Anti-Infective Research Laboratory, Department of Pharmacy Practice, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA.
Pharmacotherapy. 2010 Apr;30(4):375-89. doi: 10.1592/phco.30.4.375.
Ceftaroline is a novel, broad-spectrum, advanced-generation cephalosporin whose action is mediated by binding to penicillin-binding proteins in bacteria, consistent with other beta-lactam antibiotics. Ceftaroline is distinct in that it has antimicrobial activity against multidrug-resistant Staphylococcus aureus (including methicillin-resistant S. aureus, vancomycin-intermediate S. aureus [VISA], heteroresistant VISA, and vancomycin-resistant S. aureus), Streptococcus pneumonia (including drug-resistant strains), and respiratory gram-negative pathogens such as Moraxella catarrhalis and Haemophilus influenzae (including beta-lactamase-positive strains). Development of resistance to ceftaroline occurs rarely in gram-positive bacteria and at a similar rate to that of other oxyimino-cephalosporins in gram-negative bacteria. The inactive prodrug, ceftaroline fosamil, is administered by intravenous infusion and rapidly undergoes biotransformation to ceftaroline. Ceftaroline then follows a two-compartment pharmacokinetic model and is eliminated primarily by renal excretion, with a half-life of approximately 3 hours. Similar to other cephalosporins, time above the minimum inhibitory concentration is the pharmacodynamic parameter that best predicts efficacy for ceftaroline. Ceftaroline 600 mg intravenously every 12 hours has been shown to have similar efficacy to vancomycin plus aztreonam for the treatment of complicated skin and skin structure infections and to ceftriaxone for the treatment of community-acquired bacterial pneumonia in phase III clinical trials. Ceftaroline displayed a safety profile similar to that of other cephalosporins in clinical trials. Dosage adjustment is required for moderate renal impairment and for patients receiving hemodialysis. Ceftaroline breakpoints have been proposed but not confirmed. Ceftaroline is a renally excreted broad-spectrum cephalosporin that is clinically effective for the treatment of complicated skin and skin structure infections and community-acquired bacterial pneumonia, and it has distinctive activity against some difficult-to-treat multidrug-resistant gram-positive organisms.
头孢洛林是一种新型、广谱、高级代头孢菌素，其作用通过与细菌中的青霉素结合蛋白结合来介导，与其他β-内酰胺类抗生素一致。头孢洛林的独特之处在于它对多种耐药金黄色葡萄球菌（包括耐甲氧西林金黄色葡萄球菌、中间耐药金黄色葡萄球菌[VISA]、异质耐药 VISA 和耐万古霉素金黄色葡萄球菌）、肺炎链球菌（包括耐药株）以及呼吸道革兰氏阴性病原体，如卡他莫拉菌和流感嗜血杆菌（包括β-内酰胺酶阳性株）具有抗菌活性。革兰氏阳性菌对头孢洛林的耐药性很少发生，耐药率与革兰氏阴性菌中的其他氧肟头孢菌素相似。无活性前药头孢洛林磷酸酯通过静脉输注给药，并迅速在体内转化为头孢洛林。头孢洛林随后遵循二室药代动力学模型，主要通过肾脏排泄消除，半衰期约为 3 小时。与其他头孢菌素类似，时间超过最低抑菌浓度是预测头孢洛林疗效的药效学参数。在 III 期临床试验中，头孢洛林 600mg 每 12 小时静脉滴注与万古霉素加氨曲南治疗复杂性皮肤和皮肤结构感染以及头孢曲松治疗社区获得性细菌性肺炎的疗效相似。头孢洛林在临床试验中的安全性与其他头孢菌素相似。中度肾功能不全和接受血液透析的患者需要调整剂量。已经提出了头孢洛林的折点，但尚未得到证实。头孢洛林是一种经肾脏排泄的广谱头孢菌素，对治疗复杂性皮肤和皮肤结构感染和社区获得性细菌性肺炎具有临床疗效，并且对一些难以治疗的多重耐药革兰氏阳性菌具有独特的活性。
