Becotide (Aerosol) Instructions for Use

Marketing Authorization Holder

Glaxo Wellcome Production (France)

ATC Code

R03BA01 (Beclomethasone)

Active Substance

Beclometasone

Dosage Forms

	Becotide	Metered dose inhalation aerosol 50 mcg/1 dose: inhaler 200 doses
		Metered dose inhalation aerosol 250 mcg/1 dose: inhaler 200 doses

Dosage Form, Packaging, and Composition

Metered dose inhalation aerosol as a clear, colorless solution; the aluminum inhaler must be hermetically sealed with a metering valve and show no signs of corrosion.

Excipients: glycerol, anhydrous ethanol, norflurane (HFA-134a).

200 doses – aluminum inhalers (1) – cardboard packs.

Metered dose inhalation aerosol as a clear, colorless solution; the aluminum inhaler must be hermetically sealed with a metering valve and show no signs of corrosion.

Excipients: glycerol, anhydrous ethanol, norflurane (HFA-134a).

200 doses – aluminum inhalers (1) – cardboard packs.

Clinical-Pharmacological Group

Inhaled corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Inhaled glucocorticosteroid. Beclometasone dipropionate is a prodrug with low affinity for glucocorticosteroid receptors. Under the action of esterases, it is converted into an active metabolite, beclometasone-17-monopropionate, which exerts a pronounced local anti-inflammatory effect.

Pharmacokinetics

Absorption

When administered by inhalation (using a metered dose inhaler), unchanged beclometasone dipropionate is absorbed into the systemic circulation through the lungs, with negligible absorption of the swallowed portion of the drug. Even before absorption begins, beclometasone dipropionate is converted into its active metabolite, beclometasone-17-monopropionate. Systemic absorption occurs both from the lungs and from the gastrointestinal tract due to the swallowed portion of the drug. The absolute bioavailability of beclometasone-17-monopropionate from the lungs is approximately 60% of the nominal dose. Beclometasone dipropionate is rapidly absorbed, its C_max in plasma is observed at 0.3 hours. The plasma concentration of beclometasone-17-monopropionate increases more slowly, with a T_max of 1 hour. An increase in the inhaled dose is accompanied by an almost linear increase in the systemic concentration of the drug. The bioavailability of beclometasone dipropionate after oral administration is negligible; however, the bioavailability of beclometasone-17-monopropionate formed in the gastrointestinal tract is 40%.

Metabolism

Beclometasone dipropionate is very rapidly metabolized by esterases, which are present in most tissues. The main metabolite is the active metabolite beclometasone-17-monopropionate. Inactive minor metabolites, Beclomethasone-21-monopropionate and Beclomethasone, are also formed, but they do not constitute a significant part of the systemic drug content.

Distribution

At steady state, the V_d of beclometasone dipropionate averages 20 L, while that of beclometasone-17-monopropionate is much higher – 424 L. Plasma protein binding is relatively high – 87%.

Elimination

The elimination of beclometasone dipropionate and beclometasone-17-monopropionate is characterized by high plasma clearance (150 L/h and 120 L/h, respectively) with T_1/2 of 0.5 hours and 2.7 hours, respectively. After oral administration, approximately 60% of the beclometasone dipropionate dose is excreted in the feces, mainly as free and conjugated polar metabolites, within 96 hours. Approximately 12% of the dose is excreted in the urine as free and conjugated polar metabolites. The renal clearance of beclometasone dipropionate and its metabolites is negligible.

Indications

• Maintenance therapy of bronchial asthma in adults and children over 4 years of age.

ICD codes

Dosage Regimen

Becotide is intended for inhalation use only.

The doses of Becotide should be set individually.

Adults and children over 12 years of age: the drug is prescribed at an initial dose that depends on the severity of the disease.

Mild bronchial asthma – 200-600 mcg/day in divided doses.

Moderate bronchial asthma – 600-1000 mcg/day in divided doses.

Severe bronchial asthma – 1000-2000 mcg/day in divided doses.

Depending on the individual response, the drug dose can be increased or decreased to achieve the optimal effect.

Children aged 4 years and older: up to 400 mcg/day in divided doses.

Becotide should be prescribed to children at an initial dose corresponding to the severity of their condition. Depending on the individual patient response, the drug dose can be increased or decreased to achieve the optimal effect.

The maximum daily dose of the drug is 500 mcg.

For elderly patients, as well as patients with renal or hepatic impairment, no dose adjustment of the drug is required.

Patients should be aware of the prophylactic nature of the drug’s action and the need for its regular use even in the absence of symptoms of bronchial asthma.

If the patient feels that short-acting bronchodilators have become less effective or they require more inhalations than usual, they should consult a doctor. If patients find it difficult to coordinate pressing the canister of the metered dose inhaler with inhalation, Becotide can be inhaled through a spacer.

When treating young children, it is more convenient to use a “Babyhaler” spacer for inhalation of Becotide.

Adverse Reactions

The frequency of adverse reactions is presented according to the following gradation: very common (≥10%), common (≥1% and <10%), uncommon (≥ 0.1% and < 1%), rare (≥ 0.01%, < 0.1%), very rare (< 0.01%).

