化合物信息

Drug Groups

approved

Description

Felbamate is an anticonvulsant drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. It has a weak inhibitory effect on GABA receptor binding sites.

Indication

For use only in those patients who respond inadequately to alternative treatments and whose epilepsy is so severe that a substantial risk of aplastic anemia and/or liver failure is deemed acceptable in light of the benefits conferred by its use.

Pharmacology

Felbamate is an antiepileptic indicated as monotherapy or as an adjunct to other anticonvulsants for the treatment of partial seizures resulting from epilepsy. Receptor-binding studies in vitro indicate that felbamate has weak inhibitory effects on GABA-receptor binding, benzodiazepine receptor binding, and is devoid of activity at the MK-801 receptor binding site of the NMDA receptor-ionophore complex. However, felbamate does interact as an antagonist at the strychnine-insensitive glycine recognition site of the NMDA receptor-ionophore complex.

Toxicity

LD₅₀=5000 mg/kg (Orally in rats)

Affected Organisms

Biotransformation

Hepatic

Absorption

>90%

Half Life

20-23 hours

Protein Binding

20-36%

Distribution

* 756±82 mL/kg

Clearance

* 26 +/- 3 mL/hr/kg [single 1200 mg dose]
* 30 +/- 8 mL/hr/kg [multiple daily doses of 3600 mg]

References

External Links