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Darifenacin
- indication:For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Overdosage can potentially result in severe central anticholinergic effects.
- absorprion: The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.
- halflife: The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.
- roouteelimination:
- volumedistribution: * 163 L
- clearance: * 40 L/h [extensive metabolizers] * 32 L/h [poor metabolizers]