Beclomethasone - instructions for use, dose, side effects, contraindications

Excipients: ethanol (rectified ethyl alcohol) * 2 mg / 4 mg / 10 mg, propellant HFC-134 a (1,1,1,2-tetrafluoroethane) - 70.583 mg / 67.583 mg / 58.625 mg.

* The volume fraction of ethyl alcohol is not less than 96.3%.

Composition per 1 cylinder:

active substance: beclomethasone dipropionate 0.012 g (0.024 g) 0.060 g;

Excipients: ethanol (rectified ethyl alcohol) * - 0.480 g / 0.960 g / 2.400 g, propellant HFC-134 a (1,1,1,2-tetrafluoroethane) 16.940 g (16.220 g) 14.070 g

* The volume fraction of ethyl alcohol is not less than 96.3%.

Description:

The preparation is a colorless or almost colorless solution, under pressure in an aluminum monoblock tank with a metering valve, equipped with an inhaler head with a protective cap; The drug is sprayed out of the balloon as an aerosol spray.

Pharmacotherapeutic group:Glucocorticosteroid for topical application

ATX: & nbsp

R.01.A.D.01 Beclomethasone

Pharmacodynamics:

Beclomethasone is a glucocorticosteroid (GCS) and has a weak tropism for GCS receptors. Under the action of enzymes it turns into an 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 (effect on the "late" allergy reaction), 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. Under the action of beclomethasone, the number of mast cells in the bronchial mucosa decreases, the epithelial edema diminishes, the mucus secretion by the bronchial glands, the bronchial hyperreactivity, the neutrophil vascular congestion, the inflammatory exudate and the production of lymphokines, the macrophage migration is inhibited, the intensity of the infiltration and granulation processes decreases. Increases the number of active beta-adrenergic receptors, restores the patient's response to bronchodilators. can reduce the frequency of their use. Virtually does not have a resorptive effect after inhalation.

Do not stop bronchospasm, the therapeutic effect develops gradually, usually after 5-7 days of course use beclomethasone.

Pharmacokinetics:

Suction: more than 25% of the dose of inhaled beclomethasone deposits in the respiratory tract; The remaining amount settles in the mouth, pharynx and is swallowed. In the lungs before absorption beclomethasone is extensively metabolized to the active metabolite B-17-MP. Systemic absorption of B-17-MP occurs in the lungs (36% of the pulmonary fraction), in the gastrointestinal tract (26% of the dose that has been ingested here when the dose is ingested). The absolute bioavailability of unchanged beclomethasone and B-17-MP is approximately 2% and 62% of the inhalation dose, respectively. Beclomethasone quickly absorbed, time to reach the maximum concentration in the blood plasma (T_mOh) is 0.3 hours. The B-17-MP is absorbed more slowly, T_mOh is approximately 1 hour. There is an approximately linear relationship between the increase in the inhaled dose and the system exposure of beclomethasone.

Distribution: the distribution in tissues is 20 liters for beclomethasone and 424 liters for B-17-MP. The connection with plasma proteins is relatively high - 87%.

Metabolism and excretion: beclomethasone and B-17-MP have a high plasma clearance (150 l / h and 120 l / h, respectively). The half-life is 0.5 h and 2.7 h, respectively.

Indications:

Basic therapy of various forms of bronchial asthma in adults and children.

Contraindications:

Hypersensitivity to beclomethasone and other components of the drug.

Children under 4 years.

Beclomethasone, containing 250 μg in 1 dose, is not intended for use in pediatrics (ie in children under 18 years of age).

Carefully:

With glaucoma, systemic infections (bacterial, viral, fungal, parasitic), osteoporosis, pulmonary tuberculosis, liver cirrhosis, hypothyroidism, pregnancy, lactation.

Pregnancy and lactation:

With extreme caution, the drug should be used during pregnancy and during breastfeeding only if the expected benefit for the mother exceeds the possible risk to the fetus and the baby.

Dosing and Administration:

The drug is intended for inhalation with an inhalation device (see "Instructions for the patient on the use of an inhalation device"). After each inhalation, it is necessary to thoroughly rinse the mouth and throat with water.

Apply regularly (even in the absence of symptoms of the disease). The dose is selected taking into account individual clinical efficacy, increasing to the appearance of a clinical effect or reducing to the minimum effective dose.When switching to a high dose of inhaled beclomethasone, many patients receiving systemic GCS can reduce their dose or cancel them altogether.

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

With an easy course of bronchial asthma, the volume of forced expiration (FEV) or peak expiratory flow (PSV) is more than 80% of the required values with a PSV score of less than 20%.

With moderate bronchial asthma, FEV or PSV is 60-80% of the required values, the daily spread of PSV parameters is 20-30%.

