An inhalation aerosol formulation containing budesonide and the fumarate dihydrate salt of formoterol with anti-inflammatory and bronchial smooth muscle-relaxing activities.
The synthetic corticosteroid steroid budesonide binds to intracellular glucocorticosteroid receptors (GRs), exhibiting inhibitory activities against multiple cell types and mediators associated with allergic inflammation.
The long-acting beta-adrenergic receptor agonist formoterol selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP); increased intracellular cAMP result in the relaxation of bronchial smooth muscle and inhibition of the cellular release of mediators of immediate hypersensitivity, especially from mast cells.
Asthma, COPD: per inhalation contains budesonide(mcg)/formoterol fumarate(mcg) 80/4.5 or 160/4.5: 2 inhalations twice daily. Not to use more than 4 inhalations/day of either strength.
Adverse drug reactions: headache, nasopharyngitis, upper respiratory tract infections, stomach discomfort, vomiting, oral candidiasis, back pain, nasal congestion, sinusitis.
Long term inhaled corticosteroids reach systemic circulation via both the pulmonary circulation and the gastro-intestinal tract. Long-term high-dose inhaled corticosteroids have been associated with adrenal suppression.
Indications in palliative care: reversible and irreversible airways obstruction, stridor, lymphangitis carcinomatosa, radiation pneumonitis, cough after insertion of bronchial stent.