Literature DB >> 15493952

Darifenacin: in the treatment of overactive bladder.

Katherine F Croom1, Gillian M Keating.   

Abstract

Darifenacin is a selective muscarinic M3-receptor antagonist that has been evaluated in clinical trials in patients with overactive bladder syndrome (OAB) using a controlled-release formulation. In multicentre, randomised, double-blind trials in patients with OAB, darifenacin 7.5 or 15 mg once daily for 12 weeks significantly reduced the frequency of urinary incontinence, frequency of micturition and frequency and severity of urgency versus placebo. A significant difference from placebo was apparent 2 weeks after starting treatment. At a dosage of 30 mg once daily, darifenacin significantly prolonged warning time compared with placebo. Darifenacin 15 mg once daily for 2 weeks was as effective as oxybutynin 5 mg three times daily at reducing the frequency of urinary incontinence and frequency and severity of urgency in patients with OAB. Darifenacin was generally well tolerated in clinical trials. The most common adverse events were dry mouth and constipation. CNS tolerability appeared to be similar to that of placebo. Darifenacin had no adverse effect on cognitive function in healthy elderly volunteers.

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Year:  2004        PMID: 15493952     DOI: 10.2165/00002512-200421130-00005

Source DB:  PubMed          Journal:  Drugs Aging        ISSN: 1170-229X            Impact factor:   3.923


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2.  Assessment of the relative in vivo potency of the hydroxylated metabolite of darifenacin in its ability to decrease salivary flow using pooled population pharmacokinetic-pharmacodynamic data.

Authors:  Thomas Kerbusch; Peter A Milligan; Mats O Karlsson
Journal:  Br J Clin Pharmacol       Date:  2004-02       Impact factor: 4.335

3.  In vitro and in vivo tissue selectivity profile of solifenacin succinate (YM905) for urinary bladder over salivary gland in rats.

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Journal:  Eur J Pharmacol       Date:  2004-05-25       Impact factor: 4.432

4.  Multiple functional defects in peripheral autonomic organs in mice lacking muscarinic acetylcholine receptor gene for the M3 subtype.

Authors:  M Matsui; D Motomura; H Karasawa; T Fujikawa; J Jiang; Y Komiya; S Takahashi; M M Taketo
Journal:  Proc Natl Acad Sci U S A       Date:  2000-08-15       Impact factor: 11.205

Review 5.  Muscarinic antagonists in development for disorders of smooth muscle function.

Authors:  R M Wallis; C M Napier
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6.  Functional selectivity of muscarinic receptor antagonists for inhibition of M3-mediated phosphoinositide responses in guinea pig urinary bladder and submandibular salivary gland.

Authors:  Carl P Nelson; Paul Gupta; Carolyn M Napier; Stefan R Nahorski; R A John Challiss
Journal:  J Pharmacol Exp Ther       Date:  2004-05-12       Impact factor: 4.030

7.  Prevalence and burden of overactive bladder in the United States.

Authors:  W F Stewart; J B Van Rooyen; G W Cundiff; P Abrams; A R Herzog; R Corey; T L Hunt; A J Wein
Journal:  World J Urol       Date:  2002-11-15       Impact factor: 4.226

8.  Population pharmacokinetic modelling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability.

Authors:  Thomas Kerbusch; Ulrika Wählby; Peter A Milligan; Mats O Karlsson
Journal:  Br J Clin Pharmacol       Date:  2003-12       Impact factor: 4.335

9.  Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists.

Authors:  P G Gillberg; S Sundquist; L Nilvebrant
Journal:  Eur J Pharmacol       Date:  1998-05-22       Impact factor: 4.432

Review 10.  Darifenacin, an M3 selective receptor antagonist, is an effective and well-tolerated once-daily treatment for overactive bladder.

Authors:  F Haab; L Stewart; P Dwyer
Journal:  Eur Urol       Date:  2004-04       Impact factor: 20.096

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Authors:  Sarvpreet S Ubee; Ramaswamy Manikandan; Gurpreet Singh
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3.  Darifenacin hydro-bromide.

Authors:  S Selvanayagam; B Sridhar; K Ravikumar
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Review 4.  Treatment of overactive bladder in the aging population: focus on darifenacin.

Authors:  Swati Jha; Matthew Parsons
Journal:  Clin Interv Aging       Date:  2006       Impact factor: 4.458

Review 5.  Similarities and differences in the autonomic control of airway and urinary bladder smooth muscle.

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