БЕКЛОСПИР®

General characteristics. Structure:

Structure: 200 doses Active ingredient: Beclomethasone Dipropionas 0,012g, 0,024g and 0,060g Excipients: ethanol (the alcohol absolutized), гидрофторалкан (HFA134a) to 14,02g. Description. Contents of an aerosol aluminum can with the valve of the dosing action – the suspension which is under pressure and forming a spot of white color when spraying on a slide plate.

Pharmacological properties:

Pharmacodynamics. Beclomethasone Dipropionas is pro-medicine and possesses a weak tropnost to glucocorticosteroid (GKS) receptors. Under the influence of esterases turns into an active metabolite – beclomethasone-17-monopropionate which renders the expressed local antiinflammatory effect due to decrease in formation of substance of a chemotaxis (influence on allergic reactions of the slowed-down type). Suppressing products of metabolites of arachidonic acid and reducing allocation from mast cells of mediators of an inflammation, slows down development of allergic reaction of immediate type. Improves mukotsiliarny transport, reduces quantity of mast cells in a mucous cover of bronchial tubes, reduces epithelium hypostasis, slime secretion by bronchial glands, hyperreactivity of bronchial tubes, regional accumulation of neutrophils, inflammatory exudate and products of lymphokines, slows down migration of macrophages, reduces intensity of processes of infiltration and granulation. After inhalation introduction has practically no resorptive effect. Does not stop a bronchospasm. The therapeutic effect develops gradually, usually in 5-7 days of course use. Due to increase in active beta adrenoceptors recovers reaction of the patient to bronchodilators, allowing to reduce the frequency of their use.  

Pharmacokinetics. More than 25% of the inhalated dose settle in respiratory tracts, the remained quantity – in a mouth, a throat and is swallowed. In lungs before beclomethasone absorption Dipropionas is intensively metabolized to an active metabolite beklome-tazona-17-monopropionate. Its system absorption happens in lungs (36% - pulmonary fraction), in a GIT (26% of the dose which arrived at a proglatyvaniye). Absolute bioavailability of not changed beclomethasone of Dipropionas and beclomethasone-17-monopropionate makes, respectively, about 2 and 62% of the inhalated dose. Beclomethasone Dipropionas is soaked up quickly (Tmax is 0,3 h), beclomethasone-17-monopropionate – more slowly (Tmax - 1 h). Distribution in fabrics for beclomethasone of Dipropionas makes 20 l and for beclomethasone-17-monopropionate - 424 l. Communication with proteins of a blood plasma rather high – 87%. Beclomethasone Dipropionas and beclomethasone-17-monopropionate have high plasma clearance (150 and 120 l/h, respectively). T1/2 makes 0,5 and 2,7 h, respectively.

Indications to use:

Bronchial asthma of various forms at adults and children is more senior than 4 years (basic therapy).

Route of administration and doses:

It is inhalation. The dose is selected individually (it can be increased before emergence of clinical effect or to reduce to a minimal effective dose). The initial dose is defined by severity of bronchial asthma. The daily dose is divided into several receptions. Adults and children at the age of 12 years are also more senior. The recommended initial doses of drug: - bronchial asthma of easy severity (the volume of the forced exhalation (VFE) or the peak expiratory rate (PER) - more than 80%, daily dispersion of indicators of PSV - less than 20%) - 200–600 mkg/days; - bronchial asthma of moderate severity (OFV or PSV — 60–80%, daily dispersion of indicators of PSV — 20–30%) — 600–1000 mkg/days; - bronchial asthma of heavy degree (OFV or PSV — 60%, daily dispersion of indicators - more than 30%) — 1000–1200 mkg/days. Treatment of bronchial asthma is based on step approach - therapy is begun according to a step, the corresponding disease severity. GKS is inhalation appoint at the second step of therapy. Step 2. Basic therapy: beclomethasone Dipropionas - 100–400 mkg 2 times a day. Step 3. Basic therapy: GKS in a high or standard dose, but in combination with inhalation introduction of agonists of beta2-adrenoceptors of long action is inhalation. Beclomethasone Dipropionas — in a high dose (800–1600, in some cases to 2000 mkg/days). Step 4 (heavy asthma). Beclomethasone Dipropionas - 800–1600 mkg/days, in some cases - megadoses to 2000 mkg/days. Step 5 (heavy asthma). Beclomethasone Dipropionas - in a high dose (see a step 3,4). Children aged from 4 up to 12 years: to 400 mkg a day in stages. Special groups of patients: there is no need to adjust a dose at elderly people, at patients with a renal and liver failure. Admission of reception of one dose of drug: at the accidental admission of inhalation the following dose needs to be accepted according to the scheme of treatment in due time.

