Beclospir^® (Aerosol) Instructions for Use

Marketing Authorization Holder

Pharmaceutical Factory Of St. Petersburg, PJSC (Russia)

Contact Information

PHARMACEUTICAL FACTORY OF ST. PETERSBURG, PJSC (RUSSIA)

ATC Code

R03BA01 (Beclometasone)

Active Substance

Beclometasone (Rec.INN registered by WHO)

Dosage Forms

	Beclospir®	Metered dose inhalation aerosol 50 mcg/1 dose: 200 dose canisters with metering valves, mouthpieces
		Metered dose inhalation aerosol 100 mcg/1 dose: 200 dose canisters with metering valves, mouthpieces
		Metered dose inhalation aerosol 250 mcg/1 dose: 200 dose canisters with metering valves, mouthpieces

Dosage Form, Packaging, and Composition

Metered dose inhalation aerosol in the form of a suspension under pressure, forming a white spot when sprayed onto a glass slide.

Excipients: ethanol (absolute ethyl alcohol), hydrofluoroalkane (HFA-134a) – up to 14.02 g.

200 doses (14.02 g) – aluminum canisters (1) with metering valves, mouthpieces – cardboard packs.

Metered dose inhalation aerosol in the form of a suspension under pressure, forming a white spot when sprayed onto a glass slide.

Excipients: ethanol (absolute ethyl alcohol), hydrofluoroalkane (HFA-134a) – up to 14.02 g.

200 doses (14.02 g) – aluminum canisters (1) with metering valves, mouthpieces – cardboard packs.

Metered dose inhalation aerosol in the form of a suspension under pressure, forming a white spot when sprayed onto a glass slide.

Excipients: ethanol (absolute ethyl alcohol), hydrofluoroalkane (HFA-134a) – up to 14.02 g.

200 doses (14.02 g) – aluminum canisters (1) with metering valves, mouthpieces – cardboard packs.

Clinical-Pharmacological Group

Inhaled corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Topically applied glucocorticosteroid. Beclometasone dipropionate is a prodrug and has low affinity for glucocorticoid receptors. Under the action of esterases, it is converted into an active metabolite – beclometasone-17-monopropionate, which exerts a pronounced local anti-inflammatory effect by reducing the formation of chemotaxis substance (affecting delayed-type allergic reactions).

By suppressing the production of arachidonic acid metabolites and reducing the release of inflammatory mediators from mast cells, it inhibits the development of immediate-type allergic reactions. It improves mucociliary transport, reduces the number of mast cells in the bronchial mucosa, reduces epithelial edema, mucus secretion by bronchial glands, bronchial hyperreactivity, marginal neutrophil accumulation, inflammatory exudate, and lymphokine production, inhibits macrophage migration, and reduces the intensity of infiltration and granulation processes.

After inhalation administration, it has practically no resorptive effect. It does not relieve bronchospasm. The therapeutic effect develops gradually, usually after 5-7 days of course use.

By increasing active β-adrenergic receptors, it restores the patient’s response to bronchodilators, allowing to reduce the frequency of their use.

Pharmacokinetics

Absorption

More than 25% of the inhaled dose is deposited in the airways, the remaining amount is in the mouth, pharynx and is swallowed. In the lungs, before absorption, beclometasone dipropionate is intensively metabolized to the active metabolite beclometasone-17-monopropionate. Its systemic absorption occurs in the lungs (36% – pulmonary fraction), in the gastrointestinal tract (26% of the dose received by swallowing).

The absolute bioavailability of unchanged beclometasone dipropionate and beclometasone-17-monopropionate is about 2% and 62% of the inhaled dose, respectively. Beclometasone dipropionate is absorbed rapidly (T_max – 0.3 h), beclometasone-17-monopropionate – more slowly (T_max – 1 h).

Distribution

Plasma protein binding is relatively high – 87%. V_d in tissues for beclometasone dipropionate is 20 L and for beclometasone-17-monopropionate is 424 L.

Elimination

Beclometasone dipropionate and beclometasone-17-monopropionate have high plasma clearance (150 and 120 L/h, respectively). T_1/2 is 0.5 h and 2.7 h, respectively.

Indications

• Bronchial asthma of various forms in adults and children over 4 years of age (basic therapy).

ICD codes

Dosage Regimen

The drug is used by inhalation.

The dose is selected individually by increasing until a clinical effect appears or reducing to the minimum effective dose. The initial dose is determined by the severity of bronchial asthma. The daily dose is divided into several doses.

