Merker Andrew, Danziger Larry H, Rodvold Keith A, Glowacki Robert C
HIV PGY2 Resident,University of Illinois at Chicago, College of Pharmacy , 833 South Wood Street, Chicago, 60612 , USA.
Expert Opin Drug Metab Toxicol. 2014 Dec;10(12):1741-50. doi: 10.1517/17425255.2014.972932. Epub 2014 Oct 27.
Ceftaroline fosamil is a 5th generation cephalosporin with an in vitro spectrum of activity including Streptococcus agalactiae, penicillin- and cephalosporin-resistant S. pneumoniae, S. pyogenes, methicillin-susceptible S. aureus and methicillin-resistant S. aureus, Haemophilus influenzae, Klebsiella oxytoca, K. pneumoniae and Moraxella catarrhalis. It is currently approved by the FDA for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP) in adults.
This review covers the mechanism of action; bacterial resistance; pharmacokinetic characteristics in various patient populations; pharmacodynamic data in animal and in vitro models as well as human studies; efficacy observed in clinical trials for ABSSSI and CABP; and adverse effects.
Ceftaroline provides in vitro bactericidal activity against methicillin-, vancomycin-, daptomycin-, and linezolid-resistant Gram-positive organisms and select Gram-negative pathogens. The pharmacodynamics of ceftaroline is similar to other β-lactam agents. Ceftaroline exhibits a favorable adverse effect profile and is generally well tolerated. There is little data on clinical success of ceftaroline in patients with bacteremia or endocarditis other than what has been published in a small series of case reports. Randomized-control studies are needed to establish clinical outcomes and safety in these patient populations.
头孢洛林酯是一种第五代头孢菌素，其体外抗菌谱包括无乳链球菌、对青霉素和头孢菌素耐药的肺炎链球菌、化脓性链球菌、甲氧西林敏感金黄色葡萄球菌和甲氧西林耐药金黄色葡萄球菌、流感嗜血杆菌、产酸克雷伯菌、肺炎克雷伯菌和卡他莫拉菌。它目前已获美国食品药品监督管理局批准，用于治疗成人急性细菌性皮肤及皮肤结构感染（ABSSSI）和社区获得性细菌性肺炎（CABP）。
本综述涵盖了作用机制；细菌耐药性；不同患者群体的药代动力学特征；动物和体外模型以及人体研究中的药效学数据；ABSSSI和CABP临床试验中观察到的疗效；以及不良反应。
头孢洛林对耐甲氧西林、耐万古霉素、耐达托霉素和耐利奈唑胺的革兰氏阳性菌以及特定革兰氏阴性病原体具有体外杀菌活性。头孢洛林的药效学与其他β-内酰胺类药物相似。头孢洛林的不良反应情况良好，总体耐受性较好。除了一小系列病例报告中发表的内容外，关于头孢洛林在菌血症或心内膜炎患者中的临床成功数据很少。需要进行随机对照研究来确定这些患者群体的临床疗效和安全性。
