Psychopharmacology is a challenge for health care providers treating adolescents. A detailed and accurate assessment, including developmental issues relevant to adolescence in general and to the individual adolescent, guides clinicians in formulating thoughtful and effective treatment plans to meet the needs of each patient. Parents play an important role in providing family history regarding psychiatric diagnoses and the response to various drugs, in making decisions to initiate medication and to change a medication regimen, and in monitoring an adolescent's adherence to a prescribed regimen. The role of parents is especially important for younger patients. Following the biopsychosocial model, rarely should psychopharmacologic agents be used as the sole means to treat a psychiatric condition in adolescents. Pharmacologic agents described in this article are tools that have their effect in the biological domain of central neurotransmitters, but psychosocial interventions addressing the emotional and behavioral issues that are the indications for such medication are generally also required. The development of newer medications holds promise for more effective treatment of target symptoms with minimal side effects.