Tic disorder is a common neurodevelopmental disorder that develops in childhood, mainly characterized by motor and/or vocal tics. The treatment methods for tic disorders include both pharmacological and non-pharmacological interventions. α₂-adrenoceptor receptor agonists (including clonidine and guanfacine) are the first-line drugs for treating tic disorders, especially for mild to moderate tic disorders with comorbid attention-deficit hyperactivity disorder. Moreover, the usage of α₂-adrenoceptor receptor agonists has been increasing year by year, and their rational use has attracted closed attention. To summarize the evidence regarding clinical efficacy and safety, this article systematically reviews the mechanism, pharmacokinetic and pharmacodynamic characteristics, and relative clinical researches of α₂-adrenoceptor receptor agonists in treating tic disorders. However, data quality, long-term efficacy monitoring, and genetic polymorphisms related to drug metabolism still have limitations, providing insights for further research.

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