Darifenacin, an M3 Selective Receptor Antagonist, is an Effective and Well-Tolerated Once-Daily Treatment for Overactive Bladder

Haab, F.; Stewart, Lawrence H.; Dwyer, Peter

doi:10.1016/j.eururo.2004.01.008

Cited by 226 publications

(122 citation statements)

References 28 publications

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“…With the recent release of several M 3 -selective muscarinic antagonists has come the realization that there are only slight di¡erences in the clinical e⁄cacy between the M 3 -selective antagonists (darifenacin and solifenacin) and the more M 2 /M 3 balanced antagonists (tolterodine and trospium). Clinically, distinctions between these new agents may appear to be in their side e¡ects [Drutz et al, 1999;Appell et al, 2001;Chancellor et al, 2001;Diokno et al, 2002;Rovner and Wein, 2002;Siami et al, 2002;Sussman and Garely, 2002;Halaska et al, 2003;Haab et al, 2004;Chapple et al, 2005;MacDiarmid et al, 2005]. No studies have been reported on M 2 -selective anticholinergic medications in humans.…”

Section: Introductionmentioning

confidence: 99%

M₂ mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

Braverman¹,

Лебед²,

Linder³

et al. 2006

Neurourology and Urodynamics

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Aims: Previous studies have shown increased density of M 2 receptors in hypertrophied rat bladders that possess an M 2 contractile phenotype. The aim of the current study is to determine whether human bladders with an M 2 contractile phenotype also have a greater density of bladder M 2 receptors. Materials and Methods: Human bladders were obtained from 24 di¡erent organ transplant donors. Darifenacin and methoctramine a⁄nity was determined by the rightward shift of cumulative carbachol concentration contractile response curves for each bladder. Radioligand binding and immunoprecipitation was used to quantify M 2 and M 3 subtypes in isolated detrusor muscle and urothelium. In addition, pig bladder muscle and urothelial receptors were quanti¢ed for comparison. Results: In the human urothelium total, M 2 and M 3 muscarinic receptor density is signi¢cantly negatively correlated with the a⁄nity of darifenacin for inhibition of contraction of the detrusor muscle. In the detrusor muscle there is no correlation between receptor density and darifenacin a⁄nity for inhibition of contraction. Muscarinic receptor density is greater in the muscle than in the urothelium in human bladders whereas in the pig bladder the density is greater in the urothelium than in the muscle. Conclusions: The greater density of urothelial muscarinic receptors in human bladders with lower darifenacin a⁄nity, indicative of a greater contribution of M 2 receptors to the contractile response, points towards a possible role of the urothelium in controlling M 2 mediated contractile phenotype. In comparison between human and pig bladders, the distribution of muscarinic receptor subtypes in the muscle and urothelium are quite di¡erent.

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Section: Introductionmentioning

confidence: 99%

M₂ mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

Braverman¹,

Лебед²,

Linder³

et al. 2006

Neurourology and Urodynamics

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“…Die Behandlung des OAB Syndroms ist im weiteren jedoch Domäne der medikamentösen Therapie, in erster Linie mit Anticholinergika wie Oxybutynin, Tolterodin, Solifenacin, Trospiumchlorid oder Propiverine (Andersson and Chapple, 2001;Appell et al, 2001a;Haab et al, 2004;Madersbacher and Murtz, 2001;Nilvebrant et al, 1997;Rovner and Wein, 2003).…”

Section: Medikamentöse Therapieunclassified

Botulinumtoxin in der Urologie

Schulte-Baukloh

Knispel

2004

Urologe [A]

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“…45,46 It is available in two doses, 7.5 and 15 mg. Owing to its extensive metabolism by liver CYP2D6 and CYP3A4, the renal excretion of darifenacin is negligible. 47 Solifenacin succinate is a competitive M3 antagonist available in 5 and 10 mg doses.…”

Section: Darifenacin Solifenacin and Fesoterodinementioning

confidence: 99%

“…Unfortunately, the actual number of patients receiving treatment may be quite low despite the obvious effects of OAB on QoL and costs to society. 7 Out of over 160,000 survey respondents with probable OAB, only 45.7% had discussed the symptoms with a medical provider, 22.5% had previously used prescription medications for OAB, 13.5% had used OAB medications in the last 12 months, and 8.1% were currently undergoing treatment.…”

Section: Introductionmentioning

confidence: 99%

Update on the management of overactive bladder: patient considerations and adherence

Dmochowski¹,

Gomelsky²

2010

RRU

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Overactive bladder (OAB) is a common condition that causes a profound impact on an individual's overall health and quality of life. Muscarinic receptor antagonists are the mainstay of oral pharmacotherapy for OAB. Although all of the medications in this class are significantly more effective than placebo, they are also associated with more adverse events that may limit their overall use. Although newer preparations of these medications have sought to improve tolerability and efficacy through alternative routes of delivery and once-daily dosing, improved adherence to treatment and treatment persistence continue to be an ongoing challenge. An improved understanding of the factors involved in persistence of medical OAB therapy is imperative in efforts to optimize therapeutic benefits in this chronic and potentially morbid condition.

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Darifenacin, an M3 Selective Receptor Antagonist, is an Effective and Well-Tolerated Once-Daily Treatment for Overactive Bladder

Cited by 226 publications

References 28 publications

M₂ mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

M₂ mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

Botulinumtoxin in der Urologie

Update on the management of overactive bladder: patient considerations and adherence

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Darifenacin, an M3 Selective Receptor Antagonist, is an Effective and Well-Tolerated Once-Daily Treatment for Overactive Bladder

Cited by 226 publications

References 28 publications

M2 mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

M2 mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

Botulinumtoxin in der Urologie

Update on the management of overactive bladder: patient considerations and adherence

Contact Info

Product

Resources

About

M₂ mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors

M₂ mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors