General Description
Isoetharine mesylate is a selective beta-2 adrenergic agonist belonging to the catecholamine class, with a structure similar to isoproterenol but with an ethyl substitution on the α-carbon. The mesylate salt improves aqueous stability. The molecule has two hydroxyl groups on the benzene ring (catechol moiety) and a secondary amine group. It is rapidly metabolized by catechol-O-methyltransferase (COMT), limiting its duration of action.
Mechanism of Action
Isoetharine binds to and activates beta-2 adrenergic receptors on bronchial smooth muscle cells, stimulating adenylate cyclase and increasing intracellular cyclic AMP. This leads to relaxation of bronchial smooth muscle, bronchodilation, and inhibition of mast cell mediator release. The drug has minimal beta-1 activity at therapeutic doses, thus causing less cardiac stimulation than isoproterenol. The catechol structure makes it susceptible to rapid inactivation.
Application
Isoetharine was indicated as a bronchodilator for the treatment of asthma, chronic bronchitis, and emphysema, particularly in acute bronchospasm. It was available as an inhalation aerosol and solution for nebulization.