OBJECTIVE To review the options for acute and maintenance pharmacological treatment of bipolar disorder in children and adolescents. METHODS A comprehensive literature review of randomized clinical trials and open-label studies was conducted. RESULTS Published data from randomized controlled trials show that antipsychotics are significantly more effective than mood stabilizers in the treatment of manic or mixed episodes. Few data are available related to the treatment of depressive episodes. No trials of selective serotonin reuptake inhibitors have been conducted. Only open trials suggest that lithium and lamotrigine may be effective, whereas quetiapine did not demonstrate efficacy relative to placebo in two studies. Studies regarding the effectiveness of antipsychotics and mood stabilizers for the comorbid disorders are also few and inconclusive. Although long-term treatment is a core aspect of the management of children and adolescents with bipolar disorder, there is a lack of consistent efficacy data. If non-controlled trials suggest that lithium, lamotrigine, quetiapine, ziprazidone, and the combination of risperidone and divalproex or lithium may be useful in some conditions, only aripiprazole has shown efficacy relative to placebo for long-term symptom reduction and relapse prevention. Safety data show that the most frequently reported adverse events in children and adolescents treated with mood stabilizers are gastrointestinal and neurological, whereas use of antipsychotics is mainly related to weight gain and sedation. Lastly, while results from studies having evaluated the impact of pharmacological treatment on neuropsychological functioning are inconsistent, some of them nevertheless suggest that treatment with mood stabilizers may be associated with specific impairments. CONCLUSIONS Despite recent developments in identifying effective pharmacological interventions, numerous critical gaps remain.