Index of drugs

Supportive bronchodilatory treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).

Each single inhalation provides a dose delivery (dose exiting the mouthpiece) containing 65 μg of umeclidinium bromide (corresponding to 55 μg of umeclidinium) and 22 μg of vilanterol (as triphenylacetate). This corresponds to a divided dose containing 74.2 μg of umeclidinium bromide (corresponding to 62.5 μg of umeclidinium) and 25 μg of vilanterol (as triphenylacetate). The preparation contains lactose.

Association of inhaled long-acting muscarinic receptor antagonist (umeclidinium) with inhaled long-acting β-receptor agonist₂-renergic (vilanterol). Both substances, acting locally in the respiratory tract, in separate mechanisms, cause bronchodilation. The mechanism of action of the bronchodilator umeklidynium consists in the competitive inhibition of the binding of acetylcholine to muscarinic receptors in the smooth muscle of the respiratory tract. The effects of vilanterol include on the stimulation of intracellular adenylyl cyclase, which 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. Umeclidinium and vilanterol reach C_max within 5-15 min. The absolute bioavailability of umeclidinium is on average 13% of the dose, vilanterol 27%, with a negligible share of both substances absorbed from the gastrointestinal tract. After repeated administration, the steady state of umeclidinium is reached within 7-10 days, vilanterol within 6 days. Umeclidinium is mainly metabolised by cytochrome P450 2D6 (CYP2D6) and is a substrate of the P-glycoprotein transporter (P-gp). Wilanterol is mainly metabolised by cytochrome P450 3A4 (CYP3A4) and is a substrate of the P-glycoprotein transporter (P-gp). T_0,5 in the elimination phase after inhaled administration of umeclidinium for 10 days is an average of 19 h, of which 3-4% is excreted unchanged in the urine. T_0,5 in the elimination phase after inhalation of vilanterol for 10 days is on average 11 hours.

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

It should not be used in patients with asthma and in the treatment of acute bronchospasm. After applying the medicine there is a risk of paradoxical bronchospasm that may be life-threatening; if this side effect occurs, the preparation should be discontinued immediately and other treatment as necessary. Increasing the amount of short-acting bronchodilators used to relieve symptoms is indicative of worsening disease control; in the event of worsening COPD during treatment, the patient should be re-evaluated and the treatment of COPD verified. Caution should be exercised when using umeclidinium with vilanterol in patients with severe cardiovascular disease (risk of developing atrial fibrillation and tachycardia). Due to the antimuscarinic effect, caution should be exercised when administering the patient in patients with urinary retention or narrow-angle glaucoma. The use of β-receptor agonists₂-adrenergic may cause significant hypokalaemia in some patients, which may potentially cause cardiovascular side effects. Caution should be exercised when the product is used with other medicines that may also cause hypokalaemia. When starting treatment with umanclidinum with vilanterol, patients with diabetes should be monitored carefully for plasma Glucose (possible transient hyperglycaemia). The drug should be used with caution in patients with seizures or thyrotoxicosis, in patients particularly sensitive to β-receptor agonists₂-adrenergic and in patients with severe hepatic impairment.The use of the preparation in children and adolescents <18 years is not appropriate in the indication of COPD. 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.

It should only be used during pregnancy if the expected benefit to the mother outweighs the potential risk to the fetus. It is not known whether umeclidinium or vilanterol are excreted in human milk. However, β-receptor agonists are detected in human milk₂adrenergic. A decision should be made whether to discontinue breast-feeding or discontinue the treatment, taking into account the benefits of breastfeeding for the baby and the benefits of treatment for the woman.

Common: urinary tract infection, sinusitis, nasopharyngitis, pharyngitis, inflammation of the upper respiratory tract, headache, cough, mouth and throat pain, constipation, dry mouth. Uncommon: atrial fibrillation, supraventricular tachycardia, idiopathic rhythm, tachycardia, extra supraventricular cramps, subcutaneous rash.

Inhalation. Adults: the recommended dose is one inhalation (55 μg / 22 μg) once a day (maximum dose). The product should be used once a day every day at the same time. No dose adjustment is required in patients> 65 years, in patients with impaired renal function, or in patients with mild or moderate hepatic impairment. Severe caution should be used in patients with severe hepatic impairment.