Registration number: LSR-000 189/09 of 16.01.2009
The trade name of the drug: Beklospir®
International nonproprietary name: Beclomethasone
Dosage form: spray for inhalation dose
Ingredients on one cylinder: 200 doses
Active ingredient: BDP 0,012g, 0,024g and 0,060g
Excipients: ethanol (ethyl alcohol, absolute), a hydrofluoroalkane (HFA134a) to 14,02g.
The contents of an aerosol aluminum bottle with a metering valve action - suspension under pressure and forming a white spot when sprayed onto a glass slide.
ATC code: [R03BA01]
Pharmacotherapeutic group: Glucocorticosteroids for local use.
Pharmacodynamics: BDP is a prodrug and has a weak affinity for glucocorticosteroid (GCS) receptors. Under the action of esterase converted to an active metabolite - beclomethasone-17-monopropionat that turns out, by the expression a local anti-inflammatory effect by reducing the formation Substance chemotaxis (effect on delayed-type hypersensitivity). Bring-Laa production of arachidonic acid metabolites and reducing the release of mast cell mediators of inflammation, inhibits the development of immediate allergic reaction. It improves mucociliary transport, reduces the number of mast cells in the mucosa-hull about bronchial epithelium reduces swelling, mucus secretion of bronchial glands, Ki-perreaktivnost bronchial accumulation of neutrophils boundary, inflammatory exudate and the production of lymphokines, inhibits the migration of macrophages, reduces the intensity of processes, infiltration and owls granulation. After inhalation almost no resorptive action. Not relieves bronchospasm. The therapeutic effect develops gradually, usually within 5-7 days of the course application. By increasing the activity of beta-adrenergic receptors restores the patient's response to bronchodilators, allowing you to reduce the frequency of their use.
Pharmacokinetics: Over 25% of an inhaled dose is deposited in the respiratory tract, the remaining amount - in the mouth, throat, and swallowed. The absorption of light to back-lometazona dipropionate extensively metabolized to the active metabolite beklome-tazona-17 monopropionat. Its systemic absorption occurs in the lung (36% -legochnaya fraction) in blood (26% of the dose received by ingestion). Absolute-bioavailable of unmodified beclomethasone dipropionate and beclomethasone-17-monopropionat is respectively about 2 and 62% of the inhaled dose. Beclomethasone dipropionate rapidly absorbed (Tmax - 0,3 h), beclomethasone 17-monopropionat - more slowly (Tmax - 1 h). Tissue distribution of beclomethasone Dipri-propionate is 20 liters and beclomethasone-17-monopropionat - 424 l. Communication with plasma proteins is relatively high - 87%. Beclomethasone dipropionate and beclomethasone-17-monopropionat have high plasma clearance (150 and 120 l / hr, respectively). T1 / 2 was 0.5 and 2.7 hours, 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 extreme caution only if the potential benefit to the mother outweighs the potential risk to the fetus and child.
Dosing and Administration
Dose selected individually (it can be increased until a clinical effect or reduce 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 (PSV) - more than 80%, the daily disorder of indicators PSV - less than 20%) - 200-600 mg / day;
- Bronchial asthma of moderate severity (FEV or PEF - 60-80%, PEF diurnal variation - 20-30%) - 600-1000 mg / day;
- Severe bronchial asthma (FEV or PEF - 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 appropriate severity. Corticosteroids administered by inhalation in the second step therapy.
Step 2. Basic therapy: beclomethasone dipropionate - 100-400 mg 2 times a day. Step 3. Basic therapy: inhaled corticosteroids in high or standard doses, but when combined with inhaled beta2-adrenergic agonists, long-acting. Beclomethasone dipropionate - high-dose (800-1600, in some cases up to 2000 mg / day).
Stage 4 (severe asthma). Beclomethasone dipropionate - 800-1600 mg / day, in some cases - megadoses to 2000 mg / day.
Step 5 (severe asthma). Beclomethasone dipropionate - 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 the elderly, in patients with renal and hepatic impairment. Skipping a single dose of the drug: Accidental inhalation skipping the next dose should be taken in due time in accordance with the treatment.
