Darifenacin

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Darifenacin
Darifenacin.svg
Darifenacin-hydrobromide-from-xtal-2009-CM-3D-balls.png
Systematic (IUPAC) name
(S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
Clinical data
Trade names Enablex
AHFS/Drugs.com monograph
MedlinePlus a605039
Pregnancy cat. B3 (AU) C (US)
Legal status POM (UK) -only (US)
Routes Oral
Pharmacokinetic data
Bioavailability 15 to 19% (dose-dependent)
Protein binding 98%
Metabolism Hepatic (CYP2D6- and CYP3A4-mediated)
Half-life 13 to 19 hours
Excretion Renal (60%) and biliary (40%)
Identifiers
CAS number 133099-04-4 YesY
ATC code G04BD10
PubChem CID 444031
DrugBank DB00496
ChemSpider 392054 YesY
UNII APG9819VLM YesY
KEGG D01699 N
ChEBI CHEBI:391960 YesY
ChEMBL CHEMBL1346 YesY
Chemical data
Formula C28H30N2O2 
Mol. mass 426.55 g/mol
 N (what is this?)  (verify)

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 previously was marketed by Novartis; however in 2010 US rights for were sold to Warner Chilcott for 400 million US$.

Mechanism of action[edit]

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 Enablex, may also produce constipation and blurred vision. Heat prostration (due to decreased sweating) can occur when anticholinergics such as Enablex are used in a hot environment.[1]

Clinical uses[edit]

Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency in adults.

References[edit]

External links[edit]