Salmeterol xinafoate is a potent and highly selective beta 2-adrenoreceptor agonist with a duration of action greater than 12 hours. When inhaled twice daily in the management of chronic asthma, it results in improved lung function, reduces acute asthmatic exacerbations, and improves the patient's quality of life. This agent has shown particular benefit for patients who continue to have symptomatic asthma despite the regular use of inhaled corticosteroid therapy and the frequent use of a short-acting beta 2-agonist. Although there is some evidence that salmeterol induces some tolerance to the bronchoprotective effect of beta 2-agonist therapy, improvement in lung function and asthma symptoms scores, during both the daytime and nighttime, are sustained. Importantly, patients must be educated in the proper use of salmeterol; for many asthmatics, this medication should be administered with inhaled or oral corticosteroid therapy, and salmeterol should not be used for rescue bronchodilation. When used properly, salmeterol is an effective and safe adjunctive therapy in the management of chronic asthma in adolescents and adults.