Journal
EXPERT OPINION ON PHARMACOTHERAPY
Volume 9, Issue 10, Pages 1787-1796Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/14656566.9.10.1787
Keywords
blood-brain barrier; cytochrome P450 2D6; fesoterodine; 5-hydroxymethyltolterodine; muscarinic receptor antagonist; overactive bladder syndrome
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Background: Fesoterodine is a newly approved drug for the treatment of overactive bladder syndrome. Objective: The aim of this study was to review the preclinical and clinical data on fesoterodine. Methods: The study involved a search of the Medline database and the proceedings volumes of urological congresses. Results/conclusions: Fesoterodine functions as an orally active prodrug that is converted to the active metabolite 5-hydroxymethyltolterodine by non-specific esterases. 5-Hydroxymethyltolterodine is a muscarinic receptor antagonist. Fesoterodine is primarily eliminated as inactive metabolites along with significant renal excretion as the unchanged active metabolite 5-hydroxymethyltolterodine. Fesoterodine is indicated for use at doses of 4 and 8 mg once daily. In clinical studies both doses of fesoterodine were consistently superior to placebo in improving the symptoms of overactive bladder syndrome, with 8 mg/day having significantly greater effects than 4 mg/day.
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