Budesonide-Native solution 0.5mg/ml 2ml #10

Budesonide-Native instruction

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Composition per ml of solution

Active substance:
budesonide 0.25 mg 0.50 mg
Excipients:
methylparahydroxybenzoate (nipagine) 0.50 mg 0.50 mg
propylene glycol 200 mg 200 mg
Macrogol 400 (polyethylene oxide-400) 350 mg 350 mg
succinic acid 1.5 mg 1.5 mg
disodium edetate (Trilon B) 0.5 mg 0.5 mg
water purified to 1 ml 1 ml
Description: colorless or slightly yellowish liquid. Light opalescence is permissible.
Pharmacological group: Glucocorticosteroid for topical application.
ATC code: R03BA02

Pharmacological properties

Budesonide - a synthetic glucocorticosteroid (GCS) for topical use, at recommended doses has anti-inflammatory, antiallergic and immunosuppressive effects in the bronchi. In an in vitro study in animal models, budesonide has approximately 200 times higher affinity for glucocorticoid receptors and a 1000-fold stronger anti-inflammatory effect than cortisol. Budesonide increases the production of lipomodulin, an inhibitor of phospholipase A, inhibits the release of arachidonic acid, inhibits the synthesis of metabolic products of arachidonic acid-cyclic endoperoxides and prostaglandins (Pg), prevents the accumulation of neutrophils, reduces inflammatory exudation and production of cytokines, inhibits the migration of macrophages, reduces the intensity of infiltration processes , the formation of a chemotactic substance, inhibits the release of inflammatory mediators from mast cells.
Budesonide increases the number of "active" β-adrenergic receptors, restores the bronchial response to bronchodilators, reducing the frequency of their use, reduces edema of the bronchial mucosa, mucus production, sputum production and reduces airway hyperreactivity, reducing the severity of symptoms and the frequency of exacerbations of bronchial asthma with a lower frequency side effects than when using systemic GCS; improves mucociliary transport. Budesonide is well tolerated with long-term treatment, does not have mineralocorticosteroid activity, at recommended doses practically does not have a systemic effect.
Improvement of pulmonary function is achieved several hours after the administration of a single dose of budesonide with the help of a nebulizer. The therapeutic effect begins a few hours after inhalation. The maximum therapeutic effect develops 1-2 weeks after the administration of therapeutic doses of inhaled budesonide, in some cases after 4-6 weeks.
In recommended doses, the drug has a significantly lower effect on adrenal function than prednisone in a dose of 10 mg.

Pharmacokinetics

Suction
Budesonide is rapidly absorbed. After inhalation using a nebulizer, bioavailability is 15% of the total dose and 40-70% of the delivered dose, since about 1/3 of the budesonide that enters the alveoli is absorbed, a significant part is deposited on the mucous membrane of the oropharynx and is swallowed. The maximum concentration (Cmax) in the blood plasma is reached 30 minutes after the start of inhalation.
Distribution
Budesonide almost does not bind to corticosteroid-binding globulin. Connection with blood plasma proteins - 85-90%. The volume of budesonide distribution is approximately 3 l / kg.
Budesonide penetrates into breast milk.
Metabolism
Part of the dose that has entered the gastrointestinal tract (GIT) is absorbed and almost completely (85-95%) undergoes biotransformation in the liver with the enzyme CYP3A4 to 6β-hydroxy-budesonide and 16α-hydroxyprednisolone, metabolites with low activity (less than 1% glucocorticosteroid activity of budesonide).
Excretion
Budesonide is excreted in urine and feces in the form of metabolites or conjugates and only in a small amount - unchanged. Budesonide has a high system clearance (approximately 1.2 l / min). The half-life (T1 / 2) is 2.0-3.6 hours.
The pharmacokinetics of budesonide is proportional to the magnitude of the administered dose of the drug.
Data on the pharmacokinetics of budesonide in patients with renal insufficiency or impaired liver function are not available. In patients with liver disease, the time of budesonide in blood plasma can increase. There is a dose-dependent effect on the cortisol content in blood plasma and urine in the presence of budesonide.
There are no differences in pharmacokinetics due to race, sex or age.