Local reactions: very common – candidiasis of the oral mucosa and pharynx (aphthous stomatitis), the likelihood of which increases with the use of Becotide in doses exceeding 400 mcg/day. This complication is most likely to develop in patients with a high level of antibodies to Candida in the blood, indicating a previous infection. Rinsing the mouth with water after each use of the inhaler may be of some help in prevention. To treat candidiasis during ongoing therapy with Becotide, topical antifungal agents can be used.

Allergic reactions uncommon – rash, urticaria, itching, erythema; very rare – swelling of the eyes, face, lips, pharynx.

Endocrine system: very rare – Cushing’s syndrome, cushingoid appearance, adrenal cortex suppression, growth retardation in children and adolescents, decreased bone mineral density.

Central nervous system: very rare – anxiety, sleep disorders, behavioral changes, including hyperactivity and irritability (mainly in children).

Respiratory system: common – hoarseness, irritation of the pharyngeal mucosa. Rinsing the mouth with water immediately after inhalation may be of some benefit in this case. Using a spacer reduces the likelihood of these side effects.

Very rare – paradoxical bronchospasm, which manifests as increased wheezing after inhalation of the drug. This condition should be immediately relieved with a fast-acting inhaled bronchodilator. The use of Becotide should be discontinued immediately and alternative therapy prescribed if necessary.

Organ of vision: cataract, glaucoma.

Contraindications

• Hypersensitivity to the components of the drug.

Use in Pregnancy and Lactation

The use of the drug during pregnancy and lactation (breastfeeding) is possible only if the potential benefit to the mother outweighs the possible risk to the fetus or infant.

Use in Hepatic Impairment

No dose adjustment of the drug is required for patients with hepatic impairment.

Use in Renal Impairment

No dose adjustment of the drug is required for patients with renal impairment.

Pediatric Use

The growth of children receiving long-term inhaled glucocorticosteroids should be regularly monitored.

Special Precautions

Becotide is not a means of relieving acute asthma attacks and is used for regular long-term treatment.

Asthma treatment should be carried out in accordance with a stepwise program. The effect of treatment should be monitored clinically and by examining lung function.

An increased need for short-acting β₂-adrenergic receptor agonists to control symptoms indicates a worsening of the condition. In such a case, the patient’s treatment plan should be reconsidered.

If the effect is insufficient or in case of a severe exacerbation of asthma, it is necessary to increase the dose of inhaled Becotide and, if necessary, prescribe systemic glucocorticosteroids, and in the presence of infection, antibiotics.

Sudden and progressive worsening of asthma symptoms is a potentially life-threatening condition and requires an increase in the dose of glucocorticosteroids.

The patient’s inhalation technique should be checked to ensure that pressing the inhaler canister is synchronized with inhalation and ensures optimal delivery of the drug to the lungs.

Systemic effects may occur with the use of any inhaled glucocorticosteroid, especially with long-term use in high doses. These effects are significantly more likely to occur with the prescription of oral glucocorticosteroids. Therefore, it is especially important to select the minimum dose of inhaled glucocorticosteroid that controls the course of the disease.

Due to the possible impairment of adrenal cortex function, transferring patients from treatment with oral steroids to inhaled Becotide should be carried out under close medical supervision and regular monitoring of adrenal function. When introducing inhaled Becotide into therapy, discontinuation of systemic steroid treatment should be gradual, and patients should be advised to carry a warning card stating that in stressful situations the patient needs additional systemic administration of glucocorticosteroids.

Sometimes switching from systemic glucocorticosteroids to inhaled administration may lead to the manifestation of previously suppressed forms of allergy, such as allergic rhinitis or eczema. Abrupt discontinuation of Becotide is not recommended.

As with the prescription of other inhaled glucocorticosteroids, special caution should be exercised when treating patients with active or inactive forms of pulmonary tuberculosis.

The drug contains small amounts of ethanol and glycerol. Within the range of therapeutic doses, the content of these substances is extremely low and does not pose a risk to patients.

Daily administration of the non-CFC propellant HFA-134a to various animal species for 2 years has shown that the substance used has no toxic effect even at very high concentrations, significantly exceeding those that could be used by patients.

Use in pediatrics

The growth of children receiving long-term inhaled glucocorticosteroids should be regularly monitored.

Effect on ability to drive vehicles and operate machinery

There are no data on the effect of Becotide on the ability to drive vehicles and engage in other potentially hazardous activities.

Overdose

Symptoms: a single inhalation of Becotide in doses exceeding the recommended ones may lead to a temporary decrease in adrenal cortex function, which does not require emergency therapy, as adrenal cortex function recovers within a few days, as confirmed by plasma cortisol level measurements.

However, exceeding the recommended doses over a long period of time may cause a more persistent decrease in adrenal function.

Treatment: in such cases, it is recommended to monitor the reserve function of the adrenal cortex. In case of overdose, treatment with Becotide can be continued at doses sufficient for symptomatic control of the condition.

Drug Interactions

Becotide contains a small amount of ethanol. There is a theoretical possibility of interaction with disulfiram or metronidazole, especially in predisposed patients.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C (86°F).

Shelf Life

The shelf life is 2 years.

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.