Beclometasone dipropionate is a prodrug and has weak affinity for glucocorticosteroid (GCS) receptors. Under the action of esterase is converted to an active metabolite – andriol dosage-17-monopropionat, which has a pronounced local anti-inflammatory effect by reducing the formation of chemotactic substances (effect on delayed-type hypersensitivity). Suppressing the production of arachidonic acid metabolites and reducing the release of mast cell mediators of inflammation, inhibits the development of allergic reactions immediate type. It improves mucociliary transport, reduces the number of mast cells in bronchial mucosa, reduces epithelial edema, mucus secretion of bronchial glands, bronchial hyperreactivity, accumulation of neutrophils boundary, inflammatory exudate and limfoknnov products, inhibits the migration of macrophages, reduces the intensity of infiltration and granulation processes. After inhalation almost no resorptive action. Not relieves bronchospasm. The therapeutic effect develops gradually, usually after 5-7 days use of the course.
By increasing the activity of beta-adrenergic receptors restores the patient’s response to bronchodilators, allowing you to reduce the frequency of their use.
More than 25% of the inhaled dose is deposited in the respiratory tract, the remaining amount – in the mouth, throat, and swallowed. The light absorption before andriol dosage dipropionate is extensively metabolized to the active metabolite andriol dosage-17-monopropionat. Its systemic absorption occurs in the lung (36% -legochiaya fraction) in blood (26% of the ingested dose received at). The absolute bioavailability of unchanged andriol dosage dipropionate and andriol dosage-17-monoproshyunat is respectively about 2 and 62% of the inhaled dose.
andriol dosage dipropionate is rapidly absorbed (T max – 0.3 h), andriol dosage 17-monopropionat – slow (T max – 1 h). Tissue distribution of andriol dosage dipropionate is 20 liters and for andriol dosage-17-monopropionat – 424 l. Communication to plasma proteins is relatively high – 87%. andriol dosage dipropionate and andriol dosage-17-monopropionat have high plasma clearance (150 and 120 l / h, respectively). T ½ is 0.5 and 2.7 h, respectively.
Asthma different forms in adults and children older than 4 years (basic therapy).
Hypersensitivity to any component of the formulation. Be wary of Glaucoma, systemic infections (bacterial, including pulmonary tuberculosis, viral, fungal, parasitic), osteoporosis, liver cirrhosis, hypothyroidism.
Pregnancy and lactation
With caution only if the potential benefit to the mother outweighs the potential risk to the fetus and child.
Dosing and Administration
The dose is adjusted individually (it can be increased until clinical response or reduced to the minimum effective dose). The initial dose is determined by the severity of asthma. The daily dose is divided into several stages. Adults and children aged 12 years and older. The recommended initial dose: – asthma mild (forced expiratory volume (FEV) or peak expiratory flow rate (LSV) – more than 80%, the daily disorder of indicators PSV – less than 20%) – 200-600 mg / day;
- asthma moderate (FEV or PEF – 60-80%, the daily disorder of indicators PSV – 20-30%) – 600-1000 mg / day;
- bronchial asthma, severe (PFD or PSV – 60%, the daily disorder of indicators – 30%) – 1000-1200 mg / day.
Treatment of asthma is based on a stepwise approach – according to the stage of therapy begins, the corresponding severity of the disease. Glucocorticosteroids administered by inhalation to the second stage of therapy. Stage 2. Basic therapy: andriol dosage dipropionate – 1 00-400 mg 2 times a day. Step 3. Basic therapy: inhaled corticosteroids in high or standard doses, but when combined with inhalation betaz- agonists adrekoretseptorov long-acting. andriol dosage dipropionate -. High-dose (800-1600, in some cases up to 2000 mg / day) Stage 4 (severe asthma). andriol dosage dipropionate – 800-1600 mg / day, in some cases – megadoses of up to 2000 mg / day. Step 5 (severe asthma). BDP – at the high dose (see step 3.4.). Children aged 4 to 12 years: 400 mg per day in divided doses. Special groups of patients: there is no need to adjust the dose in elderly patients, in patients with renal and hepatic insufficiency. Skipping a single dose of the drug: Accidental inhalation passage of the next dose should be taken in due time in accordance with the scheme of treatment.
Side effects Respiratory system: Candidiasis of the upper respiratory tract (the likelihood of developing increased at doses over 400 mg / day), dysphonia (hoarseness), irritation of the mucous membrane of the pharynx (the use of a spacer reduces the likelihood of development), paradoxical bronchospasm (immediately cropped via inhalation beta-agonists short-acting). From the digestive tract: oral candidiasis (likelihood of developing increased at doses over 400 mg / day), nausea, unpleasant taste. Allergic reactions: giperchuvstvitelnosti reactions, including rash, hives, itching, redness and swelling eyes, face, lips and mucous membranes of the mouth and throat. Other: possible systemic effects, including headache, bruising, or thinning of the skin, reduced adrenocortical function, osteoporosis, growth retardation in children and adolescents, cataract, glaucoma.
Interaction with other medicinal products
There are no confirmed data on the interaction of andriol dosage diprottionata with other drugs.
Acute overdose could lead to a temporary decrease in adrenocortical function that does not require emergency treatment, since it is restored within a few days, as evidenced by the level of cortisol in the plasma.
