Bitolterol, (3-4 diester colterol) is a new beta 2-adrenergic agonist. Since it in itself is biologically inactive, bitolterol is considered a pro-drug. When administered it is activated within the lung by esterase hydrolysis to the active compound colterol catecholamine N-t-butyl-arterenol). In preclinical and clinical studies to date, bitolterol has proved to be an effective bronchodilator for adult and pediatric patients with chronic stable asthma and for some with chronic obstructive pulmonary disease. Bitolterol has been compared with other beta 2 agents, including isoproterenol, metaproterenol and albuterol. There is no evidence for cardiotoxicity when bitolterol is used in combination with theophylline in human studies. It is effective for control of exercise-induced asthma.

Animals↗

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Exercise-induced asthma.

Though exercise-induced asthma (EIA) has been recognized for centuries, its characteristics, standardized testing, and pharmacologic management have been clarified only in the last two decades. Controversy continues concerning etiology; whether or not cold air, hypertonic and hypotonic bronchial challenges involve the same mechanism(s); and the incidence and clinical significance of late phase reactions. Aerosolized adrenergic agents such as albuterol or terbutaline, when administered prior to exercise, are usually effective in preventing EIA. Theophylline varies in effectiveness from subject-to-subject as does cromolyn sodium. Other agents such as H-1 antihistamines, ipratropium bromide, calcium channel blockers and adrenocorticosteroids are less effective when used alone, but may be useful when used in association with the more potent drugs.

Asthma↗