Budenit Steri-Neb suspension for inhalation dosed 0.25 mg/ml 2 ml ampoules 60 pcs. in Moscow

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The drug is for local use and has anti-allergic and anti-inflammatory effects. Enhances the production of phospholipase A2 ( lipocortin ), inhibits the process of release of arachidonic acid and the synthesis of its metabolic products. Reduces the exudation of the inflammatory process, reduces the intensity of granulation and infiltration, inhibits the migration of macrophages and the formation of chemotaxis, prevents the release of inflammatory mediators from cells, which plays an important role in the mechanism of symptoms of allergic chronic rhinitis .

The drug does not have MCS activity, is well tolerated by patients with long-term use, and does not have a resorptive effect.

Pharmacokinetics

Budesonide is quickly adsorbed after inhalation; the systemic bioavailability of the drug after inhalation through a nebulizer is about 15% of the administered dose. In the blood, the maximum concentration is reached on average after 30 minutes. Binding to blood proteins is high.

Biotransformation of budesonide occurs with the participation of the liver isoenzyme CYP3A4 . The main metabolites have extremely weak pharmacological activity. The drug is excreted by the kidneys, mainly in the form of metabolites (up to 70%) and in small quantities (about 10%) through the intestines.

Budenit Steri-Neb suspension for inhalation dosed 0.25 mg/ml 2 ml ampoules 60 pcs. in Moscow

Pharmacological action: Glucocorticosteroid with pronounced glucocorticoid and weak mineralocorticoid activity. In standard in vitro

and animal models have shown that the affinity of budesonide for specific glucocorticoid receptors exceeds that of cortisol by 200 times, and the local anti-inflammatory effect of budesonide is 1000 times higher than that of cortisol. When studying the systemic activity of budesonide in animal experiments, it was shown that when administered subcutaneously, the effect of budesonide was 40 times stronger than that of cortisol, and when administered orally, it was 25 times stronger.

Inhibits the synthesis of leukotrienes and PGs, inhibits the production of cytokines, prevents the migration and activation of inflammatory cells.

Increases the number of active beta-adrenergic receptors, restores the body's response to beta-adrenergic bronchodilators after their long-term use.

Rapidly absorbed from the lungs and gastrointestinal tract. When administered intranasally, very little is absorbed from the nasal mucosa (only 20% enters the systemic circulation). After inhalation, about 25% of the dose enters the alveoli. The part that enters the gastrointestinal tract is almost completely (90%) destroyed (inactive metabolites are formed) during the “first pass” through the liver. Bioavailability is 10% of the amount that enters the stomach; 25–30% of budesonide that enters the alveoli is absorbed. Cmax in the blood is reached 15–45 minutes after inhalation and intranasal administration. Plasma protein binding is 88%. Has high systemic clearance (84 l/h). T1/2 from plasma - 2.8 hours. Excreted in urine, partially in bile in the form of metabolites.

After oral administration, Cmax and Tmax values ​​are variable (Tmax in individual patients - from 30 to 600 minutes). Systemic availability after a single dose is higher in patients with Crohn's disease compared to healthy volunteers (21% and 9%, respectively), but approaches that of healthy volunteers after repeated doses. About 90% of absorbed budesonide is metabolized during the “first pass” through the liver with the participation of microsomal enzymes (mainly CYP3A4) to 2 main metabolites - 6-beta-hydroxy-budesonide and 16-alpha-hydroxyprednisolone (the glucocorticoid activity of the metabolites is less than 1/100 of the activity of budesonide , of the remaining amount, about 90% binds to albumin and is in an inactive state.

The effectiveness of budesonide (oral dosage form) has been shown for inflammatory bowel diseases, incl. with collagenous colitis.

The intranasal form is effective in the treatment of non-infectious inflammatory processes in the nasal cavity, to prevent the recurrence of polyps in the nasal cavity after their surgical removal and complete healing of the mucous membrane.

Carcinogenicity, mutagenicity, effect on fertility

The potential carcinogenicity of budesonide was assessed in long-term studies in rats and mice. No carcinogenic effect of budesonide was detected in mice when administered orally for 91 weeks at doses up to 200 mcg/kg/day (600 mcg/m2/day, approximately 0.1 MRDC based on body surface area).

