Budesonide-Nativ, 0.5 mg/ml 2 ml 10 pcs

Synthetic glucocorticosteroid (GCS) for topical use, has anti-inflammatory, anti-allergic and immunosuppressive effects. Increases production of lipomodulin, which is an inhibitor of phospholipase A, inhibits the release of arachidonic acid, inhibits the synthesis of products of metabolism of arachidonic acid – cyclic endoperoxides and prostaglandins (Pg). It prevents marginal accumulation of neutrophils, decreases inflammatory exudation and cytokine production, inhibits macrophage migration, decreases intensity of infiltration processes, formation of chemotaxis substance, inhibits release of inflammatory mediators from mast cells.

Lengthens the number of “active” beta-adrenoreceptors, restores bronchial response to bronchodilators, allowing to reduce the frequency of their use, reduces mucosal bronchial edema, mucus production, sputum formation and reduces airway hyperresponsiveness. It improves mucociliary transport. It is well tolerated during long-term treatment, has no mineralocorticosteroid activity, and in the recommended doses it has practically no systemic effect.

Therapeutic effect begins several hours after inhalation. The maximum therapeutic effect develops only a few days after inhaled doses of Budesonide, on average 5-7 days.
Inhalation of Budesonide is able to prevent an attack of bronchial asthma, but does not stop acute bronchospasm.

The absorption is low. After inhalation, 20-25% reaches the small bronchi, part of the dose that enters the gastrointestinal tract (GIT) is absorbed and almost completely (90%) undergoes biotransformation in the liver to inactive metabolites.

The systemic bioavailability of Budesonide is 38% of the administered dose, and 1/6 of this value is formed due to swallowing a portion of the drug. Time of onset of maximum plasma concentration is 15-45 min after inhalation administration. Binding with plasma proteins is 88%. Budesonide distribution volume is about 3 l/kg. It has high systemic clearance – 84 l/h. The elimination half-life is ~ 2.8 h, maximum plasma concentration is 0.01 mmol/l. It is excreted through the intestine as metabolites – 10%, by the kidneys – 70%.

Indications

Bronchial asthma (BA), requiring maintenance therapy with GCS; chronic obstructive pulmonary disease (COPD).

Pharmacological effect

Synthetic glucocorticosteroid (GCS) for local use, has anti-inflammatory, antiallergic 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 arachidonic acid metabolic products – cyclic endoperoxides and prostaglandins (Pg). Prevents the marginal accumulation of neutrophils, reduces inflammatory exudation and the production of cytokines, inhibits the migration of macrophages, reduces the intensity of infiltration processes, the formation of a 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, allowing to reduce the frequency of their use, reduces swelling of the bronchial mucosa, mucus production, sputum formation and reduces airway hyperreactivity. Improves mucociliary transport. It is well tolerated during long-term treatment, does not have mineralocorticosteroid activity, and in recommended doses has virtually no systemic effects.

The therapeutic effect begins a few hours after inhalation. The maximum therapeutic effect develops only a few days after the administration of therapeutic doses of inhaled Budesonide, on average after 5-7 days.
Inhalation of Budesonide can prevent an attack of bronchial asthma, but does not relieve acute bronchospasm.

Absorption is low. After inhalation, 20-25% reaches the small bronchi, part of the dose entering the gastrointestinal tract (GIT) is absorbed and almost completely (90%) undergoes biotransformation in the liver to inactive metabolites.

The systemic bioavailability of Budesonide is 38% of the dose taken, with 1/6 of this value formed due to ingestion of part of the drug. The time for maximum concentration in blood plasma is 15-45 minutes after inhalation administration. Communication with plasma proteins – 88%. The volume of distribution of Budesonide is approximately 3 l/kg. It has a high systemic clearance – 84 l/h. The half-life is ~ 2.8 hours, the maximum concentration in blood plasma is 0.01 mmol/l. Excreted through the intestines in the form of metabolites – 10%, by the kidneys – 70%.

Special instructions

Budesonide native is not intended for the relief of acute symptoms of asthma and COPD. The instructions for use of the inhaler should be strictly followed. Avoid getting the drug in your eyes. After using the drug, it is recommended to rinse your mouth with water to reduce the risk of candidal stomatitis.

When switching from therapy with oral glucocorticosteroids to the drug “Budesonide-native”, the dosage reduction of systemic corticosteroids must be carried out very slowly and in small doses (for example, 2.5 mg of prednisolone). In patients who have been on long-term therapy with systemic corticosteroids, pseudorheumatism syndrome is possible.

In these cases, it is sometimes necessary to temporarily increase the dose of oral corticosteroids. In rare cases, symptoms such as fatigue, headaches, nausea, and vomiting are observed. After complete withdrawal, long-term observation of the patient is recommended (risk of developing adrenal insufficiency), as well as assessment of external respiratory function. The drug “Budesonide-native” can be prescribed to patients who cannot use other dosage forms of inhaled corticosteroids (elderly and senile patients).

The drug does not affect the ability to engage in potentially hazardous activities that require special attention and quick reactions (driving a car and other vehicles, working with moving mechanisms, working as a dispatcher and operator, etc.).

Active ingredient

Budesonide

Pregnancy

Use during pregnancy and breastfeeding

During pregnancy and lactation, caution should be exercised.

Prescribing the drug is rational if the benefit of its use for the mother outweighs the potential risk for the fetus or child.

There are no data on the excretion of Budesonide in breast milk.

Contraindications

Hypersensitivity to the components of the drug, children under 16 years of age.

With caution.

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

Side Effects

Common (> 1/100): cough, dry mouth, hoarseness, dysphonia, irritation of the oral and pharyngeal mucosa, candidal stomatitis, dry pharyngeal mucosa, headache, nausea.

Rarely (<1/1000): bruising or thinning of the skin, unpleasant taste, paradoxical bronchospasm (for prevention - a combination of inhalations with beta2-agonists), esophageal candidiasis.

High doses of the drug can lead to the development of systemic side effects: depletion of the adrenal cortex, hyperglycemia, arterial hypertension.

Interaction

In the treatment of bronchial asthma, Budesonide-native combines well with beta2-adrenergic agonists, cromoglycic acid or nedocromil, methylxanthines and ipratropium bromide. Phenobarbital, phenytoin, rifampicin reduce effectiveness (induction of microsomal liver enzymes).

Methandienone and estrogens increase the concentration of budesonide in the blood plasma.

Taking 200 mg of ketoconazole once a day increases the plasma concentration of orally administered budesonide at a dose of 3 mg by an average of 6 times. When ketoconazole is prescribed 12 hours after taking budesonide, the plasma concentration of the latter increases 3 times.

There is no information on such interactions with inhaled dosage forms of budesonide, but a noticeable increase in plasma concentrations of the drug should be expected.

Other potential CYP3A4 inhibitors, such as itraconazole, also significantly increase plasma concentrations of budesonide. The drug can be diluted with 0.9% sodium chloride solution.

Overdose

In case of acute overdose, no clinical manifestations occur.

With prolonged use of the drug in doses significantly higher than recommended, a systemic glucocorticosteroid effect may develop in the form of hypercortisolism and suppression of adrenal function.

Storage conditions

In a dry place, protected from light, out of reach of children, at a temperature not exceeding 25°C.

Shelf life

3 years

Manufacturer

Nativa, Russia