Beclazon Eco, aerosol 250 mcg/dose 200 doses

Pharmacotherapeutic group: glucocorticosteroid for topical use

ATX code: R03VA01

Pharmacological properties

Pharmacodynamics. Beclomethasone is a glucocorticosteroid (GCS) and has weak tropism to GCS receptors. Under the action of enzymes it is converted into the active metabolite – beclomethasone-17-monopropionate (B-17-MP), which has a pronounced local anti-inflammatory effect. It reduces inflammation by reducing the formation of chemotaxis substance (effect on “late” allergy reactions), inhibits the development of an “immediate” allergic reaction (due to inhibition of production of arachidonic acid metabolites and reducing the release of inflammatory mediators from mast cells) and improves mucociliary transport. Beclomethasone reduces the number of mast cells in the bronchial mucosa, decreases epithelial edema, mucus secretion by bronchial glands, bronchial hyperresponsiveness, marginal accumulation of neutrophils, inflammatory exudate and lymphokine production, inhibits macrophage migration, reduces the intensity of infiltration and granulation. It increases the number of active beta-adrenoreceptors, restores the patient’s response to bronchodilators, allows reducing the frequency of their use. It has practically no resorptive effect after inhalation administration.

It does not relieve bronchospasm; the therapeutic effect develops gradually, usually after 5-7 days of course use of beclomethasone.

Pharmacokinetics. More than 25% of the dose of inhaled beclomethasone is deposited in the respiratory tract; the remaining amount is deposited in the mouth, pharynx, and swallowed. In the lungs, beclomethasone is extensively metabolized to the active metabolite B-17-MP prior to absorption. Systemic absorption of B-17-MP occurs in the lungs (36% of the pulmonary fraction) and in the gastrointestinal tract (26% of the ingested dose). The absolute bioavailability of unchanged beclomethasone and B-17-MP is approximately 2% and 62% of the inhaled dose, respectively. Beclomethasone is rapidly absorbed; time to reach maximum plasma concentration (Tmax) is 0.3 h. B-17-MP is more slowly absorbed, with a Tmax of 1 h. There is an approximately linear relationship between increasing inhaled dose and systemic exposure to beclomethasone.

Tissue distribution is 20 L for beclomethasone and 424 L for B-17-MP. The binding to plasma proteins is relatively high at 87%.

Beclomethasone and B-17-MP have high plasma clearance (150 l/h and 120 l/h, respectively). The elimination half-life is 0.5 h and 2.7 h, respectively.

Indications

Bronchial asthma, Chronic obstructive pulmonary diseaseBasic therapy for various forms of bronchial asthma in adults and children.

Active ingredient

Beclomethasone

Composition

Each inhaler contains 200 doses of the drug. Each dose of the drug contains the active ingredient beclomethasone dipropionate 50.0 µg/ 100.0 µg/ 250.0 µg; excipients: hydrofluralcane (HFA-134a) 75.86 mg/ 74.79 mg/ 71.75 mg; ethanol 2.09 mg/ 3.11 mg/ 6.00 mg.

How to take, the dosage

Beclazon Eco is intended for inhalation with an inhalation device (see “Instructions for the patient to use the inhalation device”). After each inhalation, rinse your mouth and throat thoroughly with water.

Perform regularly (even if there are no symptoms of the disease). The dose should be adjusted to individual clinical effectiveness, increasing until a clinical effect is seen or decreasing to the lowest effective dose. Many patients who are on a high-dose inhaled beclomethasone regimen will be able to reduce the dose or stop the inhaled beclomethasone altogether if they switch to a high-dose inhaled beclomethasone regimen.

The starting dose is determined by the severity of the bronchial asthma.

In mild bronchial asthma, the forced expiratory volume (EFV) or peak expiratory velocity (PEF) is greater than 80% of proper values, with a variation of less than 20% in EFV.

In a moderate course of bronchial asthma the PEF or PSV is 60-80% of the proper values, the daily variation of PSV is 20-30%.

In severe bronchial asthma, the SPH or PSV is less than 60% of the proper values, the daily variation in PSV is more than 30%.

The daily dose is divided into several doses (2-4 inhalations per day).

Adults and children 12 years of age and older

The recommended initial daily dose:

• mild bronchial asthma, 200-600 mcg/day (in 2 inhalations per day);
• Moderate bronchial asthma – 600-1000 mcg/day (2-4 inhalations/day);
• Severe bronchial asthma – 1000-2000 mcg/day (2-4 inhalations/day).

The standard maximum daily dose is 1000 mcg. In some very severe cases, the daily dose may be increased to 1500-2000 mcg (in 2-4 inhalations per day).

