Comparative Pharmacology
Head-to-head clinical analysis: DEPAKOTE ER versus FELBAMATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DEPAKOTE ER versus FELBAMATE.
DEPAKOTE ER vs FELBAMATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Increases GABAergic activity by inhibiting GABA transaminase and succinate semialdehyde dehydrogenase; blocks voltage-gated sodium and T-type calcium channels; reduces glutamate release.
Felbamate enhances GABAergic transmission and inhibits NMDA receptor activity, likely through interaction with the glycine recognition site.
500-1000 mg orally once daily; usual maximum dose 60 mg/kg/day.
1200-3600 mg/day orally in 3-4 divided doses; initiate at 1200 mg/day and titrate by 600-1200 mg/day every 2 weeks.
None Documented
None Documented
Terminal elimination half-life is approximately 20 hours (range 10-60 hours); clinical context: extended-release formulation allows once-daily dosing, steady-state achieved in 4-5 days
Clinical Note
moderateFelbamate + Estrone sulfate
"The serum concentration of Estrone sulfate can be decreased when it is combined with Felbamate."
Clinical Note
moderateFelbamate + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Felbamate."
Clinical Note
moderateFelbamate + Fluconazole
"The metabolism of Fluconazole can be decreased when combined with Felbamate."
Clinical Note
moderateFelbamate + Clotrimazole
Terminal elimination half-life: 13-23 hours in adults (mean ~20 hours); may be prolonged to 30-40 hours in patients with hepatic impairment or those on enzyme inhibitors; clinical context: requires twice-daily dosing; steady-state reached in 4-5 days
Primarily renal (30-50% as glucuronide conjugates, <3% as unchanged drug); minor fecal (10-20%)
Renal: approximately 90% (40-50% unchanged, remainder as metabolites including p-hydroxyfelbamate, 2-hydroxyfelbamate, and felbamate monocarbamate); fecal < 5%
Category C
Category C
Anticonvulsant
Anticonvulsant
"The metabolism of Clotrimazole can be decreased when combined with Felbamate."