Darifenacin

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 Y
ATC code	G04BD10
PubChem	CID 444031
DrugBank	DB00496
ChemSpider	392054 Y
UNII	APG9819VLM Y
KEGG	D01699 N
ChEBI	CHEBI:391960 Y
ChEMBL	CHEMBL1346 Y
Chemical data
Formula	C28H30N2O2
Mol. mass	426.55 g/mol
SMILES O=C(N)C(c1ccccc1)(c2ccccc2)[C@H]3CN(CC3)CCc5cc4c(OCC4)cc5
InChI InChI=1S/C28H30N2O2/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26/h1-12,19,25H,13-18,20H2,(H2,29,31)/t25-/m1/s1 Y Key:HXGBXQDTNZMWGS-RUZDIDTESA-N Y
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]

• Enablex product website, run by Warner Chilcott

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