A two-year study in Sprague-Dawley rats revealed a statistically significant increase in the incidence of gliomas in male rats receiving an oral dose of budesonide 50 mcg/kg/day (300 mcg/m2/day); similar changes were not observed in males at doses of 10 and 25 μg/kg/day (60 and 150 μg/m2/day) and in females at all doses tested. In 2 additional two-year studies in male Fischer and Sprague-Dawley rats at doses of 50 μg/kg/day (less than the MRV when converted to body surface area), there was no increase in the incidence of gliomas compared with other glucocorticoids (prednisolone and triamcinolone). However, with all 3 glucocorticoids studied, a statistically significant increase in the incidence of hepatocellular tumors in rats was observed.

No mutagenic or clastogenic properties of budesonide were detected in a number of standard tests.

With subcutaneous administration of budesonide to rats in doses up to 80 mcg/kg/day (less than the MRDC when calculated per body surface area), no adverse effects on fertility were recorded, but a decrease in weight gain in females was noted along with a decrease in the viability of pups in the prenatal period, at birth and during the lactation period. At doses of 5 mcg/kg/day (30 mcg/m2/day), similar effects were not observed.

Pregnancy

Like other corticosteroids, budesonide was teratogenic and embryotoxic in rabbits and rats. Experimental studies on animals (rats, rabbits) have shown that subcutaneous administration of budesonide leads to congenital malformations in the fetus (mainly skeletal defects).

Side effects

They manifest themselves mainly in the form of local reactions on the nasal mucosa (dryness, burning, irritation). Runny nose , atrophy or ulceration of the nasal mucosa, nosebleeds, sore throat, sneezing, sore throat, headache , allergic reactions on the skin, perforation of the nasal septum, myalgia , conjunctival hyperemia , nasal congestion, drowsiness , cough, nausea, vomiting, palpitations , candidiasis of the nasal and pharyngeal mucosa, growth retardation.

Budenit Steri-Neb, instructions for use (Method and dosage)

The drug is administered by inhalation through an inhaler-nebulizer . Before using it, you must carefully study the instructions and techniques for working with it.

The recommended daily dosage of the drug for severe bronchial asthma for inhaled GCS therapy, for adults and children over 12 years of age is 1–2 mg twice a day, a maintenance dose is 0.5–4 mg per day. At the age of 6 months to 12 years, the daily dosage ranges from 0.25 to 0.5 mg twice a day, the maintenance dose is 0.25–2 mg per day. If the prescribed dose is no more than 1 mg/day, then it can be taken in one dose.

As a rule, the maintenance dose is selected by the doctor individually, and when a therapeutic effect is achieved, it should be reduced to the lowest effective dose. If it is necessary to enhance the therapeutic effect, the dose of the drug can be increased or a combination of the drug with oral corticosteroids is recommended.

Budenit Steri-Neb 0.25 mg/ml suspension d/ing 2ml amp No. 20

Dosage

0.25 mg/ml

Active substance

Budesonide

Manufacturer

Norton Healthcare Limited (United Kingdom)

Shelf life

2 years

Storage conditions

At a temperature not exceeding 25 °C

Registration certificate number

LSR-004200/10 dated 07/24/2019

Compound

Characteristic

Description of the dosage form

A fine suspension of almost white color, practically odorless.

Pharmacokinetics

After inhalation, budesonide is rapidly absorbed. In adults, systemic bioavailability after inhalation of budesonide via nebulizer is approximately 15% of the total prescribed dose.

Cmax in blood plasma is 3.5 nmol/l and is achieved 30 minutes after the start of inhalation.

Plasma protein binding is 85–90%. Vd is 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%. Systemic clearance of the drug administered by inhalation is 0.5 l/min. Systemic clearance of metabolites is 1.4 l/min. T1/2 - about 2–2.8 hours.

Pharmacodynamics

GCS with a pronounced local anti-inflammatory and antiallergic 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 PGs, reduces inflammatory exudation and the production of cytokines, inhibits the migration of macrophages, reduces the severity of the processes of infiltration, granulation, formation of chemotaxis substance (which explains the effectiveness in delayed hypersensitivity reactions type), inhibits the release of inflammatory mediators from mast cells (immediate hypersensitivity reaction).

Budesonide restores the patient's sensitivity to bronchodilators, allowing them to reduce the frequency of their use, reduces swelling of the bronchial mucosa, mucus production, sputum formation and reduces airway hyperresponsiveness. Increases mucociliary transport. It is well tolerated during long-term treatment and does not have mineralocorticoid activity.

The time for the onset of the therapeutic effect after inhalation of one dose of the drug is several hours. The maximum therapeutic effect is achieved 1–2 weeks after treatment. Budesonide effectively prevents attacks of bronchial asthma of physical exertion, but does not stop an acute attack of bronchospasm.