Adults and children aged 12 years and older: treatment of bronchial asthma is based on a stepwise approach – therapy is started according to the step corresponding to the severity of the disease.

Step 1. Recommended initial doses of the drug

mild bronchial asthma (forced expiratory volume /FEV/ or peak expiratory flow /PEF/ – more than 80%, daily PEF variability – less than 20%) – 200-600 mcg/day;

moderate bronchial asthma (FEV or PEF – 60-80%, daily PEF variability – 20-30%) – 600-1000 mcg/day;

severe bronchial asthma (FEV or PEF – 60%, daily variability – more than 30%) – 1000-1200 mcg/day.

Step 2. Basic therapy: 100-400 mcg 2 times/day.

Step 3. Basic therapy: inhaled glucocorticosteroids in high or standard dose, but in combination with inhaled long-acting β₂-adrenergic receptor agonists. Beclospir^® in high dose 800-1600 mcg/day, in some cases – up to 2000 mcg/day.

Step 4 ( severe bronchial asthma ). Beclospir^® – 800-1600 mcg/day, in some cases – megadoses up to 2000 mcg/day.

Step 5 ( severe bronchial asthma ). Beclospir^® is prescribed in a high dose (see step 3,4).

Children aged 4 to 12 years: the dose is up to 400 mcg/day in several doses.

Elderly patients, patients with renal and/or hepatic impairment dose adjustment is not required.

If an inhalation is accidentally missed, the next dose should be taken at the usual time according to the treatment regimen.

Adverse Reactions

From the respiratory system: upper respiratory tract candidiasis (the likelihood of development increases with doses greater than 400 mcg/day), dysphonia (hoarseness), irritation of the pharyngeal mucosa (using a spacer reduces the likelihood of their development), paradoxical bronchospasm (immediately relieved with an inhaled short-acting beta₂-adrenergic agonist).

From the gastrointestinal tract: oral candidiasis (the likelihood of development increases with doses greater than 400 mcg/day), nausea, unpleasant taste sensations.

Allergic reactions: hypersensitivity reactions, including rash, urticaria, itching, redness and swelling of the eyes, face, lips, and mucous membrane of the mouth and pharynx.

Other: systemic effects are possible, including headache, bruising or thinning of the skin, decreased adrenal cortex function, osteoporosis, growth retardation in children and adolescents, cataract, glaucoma.

Contraindications

• Hypersensitivity to the components of the drug.

Use with caution in glaucoma, systemic infections (bacterial, including pulmonary tuberculosis, viral, fungal, parasitic), osteoporosis, liver cirrhosis, hypothyroidism.

Use in Pregnancy and Lactation

During pregnancy and lactation (breastfeeding), Beclospir^® should be used with extreme caution only if the potential benefit to the mother outweighs the possible risk to the fetus and child.

Use in Hepatic Impairment

Use with caution in liver cirrhosis.

Patients with hepatic impairment do not require dose adjustment.

Use in Renal Impairment

Patients with renal impairment do not require dose adjustment.

Pediatric Use

The drug is used in children over 4 years of age.

It is recommended to regularly monitor the growth dynamics of children receiving inhaled glucocorticosteroids for a long time.

Geriatric Use

Elderly patients do not require dose adjustment.

Special Precautions

When prescribing the drug against the background of oral glucocorticosteroids, the dose of the latter remains the same. In this case, the patient should be in a relatively stable condition. Approximately after 1-2 weeks, the daily dose of the oral glucocorticosteroid begins to be gradually reduced according to a scheme depending on the duration of previous therapy and the initial dose of the glucocorticosteroid.

Regular use of inhaled glucocorticosteroids allows in most cases to cancel oral glucocorticosteroids (patients requiring no more than 15 mg of prednisolone can be completely switched to inhalation therapy), while in the first months after the transition, the patient’s condition should be carefully monitored until their pituitary-adrenal system recovers sufficiently to provide an adequate response to stressful situations (for example: trauma, surgery or infection).

When transferring patients from systemic glucocorticosteroids to inhaled ones, allergic reactions (for example, allergic rhinitis, eczema) that were previously suppressed by systemic drugs are possible.

Patients with reduced adrenal cortex function transferred to inhalation therapy should have a supply of glucocorticosteroids and always carry a warning card indicating that in stressful situations they need additional systemic administration of glucocorticosteroids (after the stressful situation is eliminated, the dose of glucocorticosteroids can be reduced again).

Sudden and progressive worsening of asthma symptoms is a potentially dangerous condition, often life-threatening, and requires an increase in the dose of glucocorticosteroids. An indirect indicator of therapy ineffectiveness is more frequent than before use of short-acting beta₂-adrenergic agonists.

