Treatment of bronchial asthma in patients who use inhaled corticosteroids or require treatment with long-acting β2 agonists. To reduce the symptoms of airway obstruction in patients with chronic obstructive pulmonary disease (COPD) who need treatment with long-acting β2 agonists.
active substance: formoterol;
1 dose coming out of the mouthpiece contains 12 μg of formoterol fumarate dihydrate;
Powder for inhalation.
Main physical and chemical properties:
white or yellowish-white powder.
Selective β2-adrenoceptor agonists. ATX code R03A C13.
Mechanism of action. It is a selective stimulant of β2-adrenoceptors. In patients with reversible airway obstruction, it has a bronchodilator effect. This effect develops rapidly (within 1-3 minutes) and remains quite pronounced 12 hours after inhalation of the drug.
Absorption. As with other inhalations, there is a high probability that about 80% of formoterol administered through the Easyhaler inhaler is swallowed and then absorbed in the gastrointestinal tract. Therefore, data on the pharmacokinetic properties of oral dosage forms are largely applicable to inhaled powder. After inhalation of therapeutic doses of the drug formoterol is not detected in plasma using existing analytical methods.
Absorption occurs rapidly and extensively: at doses exceeding therapeutic (120 μg), the maximum concentration of the drug in plasma is observed 5 minutes after inhalation, while when ingested 80 μg dose with a radiolabel is absorbed at least 65%, and the drug is taken orally in doses up to 300 mcg it is accompanied by its fast absorption with achievement of the maximum concentration of unchanged formoterol fumarate within 0,5–1 hours. In patients with chronic obstructive pulmonary disease (COPD) treated for 12 weeks with formoterol fumarate 12 or 24 mcg twice daily, plasma concentrations of formoterol were in the range of 11.5–25.7 pmol / L and 23.3 -50.3 pmol / l, respectively, 10 minutes, 2 hours and 6 hours after inhalation.
The pharmacokinetics of formoterol in the dose range from 20 to 300 mcg is linear. No significant accumulation of the drug was detected during repeated oral administration at a dose of 40–160 μg / day. The maximum rate of excretion after administration of 12-96 mcg is reached within 1-2 hours after inhalation.
After 12 weeks of taking 12 mcg or 24 mcg of formoterol powder twice daily, urinary excretion of formoterol in unchanged form increases by 63–73% in adults and by 18–84% in children, indicating moderate and self-limiting accumulation of formoterol in plasma. after repeated administration of the drug.
Treatment of bronchial asthma in patients who use inhaled corticosteroids or who require treatment with long-acting β2-agonists.
To reduce the symptoms of airway obstruction in patients with chronic obstructive pulmonary disease (COPD) who require treatment with long-acting β2-agonists.
Hypersensitivity to formoterol fumarate or lactose monohydrate (contains a small amount of milk protein). Hypersensitivity to other β2-adrenergic stimulants.
Tachyarrhythmia, atrioventricular block of the third degree, idiopathic subvalvular aortic stenosis, hypertrophic obstructive cardiomyopathy, thyrotoxicosis.
Suspected or established prolongation of the QT interval (QTc> 0.44 s).