Felbamate

CAS No:
25451-15-4 Category:
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Product Details:

  • CAS No: 25451-15-4
  • AHFC code:
  • Synonyms:
  • ATC Code: N03AX10
  • Chemical Formula: C23H36N2O2
  • Molecular Weight: 238.2399
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00949 (APRD00505)
  • SMILES: NC(=O)OCC(COC(N)=O)C1=CC=CC=C1
  • InChl: WKGXYQFOCVYPAC-UHFFFAOYSA-N
  • PubChem: 3331
  • IUPAC: 3-(carbamoyloxy)-2-phenylpropyl carbamate

Additional Details

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.
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.
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.
Metabolism:
Hepatic
Toxicity:
LD50=5000 mg/kg (Orally in rats)
General Reference:
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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