title: Darifenacin in the treatment of overactive bladder.
abstract: Darifenacin is a novel muscarinic M(3) selective receptor antagonist developed for the once-daily treatment of overactive bladder, a chronic, debilitating and highly prevalent condition affecting adults of all ages. Preclinical research has confirmed the pharmacological profile of darifenacin as a potent antimuscarinic agent with up to 59-fold higher affinity for M(3) receptors than other muscarinic receptor subtypes and selectivity for the bladder over other tissues expressing these receptors. Extensive research in large, randomized, placebo-controlled trials have demonstrated that darifenacin, at doses of 7.5 and 15 mg once daily (q.d.), is efficacious in the treatment of overactive bladder, improving the core symptoms of urinary urgency, urge incontinence, increased micturition frequency and bladder capacity. In addition, post-hoc analyses have shown that many patients can achieve clinically meaningful continence levels, e.g., > or =90% reduction in incontinence episodes or > or =7 consecutive dry days. These results are supported by significant improvements in quality of life, which have paralleled the overactive bladder symptom reductions. Both fixed and flexible darifenacin dosing regimens produce these beneficial effects, which extend to the more vulnerable population of older patients. Hence, in conjunction with data showing that this agent has a good safety and tolerability profile, these findings indicate that darifenacin may provide an effective alternative pharmacotherapy for the treatment of patients with overactive bladder.
authors.affiliation: Department of Urology, Tenon Hospital, Paris, France. francois.haab@tnn.ap-hop-paris.fr
authors.forename: Francois
authors.initials: F
authors.lastname: Haab
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004347:Drug Interactions; D006801:Humans; D018727:Muscarinic Antagonists / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011759:Pyrrolidines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011788:Quality of Life; D043587:Receptor, Muscarinic M3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D016896:Treatment Outcome; D014549:Urinary Incontinence / Q000188:drug therapy*
chemical_list: D001572:Benzofurans; D018727:Muscarinic Antagonists; D011759:Pyrrolidines; D043587:Receptor, Muscarinic M3; C101207:darifenacin