Medication for urinary incontinence
Routes of administration | By mouth |
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ATC code | |
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Legal status |
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Legal status | - AU: S4 (Prescription only)
- UK: POM (Prescription only)
- US: ℞-only
- EU: Rx-only
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Pharmacokinetic data |
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Bioavailability | 15 to 19% (dose-dependent) |
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Protein binding | 98% |
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Metabolism | Liver (CYP2D6- and CYP3A4-mediated) |
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Elimination half-life | 13 to 19 hours |
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Excretion | Kidney (60%) and biliary (40%) |
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Identifiers |
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CAS Number | - 133099-04-4 Y
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PubChem CID | |
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IUPHAR/BPS | |
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DrugBank | - DB00496 Y
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ChemSpider | - 392054 Y
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UNII | |
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KEGG | - D03654 N
- as salt: D01699 N
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ChEBI | - CHEBI:391960 Y
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ChEMBL | - ChEMBL1346 Y
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CompTox Dashboard (EPA) | - DTXSID2048290
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ECHA InfoCard | 100.118.382 |
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Chemical and physical data |
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Formula | C28H30N2O2 |
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Molar mass | 426.560 g·mol−1 |
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3D model (JSmol) | |
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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 YKey:HXGBXQDTNZMWGS-RUZDIDTESA-N Y |
NY (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 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.[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 alpha blocker to help provide symptomatic benefit for overactive bladder and obstructive symptoms such as likely associated with benign prostatic hypertrophy. [5]
Mechanism of action
Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to 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
- ^ 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. PMID 15493952. S2CID 41549419.
- ^ 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. PMID 15963212. S2CID 39061659.
- ^ 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. PMC 2682382. PMID 18982920.
- ^ a b "Enablex- darifenacin tablet, extended release". DailyMed. 24 September 2016. Retrieved 22 October 2020.
- ^ 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. PMID 15500396. S2CID 19259076.
External links
- "Darifenacin". Drug Information Portal. U.S. National Library of Medicine.
- "Darifenacin hydrobromide". Drug Information Portal. U.S. National Library of Medicine.
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mAChRsTooltip Muscarinic acetylcholine receptors | Agonists | |
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Antagonists | - 3-Quinuclidinyl benzilate
- 4-DAMP
- Aclidinium bromide (+formoterol)
- Abediterol
- AF-DX 250
- AF-DX 384
- Ambutonium bromide
- Anisodamine
- Anisodine
- Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, dimetindene, diphenhydramine, doxylamine, meclizine, mequitazine, perlapine, phenindamine, pheniramine, phenyltoloxamine, promethazine, propiomazine, triprolidine)
- AQ-RA 741
- Atropine
- Atropine methonitrate
- Atypical antipsychotics (e.g., clozapine, fluperlapine, olanzapine (+fluoxetine), rilapine, quetiapine, tenilapine, zotepine)
- Benactyzine
- Benzatropine (benztropine)
- Benzilone
- Benzilylcholine mustard
- Benzydamine
- BIBN 99
- Biperiden
- Bornaprine
- Camylofin
- CAR-226,086
- CAR-301,060
- CAR-302,196
- CAR-302,282
- CAR-302,368
- CAR-302,537
- CAR-302,668
- Caramiphen
- Cimetropium bromide
- Clidinium bromide
- Cloperastine
- CS-27349
- Cyclobenzaprine
- Cyclopentolate
- Darifenacin
- DAU-5884
- Desfesoterodine
- Dexetimide
- DIBD
- Dicycloverine (dicyclomine)
- Dihexyverine
- Difemerine
- Diphemanil metilsulfate
- Ditran
- Drofenine
- EA-3167
- EA-3443
- EA-3580
- EA-3834
- Emepronium bromide
- Etanautine
- Etybenzatropine (ethybenztropine)
- Fenpiverinium
- Fentonium bromide
- Fesoterodine
- Flavoxate
- Glycopyrronium bromide (+beclometasone/formoterol, +indacaterol, +neostigmine)
- Hexahydrodifenidol
- Hexahydrosiladifenidol
- Hexbutinol
- Hexocyclium
- Himbacine
- HL-031,120
- Homatropine
- Imidafenacin
- Ipratropium bromide (+salbutamol)
- Isopropamide
- J-104,129
- Hyoscyamine
- Mamba toxin 3
- Mamba toxin 7
- Mazaticol
- Mebeverine
- Meladrazine
- Mepenzolate
- Methantheline
- Methoctramine
- Methylatropine
- Methylhomatropine
- Methylscopolamine
- Metixene
- Muscarinic toxin 7
- N-Ethyl-3-piperidyl benzilate
- N-Methyl-3-piperidyl benzilate
- Nefopam
- Octatropine methylbromide (anisotropine methylbromide)
- Orphenadrine
- Otenzepad (AF-DX 116)
- Otilonium bromide
- Oxapium iodide
- Oxitropium bromide
- Oxybutynin
- Oxyphencyclimine
- Oxyphenonium bromide
- PBID
- PD-102,807
- PD-0298029
- Penthienate
- Pethidine
- pFHHSiD
- Phenglutarimide
- Phenyltoloxamine
- Pipenzolate bromide
- Piperidolate
- Pirenzepine
- Piroheptine
- Pizotifen
- Poldine
- Pridinol
- Prifinium bromide
- Procyclidine
- Profenamine (ethopropazine)
- Propantheline bromide
- Propiverine
- Quinidine
- 3-Quinuclidinyl thiochromane-4-carboxylate
- Revefenacin
- Rociverine
- RU-47,213
- SCH-57,790
- SCH-72,788
- SCH-217,443
- Scopolamine (hyoscine)
- Scopolamine butylbromide (hyoscine butylbromide)
- Silahexacyclium
- Sofpironium bromide
- Solifenacin
- SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., femoxetine, paroxetine)
- Telenzepine
- Terodiline
- Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
- Tiemonium iodide
- Timepidium bromide
- Tiotropium bromide
- Tiquizium bromide
- Tofenacin
- Tolterodine
- Tricyclic antidepressants (e.g., amitriptyline (+perphenazine), amitriptylinoxide, butriptyline, cidoxepin, clomipramine, desipramine, desmethyldesipramine, dibenzepin, dosulepin (dothiepin), doxepin, imipramine, lofepramine, nitroxazepine, northiaden (desmethyldosulepin), nortriptyline, protriptyline, quinupramine, trimipramine)
- Tridihexethyl
- Trihexyphenidyl
- Trimebutine
- Tripitamine (tripitramine)
- Tropacine
- Tropatepine
- Tropicamide
- Trospium chloride
- Typical antipsychotics (e.g., chlorpromazine, chlorprothixene, cyamemazine (cyamepromazine), loxapine, mesoridazine, thioridazine)
- Umeclidinium bromide (+vilanterol)
- WIN-2299
- Xanomeline
- Zamifenacin
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Precursors (and prodrugs) | |
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- See also
- Receptor/signaling modulators
- Nicotinic acetylcholine receptor modulators
- Acetylcholine metabolism/transport modulators
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