Pulmicort^® Turbuhaler (Powder) Instructions for Use

Marketing Authorization Holder

AstraZeneca AB (Sweden)

ATC Code

R03BA02 (Budesonide)

Active Substance

Budesonide

Dosage Forms

	Pulmicort® Turbuhaler®	Powder for inhalation, metered dose 100 mcg/1 dose: turbuhaler 200 doses
		Powder for inhalation, metered dose 200 mcg/1 dose: turbuhaler 100 or 200 doses

Dosage Form, Packaging, and Composition

Powder for inhalation, metered dose in the form of round granules from white to almost white in color, easily destroyed by the slightest mechanical impact; a small part may be present in the form of a powder.

200 doses – turbuhalers (1) consisting of a dosing device, a powder storage reservoir, a desiccant reservoir, a mouthpiece, and a cap – cardboard packs.

Powder for inhalation, metered dose in the form of round granules from white to almost white in color, easily destroyed by the slightest mechanical impact; a small part may be present in the form of a powder.

100 doses – plastic inhalers (1) consisting of a dosing device, a powder storage reservoir, a desiccant reservoir, a mouthpiece, and a cap – cardboard packs.
200 doses – plastic inhalers (1) consisting of a dosing device, a powder storage reservoir, a desiccant reservoir, a mouthpiece, and a cap – cardboard packs.

Clinical-Pharmacological Group

Inhaled corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid with pronounced local anti-inflammatory and anti-allergic action. Budesonide increases the production of lipocortin, which is an inhibitor of phospholipase A₂, inhibits the release of arachidonic acid, suppresses the synthesis of leukotrienes and prostaglandins, reduces inflammatory exudation and the production of cytokines, inhibits macrophage migration, reduces the severity of infiltration and granulation processes, the formation of chemotaxis substance (which explains the effectiveness in delayed-type hypersensitivity reactions), inhibits the release of inflammatory mediators from mast cells (immediate-type hypersensitivity reaction).

Budesonide restores the patient’s sensitivity to bronchodilators, allowing to reduce the frequency of their use, reduces swelling of the bronchial mucosa, mucus production, sputum formation and reduces airway hyperreactivity. Increases mucociliary transport. Well tolerated during long-term treatment, does not possess mineralocorticoid activity.

The onset of the therapeutic effect after inhalation of a single dose of the drug is several hours. The maximum therapeutic effect is achieved after 1-2 weeks of treatment. Budesonide effectively prevents exercise-induced bronchial asthma attacks but does not relieve an acute bronchospasm attack.

Pharmacokinetics

After inhalation, Budesonide is rapidly absorbed. In adults, the systemic bioavailability after inhalation of budesonide via a nebulizer is approximately 15% of the total prescribed dose. C_max in blood plasma is 3.5 nmol/L and is reached 30 minutes after the start of inhalation. Plasma protein binding is 85-90%. V_d is 3 L/kg. Budesonide undergoes biotransformation with the participation of hepatic microsomal enzymes, primarily the isoenzyme CYP3A4. 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 as metabolites – 70%, through the intestines – 10%. Systemic clearance of the inhalationally administered drug is 0.5 L/min. Systemic clearance of metabolites is 1.4 L/min. T_1/2 is 2-2.8 hours.

Indications

Treatment of bronchial asthma (as basic therapy; for insufficient effectiveness of beta₂-adrenergic agonists; to reduce the dose of oral glucocorticosteroids); treatment of COPD; stenosing laryngotracheitis (false croup).

ICD codes

Dosage Regimen

Budenit Steri-Neb is used by inhalation using nebulizer inhalers (see below – “Usage Technique”).

Recommended doses of the drug when initiating inhaled glucocorticosteroid therapy for severe bronchial asthma, as well as when reducing the dose or discontinuing oral glucocorticosteroids for adults (including the elderly) and children over 12 years – 1-2 mg 2 times/day, maintenance dose – 0.5-4 mg/day; for children from 6 months to 12 years – 0.25-0.5 mg 2 times/day, maintenance dose – 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 (as a single dose).

The maintenance dose must be selected individually. Upon achieving a therapeutic effect, the maintenance dose should be reduced to the lowest dose at which the patient has no symptoms of the disease: for adults (including the elderly) and children over 12 years – 0.5-1 mg 2 times/day; for children from 6 months to 12 years – 0.25-0.5 mg 2 times/day.

