Puneet Varma (Editor)

Formoterol

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Trade names
  
See below

ATC code
  
R03AC13 (WHO)

CAS ID
  
73573-87-2

AHFS/Drugs.com
  
Monograph

Molar mass
  
344.405 g/mol

Formoterol

Pregnancy category
  
AU: B3 US: C (Risk not ruled out)

Routes of administration
  
Inhalation (capsules for oral inhalation, DPI, MDI)

Legal status
  
UK: POM (Prescription only) US: ℞-only In general: ℞ (Prescription only)

Budesonide formoterol symbicort get the facts save


Formoterol (INN) or eformoterol (former BAN) is a long-acting β2 agonist (LABA) used in the management of asthma and COPD. It is marketed in three forms: a dry-powder inhaler, a metered-dose inhaler and an inhalation solution, under various trade names including Atock, Atimos/Atimos Modulite, Foradil/Foradile, Oxeze/Oxis, and Perforomist. It is also marketed in the combination formulations budesonide/formoterol and mometasone/formoterol.

Contents

Formoterol has an extended duration of action (up to 12 hours) compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4–6 hours. LABAs such as formoterol are used as "symptom controllers" to supplement prophylactic corticosteroid therapy. A "reliever" short-acting β2 agonist (e.g., salbutamol) is still required, since LABAs are not recommended for the treatment of acute asthma.

How to use symbicort turbuhaler inhaler technique


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.

Safety

In November 2005, the US FDA 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.

β2 agonists in treatment of obesity

β2 agonists increase energy utilization and fat metabolism, however, therapeutic use for obesity has been limited by the concomitant activation of β1 receptors resulting in excessive increases in heart rate. A recent 2012 dose-finding study (in healthy men) demonstrated significantly increased resting energy expenditure, and fat oxidation at a dose of 160 μg of formoterol per day without significantly increased heart rate. Formoterol's specificity for the β2 receptor (relative to β1 receptors) may facilitate its use for this purpose. A combination of a highly selective β2 agonist like formeterol with a low dose highly selective β1 blocker may further improve the differential therapeutic ability to selectively agonize β2 receptors for metabolic benefits in treating obesity without adverse β1 agonist effects.

Stimulation of mitochondrial biogenesis

Formoterol may also help stimulate mitochondrial biogenesis. Mitochondrial dysfunction is related to many degenerative diseases — particularly neurodegenerative disorders.

Treatment for Down syndrome

Preliminary research offers hope that formoterol may be a useful treatment in Down syndrome. In a mouse model of the disease, the drug strengthened nerve connections in the hippocampus, a brain center used for spatial navigation, paying attention and forming new memories.

Trade names

  • Foradil/Foradile capsules for oral inhalation (Schering-Plough in the U.S., Novartis rest of world)
  • Oxeze/Oxis Turbuhaler DPI (AstraZeneca)
  • Atock (Astellas)
  • Atimos/Atimos Modulite MDI (Chiesi)
  • Perforomist inhalation solution (Mylan N.V.)
  • References

    Formoterol Wikipedia


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