Emtricitabine /替诺福韦治疗艾滋病毒感染:当前PK / PD评估。

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Uglietti, Zanaboni D, Gnarini M,玛莎拉蒂R

Emtricitabine /替诺福韦治疗艾滋病毒感染:当前PK / PD评估。

专家当今药物金属底座Toxicol。2012年10月8日(10):1305 - 14所示。doi: 10.1517 / 17425255.2012.714367。Epub 2012年9月4。

PubMed ID

22943210 (在PubMed

]

文摘

简介:Emtricitabine /替诺福韦disoproxil延胡索酸酯(FTC / TDF FDC)固定剂量组合的co-formulation核苷和核苷酸,分别。口服后,这两种药物表现出等离子体和胞内半衰期适合每天换一次剂量。在宿主细胞内,活性代谢物FTC-TP和TFV-DP作为新合成病毒DNA链终止剂,显示协同酶水平(病毒逆转录酶)。鸡尾酒疗法的组合,FTC / TDF FDC有显著的有效性控制艾滋病毒复制和获得一个重要的CD4(+)细胞复苏。如果患者FTC / TDF FDC失败,一个较低的发病率TDF-associated K65R电阻突变似乎发展。此外,胞嘧啶核苷analog-associated M184V不大可能出现与FTC比拉米夫定在了TDF。FTC和TFV不是由CYP450酶和代谢消除肾路线。TFV可能积聚在管状细胞和引起肾小球滤过率(GFR)下降和磷酸盐的丧失。onsequence, FTC / TDF FCD患者可能经历不同程度的肾功能损害和骨量减少、骨质疏松症。覆盖区域:本文集中在贸易委员会和TDF的PK / PD特性,当作为单药或当FDC管理。 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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药物

替诺福韦disoproxil