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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2019, Vol. 24 ›› Issue (2): 235-240.doi: 10.12092/j.issn.1009-2501.2019.02.019

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Effects of genetic polymorphisms on metabolic kinetics, pharmacodynamics and adverse reactions of amitriptyline

WANG Ente 1,2, ZHANG Xiaodan 1, ZHOU Shuang 1, ZHAO Xia 1,2,  ZHOU Ying 1,2, CUI Yimin 1,2   

  1. 1 First Hospital of Peking University, Beijing 100034, China; 2 Peking University, Beijing 100191, China
  • Received:2018-09-03 Revised:2018-12-17 Online:2019-02-26 Published:2019-03-04

Abstract:

Amitriptyline is a tricyclic antidepressant for the treatment of severe depression, post-traumatic stress disorder and other psychiatric diseases, which is widely used in clinical application. However, there are significant individual differences in the response of amitriptyline. Research has shown that genetics polymorphisms of CYP2D6, CYP2C19 and ABCB1 have certain effects on the pharmacokinetics (PK), pharmacodynamics (PD) and adverse reactions (ADR) of amitriptyline. In this paper, we have drawn a preliminary conclusion by comparing the effects of CYP2D6 and CYP2C19 gene polymorphisms on amitriptyline PK, PD and ADR. For CYP2C19 ultrarapid metabolizers or extensive metabolizers, the genetic polymorphism of CYP2D6 has a greater effect on the overall metabolism of amitriptyline. However, for CYP2C19 poor metabolizers, the genetic polymorphisms of CYP2C19 have greater influence. Hopefully, this article can provide genetic-based advice and assistance for the individualized administration of amitriptyline.

Key words: amitriptyline, gene polymorphism, CYP2C19, CYP2D6, ABCB1

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