- Molecular NameFelbamate
- SynonymNA
- Weight238.243
- Drugbank_IDDB00949
- ACS_NO25451-15-4
- Show 2D model
- LogP (experiment)0.76
- LogP (predicted, AB/LogP v2.0)0.92
- pkaN/A
- LogD (pH=7, predicted)0.92
- Solubility (experiment)Slightly soluble in water
- LogS (predicted, ACD/Labs)(ph=7)-1.95
- LogSw (predicted, AB/LogsW2.0)2.74
- Sw (mg/ml) (predicted, ACD/Labs)2.67
- No.of HBond Donors4
- No.of HBond Acceptors6
- No.of Rotatable Bonds7
- TPSA104.64
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn 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. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drugs usage to severe refractory epilepsy.
- Absorption_value90.0
- Absorption (description)Felbamate is well absorbed (approx. 90%) after oral administration
- Caco_2N/A
- Bioavailability80.0
- Protein binding28.0
- Volume of distribution (VD)0.76 to 0.81 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmPartly metabolised in the liver by hydroxylation and conjugation, to produce active and inactive metabolites.
- Half lifeElimination half-life, 14~23 h
- ExcretionThe drug is excreted in urine unchanged (40 to 50%), as unidentified metabolites and conjugates (40%) and known active metabolites (15%), including 2-hydroxyfelbamate, p-hydroxyfelbamate, a monocarbamate derivative, and 3-carbamoyloxy-2-phenyl propionic acid. <5% of the dose is excreted in faeces.
- Urinary ExcretionN/A
- Clerance25 ml/min/kg (single dose), 41 ml/min/kg (repeated dose).
- ToxicityAcute liver failure has been reported with 4 fatalities out of 8 cases [Schering-Plough manufacturers report, 1994] and aplastic anaemia with 2 out of 10 cases resulting in death [US Food and Drug Administration report, 1994].
- LD50 (rat)LD50=5000 mg/kg
- LD50 (mouse)N/A