Adis, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, 0754 Auckland, New Zealand.
Drugs. 2013 Jul;73(10):1067-94. doi: 10.1007/s40265-013-0075-6.
Ceftaroline, the active metabolite of the prodrug ceftaroline fosamil (Zinforo, Teflaro), is an advanced-generation, parenteral cephalosporin with broad-spectrum antibacterial activity in vitro against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and multidrug resistant Streptococcus pneumoniae and Gram-negative bacteria, including Haemophilus influenzae and Moraxella catarrhalis, but not Pseudomonas aeruginosa. Ceftaroline has demonstrated a low potential for the selection of resistance in vitro for drug-resistant Gram-positive organisms, including MRSA, as well as for Gram-negative respiratory pathogens. In pivotal phase III studies, intravenous ceftaroline fosamil demonstrated noninferiority to intravenous vancomycin plus aztreonam in patients hospitalized with complicated skin and soft tissue infections (cSSTIs) and intravenous ceftriaxone in patients hospitalized with community-acquired pneumonia (CAP) [Pneumonia Outcomes Research Team (PORT) risk class III or IV]; however, patients with CAP admitted to the intensive care unit were not evaluated. Ceftaroline fosamil was generally well tolerated in these trials, with an adverse event profile similar to that of other cephalosporins. Diarrhoea was the most commonly reported adverse event; however, the risk of Clostridium difficile-associated diarrhoea with ceftaroline fosamil appeared to be low. Potential limitations of the drug include the lack of an oral formulation and the requirement for twice-daily administration. Nonetheless, ceftaroline fosamil represents an attractive option (either alone or in combination with other agents) for the initial empirical treatment of patients hospitalized with cSSTIs (including those with suspected MRSA infection) or CAP (PORT risk class III or IV) who require intravenous antimicrobial therapy. As with all antibacterial agents, ceftaroline fosamil should be used in accordance with good antimicrobial stewardship.
头孢洛林，前药头孢洛林磷酸酯（赞诺福、特福瑞）的活性代谢物，是一种具有广谱体外抗菌活性的新型注射用头孢菌素，对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA）和多重耐药肺炎链球菌）和革兰氏阴性菌（包括流感嗜血杆菌和卡他莫拉菌）具有活性，但对铜绿假单胞菌无效。头孢洛林在体外对耐药革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌）和革兰氏阴性呼吸道病原体具有较低的耐药选择潜力。在关键性 III 期研究中，静脉用头孢洛林磷酸酯在治疗复杂性皮肤和软组织感染（cSSTIs）的住院患者中与静脉用万古霉素加氨曲南、治疗社区获得性肺炎（CAP）的住院患者中与静脉用头孢曲松相比，非劣效性[肺炎结局研究团队（PORT）风险分类 III 或 IV]；然而，未评估入住重症监护病房的 CAP 患者。在这些试验中，头孢洛林磷酸酯总体上具有良好的耐受性，其不良事件谱与其他头孢菌素相似。腹泻是最常见的报告不良事件；然而，头孢洛林磷酸酯相关的艰难梭菌相关性腹泻风险似乎较低。该药物的潜在局限性包括缺乏口服制剂和需要每日两次给药。尽管如此，头孢洛林磷酸酯代表了一种有吸引力的选择（单独使用或与其他药物联合使用），可用于治疗需要静脉用抗菌药物治疗的 cSSTIs（包括疑似耐甲氧西林金黄色葡萄球菌感染）或 CAP（PORT 风险分类 III 或 IV）住院患者的初始经验性治疗。与所有抗菌药物一样，头孢洛林磷酸酯应根据良好的抗菌药物管理原则使用。
