HIV 感染患者精浆中的依曲韦林浓度。

Etravirine concentrations in seminal plasma in HIV-infected patients.

机构信息

HIV Unit, Infectious Disease Service, Hospital Universitari de Bellvitge, L'Hospitalet de Llobregat, 08907 Barcelona, Spain.

出版信息

J Antimicrob Chemother. 2013 Jan;68(1):184-7. doi: 10.1093/jac/dks360. Epub 2012 Sep 6.

DOI:10.1093/jac/dks360

PMID:22954493

Abstract

OBJECTIVES

To determine etravirine concentrations and the HIV-1 viral load (VL) in blood plasma (BP) and seminal plasma (SP) of HIV-infected patients.

METHODS

Ten adult antiretroviral-experienced HIV-1 patients receiving an etravirine-containing regimen for at least 1 month were enrolled. Semen and blood samples were collected ~12 or 24 h after the last etravirine dose, depending on twice-daily or once-daily dosing, respectively. Liquid chromatography tandem mass spectrometry was used to determine etravirine concentrations and HIV-1 VL was determined by real-time PCR (detection limit 40 copies/mL). Results are presented as the median (range) unless otherwise indicated.

RESULTS

Ten blood and 20 semen samples were collected. The CD4 count was 502 (252-817) cells/mm(3) and the BP VL was <40 (<40-362) copies/mL. The time on etravirine was 52 (12-124) weeks. The BP etravirine concentration was 452.5 (258-751) ng/mL. The SP etravirine concentration was 62.9 (31.2-166.0) ng/mL and values were above the IC(50) range (0.39-2.4 ng/mL) in all cases. The median etravirine SP:BP ratio was 0.16 (0.07-0.26). The SP VL was <40 copies/mL in all patients, whereas the BP VL was detectable in one patient with poor adherence to treatment.

CONCLUSIONS

Etravirine concentrations in male genital secretions are modest, reaching only 16% of the BP concentration. Nevertheless, they are more than 10 times greater than the wild-type IC(50) range (not adjusted for protein binding).

摘要

目的

测定接受依曲韦林（etravirine）治疗的 HIV 感染者的血血浆（BP）和精浆（SP）中的依曲韦林浓度和 HIV-1 病毒载量（VL）。

方法

共纳入 10 例接受含依曲韦林方案治疗至少 1 个月的成年、有抗逆转录病毒治疗史的 HIV-1 感染者。根据每日 2 次或 1 次给药方案，分别在末次依曲韦林给药后 12 或 24 h 采集精液和血液样本。采用液相色谱串联质谱法测定依曲韦林浓度，采用实时 PCR 法（检测限 40 拷贝/ml）测定 HIV-1 VL。结果以中位数（范围）表示，除非另有说明。

结果

共采集 10 份 BP 样本和 20 份 SP 样本。CD4 计数为 502（252-817）个细胞/mm3，BP VL<40（<40-362）拷贝/ml。依曲韦林治疗时间为 52（12-124）周。BP 中依曲韦林浓度为 452.5（258-751）ng/ml。SP 中依曲韦林浓度为 62.9（31.2-166.0）ng/ml，所有患者的浓度均在 IC50 范围（0.39-2.4 ng/ml）之上。SP 中依曲韦林与 BP 中依曲韦林浓度比值的中位数为 0.16（0.07-0.26）。所有患者 SP VL<40 拷贝/ml，而 1 例患者因治疗依从性差 BP VL 可检测到。