Department of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, H-6720 Szeged, Hungary.
Int J Mol Sci. 2023 Aug 23;24(17):13089. doi: 10.3390/ijms241713089.
ABC transporters are ubiquitous in the human body and are responsible for the efflux of drugs. They are present in the placenta, intestine, liver and kidney, which are the major organs that can affect the pharmacokinetic and pharmacologic properties of drugs. P-gp and BCRP transporters are the best-characterized transporters in the ABC superfamily, and they have a pivotal role in the barrier tissues due to their efflux mechanism. Moreover, during pregnancy, drug efflux is even more important because of the developing fetus. Recent studies have shown that placental and intestinal ABC transporters have great importance in drug absorption and distribution. Placental and intestinal P-gp and BCRP show gestational-age-dependent expression changes, which determine the drug concentration both in the mother and the fetus during pregnancy. They may have an impact on the efficacy of antibiotic, antiviral, antihistamine, antiemetic and oral antidiabetic therapies. In this review, we would like to provide an overview of the pharmacokinetically relevant expression alterations of placental and intestinal ABC transporters during pregnancy.
ABC 转运蛋白在人体中广泛存在,负责药物的外排。它们存在于胎盘、肠道、肝脏和肾脏中,这些是主要的器官,可以影响药物的药代动力学和药效学特性。P-糖蛋白和 BCRP 转运蛋白是 ABC 超家族中研究得最好的转运蛋白,由于它们的外排机制,它们在屏障组织中起着关键作用。此外,在怀孕期间,由于胎儿的发育,药物外排更为重要。最近的研究表明,胎盘和肠道 ABC 转运蛋白在药物吸收和分布中具有重要意义。胎盘和肠道 P-糖蛋白和 BCRP 的表达变化随孕龄而变化,这决定了孕妇和胎儿在怀孕期间的药物浓度。它们可能对抗生素、抗病毒、抗组胺、止吐药和口服降糖药的疗效产生影响。在这篇综述中,我们将概述怀孕期间胎盘和肠道 ABC 转运蛋白的药代动力学相关表达变化。