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首页> 外文期刊>International journal of clinical pharmacology and therapeutics >Intake of grapefruit juice alters the metabolic pattern of cyclosporin A in renal transplant recipients.
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Intake of grapefruit juice alters the metabolic pattern of cyclosporin A in renal transplant recipients.

机译：摄入葡萄柚汁会改变肾移植受者中环孢菌素A的代谢模式。

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OBJECTIVE: The aim of the present study was to investigate the effect of grapefruit juice on the pharmacokinetics of cyclosporin A (CsA), as Sandimmun Neoral, and its main metabolites, M1, M9 and M4N, in renal transplant recipients. METHODS: Ten renal transplant recipients, on CsA-based immunosuppressive therapy, were included in this open, randomized crossover study. Patients were given their individualized morning dose of CsA, administered with either 250 ml water or 250 ml grapefruit juice and 12-hour CsA pharmacokinetic investigations were performed. The 2 investigation days were separated by at least 7 days. RESULTS: Administration of CsA with grapefruit juice compared with water significantly increased the area under the whole blood concentration versus time curve in the interval from 0-12 hours (AUC(0-12)) of CsA, by an average of 25 +/- 19% (p = 0.002). Intake of grapefruit juice did not have any significant influence on maximum whole blood concentration (Cmax) or time to Cmax (tmax) of CsA. AUC(0-12) and Cmax of M9 decreased significantly with intake of grapefruit juice, on average 22 +/- 11% (p = 0.0007) and 36 +/- 6% (p = 0.0001), respectively. AUC(0-12) of M1, however, was on average 13 +/- 14% (p = 0.02) higher upon co-administration of CsA with grapefruit juice as compared with water. The level of M4N was below the limit of quantification in most samples, and an effect of co-administration of CsA with grapefruit juice could not be determined for this metabolite. CONCLUSION: The present study shows that co-administration of grapefruit juice with CsA compared with water affects the formation and/or elimination of the 2 metabolites M1 and M9 differently. In addition, administration of CsA with grapefruit juice compared with water induced a moderate, but significant increase in systemic exposure of CsA in renal transplant recipients.
机译：目的：本研究的目的是研究葡萄柚汁对肾移植受者中环孢菌素A（CsA）（Sandimmun Neoral）及其主要代谢产物M1，M9和M4N的药代动力学的影响。方法：十名接受基于CsA免疫抑制治疗的肾移植受者包括在这项开放的随机交叉研究中。给予患者各自的早晨CsA剂量，并用250 ml水或250 ml葡萄柚汁给药，并进行12小时CsA药代动力学研究。 2个调查日至少间隔7天。结果：与水相比，西柚汁与水一起施用CsA显着增加了CsA在0-12小时（AUC（0-12））间隔内全血浓度-时间曲线下的面积，平均增加了25 +/- 19％（p = 0.002）。摄入柚子汁对CsA的最大全血浓度（Cmax）或达到Cmax的时间（tmax）没有任何显着影响。随着葡萄柚汁的摄入，M9的AUC（0-12）和Cmax显着降低，分别平均为22 +/- 11％（p = 0.0007）和36 +/- 6％（p = 0.0001）。然而，与水相比，将CsA与葡萄柚汁并用时，M1的AUC（0-12）平均高出13 +/- 14％（p = 0.02）。在大多数样品中，M4N的水平低于定量极限，并且无法确定CsA与葡萄柚汁共同给药的效果。结论：本研究表明，与水相比，葡萄柚汁与CsA的共同给药对M1和M9两种代谢物的形成和/或消除有不同的影响。另外，与水相比，葡萄柚汁与CsA的给药在肾移植受者中引起CsA全身暴露的适度但显着增加。

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