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Darifenacin



Darifenacin
Systematic (IUPAC) name
2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
Identifiers
CAS number 133099-04-4
ATC code G04BD10
PubChem 444031
DrugBank APRD00903
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.

B3(AU) C(US)

Legal status

-only(US)

Routes Oral

Darifenacin (Enablex®, Novartis) is a medication used to treat urinary incontinence.

Additional recommended knowledge

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)


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Darifenacin". A list of authors is available in Wikipedia.
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