Department of Clinical Pharmacology, University of Greifswald, Greifswald, Germany.
Clin Pharmacol Ther. 2011 Apr;89(4):524-8. doi: 10.1038/clpt.2011.4. Epub 2011 Mar 2.
Immunosuppressive therapy is frequently associated with hypercholesterolemia, calling for lipid-lowering treatment without adverse drug interactions. One option is treatment with the cholesterol absorption inhibitor ezetimibe. We have shown in vitro that ezetimibe and tacrolimus may interact in competition for intestinal UGT1A1 and ABCB1 at concentrations reached in gut lumen after oral administration. However, this clinical study in healthy volunteers showed that the expected pharmacokinetic interaction between ezetimibe and tacrolimus is not of clinical relevance.
免疫抑制疗法常伴有高胆固醇血症，需要进行降脂治疗而不产生药物相互作用。一种选择是使用胆固醇吸收抑制剂依折麦布进行治疗。我们已经在体外证明，依折麦布和他克莫司可能在口服后到达肠道腔时达到的浓度下通过肠道 UGT1A1 和 ABCB1 竞争发生相互作用。然而，这项在健康志愿者中的临床研究表明，依折麦布和他克莫司之间预期的药代动力学相互作用没有临床相关性。
