Autism spectrum disorder (previously known as pervasive developmental disorders) is characterized by social communication deficits, impaired functioning, and restrictive or repetitive behaviors and interests. Patients with autism spectrum disorder also commonly experience core maladaptive behaviors such as aggression and irritability, self-injurious behaviors, hyperactivity, and sleep abnormalities. These behaviors may be sources of stress for caregivers and patients alike and may require pharmacologic management. Risperidone and aripiprazole are frequently used to treat both irritability and self-injurious behavior related to autism spectrum disorder. The opioid antagonist naltrexone has also been studied for self-injurious behaviors, although long-term data are lacking when used in the autism spectrum disorder population. Methylphenidate, atomoxetine, clonidine, and guanfacine are all potential options for the treatment of hyperactivity or attention-deficient hyperactivity disorder-like symptoms in patients with autism spectrum disorder. Lastly, melatonin is the most widely researched medication strategy for the management of sleep disorders in autism spectrum disorder. Future studies reviewing new pharmacologic treatment approaches in combination with non-pharmacologic therapies are warranted to ensure that target behaviors of autism spectrum disorder are appropriately managed.