Darifenacin

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Darifenacin
Systematic (IUPAC) name
2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
Identifiers
CAS number	133099-04-4
ATC code	G04BD10
PubChem	444031
DrugBank	APRD00903
Chemical data
Formula	C28H30N2O2
Mol. mass	426.55 g/mol
Pharmacokinetic data
Bioavailability	15 to 19% (dose-dependent)
Protein binding	98%
Metabolism	Hepatic (CYP2D6- and CYP3A4-mediated)
Half life	13 to 19 hours
Excretion	Renal (60%) and biliary (40%)
Therapeutic considerations
Pregnancy cat.	B3(AU) C(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral

Darifenacin (Enablex, Emselex, Novartis) is a medication used to treat urinary incontinence.

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 should not be used in people with urinary retention.

It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.(1)

[edit] Clinical uses

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

[edit] External links

• Enablex product website, run by Novartis Pharmaceuticals Corporation

[edit] References

(1) SPC for emselex-revised on 29/11/06 (available at www.medicines.org.uk)

v • d • e Urologicals (G04) Acidifiers Ammonium chloride, Calcium chloride Urinary antispasmodics (primarily antimuscarinics) Darifenacin, Emepronium, Fenoverine, Fesoterodine, Flavoxate, Meladrazine, Oxybutynin, Propiverine, Solifenacin, Terodiline, Tolterodine, Trospium For erectile dysfunction prostaglandins: Alprostadil PDE5 inhibitors: Avanafil - Sildenafil - Tadalafil - Udenafil - Vardenafil alpha blockers: Moxisylyte - Phentolamine - Yohimbine others: Apomorphine - Papaverine Other urologicals Acetohydroxamic acid, Collagen, Dimethyl sulfoxide, Magnesium hydroxide, Pentosan polysulfate, Phenazopyridine, Phenyl salicylate, Succinimide For benign prostatic hypertrophy 5α-reductase inhibitors: Dutasteride, Finasteride Alpha blockers: Alfuzosin, Doxazosin, Silodosin, Tamsulosin, Terazosin Herbals: Pygeum africanum, Serenoa repens