Respiratory system: upper respiratory tract candidiasis (probability of increases at doses of 400 mg / day), dysphonia (hoarseness), throat irritation (use the spacer reduces the likelihood of development), paradoxical bronchospasm (immediately cropped via inhalation beta2- adrenomimetic short-acting).
From the digestive tract: oral candidiasis (probability of increases at doses of 400 mg / day), nausea, unpleasant taste.
Allergic reactions: hypersensitivity reactions, including rash, hives, itching, redness and swelling of the 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 drugs
There is no confirmed data on the interaction of beclomethasone dipropionate with other drugs.
Acute overdose could lead to a temporary decrease in the function of the adrenal cortex, which requires emergency treatment, as it can be recovered in a few days, as evidenced by levels of plasma cortisol.
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 can be continued in dosages sufficient to maintain therapeutic effect.
If the drug is given to patients receiving corticosteroids inside the last dose is 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 prior 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 prednisone can be fully transferred to inhalation therapy), while in the first months after the transition should carefully monitor the patient until his pituitary-adrenal the system does not recover sufficiently to provide an 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, transferred to inhalation therapy, should have a supply of Valium and always carry a warning card indicating that in stressful situations, they require additional systemic administration of corticosteroids (after the elimination of stress dose of corticosteroids may be reduced again). Sudden and progressive deterioration of asthma symptoms is a potentially dangerous condition, often life-threatening patient, and requires increasing dose corticosteroids. An indirect measure of treatment failure is more frequent than before, the use of beta2-agonists of short action. With the development of paradoxical bronchospasm should immediately stop using the product, to assess the condition of the patient, conduct a survey and assign therapy with other drugs. 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 in the appointment of corticosteroids inside. It is therefore particularly important that a therapeutic effect, the dose of inhaled corticosteroids has been reduced to the minimum effective dose for controlling diseases. The drug at a dose of 1500 mg / day does not cause most patients significant adrenal suppression. Due to possible adrenal insufficiency when transferring patients receiving GCS inside, inhalation therapy should be particularly careful and regular monitoring of indicators of function of the adrenal cortex. 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 / mechanism is absent.
Before the appointment of inhaled drugs should instruct the patient on the rules of their application, provides the most comprehensive drug penetration into the lungs. The development of oral candidiasis is most likely in patients with high levels of antibodies precipitating antikandidoznyh (indicates adjourned earlier candidiasis). After inhalation of the mouth and throat should be rinsed with water. For the treatment of candidiasis, while continuing therapy with antifungal agents may be used for local effects. The drug is not for relief of attacks, and regular everyday use. For cupping apply beta2-agonists short-acting (such as salbutamol). In severe asthma exacerbation or lack of effectiveness of the therapy should increase the dose of inhaled beclomethasone dipropionate and, if necessary, appoint a systemic corticosteroids and / or developing an infection - 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. Protect the eyes from getting the drug; for the prevention of skin lesions eyelids, nose washing is recommended after inhalation. The balloon with the drug can not puncture, disassemble, or throw in a fire, even if it is empty. Upon cooling spray is recommended to take it out of the plastic housing and warm hands for a few minutes (at low temperatures the drug may be ineffective).
Instructions for the patient on the use of the inhaler:
Check the operation of the inhaler before the first use, and if you have not used it for some time.
1. Remove the inhaler cap. Make sure that the outlet tube is no dust and dirt.
2. Hold the can upright, put your thumb on the bottom, and the index - to the top of the balloon.Shake the cartridge up and down.
3. Make the best possible deep breath (without voltage). Firmly hold lips outlet pipe can.
4. Slow deep breathing, press your index finger on the valve cartridge, releasing a dose of medicine. Continue to slowly inhale.
5. Remove the tube from the mouth of the inhaler and hold your breath for 10 seconds or as you can without strain. Exhale slowly.
6. If more than one dose, wait about a minute and then repeat the procedure from step 2. Put the cap back on the inhaler.
If steps 3 and 4 are not in a hurry. At the time of release of the dose is important to breathe in as slowly as possible. First Practice in front of a 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.