Formoterol
Encyclopedia
Formoterol or eformoterol (former BAN
) is a long-acting β2-agonist used in the management of asthma
and/or chronic obstructive pulmonary disease
(COPD). It is marketed in four forms: a dry-powder inhaler (DPI), a metered-dose inhaler (MDI), an oral tablet, and an inhalation solution, under various trade names including Foradil/Foradile (Schering-Plough
in the U.S., Novartis
rest of world), Oxeze/Oxis (AstraZeneca
), Atock (Astellas
), Atimos (Modulite) (Chiesi), and Perforomist (Dey).
Formoterol is a long-acting β2 agonist (LABA) that has an extended duration of action (up to 12 hours) compared to short-acting β2 agonists such as salbutamol
, which are effective for 4–6 hours. LABAs such as formoterol are used as "symptom controllers" to supplement prophylactic corticosteroid
therapy (e.g., fluticasone
). A "reliever" short-acting β2 agonist (e.g., salbutamol
) is still required, since LABAs are not recommended for the treatment of acute asthma.
s. Formoterol has been demonstrated to have a faster onset of action than salmeterol
as a result of lower lipophilicity, and has also been demonstrated to be more potent - a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.
released a health advisory alerting the public to findings that show the use of long-acting β2-agonists could lead to a worsening of wheezing symptoms in some patients.
At the current time, available long-acting β2-agonists
include salmeterol
, formoterol, bambuterol
, and sustained-release oral salbutamol
. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread – combination preparations include fluticasone/salmeterol
and budesonide/formoterol
.
British Approved Name
A British Approved Name is the official non-proprietary or generic name given to a pharmaceutical substance, as defined in the British Pharmacopoeia...
) is a long-acting β2-agonist used in the management of asthma
Asthma
Asthma is the common chronic inflammatory disease of the airways characterized by variable and recurring symptoms, reversible airflow obstruction, and bronchospasm. Symptoms include wheezing, coughing, chest tightness, and shortness of breath...
and/or chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease , also known as chronic obstructive lung disease , chronic obstructive airway disease , chronic airflow limitation and chronic obstructive respiratory disease , is the co-occurrence of chronic bronchitis and emphysema, a pair of commonly co-existing diseases...
(COPD). It is marketed in four forms: a dry-powder inhaler (DPI), a metered-dose inhaler (MDI), an oral tablet, and an inhalation solution, under various trade names including Foradil/Foradile (Schering-Plough
Schering-Plough
Schering-Plough Corporation was a United States-based pharmaceutical company. It was founded in 1851 by Ernst Christian Friedrich Schering as Schering AG in Germany. In 1971, the Schering Corporation merged with Plough to form Schering-Plough. On November 4, 2009 Merck & Co...
in the U.S., Novartis
Novartis
Novartis International AG is a multinational pharmaceutical company based in Basel, Switzerland, ranking number three in sales among the world-wide industry...
rest of world), Oxeze/Oxis (AstraZeneca
AstraZeneca
AstraZeneca plc is a global pharmaceutical and biologics company headquartered in London, United Kingdom. It is the world's seventh-largest pharmaceutical company measured by revenues and has operations in over 100 countries...
), Atock (Astellas
Astellas Pharma
is a Japanese pharmaceutical company, formed on 1 April 2005 from the merger of and .Astellas' franchise areas are urology, immunology , dermatology, cardiology, and infectious disease...
), Atimos (Modulite) (Chiesi), and Perforomist (Dey).
Formoterol is a long-acting β2 agonist (LABA) that has an extended duration of action (up to 12 hours) compared to short-acting β2 agonists such as salbutamol
Salbutamol
Salbutamol or albuterol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names....
, which are effective for 4–6 hours. LABAs such as formoterol are used as "symptom controllers" to supplement prophylactic corticosteroid
Corticosteroid
Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex. Corticosteroids are involved in a wide range of physiologic systems such as stress response, immune response and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte...
therapy (e.g., fluticasone
Fluticasone
Fluticasone is a synthetic glucocorticoid.Both the furoate and propionate forms are used as topical anti-inflammatories:*Fluticasone propionate*Fluticasone furoateTreatment of asthma - Fluticasone in combination with Salmeterol - "[]" - aerosol....
). A "reliever" short-acting β2 agonist (e.g., salbutamol
Salbutamol
Salbutamol or albuterol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names....
) is still required, since LABAs are not recommended for the treatment of acute asthma.
Mechanism of action
Inhaled formoterol works like other β2-agonists, causing bronchodilation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. The long duration of formoterol action occurs because the formoterol molecules initially diffuse into the plasma membrane of the lung cells, and then are slowly released back outside, where they can come into contact with β2 adrenergic receptorAdrenergic receptor
The adrenergic receptors are a class of metabotropic G protein-coupled receptors that are targets of the catecholamines, especially noradrenaline and adrenaline ....
s. Formoterol has been demonstrated to have a faster onset of action than salmeterol
Salmeterol
Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease. It is currently available as a dry powder inhaler that releases a powdered form of the drug...
as a result of lower lipophilicity, and has also been demonstrated to be more potent - a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.
Safety
In November 2005, the US FDAFood and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
released a health advisory alerting the public to findings that show the use of long-acting β2-agonists could lead to a worsening of wheezing symptoms in some patients.
At the current time, available long-acting β2-agonists
Beta2-adrenergic receptor agonist
β2-adrenergic agonists, also known as β2-adrenergic receptor agonists, are a class of drugs used to treat asthma and other pulmonary disease states.-Uses:...
include salmeterol
Salmeterol
Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease. It is currently available as a dry powder inhaler that releases a powdered form of the drug...
, formoterol, bambuterol
Bambuterol
Bambuterol is a long acting beta-adrenoceptor agonist used in the treatment of asthma; it also is a prodrug of terbutaline. Commercially, the AstraZeneca pharmaceutical company produces and markets bambuterol as Bambec and Oxeol ....
, and sustained-release oral salbutamol
Salbutamol
Salbutamol or albuterol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names....
. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread – combination preparations include fluticasone/salmeterol
Fluticasone/salmeterol
The combination preparation fluticasone/salmeterol is a formulation containing fluticasone propionate and salmeterol xinafoate used in the management of asthma and chronic obstructive pulmonary disease...
and budesonide/formoterol
Budesonide/formoterol
Budesonide/formoterol is a combination formulation containing budesonide and formoterol used in the management of asthma and chronic obstructive pulmonary disease in the EU...
.
See also
- ArformoterolArformoterolArformoterol is a long acting beta-adrenoceptor agonist drug indicated for the treatment of chronic obstructive pulmonary disease . It is sold by Sunovion, under the trade name Brovana, as a solution of arformoterol tartrate to be administered twice daily by nebulization.It is the active...
- Budesonide/formoterolBudesonide/formoterolBudesonide/formoterol is a combination formulation containing budesonide and formoterol used in the management of asthma and chronic obstructive pulmonary disease in the EU...
- Beclomethasone/formoterol