Contraindications

hypersensitivity to budesonide or to any other component of the drug;

children's age (up to 6 months).

Carefully:

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

Use during pregnancy and breastfeeding

The use of budesonide during pregnancy is only possible if the benefit to the mother outweighs the possible risk to the fetus. If necessary, use the drug in the minimum effective dose.

There are no data on the excretion of budesonide in breast milk. Prescribing the drug during lactation is possible only under the supervision of a physician in cases where the expected benefit to the mother outweighs the possible risk to the child.

Directions for use and doses

Inhalation

using inhalers-nebulizers (see “Techniques of use” of these instructions).

Recommended doses of the drug in case of initiation of inhaled GCS therapy for severe bronchial asthma, as well as against the background of dose reduction or discontinuation of oral GCS, are as follows:

Adults (including the elderly) and children over 12 years of age: usually 1–2 mg 2 times daily. The maintenance dose is 0.5–4 mg/day.

Children from 6 months to 12 years: 0.25–0.5 mg 2 times a day. The maintenance dose is 0.25–2 mg/day. If the recommended dose does not exceed 1 mg/day, the entire dose of the drug can be taken at one time (at one 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.

Adults (including the elderly) and children over 12 years of age: 0.5–1 mg 2 times a day.

Children from 6 months to 12 years: 0.25–0.5 mg 2 times a day.

Table

Dose conversion table for patients receiving oral corticosteroids in terms of budesonide

If it is necessary to achieve an additional therapeutic effect, it can be recommended to increase the dose of Budenit Steri-Neb instead of combination with oral corticosteroids (to reduce the risk of developing systemic effects).

Stenosing laryngotracheitis (false croup)

. Children from 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.

Side effects

Often (≥1/100, but <1/10) - irritation and dryness of the pharyngeal mucosa, candidal stomatitis, hoarseness, cough, dry oral mucosa, unpleasant taste.

Rarely (≥1/10,000 but <1/1000) - nervousness, irritability, depression, behavioral disturbances, immediate and delayed hypersensitivity reactions (including rash, contact dermatitis, urticaria, angioedema and bronchospasm), skin bruising or thinning skin, headache, nausea, esophageal candidiasis.

When inhaled treatment of GCS, systemic effects may occur, especially with long-term treatment with high doses. The likelihood of such effects occurring is significantly less than with the treatment of oral corticosteroids. Possible systemic effects include adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, cataracts, and glaucoma.

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

As with other inhaled therapies, paradoxical bronchospasm may occur with rapid worsening of dyspnea after dosing. If a severe reaction occurs, alternative therapy should be considered.

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

Interaction

Pharmaceutical:

Budenit Steri-Neb can be mixed with 0.9% sodium chloride solution and “other” solutions intended for use via nebulizers, such as terbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglycate or ipratropium bromide.

Pharmacological:

The metabolism of budesonide is mainly carried out with the participation of the CYP3A4 isoenzyme. Taking 100 mg of ketoconazole 2 times a day increases the plasma concentration of orally administered budesonide at a dose of 10 mg once by an average of 7.8 times. There is no information on such interactions with inhaled dosage forms of budesonide, but a marked increase in plasma concentrations of the drug should be expected, therefore, inhibitors of the CYP3A4 isoenzyme such as ketoconazole and itraconazole may increase the systemic exposure of budesonide. Other strong CYP3A4 inhibitors are also likely to markedly increase budesonide plasma concentrations.

Pre-inhalation of β-adrenergic agonists dilates the bronchi, improves the entry of budesonide into the respiratory tract and enhances its therapeutic effect.

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

Methandienone and estrogens enhance the effect of budesonide.

Overdose

In case of acute overdose of budesonide, clinical manifestations usually do not occur.

Treatment:

drug withdrawal, inhalation of short-acting bronchodilators.

With long-term use in doses exceeding the recommended ones, a systemic GCS effect may develop in the form of hypercortisolism and suppression of adrenal function.

special instructions

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

Patients not receiving GCS

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

Patients on GCS therapy

Before transferring a patient from treatment with oral corticosteroids to treatment with Budenit Steri-Nab, the patient's condition should be relatively stable. After which the drug Budenit Steri-Neb is used in combination with the previously used dose of GCS for oral administration for about 10 days. Subsequently, the dose of oral corticosteroids should be gradually reduced (for example, by 2.5 mg of prednisolone or its equivalent every month) as far as possible to the lowest level. In most cases, oral GCS can be completely replaced with Budenit Steri-Neb.

