Pulmicort turbulence, inhalation powder 100 µg/dose, 200 doses

Composition

One dose contains the Active ingredient – budesonide 100 mcg.

Pharmacological action

Pharmacodynamicabudesonide with a strong local anti-inflammatory effect. The exact mechanism of action of glucocorticosteroids in the treatment of bronchial asthma is not fully clear. Anti-inflammatory effects, such as inhibition of the release of inflammatory mediators and cytokine-mediated immune response, may be most important. The affinity of budesonide for glucocorticoid receptors is 15 times higher than that of prednisone. The anti-inflammatory effect of budesonide is mediated by a reduction in the degree of airway obstruction during the early and late allergic response. Budesonide reduces the reactivity of the respiratory tract in response to inhalation of histamine and methacholine. The earlier treatment with budesonide is initiated after the diagnosis of persistent bronchial asthma, the greater improvement in lung function should be expected. A dose-dependent effect on plasma and urinary cortisol levels was shown when taking Pulmicort Turbuhalsra. At recommended doses, the drug has a significantly lower effect on adrenal function than prednisone at a dose of 10 mg, as shown in ACTH tests. The use of budesonide at a dose of up to 400 mcg per day in children over 3 years of age did not lead to systemic effects. Biochemical signs of a systemic effect of the drug may occur when taking the drug at a dose of 400 to 800 mcg per day. When exceeding the dose of 800 mcg per day, systemic effects of the drug are common. The use of glucocorticosteroids for the treatment of bronchial asthma can cause growth retardation. Initially, there was a slight, usually transient growth retardation (approximately 1 cm), usually during the first year of treatment. Long-term studies in clinical practice have shown that children and adolescents treated with inhaled budesonide on average reach the estimated height for adults. However, in a long-term double-blind study, mainly without titration of the budesonide dose to the minimum effective level, the average height of children and adolescents taking inhaled budesonide after reaching adulthood was 1.2 cm less than in the placebo group (see dosage and growth control recommendations in the sections “Dosage and use” and “Special Instructions”). Inhaled budesonide therapy once or twice a day has been shown to be effective in preventing physical exertion asthma. Pharmacokineticsabsorptioningalated budesonide is rapidly absorbed. After inhalation using a Turbuhaler, about 25-35% of the measured dose enters the lungs. The maximum concentration in the blood plasma is reached 30 minutes after inhalation. The systemic bioavailability of the drug is about 38% of the dose taken. Metabolism and distribution Plasma protein binding averages 90%. The volume of distribution of budesonide is approximately 3 l / kg. After absorption, budesonide undergoes intensive (more than 90%) biotransformation in the liver with the formation of metabolites with low glucocorticoid activity. The glucocorticosteroid activity of the main metabolites 6β-hydroxybudesonide and 16α-hydroxyprednisolone is less than 1% of the glucocorticosteroid activity of budesonide. Elimination Budesonide is mainly metabolized by the enzyme CYP3A4. Metabolites are excreted unchanged in the urine or in conjugated form. A small amount of unchanged budesonide is excreted in the urine. Budesonide has a high systemic clearance (about 1.2 l / min). The pharmacokinetics of budesonide are proportional to the amount of the administered dose of the drug. The pharmacokinetics of budesonide in children and patients with impaired renal function are unknown. In patients with liver diseases, the time spent in the body of budesonide may increase.

Indications

Bronchial asthma that requires maintenance therapy with corticosteroids to control the inflammatory process; chronic obstructive pulmonary disease (COPD).

Use during pregnancy and lactation

When pregnant women take budesonide, there is no increase in the risk of fetal malformations, however, the risk of their development cannot be completely excluded, so during pregnancy, the minimum effective dose of budesonide should be used, not forgetting the possibility of worsening the course of bronchial asthma.

The results of animal studies have shown that corticosteroids can cause abnormalities in fetal development, but these data cannot be extrapolated to people receiving corticosteroids at the recommended doses.

There are no data on the ingestion of budesonide in breast milk.

When prescribing the drug, the ratio of the intended benefit to the mother and the potential risk to the child should be taken into account.

Contraindications

Hypersensitivity to budesonide; children under 6 years of age.

With caution:  in the treatment of inhaled corticosteroids in patients with active or inactive forms of pulmonary tuberculosis, fungal, viral or bacterial infections of the respiratory system.

Side effects

From the respiratory tract:  oropharyngeal candidiasis, irritation of the pharyngeal mucosa, cough, hoarseness of voice.

