- Molecular NameGalantamine
- Synonym(-)-Galanthamine; Galanthamine; Galanthamine hydrobromide
- Weight287.359
- Drugbank_IDDB00674
- ACS_NO357-70-0
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)1.16
- pka8.2
- LogD (pH=7, predicted)-0.72
- Solubility (experiment)10 mg/ml (HBr salt)
- LogS (predicted, ACD/Labs)(ph=7)-0.87
- LogSw (predicted, AB/LogsW2.0)2.06
- Sw (mg/ml) (predicted, ACD/Labs)4.21
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds1
- TPSA41.93
- StatusFDA approved
- AdministrationN/A
- PharmacologyA chemical used for the treatment of mild to moderate Alzheimer’s disease and various memory impairments.
- Absorption_value100.0
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability100.0
- Protein binding18.0
- Volume of distribution (VD)2.64 L/kg (194.8 L)
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmGalantamine is metabolised in the liver by the cytochrome P450 isoenzymes, CYP2D6 and CYP3A4, and approx. 75% of the dose is metabolised. Metabolites include norgalantamine (active), N-oxide-galantamine, O-desmethylgalantamine (active), O-desmethylnorgalantamine (active), epigalantamine and galantaminone. No active metabolites have been detected in the unconjugated forms in plasma.
- Half life5.7 h
- ExcretionThe majority of the dose is excreted in urine; 18 to 22% as the unchanged drug during the 24 h period after dosing. A minor amount is excreted in faeces. The drug does not appear to accumulate after multiple dosing.
- Urinary Excretion20
- Clerance5.7 ml/min/kg
- ToxicitySignificant overdosing of galantamine can lead to signs and symptoms similar to those observed with overdosing of other cholinomimetics; generally involving the central nervous system, the parasympathetic nervous system and the neuromuscular junction. Symptoms include muscle weakness or fasciculations, severe nausea, vomiting, gastro-intestinal cramping, salivation, lacrimation, urination, defecation, sweating, bradycardia, hypotension, collapse and convulsions. Increasing muscle weakness along with tracheal hypersecretions and bronchospasm, may result in vital airway compromise. [Patient information leaflet, Janssen-Cilag Ltd.]
- LD50 (rat)LD50=75 mg/kg
- LD50 (mouse)LD50=10 (ip)