The safety of the use of medications in adolescents and children to treat bipolar disorder has not been extensively studied. The prevalence of bipolar disorder in children and adolescents is unknown due to the lack of completed large-scale epidemiological studies. In addition, the diagnosis of this disorder is still questionable in this age group because the same explicit diagnostic criteria used in adults potentially cannot be applied to children and adolescents since the early-onset symptoms often overlap with other disorders such as attention-deficit disorder. The safety of drugs used to treat bipolar disorder is of growing concern, particularly because this population usually requires more than one psychotropic medication to manage the disease. Common side effects seen with several agents, particularly antipsychotics, are somnolence, weight gain, extrapyramidal symptoms, dyslipidemia, type-2 diabetes, and hyperprolactinemia. This review will discuss the most advanced practice guidelines in assessing and treating bipolar disorder in children and adolescents, the safety and effectiveness of the drugs currently used based on clinical trials and post-marketing surveillance, and the risks versus benefits associated with their use.