Index of drugs

Bronchodilatory supportive treatment to relieve symptoms of the disease in adult patients with chronic obstructive pulmonary disease (COPD).

One capsule contains 143 μg of indacaterol maleate, corresponding to 110 μg of indacaterol and 63 μg of glycopyrronium bromide, equivalent to 50 μg of glycopyrronium. 1 delivered dose (the dose that escapes from the mouthpiece of the inhaler) contains 110 μg of indacaterol maleate, equivalent to 85 μg of indacaterol and 54 μg of glycopyrronium bromide, equivalent to 43 μg of glycopyrronium. The preparation contains lactose.

Preparation for inhalation containing a long-acting β-agonist₂-renergic and long-acting muscarinic receptor antagonists. When indacaterol and glycopyrronium are administered simultaneously, the efficacy of both compounds is added due to the different ways of their action directed at different receptors and mechanisms leading to smooth muscle relaxation. Β-receptor agonists₂ they are more effective in relaxing the peripheral airways, while the anticholinergic compound can more effectively affect the central airways. The combination of indacaterol and glycopyrronium shows a rapid onset of action within 5 min after dosing. This effect remains constant throughout the 24-hour dosing period. After inhalation of the preparation, the median time to the maximum plasma concentration of indacaterol and glycopyrronium was approximately 15 min and 5 min, respectively. The absolute bioavailability of indacaterol after inhalation of the preparation is 61-85% of the delivered dose, and the absolute bioavailability of glycopyrronium - about 47% of the delivered dose. Steady state levels of indacaterol were achieved within 12-15 days after administration once daily; in the case of glycopyrronium - within 1 week of starting treatment. The binding of indacaterol to proteins of human serum and plasma is about 95%, glycopyrronium - 38-41%. UGT1A1 is the major isoform that metabolizes indacaterol; CYP3A4 is the dominant isoenzyme responsible for the hydroxylation of indacaterol. Numerous CYP isoenzymes participate in the oxidative transformation of glycopyrronium. The concentration of indacaterol in the blood serum decreases in a multiphase with the mean end T_0,5 45.5-126 h; effective T_0,5, calculated on the basis of the accumulation of indacaterol after repeated administration is 40-52 h. Plasma glycopyrronium concentrations decreased in multiphase; average T_0,5 in the final phase is 33-57 h.

Hypersensitivity to the active substances or to any of the excipients.

The preparation should not be used to treat asthma due to the lack of data in this indication (long-acting β-receptor agonists₂-adrenergic agents may increase the risk of serious adverse events associated with asthma). The preparation is not indicated for the treatment of acute bronchospasm. In case of symptoms of allergic reactions or paradoxical bronchoconstriction, treatment should be discontinued immediately and alternative therapy should be applied. Caution should be exercised in patients with narrow-angle glaucoma and in patients with urinary retention (data not available). In case of signs or symptoms of acute narrow-angle glaucoma, treatment with the preparation should be discontinued. In patients with severe renal impairment (calculated glomerular filtration rate below 30 ml / min / 1.73 m² pc.), including patients with end-stage renal disease requiring dialysis, the preparation should only be used if the expected benefit outweighs the potential risk. These patients should be closely monitored for adverse reactions. Caution should be exercised in patients with severe hepatic impairment (no data). Caution should be exercised when using the drug in patients with cardiovascular disease (coronary heart disease, acute myocardial infarction, arrhythmias, hypertension).If clinically significant effects on the cardiovascular system occur (increased heart rate, blood pressure and / or other symptoms), it may be necessary to stop treatment. Caution should be exercised when using long-acting β-receptor agonists₂-adrenergic in patients who have or may have QT prolongation and in patients who are taking medicines that affect the QT interval. Caution should be exercised in patients with unstable ischemic heart disease, left ventricular failure, a history of myocardial infarction, arrhythmias (other than chronic, stable atrial fibrillation), a history of QT prolonged QTc or patients in whom QTc (determined by the Frideric method) was prolonged (> 450 ms) - lack of experience regarding the use of the drug in these patient groups. Β-receptor agonists₂-adrenergic agents may cause clinically significant hypokalemia; in patients with severe COPD, hypoxia and concomitant medication may increase hypokalaemia, which may increase susceptibility to arrhythmias. Because of the risk of increased blood Glucose levels after starting treatment with diabetic patients, the plasma glucose should be monitored even more closely. The preparation has not been studied in patients with inadequately controlled diabetes. Caution should be exercised in patients with seizures or thyrotoxicosis, and in patients who are very sensitive to β-receptor agonists.₂adrenergic. Use of the preparation in children and adolescents under 18 years of age in the indication of COPD is not appropriate; the safety and efficacy of the medicine in children has not been determined. The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

The preparation can be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus. Indacaterol may inhibit labor by virtue of a relaxant effect on the uterine smooth muscle. It is not known whether indacaterol, glycopyrronium and their metabolites are excreted in human milk. Use of the preparation in breastfeeding women should only be considered if the expected benefit to a woman outweighs the possible risk to the child.

Very common: upper respiratory tract infection. Common: pharyngitis, urinary tract infection, sinusitis, rhinitis, headache and dizziness, cough, mouth and throat pain (including throat irritation), indigestion, tooth decay, gastroenteritis, musculoskeletal pain, fever, chest pain. Uncommon: hypersensitivity, angioedema, diabetes and hyperglycemia, insomnia, paresthesia, glaucoma, ischemic heart disease, atrial fibrillation, tachycardia, palpitations, paradoxical bronchospasm, epistaxis, dry mouth, pruritus, rash, muscle spasms , muscle pain, limb pain, bladder obstruction and urinary retention, peripheral edema, fatigue.

Inhalation. Adults: the recommended dose is inhalation of 1 capsule once daily with the Ultibro Breezhaler inhaler. It is recommended that the preparation be administered at the same time each day. If you miss a dose, take it as soon as possible on the same day. Do not take more than 1 dose a day. It can be used at the recommended doses in elderly patients (aged 75 years and over), in patients with mild to moderate renal impairment and in patients with mild to moderate hepatic impairment. In patients with severe renal impairment or end-stage renal disease requiring dialysis, it should be used only if the expected benefit outweighs the potential risk and care should be taken in patients with severe hepatic impairment.