他克莫司溶剂量的药代动力学。
Meltdose Tacrolimus Pharmacokinetics.
作者信息
Baraldo M
机构信息
Department of Experimental and Clinical Medicine, Medical School, University of Udine; SOC Institute of Clinical Pharmacology, University-Hospital S. Maria della Misercordia, Udine, Italy.
出版信息
Transplant Proc. 2016 Mar;48(2):420-3. doi: 10.1016/j.transproceed.2016.02.002.
BACKGROUND
Nonadherence to immunosuppressive therapy contributes to the loss of grafts. One of the problem is the fractioning of immunosuppressive dose. In fact, it was demonstrated that a single daily dose (QD) is associated with an increased adherence to therapy compared with twice daily dosing (BID). Tacrolimus (TAC), calcineurin inhibitor, is one of immunosuppression pillar in organ transplantation and its action is strongly correlated with blood concentration and therefore the therapeutic drug monitoring is recommended in the guidelines. However, one of the critical points of TAC is the poor and variable bioavailability that influences immunosuppression, and is also responsible for adverse effects.
METHODS
MeltDose® Technology is a new technology to improve efficacy and/or reduce side effects. This new technology applied to TAC (Envarsus® or LCP-TAC) has achieved 4 main objectives: (1) improved bioavailability, (2) reduced dose fractioning to one tablet per day, (3) limited variability concentrations of TAC, and (4) lower doses of TAC will be administered.
RESULTS
We analyzed the pharmacokinetic profile, efficacy, and security of Envarsus®.
背景
免疫抑制治疗依从性差会导致移植物丧失。问题之一是免疫抑制剂量的分割。事实上，已证明与每日两次给药（BID）相比，每日单次剂量（QD）与治疗依从性增加相关。他克莫司（TAC），一种钙调神经磷酸酶抑制剂，是器官移植中免疫抑制的支柱之一，其作用与血药浓度密切相关，因此指南建议进行治疗药物监测。然而，TAC的关键点之一是生物利用度差且变化不定，这会影响免疫抑制，也会导致不良反应。
方法
MeltDose®技术是一种提高疗效和/或减少副作用的新技术。应用于TAC（Envarsus®或LCP-TAC）的这项新技术实现了4个主要目标：（1）提高生物利用度，（2）将剂量分割减少至每日一片，（3）TAC浓度变异性有限，（4）将给予更低剂量的TAC。
结果
我们分析了Envarsus®的药代动力学特征、疗效和安全性。
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