Tourette syndrome is now widely accepted as a neurological disorder characterized by chronic multiple tics and uncontrollable sounds. The exact etiology of Tourette syndrome is still unknown, although an organic etiology is suspected. Hypotheses of the pathophysiologic mechanism of Tourette syndrome have generally included a component of neurotransmitter system "imbalance". Dopaminergic, cholinergic, serotoninergic, noradrenergic and peptidergic neurotransmitters have all been proposed as components of this "imbalance". The two most utilized agents, haloperidol and pimozide, decrease central dopaminergic activity by blocking dopamine receptors and have been shown to improve the symptomatology of Tourette syndrome. However, adverse effects limit their usefulness and new drugs that have fewer adverse effects and greater efficacy are needed. Some of the new therapeutic agents evaluated in Tourette syndrome are mentioned. The purpose of this paper is to provide physicians with guidelines for the pharmacological treatment of Tourette syndrome, based on the present available literature.