Pulmicort turbuhaler, powder for inhalation 200mcg/dose, 100 doses

topical glucocorticosteroid

ATX Code: R03BA02

Pharmacodynamics

Budesonide with a strong local anti-inflammatory effect.

The exact mechanism of action of glucocorticosteroids in the treatment of bronchial asthma is not fully understood. An anti-inflammatory effect, such as inhibiting the release of inflammatory mediators and a cytokine-mediated immune response, is perhaps the most important. The affinity of budesonide for glucocorticosteroid receptors is 15 times higher than that of prednisolone.

The anti-inflammatory effect of budesonide is mediated by a decrease in the degree of airway obstruction during the early and late allergic response. Budesonide decreases airway reactivity in response to inhaled histamine and methacholine.

The sooner a diagnosis of persistent bronchial asthma is established, treatment with budesonide is started, the greater the improvement in lung function should be expected.

A dose-dependent effect on the content of cortisol in plasma and urine was shown with the use of Pulmicort Turbuhalsra. In recommended doses, the drug has a significantly less effect on adrenal function than prednisone at a dose of 10 mg, as was shown in ACTH tests.

The use of budesonide at a dose of up to 400 mcg per day in children older than 3 years did not lead to systemic effects. Biochemical signs of the systemic effect of the drug can occur when taking the drug at a dose of 400 to 800 mcg per day. When a dose is exceeded 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.
An initially small, usually transient growth retardation (approximately 1 cm) was noted, 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, achieve a calculated growth for adults. 

However, in a long-term double-blind study, predominantly without titration of the dose of budesonide to the minimum effective, the growth of children and adolescents taking inhaled budesonide was 1.2 cm less on average than in the placebo group when they reached adulthood (see dosage and control recommendations growth in the sections "Dosage and Administration" and "Special Instructions").
Once or twice daily inhaled budesonide therapy has been shown to be effective in preventing asthma in physical effort.

Pharmacokinetics

Absorption

Inhaled budesonide is rapidly absorbed. After inhalation using Turbuhaler, about 25-35% of the measured dose enters the lungs. The maximum plasma concentration is reached 30 minutes after inhalation. 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 glucocorticosteroid activity. The glucocorticosteroid activity of the main metabolites of 6β-hydroxybudesonide and 16α-hydroxyprednisolone is less than 1% of the glucocorticosteroid activity of budesonide.

Breeding

Budesonide is metabolized primarily by the CYP3A4 enzyme. Metabolites are excreted unchanged in 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 is proportional to the magnitude of the administered dose of the drug.
The pharmacokinetics of budesonide in children and patients with impaired renal function is unknown. In patients with liver disease, the residence time of budesonide in the body may increase.

Bronchial asthma, requiring maintenance therapy of corticosteroids to control the inflammatory process;

chronic obstructive pulmonary disease (COPD).

Against the background of taking budesonide by pregnant women, there was no increased risk of fetal developmental abnormalities, however, the risk of their development cannot be completely excluded, therefore, during pregnancy, you should use the minimum effective dose of budesonide, not forgetting about the possibility of worsening the course of bronchial asthma.

Animal studies have shown that corticosteroids can cause abnormalities in the development of the fetus, but these data cannot be extrapolated to people receiving corticosteroids in the recommended doses.

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

When prescribing the drug, the ratio of the expected benefit to the mother and the potential risk to the child should be considered.

Hypersensitivity to budesonide; children under 6 years old.

Carefully:

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.

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

General: angioedema.

On the part of the skin: urticaria, rash, contact dermatitis.

From the respiratory tract: bronchospasm.

No interaction of budesonide with other drugs used in the treatment of bronchial asthma was observed.

Ketoconazole (200 mg once a day) increases the plasma concentration of oral budesonide (3 mg once a day) by an average of 6 times with co-administration.

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

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

You should not prescribe these drugs at the same time due to lack of data.

If necessary, the joint appointment of ketoconazole and budesonide, the time between doses should be increased to the maximum possible.

You should also consider reducing the dose of budesonide.

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

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 a background of dose reduction or withdrawal of oral corticosteroids, are as follows:

Children over 6 years old - 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 1 time (at a time).

In children, the transition 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 1 time (at a time).

When selecting a maintenance dose, you must strive to prescribe the minimum 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 ^®  has a prophylactic effect on the course of bronchial asthma and does not affect the acute manifestations of the disease.

