Budenit Steri-Neb, 0.5 mg/ml suspension 2 ml 20 pcs

Pharmacotherapeutic group: Glucocorticosteroid for topical use.

ATX code: R03BA02

Pharmacological properties

Pharmacodynamics. Glucocorticosteroid (GCS) with pronounced local anti-inflammatory and anti-allergic effects. 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 cytokine production, inhibits macrophage migration, it reduces intensity of the processes of infiltration and granulation, formation of chemotaxis substance (which explains its effectiveness with delayed-type hypersensitivity reactions), inhibits release of inflammatory mediators from mast cells (immediate-type hypersensitivity reactions).

Budesonide restores the patient’s sensitivity to bronchodilators, allowing to reduce the frequency of their use, reduces bronchial mucosal edema, mucus production, sputum formation and reduces airway hyperresponsiveness. Increases mucociliary transport. It is well tolerated with long-term treatment and has no mineralocorticoid activity.

The time of onset of therapeutic effect after inhalation of a single dose of the drug is several hours. The maximum therapeutic effect is reached 1-2 weeks after treatment. Budesonide effectively prevents attacks of bronchial asthma of physical stress, but does not stop an acute attack of bronchospasm.

Pharmacokinetics. Budesonide is rapidly absorbed after inhalation. In adults, systemic bioavailability after inhalation of budesonide via nebulizer is approximately 15% of the total dose administered. The maximum concentration (C_max) in plasma is 3.5 nmol/L and is reached 30 min after the start of inhalation.

The binding to plasma proteins is 85-90%. Volume of distribution is 3 l/kg.

Budesonide undergoes biotransformation with the participation of liver microsomal enzymes, primarily CYP3A4 isoenzyme. The main metabolites – 6-β-hydroxybudesonide and 16-α-hydroxyprednisolone have almost no biological activity (100 times less than budesonide).

It is excreted by the kidneys as metabolites – 70%, through the intestine – 10%. Systemic clearance of inhaled drug is 0.5 l/min. Systemic clearance of metabolites is 1.4 l/min. Period of half-life – 2-2.8 hours.

Indications

Bronchial asthma, Chronic obstructive pulmonary disease, Bronchitis, Cough

• Treatment of bronchial asthma (as baseline therapy; if β₂-adrenomimetics are not effective; To reduce the dose of oral GCS when budesonide is ineffective or cannot be used in an airway-pressure inhaler or powder inhaler.
• Treatment of chronic obstructive pulmonary disease (COPD).
• Stenotic laryngotracheitis (false croup).

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Active ingredient

Budesonide

Composition

1 ml contains:

Active substance:budesonide 0.25 mg and 0.50 mg.

Associates:
polysorbate-80 0.20 mg, sodium chloride 8.50 mg, sodium citrate dihydrate 0.50 mg, citric acid monohydrate 0.31 mg, diatrium edetate 0.10 mg, water for injection to 1.0 ml.

How to take, the dosage

Budenit Steri-Neb is used by inhalation with the help of nebulizer inhalers (see section “Techniques of Use” of these instructions).

The recommended doses of the drug when initiating inhaled glucocorticosteroid therapy for severe bronchial asthma, as well as against the background of dose reduction or withdrawal of oral glucocorticosteroids, are as follows:

Adults (including the elderly) and children over 12 years: usually 1-2 mg twice daily. Supportive dose is 0.5-4 mg/day.

Children 6 months to 12 years: 0.25-0.5 mg twice daily.

The maintenance dose is 0.25-2 mg/day. If the recommended dose is less than 1 mg/day, the entire dose can be taken at a time (one time).

The maintenance dose needs to be adjusted individually. When a therapeutic effect is achieved, the maintenance dose should be reduced to the lowest dose at which the patient is symptom-free.

Adults (including elderly) and children 12 years and older: 0.5-1 mg twice daily.

Children 6 months to 12 years: 0.25-0.5 mg twice daily.

Dose conversion table for patients receiving oral glucocorticosteroids converted to budesonide

If additional therapeutic benefit is needed, increasing the dose of Budenit Steri-Neb may be recommended instead of combining it with an oral GCS (to reduce the risk of systemic effects).

Stenotic laryngotracheitis (false croup)

Children 6 months and older: Recommended dose is 2 mg/day at a time or in 2 doses of 1 mg at 30-minute intervals.

Interaction

Pharmaceutical: Budesonide Steri-Neb may be mixed with 0.9% sodium chloride solution and with other solutions designed for use with nebulizers, e.g. terbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglycate or ipratropium bromide.

Pharmacological:The metabolism of budesonide is mainly mediated by the CYP3A4 isoenzyme. Administration of 100 mg ketoconazole 2 times daily increases the plasma concentration of orally administered budesonide in dose of 10 mg once on average by 7-8 times. There is no information on such interaction with inhaled dosage forms of budesonide, but a marked increase in plasma concentrations of the drug should be expected; therefore, such CYP3A4 isoenzyme inhibitors as ketoconazole and itraconazole may increase systemic exposure to budesonide. Other potent CYP3A4 inhibitors are also likely to markedly increase plasma concentrations of budesonide.

Preinhalation of beta-adrenomimetics dilates the bronchi, improves the entry of budesonide into the airways, and enhances its therapeutic effect.

Phenobarbital, phenytoin, rifampicin reduce efficacy (induction of microsomal liver enzymes).

Methandienone, estrogens increase the effect of budesonide.

Special Instructions

The drug Budenit Steri-Neb is not intended for rapid relief of bronchial asthma attacks, for relief of acute bronchospasm it is recommended to use inhaled bronchodilators of short action.

