Abstract
Overactive bladder is a chronic condition that affects millions of people worldwide. Antimuscarinic agents are the predominant pharmacotherapy for overactive bladder. Tolterodine is a potent, competitive muscarinic receptor antagonist that exhibits in vivo selectivity for the bladder over other tissues that contain muscarinic receptors (such as the salivary glands and the eye), which helps explain why it has such a good tolerability profile compared to oxybutynin. Tolterodine is the first drug specifically developed for the treatment of overactive bladder and is available as both an immediate- and extended-release formulation. This review summarizes the primary antimuscarinic profile of tolterodine and reviews the efficacy, safety and tolerability of tolterodine in studies of patients with overactive bladder.