Darifenacin
- Atc Codes:G04BD10
- CAS Codes:133099-07-7#133099-04-4
- PHARMGKB ID:133099-07-7#133099-04-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Emselex; Belgium: Emselex; Bulgaria: Emselex; Cyprus: Emselex; Czech Republic: Emselex; Denmark: Emselex; Estonia: Emselex; Finland: Emselex; France: Emselex; Germany: Emselex; Greece: Emselex; Hungary: Emselex; Ireland: Emselex; Latvia: Emselex; Lithuania: Emselex; Luxembourg: Emselex; Malta: Emselex; Netherlands: Emselex; Poland: Emselex; Portugal: Emselex; Romania: Emselex; Slovakia: Emselex; Slovenia: Emselex; Sweden: Emselex; UK: Emselex.
North America
Canada: Enablex; USA: Enablex.
Latin America
Argentina: Darisec, Enablex.
Drug combinations
Chemistry
Darifenacin Hydrobromide: C~28~H~30~N~2~O~2~ HBr. Mw: 507.46. (1) 3-Pyrrolidineacetamide, 1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-, monohydrobromide, (3S)-; (2)(S)-2-{1-[2-(2,3-Dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidnyl}-2,2-diphenylacetamide hydrobromide. CAS-133099-07-7; CAS-133099-04-4 (darifenacin)(2004).
Pharmacologic Category
Genitourinary Smooth Muscle Relaxants. Anticholinergic Agent. (ATC-Code: G04BD10).
Mechanism of action
Antimuscarinic agent, genitourinary antispasmodic. Selective antagonist of the M~3~ muscarinic (cholinergic) receptors, involved in contraction of the detrusor muscle of the bladder and GI smooth muscle, saliva production, and iris sphincter function. Darifenacin exhibits functional selectivity for urinary bladder over secretory (e.g. salivary) glands. Blockade of the receptor limits bladder contractions, reducing the symptoms of bladder irritability/overactivity.
Therapeutic use
Management of symptoms of bladder overactivity (urge incontinence, urgency, and frequency).
Pregnancy and lactiation implications
Teratogenic effects in animal studies. Caution when administering drug during pregnancy or lactation.
Unlabeled use
Contraindications
Hypersensitivity to darifenacin or any component of the formulation. Uncontrolled narrow-angle glaucoma. Urinary retention, paralytic ileus, GI or GU obstruction.
Warnings and precautions
May cause drowsiness and/or blurred vision. Caution in hot weather and/or exercise due to heat prostration. Use with caution in decreased GI motility, constipation, hiatal hernia, reflux esophagitis, or ulcerative colitis (may decrease GI motility). Should be used with extreme caution and only when potential benefit outweighs risks of treatment in controlled narrow-angle glaucoma. Use cautiously in hepatic impairment (not recommended in severe impairment), myasthenia gravis (may decrease GI motility), prostatic hyperplasia (nonobstructive) or bladder outlet obstruction (may increase risk of urinary retention). Risk of drug interactions (use with caution in patients taking strong CYP inhibitors).