If paradoxical bronchospasm develops, it is necessary to immediately stop using the drug, assess the patient’s condition, conduct an examination and prescribe therapy with other drugs.

With long-term use of any inhaled glucocorticosteroids, especially in high doses, systemic effects may be noted, but the likelihood of their development is significantly lower than with oral glucocorticosteroids.

Therefore, it is especially important that after achieving a therapeutic effect, the dose of inhaled glucocorticosteroids is reduced to the minimum effective dose that controls the course of the disease.

The drug at a dose of 1500 mcg/day does not cause significant suppression of adrenal function in most patients. Due to possible adrenal insufficiency when transferring a patient taking oral glucocorticosteroids to inhalation therapy, special caution is necessary and regular monitoring of adrenal cortex function indicators should be carried out.

Special caution should be exercised when treating patients with tuberculosis, both active and inactive, with inhaled glucocorticosteroids.

Before prescribing inhalation drugs, it is necessary to instruct the patient on the rules of their use, ensuring the most complete entry of the drug into the lungs. The development of oral candidiasis is most likely in patients with a high level of precipitating anti-candidal antibodies (indicating previous candidiasis). After inhalation, the mouth and throat should be rinsed with water. To treat candidiasis while continuing therapy with the drug, local antifungal agents can be used.

The drug is intended not for relieving attacks, but for regular daily use. For relieving attacks, short-acting β₂-adrenergic agonists (for example, salbutamol) are used.

In case of severe exacerbation of bronchial asthma or insufficient effectiveness of the therapy, the dose of inhaled beclometasone dipropionate should be increased and, if necessary, a systemic glucocorticosteroid and/or, in case of infection development, an antibiotic should be prescribed.

Abrupt discontinuation of the drug is not recommended.

It is necessary to protect the eyes from getting the drug; to prevent damage to the skin of the eyelids and nose, it is recommended to wash the face after inhalation.

The drug canister must not be punctured, disassembled or thrown into fire, even if it is empty. If the canister is cooled, it is recommended to remove it from the plastic case and warm it with hands for several minutes (at low temperatures the drug may be ineffective).

Use in pediatrics

It is recommended to regularly monitor the growth dynamics of children receiving inhaled glucocorticosteroids for a long time.

Effect on ability to drive vehicles and mechanisms

Data on the effect of the drug on the ability to drive a car/mechanisms are not available.

Patient instructions for using the inhaler

Check the operation of the inhaler before first use, as well as if it has not been used for some time.

1. Make sure there is no dust or dirt in the canister outlet tube.
2. Place the mouthpiece on the canister so that the canister outlet tube enters the hole in the mouthpiece, remove the protective cap.
3. Hold the canister in the mouthpiece vertically with the bottom up, placing your index finger on the bottom and your thumb on the mouthpiece. Shake the canister vigorously 3-4 times up and down.
4. Take the mouthpiece into your mouth, tightly wrapping your lips around it, and exhale completely through your nose (without straining).
5. While slowly taking a deep breath, press the bottom of the canister with your index finger, releasing a dose of the medicine. Continue to inhale slowly.
6. Remove the inhaler tube from your mouth and hold your breath for 10 seconds or as long as possible without straining. Exhale slowly.
7. If more than one dose of the drug is required, wait about a minute and then repeat the actions, starting from step 2. Put the cap back on the inhaler.

When performing steps 4 and 5, do not rush. At the moment of releasing the dose of the drug, it is important to inhale as slowly as possible. At first, you should practice in front of a mirror. If “steam” is observed coming out of the top of the canister or from the corners of the mouth, then you should start again from step 2.

Cleaning the inhaler

The inhaler should be cleaned at least once a week. Remove the metal canister from the plastic case and rinse the case and cap with warm water. Do not use hot water. Dry thoroughly without using heating devices. Place the canister back into the case and put on the cap. Do not immerse the metal canister in water.

Overdose

Symptoms acute overdose may lead to temporary decrease in adrenal cortex function; with chronic overdose, persistent suppression of adrenal cortex function may be noted.

Treatment in case of acute overdose does not require emergency therapy, because the function recovers within a few days, which is confirmed by the plasma cortisol level.

In case of chronic overdose, it is necessary to monitor the reserve function of the adrenal cortex. Treatment with the drug can be continued in doses sufficient to maintain the therapeutic effect.

Drug Interactions

There are no confirmed data on the interaction of beclometasone dipropionate with other drugs.

Storage Conditions

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

Shelf Life

Shelf life – 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.