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Long-acting bronchiodilator

Formoterol

Formoterol
All data from the card 26
Trade names
Oxeze, Foradil, Symbicort, others
AHFS/Drugs.com
Monograph
License data
EU EMA: by formoterol fumarate dihydrate
Pregnancycategory
AU: B3
Routes ofadministration
Inhalation (capsules for oral inhalation, DPI, MDI)
ATC code
R03AC13 (WHO) R03CC15 (WHO)
Legal status
AU: S4 (Prescription only) NZ: Prescription only UK: POM (Prescription only) US: ℞-only EU: Rx-only In general: ℞ (Prescription only)
Protein binding
61% to 64%
Metabolism
Liver demethylation and glucuronidation (CYP2D6, CYP2C19, CYP2C9 and CYP2A6 involved)
Elimination half-life
10 h
Excretion
Kidney and fecal
CAS Number
73573-87-2
PubChem CID
30835443034756
IUPHAR/BPS
3465
DrugBank
DB00983
ChemSpider
2340731
UNII
5ZZ84GCW8B
KEGG
D07990
ChEBI
CHEBI:408174
ChEMBL
ChEMBL1363
CompTox Dashboard (EPA)
DTXSID20860603 DTXSID1023077, DTXSID20860603
ECHA InfoCard
100.131.654
Formula
C19H24N2O4
Molar mass
344.411 g·mol−1
3D model (JSmol)
Interactive image
Chirality
Racemic mixture

Formoterol, also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action (up to 12 h) compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4 h to 6 h. Formoterol has a relatively rapid onset of action compared to other LABAs, and is effective within 2-3 minutes. The 2022 Global Initiative for Asthma report recommends a combination formoterol/inhaled corticosteroid inhaler as both a preventer and reliever treatment for asthma in adults. In children, a short-acting β2 adrenergic agonist (e.g., salbutamol) is still recommended.

It was patented in 1972 and came into medical use in 1998. It is available as a generic medication. It is also marketed in the combination formulations budesonide/formoterol and mometasone/formoterol.

Side effects

In November 2005, the US Food and Drug Administration (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.

Nowadays, 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.

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. It has also been reported to target tubulin, favorizing its polymerization.

Society and culture

Inhaler for a powder based in budesonide and formoterol
Inhaler for a powder based in budesonide and formoterol

Brand names

Formoterol is marketed in three forms: a dry-powder inhaler (DPI), a metered-dose inhaler (MDI) and an inhalation solution, under various brand names including Atock, Atimos/Atimos Modulite, Foradil/Foradile, Fostair, Oxeze/Oxis, Perforomist and Symbicort.

In some countries, Perforomist is marketed by Viatris after Upjohn merged with Mylan to create Viatris.

Uses and combinations

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Text from Wikipedia, CC BY-SA 4.0 · Source article