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头孢呋辛酯:一种新型的广谱头孢菌素。

Ceftaroline fosamil: a new broad-spectrum cephalosporin.

机构信息

Medical Affairs, Forest Research Institute, Harborside Financial Center, Jersey City, NJ 07311, USA.

出版信息

J Antimicrob Chemother. 2011 Apr;66 Suppl 3:iii11-8. doi: 10.1093/jac/dkr095.

Abstract

Ceftaroline fosamil, the prodrug of the active metabolite, ceftaroline, is a new, broad-spectrum cephalosporin recently approved in the USA for the treatment of acute bacterial skin and skin structure infections (ABSSSIs) and community-acquired bacterial pneumonia (CABP). Ceftaroline has potent in vitro activity against Gram-positive organisms, including methicillin-resistant Staphylococcus aureus and Streptococcus pneumoniae, as well as common Gram-negative organisms. The high affinity of ceftaroline for penicillin-binding proteins is responsible for the potent activity observed against clinically relevant pathogens. With respect to the treatment of CABP, the activity of ceftaroline against pathogens such as S. pneumoniae, S. aureus, Haemophilus influenzae and Moraxella catarrhalis demonstrates coverage across a broad range of pathogens typically encountered in clinical practice. Ceftaroline is also very active against common pathogens seen in ABSSSIs such as S. aureus (methicillin-susceptible S. aureus and methicillin-resistant S. aureus) and Streptococcus pyogenes. Ceftaroline exhibits a dose-proportional pharmacokinetic profile, similar to other renally excreted cephalosporins, and has a well-tolerated safety profile consistent with the cephalosporin class. Ceftaroline fosamil is compatible via Y-site administration with many other commonly administered parenteral drugs.

摘要

头孢洛林酯氨丁三醇,其活性代谢产物头孢洛林的前药,是一种新型的、广谱头孢菌素,最近在美国被批准用于治疗急性细菌性皮肤和皮肤结构感染(ABSSSIs)和社区获得性细菌性肺炎(CABP)。头孢洛林对革兰氏阳性菌具有强大的体外活性,包括耐甲氧西林金黄色葡萄球菌和肺炎链球菌,以及常见的革兰氏阴性菌。头孢洛林对青霉素结合蛋白的高亲和力是其对临床相关病原体具有强大活性的原因。在治疗 CABP 方面,头孢洛林对肺炎链球菌、金黄色葡萄球菌、流感嗜血杆菌和卡他莫拉菌等病原体的活性表明,其涵盖了临床实践中常见的广泛病原体。头孢洛林对 ABSSSIs 中常见的病原体也非常有效,如金黄色葡萄球菌(甲氧西林敏感金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌)和化脓性链球菌。头孢洛林表现出剂量比例的药代动力学特征,类似于其他经肾排泄的头孢菌素,且具有与头孢菌素类一致的良好耐受安全性特征。头孢洛林酯氨丁三醇与许多其他常用的静脉内给药药物通过 Y 型部位给药兼容。

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