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).

Active ingredient

How to take, the dosage

Pregnancy and lactation

Pregnancy and lactation should be treated with caution. Administration of 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 in the breast milk.

Pop open the vial of the product. Fill the nebulizer through the top opening with the desired amount of product. Nebulization according to the instructions for the type of 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:
-Time of inhalation;
-Level of chamber filling;
-Technical characteristics of the nebulizer;
-Inhalation/exhalation volume ratios to patient respiratory volume;
-Use of mouthpiece or mask.

Rinse your mouth with water after each inhalation.
If you are using a mask, make sure the mask fits snugly over your face when inhaling. Wash your face after inhalation.

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 the plasma concentration of budesonide.

The administration of 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. If ketoconazole is administered 12 hours after budesonide administration, the plasma concentration of the latter is increased by 3 times.

There is no information about this interaction with inhaled dosage forms of budesonide, but a marked increase in plasma concentrations of the drug should be expected.

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

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 switching from oral glucocorticosteroid therapy to Budesonide-Nativ, reduce the dosage of systemic GCS very slowly and in small doses (e.g., 2.5 mg prednisolone). Pseudorheumatism syndrome is possible in patients 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, vomiting are 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 indicated in patients who are unable to use other forms of inhaled GCS (elderly and senile patients).

The drug does not affect the ability to engage in potentially hazardous activities requiring particular attention and quick reactions (driving a car and other vehicles, operating moving machinery, work of dispatcher and operator, etc.).

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

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

Rarely (< 1/1000): bruising or thinning of skin, unpleasant taste sensation, paradoxical bronchospasm (for prevention – combination of inhalation with beta2-adrenomimetics), esophageal candidiasis.

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

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

Pregnancy and breastfeeding

Pregnancy and lactation should be treated with caution.

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