Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0677481 (urinary frequency)
 1,126 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Solifenacin succinate [YM905; (3R)-1-azabicyclo[2.2.2]oct-3-yl(1S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate monosuccinate] is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The aim of the present study was to evaluate the antimuscarinic properties of solifenacin and to compare the results with those obtained for tolterodine, oxybutynin, darifenacin, propiverine and atropine. In radioligand receptor binding assay, Ki values of solifenacin for human muscarinic M1, M2, M3, M4 and M5 receptors were 26, 170, 12, 110 and 31 nM, respectively. In isolated rat urinary bladder, solifenacin competitively antagonized carbachol-induced contractions, with a pA2 value of 7.44+/-0.09. In these in vitro studies, the antimuscarinic action of solifenacin was more potent than that of propiverine and less potent than those of tolterodine, oxybutynin, darifenacin and atropine. In anesthetized rats, solifenacin and oxybutynin increased the maximum bladder capacity in a dose-dependent manner and also decreased the maximum intravesical pressure. The dosages required to produce a 30% increase in maximum bladder capacity (ED30 values) of solifenacin and oxybutynin were 0.35 and 0.30 mg/kg i.v., respectively, indicating approximately equal efficacies. These results support the fact that solifenacin, similarly to currently used antimuscarinic agents, is an effective agent in the treatment of overactive bladder symptoms such as urinary frequency and urge incontinence.
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PMID:Pharmacological characterization of a new antimuscarinic agent, solifenacin succinate, in comparison with other antimuscarinic agents. 1720 59

Around 1.5% of adults in Europe and the USA have urge urinary incontinence (involuntary leakage immediately preceded or accompanied by urgency). This is usually due to overactive bladder syndrome (defined as urgency, with or without urge incontinence, and usually with frequency and nocturia), which occurs in around 12% of adults, and is similarly prevalent in men and women. We last reviewed this condition in 2001. Since then, two new antimuscarinic drugs, darifenacin (Emselex) and solifenacin (Vesicare) have been licensed in the UK for urge incontinence and/or increased urinary frequency and urgency (as may occur in patients with overactive bladder syndrome), as have transdermal oxybutynin (Kentera) and modified-release formulations of tolterodine (Detrusitol XL) and propiverine (Detrunorm XL). Here we review the place of these newer drugs and formulations.
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PMID:Update on drugs for overactive bladder syndrome. 1758 29