Heykants J, Huang M L, Mannens G, Meuldermans W, Snoeck E, Van Beijsterveldt L, Van Peer A, Woestenborghs R
Department of Drug Metabolism and Pharmacokinetics, Janssen Research Foundation, Beerse, Belgium.
J Clin Psychiatry. 1994 May;55 Suppl:13-7.
Risperidone is rapidly and completely absorbed after oral administration; less than 1% is excreted unchanged in the feces. The principal metabolite was found to be 9-hydroxyrisperidone. Hydroxylation of risperidone is subject to the same genetic polymorphism as debrisoquine and dextromethorphan. In poor metabolizers the half-life of risperidone was about 19 hours compared with about 3 hours in extensive metabolizers. However, becuase the pharmacology of 9-hydroxyrisperidone is very similar to that of risperidone, the half-life for the "active fraction" (risperidone +9-hydroxyrisperidone) was found to be approximately 20 hours in extensive and poor metabolizers. We found that risperidone exhibited linear elimination kinetics and that steady state was reached within 1 day for risperidone and within 5 days for the active fraction.
利培酮口服后迅速且完全吸收；粪便中以原形排泄的不到1%。主要代谢产物为9-羟利培酮。利培酮的羟基化与异喹胍和右美沙芬存在相同的基因多态性。在代谢缓慢者中，利培酮的半衰期约为19小时，而在代谢快者中约为3小时。然而，由于9-羟利培酮的药理作用与利培酮非常相似，发现“活性部分”（利培酮 + 9-羟利培酮）在代谢快者和代谢缓慢者中的半衰期约为20小时。我们发现利培酮呈现线性消除动力学，利培酮在1天内达到稳态，活性部分在5天内达到稳态。
