NCIt definition : A diester sympathomimetic amine with bronchodilator activity. As an ester prodrug,
bitolterol is hydrolyzed by esterases to its active metabolite colterol (N-t-butylarterenol).
Colterol selectively binds to and activates beta-2 adrenergic receptors in bronchiolar
smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes
the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate
(cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle.
This increases air flow and prevents bronchospasms and may eventually lead to an improvement
of airway function.;