Common:  angioedema.

From the side of the skin:  urticaria, rash, contact dermatitis.

From the respiratory tract:  bronchospasm.

Interaction

There was no interaction of budesonide with other drugs used in the treatment of bronchial asthma.

Ketoconazole (200 mg once daily) increases the plasma concentration of oral budesonide (3 mg once daily) by an average of 6 times when taken together.

When taking ketoconazole 12 hours after taking budesonide, the concentration of the latter in the blood plasma increased by an average of 3 times.

There is no information about such an interaction when taking inhaled budesonide, but it is assumed that in this case, too, an increase in the concentration of budesonide in blood plasma should be expected.

These medications should not be administered simultaneously due to lack of data.

If it is necessary to co-prescribe ketoconazole and budesonide, the time between taking medications should be increased to the maximum possible.

Reducing the budesonide dose should also be considered.

Other potential inhibitors of the CYP3A4 enzyme (e. g., itraconazole ) they also cause a significant increase in the plasma concentration of budesonide.

How to take, course of use and dosage

By inhalation. The dose is selected individually. Recommended doses of the drug in case of initiation of inhaled glucocorticoid therapy during severe exacerbations of bronchial asthma, as well as against the background of dose reduction or discontinuation of oral corticosteroids, are as follows: :

Children over 6 years of age — 100-800 mcg / day (the total daily dose can be divided into 2-4 inhalations). If the recommended dose does not exceed 400 mcg / day, the entire dose of the drug can be taken at 1 time (at a time).

In children, switching to a single dose of the drug should be carried out under the supervision of a pediatrician.

Adults-the usual dose is 200-800 mcg / day (the total daily dose can be divided into 2-4 inhalations). For the treatment of severe exacerbation of bronchial asthma, the daily dose can be increased to 1600 mcg.

If the recommended dose does not exceed 400 mcg / day, the entire dose of the drug can be taken at 1 time (at a time).

When selecting a maintenance dose, aim for the lowest effective dose.

The start time of the therapeutic effect after inhalation of 1 dose is several hours. The maximum therapeutic effect is achieved 1-2 weeks after treatment. Pulmicort ® Turbuhaler® It has a preventive effect on the course of bronchial asthma and does not affect the acute manifestations of the disease.

The best efficiency of budesonide was demonstrated when using Turbuhaler® compared to a similar dose of budesonide in the form of a metered-dose aerosol. If a patient is transferred in a stable condition from Pulmicort® in aerosol form to Pulmicort® Turbuhaler®, the possibility of reducing the daily dose of budesonide should be considered.

To enhance the therapeutic effect, an increase in the daily dose of Pulmicort® Turbuhaler®can be recommended. instead of combining the drug with oral corticosteroids, due to a lower risk of developing systemic effects.

Patients receiving oral corticosteroids

Discontinuation of oral corticosteroids should be carried out against the background of a stable state of health of the patient. Within 10 days, it is recommended to take a high dose of Pulmicort® against the background of taking oral corticosteroids in a selected dose. In the future, the dose of oral corticosteroids should be gradually reduced (for example,2.5 mg of prednisone or its analog) to the lowest possible level. In many cases, it is possible to completely abandon the use of oral corticosteroids.

There are no data on the use of budesonide in patients with renal insufficiency or impaired liver function. Taking into account the elimination of budesonide due to biotransformation in the liver, we can expect an increase in the duration of action of the drug in patients with severe cirrhosis of the liver.

Overdose

When an overdose of Pulmicort ® Turbuhaler® in doses significantly higher than recommended, no clinical manifestations occur.

With prolonged use of the drug in doses significantly higher than recommended, a systemic glucocorticoid effect may develop in the form of hypercorticism and suppression of adrenal function.

Special instructions

To minimize the risk of fungal infection of the oropharynx, the patient should be instructed to rinse his mouth thoroughly with water after each inhalation of the drug.

Co-use of budesonide with ketoconazole, itraconazole, or other potential CYP3A4 inhibitors should be avoided. If budesonide and ketoconazole or itraconazole or other potential CYP3A4 inhibitors have been prescribed, the time between drug use should be increased to the maximum possible.

Due to the possible risk of pituitary-adrenal function deterioration, special attention should be paid to patients who are switching from oral corticosteroids to Pulmicort®.

Special attention should also be paid to patients who have taken high doses of corticosteroids, or who have received the highest recommended doses of inhaled corticosteroids for a long time. In stressful situations, these patients may show signs and symptoms of adrenal insufficiency. In case of stress or in cases of surgical intervention, it is recommended to conduct additional therapy with systemic corticosteroids.

