Bipolar disorder (BPD) is a recurrent psychiatric disorder characterized by episodes of mania and hypomania, depression, or mixed episodes. Individuals with BPD often experience anxiety and decreased cognitive performance and productivity. BPD has emerged as a major health concern, with lifelong social and occupational impairment and poor prognosis secondary to its substantially elevated morbidity and mortality rates, which are largely due to associated cardiovascular disease, metabolic syndrome, substance abuse or misuse, and potential for physical self-harm. The lifetime prevalence of bipolar spectrum disorders is approximately 3% to 7% of the population. Given the disease complexity, individuals with BPD often require lifelong pharmacological therapy to achieve desired treatment outcomes. In recent years there has been an explosion of new investigations into the pathophysiology of BPD and its medication therapies. This article will review current, emerging, and controversial therapies for the treatment of BPD, specifically the mania aspect. (Formulary. 2011;46:82-97.)