环孢素A与钙离子通道拮抗剂的相互作用及临床意义

    Interaction and Clinical Significance of Cyclosporine A and Calcium Channel Blockers

    • 摘要: 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。

       

      Abstract: Calcium channel blockers are often chosen as a first-line hypotensor in the treatment of high blood pressure after organ transplantation, especially after using cyclosporine A. Calcium channel blockers and cyclosporine A are mainly metabolized by CYP450 enzyme system of liver microsomes, and both are P-glycoprotein substrates and inhibitors, so there are many interactions. The influence of different calcium channel blockers on the plasma concentration of cyclosporine A is very different. However, the immune inhibition strength, liver and kidney toxicity of cyclosporine A and it's plasma concentration are dose-dependent. Therefore it is necessary to explore the interaction of cyclosporine A and calcium channel blockers. In this paper, by analyzing the pharmacokinetic and pharmacodynamics interaction and related research progress, it is provided reasonable advice for clinical combination cyclosporine A and calcium channel blockers.

       

    /

    返回文章
    返回