Detail of "133099-04-4"

Reference

Darifenacin

Darifenacin. Agent for irritable bowel syndrome and urinary incontinence, a muscarinic M3 antagonist.In this study，133099-04-4 is also used. Graul, A.; Castaner, J. (Prous Science Publishers, Barcelona 08080, Spain). Drugs of the Future, 21(11), 1105-1108 (English) 1996 Prous. CODEN: DRFUD4. ISSN: 0377-8282. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review, with 12 refs., of the clin. pharmacol. of darifenacin for treatment of irritable bowel syndrome and urinary incontinence as a muscarinic M3 antagonist. .

Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder

Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder. Chapple, Christopher R. (Royal Hallamshire Hospital, Department of Urology, Sheffield S10 2JF, UK). Expert Opinion on Investigational Drugs, 13(11), 1493-1500 (English) 2004 Ashley Publications Ltd. CODEN: EOIDER. ISSN: 1354-3784. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. Darifenacin is a novel M3 muscarinic selective receptor antagonist for once-daily treatment of overactive bladder (OAB), a highly prevalent, chronic and debilitating disease defined by urinary urgency with or without urge incontinence, usually with increased frequency of micturition and nocturia. In vitro, darifenacin is a potent and specific muscarinic receptor antagonist with ￡ 59-fold higher selectivity for muscarinic M3 receptors relative to other muscarinic receptor subtypes. This profile may, therefore, confer clin. efficacy in the treatment of OAB, with a lower propensity for adverse effects and safety issues related to blockade of other muscarinic receptor subtypes. Indeed, consistent with its low relative affinity for M1 and M2 receptors, no effects on cognitive function and heart-rate variability, resp., have been obsd. with darifenacin. Subsequent large-scale clin. trials have confirmed that darifenacin (at doses of 7.In this experiment, several chemicals are used like 133099-04-4 5 and 15 mg/day) results in central nervous system and cardiac adverse events comparable to placebo, and provides early and meaningful improvement across a range of OAB symptoms including incontinence episodes, urgency and urinary frequency. On the basis of such findings, darifenacin would appear to meet the current need for an effective OAB pharmacotherapy that is efficacious, well-tolerated and, more importantly, minimizes the risk of safety-related adverse effects. .