Published data concerning drugs currently used for the treatment of overactive bladder (OAB) syndrome are reviewed. Modern notions about the physiology and pathophysiology of micturition are considered and data on the pharmacological properties, tolerance, and therapeutic efficiency of anticholinergic drugs (antimuscarinic agents) are presented. These drugs are still the first-line of OAB treatment, although they often poorly control the disease and induce a number of side effects. Progress in the knowledge of physiology and pathophysiology of micturition is a basis for the development of new promising treatments for the management of OAB symptoms, including β 3 -adrenoceptor agonists, agonists of vitamin D receptor, drugs influencing KCNQ/Kv7 channels, and some other.