Démolis J L, Angebaud P, Grangé J D, Coates P, Funck-Brentano C, Jaillon P
Clinical Pharmacology Unit, Saint-Antoine University Hospital, Paris, France.
Br J Clin Pharmacol. 1996 Sep;42(3):394-7. doi: 10.1046/j.1365-2125.1996.42817.x.
Sertraline is a serotonin reuptake inhibitor. The enhancement of serotoninergic transmission is associated with antidepressant activity. In order to determine the pharmacokinetics of sertraline in patients with chronic stable hepatic insufficiency, 10 patients were matched (age, weight, sex) with 10 healthy subjects in an open study. Each participant received a single capsule containing the equivalent of 100 mg sertraline base. Blood samples were taken during 264 h after administration for measurement of plasma concentrations of sertraline. The results confirm that the oral clearance of sertraline is reduced with a 1.7-fold increase in Cmax and a significant prolongation in elimination half-life in hepatically impaired patients.
舍曲林是一种血清素再摄取抑制剂。血清素能传递的增强与抗抑郁活性相关。为了确定舍曲林在慢性稳定型肝功能不全患者中的药代动力学，在一项开放性研究中，将10名患者（年龄、体重、性别）与10名健康受试者进行匹配。每位参与者服用一粒含有相当于100毫克舍曲林碱的胶囊。给药后264小时内采集血样，以测量舍曲林的血浆浓度。结果证实，肝功能受损患者中舍曲林的口服清除率降低，Cmax增加1.7倍，消除半衰期显著延长。
