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Joint population pharmacokinetic analysis of zidovudine, lamivudine, and their active intracellular metabolites in HIV patients.齐多夫定、拉米夫定及其在 HIV 患者体内的活性代谢物的联合群体药代动力学分析。
Antimicrob Agents Chemother. 2011 Jul;55(7):3423-31. doi: 10.1128/AAC.01487-10. Epub 2011 May 16.
2
Nonnucleoside reverse transcriptase inhibitor concentrations during treatment interruptions and the emergence of resistance: a substudy of the ISS-PART Trial.治疗中断期间非核苷类逆转录酶抑制剂浓度与耐药性的出现:ISS-PART试验的一项子研究
AIDS Res Hum Retroviruses. 2010 May;26(5):541-5. doi: 10.1089/aid.2009.0116.
3
A novel polymorphism in ABCB1 gene, CYP2B6*6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans.一种新的 ABCB1 基因、CYP2B6*6 和性别多态性可预测乌干达人体内单剂量依非韦伦的群体药代动力学。
Br J Clin Pharmacol. 2009 Nov;68(5):690-9. doi: 10.1111/j.1365-2125.2009.03516.x.
4
Efficacy of short-course AZT plus 3TC to reduce nevirapine resistance in the prevention of mother-to-child HIV transmission: a randomized clinical trial.短程 AZT 加 3TC 降低奈韦拉平耐药性预防母婴 HIV 传播的疗效:一项随机临床试验。
PLoS Med. 2009 Oct;6(10):e1000172. doi: 10.1371/journal.pmed.1000172. Epub 2009 Oct 27.
5
Substrate specificity, regulation, and polymorphism of human cytochrome P450 2B6.人细胞色素 P450 2B6 的底物特异性、调控和多态性。
Curr Drug Metab. 2009 Sep;10(7):730-53. doi: 10.2174/138920009789895534.
6
CYP2B6 variants and plasma efavirenz concentrations during antiretroviral therapy in Port-au-Prince, Haiti.海地太子港抗逆转录病毒治疗期间CYP2B6基因变体与血浆依非韦伦浓度
J Infect Dis. 2009 Sep 15;200(6):955-64. doi: 10.1086/605126.
7
CYP2B6 G516T genotyping in a UK cohort of HIV-positive patients: polymorphism frequency and influence on efavirenz discontinuation.英国 HIV 阳性患者队列中的 CYP2B6 G516T 基因分型:多态性频率及对依非韦伦停药的影响。
HIV Med. 2009 Sep;10(8):520-3. doi: 10.1111/j.1468-1293.2009.00718.x. Epub 2009 May 21.
8
Associations between CYP2B6 polymorphisms and pharmacokinetics after a single dose of nevirapine or efavirenz in African americans.非裔美国人单次服用奈韦拉平或依非韦伦后CYP2B6基因多态性与药代动力学之间的关联。
J Infect Dis. 2009 Mar 15;199(6):872-80. doi: 10.1086/597125.
9
In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function.对CYP2A6功能受损个体中依非韦伦代谢的体内分析。
Pharmacogenet Genomics. 2009 Apr;19(4):300-9. doi: 10.1097/FPC.0b013e328328d577.
10
HIV-1-resistant strains during 8-week on 8-week off intermittent therapy and their effect on CD4+ T-cell counts and antiviral response.8周治疗、8周停药间歇疗法期间的HIV-1耐药毒株及其对CD4+T细胞计数和抗病毒反应的影响。
Antivir Ther. 2008;13(4):537-45.

拉米夫定或恩曲他滨的存在与基于依非韦伦的间歇性抗逆转录病毒治疗方案中非核苷类逆转录酶抑制剂突变的减少有关。

Presence of lamivudine or emtricitabine is associated with reduced emergence of nonnucleoside reverse transcriptase inhibitor mutations in an efavirenz-based intermittent antiretroviral treatment regimen.

机构信息

Laboratory of Pharmacology, Hospital Purpan, Toulouse, France.

出版信息

Antimicrob Agents Chemother. 2012 Mar;56(3):1655-7. doi: 10.1128/AAC.05452-11. Epub 2011 Dec 27.

DOI:10.1128/AAC.05452-11
PMID:22203586
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3294880/
Abstract

Efavirenz concentrations were measured in 21 patients during an interruption cycle of the ANRS 106 Window trial. The median efavirenz concentrations in the patients 12 h, 3 days, and 7 days after discontinuation of the drug were 1,962 ng/ml, 416 ng/ml, and 112 ng/ml, respectively. The half-life ranged from 27 to 136 h. No relationship between efavirenz exposure and detection of nonnucleoside reverse transcriptase inhibitor (NNRTI) mutations was demonstrated. Patients who were treated by a lamivudine- or emtricitabine-based regimen had a lower risk of NNRTI mutation selection.

摘要

在 ANRS 106 Window 试验的中断周期中,对 21 名患者进行了依非韦伦浓度检测。停药后 12 小时、3 天和 7 天,患者依非韦伦浓度中位数分别为 1962ng/ml、416ng/ml 和 112ng/ml。半衰期范围为 27 至 136 小时。未发现依非韦伦暴露与非核苷类逆转录酶抑制剂(NNRTI)突变检测之间存在关系。接受拉米夫定或恩曲他滨为基础的方案治疗的患者,NNRTI 突变选择的风险较低。