Boson - instructions for use, doses, side effects, contraindications

Beclomethasone dipropionate is a prodrug and has a weak tropism for GCS receptors. Under the action of esterases, 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 mucous membrane of the bronchi decreases, the epithelial edema decreases, the mucus secretion by the bronchial glands, the hyperreactivity of the bronchi,the marginal accumulation of neutrophils, inflammatory exudate and production of lymphokines, the migration of macrophages is inhibited, the intensity of the processes of infiltration and granulation is reduced. Increases the number of active beta-adrenergic receptors, restores the patient's response to bronchodilators, and reduces 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 dipropionate.

Pharmacokinetics:

In the lung tissue of beclomethasone, dipropionate is rapidly hydrolyzed to B-17-MP, which in turn hydrolyses to beclomethasone. Part of the dose, which is accidentally swallowed, is largely inactivated by "first passing" through the liver. In the liver, the process of conversion of beclomethasone dipropionate into B-17-MP and then into polar metabolites occurs. The binding with plasma proteins of the active substance in the systemic circulation is 87%. The main part of the preparation (35-76%) is excreted within 96 hours through the gastrointestinal tract, mainly in the form of polar metabolites,10-15% - with the kidneys.

Indications:Basic therapy of various forms of bronchial asthma in adults and children older than 4 years.

Contraindications:

Hypersensitivity to any component of the drug.

Children up to 4 years.

Carefully:

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

Pregnancy and lactation:The boson should be used during pregnancy and lactation and only if the potential benefit to the mother exceeds the possible risk to the fetus and the baby.

Dosing and Administration:

The Boson is only for inhalation use.

The boson 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 specific case.

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

In the medium-heavy current FEV or PSV is 60-80% of the required values, the daily spread of PSV indicators is 20-30%.

In severe conditions FEV or PSV is 60% of the required values, 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 Boson 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 appearance of a clinical effect or reduced to the minimum effective dose.

Children between the ages of 4 and 12

The initial dose is 100 μg 2 times a day. The maximum single dose of 200 mcg. The maximum daily dose is 400 mcg. The daily dose is divided into 2-4 admission.

Adults and children aged 12 years and over:

Recommended initial doses of the drug:

bronchial asthma of mild course - 200-600 mcg / day;
bronchial asthma of moderate course - 600-1000 mcg / day;
A bronchial asthma of a heavy current - 1000-2000 mkg / sut.

Treatment of bronchial asthma is based on a stepwise approach - therapy is started according to the stage corresponding to the severity of the disease.

Inhalation GCS is prescribed at the second stage of therapy.

Step 2. Basic therapy.

Beclomethasone dipropionate is 100-400 mcg 2 times a day.

Step 3.Basic therapy.

Apply inhaled GCS in high dose or in a standard dose, but in combination with inhalation β-2-adrenomimetics long-acting.

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

Step 4. Severe bronchial asthma.

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

Step 5. Severe bronchial asthma.

Beclomethasone dipropionate in a high dose (see steps 3 and 4).

Special patient groups

There is no need to adjust the dose of Boson 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.

Side effects:

Undesirable reactions are listed depending on the anatomical and physiological classification and occurrence. The frequency of occurrence is determined in this way: very often ≥1 / 10, often ≥1 / 100 and <1/10, infrequently ≥1 / 1000 and <1/100, rarely ≥1 / 10000 and <1/1000, very rarely <1 / 10000, the frequency is unknown (insufficient data to estimate the frequency of development).

Infections: very often - candidiasis of the oral cavity, pharynx and upper respiratory tract. The use of a spacer and the rinsing of the mouth and throat with water after inhalation reduces the likelihood of these side effects.

From the immune system: infrequently - hypersensitivity reactions, including rash, hives, itching, redness; very rarely - angioedema (edema of the eyes, face, lips and mucous membranes of the mouth and pharynx), anaphylactic reactions.

From the endocrine system: Systemic effects are possible: very rarely - oppression of adrenal cortex function, growth retardation in children and adolescents.

From the respiratory system: often dysphonia (hoarseness of voice) or irritation of the mucous membrane of the pharynx, cough; very rarely - paradoxical bronchospasm, which must be immediately stopped with the help of inhalation β-2-adrenostimulator of short action. In the case of paradoxical bronchospasm, it is necessary to immediately stop the use of 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.

From the side of the organ of vision: cataract, glaucoma.

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

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

Overdose:

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 for several days, which is confirmed by the concentration of cortisol in the plasma. With a chronic overdose, there can be a persistent suppression of the function of the adrenal cortex. In such cases, it is recommended to monitor the reserve function of the adrenal cortex. In case of an overdose, treatment with beclomethasone dipropionate can be continued at doses sufficient to maintain a therapeutic effect.

Interaction:

Beclomethasone restores the patient's response to beta-adrenomimetics,allowing to reduce the frequency of their application.

When combined with inducers of microsomal oxidation (incl. phenobarbital, phenytoin, rifampicin and others) may reduce the effectiveness of beclomethasone.

With simultaneous use with methandienone, estrogen, betaa₂-adrenomimetics, theophylline, as well as systemic GCS, the efficacy of beclomethasone increases.

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

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

Special instructions:

Before prescribing inhalants, the patient should be instructed on the rules for their use, ensuring the most complete entry of the drug into the right areas of the lungs.

The development of oral candidiasis is most likely in patients with a high level of precipitating antibodies in the blood against the fungus Candida, which indicates an earlier transferred fungal infection. After inhalation, rinse the mouth and throat with water. For the treatment of candidiasis, antifungal agents of local action can be used while continuing therapy with Boson.

