Inhaled beta -adrenoceptor agonists (beta -agonists) are among the most used substances in competitive sports. The 2019 Prohibited List issued by the World Anti-Doping Agency, restricts use of all selective and non-selective beta -agonists in and out competition with few exemptions. Formoterol, salbutamol and salmeterol are allowed by inhalation within defined dosing limits. These restrictions are in place because supratherapeutic use of beta -agonist has the potential to be anabolic and enhance performance, as well as due to potential side effects. However, despite substantial documentation that beta -agonists exert anabolic and lipolytic actions, these actions are not widely recognised. Furthermore, a common misconception is that the inhaled route does not exert these effects. However, given the high relative systemic bioavailability of the inhaled route, it is likely that inhalation at high doses exerts anabolic and lipolytic actions. In this review, we highlight that beta -agonists can exert anabolic and lipolytic actions, regardless of type of beta -agonist and route of administration. However, the doses needed to provide such effects are also associated with adverse effects and would in most cases be detected in routine doping control. Notwithstanding, the beta -agonist regulations are associated with some challenges and given their ability to induce muscle growth and enhance performance, it is important to continue developing effective detection strategies to lessen potential misuse of beta -agonists and allow treatment of asthmatic subjects without causing adverse side effects or ergogenic actions.
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