Product Name

Felbamate

CAS Number

25451-15-4

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Product Name:
Felbamate
CAS Number:
25451-15-4
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.
Mode of Action:

The mechanism by which felbamate exerts its anticonvulsant activity is unknown, but in animal test systems designed to detect anticonvulsant activity, felbamate has properties in common with other marketed anticonvulsants. In vitro receptor binding studies suggest that felbamate may be an antagonist at the strychnine-insensitive glycine-recognition site of the N-methyl-D-aspartate (NMDA) receptor-ionophore complex. Antagonism of the NMDA receptor glycine binding site may block the effects of the excitatory amino acids and suppress seizure activity. Animal studies indicate that felbamate may increase the seizure threshold and may decrease seizure spread. It is also indicated that felbamate has weak inhibitory effects on GABA-receptor binding, benzodiazepine receptor binding.

Pharmacodynamics:

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.

Metabolism:

Hepatic

Toxicity:

LD50=5000 mg/kg (Orally in rats)

IUPAC:
3-(carbamoyloxy)-2-phenylpropyl carbamate
ATC:
N03AX10
PubChem:
3331
DrugBank:
DB00949 (APRD00505)
Formula:
C23H36N2O2
Molecular Mass:
238.2399
SMILES:
NC(=O)OCC(COC(N)=O)C1=CC=CC=C1
InChi:
WKGXYQFOCVYPAC-UHFFFAOYSA-N
General Reference:
General Reference:

  1. Leppik IE, Dreifuss FE, Pledger GW, Graves NM, Santilli N, Drury I, Tsay JY, Jacobs MP, Bertram E, Cereghino JJ, et al.: Felbamate for partial seizures: results of a controlled clinical trial. Neurology. 1991 Nov;41(11):1785-9. Pubmed

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