Index of drugs

The preparation is indicated for use in maintenance bronchodilatory therapy to relieve the symptoms of the disease in adult patients with chronic obstructive pulmonary disease (COPD).

One capsule contains 63 μg of glycopyrronium bromide, equivalent to 50 μg of glycopyrronium. 1 delivered dose (the dose that escapes through the mouthpiece of the inhaler) contains 55 μg of glycopyrronium bromide, equivalent to 44 μg of glycopyrronium. The preparation contains lactose.

Long-acting anticholinergic for inhalation. Glycopyrronium bromide is a muscarinic receptor antagonist with high affinity for them (more than 4-fold selectivity for M3 receptors relative to M2 receptors). It works by blocking the constricting bronchi of acetylcholine activity on the smooth muscle of the airways, thus causing their extension. The drug is characterized by a rapid onset and long duration of action. After oral inhalation with the Seebri Breezhaler inhaler, the drug is rapidly absorbed and maximum plasma concentrations occur within 5 minutes of dosing. The absolute bioavailability is about 45% of the delivered dose. Approx. 90% AUC after inhalation is the result of absorption from the lungs, and 10% - absorption from the gastrointestinal tract. In patients with COPD, pharmacokinetic steady-state is achieved within 1 week of starting treatment. Binding of glycopyrronium to plasma proteinsin vitro ranges from 38-41%. The drug is metabolized by hydroxylation and direct hydrolysis. Numerous CYP isoenzymes participate in the oxidative transformation of glycopyrronium. Elimination of parent drug through the kidneys is approximately 60-70% of the total systemic glycopyrronium clearance, while non-adrenal clearance accounts for approximately 30-40% of the dose. Non -renal clearance consists of excretion of the drug with bile, however, it is believed that the majority of non-adrenal clearance are metabolic changes. Up to 23% of the delivered dose was detected in the urine as a parent drug. Plasma glycopyrronium concentrations decrease in a multiphase manner. Medium T_0,5 in the final phase after inhalation of the drug is 33-57 h. The course of elimination indicates long-term absorption of the drug from the lung and / or passage of glycopyrronium to the systemic circulation after 24 h from inhalation and later.

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

The preparation is not intended for use in acute conditions (it is not a medicine for temporary use). If paradoxical bronchospasm occurs, immediately discontinue use and alternative treatment. It should be used with caution in patients with narrow-angle glaucoma or in patients with urinary retention. Patients should be informed of the signs and symptoms of acute narrow-angle glaucoma and the need to discontinue treatment with the agent immediately contacting a physician if any of these symptoms occur. In patients with severe renal impairment (calculated glomerular filtration rate below 30 ml / min / 1.73 m²pc.), including patients with end-stage renal failure requiring dialysis, should be used only if the expected benefits outweigh the potential risk; these patients should be closely monitored for adverse reactions. Patients with unstable ischemic heart disease, left ventricular failure, history of myocardial infarction, arrhythmia (non-chronic, stable atrial fibrillation), QT syndrome or QTc patients (determined by the Frideric method) were excluded from participation in clinical trials it was prolonged (> 450 ms for men or> 470 ms for women) and therefore the experience of using the drug in this group of patients is limited, the preparation should be used with caution. The use of the preparation in children and adolescents (under 18 years) in the indication of COPD is not appropriate.The preparation contains lactose - 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 patient justifies the potential risk to the fetus. It is not known whether glycopyrronium bromide is excreted in human milk. The use of glycopyrronium by breastfeeding women should only be considered if the expected benefit to a woman outweighs the possible risk to the child.

Common: pharyngitis, insomnia, headache (in patients over 75 years), dry mouth (mainly during the first 4 weeks of treatment), gastroenteritis, urinary tract infection (in patients over 75 years of age). Uncommon: rhinitis, cystitis, hyperglycemia, hypoaesthesia, atrial fibrillation, palpitations, sinus congestion, coughing with expectoration, throat irritation, nosebleed, indigestion, tooth decay, rash, limb pain, musculoskeletal pain in the cage thoracic, painful or difficult urination, urinary retention, fatigue, asthenia.

Inhalation. Adults: the recommended dose is inhalation of 1 capsule once daily with the Seebri Breezhaler inhaler. It is recommended that the preparation be administered at the same time of the day every day. If a dose is missed, the Next dose should be taken as soon as possible. Do not take more than 1 dose a day. The preparation can be used at the recommended dose in elderly patients (aged 75 years and older) and in patients with mild to moderate renal impairment. Patients with hepatic impairment should not be expected to significantly increase their exposure.