Dose conversion table for patients receiving oral glucocorticosteroids converted to Budesonide

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

For stenosing laryngotracheitis (false croup) in children aged 6 months and older, the recommended dose is 2 mg/day as a single dose or in 2 doses of 1 mg with an interval of 30 minutes.

Usage Technique

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 drug dose depend on the air flow rate, nebulizer chamber volume and fill volume. Therefore, to inhale 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 an appropriate air flow. Before using the medicinal product, it is necessary to read the manufacturer’s instructions for the nebulizer.

1. Prepare the nebulizer according to the manufacturer’s instructions.
2. Separate the Steri-Neb (ampoule with sterile solution) from the block by twisting and pulling it.
3. Holding the ampoule vertically upwards with the cap, break off the cap.
4. Squeeze the solution into the nebulizer reservoir.
5. Use the nebulizer according to the manufacturer’s instructions.

Rinse the mouth after finishing the inhalation. If a mask was used, the facial skin should be washed.

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

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

Adverse Reactions

From the respiratory system: often – irritation and dryness of the pharyngeal mucosa, hoarseness, cough. During inhalation therapy, there is a possibility of paradoxical bronchospasm with rapid increase in shortness of breath after dose administration.

From the digestive system: often – candidal stomatitis, dryness of the oral mucosa, unpleasant taste sensations; rarely – nausea, esophageal candidiasis.

From the nervous system: rarely – nervousness, excitability, depression, behavioral disorders, headache,

Allergic reactions: rarely – immediate and delayed-type hypersensitivity reactions (including rash, contact dermatitis, urticaria, angioedema and bronchospasm),

From the skin: rarely – appearance of skin bruises or thinning of the skin,

During inhalation treatment with glucocorticosteroids, systemic effects may occur, primarily during long-term treatment with high doses. The likelihood of such effects is significantly less than during treatment with oral glucocorticosteroids.

From the endocrine system: with long-term treatment in high doses, suppression of adrenal cortex function, growth retardation in children and adolescents, decreased bone mineral density, cataract, glaucoma are possible.

Contraindications

Children under 6 months of age; children over 6 months of age – depending on the dosage form used; hypersensitivity to budesonide.

With caution

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

Use in Pregnancy and Lactation

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

Data on the excretion of budesonide in breast milk are not available. The use of the drug during lactation is possible only under medical supervision when the expected benefit to the mother outweighs the potential risk to the child.

Use in Hepatic Impairment

The drug should be prescribed with caution in liver cirrhosis.

Pediatric Use

Contraindicated in children under 6 months of age. Use in older children is possible in dosage forms intended for this category of patients.

Geriatric Use

There are no instructions for restricting use in elderly patients.

Special Precautions

Drugs containing Budesonide are not intended for the rapid relief of bronchial asthma attacks; short-acting inhaled bronchodilators are recommended to relieve acute bronchospasm.

The systemic side effect of inhaled glucocorticosteroids may manifest primarily when high doses are administered over a long period of time. The likelihood of this effect is significantly less than during treatment with oral glucocorticosteroids. Possible systemic effects include adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, cataract and glaucoma. Therefore, it is very important to titrate the dose of inhaled glucocorticosteroids to the lowest dose at which effective disease control is maintained. It is recommended to regularly monitor the growth of children receiving inhaled glucocorticosteroids for a long period of time. In case of growth retardation, treatment should be adjusted to reduce the dose of inhaled glucocorticosteroids to the lowest dose that maintains effective control of bronchial asthma.

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.

Effect on ability to drive vehicles and mechanisms

In case of rare adverse reactions from the nervous system, activities requiring speed of psychomotor reactions should be avoided.

Drug Interactions

The metabolism of budesonide is mainly carried out with the participation of the isoenzyme CYP3A4. Taking ketoconazole at a dose of 100 mg 2 times/day increases the plasma concentration of orally taken budesonide at a dose of 10 mg as a single dose by an average of 7.8 times. Information on such interaction with inhaled dosage forms of budesonide is not available, but a significant increase in the plasma concentration of the drug should be expected, therefore, such inhibitors of the CYP3A4 isoenzyme as ketoconazole and itraconazole may increase the systemic exposure of budesonide. Other potent CYP3A4 inhibitors are also likely to significantly increase the plasma concentration of budesonide. If concomitant use is necessary, they should be taken with the maximum possible interval. The possibility of reducing the dose of budesonide should also be considered.

Preliminary inhalation of beta-adrenergic agonists dilates the bronchi, improves the delivery of budesonide to the airways and enhances its therapeutic effect.

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

Methandienone, estrogens enhance the effect of budesonide.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.