| Clinical data | |
|---|---|
| Trade names | Enablex, Emselex |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605039 |
| Pregnancy category |
|
| Routes of administration | By mouth |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 15 to 19% (dose-dependent) |
| Protein binding | 98% |
| Metabolism | Liver (CYP2D6- andCYP3A4-mediated) |
| Eliminationhalf-life | 13 to 19 hours |
| Excretion | Kidney (60%) and biliary (40%) |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| IUPHAR/BPS | |
| DrugBank |
|
| ChemSpider |
|
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.118.382 |
| Chemical and physical data | |
| Formula | C28H30N2O2 |
| Molar mass | 426.560 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| | |
Darifenacin (trade nameEnablex in United States and Canada,Emselex in the European Union) is amedication used to treaturinary incontinence due to anoveractive bladder.[1][2][3] It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and used to be marketed byNovartis. In 2010, the US rights were sold toWarner Chilcott forUS$400 million.
Darifenacin should not be used in people withurinary retention.Anticholinergic agents, such as darifenacin, may also produce constipation and blurred vision.Heat prostration (due to decreased sweating) can occur when anticholinergics such as darifenacin are used in a hot environment.[4]
Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency in adults. It may also be recommended with analpha blocker to help provide symptomatic benefit for overactive bladder and obstructive symptoms such as those likely associated withbenign prostatic hyperplasia.[5]
Darifenacin works by blocking the M3muscarinic acetylcholine receptor, which is primarily responsible forbladdermuscle contractions. It thereby decreases the urgency tourinate.[6] It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms ofoveractive bladder syndrome.[4]