恩曲他滨/替诺福韦治疗HIV感染:目前PK/PD评价。
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Uglietti A, Zanaboni D, Gnarini M，玛莎拉蒂R
恩曲他滨/替诺福韦治疗HIV感染:目前PK/PD评价。
专家意见药物meta毒理学2012 Oct;8(10):1305-14。doi: 10.1517 / 17425255.2012.714367。Epub 2012 9月4日。
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22943210 (PubMed视图］
- 摘要
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介绍:恩曲他滨/富马酸替诺福韦二吡酯固定剂量组合(FTC/TDF FDC)分别是核苷和核苷酸的共配方。口服给药后，两种药物的血浆和细胞内半衰期适合每日一次给药。在宿主细胞内，活性代谢产物FTC-TP和TFV-DP作为新合成的前病毒DNA的链终止物，在酶水平上表现出协同作用(病毒逆转录酶)。当在HAART组合中给予FTC/TDF FDC时，在控制HIV复制和确保显著的CD4(+)细胞恢复方面具有显著的效果。如果患者接受FTC/TDF FDC治疗失败，则TDF相关K65R耐药突变的发病率似乎会降低。此外，与拉米夫定同时给予TDF时，与FTC相比，胞苷类似物相关的M184V更不可能出现。FTC和TFV不被CYP450酶代谢，由肾脏途径消除。TFV可能积聚在小管细胞中，导致GFR降低和磷酸盐的损失。因此，接受FTC/TDF FCD治疗的患者可能会出现不同程度的肾损害和骨质减少/骨质疏松症。研究范围:本文主要研究了FTC和TDF在单药给药或作为FDC给药时的PK/PD特性。 The interpretation of efficacy/toxicity was guided by PK/PD features. The review of the available literature included also conference presentations and recent guidelines (as of May 2012). EXPERT OPINION: FTC/TDF FDC is a potent and reliable component of most HAART combinations due to its maintained activity across time, as demonstrated in many trials and studies. Toxicity issues (kidney, bone) are still to be entirely elucidated and the drug-induced component well separated from patient- and HIV-related ones. However, the clinical gain associated with the use of FTC/TDF FDC is fully acknowledged by its leading position in most current treatment guidelines.
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