In severe bronchial asthma, FEV or PSV are 60% of the expected values, the daily spread of PSV values is more than 30%. The daily dose is divided into several doses (2-4 inhalations per day).

Adults and children over 12 years of age

Recommended initial daily doses:

- bronchial asthma of light course - 200-600 mcg / day (for 2 inhalations per day);

- bronchial asthma of moderate to severe course 600-1000 mcg / day (for 2-4 inhalations per day);

- A bronchial asthma of a heavy current of 1000-2000 mkg / day (for 2-4 inhalations a day).

The standard maximum daily dose is 1000 mcg. In some very serious cases, the daily dose can be increased to 1500-2000 μg (for 2-4 inhalations per day).Treatment of bronchial asthma is based on a stepwise approach - therapy is started according to the stage corresponding to the severity of the disease.

Inhaled glucocorticosteroids are prescribed at the second stage of therapy.

Step 2. Basic therapy.

100-400 mcg twice a day.

Step 3. Basic therapy.

Apply inhaled GCS in a high daily dose or in a standard daily dose, but in combination with inhalation beta₂-adrenomimetics long-acting.

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

Step 4. Severe bronchial asthma.

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

Step 5. Severe bronchial asthma.

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

Children from 4 to 12 years old

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

The drug containing 250 μg 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, in patients with renal or hepatic insufficiency.

Skipping a single dose of the drug

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

Introduction can be carried out using special dispensers (spacers). improving the distribution of the drug in the lungs and reducing the risk of side effects.

Application rules:

Preparation for first use:

Before the first use of the drug should be: put on the nozzle-inhaler, equipped with a protective cap, on the cylinder and valve stem, remove the protective cap from the nozzle-inhaler. Then vigorously shake the balloon with vertical movements, turn the balloon with the inhaler downward and make two sprays into the air to make sure the valve works adequately. If the product is interrupted for several days, one spray should be made into the air after a thorough shaking of the balloon.

Application:

1. Remove the protective cap from the inhaler-nozzle and make sure that the outlet tube of the nozzle-inhaler is clean.Turn the balloon with the inhaler downward, hold the inhalation device between the index and thumb in an upright position, with the thumb under the inhaler head and the index finger on the bottom of the aluminum canister.

2. Shake the aluminum canister intensively up and down.

3. Take a deep breath through your mouth. Clamp the mouth of the inhalation device tightly with your lips.

4. Take a slow and deep breath. At the moment of inspiration, press the top of the balloon, releasing the dose of the drug, continue to inhale slowly.

5. Remove the inhalation device from the mouth and hold your breath for 10 seconds or at a time that will not cause you any discomfort. Slowly exhale.

6. After inhalation, rinse your mouth with water, trying not to swallow the aerosol, which got during inhalation on the mucous membrane of the mouth.

7. If more than one dose is required, wait 1 minute and repeat all steps from step 2 to step 6.

8. Close the nozzle-inhaler with a protective cap.

In steps 3 and 4, do not rush. At the time of release, it is important to inhale as slowly as possible.Before use, practice in front of the mirror.

If you notice "steam" coming from the top of the can or from the corners of the mouth, then start again from step 2.

Cleaning:

The nozzle-inhaler should be cleaned at least once a week.

Remove the nozzle-inhaler from an aluminum cylinder. Gently rinse the nozzle-inhaler and protective cap with warm water.

Do not use hot water!

Shake the nozzle-inhaler and the protective cap to remove the remaining water, and dry them without using heating devices.

Do not allow the aluminum container to come into contact with water!

Side effects:

The frequency of side effects is classified according to the recommendations of the World Health Organization: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000, <1/1000) and very rarely (including isolated cases) (<1/10000).

Infectious diseases: often candidiasis of the oral cavity and upper respiratory pathways and pharynx (with prolonged use in high doses of more than 400 micrograms per day).

Allergic reactions: rarely skin rash, itchy skin, urticaria, erythema, anaphylactic reactions, angioedema, including edema of the paraorbital region, oral and pharyngeal mucosa, lips and face.

From the endocrine system: very rarely - oppression of the hypothalamic-pituitary-adrenal system (GGNS) (with prolonged use of high doses of more than 1.5 g / day), including growth retardation in children.

From the side of the organ of vision: very rarely - cataract, glaucoma.

On the part of the respiratory system, the organs of the thorax and the mediastinum: often - hoarseness of voice, irritation of the mucous membrane of the pharynx (application of the spacer reduces the likelihood of these side effects); rarely - paradoxical bronchospasm (stop with inhalation betaa₂short-acting adrenomimetics); very rarely - eosinophilic pneumonia.

From the musculoskeletal and connective tissue: very rarely - a decrease in bone mineral density.

Effects due to systemic action: headache, nausea; bruising or thinning of the skin; very rarely - a change in the psyche (especially in children): psychomotor hyperactivity, sleep disturbance, anxiety, depression or aggression.

