出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/24 21:16:48」(JST)[Wiki en表示]
|Systematic (IUPAC) name|
(S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
|Bioavailability||15 to 19% (dose-dependent)|
|Metabolism||Hepatic (CYP2D6- and CYP3A4-mediated)|
|Biological half-life||13 to 19 hours|
|Excretion||Renal (60%) and biliary (40%)|
|CAS Registry Number||Y|
|Molecular mass||426.55 g/mol|
|N (what is this?)|
Darifenacin (trade name Enablex in US and Canada, Emselex in Europe) is a medication used to treat urinary incontinence. It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and previously was marketed by Novartis; however in 2010 US rights for were sold to Warner Chilcott for 400 million US$.
- 1 Mechanism of action
- 2 Clinical uses
- 3 References
- 4 External links
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. It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.
It 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.
Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency in adults.
- Enablex on drugs.com
- Enablex product website, run by Warner Chilcott
- Pharmacological Characterization of Itch-Associated Response Induced by Repeated Application of Oxazolone in Mice
- , ,
- Journal of pharmacological sciences 113(3), 255-262, 2010-07-20
- … muscarinic acetylcholine–receptor antagonist darifenacin. …
- NAID 10029889358
- Noninvasive evaluation of brain muscarinic receptor occupancy of oxybutynin, darifenacin and imidafenacin in rats by positron emission tomography
- YOSHIDA A.
- Life Sci 87, 175-180, 2010
- NAID 80021166749
- Functional expression of muscarinic and purinoceptors in the urinary bladder of male and female rats and guinea pigs
- , ,
- Journal of Smooth Muscle Research 46(4), 201-215, 2010
- … The tonic component and the ACh response were inhibited by the M3 receptor antagonist, darifenacin (10–6 M, P≤0.05), but not by the M2 receptor antagonist, methoctramine (10–5 M). …
- NAID 130000860974
- ムスカリン性受容体のうちM3 receptorを選択的に阻害する(SP. 412)