Budoster^® (Spray) Instructions for Use

ATC Code

R01AD05 (Budesonide)

Active Substance

Budesonide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Inhaled corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid for intranasal use. It has a pronounced anti-inflammatory and anti-allergic effect. When used in therapeutic doses, it has practically no resorptive effect. It does not have mineralocorticoid activity and is well tolerated with long-term use.

The drug has an inhibitory effect on the release of inflammatory reaction mediators, reduces the number of mast cells and eosinophilic granulocytes. Budesonide reduces the release of toxic proteins from eosinophils, free radicals from macrophages, and lymphokines from lymphocytes. It also reduces the binding of adhesion molecules to endothelial cells, thereby reducing the influx of leukocytes to the site of allergic inflammation. Budesonide increases the number of β-adrenergic receptors in smooth muscle.

The drug inhibits the activity of phospholipase 2A, which leads to inhibition of the synthesis of prostaglandins, leukotrienes, and complete Freund’s adjuvant (CFA), which induce an inflammatory reaction. Budesonide also inhibits the synthesis of histamine, leading to a decrease in its level in mast cells.

Budesonide reduces the severity of symptoms in allergic rhinitis, suppresses the late and early phases of the allergic reaction, and reduces inflammation in the upper respiratory tract. The therapeutic effect develops on average after 5-7 days.

Pharmacokinetics

Absorption

After inhalation of 400 mcg of budesonide, C_max in plasma is reached within 0.7 hours and is 1 nmol/L. Only about 20% of the intranasally administered dose enters the systemic circulation.

Distribution

Due to good tissue distribution and binding to plasma proteins, the apparent V_d is 301 L.

Metabolism

The systemic bioavailability of budesonide is low, as more than 90% of the absorbed drug is inactivated during a single-step metabolism in the liver. The glucocorticosteroid activity of metabolites does not exceed 1%.

Excretion

T_1/2 is 2-2.8 hours. It is excreted through the intestines in the form of metabolites – 10%, by the kidneys – 70%. The concentration of budesonide in blood plasma increases in patients with liver disease.

Indications

• Prophylaxis and treatment of seasonal and perennial allergic rhinitis;
• Vasomotor rhinitis;
• Nasal polyps.

ICD codes

Dosage Regimen

Spray

For adults and children over 6 years old, at the beginning of therapy, 100 mcg into each nasal passage 2 times/day. The usual maintenance dose is 50 mcg into each nostril 2 times/day or 100 mcg into each nostril once a day in the morning. The maintenance dose should be the lowest effective dose that eliminates the symptoms of rhinitis. The maximum single dose is 200 mcg (100 mcg into each nostril), the maximum daily dose is 400 mcg for no more than 3 months.

For the full therapeutic effect of Budoster^®, regular and correct application is required.

If a dose is missed, it should be taken as soon as possible, but no less than 1 hour before the next dose.

Children should use the drug under adult supervision.

Adverse Reactions

The side effects listed below may occur with the following frequency: very common (> 1/10), common (> 1/100 < 1/10), uncommon (> 1/1000 < 1/100), rare (> 1/10,000 < 1/1000), very rare (< 1/10,000, including isolated cases).

Local reactions: burning sensation; crusting on the nasal mucosa, dizziness. The risk of systemic effects should be considered, including adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, symptoms of hypercortisolism, cataracts, and glaucoma when using budesonide in high doses. Very common – irritation of the nasal mucosa. At the beginning of therapy, for a short time, rhinorrhea, excoriations may occur. Common – sneezing; tickling and dryness in the throat, pain in the nose and throat. Uncommon – nosebleed; candidiasis of the pharyngeal and nasal mucosa, particularly after prolonged therapy. Very rare – atrophy of the mucosa, ulceration of the nasal mucosa, perforation of the nasal septum; anosmia.

Allergic reactions: rare – allergic reactions (including dermatitis, rash, urticaria).

From the digestive system: rare – nausea, vomiting, gastralgia.

From the cardiovascular system: very rare – palpitations.

