Clinical Information

Lacosamide is approved for adjunctive therapy to treat partial-onset seizures in epileptic patients aged 17 years and older. In clinical trials, the most common side effects were dizziness, headache, nausea, and double vision. Lacosamide is completely absorbed after oral administration with negligible first-pass metabolism. Peak serum concentrations occur 1 to 4 hours after oral dosing, and the elimination half-life is approximately 13 hours. Steady-state serum concentrations are achieved after 3 days of twice daily repeated administration. About 40% of the administered dose is eliminated by the renal system unchanged, and 30% is metabolized by hepatic isoenzymes (CYP2C9, CYP2C19, and CYP3A4) to the O-desmethyl inactive metabolite. The relationship between lacosamide serum concentrations and its efficacy or adverse effects is not well established. However, central nervous system toxicity has been associated with higher drug concentrations in serum.