Kaye C M, Nicholls B
Drug Metabolism and Pharmacokinetics, SmithKline Beecham Pharmaceuticals, Welwyn, Herts, England.
Clin Pharmacokinet. 2000 Oct;39(4):243-54. doi: 10.2165/00003088-200039040-00001.
Ropinirole is a selective non-ergoline dopamine D2 receptor agonist indicated for use in treating Parkinson's disease. When taken as oral tablets, ropinirole is rapidly and almost completely absorbed, and it is extensively distributed from the vascular compartment. The bioavailability is approximately 50%. Ropinirole shows low plasma protein binding. The drug is inactivated by metabolism in the liver, and none of the major circulating metabolites have pharmacological activity. The principal metabolic enzyme is the cytochrome P450 (CYP) isoenzyme CYP1A2. Ropinirole shows approximately linear pharmacokinetics when given as single or repeated doses, and is eliminated with a half-life of approximately 6 hours. Population pharmacokinetics have demonstrated that gender, mild or moderate renal impairment, Parkinson's disease stage and concomitant illnesses or the use of several common concomitant medications have no effect on the pharmacokinetics of ropinirole. Clearance is slower for patients older than 65 years compared with those who are younger, and in women taking hormone replacement therapy compared with those who are not. The CYP1A2 inhibitor ciprofloxacin produced increases in the plasma concentrations of ropinirole when these 2 drugs were coadministered, but no interaction was seen with theophylline which, like ropinirole, is also a substrate for CYP1A2. There is no obvious plasma concentration-effect relationship for ropinirole.
罗匹尼罗是一种选择性非麦角类多巴胺D2受体激动剂，用于治疗帕金森病。口服片剂时，罗匹尼罗吸收迅速且几乎完全吸收，并从血管腔广泛分布。生物利用度约为50%。罗匹尼罗与血浆蛋白的结合率较低。该药物在肝脏中通过代谢失活，主要循环代谢物均无药理活性。主要代谢酶是细胞色素P450（CYP）同工酶CYP1A2。罗匹尼罗单剂量或重复给药时表现出近似线性的药代动力学，消除半衰期约为6小时。群体药代动力学表明，性别、轻度或中度肾功能损害、帕金森病分期、合并疾病或几种常见合并用药对罗匹尼罗的药代动力学无影响。65岁以上患者的清除率比年轻患者慢，接受激素替代治疗的女性比未接受治疗的女性清除率慢。当这两种药物合用时，CYP1A2抑制剂环丙沙星会使罗匹尼罗的血浆浓度升高，但与同样是CYP1A2底物的茶碱未见相互作用。罗匹尼罗没有明显的血浆浓度-效应关系。
