Indacaterol for COPD – RGH E-Bulletin

Indacaterol is an ultra-long-acting β-2 adrenergic agonist which can be administered once daily for the treatment of Chronic Obstructive Pulmonary Disease (COPD). In Australia, indacaterol has recently been listed for subsidized supply under the auspices of the Pharmaceutical Benefits Schedule (for this indication only).

The pharmacological effects of β-2 adrenoreceptor agonists can be partly credited to the intracellular stimulation of adenyl cyclase. This enzyme catalyzes the conversion of adenosine tri phosphate (ATP) to cyclic 3’,5 adenosine monophosphate. These raised cyclic AMP levels cause relaxation of bronchial smooth muscle. In vitro studies have shown that indacaterol has more than a 24-fold greater agonist activity at β-2 receptors compared to β-1 receptors, and a 20-fold greater agonist activity compared to β-3 receptors. This degree of selectivity is similar to that observed with eformoterol.

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