Bekonaze

I N S T R U C T I O N for medical use of the medicinal product BECONASE® (BECONASE)

Composition:

Active substance: 1 dose (100 mg of suspension) contains beclometasone dipropionate 50 mcg;

Excipients: sodium carboxymethylcellulose – microcrystalline cellulose, anhydrous glucose, benzalkonium chloride, phenylethyl alcohol, polysorbate 80, purified water.

Pharmaceutical form. Nasal spray, suspension.

Main physicochemical properties: white, opaque suspension without any visible foreign particles.

Pharmacotherapeutic group.

Agents used in diseases of the nasal cavity. Anti-edematous and other preparations for local use in nasal cavity disorders. Corticosteroids. ATC code R01AD01.

Pharmacological Properties

Pharmacodynamics

After topical application, beclomethasone 17,21-dipropionate exerts a potent anti-inflammatory and vasoconstrictive effect. Beclomethasone dipropionate is a prodrug with weak affinity for glucocorticoid receptors. It is hydrolyzed by esterases to form the active metabolite beclomethasone-17-monopropionate, which has high local anti-inflammatory activity.

Beclomethasone dipropionate provides preventive baseline treatment of allergic rhinitis when used prior to allergen exposure. With regular use, beclomethasone dipropionate prevents recurrent allergic symptoms.

Pharmacokinetics

After intranasal administration of beclomethasone dipropionate, systemic absorption was determined by measuring the concentration of its active metabolite, beclomethasone 17-monopropionate (B-17-MP). The absolute bioavailability of this metabolite following intranasal administration is 44%. Beclomethasone dipropionate is rapidly cleared from the systemic circulation, and its plasma concentration after intranasal administration is not detectable (< 50 pg/mL). Metabolism occurs in all tissues via esterases. The main metabolite is the active compound (beclomethasone 17-monopropionate). Plasma protein binding is moderately high (87%). The elimination half-life in plasma is 0.5 hours for beclomethasone dipropionate and 2.7 hours for beclomethasone 17-monopropionate. After oral administration of beclomethasone dipropionate, approximately 60% of the dose is excreted in feces within 96 hours, primarily as free and conjugated polar metabolites. Approximately 12% of the dose is excreted in urine as free and conjugated polar metabolites. Renal clearance of beclomethasone dipropionate and its metabolites is negligible.

Clinical characteristics.

Indications.

Prophylaxis and treatment of perennial and seasonal allergic rhinitis.

Contraindications.

Hypersensitivity to the active substance or to any of the excipients listed in the section "Composition", in medical history. Tuberculosis, candidiasis, severe attacks of bronchial asthma. Pediatric age.

Interaction with other medicinal products and other forms of interaction.

Beclometasone is less dependent on CYP3A metabolism than some other corticosteroids, and interactions are generally unlikely; however, the possibility of systemic effects cannot be excluded when used concomitantly with strong CYP3A inhibitors (e.g., ritonavir, cobicistat). Therefore, caution is recommended and appropriate monitoring should be carried out when these drugs are used together.

Special precautions for use.

Infectious-inflammatory diseases of the nasal passages and paranasal sinuses are not a specific contraindication for the use of Beconase; however, appropriate therapy should be administered in such cases.

Beconase should be prescribed with caution to patients being transferred from systemic steroid therapy due to the possibility of adrenal suppression, as well as to patients with adrenal insufficiency.

Following recent nasal surgery or nasal trauma, and in the presence of nasal mucosal ulcers, consultation with a physician is recommended prior to using Beconase due to an increased risk of nasal septum perforation. Systemic effects of intranasal corticosteroids may occur, particularly with prolonged use of high doses. Such systemic effects are less likely than with oral corticosteroids and may vary between individual patients and with different corticosteroid products. Systemic effects may manifest as Cushing's syndrome, Cushingoid features, adrenal suppression, cataract, glaucoma, and (rarely) psychiatric and behavioral disorders, including psychomotor hyperactivity, sleep disturbances, restlessness, depression, or aggression (especially in children).

Treatment with doses higher than recommended may result in clinically significant adrenal suppression. If recommended doses of beclomethasone are exceeded, additional systemic corticosteroid therapy may be required during periods of stress or elective surgery.

The medicinal product contains benzalkonium chloride, which may cause bronchospasm and local reactions.

This product should not be used continuously for more than 1 month without medical supervision. If a patient is using other medicinal products in any dosage forms containing corticosteroids, or medications for asthma treatment, consultation with a physician is recommended before using Beconase.

