Budesonide-native solution for inhalation of 0.25 mg/ml 2 ml №10

Description:

colorless or slightly yellowish liquid. Light opalescence is allowed.

Pharmacological group:

Glucocorticosteroid for topical use.

Pharmacological properties

Synthetic glucocorticosteroid (GCS) for local use, has anti-inflammatory, anti-allergic and immunosuppressive effects. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, inhibits the release of arachidonic acid, inhibits the synthesis of products of the metabolism of arachidonic acid - cyclic endoperexia and prostaglandins (Pg). Warns neutrophil regional accumulation, reduces inflammatory exudation and cytokine production, inhibits macrophage migration, reduces the intensity of infiltration processes, the formation of chemotaxis substance, and inhibits the release of inflammatory mediators from mast cells.

Increases the number of "active" beta-adrenergic receptors, restores the bronchial response to bronchodilators, reducing the frequency of their use, reduces swelling of the mucous membrane of the bronchi, mucus production, sputum formation and reduces airway hyperreactivity. Improves mucociliary transport.It is well tolerated with long-term treatment, it does not possess mineralocorticosteroid activity, and in recommended doses it has almost no systemic effect.

The therapeutic effect begins several hours after inhalation. The maximum therapeutic effect develops only a few days after the administration of therapeutic doses of inhaled Budesonide, an average of 5-7 days.

Inhalation of budesonide can prevent an attack of bronchial asthma, but does not stop acute bronchospasm.

Pharmacokinetics

Absorption is low. After inhalation, 20–25% reaches the small bronchi, a part of the dose that entered the gastrointestinal tract (GIT) is absorbed and almost completely (90%) undergoes biotransformation in the liver to inactive metabolites. Systemic bioavailability of budesonide is 38% of the dose, and 1/6 of this value is formed by swallowing part of the drug. The time of onset of the maximum concentration in the blood plasma is 15-45 min after inhalation. Communication with plasma proteins - 88%. The volume of distribution of budesonide is approximately 3 l / kg. It has a high system clearance of 84 l / h. The half-life is ~ 2.8 h, the maximum plasma concentration is 0.01 mmol / l. Excreted through the intestine in the form of metabolites - 10%, kidneys - 70%.

Indications

·       Bronchial asthma (BA), requiring maintenance therapy GCS;

·       chronic obstructive pulmonary disease (COPD).

Contraindications

·       Hypersensitivity to the components of the drug,

·       children's age up to 16 years.

Carefully

Active and inactive forms of tuberculosis, fungal, bacterial and viral respiratory infections, pregnancy, lactation.