新型广谱头孢菌素类抗菌药物头孢吡普

A novel broad-spectrum cephalosporin ceftobiprole

随着耐甲氧西林金葡萄球菌、耐药金黄色葡萄球菌、耐青霉素肺炎链球菌和耐万古霉素肠球菌显著增加,细菌耐药性成为近年来一个重大难题。Ceftobiprole是第一个对耐甲氧西林金葡萄球菌(MRSA)和万古霉素耐药金黄色葡葡球菌(VRSA)有效的广谱头孢菌素类抗生素。现对其作用机制、合成路线、体外抗菌活性、药动学特性、临床试验等方面作一综述。

Antimicrobial resistance has become a significant problem over the past decade with marked increases in the incidence of MRSA, intermediate- and high level resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae and vancomycin-resistant enterococci. Ceftobiprole was the first of a new class of broad- spectrum cephalosporin antibiotics that had potent antibacterial activity towards methicillin-resistant Staphylococcus aureus （MRSA） and vancomycin-resistant Staphylococcus aureus （VRSA）. This review detailed its mechanism of action, synthesis methods, antibacterial activities in vivo, pharmacokinetic profle and clinical trials.