![]() ![]() ![]() Pharmacodynamic effects: In one placebo controlled clinical efficacy study Vilanterol + Umeclidinium (Anoro Ellipta) increased FEV 1 after the first dose on Day 1 with an improvement compared with placebo of 0.11 L (p120%) in two replicate, 12-week clinical studies. 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. The pharmacologic effects of beta 2-agonists, 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). Vilanterol: Vilanterol is a selective long-acting, beta 2-adrenergic receptor agonist (beta 2-agonist). It demonstrates slow reversibility at the human M3 muscarinic receptor subtype in vitro and a long duration of action in vivo when administered directly to the lungs in pre-clinical models. Umeclidinium exerts its bronchodilatory activity by competitively inhibiting the binding of acetylcholine with muscarinic acetylcholine receptors on airway smooth muscle. ![]() It is a quinuclidine derivative that is a muscarinic receptor antagonist with activity across multiple muscarinic cholinergic receptor subtypes. Umeclidinium: Umeclidinium is a long acting muscarinic receptor antagonist (also referred to as an anticholinergic). Following inhalation both compounds act locally on airways to produce bronchodilation by separate mechanisms. Pharmacology: Pharmacodynamics: Mechanism of Action: Umeclidinium/vilanterol is a combination inhaled long-acting muscarinic receptor antagonist/long-acting beta 2-adrenergic agonist (LAMA/LABA). Bronchodilation (Long-acting muscarinic receptor antagonist/Long-acting beta 2 adrenergic agonist combination). ![]()
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