Composition, form of production and packaging
The aerosol for inhalation is dosed in the form of a suspension under pressure and forms a white spot when sprayed onto a slide.
1 dose 1 bottle
beclomethasone dipropionate 50 Ојg 12 mg
Auxiliary substances: ethanol (absolute ethyl alcohol), hydrofluoroalkane (HFA-134a) - up to 14.02.
200 doses (14.02 g) - aluminum cylinders (1) with metering valves, sprayers - cardboard packs.
The aerosol for inhalation is dosed in the form of a suspension under pressure and forms a white spot when sprayed onto a slide.
1 dose 1 bottle
beclomethasone dipropionate 100 Ојg 24 mg
Auxiliary substances: ethanol (absolute ethyl alcohol), hydrofluoroalkane (HFA-134a) - up to 14.02.
200 doses (14.02 g) - aluminum cylinders (1) with metering valves, sprayers - cardboard packs.
The aerosol for inhalation is dosed in the form of a suspension under pressure and forms a white spot when sprayed onto a slide.
1 dose 1 bottle
beclomethasone dipropionate 250 Ојg 60 mg
Auxiliary substances: ethanol (absolute ethyl alcohol), hydrofluoroalkane (HFA-134a) - up to 14.02.
200 doses (14.02 g) - aluminum cylinders (1) with metering valves, sprayers - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
PHARMACHOLOGIC EFFECT
GCS for topical application. Beclomethasone dipropionate is a prodrug and has a weak tropism for glucocorticosteroid receptors. Under the action of esterases it is converted into an active metabolite - beclomethasone-17-monopropionate, which has a pronounced local anti-inflammatory effect by reducing the formation of the chemotaxis substance (effect on allergic reactions of delayed type). By suppressing the production of arachidonic acid metabolites and reducing the release of inflammatory mediators from mast cells, inhibits the development of an allergic reaction of immediate type. It improves mucociliary transport, reduces the number of mast cells in the bronchial mucosa, reduces epithelial edema, mucus secretion by the bronchial glands, bronchial hyperreactivity, neutrophil vascular congestion, inflammatory exudate and lymphokine production, inhibits the migration of macrophages, reduces the intensity of infiltration and granulation processes. After inhalation, almost no effect of resorptive action. Does not stop bronchospasm. The therapeutic effect develops gradually, usually after 5-7 days of course use.
By increasing active ОІ-adrenoreceptors, the patient's reaction to bronchodilators is restored, allowing the frequency of their use to be reduced.
PHARMACOKINETICS
Suction
More than 25% of the inhaled dose settles in the respiratory tract, the remaining amount - in the mouth, pharynx and swallowed. In the lungs before absorption of beclomethasone, dipropionate is extensively metabolized to the active metabolite beclomethasone-17-monopropionate. Its systemic absorption occurs in the lungs (36% pulmonary fraction), in the digestive tract (26% of the dose that was ingested upon ingestion). The absolute bioavailability of unchanged beclomethasone dipropionate and beclomethasone-17-monopropionate is approximately 2% and 62% of the inhaled dose, respectively. Beclomethasone dipropionate is absorbed rapidly (T max - 0.3 h), beclomethasone-17-monopropionate - more slowly (T max - 1 h).
Distribution
Binding to plasma proteins is relatively high - 87%. V d in the tissues for beclomethasone dipropionate is 20 liters and for beclomethasone-17-monopropionate is 424 liters.
Excretion
Beclomethasone dipropionate and beclomethasone-17-monopropionate have a 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 older than 4 years (basic therapy).
DOSING MODE
The drug is used inhalation.
The dose is individually selected by increasing to the appearance of a clinical effect or reducing to a 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 stage corresponding to the severity of the disease.
