- Molecular NameDonepezil
- SynonymNA
- Weight379.5
- Drugbank_IDDB00843
- ACS_NO120014-06-4
- Show 2D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)4.04
- pka8.9
- LogD (pH=7, predicted)2.35
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-3.12
- LogSw (predicted, AB/LogsW2.0)0.06
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors0
- No.of HBond Acceptors4
- No.of Rotatable Bonds6
- TPSA38.77
- StatusFDA approved
- AdministrationN/A
- PharmacologyA centrally acting reversible acetylcholinesterase inhibitor.[1] Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.
- Absorption_valueN/A
- Absorption (description)Donepezil is well absorbed from the gastro-intestinal tract after oral administration
- Caco_2N/A
- Bioavailability20.0
- Protein binding92.6
- Volume of distribution (VD)13.6~14.8 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolized by CYP2D6, CYP3A4, UGT. O-Dealkylation followed by hydroxylation and partial subsequent glucuronidation or hydrolysis produces four major metabolites which are known to be active, and several minor metabolites.
- Half lifeElimination, approx. 50 to 60 h (single dose); 75 h (steady state); 104 h (elderly).
- ExcretionOver 10 days, 57% of a single dose is recovered as metabolites in urine and 15% in faeces; 17% of the drug remains unchanged and is excreted in urine; 28% is unrecovered, possibly owing to accumulation.
- Urinary ExcretionN/A
- Clerance0.12 L/h/kg (Body clearance)
- ToxicitySide effects include galactorrhea, gynecomastia, or menstrual irregularities.
- LD50 (rat)N/A
- LD50 (mouse)N/A