Beclomethasone, inhalation aerosol 250 µg/dose, 200 doses

Composition

1 dose of the drug contains: Active ingredient:  Beclomethasone dipropionate-0.25 mg (based on 100% substance)Auxiliary substances: ethanol 96% 10.5 mg, norflurane (tetrafluoroethane) 74.4 mg. Each inhaler contains 200 doses.

Pharmacological action

Beclomethasone dipropionate is a prodrug and has a weak tropicity to corticosteroid receptors. Under the action of esterases, it is converted to the active metabolite – Beclomethasone-17-monopropionate (B-17-MP), which has a pronounced local anti-inflammatory effect. Reduces inflammation by reducing the formation of the chemotaxis substance (the effect on “late” allergy reactions), inhibits the development of an” immediate ” allergic reaction (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells), and improves mucociliary transport. Beclomethasone reduces the number of mast cells in the bronchial mucosa, reduces epithelial edema, mucus secretion by bronchial glands, bronchial hyperreactivity, marginal accumulation of neutrophils, inflammatory exudate and lymphokine production, inhibits macrophage migration, and reduces the intensity of infiltration and granulation processes. Increases the number of active beta-adrenergic receptors, restores the patient’s response to bronchodilators, and reduces the frequency of their use. Practically has no resorptive effect after inhalation use. It does not stop bronchospasm, the therapeutic effect develops gradually, usually after 5-7 days of course application of Beclomethasone dipropionate. In lung tissue, Beclomethasone dipropionate is rapidly hydrolyzed to Beclomethasone monopropionate, which in turn is hydrolyzed to Beclomethasone. The portion of the dose that is accidentally ingested is largely inactivated on the” first pass ” through the liver. In the liver, Beclomethasone dipropionate is converted into Beclomethasone monopropionate and then into polar metabolites. Binding to plasma proteins of the Active ingredient in the systemic circulation is 87%. The main part of the drug (35-76%) is excreted within 96 hours of the gastrointestinal tract, mainly in the form of polar metabolites,10-15% – by the kidneys.

Indications

Basic therapy of various forms of bronchial asthma in adults and children over 4 years of age.

Contraindications

Hypersensitivity to any component of the drug. Tuberculosis of the lungs. Children under 4 years of age. Beclomethasone, which contains 250 mcg in 1 dose, is not intended for use in pediatrics (i. e. in children under 18 years of age). Use with caution for glaucoma, systemic infections (bacterial, viral, fungal, parasitic), osteoporosis, liver cirrhosis, hypothyroidism, pregnancy, lactation.

Side effects

Adverse reactions are listed according to anatomical and physiological classification and occurrence. Infections: very common – candidiasis of the mouth and pharynx. Using a spacer and rinsing your mouth and throat with water after inhalation reduces the likelihood of these side effects. From the immune system: infrequently-hypersensitivity skin reactions, including rash, urticaria, itching, redness and swelling of the eyes, face, lips and mucous membrane of the mouth and pharynx; very rarely-angioedema, anaphylactic reactions. Endocrine system disorders: systemic effects are possible: very rarely-adrenal cortical suppression, growth retardation in children and adolescents, cataracts, glaucoma. From the respiratory system: often dysphonia (hoarseness of voice) or irritation of the pharyngeal mucosa, very rarely-paradoxical bronchospasm, which must be immediately stopped with an inhaled [3-2-short-acting adrenostimulator. In case of paradoxical bronchospasm, it is necessary to immediately stop using the drug in inhalations, assess the patient’s condition, conduct the necessary examination and prescribe the necessary treatment. From the skin and subcutaneous fat: often-bruising, thinning of the skin.

Interaction

Beclomethasone restores the patient’s response to beta-adrenomimetics, reducing the frequency of their use. When combined with inducers of microsomal oxidation ( including phenobarbital, phenytoin, rifampicin, etc. ), the effectiveness of Beclomethasone may decrease. When used concomitantly with methandienone, estrogens, beta – 2-adrenomimetics, theophylline, and systemic corticosteroids, the effectiveness of Beclomethasone increases. When used concomitantly, Beclomethasone enhances the effect of beta-adrenomimetics.

How to take, course of use and dosage

Beclomethasone is intended for inhalation use only.

Beclomethasone is used regularly (even in the absence of symptoms of the disease), the dose of Beclomethasone dipropionate is selected taking into account the clinical effect in each case.

In the mild course of bronchial asthma, the volume of forced inspiration (FEV) or peak expiratory velocity (PEP) is more than 80% of the proper values with a spread of PSV indicators of less than 20%.

