Comparative Pharmacology
Head-to-head clinical analysis: LACOSAMIDE versus VALRELEASE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LACOSAMIDE versus VALRELEASE.
LACOSAMIDE vs VALRELEASE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selectively enhances slow inactivation of voltage-gated sodium channels, stabilizing hyperexcitable neuronal membranes and inhibiting repetitive neuronal firing.
Increases GABAergic transmission by inhibiting GABA transaminase and blocking voltage-gated sodium channels.
Oral or IV: 50 mg twice daily initially; increase by 50 mg twice daily weekly to maintenance 100-200 mg twice daily. Maximum 200 mg twice daily.
500 mg orally twice daily, extended-release formulation. Maximum dose: 2000 mg/day.
None Documented
None Documented
Terminal elimination half-life is approximately 13 hours (range 12–16 hours) in adults. Steady state achieved after 3 days with BID dosing.
Clinical Note
moderateLacosamide + Sulfisoxazole
"The serum concentration of Sulfisoxazole can be increased when it is combined with Lacosamide."
Clinical Note
moderateLacosamide + Fluconazole
"The serum concentration of Fluconazole can be increased when it is combined with Lacosamide."
Clinical Note
moderateLacosamide + Ketoconazole
"The serum concentration of Ketoconazole can be increased when it is combined with Lacosamide."
Clinical Note
moderateLacosamide + Delavirdine
Terminal elimination half-life is 6-16 hours (mean 10.6 h) in adults; shorter at 4-12 h in children due to enhanced clearance; prolonged to 12-18 h in hepatic impairment or elderly. Clinical context: Once-daily dosing requires extended-release formulation (Valrelease) to maintain trough levels.
Renal: approximately 95% (40% unchanged, remainder as O-desmethyl metabolite). Fecal: <5%.
Renal: 70-80% as metabolites (valproic acid glucuronide, 3-oxo-valproate, 2-en-valproate) and <3% unchanged. Hepatic: 15-20% via bile into feces. Other: 1-3% exhaled as CO2.
Category C
Category C
Anticonvulsant
Anticonvulsant
"The serum concentration of Delavirdine can be increased when it is combined with Lacosamide."