Features of use:

If drug is appointed against the background of reception of GKS inside, the dose of the last remains former. At the same time the patient has to be in rather stable state. Approximately in 1–2 weeks the daily dose of peroral GKS begins to be reduced gradually according to the scheme depending on duration of the previous therapy and on the size of an initial dose of GKS. Regular use of inhalation GKS allows to cancel in most cases peroral GKS (the patients needing reception no more than 15 mg of Prednisolonum can be completely transferred to inhalation therapy), at the same time in the first months after transition it is necessary to control carefully a condition of the patient until his pituitary and adrenal system is recovered sufficiently to provide proper response to stressful situations (for example: injury, surgical intervention or infection). At transfer of patients from system GKS on inhalation allergic reactions are possible (for example: allergic rhinitis, eczema) which were suppressed with system drugs earlier. The patients with reduced function of bark of adrenal glands transferred to inhalation therapy have to have a stock of GKS and always carry with themselves the warning card with the instruction that in stressful situations they need additional system purpose of GKS (after elimination of a stressful situation the dose of GKS can again be lowered). The sudden and progressing deterioration in symptoms of asthma is potentially dangerous state, quite often life-threatening the patient, and demands increase in a dose of GKS. An indirect indicator of inefficiency of therapy is more frequent, than before, use of beta2-adrenomimetik of short action. At development of a paradoxical bronchospasm it is necessary to stop drug use at once, to estimate the patient's condition, to conduct examination and to appoint therapy other HP. At prolonged use of any inhalation GKS, especially in high doses, system effects can be noted (see. "Side effects"), however probability of their development are much lower, than at purpose of GKS inside. Therefore it is especially important that at achievement of therapeutic effect the dose of inhalation GKS was lowered to the minimal effective dose controlling the course of a disease. Drug in a dose of 1500 mkg/days does not cause in most of patients of essential suppression of function of adrenal glands. Due to the possible adrenal insufficiency at transfer of the patient accepting GKS inside into inhalation therapy it is necessary to observe extra care and to regularly control indicators of function of bark of adrenal glands. It is necessary to observe extra care at treatment by inhalation GKS of patients with tuberculosis, as in an active, and inactive form. Data on influence of drug on ability to manage cars/mechanisms are absent. Before purpose of inhalation drugs it is necessary to instruct the patient about the rules of their use providing the fullest hit of HP in lungs. Development of candidiasis of an oral cavity is most probable at patients with the high level of precipitant anti-candidosis antibodies (confirms the candidiasis postponed earlier). After inhalation the oral cavity and a throat should be rinsed water. At simultaneous continuation of therapy by drug it is possible to apply antifungal means of local action to treatment of candidiasis. Drug is intended not for stopping of attacks, and regular daily use. Beta2-adrenomimetik of short action are applied to stopping of attacks (for example salbutamol). At a heavy exacerbation of bronchial asthma or insufficient efficiency of the carried-out therapy it is necessary to increase a dose of inhalation beclomethasone of Dipropionas and in case of need to appoint system GKS and/or at development of an infection - an antibiotic. It is recommended to watch dynamics of growth of the children receiving inhalation GKS for a long time regularly. Sharp drug withdrawal is not recommended. It is necessary to protect eyes from drug hit; for prevention of damage of skin the century, a nose is recommended washing after inhalation. The barrel with drug cannot be punctured, sorted or thrown into fire even if it is empty. When cooling a barrel it is recommended to get it from the plastic case and to warm hands within several minutes (at low temperatures drug can be inefficient).

