arrow

From NeuroLex

Jump to: navigation, search



Formoterol

Name: Formoterol
Description: Formoterol is a long-acting beta2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD). Inhaled formoterol works like other beta2-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. Pharmacology: Formoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than 200-fold greater agonist activity at beta2-receptors than at beta1- receptors. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10%-50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2- agonists may have cardiac effects. Mechanism of action: The pharmacologic effects of beta2-adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl 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. In vitro tests show that formoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Formoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown. Drug type: Approved. Investigational. Small Molecule. Drug category: Adrenergic beta-Agonists. Bronchodilator Agents. Sympathomimetic
Synonym(s): Formoterol fumarate, Formoterolum (INN-Latin), formoterol, Foradil, Foradile, Oxeze Turbuhaler, Oxeze Turbuhaler Foradil, Oxis
Related to: Beta-2 adrenergic receptor
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00983
Id: DB00983
Link to OWL / RDF: Download this content as OWL/RDF


Contributors

Ccdbuser, Nifbot2



bookmark
Facts about FormoterolRDF feed
Commenttaken from DrugBank
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00983  +
DefinitionFormoterol is a long-acting beta2-agonist Formoterol is a long-acting beta2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD). Inhaled formoterol works like other beta2-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. Pharmacology: Formoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than 200-fold greater agonist activity at beta2-receptors than at beta1- receptors. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10%-50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2- agonists may have cardiac effects. Mechanism of action: The pharmacologic effects of beta2-adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl 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. In vitro tests show that formoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Formoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown. Drug type: Approved. Investigational. Small Molecule. Drug category: Adrenergic beta-Agonists. Bronchodilator Agents. Sympathomimetic ts. Bronchodilator Agents. Sympathomimetic
Has roleDrug  +
IdDB00983  +
LabelFormoterol  +
ModifiedDate14 April 2014  +
RelatedToBeta-2 adrenergic receptor  +
SuperCategoryMolecular entity  +
SynonymFormoterol fumarate  +, Formoterolum (INN-Latin)  +, formoterol  +, Foradil  +, Foradile  +, Oxeze Turbuhaler  +, Oxeze Turbuhaler Foradil  +, and Oxis  +