Indications for use

• Bronchial asthma (BA), requiring maintenance therapy with glucocorticosteroids.
• Chronic obstructive pulmonary disease (COPD).

Contraindications

• Hypersensitivity to the components of the drug.
• Children under 16 years.

Carefully

Caution should be applied to the preparation Budesonide-native in patients with active pulmonary tuberculosis, fungal, viral, bacterial infections of the respiratory system, liver cirrhosis, during pregnancy and during breastfeeding. When budesonide is prescribed, the possible effect of the systemic action of glucocorticosteroids should be taken into account.

Application in pregnancy and during breastfeeding

Pregnancy: observation of pregnant women taking budesonide did not reveal anomalies in the fetus, however, the risk of their development can not be completely ruled out, therefore, during pregnancy, the minimum effective dose of budesonide should be used in connection with the possibility of worsening of the course of bronchial asthma.
Lactation: Since there are data on the penetration of budesonide into breast milk, the ratio of expected benefits to the mother and the potential risk to the child should be taken into account when prescribing the drug.

Dosing and Administration

Budesonide-native is intended for use only with the help of a nebulizer.
The dose of the drug is selected individually. In the event that the recommended dose does not exceed 1 mg / day, the entire dose of the drug can be taken for 1 time (one time). In case of taking a higher dose, it is recommended to divide it into 2 doses.

Recommended initial dose

Children from 16 years of age and older: 0.25-0.5 mg per day. If necessary, the dose may be increased to 1 mg / day.
Adults / elderly patients: 1-2 mg per day.

Dose with maintenance treatment

Children from 16 years of age and older: 0.25-2 mg per day.
Adults / elderly patients: 0.5-4 mg per day. In case of severe exacerbations, the dose may be increased.
Table for determining the dose
Dose, mg Volume of preparation Budesonide-native
0.25 mg / ml 0.5 mg / ml
0.25 1 ml * -
0.5 2 ml -
0.75 3 ml -
1 4 ml 2 ml
1,5 - 3 ml
2 - 4 ml
*) should be diluted with 0.9% solution of sodium chloride to a volume of 2 ml.
For all patients, it is desirable to determine the minimum effective maintenance dose.
After receiving the effect, the dose is reduced to the minimum effective dose necessary to maintain a stable state.
If it is necessary to achieve an additional therapeutic effect, an increase in the daily dosage (up to 1 mg / day) of Budesonide-native instead of a combination of the drug with oral GCS may be recommended, due to a lower risk of systemic effects.

Patients receiving oral glucocorticosteroids

Cancellation of oral glucocorticosteroids should be started during a period of stable health of the patient. Within 10 days, it is necessary to take a high dose of Budesonide-native against the background of taking oral GCS in the usual dose. In the future, during a month should gradually reduce the dose of oral GCS (for example, 2.5 mg of prednisolone or its analog) to the minimum effective dose. In many cases, it is possible to completely stop taking oral glucocorticosteroids.
There is no data on the use of budesonide in patients with renal insufficiency. Taking into account the fact that budesonide is excreted by biotransformation in the liver, we can expect an increase in the duration of the drug in patients with severe hepatic cirrhosis.

Instructions for use

Budesonide-native is used for inhalations using a nebulizer equipped with a mouthpiece and a special mask. The nebulizer is connected to the compressor to create the required air flow (5-80 l / min), the nebulizer filling volume should be 2-4 ml.
Important:
- carefully read the instructions for using the drug, as well as the instruction manual for the nebulizer;
- when Budesonide-native is diluted with 0.9% sodium chloride solution, the resulting solution should be used within 30 minutes;
- After inhalation, rinse the mouth with water to reduce the development of candidiasis of the oropharynx;
- to prevent skin irritation after using the mask, wash the face skin with water;
- It is recommended that the nebulizer be cleaned regularly according to the manufacturer's instructions.

