Index of drugs

Asthma (dose 92 μg + 22 μg and 184 μg + 22 μg). Systematic treatment of asthma in adults and adolescents aged ≥12 years, when simultaneous use of long-acting β is recommended₂-mimetic and inhaled corticosteroid: in patients with inadequate asthma control despite inhaled corticosteroids and short-acting β₂-mimetic, used temporarily.COPD (only 92 μg + 22 μg). Symptomatic treatment of adult COPD patients with FEV1 <70% due (after administration of the bronchodilator), with exacerbations in the past despite regular treatment with bronchodilators.

Each single inhalation provides a dose delivery (dose exiting the mouthpiece) containing 92 μg or 184 μg of fluticasone furoate and 22 μg of vilanterol (as triphenylacetate); the preparation contains lactose.

Fluticasone furoate is a synthetic, three-fluorinated corticosteroid with a strong anti-inflammatory effect. The exact mechanism of action of fluticasone furoate on the symptoms of asthma and COPD is unknown. Corticosteroids have been shown to have a wide range of activities on many types of cells (e.g., eosinophils, macrophages, lymphocytes) and mediators (e.g., cytokines and chemokines involved in the inflammatory response). The vilanterol triphenylacetate is a selective, long-acting β-receptor agonist₂ (LABA). Stimulates intracellular adenylate cyclase - an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine-3 ', 5'-monophosphate (cyclic AMP). Increased concentration of cyclic AMP causes relaxation of bronchial smooth muscles and inhibition of release of mediators of the early phase of allergic reaction from cells, especially from mast cells. Between corticosteroids and long-acting β-receptor agonists₂ there are interactions at the molecular level, as a result of which the steroids activate the β receptor gene₂, increasing the sensitivity and number of receptors, and long-acting β₂-mimetic activates the glucocorticoid receptor for further activation in the presence of the steroid, and enhances translocation to the cell nucleus. These synergistic interactions are reflected in increased anti-inflammatory effects as demonstratedin vitro and in vivo for various inflammatory cells associated with the pathophysiology of both asthma and COPD. The absolute oral bioavailability of fluticasone and vilanterol furoate after inhalation is 15.2% and 27.3%, respectively. Given the low oral bioavailability (1.26% and <2%, for fluticasone and vilanterol furoate respectively), systemic exposure to fluticasone and vilanterol is primarily dependent on the inhaled part of the dose delivered to the lungs after inhalation. The metabolism of both fluticasone furoate and vilanterol is mainly mediated by CYP3A4. Fluticasone furoate is metabolized mainly by hydrolysis of the S-fluoromethylcarbothiol group to metabolites with significantly reduced corticosteroid activity. Wilanterol is mainly metabolised by O-dealkylation to a number of metabolites with significantly reduced agonist activity relative to β-receptors₁ and β₂. Fluticasone fluroate is excreted almost exclusively in faeces, in the form of metabolites. Wilanterol is excreted in urine (70%) and faeces (30%) in the form of metabolites.

