|Bioavailability||15 to 19% (dose-dependent)|
|Metabolism||Hepatic (CYP2D6- and CYP3A4-mediated)|
|Elimination half-life||13 to 19 hours|
|Excretion||Renal (60%) and biliary (40%)|
|Chemical and physical data|
|Molar mass||426.55 g/mol|
|3D model (JSmol)|
|(what is this?)|
Darifenacin (trade name Enablex in US and Canada, Emselex in Europe) is a medication used to treat urinary incontinence. It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and used to be marketed by Novartis. In 2010 the US rights were sold to Warner Chilcott for 400 million US$.
Mechanism of action
Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to urinate. It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.
It should not be used in people with urinary 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.
Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency in adults.
- Enablex product website, run by Warner Chilcott