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**Bitolterol** is a synthetic **small molecule bronchodilator**, classified as a **beta-2-adrenergic receptor agonist**. It acts as a prodrug, metabolized to colterol in the lungs, where it selectively stimulates beta-2 adrenergic receptors on airway smooth muscle, causing muscle relaxation and bronchodilation. Its primary clinical use was for the treatment and maintenance of symptoms in **asthma** and **chronic obstructive pulmonary disease (COPD)**, relieving bronchospasm and assisting airflow. Bitolterol has a rapid onset (2–5 minutes) and a duration of action of 6–8 hours. It does not actively reduce underlying inflammation. Developed in the early 1980s, bitolterol was withdrawn from market in 2001 due to the availability of other agents and limited use[1][3][4][6][7].
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