It demonstrated a better efficacy of budesonide using turbuhaler ^®  compared to the same dose of budesonide in the form of metered aerosols. If a patient who is in stable condition is transferred 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, it is possible to recommend an increase in the daily dose of Pulmicort ^®  Turbuhaler ^®  instead of a combination of the drug with oral GCS, due to the lower risk of developing systemic effects.

Patients Receiving Oral GCS

Cancellation of oral GCS should be carried out against the background of a stable patient’s health. Within 10 days, it is recommended to take a high dose of Pulmicort ^® while  taking oral GCS in a selected dose. In the future, the dose of oral GCS should be gradually reduced (for example, 2.5 mg of prednisone or its analogue) to the lowest possible level. In many cases, it is possible to completely refuse to take oral GCS.

There is no data on the use of budesonide in patients with renal failure or impaired liver function. Taking into account the elimination of budesonide due to biotransformation in the liver, an increase in the duration of the drug in patients with severe cirrhosis can be expected.

With an overdose of Pulmicort ^®  Turbuhaler ^®  in doses significantly higher than recommended, clinical manifestations do not occur.

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

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

Co-administration 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, you should increase the time between doses to the maximum possible.

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

Also, special attention should be given to patients who took high doses of GCS, or for a long time received the highest recommended doses of inhaled GCS. In stressful situations, these patients may manifest 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.

Particular attention should be paid to patients who are transferred from systemic to inhaled corticosteroids (Pulmicort ^®  Turbuhaler ^® ), or in cases where a violation of the pituitary-adrenal function can be expected.

In such patients, with extreme caution, reduce the dose of systemic corticosteroids and control the hormonal function of the adrenal glands. Also, patients may require the appointment of oral corticosteroids during stressful situations, such as trauma, surgery, etc.

When switching from oral GCS 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 a feeling of fatigue, headache, nausea, and vomiting can be observed, indicating systemic GC deficiency.

Replacing oral GCS with inhaled ones sometimes leads to the manifestation of an existing allergy (for example, rhinitis and eczema), which were previously stopped by systemic drugs.

In children and adolescents receiving GCS treatment (regardless of the delivery method) for an extended period, it is recommended to regularly monitor growth indicators.

Patients should be instructed on the need to contact their doctor if the effectiveness of the therapy with short-acting bronchodilators decreases. an independent increase in the frequency of use of the drug can lead to a delay in the appointment of adequate treatment. In the event of a sudden deterioration in the condition, it is necessary to consider the possibility of a course of treatment with oral corticosteroids.

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

Instructions for the proper use of Turbuhaler ^®

The preparation contained in Turbuhaler ^® enters the patient's respiratory tract along with air currents when an active breath is taken through the mouthpiece of Turbuhaler ^® .

Caution: it is important to convince the patient to carefully read the instructions for use of Pulmicort ^®  Turbuhaler ^® .

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

Do not exhale through the mouthpiece under any circumstances.

After inhalation of the required dose of the drug, rinse your mouth with water in order to minimize the risk of fungal infections of 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 takes a breath, the powder from Turbuhaler ^{® is}  delivered to the lungs. Therefore, it is important that the patient takes a deep, deep breath through the mouthpiece.

Turbuhaler ^{® is}  very easy to use. You just need to follow the instructions below:

1. Unscrew and remove the cap.

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

3. Breathe out. Do not exhale through the mouthpiece. Before exhaling, remove the inhaler from the mouth.

4. Gently squeeze the mouthpiece with your teeth, squeeze your lips and inhale deeply and strongly through your mouth. The mouthpiece must not be chewed and gritted with teeth.

If inhalation of more than one dose is required, repeat steps 2–5.

5. Close the inhaler with a cap.

6. Rinse your mouth with water.

IMPORTANT!

Never exhale through the mouthpiece. Always close the inhaler with a cap after use.

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

Cleaning

Regularly (once a week), clean the mouthpiece from the outside with a dry cloth.

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

How to find out that the inhaler is empty?

If a red indicator appears in the dose window, there are approximately 20 doses left in the inhaler. The inhaler is empty when the red mark reaches the lower edge of the indicator dose window.

The sound that is heard when the inhaler is shaken is made by a drying agent, not a medicine.

Dosage powder for inhalation