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头孢洛林酯:一种新型广谱头孢菌素。

Ceftaroline fosamil: a novel broad-spectrum cephalosporin.

作者信息

Bazan J A, Martin S I

机构信息

Division of Infectious Diseases, The Ohio State University Medical Center, Columbus, Ohio, USA.

出版信息

Drugs Today (Barc). 2010 Oct;46(10):743-55. doi: 10.1358/dot.2010.46.10.1519172.

Abstract

Ceftaroline fosamil is a new extended-spectrum cephalosporin with activity against drug-resistant Grampositive pathogens such as methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae. At the same time, its Gramnegative spectrum of coverage includes common respiratory pathogens such as Haemophilus influenzae and Moraxella catarrhalis, as well as wild-type Enterobacteriaceae. In vivo efficacy for the treatment of experimental endocarditis, pneumonia, myositis and osteomyelitis has been demonstrated in animal models, while efficacy in the treatment of complicated skin and soft tissue infections and community-acquired pneumonia has been demonstrated in phase II and III clinical trials in humans. The drug is well tolerated and has a low rate of reported adverse events. The dose of ceftaroline fosamil used is 600 mg i.v. every 12 h for patients with normal renal function or mild renal dysfunction. In patients with moderate renal dysfunction, it has been suggested that ceftaroline fosamil be dosed at 400 mg i.v. over 60 min every 12 h. Ceftaroline fosamil is still under review by the U.S. FDA, and when approved, will be one of the first commercially available β-lactams with the ability to treat infections due to MRSA and other drug-resistant Gram-positive pathogens.

摘要

头孢洛林酯是一种新型广谱头孢菌素,对耐甲氧西林金黄色葡萄球菌(MRSA)和耐青霉素肺炎链球菌等耐药革兰氏阳性病原体具有活性。同时,其革兰氏阴性菌覆盖范围包括流感嗜血杆菌和卡他莫拉菌等常见呼吸道病原体,以及野生型肠杆菌科细菌。在动物模型中已证明其对治疗实验性心内膜炎、肺炎、肌炎和骨髓炎具有体内疗效,而在人类的II期和III期临床试验中已证明其对治疗复杂皮肤和软组织感染及社区获得性肺炎有效。该药物耐受性良好,报告的不良事件发生率较低。对于肾功能正常或轻度肾功能不全的患者,使用的头孢洛林酯剂量为静脉注射600mg,每12小时一次。对于中度肾功能不全的患者,建议头孢洛林酯以400mg静脉注射,在60分钟内给药,每12小时一次。头孢洛林酯仍在美国食品药品监督管理局(FDA)的审查中,一旦获批,将成为首批可用于治疗由MRSA和其他耐药革兰氏阳性病原体引起的感染的商业化β-内酰胺类药物之一。

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