With a moderate course of FEV or PSV is 60-80% of the proper values, the daily spread of PSV indicators is 20-30%.

In severe cases, FEV or PSV is 60% of the required values, and the daily spread of PSV indicators is more than 30%.

When switching to a high dose of inhaled Beclomethasone dipropionate, many patients receiving systemic glucocorticosteroids will be able to reduce their dose, cancel them altogether.

The initial dose of Beclomethasone is determined by the severity of bronchial asthma. The daily dose is divided into several doses.

Depending on the individual response of the patient, the dose of the drug can be increased until the clinical effect appears or reduced to the minimum effective dose.

Children aged 4-12 years

The initial dose is 50 mcg 2 times a day. If necessary, the initial dose can be increased to 100 mcg 2 times a day. The maximum single dose is 200 mcg.

The maximum daily dose is 400 mcg. The daily dose is divided into 2-4 doses.

Adults and children aged 12 years and older:

Recommended starting doses of the drug:

• mild bronchial asthma – 200-600 mcg/day;
• moderate bronchial asthma-600-1000 mcg/day;
• severe bronchial asthma-1000-2000 mcg/day.

Treatment of bronchial asthma is based on a step – by-step approach-therapy begins according to the stage corresponding to the severity of the disease. Inhaled corticosteroids are prescribed at the second stage of therapy.

Step 2. Basic therapy.

Beclomethasone dipropionate 100-400 mcg 2 times a day.

Step 3. Basic therapy.

Use inhaled corticosteroids in a high dose or in a standard dose, but in combination with inhaled p-2-adrenomimetics of long action.

Beclomethasone dipropionate in a high dose – 800-1600 mcg / day, in some cases megadoses up to 2000 mcg/day.

Stage 4. Severe asthma.

Beclomethasone dipropionate in a high dose – 800-1600 mcg / day, in some cases megadoses up to 2000 mcg/day.

Step 5. Severe asthma.

High-dose Beclomethasone dipropionate (see steps 3 and 4).

Special patient groups

There is no need to adjust the dose of Beclomethasone in the elderly, in patients with renal or hepatic insufficiency.

Skipping a single dose of the drug

If you accidentally miss an inhalation, the next dose should be taken at the appropriate time in accordance with the treatment regimen.

Patient instructions for using the inhaler

Check the inhaler’s performance before using it for the first time, and also if you haven’t used it in a while, or if the balloon was cooled to a low temperature and then you warmed it to room temperature. To check, remove the protective cap from the inhaler nozzle, turn the cylinder upside down, placing your index finger on the bottom of the cylinder, and your thumb on the top of the inhaler nozzle, shake the can up and down and make 2 taps with your thumb and index finger, pointing the outlet of the inhaler nozzle to the side. After the spray jet appears after the second push, proceed as described below, starting with the words: “Make sure that there is no dust or dirt in the outlet tube. “

With regular use of the drug, you should do this: :

• Remove the protective cap from the inhaler nozzle. Make sure that the outlet pipe is free of dust and dirt.
• Hold the balloon in an upright position with the bottom facing up, placing your index finger on the bottom of the balloon and your thumb on the top of the inhaler nozzle. Shake the can up and down.
• Exhale as deeply as possible (without exertion). Press the outlet tube of the inhaler nozzle firmly between your lips.
• Take a slow, deep breath. At the moment of inhalation, use your thumb and forefinger to release the dose of the drug. Continue to inhale slowly.
• Remove the tube of the inhaler nozzle from your mouth and hold your breath for 10 seconds or as long as you can without straining. Exhale slowly.
• If more than one dose of medication is required, wait for about a minute and then repeat the steps from step 2. Put the protective cap back on the inhaler nozzle.

When completing steps 3 and 4, take your time. When releasing a dose of medication, it is important to inhale as slowly as possible. First, practice in front of the mirror. If you notice steam coming out of the corners of your mouth, start again with step 2.

Cleaning the inhaler.

The inhaler nozzle should be cleaned at least once a week. Remove the inhaler nozzle from the cylinder and rinse it and the protective cap with warm water. Do not use hot water. Dry thoroughly, but do not use heating devices for this purpose.Put the protective cap back on the inhaler nozzle and put it back on the balloon. Do not dip the cylinder in water.

Overdose

Symptoms:Acute overdose of the drug can lead to a temporary decrease in the function of the adrenal cortex, which does not require emergency therapy, since the function of the adrenal cortex is restored within a few days, which is confirmed by the concentration of cortisol in plasma. With chronic overdose, persistent suppression of the function of the adrenal cortex can be observed. Treatment:In such cases, it is recommended to monitor the reserve function of the adrenal cortex. In case of overdose, treatment with Beclomethasone dipropionate can be continued in doses sufficient to maintain the therapeutic effect.

