- Molecular NameSolifenacin
- Synonymsolifenacin succinate
- Weight362.473
- Drugbank_IDDB01591
- ACS_NO242478-38-2
- Show 2D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)4.24
- pkaN/A
- LogD (pH=7, predicted)2.04
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.29
- LogSw (predicted, AB/LogsW2.0)0.04
- Sw (mg/ml) (predicted, ACD/Labs)0.03
- No.of HBond Donors0
- No.of HBond Acceptors4
- No.of Rotatable Bonds3
- TPSA32.78
- StatusFDA approved
- AdministrationN/A
- PharmacologyA urinary antispasmodic of the anticholinergic class. It is used in the treatment of overactive bladder with or without urge incontinence.
- Absorption_valueN/A
- Absorption (description)The absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding98.0
- Volume of distribution (VD)8.6 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmSolifenacin is extensively metabolized in the liver. The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist. The primary metabolic routes of solifenacin are through N-oxidation of the quinuclidin ring and 4R-hydroxylation of tetrahydroisoquinoline ring. One pharmacologically active metabolite (4R-hydroxy solifenacin), occurring at low concentrations and unlikely to contribute significantly to clinical activity, and three pharmacologically inactive metabolites (N-glucuronide and the N-oxide and 4R-hydroxy-N-oxide of solifenacin) have been found in human plasma after oral dosing.
- Half life45~68 h
- ExcretionRenal (69.2%) and fecal (22.5%)
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityOverdosage with solifenacin can potentially result in severe anticholinergic effects and should be treated accordingly. The highest solifenacin dose given to human volunteers was a single 100 mg dose. Intolerable anticholinergic side effects (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors and dry skin) occurred on day 3 in normal volunteers taking 50 mg daily (5 times the maximum recommended therapeutic dose).
- LD50 (rat)N/A
- LD50 (mouse)N/A