Felbamate

Felbamate Uses, Dosage, Side Effects, Food Interaction and all others data.

Felbamate is an anticonvulsant drug used in the treatment of epilepsy. In particular, in the adult patient population, it can be employed to treat partial seizures (with and without generalization). Alternatively, it is used to treat partial and generalized seizures associated with Lennox-Gastaut syndrome in children. It has a weak inhibitory effect on GABA receptor binding sites.

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.

Trade Name Felbamate
Availability Prescription only
Generic Felbamate
Felbamate Other Names Felbamate, Felbamato, Felbamatum
Related Drugs gabapentin, clonazepam, lamotrigine, pregabalin, Lyrica, topiramate, Topamax, cannabidiol, clobazam, Epidiolex
Weight 600mg/5ml, 400mg, 600mg
Type Oral suspension, oral tablet
Formula C11H14N2O4
Weight Average: 238.2399
Monoisotopic: 238.095356946
Protein binding

20-36%

Groups Approved
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Felbamate
Felbamate

Uses

Felbamate is an anticonvulsant used to treat severe epilepsy.

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.

Felbamate is also used to associated treatment for these conditions: Refractory Partial Seizures, Refractory Lennox-Gastaut syndrome, Refractory seizure disorders

How Felbamate works

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.

Toxicity

LD50=5000 mg/kg (Orally in rats)

Food Interaction

  • Avoid alcohol.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Volume of Distribution

  • 756±82 mL/kg

Elimination Route

>90%

Half Life

20-23 hours

Clearance

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

Innovators Monograph

You find simplified version here Felbamate

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http://classyfire.wishartlab.com/tax_nodes/C0000278
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0001831
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4995
http://www.hmdb.ca/metabolites/HMDB0015084
http://www.genome.jp/dbget-bin/www_bget?drug:D00536
http://www.genome.jp/dbget-bin/www_bget?cpd:C07501
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3331
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506375
https://www.chemspider.com/Chemical-Structure.3214.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50088430
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=24812
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=4995
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1094
https://zinc.docking.org/substances/ZINC000001530803
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000093
http://www.pharmgkb.org/drug/PA449590
http://www.rxlist.com/cgi/generic3/felbamate.htm
https://www.drugs.com/cdi/felbamate.html
https://en.wikipedia.org/wiki/Felbamate
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