The treatment of bronchial asthma is based on a step-by-step approach – therapy is started according to the stage corresponding to the severity of the disease.

Inhaled GCSs are prescribed in the second step of therapy.

Stage 2. Basic therapy.

100-400 mcg 2 times daily.

Stage 3. Basic therapy.

The use of inhaled GCS in a high daily dose or in a standard daily dose, but in combination with long-acting inhaled beta2-adrenomimetics.

The recommended daily dose is 800-1600 mcg, in some cases the daily dose can be increased to 2000 mcg.

Stage 4. Severe bronchial asthma.

The recommended daily dose is 800-1600 mcg, the daily dose may be increased to 2000 mcg in individual cases.

Stage 5. Severe bronchial asthma.

The recommended daily dose is 800-1600 mcg, the daily dose may be increased to 2000 mcg in individual cases.

Children aged 4 to 12 years

The recommended initial daily dose is 100-200 mcg (for 2 inhalations per day). The standard maximum daily dose is 200 micrograms. In some very severe cases, the daily dose may be increased to 400 mcg (in 2-4 inhalations per day).

Beclazon Echo, which contains 250 micrograms of beclomethasone in 1 dose, is not intended for use in this group of patients.

Special patient groups

There is no need to adjust the dose in the elderly or in patients with renal or hepatic impairment.

Missing a dose of the drug

If you accidentally miss an inhalation, the next dose should be taken at the correct time according to the treatment regimen.

Injection can be done using special dispensers (spacers) to improve distribution of the drug in the lungs and reduce the risk of side effects.

Patient Instructions for Use of the Inhaler

When using the inhaler for the first time or if you have not used it for a while, test it by pressing the can valve and letting the dose of medicine in the air.

1. Remove the protective cap from the inhaler and make sure the outlet tube of the inhaler is clean. Hold the inhaler upright between your thumb and index finger, with your thumb on the bottom of the inhaler and your index finger on top of the aluminium cylinder.
2. Shake the aluminium cylinder vigorously up and down.
3. Let your mouth breathe out deeply. Grip the outlet tube of the inhalation device firmly with your lips. Whilst breathing in, press with your index finger on the dosing valve of the cylinder releasing the dose of Beclazon Echo, continue breathing in slowly.
4. Remove the inhalation device from your mouth and hold your breath for 10 seconds or as long as you feel comfortable. Slowly breathe out.
5. After inhalation, rinse your mouth with water, taking care not to swallow any aerosol that got into your oral mucosa during inhalation.
6. If more than one dose of medicine is required, wait for 1 minute and repeat all steps from step 2 to step 6.
7. Close the inhaler with the protective cap.

In steps 3 and 4, take your time. It is important to breathe in as slowly as possible as you release the dose of medicine. Practice in front of a mirror before application. If you notice “vapor” coming from the top of the can or from the corners of your mouth, start again with step 2.

Cleaning your inhaler

The inhaler should be cleaned at least once a week. Remove the aluminum canister from the inhaler. Gently rinse the inhalation device and the protective cap with warm water. Do not use hot water! Shake the inhalation device and protective cap to remove any residual water and dry them without using heating devices. Do not allow the aluminum canister to come in contact with water!

Interaction

Beclomethasone restores the patient’s response to beta-adrenomimetics, allowing a reduction in the frequency of their use. When used concomitantly with phenobarbital, phenytoin, rifampicin and other inducers of microsomal liver enzymes, the effectiveness of beclomethasone is reduced. When used concomitantly with methandienone, estrogens, beta2-adrenomimetics, theophylline, and systemic GCS, beclomethasone has increased efficacy. When used concomitantly beclomethasone increases the effect of beta-adrenomimetics.

Special Instructions

Beclazon Echo should be used to ensure that the patient is using the inhalation device correctly to ensure adequate dosing.

Patients using Beklazone Eco at home should be cautioned that if the effects of the usual dose become less effective or less prolonged, the dose or frequency of use should not be increased on their own, but should see a physician immediately.

Long-term use of beclomethasone at high doses (more than 400 mcg/day) causes oral and pharyngeal candidiasis, especially in patients who have previously had fungal infections, as evidenced by high blood levels of precipitating antibodies against Candida fungi. As a rule, the use of antifungal drugs contributes to the rapid elimination of fungal infection. The dose of beclomethasone should not be changed in this case.

If treatment with inhaled beclomethasone begins with oral GCS, reduction of the GCS dose should not begin until 1-2 weeks after starting concomitant use. Dose reduction scheme for oral GCS depends on the dose and duration of GCS use. Regular use of inhaled beclomethasone in most cases can reduce the dose of oral GCS. Patients taking 15 mg or less of prednisolone can usually switch completely to inhaled beclomethasone alone. For the first few months after switching to inhaled beclomethasone therapy, GGNS should be monitored closely to prevent suppression.

