Distinct effects of omeprazole and rabeprazole on the tacrolimus blood concentration in a kidney transplant recipient
Distinct effects of omeprazole and rabeprazole on the tacrolimus blood concentration in a kidney transplant recipient
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DOI：
10.2133/dmpk.22.441
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发表时间：
2007-01-01
影响因子：
2.1
通讯作者：
Inui, Ken-ichi
中科院分区：
文献类型：
--
作者：
Takahashi, Kazushige;Yano, Ikuko;Inui, Ken-ichi
质子泵抑制剂(PPI，如奥美拉唑和雷贝拉唑)通常用于移植患者，作为手术后溃疡的治疗或预防。由于他克莫司和PPI在代谢方面共享CYP3A4系统，当它们同时服用时，药代动力学相互作用是可以预见的。我们报告一位接受活体供肾移植的日本男性患者，他克莫司、霉酚酸酯和强的松龙用于免疫抑制。奥美拉唑治疗期间他克莫司的浓度/剂量比(C/D)明显高于雷尼替丁或雷贝拉唑。三种抗酸药使用期间肝功能检测结果均在正常范围内。由于使用奥美拉唑时他克莫司的C/D比值较高，并不是由于肝功能障碍导致他克莫司排泄减少所致，因此人们强烈怀疑奥美拉唑和他克莫司之间的药物相互作用。本病例表明，在接受他克莫司治疗的肾移植受者中，雷贝拉唑可以安全地替代奥美拉唑。
Proton-pump inhibitors (PPIs, e. g. omeprazole and rabeprazole) are often administered to transplant patients as a treatment or prophylaxis for ulcers after surgery. Since tacrolimus and PPIs share the CYP3A4 system for metabolism, pharmacokinetic interactions are anticipated when they are administered simultaneously. We present a Japanese male patient who underwent a living-donor kidney transplantation having received tacrolimus, mycophenolate mofetil, and prednisolone for immunosuppression. The concentration/dose (C/D) ratio for tacrolimus was markedly higher during the period of treatment with omeprazole than ranitidine or rabeprazole. The results of liver functional tests were within the normal range during the use of these three antacid drugs. Since the higher C/D ratio for tacrolimus when omeprazole was being administered did not result from a decrease in the elimination of tacrolimus due to hepatic dysfunction, drug interaction between omeprazole and tacrolimus was strongly suspected. The present case indicates that rabeprazole can be used safely in place of omeprazole in kidney transplant recipients receiving tacrolimus.