Lluita contra la SIDA Foundation, HIV Clinic, Hospital Universitari Germans Trias i Pujol, Badalona, Spain.
Antimicrob Agents Chemother. 2012 Oct;56(10):5328-31. doi: 10.1128/AAC.01205-12. Epub 2012 Aug 6.
The aim of this open-label, fixed-sequence study was to investigate the potential of the botanical supplement Echinacea purpurea to interact with etravirine, a nonnucleoside reverse transcriptase inhibitor of HIV. Fifteen HIV-infected patients receiving antiretroviral therapy with etravirine (400 mg once daily) for at least 4 weeks were included. E. purpurea root/extract-containing capsules were added to the antiretroviral treatment (500 mg every 8 h) for 14 days. Etravirine concentrations in plasma were determined by high-performance liquid chromatography immediately before and 1, 2, 4, 6, 8, 10, 12, and 24 h after a morning dose of etravirine on day 0 and etravirine plus E. purpurea on day 14. Individual etravirine pharmacokinetic parameters were calculated by noncompartmental analysis and compared between days 0 and 14 by means of the geometric mean ratio (GMR) and its 90% confidence interval (CI). The median age was 46 years (interquartile range, 41 to 50), and the median body weight was 76 kg (interquartile range, 68 to 92). Echinacea was well tolerated, and all participants completed the study. The GMR for etravirine coadministered with E. purpurea relative to etravirine alone was 1.07 (90% CI, 0.81 to 1.42) for the maximum concentration, 1.04 (90% CI, 0.79 to 1.38) for the area under the concentration-time curve from 0 to 24 h, and 1.04 (90% CI, 0.74 to 1.44) for the concentration at the end of the dosing interval. In conclusion, the coadministration of E. purpurea with etravirine was safe and well tolerated in HIV-infected patients; our data suggest that no dose adjustment for etravirine is necessary.
这项开放标签、固定序列研究的目的是研究草药紫锥菊提取物(Echinacea purpurea)与依曲韦林（一种非核苷类逆转录酶抑制剂，用于治疗 HIV）相互作用的潜力。研究纳入了 15 名接受依曲韦林（每日一次，400mg）治疗至少 4 周的 HIV 感染者。在接受依曲韦林（每日一次，400mg）治疗的基础上添加紫锥菊根/提取物胶囊（每 8 小时 500mg），治疗 14 天。在第 0 天和第 14 天的早晨服用依曲韦林和依曲韦林加紫锥菊后，分别在 1、2、4、6、8、10、12 和 24 小时，通过高效液相色谱法测定血浆中依曲韦林的浓度。通过非房室分析计算个体依曲韦林药代动力学参数，并通过几何均数比值（GMR）及其 90%置信区间（CI）比较第 0 天和第 14 天的参数。中位年龄为 46 岁（四分位间距，41 至 50），中位体重为 76kg（四分位间距，68 至 92）。紫锥菊耐受性良好，所有参与者均完成了研究。与单独使用依曲韦林相比，依曲韦林与紫锥菊合用的最大浓度的 GMR 为 1.07（90%CI，0.81 至 1.42），0 至 24 小时的浓度-时间曲线下面积的 GMR 为 1.04（90%CI，0.79 至 1.38），浓度达峰时间的 GMR 为 1.04（90%CI，0.74 至 1.44）。结论：在 HIV 感染者中，依曲韦林与紫锥菊联合应用安全且耐受良好；我们的数据表明，依曲韦林无需调整剂量。
