Bartelink Imke H, Savic Rada M, Mwesigwa Julia, Achan Jane, Clark Tamara, Plenty Albert, Charlebois Edwin, Kamya Moses, Young Sera L, Gandhi Monica, Havlir Diane, Cohan Deborah, Aweeka Francesca
Department of Clinical Pharmacy, Drug Research Unit, University of California, San Francisco, CA, USA.
J Clin Pharmacol. 2014 Feb;54(2):121-32. doi: 10.1002/jcph.167. Epub 2013 Sep 21.
Pregnancy and food insecurity may impact antiretroviral (ART) pharmacokinetics (PK), adherence and response. We sought to quantify and characterize the PK of lopinavir/ritonavir (LPV/r) and efavirenz (EFV) by pregnancy and nutritional status among HIV-infected women in Tororo, Uganda. In 2011, 62/225 ante-partum/post-partum single dried blood spot samples DBS and 43 post-partum hair samples for LPV/r were derived from 116 women, 51/194 ante-/post-partum DBS and 53 post-partum hair samples for EFV from 105 women. Eighty percent of Ugandan participants were severely food insecure, 26% lost weight ante-partum, and median BMI post-partum was only 20.2 kg/m(2) . Rich PK-data of normally nourished (pregnant) women and healthy Ugandans established prior information. Overall, drug exposure was reduced (LPV -33%, EFV -15%, ritonavir -17%) compared to well-nourished controls (P < 0.001), attributable to decreased bioavailability. Pregnancy increased LPV/r clearance 68% (P < 0.001), whereas EFV clearance remained unchanged. Hair concentrations correlated with plasma-exposure (P < 0.001), explaining 29% PK-variability. In conclusion, pregnancy and food insecurity were associated with lower ART exposures in this cohort of predominantly underweight women, compared to well-nourished women. Much variability in plasma-exposure was quantified using hair concentrations. Addressing malnutrition as well as ART-PK in this setting should be a priority.
怀孕和粮食不安全可能会影响抗逆转录病毒(ART)药物动力学(PK)、依从性及疗效。我们试图在乌干达托罗罗的HIV感染女性中,根据怀孕情况和营养状况,对洛匹那韦/利托那韦(LPV/r)和依非韦伦(EFV)的PK进行量化和特征分析。2011年,116名女性提供了62份用于LPV/r检测的产前/产后单份干血斑样本(DBS)和43份产后毛发样本,105名女性提供了51份用于EFV检测的产前/产后DBS样本和53份产后毛发样本。80%的乌干达参与者存在严重的粮食不安全问题,26%的女性在产前体重减轻,产后BMI中位数仅为20.2kg/m²。正常营养(怀孕)女性和健康乌干达人的丰富PK数据提供了先验信息。总体而言,与营养良好的对照组相比,药物暴露量降低(LPV降低33%,EFV降低15%,利托那韦降低17%)(P<0.001),这归因于生物利用度降低。怀孕使LPV/r清除率提高了68%(P<0.001),而EFV清除率保持不变。毛发浓度与血浆暴露相关(P<0.001),可解释29%的PK变异性。总之,与营养良好的女性相比,在这个以体重过轻女性为主的队列中,怀孕和粮食不安全与较低的ART暴露相关。利用毛发浓度对血浆暴露的很大变异性进行了量化。在这种情况下,解决营养不良以及ART-PK问题应成为优先事项。