Sometimes, during the transfer from treatment with oral corticosteroids to treatment with Budenit Steri-Neb, symptoms that were previously relieved by systemic drugs are observed: for example, rhinitis, eczema and muscle and joint pain. The occurrence of symptoms such as fatigue, headache, nausea and vomiting may indicate the development of systemic insufficiency of GCS. In such cases, it may even be necessary to temporarily increase the dose of oral corticosteroids.

Systemic side effects of inhaled corticosteroids may occur primarily when high doses are administered over a long period of time. The likelihood of this effect occurring is significantly less than with treatment with oral corticosteroids. 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 corticosteroids to the lowest dose at which effective disease control is maintained. It is recommended to regularly monitor growth in children receiving inhaled corticosteroids for an extended period of time. In case of growth retardation, treatment should be adjusted to reduce the dose of GCS for inhalation to the lowest dose at which effective control of bronchial asthma is maintained.

Oral administration of ketoconazole and itraconazole or other inhibitors of the CYP3A4 isoenzyme increases the systemic exposure of budesonide. Therefore, if combined use is necessary, they should be taken at maximum intervals. A dose reduction of budesonide should also be considered.

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

Impact on the ability to drive a vehicle and operate machinery.

The drug Budenit Steri-Neb does not have a negative effect on the ability to drive a vehicle or operate machinery. In case of rare adverse reactions from the nervous system, activities that require rapid psychomotor reactions should be avoided.

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. Inhalation time and dose of the drug depend on the air flow speed, the volume of the nebulizer chamber and the filling volume. Therefore, to inhale 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 adequate air flow.

Before using the drug, you must read the instructions from the nebulizer manufacturer.

1. Prepare the nebulizer according to its manufacturer's instructions.

2. Separate STERI-NEB (ampoule with a sterile solution) from the block by turning and pulling it (Fig. 1).

Picture 1.

3. Holding the ampoule vertically with the cap up, break off the cap (Fig. 2).

Figure 2.

4. Squeeze the solution into the nebulizer reservoir (Fig. 3).

Figure 3.

5. Use the nebulizer according to its manufacturer's instructions.

6. Rinse your mouth after finishing inhalation.

7. If a mask was used, it is necessary to rinse your facial skin.

8. The solution remaining unused in the nebulizer chamber should be discarded.

9. Wash the nebulizer thoroughly.

10. When using the drug, avoid getting the solution into the eyes.

Conditions for dispensing from pharmacies

On prescription.

BUDN-RU-00117-DOC-PHARM

Pharmgroups

Glucocorticosteroid for local use (Glucocorticosteroids)

Pharmaceutical actions

anti-inflammatory, antiallergic, antiexudative

Analogs of Budenit Steri-Neb

Level 4 ATX code matches:
Alvesco

Asmanex

Beclazon

Budesonide

Flixotide

Pulmicort

Aldecin

Apulein , Budecort , Gorakort , Benacort , Budesonide , Benarin Budenofalk , Buderin , Cicortide Cyclocaps , Budiair , Pulmicort , Tafen Nasal .

Reviews of Budenit Steri-Neb

Reviews of the drug from most patients are positive:

• “... The doctor diagnosed my child with chronic obstructive bronchitis, bronchial asthma is in question. We periodically undergo treatment in the allergy department”;
• “... After discharge, the doctor prescribed Budenit Steri-Neb inhalations for severe wheezing and coughing attacks. The drug stops attacks well, but we are afraid to take it often, because it contains hormones.”

Many patients on forums on the Internet are interested in: “Budenit Steri-Neb or Pulmicort - which is better?” If we talk about an inhalation suspension as a form of release of the drug for a nebulizer, then there are no significant differences. Same active ingredient, similar indications for use. However, there is a slight difference in the cost of these drugs in the pharmacy chain.

Price Budenit Steri-Neb, where to buy

The price of Budenit Steri-Neb suspension ampoules 0.25 mg/ml, 2 ml, No. 20 varies from 725 to 1120 rubles per package. Ampoules 0.5 mg/ml 2 ml No. 20 988 - 1280 rubles. You can buy Budenit Steri-Neb in the pharmacy chain of Moscow and other Russian cities without any difficulty.

