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Chronic obstructive pulmonary disease (COPD) is a disease state characterized by the progressive development of airflow limitation that is not fully reversible. The airflow limitation is associated with an abnormal inflammatory response of the lungs to noxious particles or gases. It affects approximately 15 million Americans and is associated with high morbidity and mortality. Previously, pharmacologic therapeutic options were limited by relatively short durations of action in the first-line medications and limited efficacy data and/or a high rate of adverse effects in the second-line medications. Today, there are several new and emerging medications to treat this disease state, and new guidelines have been published for disease management. This review examines current therapeutic options, compares efficacy data, and highlights the recommendations from international guidelines.