From the nervous system: rare – myalgia, drowsiness, headache.

From the respiratory system: very rare – cough, nasal congestion.

Contraindications

• Fungal, bacterial, and viral infections of the respiratory tract;
• Active form of pulmonary tuberculosis;
• Children under 6 years of age;
• Hypersensitivity to budesonide or any other component of the drug.

With caution: recent surgical interventions in the nasal cavity, recent nasal trauma, tuberculosis.

Use in Pregnancy and Lactation

The use of Budoster^® during pregnancy is allowed only if the expected benefit to the mother outweighs the possible risk to the fetus. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Pediatric Use

Contraindicated in children under 6 years of age.

For children over 6 years old, at the beginning of therapy, 100 mcg into each nasal passage 2 times/day. The usual maintenance dose is 50 mcg into each nostril 2 times/day or 100 mcg into each nostril once a day in the morning. The maintenance dose should be the lowest effective dose that eliminates the symptoms of rhinitis. The maximum single dose is 200 mcg (100 mcg into each nostril), the maximum daily dose is 400 mcg for no more than 3 months.

For the full therapeutic effect of Budoster^®, regular and correct application is required.

If a dose is missed, it should be taken as soon as possible, but no less than 1 hour before the next dose.

Children should use the drug under adult supervision.

With long-term use of intranasal glucocorticosteroids in children, dynamic monitoring of growth is recommended. If growth slows down, the pediatrician should reconsider the method of drug administration, aiming to reduce the dose and switch to the minimum therapeutic dose that allows control over the symptoms of the disease.

Special Precautions

The use of budesonide nasal spray is not recommended in patients with respiratory tract infections.

Patients should be informed that the effect of using budesonide nasal spray is achieved on average after 5-7 days.

If after three months of treatment the symptoms of the disease do not decrease, the drug should be discontinued.

When switching from treatment with systemic glucocorticosteroids to topical glucocorticosteroids, there is a risk of developing adrenal insufficiency, therefore, caution is required during the recovery period of the hypothalamic-pituitary-adrenal system function. The drug should be discontinued by gradually reducing the dose until the function of the hypothalamic-pituitary-adrenal system normalizes. During the dose reduction phase, some patients may experience symptoms of corticosteroid withdrawal, such as muscle and/or joint pain, apathy, depression. If such symptoms are detected, a temporary increase in the dose of systemic glucocorticosteroids may be required, followed by further withdrawal at a slower pace.

Regular administration of the drug is required to achieve a therapeutic effect in allergic rhinitis.

It is recommended to monitor the growth of children receiving prolonged treatment with intranasal glucocorticosteroids. If the child’s growth rate slows down, the dose of the nasal spray should be reduced.

Since glucocorticosteroids slow down wound healing, caution should be exercised when prescribing Budoster^® to patients who have recently suffered trauma or surgery in the nasal area.

Avoid getting Budesonide nasal spray into the eyes.

With long-term therapy with the drug, it is necessary to assess the condition of the nasal mucosa.

With long-term use of intranasal glucocorticosteroids in children, dynamic monitoring of growth is recommended. If growth slows down, the pediatrician should reconsider the method of drug administration, aiming to reduce the dose and switch to the minimum therapeutic dose that allows control over the symptoms of the disease.

Effect on the ability to drive vehicles and mechanisms

Budoster^® does not affect the ability to drive a car or operate machinery.

Overdose

Symptoms (with chronic overdose) acne, Cushing’s syndrome, dysmenorrhea.

Treatment gradual withdrawal of the drug.

Drug Interactions

Phenytoin, phenobarbital, rifampicin may reduce effectiveness, methandienone, estrogens, ketoconazole and other potent inhibitors of the CYP3A4 isoenzyme may increase it.

Storage Conditions

Store at a temperature not exceeding 25°C (77°F). Do not freeze.

Keep out of reach of children.

Shelf Life

Shelf life – 2 years. After opening the bottle, the shelf life is 3 months.

Do not use after the expiration date printed on the packaging.

Dispensing Status

The drug is dispensed by prescription.

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.