Budesonide/Glycopyrrolate/Formoterol Inhalation Aerosol

**Semantic type:** Pharmacologic Substance

**Definition:** A pressurized metered dose inhaler formulation containing a fixed combination of the anti-inflammatory agent and synthetic corticosteroid budesonide, the synthetic quaternary ammonium bromide salt and anticholinergic agent glycopyrrolate, and the fumarate dihydrate salt form of formoterol, a long-acting beta-2-adrenergic agonist and bronchodilator, with anti-inflammatory, anti-spasmodic, and bronchial smooth muscle-relaxing activities. Upon oral inhalation of the budesonide/glycopyrrolate/formoterol inhalation aerosol, budesonide targets and binds to intracellular glucocorticoid receptors (GRs), thereby exhibiting inhibitory activities against multiple cell types and mediators associated with both allergic-mediated and non-allergic-mediated inflammation. Glycopyrronium (R,S-enantiomer), the active moiety in glycopyrrolate, competitively binds to M3 muscarinic receptors located on smooth muscle cells, thereby inhibiting cholinergic transmission. This causes smooth muscle relaxation and prevents the occurrence of painful bronchospasms. Formoterol selectively targets and binds to beta-2-adrenergic receptors in bronchial smooth muscle, thereby activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels result in the relaxation of bronchial smooth muscle, relieve bronchospasms, and inhibit cellular release of mediators of immediate hypersensitivity, especially from mast cells.

**Synonyms:** - Breztri - Breztri - Breztri (TM) Aerosphere - Budesonide/Glycopyrrolate/Formoterol Fumarate Inhalation Aerosol