Felbamatum
Felbamatum Uses, Dosage, Side Effects, Food Interaction and all others data.
Felbamatum 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.
Felbamatum 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 | Felbamatum |
Availability | Prescription only |
Generic | Felbamate |
Felbamate Other Names | Felbamate, Felbamato, Felbamatum |
Related Drugs | gabapentin, clonazepam, lamotrigine, pregabalin, Lyrica, topiramate, Topamax, cannabidiol, clobazam, Epidiolex |
Type | |
Formula | C11H14N2O4 |
Weight | Average: 238.2399 Monoisotopic: 238.095356946 |
Protein binding | 20-36% |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Felbamatum 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.
Felbamatum is also used to associated treatment for these conditions: Refractory Partial Seizures, Refractory Lennox-Gastaut syndrome, Refractory seizure disorders
How Felbamatum 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.
Felbamatum Drug Interaction
Moderate: diazepam, diazepam, cannabidiol, cannabidiol, levetiracetam, levetiracetam, clobazam, clobazam, cholecalciferol, cholecalciferolUnknown: levocarnitine, levocarnitine, polyethylene glycol 3350, polyethylene glycol 3350, ibuprofen, ibuprofen, acetaminophen, acetaminophen, lacosamide, lacosamide
Felbamatum Disease Interaction
Major: aplastic anemia, liver disease, renal dysfunctionModerate: suicidal tendency
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
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