de Kock M, Tarning J, Workman L, Nyunt M M, Adam I, Barnes K I, Denti P
Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Cape Town, South Africa.
World Wide Antimalarial Resistance Network (WWARN), Oxford, UK.
CPT Pharmacometrics Syst Pharmacol. 2017 Jul;6(7):430-438. doi: 10.1002/psp4.12181. Epub 2017 Jun 9.
Sulfadoxine/pyrimethamine is recommended for intermittent preventative treatment of malaria during pregnancy. Data from 98 women during pregnancy and 77 after delivery in four African countries were analyzed using nonlinear mixed-effects modeling to characterize the effects of pregnancy, postpartum duration, and other covariates such as body weight and hematocrit on sulfadoxine/pyrimethamine pharmacokinetic properties. During pregnancy, clearance increased 3-fold for sulfadoxine but decreased by 18% for pyrimethamine. Postpartum sulfadoxine clearance decreased gradually over 13 weeks. This finding, together with hematocrit-based scaling of plasma to whole-blood concentrations and allometric scaling of pharmacokinetics parameters with body weight, enabled site-specific differences in the pharmacokinetic profiles to be reduced significantly but not eliminated. Further research is necessary to explain residual site-specific differences and elucidate whether dose-optimization, to address the 3-fold increase in clearance of sulfadoxine in pregnant women, is necessary, viable, and safe with the current fixed dose combination of sulfadoxine/pyrimethamine.
磺胺多辛/乙胺嘧啶被推荐用于孕期疟疾的间歇性预防治疗。利用非线性混合效应模型分析了四个非洲国家98名孕期妇女和77名产后妇女的数据,以表征怀孕、产后持续时间以及体重和血细胞比容等其他协变量对磺胺多辛/乙胺嘧啶药代动力学特性的影响。孕期,磺胺多辛的清除率增加了3倍,但乙胺嘧啶的清除率下降了18%。产后磺胺多辛的清除率在13周内逐渐下降。这一发现,连同基于血细胞比容将血浆浓度换算为全血浓度以及药代动力学参数随体重的异速生长换算,使得药代动力学曲线中的位点特异性差异显著减小但并未消除。有必要开展进一步研究以解释残留的位点特异性差异,并阐明对于孕妇中磺胺多辛清除率增加3倍的情况,使用当前固定剂量组合的磺胺多辛/乙胺嘧啶进行剂量优化是否必要、可行且安全。