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肾脏病与透析肾移植杂志 ›› 2019, Vol. 28 ›› Issue (1): 63-67.DOI: 10.3969/j.issn.1006-298X.2019.01.014

• 论文 • 上一篇    下一篇

他克莫司、环孢素与三唑类抗真菌药的代谢及药物相互作用

  

  • 出版日期:2019-02-28 发布日期:2019-03-04

Metabolism and drugdrug interaction of tacrolimus,cyclosporine and triazole antifungals

  • Online:2019-02-28 Published:2019-03-04

摘要:

他克莫司和环孢素是广泛用于器官移植领域和自身免疫系统疾病治疗的钙调磷酸酶抑制剂,主要经细胞色素P450(CYP450)代谢,其中CYP3A5基因多态性对他克莫司代谢有显著影响。免疫抑制剂的使用是真菌感染的危险因素,目前三唑类抗真菌药作为广谱抗真菌药在临床上使用广泛。各个三唑类抗真菌药的代谢途径有所差异,其中伏立康唑的代谢受CYP2C19基因多态性影响大。他克莫司、环孢素与三唑类抗真菌药联用时可能发生药物相互作用。本文就他克莫司、环孢素与三唑类抗真菌药的代谢及其药物相互作用做一综述,以期为临床应用提供参考。

关键词: 他克莫司, 环孢素, 三唑类抗真菌药, 基因多态性, 药物相互作用

Abstract:

Tacrolimus and cyclosporine are calcineurin inhibitors widely used in organ transplantation and autoimmune diseases,both of them mainly metabolized by cytochrome P450 (CYP450),and the gene polymorphism of CYP3A5 has a significant effect on tacrolimus metabolism.The usage of immunosuppressive agents is a risk factor for fungal infection,and triazole antifungals are widely used as broadspectrum antifungal drugs in clinical practice.The metabolic pathway of each triazole antifungal is different,and the metabolism of voriconazole is greatly affected by the gene polymorphism of CYP2C19.Administration of tacrolimus,cyclosporine and triazole antifungals may results in a drugdrug interaction(DDI).This review summarizes the metabolism and DDI of tacrolimus,cyclosporine and triazole antifungals in order to provide reference for clinical application.

Key words: tacrolimus, cyclosporine, triazole antifungals, gene polymorphism, drug-drug interaction