Attention-deficit/hyperactivity disorder (ADHD) is a common neuropsychiatric disorder that affects many domains of life. Studies have shown that adequate treatment of ADHD can affect the course of the disorder in a fundamental manner. While nonpharmacologic treatments such as education and various psycho-social interventions are used in the management of ADHD, pharmacotherapy is the mainstay of treatment for this disorder. Psychostimulants are the only group of agents that have been approved for the ADHD indication and are considered to be first-line treatment for the disorder. Methylphenidate, amphetamines, and pemoline are the most commonly used agents in this group. The stimulants have been successfully used for many years and their efficacy has been confirmed by a large number of clinical studies. Recent pharmacological advances have been made with longer-acting stimulants, new isomers, and more advanced drug delivery systems that enable more convenient dosing schedules with drug effects lasting throughout the day. Other nonstimulant medications have been shown to have anti-ADHD activity as well, although more research is needed on the efficacy and utility of these treatments. Antihypertensive medications and antidepressants, such as tricyclics and bupropion, have been studied and may have applications in the treatment of specific subgroups of patients with comorbid conditions or for patients who do not respond to stimulant treatment.