How to use budesonide-native with a nebulizer

1. Open the bottle with the drug.
2. Fill the nebulizer through the upper hole with the required amount of the drug.
3. Perform nebulization according to the instructions for the type of nebulizer in use.
4. If you are using a mask, make sure that the mask is snug against the face when inhaled. As Budesonide-native enters the lungs during inspiration, it is important to inhale the drug through the mouthpiece of the nebulizer calmly and smoothly.
The open vial is stored in a place protected from light. The open vial should be used within 12 hours.

Cleaning

The nebulizer chamber and the mouthpiece or mask are washed with warm water or a mild detergent, in accordance with the manufacturer's instructions, after each use.
Rinse well and dry the nebulizer by connecting the chamber to the compressor or the air inlet valve.

Side effects of Budesonide-native

The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems. Frequency of occurrence is estimated as follows: very often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10000 and <1 / 1000), very rarely (<1/10000).
Immune system disorders: rarely - immediate and delayed hypersensitivity reactions, including rash, contact dermatitis, hives, angioedema, bronchospasm and anaphylactic reaction.
Violations from the nervous system: rarely - nervousness, excitability, depression, behavioral disorders.
Disorders from the side of the organ of vision: very rarely - cataract, glaucoma (systemic action).
Disturbances from the respiratory system, chest and mediastinal organs: often - candidiasis of the oropharynx, mild irritation of the mucous membrane of the throat, cough, hoarseness of voice, dry mouth; rarely - bronchospasm.
Disorders from the gastrointestinal tract: rarely - nausea.
Disturbances from the skin and subcutaneous tissues: rarely - the appearance of bruises on the skin.
General disorders and disorders at the site of administration: rarely - angioedema.
Laboratory and instrumental data: very rarely - a decrease in bone mineral density (systemic action).
Taking into account the risk of developing candidiasis of the oropharynx, the patient should thoroughly rinse the mouth with water after each inhalation of the drug.
In rare cases, symptoms can occur due to systemic effects of glucocorticosteroids, including adrenal hypofunction and growth retardation in children. The severity of these symptoms probably depends on the dose of the drug, the duration of therapy, concomitant or previous therapy with glucocorticosteroids, and individual sensitivity.
There are also cases of skin irritation when using a nebulizer with a mask. To prevent irritation after using the mask, the face should be washed with water.

Overdose

In acute overdose, clinical manifestations do not occur. With prolonged use of the drug in doses much higher than recommended, a systemic glucocorticosteroid effect may develop.

Interaction with other medicinal products

Preliminary inhalation of β2-adrenomimetics expands bronchi, improves the flow of budesonide and enhances its therapeutic effect.
In the treatment of bronchial asthma Budesonide-native is well combined with β2-adrenomimetics, preparations of cromoglycic acid or nedocromil, methylxanthines and ipratropium bromide. Phenobarbital, phenytoin, rifampicin and other inducers of microsomal oxidation reduce the effectiveness of budesonide due to the induction of microsomal liver enzymes.
The administration of 200 mg of ketoconazole once a day increases the concentration in the blood plasma of orally administered budesonide at a dose of 3 mg on average 6-fold. With the appointment of ketoconazole 12 hours after the administration of budesonide, the concentration in the plasma of the latter increases threefold. Information on such interaction with inhaled dosage forms of budesonide is absent, but a significant increase in the concentration of the drug in the blood plasma should be expected. Other potential inhibitors of the CYP3A4 isoenzyme, for example itraconazole, also significantly increase the plasma concentration of budesonide.
Methandrostenolone, estrogens increase the concentration of budesonide in blood plasma.