Special attention should be paid to patients who are being transferred from systemic to inhaled corticosteroids (Pulmicort ® Turbuhaler®), or in cases where a violation of pituitary-adrenal function can be expected. In such patients, the dose of systemic corticosteroids should be reduced with extreme caution and the hormonal function of the adrenal glands should be monitored.

Patients may also need to be prescribed oral corticosteroids during stressful situations, such as trauma, surgery, etc.

When switching from oral corticosteroids to Pulmicort® Turbuhaler®, patients may experience previously observed symptoms such as muscle pain or joint pain. In such cases, a temporary increase in the dose of oral corticosteroids may be necessary. In rare cases, symptoms such as fatigue, headache, nausea and vomiting may occur, indicating systemic insufficiency of corticosteroids.

Replacing oral corticosteroids with inhaled ones sometimes leads to existing allergies (for example, rhinitis and eczema) that were previously treated with systemic medications.

In children and adolescents who are treated with corticosteroids (regardless of the method of delivery) for an extended period, it is recommended to regularly monitor their growth indicators.

Patients should be instructed to contact their healthcare provider if the effectiveness of short-acting bronchodilator therapy decreases, as an independent increase in the frequency of use of the drug may lead to a delay in the appointment of adequate treatment. In case of sudden deterioration of the condition, the possibility of conducting a course of treatment with oral corticosteroids should be considered.

Influence on the ability to drive a car or other mechanisms. Pulmicort ® Turbuhaler® it does not affect the ability to drive a car or other mechanisms.

Instructions for proper use of the Turbuhaler®

The drug contained in the Turbuhaler ® enters the patient’s respiratory tract along with air flows when performing active inhalation through the Turbuhaler®mouthpiece.

Attention: It is important to convince the patient to carefully read the instructions for using Pulmicort ® Turbuhaler®.

To be sure that the optimal dose of the drug has reached the lungs, it is necessary to inhale deeply and strongly through the Turbuhaler ® mouthpiece.

Do not exhale through the mouthpiece under any circumstances.

After inhaling the required dose of the drug, rinse your mouth with water in order to minimize the risk of fungal damage to the oropharynx.

How to use Pulmicort ® Turbuhaler®

Turbuhaler® is a multi-dose inhaler that allows you to dose and inhale the drug in very small doses. When the patient inhales, the powder from Turbuhaler® is delivered to the lungs. Therefore, it is important that the patient inhales strongly and deeply through the mouthpiece.

Turbuhaler® very easy to use. You just need to follow the instructions below:

1. Unscrew and remove the cap.

2. Hold the inhaler vertically, with the dispenser facing down. Load the dose into the inhaler by turning the dispenser counterclockwise until it stops, and then turn the dispenser back to its original position until it clicks into place.

3. Exhale. Do not exhale through the mouthpiece. Remove the inhaler from your mouth before exhaling.

4. Gently squeeze the mouthpiece between your teeth, press your lips together, and inhale deeply and strongly through your mouth. The mouthpiece must not be chewed or clenched tightly with your teeth.

If more than one dose is required to be inhaled, repeat steps 2-5.

5. Close the inhaler cap.

6. Rinse your mouth with water.

IMPORTANT!

Never exhale through the mouthpiece. Always cap the inhaler tightly after use.

Since the amount of powder inhaled is very small, the patient may not feel the taste of the powder after inhalation. However, if he followed the instructions, he can be sure that he inhaled the necessary dose of the drug.

Cleaning up

Clean the outside of the mouthpiece regularly (once a week) with a dry cloth.

Do not use water or other liquids to clean the mouthpiece.

How do I know if the inhaler is empty?

When the red indicator appears in the dose window, it means that approximately 20 doses are left in the inhaler. The inhaler is empty when the red mark reaches the lower edge of the dose window of the indicator.

The sound that is heard when the inhaler is shaken is produced by the desiccant agent, not the medicine.

Form of production

Powder for inhalation dosed

Storage conditions

At temperatures below 30 °C

Shelf life

2 years

Active ingredient

Budesonide

Conditions of release from pharmacies

By prescription

Dosage form

powder for inhalation

Purpose

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor, For Children as prescribed by a doctor, for Nursing mothers as prescribed by a doctor

Indications

Bronchitis, Chronic obstructive pulmonary disease, Bronchial asthma