Drug reference

Darifenacin

Antimuscarinic · Overactive Bladder Treatment

Also known as Darifenacin hydrobromide, Emselex

AntimuscarinicOveractive Bladder Treatment

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid—toxicity in animal studies.

FDA category + note

Top interactionssee all 12 →

AmprenavirSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter
BoceprevirSevereDatabaseDDInter
BrexpiprazoleSevereDatabaseDDInter

Mechanism

Darifenacin is a selective muscarinic M3 receptor antagonist with 9- to 59-fold higher affinity for M3 over M1 and M5 subtypes. By preferentially blocking M3 receptors in the detrusor muscle of the bladder, it reduces involuntary detrusor contractions while sparing M1-mediated cognitive function and M2-mediated cardiac effects. This M3 selectivity provides effective relief from overactive bladder symptoms (urgency, frequency, incontinence) with fewer anticholinergic CNS and cardiovascular side effects.

Indications

Urinary frequencyUrinary urgencyIncontinenceOveractive bladderNeurogenic bladder

Dosing

Adult: Initially 7.5 mg once daily by mouth, increased if necessary to 15 mg after 2 weeks.
Hepatic adjustment: Caution in moderate impairment; avoid in severe impairment (risk of increased exposure). Maximum 7.5 mg daily in moderate impairment.
Geriatric: Use with caution, especially if frail. Prescription potentially inappropriate with delirium or dementia (risk of exacerbation of cognitive impairment), narrow-angle glaucoma (risk of acute exacerbation of glaucoma), or chronic prostatism (risk of urinary retention) due to increased antimuscarinic toxicity.
Max dose: 15 mg once daily

Pharmacokinetics

Metabolism

Metabolized by CYP2D6 and CYP3A4

Side effects

Common

Abdominal paindry eyenasal drynessXerostomiaBlurred visionConstipationGastrointestinal discomfortDrowsiness (less likely)Dizziness (less likely)Confusion (less likely)

Serious