ATC Group: R03AK10 Vilanterol and fluticasone furoate

Vilanterol is a selective long-acting, beta₂-adrenergic agonist (LABA). The pharmacologic effects of beta₂-adrenoceptor agonist active substances, including vilanterol, are at least in part attributable to stimulation of intracellular adenylate cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

Fluticasone furoate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. Vilanterol trifenatate is a selective long-acting, beta₂-adrenergic agonist (LABA). Molecular interactions occur between corticosteroids and LABAs, whereby steroids activate the beta₂-receptor gene, increasing receptor number and sensitivity and LABAs prime the glucocorticoid receptor for steroid-dependent activation and enhance cell nuclear translocation.