Step 1. Recommended initial doses of the drug:
bronchial asthma of mild severity (volume of forced exhalation / FEV / or peak exhalation rate / PSV) - more than 80%, daily spread of PSV parameters - less than 20%) - 200-600 mcg / day;
bronchial asthma of moderate severity (FEV or PSV - 60-80%, diurnal spread of PSV parameters - 20-30%) - 600-1000 mcg / day;
bronchial asthma of a severe degree (FEV or PSV - 60%, diurnal spread of indicators - more than 30%) - 1000-1200 mcg / day.
Stage 2. Basic therapy: 100-400 mcg 2 times / day.
Step 3. Basic therapy: inhalation of SCS in a high or standard dose, but in combination with inhalation administration of agonists? 2- adrenoreceptors of long-acting.Beclospir В® at a high dose of 800-1600 Ојg / day, in some cases - up to 2000 Ојg / day.
Stage 4 ( severe bronchial asthma ). Beclospir В® - 800-1600 mcg / day, in some cases - megadoses up to 2000 mcg / day.
Step 5 ( severe bronchial asthma ). BeclospirВ® is administered 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 liver failure, dose adjustment is not required.
If you miss an inhalation accidentally, the next dose should be taken at the appropriate time in accordance with the treatment regimen.
SIDE EFFECT
On the part of the respiratory system : Candidiasis of the upper respiratory tract (the likelihood of development increases at doses of more than 400 Ојg / day), dysphonia (hoarseness), irritation of the pharyngeal mucosa (the use of the spacer reduces the likelihood of their development), paradoxical bronchospasm (immediately stopped with inhalation beta 2 short-acting adrenomimetics).
On the part of the digestive tract : candidiasis of the oral cavity (the probability of development increases at doses more than 400 mcg / day), nausea, unpleasant taste sensations.
Allergic reactions : hypersensitivity reactions, including rashes, hives, itching, redness and swelling of the eyes, face, lips and mucous membranes of the mouth and throat.
Other : systemic effects are possible, incl. headache, bruising or thinning of the skin, a decrease in the function of the adrenal cortex, osteoporosis, growth retardation in children and adolescents, cataracts, 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.
PREGNANCY AND LACTATION
During pregnancy and lactation (breastfeeding), Beclospir В® should be used with extreme caution only if the potential benefit to the mother exceeds the possible risk to the fetus and the baby.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal insufficiency do not need dose adjustment.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in cirrhosis.
Patients with hepatic insufficiency do not need a dose adjustment.
APPLICATION FOR CHILDREN
The drug is used in children older than 4 years.
It is recommended to regularly monitor the dynamics of growth in children receiving inhaled glucocorticosteroids for a long time.
APPLICATION IN ELDERLY PATIENTS
Older patients do not need a dose adjustment.
SPECIAL INSTRUCTIONS
When prescribing the drug on the background of taking GCS inside, the dose of the latter remains the same. In this case, the patient should be in a relatively stable state. After about 1-2 weeks. daily dose of oral glucocorticosteroids begin to gradually decrease according to the scheme, depending on the duration of the previous therapy and on the value of 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), and in the first months after the transition, the patient's condition should be carefully monitored until his pituitary-adrenal the system will not recover sufficiently to provide adequate response to stressful situations (for example: trauma, surgery or infection). When transferring patients from systemic GCS to inhalation, allergic reactions (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs, are possible.
Patients with a reduced function of the adrenal cortex, transferred to inhalation therapy, should have a stock of SCS and always carry a warning card with them indicating that in stressful situations they need an additional systemic appointment of GCS (after a stressful situation, the dose of GCS can again be reduced). Sudden and progressive worsening of asthma symptoms is a potentially dangerous condition, often threatening 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 beta 2 -adrenomimetics of short action. With the development of paradoxical bronchospasm it is necessary to immediately stop the use of the drug, assess the patient's condition, conduct a survey and prescribe therapy with other medications. 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 the appointment of GCS inside. Therefore, it is especially important that when a therapeutic effect is achieved, the dose of inhaled glucocorticosteroids is reduced to the lowest effective dose controlling the course of the disease.
