Lacosamide Pharmacokinetics

When administered orally in advantageous individuals, lacosamide is rapidly captivated from the gastrointestinal tract. Little of the biologic is absent via the aboriginal canyon effect, and appropriately has an articulate bioavailability of about 100%.In adults, lacosamide demonstrates a low claret protein bounden of <15, which reduces the abeyant for alternation with added drugs. Lacosamide is at its accomplished absorption in claret claret about 1 to 4 hours afterwards articulate administration. Lacosamide has a bisected activity of about 12–16 hours, which charcoal banausic if the patients is aswell demography agitator inducers. Consequently, the biologic is administered alert per day at 12-hour intervals. Lacosamide is excreted renally, with 95% of the biologic alone in the urine.40% of the admixture charcoal banausic from its aboriginal structure, while the blow of the abolishment artefact consists of metabolites of lacosamide. Just 0.5% of the biologic is alone in the feces. The above metabolic alleyway of lacosamide is CYP2C9, CY2C19, and CYP3A4-mediated demethylation.

The dose-response ambit for lacosamide is beeline and proportional for articulate doses of up to 800 mg and intravenous doses of up to 300 mg. Lacosamide has low abeyant for drug-drug interactions, and no pharmacokinetic interactions accept been begin to action with added (AEDs) that act on sodium channels. A abstraction on the bounden of lacosamide to CRMP-2 in Xenopus oocytes showed both aggressive and specific binding. Lacosamide has a Kd amount just beneath 5μM and a Bmax of about 200 pM/mg.The aggregate of administration (Vd) of lacosamide in claret is 0.6 L/kg, which is abutting to the absolute aggregate of water. Lacosamide is ampiphilic and is appropriately hydrophilic while aswell lipophilic abundant to cantankerous the blood-brain barrier.