title: Pharmacokinetic aspects of the anti-epileptic drug substance vigabatrin: focus on transporter interactions.
abstract: 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.
authors.affiliation: Drug Transporters in ADME Group, Department of Pharmacy, Faculty of Health & Medical Sciences, University of Copenhagen, DK-2100 Copenhagen, Denmark.
authors.forename: Martha Kampp
authors.initials: MK
authors.lastname: Nøhr
authors.forename: Sidsel
authors.initials: S
authors.lastname: Frølund
authors.forename: René
authors.initials: R
authors.lastname: Holm
authors.forename: Carsten Uhd
authors.initials: CU
authors.lastname: Nielsen
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000493:pharmacokinetics*; D004347:Drug Interactions; D018565:Food-Drug Interactions; D006801:Humans; D007408:Intestinal Absorption; D026901:Membrane Transport Proteins / Q000502:physiology*; D020888:Vigabatrin / Q000493:pharmacokinetics*
chemical_list: D000927:Anticonvulsants; D026901:Membrane Transport Proteins; D020888:Vigabatrin