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Functional: Pharmacological Management of LUTS
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===== Pharmacology ===== *'''<span style="color:#ff0000">Anti-cholinergics can be classified as tertiary vs. quaternary amines</span>''' ** '''<span style="color:#ff0000">Tertiary amines</span>''' *** '''<span style="color:#ff0000">Oxybutynin, tolterodine, fesoterodine, solifenacin, darifenacin,</span>''' atropine, imidafenacin, and propiverine *** '''Well absorbed from the GI tract''' *** '''Theoretically able to pass into the central nervous system (CNS)''' **** '''Factors that increase the likelihood of an anti-cholinergic passing through the blood-brain barrier (3):''' ****# '''High lipophilicity''' ****# '''Small molecular size''' ****# '''Low electrical charge''' ** '''<span style="color:#ff0000">Quaternary amines</span>''' *** '''<span style="color:#ff0000">Trospium and propantheline</span>''' *** '''Not well absorbed from the GI tract''' *** '''<span style="color:#ff0000">Pass into the CNS to a limited extent, and have a low incidence of CNS side effects</span>''' * '''<span style="color:#ff0000">Metabolism</span>''' ** '''<span style="color:#ff0000">Many metabolized by the P450 enzyme system to active and/or inactive metabolites.</span>''' *** Most commonly involved P450 enzymes are CYP2D6 and CYP3A4 *** Metabolic conversion creates '''a risk for drug-drug interactions; coadministration of a potent inhibitor of this enzyme (e.g., ketoconazole) may lead to an increase in the circulating drug'''
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