Abstract
Oxybutynin is a muscarinic receptor antagonist, which has been available for a number of years in its original immediate-release (IR) formulation. While oxybutynin IR has proven effective for the treatment of overactive bladder, its extended use can be limited by adverse effects, particularly dry mouth.
An extended-release (ER) formulation of oxybutynin based on the OROS®1 system has recently become available, which allows once daily administration.
In direct comparison to oxybutynin IR, oxybutynin ER has an increased oral bioavailability for the parent compound oxybutynin which is accompanied by a reduced bioavailability for the active metabolite N-desethyl-oxybutynin. The latter has been implicated in mediating a major part of the adverse effects of oxybutynin treatment.
Two double-blind, placebo-controlled, randomised studies in patients with overactive bladder have demonstrated that oxybutynin ER has a similar efficacy as oxybutynin IR but with improved tolerability. This is in line with clinical pharmacological studies demonstrating a smaller impairment of saliva production with oxybutynin ER than with oxybutynin IR.
Thus, the ER formulation of oxybutynin maintains the therapeutic benefits and concomitantly improves tolerability.
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Michel, M.C. A Benefit-Risk Assessment of Extended-Release Oxybutynin. Drug-Safety 25, 867–876 (2002). https://doi.org/10.2165/00002018-200225120-00004
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DOI: https://doi.org/10.2165/00002018-200225120-00004