Centre for Tropical Medicine, Nuffield Department of Medicine, University of Oxford, Oxford, United Kingdom.
Antimicrob Agents Chemother. 2013 Oct;57(10):5096-103. doi: 10.1128/AAC.00683-13. Epub 2013 Aug 5.
Pregnancy alters the pharmacokinetic properties of many drugs used in the treatment of malaria, usually resulting in lower drug exposures. This increases the risks of treatment failure, adverse outcomes for the fetus, and the development of resistance. The pharmacokinetic properties of artemether and its principal metabolite dihydroartemisinin (n = 21), quinine (n = 21), and lumefantrine (n = 26) in pregnant Ugandan women were studied. Lumefantrine pharmacokinetics in a nonpregnant control group (n = 17) were also studied. Frequently sampled patient data were evaluated with noncompartmental analysis. No significant correlation was observed between estimated gestational age and artemether, dihydroartemisinin, lumefantrine, or quinine exposures. Artemether/dihydroartemisinin and quinine exposures were generally low in these pregnant women compared to values reported previously for nonpregnant patients. Median day 7 lumefantrine concentrations were 488 (range, 30.7 to 3,550) ng/ml in pregnant women compared to 720 (339 to 2,150) ng/ml in nonpregnant women (P = 0.128). There was no statistical difference in total lumefantrine exposure or maximum concentration. More studies with appropriate control groups in larger series are needed to characterize the degree to which pregnant women are underdosed with current antimalarial dosing regimens.
妊娠改变了许多用于治疗疟疾的药物的药代动力学特性,通常导致药物暴露水平降低。这增加了治疗失败、胎儿不良结局和耐药性发展的风险。研究了在乌干达孕妇中青蒿素及其主要代谢物双氢青蒿素(n = 21)、奎宁(n = 21)和咯萘啶(n = 26)的药代动力学特性。还研究了非妊娠对照组(n = 17)中咯萘啶的药代动力学。使用非房室分析评估频繁采样患者数据。估计的胎龄与青蒿素、双氢青蒿素、咯萘啶或奎宁的暴露量之间未观察到显著相关性。与以前报道的非妊娠患者相比,这些孕妇的青蒿素/双氢青蒿素和奎宁暴露通常较低。与非妊娠妇女的 720(339 至 2150)ng/ml 相比,孕妇的中位第 7 天咯萘啶浓度为 488(范围为 30.7 至 3550)ng/ml(P = 0.128)。总咯萘啶暴露量或最大浓度无统计学差异。需要在更大的系列中进行更多具有适当对照组的研究,以描述当前抗疟剂量方案对孕妇的剂量不足程度。