Darifenacin
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| Systematic (IUPAC) name | |
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(S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
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| Clinical data | |
| Trade names | Enablex |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a605039 |
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| Routes of administration |
Oral |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 15 to 19% (dose-dependent) |
| Protein binding | 98% |
| Metabolism | Hepatic (CYP2D6- and CYP3A4-mediated) |
| Biological half-life | 13 to 19 hours |
| Excretion | Renal (60%) and biliary (40%) |
| Identifiers | |
| CAS Number | 133099-04-4  |
| ATC code | G04BD10 |
| PubChem | CID 444031 |
| IUPHAR/BPS | 321 |
| DrugBank | DB00496 |
| ChemSpider | 392054 |
| UNII | APG9819VLM |
| KEGG | D01699  |
| ChEBI | CHEBI:391960 |
| ChEMBL | CHEMBL1346 |
| Chemical data | |
| Formula | C28H30N2O2 |
| Molar mass | 426.55 g/mol |
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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 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]
- Enablex product website, run by Warner Chilcott
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