Pharmacotherapeutic group: Glucocorticosteroid for local use
pharmachologic effect
GCS with a pronounced local anti-inflammatory and anti-allergic effect. Budesonide increases the production of lipocortin, which is an inhibitor of phospholipase A2, inhibits the release of arachidonic acid, inhibits the synthesis of leukotrienes and prostaglandins, reduces inflammatory exudation and production of cytokines, inhibits the migration of macrophages, reduces the severity of infiltration and granulation processes, the formation of chemotaxis substance (which explains the effectiveness in delayed hypersensitivity reactions). type), inhibits the release of inflammatory mediators from mast cells (immediate type hypersensitivity reaction).
Budesonide restores the patient’s sensitivity to bronchodilators, allowing to reduce the frequency of their use, reduces swelling of the bronchial mucosa, mucus production, sputum production and reduces airway hyperreactivity. Increases mucociliary transport. It is well tolerated during long-term treatment, does not have mineralocorticoid activity.
The time of onset of the therapeutic effect after inhalation of a single dose of the drug is several hours. The maximum therapeutic effect is achieved 1-2 weeks after treatment. Budesonide effectively prevents asthma attacks of physical exertion, but does not stop an acute attack of bronchospasm.
Pharmacokinetics
After inhalation, budesonide is rapidly absorbed. In adults, systemic bioavailability after inhalation of budesonide through a nebulizer is approximately 15% of the total administered dose. Cmax in plasma is 3.5 nmol / l and is reached 30 minutes after the start of inhalation. Plasma protein binding – 85-90%. Vd – 3 l/kg. Budesonide undergoes biotransformation with the participation of microsomal liver enzymes, primarily the CYP3A4 isoenzyme. The main metabolites – 6-β-hydroxybudesonide and 16-α-hydroxyprednisolone are practically devoid of biological activity (100 times less than budesonide). Excreted by the kidneys in the form of metabolites – 70%, through the intestines – 10%. The systemic clearance of the inhaled drug is 0.5 l/min. Systemic clearance of metabolites – 1.4 l / min. T1 / 2 – 2-2.8 hours
Indications of the active substances of the drug Budesonide Easyhaler
Treatment of bronchial asthma (as basic therapy; with insufficient effectiveness of beta2-agonists; to reduce the dose of oral corticosteroids); COPD treatment; stenosing laryngotracheitis (false croup).Dosing regimen
The method of application and dosing regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. Compliance of the dosage form of a particular drug with indications for use and dosing regimen should be strictly observed.
Budenit Steri-Neb is used by inhalation with the help of inhalers-nebulizers (see below – “Technique of use”).
Recommended doses of the drug in case of inhalation GCS therapy in case of severe bronchial asthma, as well as against the background of dose reduction or discontinuation of oral GCS for adults (including the elderly) and children over 12 years old – 1-2 mg 2 times / day, maintenance dose – 0.5-4 mg / day; for children from 6 months to 12 years old – 0.25-0.5 mg 2 times / day, maintenance dose – 0.25-2 mg / day. In the event that the recommended dose does not exceed 1 mg / day, the entire dose of the drug can be taken at a time (at a time).
The maintenance dose must be selected individually. When a therapeutic effect is achieved, the maintenance dose should be reduced to the lowest dose at which the patient has no symptoms of the disease: for adults (including the elderly) and children over 12 years old – 0.5-1 mg 2 times / day; for children from 6 months to 12 years – 0.25-0.5 mg 2 times / day.
Dose conversion table for patients receiving oral corticosteroids in terms of budesonide
Dose (mg) of budesonide taken by mouth Budenit Steri-Neb
0.5 mg/2 ml (0.25 mg/ml)
volume (ml) Budenit Steri-Neb
1 mg/2 ml (0.5 mg/ml)
volume (ml)
0.25 1 –
0.5 2 1
0.75 3 –
1 4 2
1.5 6 3
2 8 4
If it is necessary to achieve an additional therapeutic effect, an increase in the dose of Budenit Steri-Neb can be recommended instead of a combination with oral corticosteroids (to reduce the risk of systemic effects).
With stenosing laryngotracheitis (false croup) for children aged 6 months and older, the recommended dose is 2 mg / day at a time or in 2 doses of 1 mg with an interval of 30 minutes.
Technique of use
Ultrasonic nebulizers are not suitable for use with Budenit Steri-Neb. The dose required by the patient may vary depending on the nebulizer used. The time of inhalation and the dose of the drug depend on the air flow rate, the volume of the nebulizer chamber and the filling volume. Therefore, for inhalation of the drug Budenit Steri-Neb, it is necessary to use an appropriate nebulizer, as well as a mouthpiece and a special face mask. The nebulizer must be connected to an air compressor to create the correct airflow. Before using the drug, you must read the instructions of the manufacturer of the nebulizer.
Prepare the nebulizer according to the manufacturer’s instructions.
Separate Steri-Neb (ampoule with sterile solution) from the block, to do this, turn and pull it.
Holding the ampoule vertically upwards with the cap, break off the cap.
Squeeze the solution into the nebulizer reservoir.
Use the nebulizer according to the manufacturer’s instructions.
Rinse your mouth after the end of inhalation. If a mask was used, it is necessary to wash the skin of the face.
The solution remaining unused in the nebulizer chamber should be discarded. Wash the nebulizer thoroughly.
When using the drug, avoid contact with the solution in the eyes.
Side effect
From the respiratory system: often – irritation and dryness of the mucous membrane of the pharynx, hoarseness, cough. With inhalation therapy, there is a possibility of paradoxical bronchospasm with a rapid increase in dyspnea after a dose.
From the digestive system: often – candidal stomatitis, dryness of the oral mucosa, unpleasant taste sensations; rarely – nausea, esophageal candidiasis.
From the nervous system: rarely – nervousness, irritability, depression, behavioral disorders, headache,
Allergic reactions: rarely – immediate and delayed hypersensitivity reactions (including rash, contact dermatitis, urticaria, angioedema and bronchospasm),
On the part of the skin: rarely – the appearance of skin bruises or thinning of the skin,
With inhaled treatment with corticosteroids, systemic effects may occur, especially with long-term treatment with high doses. The likelihood of such effects is much less than in the treatment of corticosteroids for oral administration.
On the part of the endocrine system: with long-term treatment at high doses, suppression of the function of the adrenal cortex, growth retardation in children and adolescents, a decrease in bone mineral density, cataracts, and glaucoma are possible.
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