Darifenacin
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| Darifenacin
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| Systematic (IUPAC) name | |
| 2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide | |
| Identifiers | |
| CAS number | |
| ATC code | G04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C28H30N2O2 |
| Mol. mass | 426.55 g/mol |
| 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%) |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral |
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Darifenacin (Enablex®, Novartis) is a medication used to treat urinary incontinence.
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 should not be used in people with urinary retention.
It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.(1)
Administration
Darifenacin is administered as a once-daily extended-release oral tablet.
References
(1) SPC for emselex-revised on 29/11/06 (available at www.medicines.org.uk)
de:Darifenacin
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