Benacort^® (Powder) Instructions for Use

Marketing Authorization Holder

Pulmomed, CJS (Russia)

ATC Code

R03BA02 (Budesonide)

Active Substance

Budesonide (Rec.INN registered by WHO)

Dosage Form

Benacort®

Metered dose powder for inhalation 200 mcg/1 dose: "Cyclohaler" inhalers 100 doses or 200 doses

Dosage Form, Packaging, and Composition

Metered dose powder for inhalation fine-crystalline, white or almost white in color.

Excipients: sodium benzoate.

100 doses – "Cyclohaler" inhalers (1) – polyethylene bags (1) – cardboard packs.
200 doses – "Cyclohaler" inhalers (1) – polyethylene bags (1) – cardboard packs.

Clinical-Pharmacological Group

Inhaled corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

A 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 cytokine production, inhibits macrophage migration, reduces the severity of infiltration and granulation processes, the formation of chemotaxis substances (which explains its effectiveness in delayed-type hypersensitivity reactions), and inhibits the release of inflammatory mediators from mast cells (immediate-type hypersensitivity reaction).

Budesonide restores the patient’s sensitivity to bronchodilators, allowing for a reduction in their frequency of use, reduces bronchial mucosal edema, mucus production, sputum formation, and reduces airway hyperreactivity. It enhances mucociliary transport. It is well tolerated during long-term treatment and 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. The 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%. The 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). It is excreted by the kidneys as metabolites – 70%, and through the intestines – 10%. The systemic clearance of the inhalationally administered drug is 0.5 L/min. The systemic clearance of metabolites is 1.4 L/min. The 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

Benacort is used by inhalation using dry powder inhalers (see below – “Instructions for Use”).

The 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 are 1-2 mg twice daily, maintenance dose is 0.5-4 mg/day; for children from 6 months to 12 years – 0.25-0.5 mg twice daily, 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 (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 twice daily; for children from 6 months to 12 years – 0.25-0.5 mg twice daily.

Table for converting doses for patients receiving oral glucocorticosteroids converted to Budesonide

If it is necessary to achieve an additional therapeutic effect, an increase in the dose of Benacort can be recommended instead of 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 a 30-minute interval.

Instructions for Use

Ultrasonic nebulizers are not suitable for use with Benacort. The dose required by the patient may vary depending on the nebulizer used. The inhalation time and drug dose depend on the airflow rate, nebulizer chamber volume, and fill volume. Therefore, to inhale Benacort, 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 airflow. Before using the medicinal product, 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 by 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, wash the skin of the face.

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

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

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

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),

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 with treatment with oral glucocorticosteroids.

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 use is necessary, the drug should be 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 restrictions for 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. The likelihood of this effect is significantly less than with 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. 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 of the need to rinse the mouth with water after each inhalation of the drug.

Effect on ability to drive vehicles and machinery

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

Drug Interactions

The metabolism of budesonide occurs mainly with the participation of the isoenzyme CYP3A4. Taking ketoconazole at a dose of 100 mg twice daily increases the plasma concentration of orally administered budesonide at a single dose of 10 mg 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 25°C (77°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.