Budesonide-Nativ, 0.25 mg/ml 2 ml 10 pcs

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

It increases the number of “active” beta-adrenoreceptors, restores the bronchial response to bronchodilators, allowing us to reduce the frequency of their use, reduces swelling of the bronchial mucosa, 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 practically does not have a systemic effect in the recommended doses.
Therapeutic effect begins several hours after inhalation. The maximum therapeutic effect develops only a few days after administration of therapeutic doses of inhaled budesonide, on average 5-7 days.
Inhalation of budesonide can prevent an attack of bronchial asthma, but does not relieve acute bronchospasm.

Pharmacokinetics

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. Systemic bioavailability of budesonide is 38% of the administered dose, and 1/6 of this value is formed by swallowing part of the drug. The time of onset of maximum plasma concentration is 15-45 minutes after inhalation administration. The binding to plasma proteins is 88%. The volume of budesonide distribution is about 3 l/kg. It has high systemic clearance – 84 l/h. The elimination half-life is ~ 2.8 hours, 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).

Active ingredient

How to take, the dosage

The dosage of the drug Budesonide-Nativ should be individualized. Initial dose in adults for treatment of BA and COPD is 1 – 2 mg per day. The dose for maintenance treatment is 0.5 – 4 mg per day. After obtaining an effect, the dose is reduced to the minimum effective dose necessary to maintain a stable condition. In some cases, in patients for whom it is necessary to achieve a rapid therapeutic effect, the dose of the drug may be increased.

If a patient has taken oral GCS, conversion to budesonide-nativ should be performed when the patient is stable, with a combination of inhalation and oral GCS for 10-14 days. During 10 days it is recommended to take high doses of Budesonide-nativ with a matching dose of oral glucocorticosteroids. Thereafter, the dose of oral glucocorticosteroids should be gradually reduced (e.g., 2.5 mg of prednisolone) to the lowest possible level. In many cases it is possible to stop taking oral glucocorticosteroids completely.

There are no data on the use of budesonide in patients with renal insufficiency or impaired liver function. As excretion of budesonide occurs due to biotransformation in liver, increase of duration of drug action can be expected in patients with severe liver cirrhosis.
Children over 16 years old: The initial dose is 0.25-0.5 mg/day. If necessary the dose may be increased up to 1 mg/day. The maintenance dose is 0.25-2 mg/day.
When administering to patients with cirrhosis more careful observation is required.
The drug is administered using a nebulizer. The bottle contains 1 single dose.

Instructions for use

Pop open the vial of product. Fill the nebulizer through the top opening with the desired amount of product. Follow the instructions for the nebulizer you are using.
The amount of budesonide solution delivered to the patient’s lungs with the nebulizer is variable and depends on several factors, including the following:

Note

Cleaning

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

Interaction

In the treatment of bronchial asthma budesonide-nativ combines well with beta2-adrenomimetics, cromoglycic acid or nedocromil, methylxanthines and ipratropium bromide. Phenobarbital, phenytoin, rifampicin reduce efficacy (induction of microsomal liver enzymes).

Methandienone, estrogens increase plasma concentration of budesonide. Taking 200 mg of ketoconazole once daily increases the plasma concentration of orally administered budesonide at a dose of 3 mg by a factor of 6 on average.

In administration of ketoconazole 12 hours after budesonide administration, the plasma concentration of budesonide increases by 3 times. There is no information about similar interaction with inhaled dosage forms of budesonide, but a marked increase in plasma concentrations of the drug should be expected.

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

Directions for use

The dosage of the drug Budesonide-Nativ should be individualized. Initial dose in adults for treatment of BA and COPD is 1 – 2 mg per day. The dose for maintenance treatment is 0.5 – 4 mg per day. After obtaining an effect, the dose is reduced to the minimum effective dose necessary to maintain a stable condition. In some cases, in patients for whom it is necessary to achieve a rapid therapeutic effect, the dose of the drug may be increased.

If a patient has taken oral GCS, conversion to budesonide-nativ should be performed when the patient is stable, with a combination of inhalation and oral GCS for 10-14 days. During 10 days it is recommended to take high doses of Budesonide-nativ with a matching dose of oral glucocorticosteroids. Thereafter, the dose of oral glucocorticosteroids should be gradually reduced (e.g., 2.5 mg of prednisolone) to the lowest possible level. In many cases it is possible to stop taking oral glucocorticosteroids completely.

There are no data on the use of budesonide in patients with renal insufficiency or impaired liver function. As excretion of budesonide occurs due to biotransformation in liver, increase of duration of drug action can be expected in patients with severe liver cirrhosis.
Children over 16 years old: The initial dose is 0.25-0.5 mg/day. If necessary the dose may be increased up to 1 mg/day. The maintenance dose is 0.25-2 mg/day.
When administering to patients with cirrhosis more careful observation is required.
The drug is administered using a nebulizer. The bottle contains 1 single dose.

Instructions for use

Pop open the vial of product. Fill the nebulizer through the top opening with the desired amount of product. Follow the instructions for the nebulizer you are using.
The amount of budesonide solution delivered to the patient’s lungs with the nebulizer is variable and depends on several factors, including the following:

Note

Cleaning

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

Special Instructions

Budesonide-Nativ is not intended to relieve acute symptoms of AD and COPD. The instructions for use of the inhaler must be strictly followed. Avoid contact of the drug with the eyes. After using the drug it is recommended to rinse your mouth with water to reduce the risk of candida stomatitis.

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

In rare cases, symptoms such as fatigue, headaches, nausea, and vomiting have been observed. After complete withdrawal, long-term monitoring of the patient is recommended (risk of adrenal insufficiency), as well as evaluation of external respiratory function. Budesonide-nativ may be administered to patients who cannot use other dosage forms of inhaled GCS (elderly and senile patients).

The drug does not affect the ability to perform potentially dangerous activities requiring particular attention and quick reactions (driving a car and other vehicles, working with moving mechanisms, controllers and operators, etc.).

Perform only in nebulizers.

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 respiratory infections, pregnancy, lactation.

Side effects

Overdose

In acute overdose there are no clinical manifestations.

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

Pregnancy use

Caution should be exercised during pregnancy and lactation.

Prescribing the drug is reasonable if the benefit to the mother exceeds the potential risk to the fetus or child.

There are no data on excretion of budesonide with breast milk.

Similarities