We present an overview of the current pharmacological treatment of urinary incontinence (UI) in women, according to the latest evidence available. After a brief description of the lower urinary tract receptors and mediators (detrusor, bladder neck, and urethra), the potential sites of pharmacological manipulation in the treatment of UI are discussed. Each class of drug used to treat UI has been evaluated, taking into account published rate of effectiveness, different doses, and way of administration. The prevalence of the most common adverse effects and overall compliance had also been pointed out, with cost evaluation after 1 month of treatment for each class of drug. Moreover, we describe those newer agents whose efficacy and safety need to be further investigated. We stress the importance of a better understanding of the causes and pathophysiology of UI to ensure newer and safer treatments for such a debilitating condition.