Taylor S, van Heeswijk R P, Hoetelmans R M, Workman J, Drake S M, White D J, Pillay D
PHLS Antiviral Susceptibility Reference Unit, Division of Immunity and Infection, University of Birmingham, UK.
AIDS. 2000 Sep 8;14(13):1979-84. doi: 10.1097/00002030-200009080-00014.
To determine the concentrations of nevirapine (NVP), lamivudine (3TC) and stavudine (D4T) in seminal and blood plasma in HIV-1-infected men.
Twelve HIV-1-infected men on NVP-containing regimens including 3TC (n = 8) or D4T (n = 11) provided 23 blood plasma and 22 seminal plasma samples for drug concentration and viral load quantitation. Concentrations of all drugs were assessed by sensitive validated high performance liquid chromatography (HPLC) assays. Blood plasma and seminal plasma viral loads were measured using nucleic acid sequence-based amplification (NASBA). Samples were grouped according to time after drug ingestion, 0-2, 2-4, 4-8 and 8-12 h. For matched seminal and blood plasma samples, obtained within 1 h of each other, a seminal:blood plasma ratio was calculated.
The concentration of NVP in seminal plasma appeared to mirror the concentrations in blood plasma. Absolute median seminal plasma NVP concentrations at 0-2, 2-4, 4-8 and 8-12 h were 3.1 microg/ml (range 1.7-4.89), 2.68 microg/ml (2.5-3.9), 2.5 microg/ml (2.3-2.7) and 3.09 microg/ml (1.3-9.1). The median seminal:blood plasma ratios for the four time periods were 0.54 (range 0.34-0.85), 0.83 (range 0.43-1.08), 0.53 (0.48-0.59), and 0.61 (0.59-0.78). 3TC and D4T appeared to reach concentrations in seminal plasma of a similar magnitude or higher than concentrations in blood plasma. The median seminal plasma viral load for all patients was less than 800 copies/ml (range < 800-11000). The median blood plasma viral load was less than 400 copies/ml (< 400-1100).
NVP reaches concentrations in the semen approximately 60% of those in the blood plasma throughout the 12 h dosing period. In a smaller dataset, 3TC and D4T concentrations in blood plasma and seminal plasma were similar. These data may well have implications for the evolution of drug-resistant virus within the genital tract.
测定感染人类免疫缺陷病毒1型（HIV-1）男性的精液和血浆中奈韦拉平（NVP）、拉米夫定（3TC）和司他夫定（D4T）的浓度。
12名接受含NVP治疗方案（包括3TC，n = 8；或D4T，n = 11）的HIV-1感染男性提供了23份血浆和22份精液样本用于药物浓度和病毒载量定量。所有药物的浓度通过经过验证的灵敏高效液相色谱（HPLC）测定法进行评估。血浆和精液中的病毒载量采用基于核酸序列的扩增（NASBA）法进行测定。样本根据服药后的时间分组，分别为0 - 2小时、2 - 4小时、4 - 8小时和8 - 12小时。对于在1小时内采集的配对精液和血浆样本，计算精液与血浆的比值。
精液中NVP的浓度似乎与血浆中的浓度相对应。在0 - 2小时、2 - 4小时、4 - 8小时和8 - 12小时，精液中NVP的绝对中位浓度分别为3.1微克/毫升（范围1.7 - 4.89）、2.68微克/毫升（2.5 - 3.9）、2.5微克/毫升（2.3 - 2.7）和3.09微克/毫升（1.3 - 9.1）。这四个时间段精液与血浆的中位比值分别为0.54（范围0.34 - 0.85）、0.83（范围0.43 - 1.08）、0.53（0.48 - 0.59）和0.61（0.59 - 0.78）。3TC和D4T在精液中的浓度似乎达到了与血浆中相似或更高的水平。所有患者精液中的病毒载量中位数低于800拷贝/毫升（范围< 800 - 11000）。血浆中的病毒载量中位数低于400拷贝/毫升（< 400 - 1100）。
在12小时的给药期内，NVP在精液中的浓度约为血浆浓度的60%。在一个较小的数据集中，血浆和精液中3TC和D4T的浓度相似。这些数据可能对生殖道内耐药病毒的演变有影响。
