Comparative Pharmacology
Head-to-head clinical analysis: FELBAMATE versus PARADIONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FELBAMATE versus PARADIONE.
FELBAMATE vs PARADIONE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Felbamate enhances GABAergic transmission and inhibits NMDA receptor activity, likely through interaction with the glycine recognition site.
Paradione (paramethadione) is an oxazolidinedione anticonvulsant that suppresses neuronal activity in the motor cortex by increasing the threshold for repetitive neuronal firing and reducing synaptic transmission. Its exact mechanism is unclear but involves modulation of T-type calcium channels and enhancement of GABAergic inhibition.
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.
100 mg orally three times daily; maximum 600 mg/day.
None Documented
None Documented
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
12-24 hours (terminal); prolonged in renal impairment
Renal: approximately 90% (40-50% unchanged, remainder as metabolites including p-hydroxyfelbamate, 2-hydroxyfelbamate, and felbamate monocarbamate); fecal < 5%
Renal: 70% unchanged; biliary/fecal: 25%; metabolic: 5%
Category C
Category C
Anticonvulsant
Anticonvulsant
"The metabolism of Clotrimazole can be decreased when combined with Felbamate."