*Department of Gynecology and Obstetrics, Medical School of Ribeirao Preto, University of São Paulo, São Paulo, Brazil. Avenida Bandeirantes, Ribeirão Preto, São Paulo, Brazil; †National Institute of Hormones and Women's Health, Brazil; ‡Department of Obstetrics and Gynecology, Faculty of Medical Sciences, University of Campinas, Campinas, São Paulo, Brazil; §Federal Technological University of Paraná, Campus Cornélio Procópio, Brazil. Avenida Alberto Carazzai, Cornélio Procópio, Paraná, Brazil; and ‖Department of Gynecology and Obstetrics, Federal University of Bahia. R. Augusto Viana, 1-Canela, CEP: 40110-060, Salvador, Bahia, Brazil.
J Acquir Immune Defic Syndr. 2014 Aug 1;66(4):378-85. doi: 10.1097/QAI.0000000000000189.
Data on the interaction between the etonogestrel (ENG) implant and antiretroviral therapy are lacking. We evaluated the effect of 2 highly active antiretroviral therapy (HAART) regimens (1 including efavirenz and the other ritonavir-boosted lopinavir) on the pharmacokinetic (PK) parameters of an ENG-releasing implant in HIV-positive women.
Prospective nonrandomized PK study.
Forty-five HIV-positive women who desired to use ENG implants were included: 15 had received zidovudine/lamivudine + lopinavir/ritonavir for ≥3 months (LPV/r-based HAART group), 15 had received zidovudine/lamivudine + efavirenz for ≥3 months (EFV-based HAART group), and 15 had not received HAART (non-HAART group). PK parameters were measured using ultra-performance liquid chromatography-mass spectrometry at baseline and 2, 4, 6, 8, 10, 12, 16, 20, and 24 weeks after implant placement.
The EFV-based HAART regimen was associated with a reduction in the bioavailability of ENG, which showed decreases of 63.4%, 53.7%, and 70% in the area under the curve (AUC), maximum concentration (Cmax), and minimum concentration (Cmin) of ENG, respectively, compared with the non-HAART group. The LPV/r-based HAART regimen was associated with an increase in ENG bioavailability, which showed 52%, 60.6%, and 33.8% increases in the ENG AUC, Cmax, and Cmin, respectively, compared with the non-HAART group.
The coadministration of EFV decreased the bioavailability of ENG released from the implant, which could impair contraceptive efficacy. However, the coadministration of LPV/r increased the bioavailability of ENG released from the implant, which suggests that this antiretroviral combination does not impair the ENG implant efficacy.
缺乏关于依托孕烯（ENG）埋植剂与抗逆转录病毒疗法相互作用的数据。我们评估了 2 种高效抗逆转录病毒疗法（HAART）方案（1 种方案包括依非韦伦，另 1 种方案为利托那韦增强洛匹那韦）对 HIV 阳性妇女中释放 ENG 的埋植剂的药代动力学（PK）参数的影响。
前瞻性非随机 PK 研究。
纳入了 45 名希望使用 ENG 埋植剂的 HIV 阳性女性：15 名女性已接受齐多夫定/拉米夫定+洛匹那韦/利托那韦治疗≥3 个月（洛匹那韦/利托那韦为基础的 HAART 组），15 名女性已接受齐多夫定/拉米夫定+依非韦伦治疗≥3 个月（依非韦伦为基础的 HAART 组），15 名女性未接受 HAART（非 HAART 组）。基线和埋植后 2、4、6、8、10、12、16、20 和 24 周时使用超高效液相色谱-质谱法测量 PK 参数。
依非韦伦为基础的 HAART 方案与 ENG 的生物利用度降低相关，与非 HAART 组相比，ENG 的 AUC、Cmax 和 Cmin 分别降低 63.4%、53.7%和 70%。洛匹那韦/利托那韦为基础的 HAART 方案与 ENG 生物利用度增加相关，与非 HAART 组相比，ENG 的 AUC、Cmax 和 Cmin 分别增加 52%、60.6%和 33.8%。
依非韦伦的联合用药降低了从埋植剂中释放的 ENG 的生物利用度，这可能会降低避孕效果。然而，洛匹那韦/利托那韦的联合用药增加了从埋植剂中释放的 ENG 的生物利用度，这表明这种抗逆转录病毒联合用药不会损害 ENG 埋植剂的疗效。
Zotero 插件