Nøhr Martha Kampp, Frølund Sidsel, Holm René, Nielsen Carsten Uhd
Drug Transporters in ADME Group, Department of Pharmacy, Faculty of Health & Medical Sciences, University of Copenhagen, DK-2100 Copenhagen, Denmark.
Ther Deliv. 2014 Aug;5(8):927-42. doi: 10.4155/tde.14.55.
Drug transporters in various tissues, such as intestine, kidney, liver and brain, are recognized as important mediators of absorption, distribution, metabolism and excretion of drug substances. This review gives a current status on the transporter(s) mediating the absorption, distribution, metabolism and excretion properties of the anti-epileptic drug substance vigabatrin. For orally administered drugs, like vigabatrin, the absorption from the intestine is a prerequisite for the bioavailability. Therefore, transporter(s) involved in the intestinal absorption of vigabatrin in vitro and in vivo are discussed in detail. Special focus is on the contribution of the proton-coupled amino acid transporter 1 (PAT1) for intestinal vigabatrin absorption. Furthermore, the review gives an overview of the pharmacokinetic parameters of vigabatrin across different species and drug-food and drug-drug interactions involving vigabatrin.
肠道、肾脏、肝脏和大脑等各种组织中的药物转运体被认为是药物吸收、分布、代谢和排泄的重要介质。本综述介绍了介导抗癫痫药物氨己烯酸吸收、分布、代谢和排泄特性的转运体的现状。对于口服给药的药物，如氨己烯酸，肠道吸收是生物利用度的前提条件。因此，详细讨论了体外和体内参与氨己烯酸肠道吸收的转运体。特别关注质子偶联氨基酸转运体1（PAT1）对肠道氨己烯酸吸收的作用。此外，本综述还概述了氨己烯酸在不同物种中的药代动力学参数以及涉及氨己烯酸的药物-食物和药物-药物相互作用。