Systemic effects, including growth suppression, may occur with overdosage of intranasal beclomethasone, individual hypersensitivity, or following recent systemic steroid therapy.

Although Beconase controls symptoms of seasonal allergic rhinitis in most cases, additional treatment may be necessary in some particularly severe cases associated with allergen exposure during summer, especially for ocular symptoms.

Visual disturbances.

Visual disturbances may occur during systemic and local use of corticosteroids. If a patient experiences symptoms such as blurred vision or other visual disturbances, they should consult an ophthalmologist to evaluate possible causes, including cataract, glaucoma, or rare conditions such as central serous chorioretinopathy (CSC), which has been reported during both systemic and local corticosteroid therapy.

Use during pregnancy or breastfeeding.

Pregnancy. There is insufficient evidence on the safety of using this medicinal product during pregnancy. Administration of corticosteroids to animals during pregnancy has been associated with fetal developmental abnormalities, including cleft palate and intrauterine growth retardation. Therefore, there may be a very small risk of such effects on the fetus. However, it should be noted that fetal developmental changes in animals occur after relatively high systemic exposure. Beconase nasal spray delivers beclomethasone dipropionate directly to the nasal mucosa, thereby minimizing systemic exposure.

Beclomethasone dipropionate should be avoided during pregnancy unless, in the opinion of the physician, the expected benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding. Specific studies investigating the passage of beclomethasone dipropionate into animal milk have not been conducted. It may be assumed that beclomethasone dipropionate passes into milk; however, the doses used for direct nasal spray have a low potential to significantly increase its concentration in breast milk.

Administration of the product to women during breastfeeding should only be considered if, in the opinion of the physician, the expected benefit to the mother outweighs the potential risk to the infant.

Fertility. There are no data available on the effect on fertility.

Ability to affect reaction speed when driving or operating machinery. No effect.

Method of Administration and Dosage.

Beconase should be used only for intranasal administration. Shake well before use.

Adults: 2 sprays into each nostril twice daily or 1 spray into each nostril 4 times daily.

The maximum daily dose should not exceed 8 sprays (400 mcg).

Regular use of the medication is required to achieve full therapeutic effect. Maximum relief is not achieved after the first few sprays.

Do not use for more than 3 months without consulting a physician.

Children. The medication is not recommended for use in children.

Overdose.

The only harmful effect that may occur after inhalation of large doses of the drug within a short period of time is suppression of the hypothalamic-pituitary-adrenal (HPA) axis function. This condition does not require emergency intervention. Beconase treatment may be continued at the recommended doses. Function of the hypothalamic-pituitary-adrenal system will recover within 1–2 days.

In such cases, management should be based on clinical indications or according to recommendations of the national toxicology center (if available).

There is no specific antidote for beclomethasone dipropionate overdose.

In case of overdose, appropriate supportive care should be provided as needed.

Adverse Reactions

Immune system side effects: Hypersensitivity reactions, including: (common: > 1/100 and < 1/10) rash, urticaria, pruritus, erythema; (very rare: < 1/10,000) angioedema, swelling of eyes, face, lips and throat, dyspnea and/or bronchospasm, anaphylactoid/anaphylactic reactions.

Nervous system side effects: (common: > 1/100 and < 1/10) unpleasant taste and smell sensations.

Eye disorders: (very rare: < 1/10,000) increased intraocular pressure, glaucoma or cataract; (frequency not known: cannot be estimated from available data) blurred vision.

Respiratory system side effects: (common: > 1/100 and < 1/10) dryness and irritation of nose and throat, epistaxis; cough, paradoxical bronchospasm, dyspnea; (very rare: < 1/10,000) isolated cases of nasal septum perforation.

With prolonged use of beclomethasone, especially in high doses, candidiasis, adrenal cortex suppression, osteoporosis, and growth retardation in children may occur.

Systemic effects of intranasal corticosteroids may occur when used in high doses over long periods.

Reporting suspected adverse reactions

Reporting of suspected adverse reactions after marketing authorization is very important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are encouraged to report any suspected adverse reactions via the automated pharmacovigilance information system of the State Enterprise "State Expert Centre of the Ministry of Health of Ukraine".

Website: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Do not store in the refrigerator.

Packaging.

100 doses or 180 doses in a polyethylene bottle connected with a metering device, nasal adapter and cap; 1 bottle per cardboard box.

Prescription status. Over-the-counter.

Manufacturer.

Richard Bittner AG / Richard Bittner AG.

Manufacturer's address and place of business.

Ossiacherstrasse 7, A-9560 Feldkirchen, Austria / Ossiacherstrasse 7, A-9560 Feldkirchen, Austria.