If patients take G'KS inside, then Boson is appointed against the background of receiving the previous dose of SCS, while patients should be in a relatively stable state. After about 1-2 weeks, the daily dose of oral glucocorticosteroids is gradually reduced. The dose reduction scheme depends on the duration of the previous therapy and on the initial dose of GCS. Regular use of inhaled glucocorticosteroids allows in most cases to cancel oral GCS (patients who need to take no more than 15 mg of prednisolone can be fully switched to inhalation therapy). In the first months after the transition, the patient's condition should be carefully monitored until his pituitary-adrenal system is sufficiently restored to provide adequate response to stressful situations (for example, trauma, surgery or infection).

When transferring patients from receiving systemic GCS to inhalation therapy, allergic reactions (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs, may appear.

Patients with a reduced function of the adrenal cortex, transferred to inhalation treatment,must have a stock of the SCS and always carry a warning card with them, which should indicate that they need additional systemic appointment of GCS in stressful situations (after a stressful situation, the dose of GCS can be reduced again). A sudden and progressive worsening of asthma symptoms is a potentially dangerous condition, not uncommon for the patient's life, and requires an increase in the dose of GCS. An indirect indicator of the ineffectiveness of therapy is the more frequent than before use of short-acting β-2 adrenostimulators.

Beclomethasone dipropionate for inhalations is not intended for relief of seizures, but for regular daily use. To stop seizures, use short-acting β-2-adrenostimulators (for example, salbutamol).

In case of severe exacerbation of bronchial asthma or insufficient effectiveness of the therapy, increase the dose of inhaled beclomethasone dipronionate and, if necessary, prescribe a systemic SCS and an antibiotic for the development of infection.

With the development of paradoxical bronchospasm, the use of Boson should immediately be discontinued, the patient's condition assessed,conduct a survey and, if necessary, prescribe therapy with other medications.

With long-term use of any inhaled glucocorticosteroids, especially at high doses, systemic effects can be noted (see "Side Effects"), but the likelihood of their development is significantly lower than when ingesting GCS inside. Therefore, it is especially important that, when the therapeutic effect is achieved, the dose of inhaled glucocorticosteroids is reduced to the lowest effective dose controlling the course of the disease. At a dose of 1500 μg / day, the drug in most patients does not cause significant suppression of adrenal function. In connection with a possible adrenal insufficiency, one should be extra careful and regularly monitor the indices of the function of the adrenal cortex when transferring patients taking SCS inward to beclomethasone.

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

The introduction can be carried out with the help of special dispensers (spacers), which improve the distribution of the drug in the lungs and reduce the risk of side effects.

It is not recommended to abruptly cancel the drug Bozon Aerosol.

It is necessary to protect eyes from getting the drug. By washing after inhalations it is possible to prevent damage to the skin of the eyelids and nose.

A canister with a Boson can not be pierced, disassembled or thrown into a fire, even if it is empty. Like most other inhalation agents in aerosol packages, the Boson can be less effective at low temperatures. When cooling the cylinder, it is recommended to remove the inhaler from it and warm it with your hands for several minutes.

Instructions for the patient to use the inhaler

Check the operation of the inhaler before first use, and if you have not used it for a while, or if the cylinder has been cooled to a low temperature, and then you warmed it to room temperature. For testing, remove the protective cap from the inhaler nozzle, turn the bottle upside down, placing the index finger on the bottom of the cylinder, and the thumb on the top of the nozzle-inhaler, shake the can up and down and make 2 clicks with the thumb and forefinger, pointing the nozzle outlet -Inhaler in the side. After the appearance of an aerosol spray, after the second press, proceed as described below, beginning with the words: "Make sure,that there is no dust and dirt in the outlet tube. "

With regular use of the drug, it is necessary to do this:

1. Remove the protective cap from the inhaler nozzle. Ensure that there is no dust and dirt in the outlet tube.

2. Hold the container upright in the vertical position, placing your index finger on the bottom of the balloon, and your thumb on the top of the nozzle-inhaler. Shake the can up and down.

3. Do as deep as possible (without tension). Clamp the mouth of the nozzle-inhaler tightly with your lips.

4. Take a slow deep breath. At the moment of inspiration, use the thumb and forefinger to release the dose of the drug. Continue to inhale slowly.

5. Take the mouthpiece of the inhaler nozzle out of your mouth and hold your breath for 10 seconds or as long as you can without tension. Slowly exhale.

6. If more than one dose is required, wait for about a minute and then repeat the procedure from step 2. Replace the protective cap on the inhaler.

In steps 3 and 4, do not rush. At the time of release, it is important to inhale as slowly as possible. First, practice in front of the mirror.If you notice steam coming from the corners of the mouth, then start again from step 2.

7. Cleaning of the inhaler. The nozzle-inhaler should be cleaned at least once a week. Remove the nozzle-inhaler from the cylinder and rinse it and protective cap with warm water. Do not use hot water. Thoroughly dry, but do not use heating devices for this. Put back the protective cap on the nozzle-inhaler, and it - on the balloon. Do not immerse the cylinder in water.

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

No data.

Form release / dosage:

Aerosol for inhalation dosed, 100 mcg / dose.

Packaging:

For 200 doses of the drug in an aluminum canister with a metering valve, equipped with a nozzle-sprayer.

Each cylinder, together with the instruction for use, is placed in a pack of cardboard.

Storage conditions:Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date.