Darifenacin
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| Clinical data | |
|---|---|
| Trade names | Enablex, Emselex |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605039 |
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| Routes of administration | By mouth |
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| Pharmacokineticdata | |
| Bioavailability | 15 to 19% (dose-dependent) |
| Protein binding | 98% |
| Metabolism | Liver(CYP2D6- andCYP3A4-mediated) |
| Eliminationhalf-life | 13 to 19 hours |
| Excretion | Kidney(60%) and biliary (40%) |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.118.382 |
| Chemical and physical data | |
| Formula | C28H30N2O2 |
| Molar mass | 426.560g·mol−1 |
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Darifenacin(trade nameEnablexin United States and Canada,Emselexin the European Union) is amedicationused to treaturinary incontinencedue to anoveractive 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 byNovartis.In 2010, the US rights were sold toWarner ChilcottforUS$400 million.
Adverse effects
[edit]Darifenacin should not be used in people withurinary 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.[4]
Medical uses
[edit]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 analpha blockerto help provide symptomatic benefit for overactive bladder and obstructive symptoms such as likely associated withbenign prostatic hypertrophy.[5]
Mechanism of action
[edit]Darifenacin works by blocking the M3muscarinic acetylcholine receptor,which is primarily responsible forbladdermuscle contractions.It thereby decreases the urgency tourinate.[6]It is not known whether this selectivity for the M3receptor translates into any clinical advantage when treating symptoms ofoveractive bladdersyndrome.[4]
References
[edit]- ^Croom KF, Keating GM (2004). "Darifenacin: in the treatment of overactive bladder".Drugs & Aging.21(13): 885–92, discussion 893–4.doi:10.2165/00002512-200421130-00005.PMID15493952.S2CID41549419.
- ^Parsons M, Robinson D, Cardozo L (July 2005)."Darifenacin in the treatment of overactive bladder".International Journal of Clinical Practice.59(7): 831–8.doi:10.1111/j.1368-5031.2005.00585.x.PMID15963212.S2CID39061659.
- ^Chughtai B, Levin R, De E (2008)."Choice of antimuscarinic agents for overactive bladder in the older patient: focus on darifenacin".Clinical Interventions in Aging.3(3): 503–9.doi:10.2147/cia.s3414.PMC2682382.PMID18982920.
- ^ab"Enablex- darifenacin tablet, extended release".DailyMed.24 September 2016.Retrieved22 October2020.
- ^American Urological Association (AUA) Guideline. Diagnosis and Treatment of Overactive Bladder in Adults: AUA/SUFA guideline 2012
- ^Chapple CR (November 2004). "Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder".Expert Opinion on Investigational Drugs.13(11): 1493–500.doi:10.1517/13543784.13.11.1493.PMID15500396.S2CID19259076.
External links
[edit]- "Darifenacin".Drug Information Portal.U.S. National Library of Medicine.
- "Darifenacin hydrobromide".Drug Information Portal.U.S. National Library of Medicine.
