The mainstay of treatment in severe asthma is β2 agonist therapy. During its treatment, toxicity may occur especially with the use of oral albuterol or its prolonged nebulization. The clinical manifestations of albuterol toxicity include tachycardia, hypokalemia, tremors, and hyperglycemia. Toxicity occurring due to the use of metered-dose inhaler is less common. Moreover, levalbuterol is believed to have a better safety profile than albuterol, making it a very unusual culprit for toxicity. We report an 8-year-old asthmatic boy who developed severe tachycardia, and agitation and exhibited signs of levalbuterol toxicity. He had been inadvertently administered 50 puffs of levalbuterol via metered drug inhaler at home for an acute exacerbation of asthma. With supportive management, his condition stabilized in 36 hours. This case illustrates that a large dose of levalbuterol administered with a metered-dose inhaler can lead to toxicity, which resolves with discontinuation of β2 agonist therapy and supportive treatment.