Formoterol fumarate

Description

Formoterol fumarate is a β2-selective adrenergic agonist useful in the treatment of bronchial asthma. It s potency and duration of action a r e reported to exceed those of salbutamol, as is its ability to inhibit allergic and non-allergic histamine release.

Chemical Properties

Crystalline Solid

Originator

Yarnanouchi (Japan)

Uses

Formoterol fumarate is a potent β2-AR agonist.

Uses

long-acting β 2-agonist, anti-asthmatic

Uses

A selective 2-adrenergic receptor agonist. Used as an antiasthmatic

Uses

antiasthmatic;2-agonist

Definition

ChEBI: (S,S)-formoterol fumarate is a fumarate salt prepared from (S,S)-formoterol by reaction of one molecule of fumaric acid for every two molecules of (S,S)-formoterol. It contains a (S,S)-formoterol(1+). It is an enantiomer of an arformoterol fumarate.

brand name

Foradil (Novartis);ATOCK.

Mechanism of action

This is believed to result from formoterol's greater water solubility, allowing it to get to the receptor sites faster, whereas its moderate lipophilicity keeps it in the lungs longer. It is indicated for the long-term maintenance treatment of asthma and for patients with symptoms of nocturnal asthma who require regular treatment with inhaled, short-acting, β2-agonists. It is not indicated for patients whose asthma can be managed by occasional use of inhaled, short-acting, β2-agonists. Formoterol is available only as a powder in a capsule for administration via the aerosolizer. Patients should be cautioned not to take the capsules orally and to keep them in a safe place to avoid accidental oral administration.

Clinical Use

Formoterol has a β-directing N-isopropyl-p-methoxyphenyl group and a unique m-formamide and p-hydroxyphenyl ring, which provides selectivity for β2-receptors. It is resistant to MAO and COMT, making it a long-acting agonist. Formoterol has a more rapid onset as compared to salmeterol while maintaining the same long duration of action.

storage

Store at RT

References

[1] ANDERSON G P. Formoterol: Pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilator[J]. Life sciences, 1993, 52 26: Pages 2145-2160. DOI:10.1016/0024-3205(93)90729-m
[2] XIN TENG . Structure–activity relationship study of novel necroptosis inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2005, 15 22: Pages 5039-5044. DOI:10.1016/j.bmcl.2005.07.077
[3] TORU NOGUCHI . Effect of beta2-adrenergic agonists on eosinophil adhesion, superoxide anion generation, and degranulation[J]. Allergology International, 2015, 64: Pages S46-S53. DOI:10.1016/j.alit.2015.05.009
[4] SÍLVIA BUSQUETS. Anticachectic effects of formoterol: a drug for potential treatment of muscle wasting.[J]. Cancer research, 2004, 64 18: 6725-6731. DOI:10.1158/0008-5472.can-04-0425
[5] EOIN O’NEILL. Pharmacological targeting of β2-adrenoceptors is neuroprotective in the LPS inflammatory rat model of Parkinson’s disease[J]. British Journal of Pharmacology, 2019, 177 2: 282-297. DOI:10.1111/bph.14862