Formoterol
生产企业：Novartis pharmaceuticals corp, Dey pharma lp
Formoterol is an inhaled long-acting beta2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD.
Formoterol is an inhaled long-acting beta2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD.
Formoterol is a relatively selective long-acting agonist of beta-adrenergic receptors, although it does carry some degree of activity at beta and beta receptors. Beta receptors are found predominantly in bronchial smooth muscle (with a relatively minor amount found in cardiac tissue) whereas beta receptors are the predominant adrenergic receptors found in the heart - for this reason, selectivity for beta receptors is desirable in the treatment of pulmonary diseases such as COPD and asthma. Formoterol has demonstrated an approximately 200-fold greater activity at beta receptors over beta receptors. On a molecular level, activation of beta receptors by agonists like formoterol stimulates intracellular adenylyl cyclase, an enzyme responsible for the conversion of ATP to cyclic AMP (cAMP). The increased levels of cAMP in bronchial smooth muscle tissue result in relaxation of these muscles and subsequent dilation of the airways, as well as inhibition of the release of hypersensitivity mediators (e.g. histamine, leukotrienes) from culprit cells, especially mast cells.
Formoterol is indicated in various formulations for the treatment of asthma and COPD. For the treatment of COPD, formoterol is available as a single-entity inhalation solution, in combination with the long-acting muscarinic antagonists (LAMAs) aclidinium and glycopyrronium, and in combination with the corticosteroid budesonide. For the treatment of asthma, formoterol is available in combination with mometasone furoate for patients 5 years and older and with budesonide for patients 6 years and older. Formoterol may also be used on an as-needed basis for prophylaxis against exercise-induced bronchospasm.
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