酮康唑(Ketoconazole),商品名(Nizoyal)是一种最新的咪唑类衍生物。自1978年临床应用以来,证明口服吸收好,疗效高,抗菌谱广,无耐药性。现就该药的代谢过程及作用机理等综述如下: 一、药物代谢:酮康唑口服后,如酸性胃液中易溶解和吸收。如人一次口服200mg后1小时,血浆浓度可达4μg/ml,2小时可达最高峰6μg/ml,8小时后降到1μg/ml,24小时后少于0.4μg/ml。上述有效的血浆浓度明显高于霉康唑,持续时间亦比霉康唑长。酮康唑吸入休内后,84%与血浆蛋白主要是白蛋白结合,1%在血浆中呈游离状态,15%与血细胞联合。酮康唑在肝、肾中代谢、氧化、分 Ketoconazole, a trade name (Nizoyal) is the latest imidazole derivative. Since its clinical application in 1978, it has been proved that oral absorption is good, efficacy is high, antibacterial spectrum is broad, and there is no drug resistance. Now on the drug’s metabolic process and mechanism of action are summarized as follows: First, the drug metabolism: After oral ketoconazole, such as acidic gastric juice easily dissolved and absorbed. One hour after an oral administration of 200 mg of human plasma, up to 4 μg / ml plasma peaked 6 μg / ml in 2 hours, 1 μg / ml in 8 hours and less than 0.4 μg / ml in 24 hours. The effective plasma concentration was significantly higher than that of meconazole, duration also longer than mycophenolate. After ketoconazole inhaled into the rest, 84% and albumin plasma protein is mainly binding, 1% in the plasma was free state, 15% and blood cells. Ketoconazole in the liver, kidney metabolism, oxidation, points