Darifenacin: Difference between revisions

{{Short description|Medication for urinary incontinence}}

| Watchedfields = changed

| verifiedrevid = 460773728

| alt =

| alt2 =

| tradename = Enablex, Emselex

| Drugs.com = {{drugs.com|monograph|darifenacin-hydrobromide}}

| ATC_prefix = G04

| ATC_suffix = BD10

| ATC_supplemental =

| legal_AU = S4

| legal_EU = Rx-only

| routes_of_administration = [[Oral administration|By mouth]]

| metabolism = [[Liver]] ([[CYP2D6]]- and [[CYP3A4]]-mediated)

| excretion = [[Kidney]] (60%) and biliary (40%)

| index2_label = as salt

| IUPHAR_ligand = 321

| KEGG = D03654

| KEGG2_Ref = {{keggcite|changed|kegg}}

| KEGG2 = D01699

| IUPAC_name = (''S'')-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide

| C=28 | H=30 | N=2 | O=2

'''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]].<ref name="Croom_2004">{{cite journal | vauthors = Croom KF, Keating GM | title = Darifenacin: in the treatment of overactive bladder | journal = Drugs & Aging | volume = 21 | issue = 13 | pages = 885–92; discussion 893–4 | date = 2004 | pmid = 15493952 | doi = 10.2165/00002512-200421130-00005 | s2cid = 41549419 }}</ref><ref name="Parsons_2005">{{cite journal | vauthors = Parsons M, Robinson D, Cardozo L | title = Darifenacin in the treatment of overactive bladder | journal = International Journal of Clinical Practice | volume = 59 | issue = 7 | pages = 831–8 | date = July 2005 | pmid = 15963212 | doi = 10.1111/j.1368-5031.2005.00585.x | s2cid = 39061659 | doi-access = free }}</ref><ref name="Chughtai_2008">{{cite journal | vauthors = Chughtai B, Levin R, De E | title = Choice of antimuscarinic agents for overactive bladder in the older patient: focus on darifenacin | journal = Clinical Interventions in Aging | volume = 3 | issue = 3 | pages = 503–9 | date = 2008 | pmid = 18982920 | pmc = 2682382 | doi = 10.2147/cia.s3414 | doi-access = free }}</ref> 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 [[urinary 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.<ref name="Enablex FDA label">{{cite web | title=Enablex- darifenacin tablet, extended release | website=DailyMed | date=24 September 2016 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a712f252-16d9-47df-b2bf-6794228f3a88 | access-date=22 October 2020}}</ref>

== 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 [[alpha blocker]] to help provide symptomatic benefit for overactive bladder and obstructive symptoms such as likely associated with [[benign prostatic hypertrophy]]. <ref>American Urological Association (AUA) Guideline. Diagnosis and Treatment of Overactive Bladder in Adults: AUA/SUFA guideline 2012</ref>

== Mechanism of action ==

Darifenacin works by blocking the M₃ [[muscarinic acetylcholine receptor]], which is primarily responsible for [[urinary bladder|bladder]] [[muscle contraction]]s. It thereby decreases the urgency to [[urinate]].<ref name="Chapple_2004">{{cite journal | vauthors = Chapple CR | title = Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder | journal = Expert Opinion on Investigational Drugs | volume = 13 | issue = 11 | pages = 1493–500 | date = November 2004 | pmid = 15500396 | doi = 10.1517/13543784.13.11.1493 | s2cid = 19259076 }}</ref> It is not known whether this selectivity for the M₃ receptor translates into any clinical advantage when treating symptoms of [[overactive bladder]] syndrome.<ref name="Enablex FDA label" />

* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/darifenacin | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Darifenacin }}

* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/darifenacin%20hydrobromide | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Darifenacin hydrobromide }}

{{Muscarinic acetylcholine receptor modulators}}

{{Portal bar | Medicine}}

[[Category:5-Benzofuranethanamines]]

[[Category:Carboxamides]]

[[Category:CYP2D6 inhibitors]]

[[Category:Drugs developed by AbbVie]]

[[Category:Drugs developed by Novartis]]

[[Category:Benzhydryl compounds]]