Agitation is a severe anxiety associated with motor restlessness. This physical and mental motor overactivity is usually nonproductive and is associated with a feeling of inner turmoil. Stimulants are the first choice in the treatment of attention deficit hyperactivity disorder (ADHD). In this report, a case of a 12 years old boy who developed acute psychomotor agitation and irritability with methylphenidate 27mg/day (0.5mg/kg) treatment for ADHD is presented. According to our knowledge, this is the first report of psychomotor agitation related to methylphenidate use in the literature (except overdose).