The present invention provides compositions and methods for administeringoxybutynin while minimizing the incidence and or severity of adverse drugexperiences associated with oxybutynin therapy. In one aspect, thesecompositions and methods provide a lower plasma concentration of oxybutyninmetabolites, such as N-desethyloxybutynin, which is presumed to becontributing at least in part to some of the adverse drug experiences, whilemaintaining sufficient oxybutynin plasma concentration to benefit a subjectwith oxybutynin therapy. The invention also provides isomers of oxybutynin andits metabolites that meet these characteristics of minimized incidence and/orseverity of adverse drug experiences, and maintenance of beneficial andeffective therapy for overactive bladder. In some aspects, the composition maybe presented in the form of an unoccluded or free form topically administeredgel.