Darifenacin

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Darifenacin
Darifenacin.svg
Darifenacin-hydrobromide-from-xtal-2009-CM-3D-balls.png
Clinical data
Trade namesEnablex
AHFS/Drugs.comMonograph
MedlinePlusa605039
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability15 to 19% (dose-dependent)
Protein binding98%
MetabolismHepatic (CYP2D6- and CYP3A4-mediated)
Elimination half-life13 to 19 hours
ExcretionRenal (60%) and biliary (40%)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.118.382 Edit this at Wikidata
Chemical and physical data
FormulaC28H30N2O2
Molar mass426.55 g/mol
3D model (JSmol)
 ‹See TfM›☒N☑Y (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 used to be marketed by Novartis. In 2010 the US rights 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 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.[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]