special instructions for Budesonide-native

Budesonide-native is not intended for relief of acute symptoms of asthma and COPD. Inhalation budesonide with admission in advance can prevent an attack of bronchial asthma, but does not stop acute bronchospasm.
Follow the instructions for using the nebulizer. Avoid contact with eyes. After applying budesonide, rinse your mouth with water to reduce the risk of candidal stomatitis.
Joint intake with CYP3A4 inhibitors (ketoconazole, itraconazole or other potential inhibitors of the CYP3A4 isoenzyme) should be avoided. In the event that budesonide and CYP3A4 inhibitors have been prescribed, the time between drug intake should be maximized or the dose of GCS should be reduced.
Because of the possible risk of weakening the function of the adrenal glands (hypokorticism), special attention should be given to patients who are transferred from oral glucocorticosteroids to the drug Budesonide-native. Also, special attention should be given to patients who have received high doses of GCS or who received long-term maximum recommended doses of inhaled glucocorticosteroids. In stressful situations, such patients may show signs and symptoms of adrenal insufficiency. When stress or in cases of surgical intervention, additional therapy with systemic GCS is recommended.
Particular attention should be given to patients who are transferred from systemic to inhaled glucocorticosteroids (budesonide-native) or in the case where a disorder of the pituitary-adrenal function can be expected. In such patients, it is necessary with special care to reduce the dose of systemic glucocorticosteroids and control the hypothalamic-pituitary-adrenal function. Also, patients may require additional administration of oral GCS during stressful situations such as trauma, surgery, etc.
When switching from oral glucocorticosteroids to Budesonide-nativ, patients may experience previously observed symptoms, such as muscle pain or joint pain. In such cases, a temporary increase in the dose of oral GCS may be necessary. In rare cases, such symptoms as fatigue, headache, nausea and vomiting, indicating a systemic insufficiency of glucocorticosteroids, can be observed.
Replacement of oral glucocorticosteroids by inhalation sometimes results in the manifestation of concomitant allergies, for example, rhinitis and eczema, which were previously stopped by systemic drugs, in rare cases - exacerbation of the existing Charge-Strauss syndrome, eosinophilia, hemorrhagic vasculitis, worsening of pulmonological symptoms not associated with the transition to budesonide.
Systemic side effects of inhaled glucocorticosteroids can be manifested, primarily, by the administration of high doses for an extended period of time. The likelihood of this effect is significantly lower than when treated with oral glucocorticosteroids. Possible systemic effects include adrenal suppression, growth retardation in children and adolescents, reduced bone mineral density, cataracts and glaucoma. Therefore, it is very important to titrate the dose of inhaled glucocorticosteroids to the lowest dose at which effective control of the disease remains. It is recommended to regularly monitor the height of growth in children receiving inhaled glucocorticosteroids for an extended period of time. In case of a delay in their growth, correction of treatment should be made to reduce the dose of inhaled glucocorticosteroids to the lowest dose at which effective control of bronchial asthma remains.
Therapy with inhaled budesonide 1 or 2 times a day has shown efficacy for preventing bronchial asthma physical effort.
The use of Budesonide-native does not affect the results of doping tests.

Impact on the ability to drive and other vehicles, to work with moving mechanisms

Studies to study the effect of the drug on the ability to drive vehicles and control mechanisms have not been conducted. In the case of development of such adverse reactions as hyperkinesia or bronchospasm in the use of the drug, one should refrain from driving vehicles and controlling mechanisms, as well as from engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.
In the production of the drug at LLC "Nativa", Russia, indicate:

Form of issue

Solution for inhalation 0.25 mg / ml, 0.5 mg / ml.
To 2 ml in bottles for medicines or in bottles of colorless glass, sealed with rubber stoppers, crimped with aluminum or aluminum-plastic caps.
For 10 vials along with the instructions for use are placed in a pack of cardboard.

Storage conditions

In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Shelf life - 3 years.
Do not use the drug after the expiration date.

Leave conditions

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