• Online pharmacies in RussiaRussia

ZdravCity

• Budenit Steri-Neb susp.
  d/ing. dosed 0.25 mg/ml amp. 2ml 20pcs Ivex Pharmaceuticals Ukey Limited RUR 513 order
• Budenit Steri-Neb susp. d/ing. dosed 0.25 mg/ml 2 ml 60 pcs Norton Healthcare Limited

  RUB 1,591 order

• Budenit Steri-Neb susp. d/ing. dosed 0.5 mg/ml amp. 2ml 20pcs Ivax Pharmaceuticals Ukey Limited

  RUR 781 order

BUDENIT STERI-NEB SUSP 500 MCG/ML 2 ML No. 20

Compound

Active substance: budesonide
Excipients:

• polysorbate 80 - 0.2 mg;
• sodium chloride - 8.5 mg;
• sodium citrate dihydrate - 0.5 mg;
• citric acid monohydrate - 0.31 mg;
• disodium edetate - 0.1 mg;
• water for injection - up to 1 ml.

pharmachologic effect

Pharmacological action - antiexudative, antiallergic, anti-inflammatory.

Directions for use and doses

Inhalation using inhalers-nebulizers (see Techniques of use).

Recommended doses of the drug in case of initiation of inhaled GCS therapy for severe bronchial asthma, as well as against the background of dose reduction or discontinuation of oral GCS, are as follows:

Adults (including the elderly) and children over 12 years of age: usually 1–2 mg 2 times daily. The maintenance dose is 0.5–4 mg/day.

Children from 6 months to 12 years: 0.25–0.5 mg 2 times a day. The maintenance dose is 0.25–2 mg/day. If the recommended dose does not exceed 1 mg/day, the entire dose of the drug can be taken at one time (at one time).

The maintenance dose must be selected individually. When a therapeutic effect is achieved, the maintenance dose should be reduced to the lowest effective dose.

Adults (including the elderly) and children over 12 years of age: 0.5–1 mg 2 times a day.

Children from 6 months to 12 years: 0.25–0.5 mg 2 times a day.

If it is necessary to achieve an additional therapeutic effect, it can be recommended to increase the dose of Budenit Steri-Neb instead of combination with oral corticosteroids (to reduce the risk of developing systemic effects).

Below is a dose conversion table for patients receiving oral corticosteroids in terms of budesonide.

Table

Stenosing laryngotracheitis (false croup). Children from 6 months and older: the recommended dose is 2 mg/day at a time or in 2 divided doses, 1 mg at intervals of 30 minutes.

Technique of use

Ultrasonic nebulizers are not suitable for use with the drug Budenit Steri-Neb; the dose required by the patient may vary depending on the nebulizer used. Inhalation time and dose of the drug depend on the air flow speed, the volume of the nebulizer chamber and the filling volume. Therefore, to inhale 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 adequate air flow.

Before using the drug, you must read the instructions from the nebulizer manufacturer.

1. Prepare the nebulizer according to its manufacturer's instructions.

2. Separate the ampoule with the sterile solution from the block by turning and pulling it (Fig. 1).

3. Holding the ampoule vertically with the cap up, break off the cap (Fig. 2).

4. Squeeze the solution into the nebulizer reservoir (Fig. 3).

5. Use the nebulizer according to its manufacturer's instructions.

6. Rinse your mouth after finishing inhalation.

7. If a mask was used, it is necessary to rinse your facial skin.

8. The solution remaining unused in the nebulizer chamber should be discarded.

9. Wash the nebulizer thoroughly.

10. When using the drug, avoid getting the solution into the eyes.

Release form

Suspension for inhalation dosed, 0.25 mg/ml and 0.5 mg/ml. In LDPE ampoules, 2 ml. 5 amp. soldered to each other in the form of a block. 1 block in laminated foil. 4 or 12 blocks in a cardboard box.

Manufacturer

Ivax Pharmaceuticals UK Limited, Preston Brook, Runcorn, Cheshire WA7 3FA, United Kingdom.

Marketing Authorization Holder: Norton Healthcare Limited, trading as Ivax Pharmaceuticals UK, United Kingdom.

Address for receiving claims: 119049, Moscow, st. Shabolovka, 10, building 2, Business.

Tel/fax/35/36.

Conditions for dispensing from pharmacies

• On prescription.
• OXYGEN-BUD-INFblock-040914-MEDIA-647-030915

Storage conditions for the drug Budenit Steri-Neb

• At a temperature not exceeding 25 °C.
• Keep out of the reach of children.

Shelf life of the drug Budenit Steri-Neb

• 2 years.
• Do not use after the expiration date stated on the package.