Patients with decreased adrenal function who are switched completely to inhaled beclomethasone treatment should always have a supply of GCS with them and carry a warning card informing them that they need systemic GCS in stressful situations. Once the stressful situation is over, the dose of GCS may be reduced or the GCS may be withdrawn.

An increase in the dose of GCS is required if there is a sudden and progressive worsening of the course of bronchial asthma. An indirect indicator of ineffectiveness of therapy is more frequent use of short-acting beta2-adrenomimetics.

A variety of allergic reactions, including allergic rhinitis and allergic dermatitis, may occur when switching patients from oral GKS to inhaled GKS, including beclomethasone, which did not manifest with systemic GKS therapy.

Beclomethasone for inhalation is intended for regular daily use, not for treatment of bronchospasm. Beta2-adronomimetics, including salbutamol, are used to relieve bronchospasm attacks. If the course of bronchial asthma is severe or if inhaled beclomethasone is not effective enough, its dose should be increased, and the use of oral GCS or, for example, the use of antibiotics in cases of infectious inflammation should be considered.

If paradoxical bronchospasm occurs, beclomethasone should be withdrawn, the patient should be evaluated, and another drug should be considered.

The treatment with inhaled beclomethasone should not be stopped abruptly.

Long-term use of inhaled beclomethasone at doses greater than 1.5 g/day may produce systemic reactions of various types, including symptoms of decreased adrenal function, reduced growth rate in children, decreased bone mineral density, cataracts, glaucoma. Therefore, when a therapeutic effect is achieved, the dose of inhaled beclomethasone should be reduced to the lowest effective dose that controls the course of the disease. Patients at high risk of adrenal insufficiency should be monitored by a physician.

Long-term use of beclomethasone in children should monitor their growth dynamics.

Cautions must be taken when using inhaled GCS in patients with active and inactive pulmonary tuberculosis.

The eyes should be protected from contact with Beclazon Echo.

The aluminum can of Beclazon Eco must not be pierced, disassembled or heated, even if empty.

Effects on ability to drive and operate machinery

Inhalation of beclomethasone has no effect on driving and engaging in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity to beclomethasone and other components of the drug; children under 4 years of age.

With caution

In glaucoma, systemic infections (bacterial, viral, fungal, parasitic), osteoporosis, pulmonary tuberculosis, liver cirrhosis, hypothyroidism, pregnancy, during breastfeeding.

Side effects

The frequency of side effects is classified according to the recommendations of the World Health Organization: very frequently – at least 10%; frequently – at least 1%, but less than 10%; infrequently – at least 0.1%, but less than 1%; rarely – at least 0.01%, but less than 0.1%; very rarely (including isolated cases) – less than 0.01%.

Infectious diseases:often, oral and upper respiratory tract and pharynx candidiasis (with long-term use in high doses over 400 mcg per day).

Allergic reactions: seldom – skin rash, skin itching, urticaria, erythema, angioedema, including edema of the para-orbital area, the mucous membrane of the oral cavity and pharynx, lips and face.

Endocrine system disorders: very rarely – oppression of hypothalamic-pituitary-adrenal system (GnA) (with prolonged use of high doses more than 1.5 g/day), including growth retardation in children.

Visual side: very rarely – cataracts, glaucoma.

As for the respiratory system, chest and mediastinum organs: often – hoarseness of the voice, irritation of the pharyngeal mucosa (use of spacer reduces the likelihood of these side effects); rarely – paradoxical bronchospasm (managed with inhaled beta2-adrenomimetics short-acting); very rarely – eosinophilic pneumonia.

Skeletal, muscular and connective tissue:very rarely – decrease in bone mineral density.

Effects due to systemic action:headache, nausea; bruising or thinning of the skin.

Overdose

Acute overdose of the drug may occur when a high single dose of more than 1 g is inhaled. The manifestation, in this case, of symptoms of inhibition of adrenal cortex function does not require emergency therapy, since the function is restored within a few days, which is confirmed by plasma cortisol levels. In chronic overdose (long-term treatment with a dose of more than 1.5 g), persistent suppression of adrenal cortical function may be observed. In such cases, it is recommended to monitor the reserve function of the adrenal cortex. In case of overdose, treatment with beclomethasone may be continued in doses sufficient to maintain the therapeutic effect.

Pregnancy use

Beclazon Eko should be used with special caution during pregnancy and breastfeeding only if the expected benefits to the mother outweigh the possible risk to the fetus and infant.

Similarities

Beclomethasone Eco Light Breathing, Beclomethasone, Beclomethasone-Aeronative