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Darifenacin


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	℞-only(US)
Routes	Oral

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

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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)

Administration

Darifenacin is administered as a once-daily extended-release oral tablet.

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, Flavoxate, Meladrazine, Oxybutynin, Propiverine, Solifenacin, Terodiline, Tolterodine, Trospium
For erectile dysfunction	Alprostadil, Apomorphine, Moxisylyte, Papaverine, Phentolamine, Yohimbine, PDE5 inhibitors (Avanafil, Sildenafil, Tadalafil, Udenafil, Vardenafil)
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, Tamsulosin, Terazosin Herbals: Pygeum africanum, Serenoa repens