Overdose:

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

Interaction:

Beclomethasone restores the patient's response to beta-adrenomimetics, thereby reducing the frequency of their use.

With simultaneous use with phenobarbital, phenytoin, rifampicin and other inducers of microsomal liver enzymes, the effectiveness of beclomethasone decreases.

When used concomitantly with metadienone, estrogen, beta₂-adrenomimetics. theophylline. as well as systemic GCS, the efficacy of beclomethasone increases.

With simultaneous application beclomethasone enhances the effect of beta-adrenomimetics.

Because of the content of ethyl alcohol, interaction in particularly sensitive patients with disulfiram and metronidazole is possible.

Special instructions:

Before using the drug, it must be ensured that the patient correctly uses the inhalation device to ensure sufficient dosing of the drug.

Patients who use the drug at home should be warned that if the effect of the usual dose becomes less effective or less prolonged, you can not independently increase the dose or frequency of the drug, and should immediately consult a doctor.

With long-term use of beclomethasone in high doses (more than 400 μg / day) candidiasis of the oral cavity and pharynx develops, especially in patients who have previously had a fungal infection, which is confirmed by the high content of precipitating antibodies against fungi in the blood Candida. 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 beclomstazone begins with ingestion of SCS, a decrease in the dose of GCS can be started only 1-2 weeks after the onset of simultaneous use.The scheme for reducing the dose of GCS for oral administration depends on the dose and duration of application of GCS. Regular use of inhaled beclomethasone in most cases can reduce the dose of GCS for oral administration. As a rule, patients taking no more than 15 mg of prednisolone. can completely switch to taking only inhaled beclomethasone. The first months after switching to inhalation therapy with beclomethasone, it is necessary to carefully monitor the state of the GGNS in order to prevent its inhibition.

Patients with reduced adrenal function, transferred completely to treatment with inhaled beclomethasone, should always have a GCS stock with them and carry a warning card with information about that. that in stressful situations they need the use of systemic GCS. After the stressful situation is completed, the dose of GCS can be reduced or the GCS can be canceled.

An increase in the dose of GCS is required if there is a sudden and progressive deterioration in the course of bronchial asthma. An indirect indicator of the ineffectiveness of therapy is the more frequent use bettinga₂-adrenomimetics short-acting.

When transferring patients from oral glucocorticosteroids intake to inhaled GCS, including beclomethasone. may manifest various allergic reactions, including allergic rhinitis and allergic dermatitis, which did not manifest themselves against the treatment of systemic SCS.

Beclomethasone for inhalations is intended for regular daily use, and not for relief of bronchospasm attacks.

For relief of attacks of bronchospasm apply beta₂short-acting adrenomimetics, including salbutamol.

In severe bronchial asthma or inadequate effectiveness of inhaled beclomethasone, it is necessary to increase its dose, and also consider the use of GCS inside or, for example, the use of antibiotics in the case of infectious inflammation.

With the development of paradoxical bronchospasm follows beclomethasone cancel, conduct a patient examination and consider the possibility of using another drug.

You can not abruptly stop treatment with inhaled beclomethasone. With long-term use of inhaled beclomethasone in a dose of more than 1.5 g / day, it is possible to develop systemic reactions of a different nature,including symptoms of suppression of the function of the adrenal cortex, a decrease in the rate of growth in children, a decrease in bone mineral density, cataracts, glaucoma. Therefore, when the therapeutic effect is achieved, the dose of inhaled beclomethasone should be reduced to the minimum effective dose that controls the course of the disease. Patients with a high risk of developing adrenocortical insufficiency should be under the supervision of a doctor.

With prolonged use of beclomethasone in children, it is necessary to monitor the dynamics of their growth.

Care should be taken when using inhaled GCS in patients with active and inactive forms of pulmonary tuberculosis.

It is necessary to protect eyes from getting the drug.

Aluminum can not be pierced, disassembled and heated, even if it is empty.

Effect on the ability to drive transp. cf. and fur:

Injections of beclomethasone do not influence the driving of motor vehicles and occupations with potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Aerosol for inhalation dosed, 50 mcg / dose, 100 mcg / dose, 250 mcg / dose.

Packaging:

For 200 doses in cylinders, aluminum monoblock with an internal lacquer coating, sealed with a metering valve and equipped with a nozzle-inhaler with a protective cap.

Each cylinder, together with a nozzle-inhaler and a protective cap, as well as instruction for medical use, is placed in a pack.

Storage conditions:

At a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003623

Date of registration:13.05.2016

Expiration Date:13.05.2021

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Representation: & nbspMOSHIMFARM PREPARATES them. NA Semashko OJSC MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp21.01.2017

Illustrated instructions

Instructions

Beclomethasone (Beclometasone)