Alagozlu Hakan, Cindoruk Mehmet, Unal Selahattin
Department of Internal Medicine, Division of Gastroenterology, Medical Faculty of Gazi University, Ankara, Turkey.
Clin Drug Investig. 2006;26(8):481-4. doi: 10.2165/00044011-200626080-00006.
Cefoperazone is a third-generation cefalosporin that contains the N-methyl- thio-tetrazole (NMTT) side chain, which inhibits vitamin K-dependent carboxylation. Administration of NMTT-containing cefalosporins can cause alterations in the hepatic glutathione redox state, resulting in a dose-related increase in oxidised glutathione, which is responsible for the inhibition of microsomal reduction of vitamin K epoxide. In addition, cefoperazone is not metabolised and is excreted predominantly through the bile. In patients with hepatic impairment, the clearance of cefoperazone has been shown to be significantly reduced and the half-life prolonged. We report a case of choledocholithiasis related to a prolonged prothrombin time and INR secondary to cefoperazone therapy.
头孢哌酮是一种第三代头孢菌素,含有N - 甲基 - 硫代 - 四氮唑(NMTT)侧链,该侧链可抑制维生素K依赖的羧化作用。使用含NMTT的头孢菌素可导致肝脏谷胱甘肽氧化还原状态改变,致使氧化型谷胱甘肽呈剂量相关增加,这是抑制维生素K环氧化物微粒体还原的原因。此外,头孢哌酮不被代谢,主要通过胆汁排泄。在肝功能损害患者中,已显示头孢哌酮的清除率显著降低,半衰期延长。我们报告1例因头孢哌酮治疗继发凝血酶原时间和国际标准化比值延长而导致胆总管结石的病例。