In chronic overdose may experience persistent suppression of adrenocortical function. In this case it is necessary to monitor the backup function of the adrenal cortex. Drug treatment may be continued at a dose sufficient to maintain therapeutic effect. Precautions If the drug is given to patients receiving CAP inside the last dose remains the same. Thus the patient should be in a relatively stable state. After about 1-2 weeks the daily dose of oral corticosteroids begin to gradually reduce the scheme, depending on the duration of previous therapy, and the magnitude of the initial dose of corticosteroids. Regular use of inhaled corticosteroids in most cases, to cancel oral corticosteroids (patients needing admission no more than 15 mg of prednisolone can be fully transferred to the inhalation therapy), while in the first months after the transfer of the patient should be closely monitored until his pituitary-yadpochechnikovaya the system does not recover sufficiently to provide adequate response to stressful situations (for example, trauma, surgery or infection). When transferring patients from systemic corticosteroids to inhaled allergic reaction (eg allergic rhinitis, eczema), which previously suppressed by systemic drugs.Patients with impaired function of the adrenal cortex, translated in inhalation therapy, GCS must have a stock, and always carry a warning card indicating that in stressful situations, they require additional systemic corticosteroids appointment (after eliminating stress dose of corticosteroids may be reduced again). Sudden and progressive deterioration of asthma symptoms is a potentially dangerous condition, often threatening the patient’s life, and require increasing doses of corticosteroids. An indirect measure of treatment failure is more frequent than in the past, the use of betaz-agonists of short action. With the development of paradoxical bronchospasm should immediately stop using the product, assess the condition of the patient, conduct a survey and assign treatment by other drugs. Prolonged use of any inhaled corticosteroids, especially in high doses, may experience systemic effects (see. “Side Effects”), but the probability of their development is much lower than in the appointment of GCS inside. It is therefore particularly important that the dose of the therapeutic effect of inhaled corticosteroids has been reduced to the minimum effective dose for controlling diseases. The preparation at a dose of 1500 mg / day does not cause a substantial majority of patients the suppression of adrenal function. Due to possible adrenal insufficiency when transferring patient taking corticosteroids by mouth, on inhalation therapy should be particularly careful and regular monitoring of performance function of the adrenal cortex. It should be particularly careful in the treatment of inhaled corticosteroids in patients with tuberculosis, both in active and inactive form. Data on the effect of the drug on the ability to drive / there are no mechanisms.
Before the appointment of inhaled drugs should instruct the patient on the rules of their application, providing the most complete entering drug to the lungs. The development of oral candidiasis is most likely in patients with high levels of antibodies precipitating antikandidoznyh (evidence of candidiasis adjourned earlier). After inhalation of the mouth and throat should be rinsed with water. For the treatment of candidiasis while continuing drug therapy can be used antifungals local action. The drug is not intended for relief of attacks, and regular daily use. For cupping apply betag-agonists short-acting (such as salbutamol). Should increase the dose of inhaled andriol dosage dipropionate and, if necessary, appoint a systemic corticosteroids and / or the development of infection in severe exacerbations of asthma or lack of efficacy of the therapy – antibiotic. It is recommended to regularly monitor the dynamics of the growth of children receiving inhaled corticosteroids for a long time. Not recommended abrupt withdrawal of the drug. It is necessary to protect the eyes from contact with the drug; for the prevention of skin lesions age, nasal washing is recommended after inhalation. The balloon with the drug can not puncture, disassemble or dispose of in fire, even if it is empty. Upon cooling spray is recommended to get it out of the plastic case and warm hands for a few minutes (at low temperatures, the drug may be ineffective). Patient Instructions for Use of the inhaler: Check the operation of the inhaler before the first use, and if you have not used it kakoe- time.
- Remove the inhaler cap. Make sure that the outlet tube is no dust and dirt.
- Keep the can upright, resting on the bottom of the thumb and the index – on top of the balloon.
- Shake the cartridge up and down.
- Make as much as possible a deep breath (without voltage). Firmly pinch the lips outlet pipe balonchika.
- Slowly breathing in deeply, press your index finger on the valve cartridge, releasing a dose of medicine. Continue to slowly inhale.
- Remove the tube from the mouth of the inhaler and hold your breath for 10 seconds or as you can without strain. Exhale slowly.
- If you need more than one dose, wait about a minute and then repeat the procedure from step 2. Put the cap back on the inhaler.
When you perform steps 3 and 4 are not in a hurry. At the time of release dose of the drug is important to breathe in as slowly as possible. First, work out in the mirror. If you notice a “steam” coming from the top of a container or out of the corners of the mouth, start again from step 2.
Cleaning the inhaler:
The inhaler should be cleaned at least once a week. Remove the metal canister out of the plastic case and rinse the case and cover with warm water. Do not use hot water. Thoroughly dry without using heating devices. Put the cartridge back in its case and put on the cap. Do not immerse the metal canister into water.
aerosol for inhalation dose of 50 mcg / dose, 100 ug / dose and 250 mg / dose At 14.02 g (200 doses) in aluminum cans fitted with metering valves, sprayers for anti-asthma drugs imported. Each cylinder together with instructions for use placed in a pile of cardboard.