In the context of increasingly intense athletic competition, athletes are motivated to enhance their performance through various methods, including the use of pharmacological substances that act on the adrenergic system. Among these, β2-adrenergic agonists are employed for their metabolic effects and their role in increasing endurance, whereas β-adrenergic antagonists are used in precision sports to reduce tremor and control anxiety. Both classes of substances present potential benefits as well as health risks, and are subject to strict regulations in high-performance sports.