beta(2)-Adrenergic agonists (beta(2)AA) produce myriad effects throughout the human body. Prescribed concurrently with theophylline for the bronchodilatory effects they offer in the treatment of asthma and chronic obstructive pulmonary disease, beta(2)AA actions include many beneficial and adverse changes when administered to animals at supraphysiological doses. Beneficial changes include improved musculoskeletal health and function, which can be maintained because adverse changes are reduced if oral beta(2)AA are given at therapeutic dosages in humans with concurrent resistive exercise administration. Combined oral beta(2)AA-resistive exercise treatments have been shown to produce gains in musculoskeletal health and function in numerous healthy and disuse atrophy human models. The mechanism(s) by which beta(2)AA exert their effects are a function of multiple factors, not the least of which includes the type of model receiving the drug treatment. Combined oral beta(2)AA-resistive exercise treatments in humans showed that adverse effects were greatly reduced when prudent and safer drug administration practices were employed (eg, screening subjects for tolerance before drug treatment). Results from human research trials suggest that administration of the combined treatment improves musculoskeletal function and performance with minimal health risk if proper precautions are followed. A related issue is administration of the combined treatment as an ergogenic aid to athletic performance. Given the results presented in this article, physicians should be wary of potential drug abuse and administer beta(2)AA only under appropriate circumstances when such a treatment is warranted.