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器官移植术后尤其使用环孢素A后所致高血压常选用钙离子通道拮抗剂作为一线降压药物。但由于两者都主要通过肝微粒体CYP450酶系代谢,同时又是P-糖蛋白的底物及抑制剂,因此存在较多相互作用。不同钙离子通道拮抗剂对环孢素A血药浓度的影响有较大区别,而环孢素A的免疫抑制作用强度、肝肾毒性与其血药浓度又呈量效依赖关系,因此有必要将两者的相互作用进行深入探讨。本文主要通过分析环孢素A与钙离子通道拮抗剂的药代学及药效学相互作用及相关研究进展,以期为临床联用环孢素A与钙离子通道拮抗剂提供合理使用建议。
Especially after organ transplantation, the use of cyclosporin A-induced hypertension often use calcium channel blockers as first-line antihypertensive drugs. However, since both are metabolized primarily by the liver microsomal CYP450 enzyme and are substrates and inhibitors of P-glycoprotein, there is more interaction. The effects of different calcium channel antagonists on the blood concentration of cyclosporin A are quite different. However, the immunosuppressive intensity of cyclosporine A and the hepatotoxicity and the plasma concentration of liver and kidney are in a dose-dependent manner. Therefore, The interaction between the two in-depth discussion. This article mainly through the cyclosporin A and calcium channel antagonists pharmacokinetics and pharmacodynamics interaction and related research, in order to provide clinical recommendations cyclosporine A and calcium channel antagonists provide reasonable use.