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

Do not use to treat acute asthma symptoms or exacerbate COPD. For this purpose, it is necessary to use a short-acting bronchodilator. Increasing the frequency of use of short-acting bronchodilators to relieve symptoms is indicative of worsening disease control and then treatment should be reviewed. After taking the drug, paradoxical bronchospasm may occur with a sudden worsening of wheezing; you should immediately use a short-acting inhaler bronchodilator; should immediately stop the administration of fluticasone furoate and vilanterol, assess the patient's condition and, if necessary, use other treatment.Use with caution in patients with severe cardiovascular disease or cardiac arrhythmias, hyperthyroidism, uncorrected hypokalaemia, or in patients prone to low levels of potassium ions in the blood (there is a risk of arrhythmias due to the content of vilanterol). Caution should be exercised when using the drug in patients with hepatic impairment due to increased systemic exposure to fluticasone furoate (both C_max and AUC); Patients should be monitored for systemic side effects of corticosteroids. Systemic effects of corticosteroids may occur with inhaled corticosteroids, especially if high doses are used over a long period of time; the occurrence of these effects is much less likely than during oral corticosteroids. It should be used with caution in patients with pulmonary tuberculosis or in patients with chronic or untreated infections. In patients with a history of diabetes mellitus, the risk of increasing blood Glucose should be taken into account. In particular, patients with COPD should be closely monitored for pneumonia, as clinical signs of pneumonia and exacerbation of COPD often overlap. Risk factors for pneumonia in patients with COPD receiving the product relate to: current smokers, patients with a history of pneumonia, patients with low body mass index (BMI <25 kg / m² pc.) and in patients with FEV1 <50% of the due value. If pneumonia occurs, treatment should be reviewed. The 184 μg + 22 μg formulation is not indicated for patients with COPD; there is no additional benefit of 184 μg + 22 μg compared to 92 μg + 22 μg, and the potential risk of systemic side effects of corticosteroids is increased. The safety and efficacy of the preparation in children <12 years of age in the treatment of asthma has not been established. The preparation is not applicable to the indication of COPD in children and adolescents. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

During pregnancy, use only if the expected benefit to the mother outweighs the potential risk to the fetus. In women's milk corticosteroids and β are detected₂-mimetic (no data on fluticasone furoate or vilanterol); a risk can not be ruled out for newborns and breast-fed infants - a decision should be made whether to discontinue breast-feeding or discontinue the use of the product, taking into account the benefits of breastfeeding and the benefits for the mother.

Very common: headache, nasopharyngitis. Common: pneumonia, upper respiratory tract infection, bronchitis, influenza, oral and pharyngeal candidiasis, mouth and throat pain, sinusitis, pharyngitis, rhinitis, cough, noises, abdominal pain, joint pain, back pain , bone fractures, fever. Uncommon: additional cramps. Rarely: hypersensitivity reactions (including anaphylaxis, angioedema, rash and urticaria), palpitations, tachycardia. With the exception of pneumonia and fractures, the safety profile was similar in patients with asthma and COPD; during clinical trials, pneumonia and fractures were usually more commonly observed in patients with COPD.

Inhalation.Asthma. Adults and adolescents aged ≥12 years: one inhalation of 92 μg + 22 μg or 184 μg + 22 μg once a day. Improvement is felt within 15 minutes of inhalation, however, patients should be advised that systematic daily use is necessary to maintain control of asthma symptoms and that it should continue to be used even when the symptoms have disappeared. If symptoms occur between doses, short-acting inhaled β should be used₂-mimetic for immediate improvement. In patients who require low dose inhalation corticosteroid in combination with long-acting β₂- as a starting dose, a dose of 92 μg + 22 μg should be considered; if asthma control is insufficient, the dose can be increased to 184 μg + 22 μg.In patients who need a higher dose of inhaled corticosteroid in combination with long-acting β₂-mimetic, a dose of 184 μg + 22 μg should be considered. The maximum recommended dose is 184 μg + 22 μg once a day. The lowest dose to ensure effective symptom control should be established. Patients with asthma should be treated with a dose of fluticasone furoate (FF) that is adjusted for the severity of their disease. It should be taken into account that in asthmatic patients the dose of 100 μg FF once daily is approximately equivalent to 250 μg fluticasone propionate (FP) twice daily, while the dose of 200 μg FF once a day is approximately equivalent to 500 μg FP 2 times a day.COPD. Adults aged ≥ 18 years: one inhalation of 92 μg + 22 μg once a day. The dose of 184 μg + 22 μg is not indicated in patients with COPD. The improvement is felt within 16-17 minutes after inhalation.Special groups of patients. No dose adjustment is necessary in elderly patients (> 65 years) or in patients with impaired renal function. In patients with moderate or severe hepatic impairment the maximum dose is 92 μg + 22 μg.Way of giving. It should be inhaled at the same time each day (morning or evening). After inhalation, rinse the mouth with water without swallowing. If you miss a dose, take the Next dose the next day at the usual time. Detailed instructions for using the inhaler - see manufacturer's materials.