Asperger syndrome (AS) is a neurobiological disorder whose core clinical symptoms include impairment in social interaction, impairments in verbal and nonverbal communication, and restricted, repetitive, and stereotyped patterns of behavior, interests, and activities. AS is often accompanied by coexisting neuropsychiatric disorders, including anxiety disorder, affective disorder, obsessive-compulsive disorder, Tourette syndrome, attention-deficit/hyperactivity disorder, and sleep disorders. These clinical features provide the rationale for the use of psychotropic medications (psychopharmacotherapy) in individuals with AS. This article describes the clinical indications for psychopharmacotherapy and provides guidelines for monitoring the effectiveness of medication treatment and for preventing and monitoring the development of side effects and/or adverse effects of psychotropic medications.