新型头孢菌素头孢比罗酯特点及临床应用

Review of the features and clinical application of a novel broad-spectrum cephalosporin: ceftobiprole medocaril

头孢比罗是前体药物头孢比罗酯的活性代谢成分,是新一代广谱静脉注射用头孢菌素,包括具有抗甲氧西林耐药金黄色葡萄球菌(methicillin-resistant Staphylococcus aureus,MRSA)以及铜绿假单胞菌的抗菌活性。头孢比罗在体外对多种导致医院获得性肺炎[(hospital acquired pneumonia,HAP),不包括呼吸机相关性肺炎(ventilator associated pneumonia,VAP)]与社区获得性肺炎(community-acquired pneumonia,CAP)的革兰阳性菌与革兰阴性菌均表现出有效的活性。现对其作用机制、体外抗菌活性、药动学特性、临床试验以及药物安全性与耐受性等方面进行综述。

Ceftobiprole,the active metabolite of the prodrug ceftobiprole medocaril,is a new generation broad-spectrum intravenous cephalosporin with activity against methicillin-resistant Staphylococcus aureus(MRSA)and Pseudomonas aeruginosa.Ceftobiprole showed potent effective activity against a number of gram-positive and gram-negative pathogens associated with hospital-acquired pneumonia[HAP,excluding ventilator associated pneumonia(VAP)]and community-acquired pneumonia(CAP)in vitro.The mechanism of action,antibacterial activities in vitro,pharmacokinetic profile,clinical trials,safety and tolerability of ceftobiprole were reviewed.