The drug at a dose of 1500 mcg / day does not cause a significant suppression of adrenal function in most patients. In connection with the possible adrenal insufficiency in the transfer of the patient taking the GCS inside, on inhalation therapy, it is necessary to observe special care and regularly monitor the indices of the function of the adrenal cortex. Special care should be taken when treating patients with tuberculosis, both active and inactive, with inhaled GCS.
Prior to the appointment of inhaled drugs, the patient should be instructed on the rules for their use, ensuring the most complete drug exposure to the lungs. The development of oral candidiasis is most likely in patients with a high level of precipitating anticancerous antibodies (indicative of a previous candidiasis). After inhalation, the mouth and throat should be rinsed with water. For the treatment of candidiasis, while continuing therapy with the drug, antifungal agents of local action can be used.
The drug is not intended for relief of seizures, but for regular daily use. For relief of seizures apply? 2- adrenomimetics of short action (eg, salbutamol).
In case of severe exacerbation of bronchial asthma or inadequate efficacy of the therapy, increase the dose of inhaled beclomethasone dipropionate and, if necessary, prescribe a systemic SCS and / or if an infection develops, an antibiotic.
Do not abruptly cancel the drug.
It is necessary to protect the eyes from getting the drug; for the prevention of skin lesions of the eyelids, nose is recommended to wash after inhalation.
The container with the drug can not be pierced, disassembled or thrown into the fire, even if it is empty. When cooling the can, it is recommended to remove it from the plastic case and warm it up with your hands for several minutes (at low temperatures the drug may not be effective).
Use in Pediatrics
It is recommended to regularly monitor the dynamics of growth in children receiving inhaled glucocorticosteroids for a long time.
Impact on the ability to drive vehicles and manage mechanisms
Data on the effect of the drug on the ability to control the car / mechanisms are absent.
Instructions for the patient to use the inhaler
Check the work of the inhaler before using it for the first time, or if it has not been used for a while.
1. Ensure that there is no dust and dirt in the exit tube of the cylinder.
2. Place the nebulizer on the cylinder so that the exit tube of the balloon enters the hole in the nebulizer, remove the protective cap.
3. Hold the canister in the sprayer vertically with the bottom up, placing the index finger on the bottom, and the thumb on the sprayer. Vigorously shake the bottle 3-4 times up and down.
4. Take the nebulizer into the mouth, tightly grasping his lips, and completely exhale through the nose (without tension).
5. Slowly inhaling deeply, press the index finger to the bottom of the bottle, releasing the dose of the medicine. Continue to inhale slowly.
6. Take the inhaler tube out of your mouth and hold your breath for 10 seconds or as much as possible without tension. Slowly exhale.
7. If more than one dose of the drug is required, you should wait about a minute and then repeat the procedure from step 2. Put the cap back on the inhaler.
When performing steps 4 and 5, do not rush. At the time of release, it is important to inhale as slowly as possible. First you need to practice before the mirror. If there is a "vapor" emerging from the top of the can or from the corners of the mouth, you should start again from step 2.
Cleaning the inhaler
The inhaler should be cleaned at least once a week. Remove the metal can from the plastic case and rinse the case and cap with warm water. Do not use hot water .Thoroughly dry without using heating devices. Place the can in the case and put on the cap. Do not immerse the metal can into the water.
OVERDOSE
Symptoms: acute overdose may lead to a temporary decrease in the function of the adrenal cortex; with chronic overdose, there can be a persistent suppression of the function of the adrenal cortex.
Treatment: with acute overdose does not require emergency therapy, t. function is restored within a few days, which is confirmed by the level of cortisol in the plasma.
In chronic overdose, it is necessary to monitor the reserve function of the adrenal cortex. Treatment with the drug can be continued at doses sufficient to maintain a therapeutic effect.
DRUG INTERACTION
There is no confirmed data on the interaction of beclomethasone dipropionate with other drugs.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Protect from freezing. Shelf life - 2 years.