Patients not receiving GCS

Therapeutic effect usually occurs within 10 days. In patients with excessive mucus secretion in the bronchi, a short (about 2 weeks) additional treatment with oral GCS may be given initially. After a course of oral therapy, in many cases it is possible to completely discontinue oral GCS.

Patients on GCS therapy

Budenit Steri-Neb must be relatively stable before transferring a patient from oral GCS therapy to treatment with Budenit Steri-Neb. Thereafter, Budenit Steri-Neb is used in combination with the previously used dose of oral GCS for about 10 days. Thereafter, the dose of oral GCS should be gradually reduced (e.g., by 2.5 mg of prednisolone or its equivalent each month) to the lowest level possible. In most cases, oral GCS can be completely replaced with Budenit Steri-Neb.

Sometimes during conversion from oral GCS treatment to treatment with Budenit Steri-Neb, symptoms that were previously controlled with systemic medications occur, such as rhinitis, eczema, and muscle and joint pain. The occurrence of symptoms such as fatigue, headache, nausea, and vomiting may indicate the development of systemic GCS failure. In these cases, it may even be necessary to temporarily increase the dose of oral GCS.

The systemic side effect of inhaled GCS may occur primarily when high doses are administered over an extended period of time. The likelihood of this effect occurring is much lower than when treating with oral GCS. Possible systemic effects include adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, cataracts and glaucoma. Therefore, it is very important to titrate the dose of inhaled GCS to the lowest dose at which effective disease control is maintained. It is recommended that growth in children receiving inhaled GCS for an extended period of time be monitored regularly. If growth is delayed, treatment adjustment should be made to reduce the inhaled GCS dose to the lowest dose at which effective bronchial asthma control is maintained.

The oral administration of ketoconazole and itraconazole or other CYP3A4 isoenzyme inhibitors causes increased systemic exposure to budesonide. Therefore, if co-administration is necessary, they should be taken at the maximum interval. Decreasing the dose of budesonide should also be considered.

In order to minimize the risk of fungal stomatitis, the patient and/or the child’s parents should be informed to rinse the mouth with water after each inhalation of the drug.

Influence on driving ability and operating machinery

Budenit Steri-Neb has no adverse effect on driving ability and operating machinery. In case of rare adverse reactions of the nervous system, activities requiring quick psychomotor reactions should be avoided.

The 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 being used. Inhalation time and dose depend on the airflow rate, the volume of the nebulizer chamber and the filling volume. Therefore, an appropriate nebulizer as well as a mouthpiece and a special face mask must be used for inhalation of Budenit Steri-Neb. Nebulizer must be connected to an air compressor to create a proper air flow.
Before using the medicine you must read the instructions of the nebulizer manufacturer.
– Prepare the nebulizer according to the instructions of its manufacturer.
– Separate the STERI-NEB (ampoule with sterile solution) from the unit by turning and pulling it.
– Holding the ampoule vertically with the cap upwards, break off the cap.
– Pour the solution into the nebulizer reservoir.
– Use the nebulizer according to the instructions of its manufacturer.
– Rinse your mouth after inhalation. If a mask was used, the skin of the face should be rinsed.
– The solution left unused in the nebulizer chamber should be poured out.
– The nebulizer should be thoroughly cleaned.

Synopsis

Finely dispersed suspension of almost white color, almost odorless.

Contraindications

• High sensitivity to budesonide or any other component of the drug; age less than 6 months.

Cautions

Pulmonary tuberculosis, fungal, bacterial, parasitic and viral respiratory infections, liver cirrhosis, pregnancy, lactation.

Side effects

Frequently (≥1/100, < 1/10): irritation and dryness of pharyngeal mucosa, candidal stomatitis, hoarseness of voice, cough, dryness of oral mucosa, unpleasant taste sensations.

Rarely (≥1/10000, < 1/1000): nervousness, agitation, depression, behavior disorders, immediate and delayed-type hypersensitivity reactions (including rash, contact dermatitis, urticaria, angioedema, and bronchospasm), appearance of skin bruising or thinning of skin, headache, nausea, esophageal candidiasis.

Systemic effects can occur with inhaled GCS treatment, especially with prolonged high-dose treatment. The likelihood of these effects occurring is much lower than with oral GCS treatment. Possible systemic effects include adrenal suppression, stunted growth in children and adolescents, decreased bone mineral density, cataracts, and glaucoma.

The drug Budenit Steri-Neb contains 0.1 mg/ml of dinatrium edetate, which can cause bronchospasm at concentrations above 1.2 mg/ml.

As with other inhalation therapies, paradoxical bronchospasm may occur with rapid increase in dyspnea after administration of the dose. If a severe reaction occurs, alternative therapy should be prescribed.

In some cases, facial skin irritation occurs when using a nebulizer with a mask. To prevent irritation, the skin of the face should be rinsed with water after using the mask.

Overdose

In acute budesonide overdose clinical manifestations usually do not occur. Treatment – drug withdrawal, inhalation of short-acting bronchodilators. When prolonged use in doses higher than recommended, a systemic glucocorticosteroid effect in the form of hypercorticism and suppression of adrenal function may develop.

Pregnancy use

The use of budesonide during pregnancy is possible only if the benefit to the mother outweighs the possible risk to the fetus. If the use is necessary, the drug is administered in the minimum effective dose. There are no data on excretion of budesonide with breast milk. Administration of the drug during lactation is possible only under the supervision of a physician in case when the expected benefits to the mother exceed the possible risk to the child.

Similarities

Pulmicort turbuhaler, Pulmicort, Budenofalk, Tafen nasal, Budenit Steri-Neb, Budesonide