Following organ engraftment, initial dosing of tacrolimus is based on recipient weight and adjusted by measured C(0) concentrations. The bioavailability and elimination of tacrolimus are affected by the patients CYP3A5 genotype. Prospective data of the clinical advantage of knowing patient's CYP3A5 genotype prior to transplantation are lacking. A nonparametric population model was developed for tacrolimus in renal transplant recipients. Data from 99 patients were used for model development and validation. A three-compartment model with first-order absorption and lag time from the dosing compartment described the data well. Clearances and volumes of distribution were allometrically scaled to body size. The final model included fat-free mass, body mass index, hematocrit, time after transplantation, and CYP3A5 genotype as covariates. The bias and imprecision were 0.35 and 1.38, respectively, in the external data set. Patients with functional CYP3A5 had 26% higher clearance and 37% lower bioavailability. Knowledge of CYP3A5 genotype provided an initial advantage, but only until 3-4 tacrolimus concentrations were known. After this, a model without CYP3A5 genotype predicted just as well. The present models seem applicable for clinical individual dose predictions but need a prospective evaluation.

译文

器官植入后,他克莫司的初始剂量基于接受者的体重,并通过测量的C(0) 浓度进行调整。他克莫司的生物利用度和消除受患者CYP3A5基因型的影响。缺乏在移植前了解患者CYP3A5基因型的临床优势的前瞻性数据。针对肾移植受者的他克莫司建立了非参数种群模型。来自99名患者的数据用于模型开发和验证。具有一阶吸收和来自给药室的滞后时间的三室模型很好地描述了数据。间隙和分布量按体型大小进行了异同比例缩放。最终模型包括无脂肪质量,体重指数,血细胞比容,移植后时间和CYP3A5基因型作为协变量。在外部数据集中分别0.35和1.38偏差和不精确性。具有功能性CYP3A5的患者26% 更高的清除率和37% 更低的生物利用度。对CYP3A5基因型的了解提供了最初的优势,但直到已知3-4他克莫司浓度为止。此后,也可以预测没有CYP3A5基因型的模型。目前的模型似乎适用于临床个体剂量预测,但需要前瞻性评估。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录