating to cefepime/enmetazobactam.

Expert opinion: The main potential role for cefepime/enmetazobactam is as a carbapenem-sparing agent for the treatment of infections caused by ESBL-producing Enterobacterales to prevent the use of carbapenems and to avoid the toxicities of non-β-lactam alternatives.There may be potential uses for cefepime/enmetazobactam for the treatment of reproductive tract infections, abdominal infections and neonatal sepsis, given the spectrum of activity and pharmacokinetic properties. However, additional non-clinical and clinical studies are required before use in these settings.

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