Budesonide-Nativ, inhalation solution 250 µg/ml, 2 ml vials 10 pcs.

Composition

Active ingredient:budesonide 0.25 mg / ml. Auxiliary substances:methylparahydroxybenzoate (nipagin) – 0.5 mg, succinic acid-1.5 mg, disodium edetate (trilon B) – 0.5 mg, macrogol 400 (polyethylene oxide-400) – 350 mg, propylene glycol-200 mg, purified water-up to 1 ml

. Pharmacological action

Budesonide-Native is a synthetic glucocorticosteroid (corticosteroid) for topical 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 arachidonic acid metabolites-cyclic endoperoxides and prostaglandins (Pg). It prevents the marginal accumulation of neutrophils, reduces inflammatory exudation and cytokine production, inhibits macrophage migration, reduces the intensity of infiltration processes, the formation of chemotaxis substances, and inhibits the release of inflammatory mediators from mast cells.

Increases the number of” active ” beta-adrenergic receptors, restores the response of the bronchi to bronchodilators, allowing you 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 has virtually no systemic effects at the recommended doses. The therapeutic effect begins a few hours after inhalation. The maximum therapeutic effect develops only a few days after the introduction 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 stop acute bronchospasm.

Pharmacokinetics

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

Indications

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

Use during pregnancy and lactation

Caution should be exercised during pregnancy and lactation.

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

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

Recommendations for use

Dosage of the drug “Budesonide-native” should be individual. The initial dose in adults for the treatment of asthma and COPD is 1-2 mg per day. The dose for maintenance treatment is 0.5-4 mg per day. After the effect is obtained, the dose is reduced to the minimum effective dose necessary to maintain a stable condition. In some cases, in patients whose treatment requires achieving a rapid therapeutic effect, the dose of the drug may be increased.

If the patient took corticosteroids orally, the transfer to treatment with Budesonide-native should be carried out with a stable state of health of the patient, for 10-14 days, inhalation and oral corticosteroids are combined. Within 10 days, it is recommended to take high doses of Budesonide-native against the background of taking oral glucocorticosteroids in a selected dose. In the future, the dose of oral glucocorticosteroids should be gradually reduced (for example,2.5 mg of prednisone) to the lowest possible level. In many cases, it is possible to completely stop taking oral glucocorticosteroids.

There are no data on the use of budesonide in patients with renal insufficiency or impaired liver function. Since budesonide is eliminated by biotransformation in the liver, an increase in the duration of action of the drug can be expected in patients with severe cirrhosis of the liver. Children over 16 years of age: the initial dose is 0.25-0.5 mg / day. If necessary, the dose can be increased to 1 mg / day. The maintenance dose is 0.25-2 mg / day. When prescribing to patients with cirrhosis of the liver, more careful monitoring is required. The drug is used with a nebulizer. The bottle contains 1 single dose.

Instructions for use

Open the medicine bottle. Fill the nebulizer through the upper opening with the required amount of the drug. Perform nebulization according to the instructions for the type of nebulizer used. The volume of budesonide solution delivered to the patient’s lungs by nebulizer is variable and depends on several factors, including the following::

• Inhalation time
• Camera fill level
• Technical characteristics of the nebulizer
• The ratio of the inhaled/exhaled volume and the patient’s respiratory volume
• Using a mouthpiece or mask

Note:

Cleaning up

The nebulizer chamber should be cleaned after each use. The nebulizer chamber and mouthpiece or mask should be washed with warm water, using a mild detergent or according to the manufacturer’s instructions.

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

Often (> 1/100): cough, dry mouth, hoarseness of voice, dysphonia, irritation of the oral and pharyngeal mucosa, candida stomatitis, dry pharyngeal mucosa, headache, nausea. Rarely (High doses of the drug can lead to the development of systemic side effects-adrenal cortex depletion, hyperglycemia, arterial hypertension.

