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QuickView for Darifenacin (compound)

Name: darifenacin
PubChem Compound ID: 444030
Molecular formula: C28H31BrN2O2
Molecular weight: 507.462 g/mol
Darifenacin hydrobromide (JAN/USAN); UK-88525; UK-88525-04; Darifenacin hydrobromide; D01699; 133099-07-7; Emselex; Enablex; Enablex (TN)
Name: darifenacin
Name (isomeric): DB00496
Drug Type: small molecule
Brand: Enablex, Emselex
Category: Muscarinic Antagonists, Urinary antispasmodics
CAS number: 133099-04-4
Indication: For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
Darifenacin is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinit...
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Mechanism of Action: Darifenacin selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function.
Absorption: The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.
Protein binding: Darifenacin is approximately 98% bound to plasma proteins (primarily to alpha-1-acid-glycoprotein).
Biotransformation: Hepatic. Primarily mediated by the cytochrome P450 enzymes CYP2D6 and CYP3A4.
Half Life: The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.
Clearance: 40 L/h [extensive metabolizers] 32 L/h [poor metabolizers]
Toxicity: Overdosage can potentially result in severe central anticholinergic effects.
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals.
Drug interaction:
ClarithromycinThis potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
TacrineThe therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Darifenacin, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
KetoconazoleThis potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
TelithromycinTelithromycin may reduce clearance of Darifenacin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Darifenacin if Telithromycin is initiated, discontinued or dose changed.
NefazodoneThis potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
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