Objective To discuss the effectiveness of salmeterol in treating a case of chronic obstructive pulmonary disease (COPD). Methods Aimed at the effectiveness of salmeterol in treating COPD patients, a comprehensive search was conducted in EMbase Web (2007 to 2011) and EBSCOhost Web (2000 to 2010) to obtain and evaluate the relevant systematic reviews, meta-analysis and randomized controlled trials (RCTs), and finally to apply the best evidence in clinical practice. Results There were 2 systematic reviews, 3 meta-analyses and 172 RCTs in the initial retrieval; and 12 RCTs and 1 meta-analysis were finally included after being screened. The results indicated a significant improvement in lung function, clinical symptoms and life quality after inhalation of sameterol in COPD patients. The patient had a good effect when the above evidence was applied at the patient’s will. Conclusion The inhalation of salmeterol for COPD can significantly improve lung function, alleviate clinic symptoms and improve life quality of the patients. But there are still some side-effects which should be considered in practical applications.