Background: Tizanidine, an α-2 adrenoceptor agonist, is widely prescribed for the management of spasticity in adults. Case reports on pediatric tizanidine overdose are limited. Here, we report a case of pediatric tizanidine toxicity that was reversed with naloxone., Case Presentation: A 3-year-old male presented to the emergency department with lethargy, bradycardia, and bradypnea after accidental ingestion of multiple tizanidine tablets. Improvements in the level of consciousness and respiratory and heart rates were observed after two intravenous administrations of naloxone at a dose of 0.05 and 0.1 mg/kg, respectively., Conclusions: This case report provides further evidence regarding the use of naloxone as a viable antidote for centrally acting α-2 receptor agonists and presents additional epidemiologic data on childhood tizanidine poisoning., (© 2021. The Author(s).)