Pharmacological treatment is usually indicated in moderate to severe tics in psychosocial and/or functional impairment. Neuroleptics with D2 antagonistic activity remain the cornerstone of anti-tic therapy. Lack of randomized controlled clinical trials base therapeutic decisions mainly on clinical expertise and common sense. Recently, aripiprazole has emerged as the neuroleptic with the most advantageous efficacy/side effect ratio for treating tics. Yet, in non-responders to aripiprazole, many neuroleptic and non-neuroleptic drugs, including botulinum toxin injections, are available and often successful. Apart from conducting methodologically sound trials (which includes sufficiently long observation periods), future efforts in the field should test the combination of cognitive-behavioral therapy with drugs or of multi-drug therapy as well as the development of biomarkers (endophenotypes) to monitor and even predict treatment response.