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Functional: Pharmacological Management of LUTS
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====== Oxybutynin (Ditropan) ====== * '''Mechanism of action:''' *# '''Blocks muscarinic receptors''' (main effect when given systemically) *# '''Direct muscle relaxant''' *# '''Local anesthetic effects''' *#* The latter 2 may be of importance when the drug is administered intravesically, but probably play no role when it is given orally. * '''Metabolism: Undergoes extensive upper gastrointestinal and first-pass hepatic metabolism via the cytochrome P450 system (CYP3A4) into multiple metabolites.''' ** '''The primary metabolite, N-desethyloxybutynin, has been implicated as the major cause of the troublesome side effect of dry mouth associated with oxybutynin.''' * Selectivity: slightly higher affinity for M1 and M3 receptors than for M2 receptors * Dosing: Immediate release and extended release formulations available, as well as a transdermal patch and gel formulations. ** '''Transdermal delivery''' also alters oxybutynin metabolism, reducing N-desethyloxybutynin production to an even greater extent than OXY-ER, and is associated with '''much less dry mouth. Side effects include application site reaction pruritus and erythema''' * '''Adverse events:''' ** '''Immediate release has high incidence of side effects (dry mouth, constipation, drowsiness, blurred vision)''' ** Extended release version was developed to decrease liver metabolite formulation of N-desethyloxybutynin with the presumption that it would result in decreased side effects ** A significant dose-response relationship for both urgency incontinence episodes and dry mouth. ** '''Studies show no effect on ECG''' ** '''May have negative effects on cognitive function, particularly in the elderly population but also in children''' *Estimated cost per month: 10$ USD[https://www.goodrx.com/]
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