Decloedt E H, van der Walt J S, McIlleron H, Wiesner L, Maartens G
Division of Clinical Pharmacology, Department of Medicine, Groote Schuur Hospital, University of Cape Town, Cape Town, South Africa.
Int J Tuberc Lung Dis. 2015 Oct;19(10):1194-6. doi: 10.5588/ijtld.15.0044.
Isoniazid preventive therapy is recommended in patients on antiretroviral treatment (ART) with latent tuberculous infection to prevent progression to active tuberculosis disease. Isoniazid (INH) inhibits cytochrome (CY) P3A4, which metabolises lopinavir (LPV). The administration of INH may cause higher LPV concentrations, which may increase LPV toxicity. LPV bioavailability is increased by co-formulated ritonavir (r), which may enhance the interaction of INH on LPV. We studied the effect of INH on LPV concentrations by administering INH for 7 days and performing intensive pharmacokinetic sampling in 16 human immunodeficiency virus infected patients established on LPV/r-based ART. INH did not significantly increase steady-state LPV area under the plasma concentration-time curve calculated for the 12 h-dosing interval.
对于接受抗逆转录病毒治疗(ART)且患有潜伏性结核感染的患者,推荐使用异烟肼预防性治疗,以防止进展为活动性结核病。异烟肼(INH)抑制细胞色素(CY)P3A4,而细胞色素P3A4可代谢洛匹那韦(LPV)。服用INH可能会导致更高的LPV浓度,这可能会增加LPV的毒性。利托那韦(r)与LPV共同配制可提高LPV的生物利用度,这可能会增强INH对LPV的相互作用。我们通过对16例接受基于LPV/r的ART治疗的人类免疫缺陷病毒感染患者给予INH 7天并进行密集的药代动力学采样,研究了INH对LPV浓度的影响。对于12小时给药间隔计算的血浆浓度-时间曲线下,INH并未显著增加稳态LPV面积。