PHARMACOKINETICS OF SCH39166 IN SUBJECTS W/ CHRONIC LIVER DISEASE

SCH39166是多巴胺D1和D5受体的选择性拮抗剂。多巴胺神经传递会被所有成瘾药物甚至美味的食物刺激。但可卡因、尼古丁、阿片类药物和乙醇等药物的成瘾特性似乎与多巴胺刺激D1和/或D5受体有关。由于SCH39166在人体中广泛葡萄糖醛酸化，因此研究不同程度的肝功能改变对药物药代动力学的影响具有临床意义，特别是考虑到药物成瘾者中肝病的患病率。本单剂量研究的主要目的是评估和比较SCH39166在肝功能正常和不同程度的稳定慢性肝病患者中的药代动力学。这项研究的数据将用于制定不同程度慢性肝病患者的剂量指南。

SCH39166 is a selective antagonist of dopamine D1 and D5 receptors. Dopamine neurotransmission is stimulated by all addictive drugs and even highly palatable food. But the addictive properties of drugs such as cocaine, nicotine, opiates and ethanol appear to be associated with dopamine stimulation of D1 and/or D5 receptors. Since SCH39166 is extensively glucuronidated in humans, it is clinically relevant to study the effects of various degrees of altered hepatic function on the pharmacokinetics of the drug -- especially in light of the prevalence of hepatic disease in substance-addicted persons. The primary objective of this single dose study is to evaluate and compare the pharmacokinetics of SCH39166 in subjects with normal liver function and with various degrees of stable chronic liver disease. Data from this study will be used to develop dosing guidelines for patients with various degrees of chronic liver disease.