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Distribution of lacosamide in the rat brain assessed by in vitro slice technique
Zsolt Ga´ ll,Szende Vancea 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.1
Lacosamide is a newer anticonvulsant and is theonly one that enhances the slow inactivation of voltagegated sodium channels. It is also claimed to have diseasemodifyingpotential, but its pharmacokinetic propertieshave been much less discussed in the literature. In rats,lacosamide shows restricted distribution to tissues, and thebrain-to-plasma partition coefficient (Kp) is only 0.553. Inthis study, the brain disposition of lacosamide was evaluatedin rat brains, and its neuropharmacokinetic parameters(i.e., protein binding and intracellular accumulation) wereassessed using in vitro methods. Brain slice experimentsand brain homogenate binding studies were performed forseveral drugs acting on the central nervous system, anddrugs were assayed by using a liquid chromatography-massspectrometry system. By applying a combined approach, itwas found that (1) the unbound volume of distribution inthe brain for lacosamide (Vu,brain = 1.37) was lower thanthat of other classical anticonvulsants; (2) the unboundfraction of lacosamide in the brain (0.899) was slightlylower than its unbound fraction in plasma (0.96); (3) theunbound intracellular-to-extracellular concentration ratioof lacosamide was 1.233, meaning that lacosamide wasaccumulated in the intracellular space because of itsphysicochemical properties and zwitterionic structure; and(4) the unbound brain-to-plasma concentration ratio oflacosamide was lower than the total brain-to-plasma concentrationratio (Kp,uu,brain = 0.42 vs. Kp = 0.553). Inconclusion, the limited brain distribution of lacosamide isnot related to its nonspecific protein-binding capacity;rather, an active transport mechanism across the blood–brain barrier may be involved, which reduces the anticonvulsantand/or antiepileptogenic actions of this drug.
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