Tourette syndrome (TS) is associated with dysregulated cortico-striatal-thalamo-cortical neural circuitry, of which the primary implicated neurotransmitters include dopamine, glutamate, and gamma-aminobutyric acid. Pharmacologic intervention for tics should be considered when tics are causing psychological, functional, or physical impairment, and behavioral treatment is either inaccessible or ineffective. Only 3 medications have Food and Drug Administration approval for TS, including 2 typical antipsychotics (pimozide and haloperidol) and 1 atypical antipsychotic (aripiprazole). As such, off-label pharmacologic interventions are frequently used. Though there is no hierarchical recommendation for medication in the treatment of TS, common first-line approaches often include alphaagonists, followed by atypical antipsychotics, followed by typical antipsychotics. Pharmacological treatment options utilizing novel mechanisms of action are emerging.