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精液中高浓度雷替拉韦:EASIER-ANRS 138 试验的亚研究结果。

High concentration of raltegravir in semen of HIV-infected men: results from a substudy of the EASIER-ANRS 138 trial.

机构信息

Department of Clinical Pharmacy, Bicêtre Hospital, Assistance Publique Hôpitaux de Paris, 78 Rue du Général Leclerc, 94275 Le Kremlin Bicêtre, France.

出版信息

Antimicrob Agents Chemother. 2010 Feb;54(2):937-9. doi: 10.1128/AAC.01261-09. Epub 2009 Dec 7.

Abstract

Raltegravir concentrations and human immunodeficiency virus type 1 (HIV-1) RNA levels in semen samples from 10 treatment-experienced HIV-1-infected patients were measured after 24 weeks of raltegravir-based highly active antiretroviral therapy (HAART). Semen and plasma HIV-1 RNA levels were below 100 copies/ml and 50 copies/ml, respectively, in all samples. The median raltegravir concentrations in semen samples (n=10) and in plasma samples (n=9) drawn simultaneously were 345 (range, 83 to 707) ng/ml and 206 (range, 106 to 986) ng/ml, respectively. The median semen-to-plasma ratio of raltegravir concentration was 1.42 (range, 0.52 to 6.66), indicating good although variable levels of drug penetration of raltegravir in the seminal compartment.

摘要

在接受拉替拉韦为基础的高效抗逆转录病毒治疗(HAART) 24 周后,检测了 10 名治疗经验丰富的 HIV-1 感染患者的精液样本中的拉替拉韦浓度和人类免疫缺陷病毒 1(HIV-1)RNA 水平。所有样本中的精液和血浆 HIV-1 RNA 水平均低于 100 拷贝/ml 和 50 拷贝/ml。同时采集的 10 份精液样本(n=10)和 9 份血浆样本(n=9)中拉替拉韦的中位数浓度分别为 345(范围,83 至 707)ng/ml 和 206(范围,106 至 986)ng/ml。拉替拉韦浓度的精液与血浆比值中位数为 1.42(范围,0.52 至 6.66),表明拉替拉韦在精液中具有良好的药物穿透性,但存在变异性。

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