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Darifenacin

Name: Darifenacin
Description: Darifenacin (Enablex, Novartis) is a medication used to treat urinary incontinence.Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to urinate. It should not be used in people with urinary retention.It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome. Pharmacology: Darifenacin is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs. Mechanism of action: Darifenacin selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function. Drug type: Approved. Investigational. Small Molecule. Drug category: Muscarinic Antagonists. Urinary antispasmodics
Synonym(s): Darifenacin, Emselex, Enablex
Has role: Drug
Super-category: Molecule
URL: http://www.drugbank.ca/drugs/DB00496
Id: DB00496
Related to: Cholinergic system, Muscarinic acetylcholine receptor M3
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Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00496  +
DefinitionDarifenacin (Enablex, Novartis) is a medic Darifenacin (Enablex, Novartis) is a medication used to treat urinary incontinence.Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to urinate. It should not be used in people with urinary retention.It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome. Pharmacology: Darifenacin is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs. Mechanism of action: Darifenacin selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function. Drug type: Approved. Investigational. Small Molecule. Drug category: Muscarinic Antagonists. Urinary antispasmodics arinic Antagonists. Urinary antispasmodics
Has roleDrug  +
IdDB00496  +
LabelDarifenacin  +
ModifiedDate29 October 2010  +
RelatedToCholinergic system  +, and Muscarinic acetylcholine receptor M3  +
SuperCategoryMolecule  +
SynonymDarifenacin  +, Emselex  +, and Enablex  +