Tourette's syndrome has been of neurologic and psychiatric interest since the original description of this condition by Gilles de la Tourette in 1885, and it has been associated with a wide variety of treatments over the years. With the advent of advances in neurochemistry and neuropharmacology, a neurobiologic approach has emerged with the application of many drugs from the fields of neurology and psychiatry. In addition, many of the comorbid conditions that coexist, such as attention deficit disorder and obsessive compulsive disorder (OCD), are amenable to both pharmacologic and behavioral approaches. Drug treatment has included dopamine receptor blockers for tics, dopamine agonists, dopamine depletors, and stimulants for attention deficit hyperactivity disorder (ADHD), noradrenergic drugs for tics and ADHD, serotonergic drugs for OCD, and chemical denervation for involuntary movements with the use of botulinum toxin and stereotactic surgery. It is the purpose of this review to outline the various approaches that are currently available as treatments, realizing that as new drugs are introduced in neurology and psychiatry, they too will find their way into treatment options.