Special instructions

Before prescribing inhaled medications, it is necessary to instruct the patient about the rules for their use, ensuring the most complete penetration of the drug into the desired areas of the lungs. Oral candidiasis is most likely to develop in patients with high levels of precipitating antibodies in the blood against Candida, which indicates a previous fungal infection. After inhalation, rinse your mouth and throat with water. For the treatment of candidiasis, local antifungal drugs can be used while continuing therapy with Beclomethasone. If patients take corticosteroids orally, Beclomethasone is prescribed against the background of taking the previous dose of corticosteroids, while patients should be in a relatively stable condition. After about 1-2 weeks, the daily dose of oral corticosteroids is gradually reduced. The scheme of dose reduction depends on the duration of previous therapy and on the initial dose of corticosteroids. Regular use of inhaled corticosteroids allows in most cases to cancel oral corticosteroids (patients who need to take no more than 15 mg of prednisone can be completely transferred to inhalation therapy). At the same time, in the first months after the transition, the patient’s condition should be carefully monitored until his pituitary-adrenal system recovers sufficiently to ensure an adequate response to stressful situations (for example, injury, surgery or infection). When transferring patients from taking systemic corticosteroids to inhaled therapy, allergic reactions may occur (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs. Patients with reduced adrenal cortex function transferred to inhaled treatment should have a supply of corticosteroids and always carry a warning card indicating that they need additional systemic use of corticosteroids in stressful situations (after the stressful situation is resolved, the corticosteroid dose can be reduced again). Sudden and progressive worsening of asthma symptoms is a potentially life-threatening condition that requires an increase in the dose of corticosteroids. An indirect indicator of the ineffectiveness of therapy is the more frequent use of short-acting 0-2-adrenostimulants than before. Beclomethasone dipropionate for inhalation is not intended for relieving seizures, but for regular daily use. To stop seizures, short-acting (3-2) adrenostimulants (for example, salbutamol) are used. In case of severe exacerbation of bronchial asthma or insufficient effectiveness of the therapy, the dose of inhaled Beclomethasone dipropionate should be increased and, if necessary, systemic corticosteroids and an antibiotic should be prescribed if infection develops. If paradoxical bronchospasm develops, you should immediately stop using Beclomethasone, assess the patient’s condition, conduct an examination and, if necessary, prescribe therapy with other medications. With prolonged use of any inhaled corticosteroids, especially in high doses, systemic effects may occur (see “Side effects”), but the likelihood of their development is much lower than with oral corticosteroids. Therefore, it is especially important that when the therapeutic effect is achieved, the dose of inhaled corticosteroids is reduced to the minimum effective dose that controls the course of the disease. At a dose of 1500 mcg / day, the drug does not cause significant suppression of adrenal function in most patients. Due to possible adrenal insufficiency, special care should be taken and the function of the adrenal cortex should be regularly monitored when transferring patients taking oral corticosteroids to Beclomethasone treatment. It is recommended to regularly monitor the growth dynamics of children receiving inhaled corticosteroids for a long time. use can be carried out using special dispensers (spacers), which improve the distribution of the drug in the lungs and reduce the risk of side effects. Abrupt discontinuation of Beclomethasone aerosol is not recommended. It is necessary to protect the eyes from ingestion of the drug. Washing after inhalation can prevent damage to the skin of the eyelids and nose. A can of Beclomethasone should not be punctured, disassembled, or thrown into the fire, even if it is empty. Like most other aerosol inhalation products, Beclomethasone may be less effective at low temperatures. When cooling the cylinder, it is recommended to remove the inhaler nozzle from it and warm it with your hands for several minutes. Influence on the ability to drive vehicles and mechanismmi Net of data.

Form of production

Aerosol for inhalation dosed 50 mcg / dose,100 mcg / dose or 250 mcg / dose. 200 doses in aluminum cylinders with a protective coating, sealed with a metering valve and equipped with a spray nozzle with a protective cap. Each cylinder, together with a spray nozzle and a protective cap, as well as instructions for use, is placed in a pack.

Storage conditions

Store at a temperature not exceeding 25°C. Keep away from the heating system and direct sunlight. Keep out of reach of children!Protect from falls and bumps.

Shelf

life is 3 years. Do not use after the expiration date.

Active ingredient

Beclomethasone

Conditions of release from pharmacies

By prescription

Dosage form

aerosol for inhalation