Darifenacin

Source: Wikipedia, the free encyclopedia.
Darifenacin
Clinical data
Trade namesEnablex, Emselex
AHFS/Drugs.comMonograph
MedlinePlusa605039
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic data
Bioavailability15 to 19% (dose-dependent)
Protein binding98%
MetabolismLiver (CYP2D6- and CYP3A4-mediated)
Elimination half-life13 to 19 hours
ExcretionKidney (60%) and biliary (40%)
Identifiers
  • (S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
JSmol)
  • O=C(N)C(c1ccccc1)(c2ccccc2)[C@H]3CN(CC3)CCc5cc4c(OCC4)cc5
  • 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 checkY
  • Key:HXGBXQDTNZMWGS-RUZDIDTESA-N checkY
 ☒NcheckY (what is this?)  (verify)

Darifenacin (trade name Enablex in United States and Canada, Emselex in the European Union) is a medication used to treat urinary incontinence due to an overactive bladder.[1][2][3] It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and used to be marketed by Novartis. In 2010, the US rights were sold to Warner Chilcott for US$400 million.

Adverse effects

Darifenacin should not be used in people with

Heat prostration (due to decreased sweating) can occur when anticholinergics such as darifenacin are used in a hot environment.[4]

Medical uses

Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency in adults. It may also be recommended with an

benign prostatic hypertrophy. [5]

Mechanism of action

Darifenacin works by blocking the M3

urinate.[6] It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.[4]

References

  1. S2CID 41549419
    .
  2. S2CID 39061659
    .
  3. PMID 18982920
    .
  4. ^ a b "Enablex- darifenacin tablet, extended release". DailyMed. 24 September 2016. Retrieved 22 October 2020.
  5. ^ American Urological Association (AUA) Guideline. Diagnosis and Treatment of Overactive Bladder in Adults: AUA/SUFA guideline 2012
  6. S2CID 19259076
    .

External links
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