Overactive bladder (OAB) is a common condition that has a profound impact on an individual's overall health and quality of life. Muscarinic receptor antagonists are the mainstay of oral pharmacotherapy for OAB. While all of the medications in this class are significantly more effective than placebo, they are also associated with more adverse events that may limit their overall use. Transdermal application of oxybutynin has been shown to avoid first-pass metabolism and, thus, may be associated with fewer antimuscarinic side effects. This paper reviews the pharmacology of transdermal oxybutynin gel and summarizes the available data regarding this product in the treatment of OAB. It also discusses the role of this product in the OAB treatment armamentarium. Oxybutynin transdermal gel has been shown to have significant advantages over placebo, in terms of urgency incontinence episodes, urinary frequency and voided volume in a Phase III study. Application site effects were higher in the gel group, but the incidence of antimuscarinic side effects were lower than those seen with oral preparations. The lower incidence of skin side effects, as compared with the transdermal patch, may confer a theoretical advantage toward the gel product. While promising, unanswered questions remain regarding persistence with treatment after this mode of therapy, and head-to-head comparisons with other antimuscarinics are absent.