Darifenacin
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| 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  |
| ATC code | G04BD10 |
| PubChem | CID 444031 |
| DrugBank | APRD00903 |
| ChemSpider | 392054 |
| UNII | APG9819VLM |
| KEGG | D01699  |
| ChEBI | CHEBI:391960 |
| ChEMBL | CHEMBL1346 |
| Chemical data | |
| Formula | C28H30N2O2 |
| Mol. mass | 426.55 g/mol |
| SMILES | eMolecules & PubChem |
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Darifenacin (trade name Enablex in US and Canada, Emselex in Europe) is a medication used to treat urinary incontinence. It used to be marketed by Novartis; however in 2010 US rights for were sold to Warner Chilcott for 400 million US$.
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[edit] 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 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]
[edit] Clinical uses
Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
[edit] References
[edit] External links
- Enablex product website, run by Warner Chilcott
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