Mwebaza Norah, Roh Michelle E, Geng Yourong Z, Opio Leonard, Opira Bishop, Marzan Florence, Mwima Moses W, Ssemukuye Timothy, Guo Kevin, Gingrich David, Fotaki Nikoletta, Kakuru Abel, Kizza Jimmy, Aguti Miriam, Adrama Harriet, Kamya Moses, Dorsey Grant, Rosenthal Philip J, Aweeka Francesca T, Huang Liusheng
Infectious Disease Research Collaboration, Kampala, Uganda.
Department of Pharmacology and Therapeutics, Makerere University, Kampala, Uganda.
Clin Pharmacol Ther. 2025 Feb;117(2):506-514. doi: 10.1002/cpt.3471. Epub 2024 Oct 14.
Co-administration of dihydroartemisinin-piperaquine (DP) and sulfadoxine-pyrimethamine (SP) for intermittent preventive treatment of malaria in pregnancy (IPTp) may be superior in preventing adverse birth outcomes compared with either therapy alone, but potential drug-drug interactions require investigation. We conducted intensive and sparse pharmacokinetic (PK) studies in a subset of Ugandan women participating in a randomized controlled trial of monthly IPTp with SP vs. DP vs. DP + SP. Intensive PK sampling was performed from day 0 to 23 after dosing at 28 weeks gestation in 87 participants across treatment arms. Sparse sampling was performed on day 28 (trough) after dosing at 20 and 28 gestational weeks in additional 196 participants receiving SP vs. DP + SP. Intensive PK analysis demonstrated that compared with SP alone, co-administration of DP + SP was associated with lower maximal concentrations, the area under the concentration-time curves (AUC), and day 23 concentrations of sulfadoxine (25%, 25%, and 27%) and pyrimethamine (26%, 34%, and 32%) (P < 0.05 for all comparisons). Sparse PK results demonstrated participants co-administered DP + SP had lower trough concentrations after dosing at 20 and 28 gestational weeks for sulfadoxine (6%, P = 0.68 and 31%, P = 0.023, respectively) and pyrimethamine (18%, P = 0.032 and 33%, P < 0.001, respectively) compared with SP alone. Co-administration of DP + SP was associated with a 19% reduction in piperaquine AUC (P = 0.046), but no significant difference in other PK parameters compared with DP alone. In summary, co-administration of DP + SP was associated with significantly reduced SP exposure, with a greater magnitude during the third vs. second trimester. The clinical consequences of this interaction are yet unknown.
在孕期疟疾间歇性预防治疗(IPTp)中,联合使用双氢青蒿素 - 哌喹(DP)和磺胺多辛 - 乙胺嘧啶(SP)预防不良分娩结局可能优于单独使用任何一种疗法,但潜在的药物相互作用需要研究。我们在参与每月IPTp随机对照试验的乌干达女性亚组中进行了密集和稀疏药代动力学(PK)研究,该试验比较了SP与DP与DP + SP。在87名各治疗组参与者妊娠28周给药后第0天至23天进行密集PK采样。在另外196名接受SP与DP + SP的参与者妊娠20周和28周给药后第28天(谷值)进行稀疏采样。密集PK分析表明,与单独使用SP相比,联合使用DP + SP与较低的最大浓度、浓度 - 时间曲线下面积(AUC)以及第23天磺胺多辛(分别降低25%、25%和27%)和乙胺嘧啶(分别降低26%、34%和32%)的浓度相关(所有比较P < 0.05)。稀疏PK结果表明,与单独使用SP相比,联合使用DP + SP的参与者在妊娠20周和28周给药后,磺胺多辛的谷值浓度较低(分别为6%,P = 0.68和31%,P = 0.023)和乙胺嘧啶(分别为18%,P = 0.032和33%,P < 0.001)。联合使用DP + SP与哌喹AUC降低19%相关(P = 0.046),但与单独使用DP相比,其他PK参数无显著差异。总之,联合使用DP + SP与显著降低的SP暴露相关,在孕晚期比孕中期幅度更大。这种相互作用的临床后果尚不清楚。