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Formoterol: Wikis

  

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1 : 1 mixture (racemate)
Systematic (IUPAC) name
(RS,SR)-N-[2-hydroxy-5-[1-hydroxy-2-[1-(4-methoxyphenyl) propan-2-ylamino]ethyl] phenyl]formamide
Identifiers
CAS number 73573-87-2
ATC code R03AC13
PubChem 3410
DrugBank APRD00641
Chemical data
Formula C19H24N2O4 
Mol. mass 344.405 g/mol
Pharmacokinetic data
Protein binding 61–64%
Metabolism Hepatic demethylation and glucuronidation (CYP2D6, CYP2C19, CYP2C9 and CYP2A6 involved)
Half life 10 hours
Excretion Renal and fecal
Therapeutic considerations
Pregnancy cat. B3(AU) C(US)
Legal status POM (UK) -only (US)
Routes Oral, Inhalation
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Formoterol (INN) 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), metered dose inhaler (MDI), an oral tablet, and as an inhalation solution, under various trade names including Foradil/Foradile (Schering-Plough in the U.S., Novartis rest of world), Oxeze (AstraZeneca), Atock (Astellas), Atimos Modulite (Trinity-Chiesi) and Perforomist (Dey).

Formoterol is a long-acting β2 agonist (LABA), which 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.

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 receptors. 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.

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.

Currently 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.

See also









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