Interaction

In the treatment of bronchial asthma, Budesonide-native is well combined with beta-2-adrenomimetics, Cromoglicic acid or nedocromil, methylxanthines and ipratropium bromide. Phenobarbital, phenytoin, rifampicin reduce the effectiveness (induction of microsomal liver enzymes).

Methandienone, estrogens increase the concentration of budesonide in 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 by 3 times. There is no information about a similar interaction with inhaled dosage forms of budesonide, but a noticeable increase in the concentration of the drug in plasma should be expected.

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

How to take, course of administration and dosage

Dosage of the drug “Budesonide-native” should be individual. The initial dose in adults for the treatment of asthma and COPD is 1-2 mg per day. The dose for maintenance treatment is 0.5-4 mg per day. After the effect is obtained, the dose is reduced to the minimum effective dose necessary to maintain a stable condition. In some cases, in patients whose treatment requires achieving a rapid therapeutic effect, the dose of the drug may be increased.

If the patient took corticosteroids orally, the transfer to treatment with Budesonide-native should be carried out with a stable state of health of the patient, for 10-14 days, inhalation and oral corticosteroids are combined. Within 10 days, it is recommended to take high doses of Budesonide-native against the background of taking oral glucocorticosteroids in a selected dose. In the future, the dose of oral glucocorticosteroids should be gradually reduced (for example,2.5 mg of prednisone) to the lowest possible level. In many cases, it is possible to completely stop taking oral glucocorticosteroids.

There are no data on the use of budesonide in patients with renal insufficiency or impaired liver function. Since budesonide is eliminated by biotransformation in the liver, an increase in the duration of action of the drug can be expected in patients with severe cirrhosis of the liver. Children over 16 years of age: the initial dose is 0.25-0.5 mg / day. If necessary, the dose can be increased to 1 mg / day. The maintenance dose is 0.25-2 mg / day. When prescribing to patients with cirrhosis of the liver, more careful monitoring is required. The drug is used with a nebulizer. The bottle contains 1 single dose.

Instructions for use

Open the medicine bottle. Fill the nebulizer through the upper opening with the required amount of the drug. Perform nebulization according to the instructions for the type of nebulizer used.The volume of budesonide solution delivered to the patient’s lungs by nebulizer is variable and depends on several factors, including the following::

• Inhalation time
• Camera fill level
• Technical characteristics of the nebulizer
• The ratio of the inhaled/exhaled volume and the patient’s respiratory volume
• Using a mouthpiece or mask

Note:

Cleaning up

The nebulizer chamber should be cleaned after each use. The nebulizer chamber and mouthpiece or mask should be washed with warm water, using a mild detergent or according to the manufacturer’s instructions.

Overdose

In acute overdose, no clinical manifestations occur.

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

Special instructions

Budesonide-native is not intended for the relief of acute asthma and COPD symptoms. You should strictly follow the instructions for using the inhaler. Avoid getting the product in your eyes. After using the drug, it is recommended to rinse your mouth with water to reduce the risk of candida stomatitis.

When switching from oral glucocorticosteroid therapy to Budesonide-native, the dosage of systemic corticosteroids should be reduced very slowly and in small doses (for example,2.5 mg of prednisone). Pseudorheumatism syndrome is possible in patients who have been on long-term therapy with systemic corticosteroids. In these cases, it is sometimes necessary to temporarily increase the dose of oral corticosteroids.

In rare cases, there are symptoms such as fatigue, headaches, nausea, vomiting. After complete withdrawal, long-term monitoring of the patient is recommended (risk of developing adrenal insufficiency), as well as an assessment of the function of external respiration. 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 dangerous 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. ).

Use only in nebulizers.

Form of production

Solution for inhalation

Storage conditions

Store in a dry place protected from light and out of reach of children at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Budesonide

Conditions of release from pharmacies

By prescription

Dosage form

solution for inhalation

Purpose

Pregnant women as prescribed by a doctor, Children over 16 years of age, Nursing mothers as prescribed by a doctor, Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Bronchial Asthma, Chronic Obstructive Pulmonary Disease

Weight

Weight: 145 g.