関: darifenacin hydrobromide

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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)

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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$.

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.^[1]

Clinical uses

Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency in adults.

References

^ Enablex on drugs.com

External links

Enablex product website, run by Warner Chilcott

UpToDate Contents

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1. 女性の切迫性尿失禁や過活動膀胱の治療 treatment of urgency incontinence overactive bladder in women
2. Lower urinary tract symptoms in men
3. Treatment of urinary incontinence in women
4. Medical treatment of benign prostatic hyperplasia
5. Urinary incontinence in men

English Journal

Patterns of use of antimuscarinic drugs to treat overactive bladder in Denmark, Sweden, and the United Kingdom.

Margulis AV1, Linder M2, Arana A1, Pottegård A3, Berglind IA2, Bui CL4, Kristiansen NS3, Bahmanyar S2, McQuay LJ4, Atsma WJ5, Appenteng K6, D'Silva M6, Perez-Gutthann S1, Hallas J3.
PloS one.PLoS One.2018 Sep 27;13(9):e0204456. doi: 10.1371/journal.pone.0204456. eCollection 2018.
PMID 30260993

Antimuscarinic use and discontinuation in an older adult population.

Vouri SM1, Schootman M2, Strope SA3, Xian H4, Olsen MA5.
Archives of gerontology and geriatrics.Arch Gerontol Geriatr.2018 Sep 22;80:1-11. doi: 10.1016/j.archger.2018.09.005. [Epub ahead of print]
PMID 30268971

Basic and clinical aspects of antimuscarinic agents used to treat overactive bladder.

Yamada S1, Ito Y2, Nishijima S3, Kadekawa K3, Sugaya K3.
Pharmacology & therapeutics.Pharmacol Ther.2018 Sep;189:130-148. doi: 10.1016/j.pharmthera.2018.04.010. Epub 2018 Apr 27.
PMID 29709423

Japanese Journal

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

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リンク元	「ダリフェナシン」
拡張検索	「darifenacin hydrobromide」

「ダリフェナシン」

Darifenacin
Systematic (IUPAC) name
	(S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
Clinical data
Trade names	Enablex
AHFS/Drugs.com	monograph
MedlinePlus	a605039
Pregnancy; category	AU: B3; US: C (Risk not ruled out);
Legal status	UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	15 to 19% (dose-dependent)
Protein binding	98%
Metabolism	Hepatic (CYP2D6- and CYP3A4-mediated)
Biological half-life	13 to 19 hours
Excretion	Renal (60%) and biliary (40%)
Identifiers
CAS Registry Number	133099-04-4
ATC code	G04BD10
PubChem	CID: 444031
IUPHAR/BPS	321
DrugBank	DB00496
ChemSpider	392054
UNII	APG9819VLM
KEGG	D01699
ChEBI	CHEBI:391960
ChEMBL	CHEMBL1346
Chemical data
Formula	C28H30N2O2
Molecular mass	426.55 g/mol
	SMILES O=C(N)C(c1ccccc1)(c2ccccc2)[C@H]3CN(CC3)CCc5cc4c(OCC4)cc5 ;
	InChI 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 ; Key:HXGBXQDTNZMWGS-RUZDIDTESA-N ;
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