The instruction for patients on use of an inhaler. Check work of an inhaler before its first use and also if you did not use it any time. 1. Remove a cap from an inhaler. Make sure that in an output tube there is no dust and dirt. 2. You hold a barrel vertically, having put a thumb on a bottom, and index - on a barrel top. Intensively stir up a barrel up-down. 3. Make deeper breath (without tension). Densely clamp lips an output tube of a barrel. 4. Slowly deeply inhaling, press an index finger the barrel valve, releasing a medicine dose. Continue to inhale slowly. 5. Take out a tube of an inhaler from a mouth and hold the breath on 10 with or on how many you will be able without tension. Slowly exhale. 6. If more than one dose of drug are required, wait about a minute and then repeat actions, since a step 2. Put on back a cap an inhaler. When performing steps 3 and 4 you do not hurry. At the time of release of a dose of drug it is important to take a breath as it is possible more slowly. In the beginning be trained in front of the mirror. If you notice "steam" which is coming out a top of a barrel or mouth corners start over again from a step 2.   Cleaning of an inhaler: It is necessary to clean an inhaler not less once a week. Take out a metal barrel from a plastic case and rinse a case and a cap warm water. Do not use hot water. Carefully dry, without using heating devices. Place a barrel back in a case and put on a cap. Do not dip a metal barrel into water.

Side effects:

From respiratory system: candidiasis of upper respiratory tracts (the probability of development increases at doses more than 400 mkg/days), a dysphonia (hoarseness), irritation of a mucous membrane of a throat (use of a spacer reduces probability of their development), a paradoxical bronchospasm (immediately stop by means of an inhalation beta2-adrenomimetik of short action). From bodies of a GIT: oral cavity candidiasis (the probability of development increases at doses more than 400 mkg/days), nausea, unpleasant flavoring feelings. Allergic reactions: hypersensitivity reactions, including rash, urticaria, the itch, reddening also swelled an eye, persons, lips and a mucous membrane of an oral cavity and a throat. Other: system effects, including a headache, bruises or thinning of skin, depression of function of bark of adrenal glands, osteoporosis, a growth inhibition at children and teenagers, a cataract, glaucoma are possible.

Interaction with other medicines:

There are no confirmed data on Dipropionas beclomethasone interaction with other medicines.

Contraindications:

Hypersensitivity to any component of drug. The Sostorozhnost примениять at glaucoma, system infections (bacterial, including a pulmonary tuberculosis, virus, fungal, parasitic), osteoporosis, cirrhosis, a hypothyroidism. Pregnancy and lactation. With extra care only if the potential advantage for mother exceeds possible risk for a fruit and the child.

Overdose:

Symptoms. The acute overdose can lead to temporary depression of function of bark of adrenal glands that does not demand the emergency therapy since it is recovered within several days that is confirmed by cortisol level in plasma. At chronic overdose permanent suppression of function of bark of adrenal glands can be noted. In this case it is necessary to carry out monitoring of reserve function of bark of adrenal glands.

Treatment by drug can be continued in the doses sufficient for maintenance of therapeutic effect.

Storage conditions:

List B. At a temperature not above 30 °C. To protect from freezing. To store in the place, unavailable to children. Period of validity 2 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Aerosol for inhalations dosed 50 mkg / a dose, 100 mkg / a dose and 250 mkg / a dose. On 14,02 g (200 doses) in cylinders aluminum, supplied with the dosing valves, sprayers for antiasthmatic medicines import. Each cylinder together with the application instruction is placed in a pack from a cardboard.