Budenit Steri-Neb, 0.25 mg/ml suspension 2 ml 20 pcs

Pharmacological group:

glucocorticosteroid for topical use.

The ATX code: R03BA02

Pharmacological action

Glucocorticosteroid (GCS) with pronounced local anti-inflammatory and anti-allergic action, budesonide increases production of lipocartin, 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, it inhibits macrophages migration, decreases intensity of granulation infiltration processes, 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 adsorbed after inhalation; in adults, the systemic bioavailability after inhaling budesonide via nebulizer is approximately 15% of the total dose administered.

The maximum concentration (Cmax) in plasma is 3.5nmol/litre and is reached 30 minutes after inhalation.

The binding to plasma proteins is 85-90%.

The volume of distribution is 3 l/kg.

Budesonide undergoes transformation with the participation of liver microsomal enzymes, primarily CYP3A4 isoenzyme. The main metabolites – 6-β-hydroxybudesonide and 16-ά-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.

The half-life (T1/2) is about 2-2.8 hours.

Indications

Active ingredient

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

Inhaled using nebulizer inhalers. Recommended doses of the drug Budenit Steri-Neb in case of initiation of inhaled GCS therapy for severe bronchial asthma, as well as against the background of dose reduction or withdrawal of oral GCS, are as follows:

If additional therapeutic effect is necessary, increasing the dosage of Budenit Steri-Neb may be recommended instead of combining with oral GCS (in order to decrease the risk of systemic effects).

Interaction

Pharmaceutical: Budesonide Steri-Neb can be mixed with 0.9% sodium chloride solution and other solutions designed for use with nebulizers, such as sterbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglycate or ipratropium bromide.

Pharmacological: budesonide is metabolized mainly with the participation of CYP3A4 isoenzyme. Administration of 100 mg ketoconazole 2 times daily increases plasma concentration of oral budesonide 10 mg once by an average of 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, CYP3A4 isoenzyme inhibitors such as ketoconazole and itraconazole may increase systemic exposure to budesonide. Other potent CYP3A4 inhibitors can probably also markedly increase the plasma concentration 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 a long 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 from the nervous system, activities requiring quick psychomotor reactions should be avoided.

In ultrasonic nebulizers are not suitable for use with Budenit Steri-Neb. The dose required by the patient may vary depending on the nebulizer 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. The nebulizer must be connected to an air compressor to create the appropriate airflow.

You must read the nebulizer manufacturer’s instructions before using the medication.

Synopsis

Contraindications

With caution: 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 overdose with budesonide clinical manifestations usually do not occur.

Treatment: drug withdrawal, inhalation of short-acting bronchodilators.

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

Pregnancy use

The use of budesonide during pregnancy is possible only if the benefit to the mother outweighs the possible risk to the fetus.

In case of necessity of use the drug is used in the minimum effective dose. There are no data on excretion of budesonide with breast milk.

The drug can only be given during lactation under medical supervision if the expected benefit to the mother outweighs the possible risk to the baby.

Similarities