Pomelo-induced increase in the blood level of tacrolimus in a renal transplant patient
Pomelo-induced increase in the blood level of tacrolimus in a renal transplant patient
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DOI：
10.1097/01.tp.0000058545.35041.be
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发表时间：
2003-04-15
期刊：
影响因子：
6.2
通讯作者：
Sawada, Y
中科院分区：
文献类型：
--
作者：
Egashira, K;Fukuda, E;Sawada, Y
背景资料。他克莫司是一种免疫抑制剂，广泛用于移植后的患者，以防止同种异体移植；排斥反应。由于他克莫司的治疗范围较窄，因此仔细控制血药浓度至关重要。已证实他克莫司主要由细胞色素P-450(CYP)3A4代谢，他克莫司是P-糖蛋白的底物。本文报告一例肾移植受者进食柚子后他克莫司血药浓度显著升高的病例。结论柚可能通过抑制CYP3A4和/或P-糖蛋白而增加他克莫司的血药浓度。服用他克莫司或环孢素等药物的患者应避免食用柚子和其他与葡萄柚相关的柑橘类水果，因为这些药物的代谢动力学会受到葡萄柚汁的影响。
Background. Tacrolimus, an immunosuppressive agent, is widely used in patients after transplantation to prevent allograft; rejection. Because tacrolimus has a narrow therapeutic range, it is essential to carefully control the blood level. It has been demonstrated that tacrolimus is metabolized mainly by cytochrome P-450 (CYP) 3A4, and that tacrolimus is a substrate of P-glycoprotein.Methods. This article reports a case of considerable increase in the blood level of tacrolimus after the intake of pomelo in a renal transplant recipient.Results. Pomelo may increase the blood concentration of tacrolimus by inhibiting CYP 3A4, P-glycoprotein, or both.Conclusions. Patients taking drugs such as tacrolimus or cyclosporine, which have their kinetics affected by grapefruit juice, should avoid pomelo and other grapefruit-related citrus fruits.