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Tacrolimus Pharmacokinetic and Pharmacogenomic Differences between Adults and Pediatric Solid Organ Transplant Recipients

机译:成人和小儿实体器官移植受者之间他克莫司的药代动力学和药物基因组学差异

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摘要

Tacrolimus is a calcineurin inhibitor immunosuppressant that has seen considerable use in both adult and pediatric solid organ transplant recipients. Though there is much pharmacokinetic data available for tacrolimus in the adult population, the literature available for children is limited. Furthermore, very little is known about the pharmacogenomic differences in the two patient groups. Based on what information is currently available, clinically significant differences may exist between the two populations in terms of absorption, distribution, metabolism and elimination. In addition, inherent physiological differences exist in the young child including: less effective plasma binding proteins, altered expression of intestinal P-glycoprotein, and increased expression of phase 1 metabolizing enzymes, therefore one would expect to see clinically significant differences when administering tacrolimus to a child. This paper examines available literature in an attempt to summarize the potential pharmacokinetic and pharmacogenomic variability that exists between the two populations.
机译:他克莫司是一种钙调神经磷酸酶抑制剂的免疫抑制剂,已在成人和儿童实体器官移植接受者中广泛使用。尽管在成人人群中有许多他克莫司的药代动力学数据,但可用于儿童的文献有限。此外,关于两个患者组的药物基因组学差异知之甚少。根据当前可获得的信息,两个人群在吸收,分布,代谢和消除方面可能存在临床上的显着差异。此外,年幼儿童还存在固有的生理学差异,包括:血浆结合蛋白的有效性降低,肠道P-糖蛋白表达的改变以及1期代谢酶表达的增加,因此,在将他克莫司给予阿司他莫司时,人们有望看到临床上的显着差异。儿童。本文研究了现有文献,以试图总结两个人群之间存在的潜在药代动力学和药代基因组变异性。

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