Beklometazon-aeronativ

General characteristics. Structure:

Active ingredient: 0,05 mg, 0,1 mg or 0,25 mg of beclomethasone of Dipropionas in 1 dose.

Excipients: Alcohol the absolutized brands A, triethyl citrate, R 134a propellant (1,1,1,2-tetraftoretan).

Pharmacological properties:

Pharmacodynamics. Beclomethasone Dipropionas is pro-medicine and possesses a weak tropnost to GKS-receptors. Under the influence of esterases it turns into an active metabolite – beclomethasone-17-monopropionate (B-17-MP) which renders the expressed local antiinflammatory effect. Reduces an inflammation due to decrease in formation of substance of a chemotaxis (influence on "late" reactions of an allergy), slows down development of "immediate" allergic reaction (it is caused by braking of products of metabolites of arachidonic acid and decrease in release from mast cells of mediators of an inflammation) and improves mukotsiliarny transport.

Under the influence of beclomethasone the quantity of mast cells in a mucous membrane of bronchial tubes decreases, epithelium hypostasis, slime secretion by bronchial glands decreases, hyperreactivity of bronchial tubes, regional accumulation of neutrophils, inflammatory exudate and products of lymphokines, is braked migration of macrophages, intensity of processes of infiltration and granulation decreases. Increases quantity of active beta adrenoceptors, recovers reaction of the patient to bronchodilators, allows to reduce the frequency of their use. Practically has no resorptive effect after inhalation introduction.

Does not stop a bronchospasm, the therapeutic effect develops gradually, usually in 5-7 days of course use of beclomethasone of Dipropionas.

Pharmacokinetics. Absorption. More than 25% of a dose of the inhalated drug settle in respiratory tracts, the remained quantity settles in a mouth, a throat and is swallowed. In lungs before beclomethasone absorption Dipropionas is intensively metabolized to an active metabolite of B-17-MP. System absorption of B-17-MP happens in lungs (36% of pulmonary fraction) in digestive tract (26% from arrived here at a dose proglatyvaniye).

Absolute bioavailability of invariable beclomethasone of Dipropionas and B-17-MP makes respectively about 2% and 62% of the inhalated dose. Beclomethasone Dipropionas is quickly soaked up, time of achievement of the maximum concentration in
to blood plasma (Tmax) makes 0,3 p. B-17-MP it is soaked up more slowly, Tmax makes 1 h.

Approximately linear dependence between increase in the inhalated dose and system exposure of drug is noted.

Distribution. Distribution in fabrics makes 20 l for beclomethasone of Dipropionas and 424 l for B-17-MP. Communication with proteins of a blood plasma rather high – 87%.

Metabolism and removal. Beclomethasone Dipropionas and B-17-MP have high plasma clearance (150 l/h and 120 l/h respectively). The elimination half-life makes 0,5 h and 2,7 h, respectively.

Indications to use:

• Basic therapy of various forms of bronchial asthma at adults and children is more senior than 4 years.
• A maintenance therapy at the chronic obstructive pulmonary disease (COPD) at patients with value of volume of the forced exhalation (OFV1) <50% of due sizes (after bronchodilator inhalation) and repeated aggravations in the anamnesis at which the expressed symptoms of a disease remain, despite regular therapy by bronchodilators.

Route of administration and doses:

The drug "Beklometazon-aeronativ" is intended only for inhalation introduction.

Bronchial asthma. Adults and children at the age of 12 years are also more senior: Beklometazon-aeronativ it is applied regularly (even in the absence of disease symptoms), the dose of beclomethasone of Dipropionas is selected taking into account severity of bronchial asthma and clinical effect in each case. The daily dose is divided into several receptions. The recommended initial doses of drug:

• bronchial asthma of an easy current – 200 – 600 mkg/days
• bronchial asthma of a medium-weight current – 600 – 1000 mkg/days
• bronchial asthma of a heavy current – 1000 – 2000 mkg/days

Children aged from 4 up to 12 years: to 400 mkg a day in stages. Depending on the individual answer of the patient, the dose of drug can be increased before emergence of clinical effect or to reduce to a minimal effective dose. Upon transition to a high dose of inhalation beclomethasone of Dipropionas many patients receiving system glucocorticosteroids will be able to reduce their dose or to cancel them absolutely.

Chronic obstructive pulmonary disease. The maximum recommended dose of Beklometazon-aeronativ at HOBL makes 2000 mkg a day. At the accidental admission of inhalation the following dose needs to be accepted according to the scheme of treatment in due time. Introduction can be carried out with use of the special dosers (spacers) improving distribution of drug in lungs and reducing risk of development of side effects.

Patients with abnormal liver functions. The dose decline is not required by abnormal liver functions from patients of c.

Patients with renal failures. The dose decline is not required by renal failures from patients of c.

Instruction for performing inhalations. Beklometazon-aeronativ it is intended only for inhalation use. Before the first use of an inhaler or if did not use an inhaler week and longer check its work. For this purpose remove a protective cap from an inhaler mouthpiece, well stir up an inhaler and press a cylinder, releasing one stream of drug in air.

Performing inhalation:
Step 1. Remove a protective cap from an inhaler mouthpiece, as shown in the figure 1.

 

Step 2. Vigorously shake an inhaler.

Step 3. To make a slow, full exhalation.

Step 4. Holding a cylinder as shown in the figure 2, to densely clasp with lips a mouthpiece. The cylinder has to be directed by a bottom up (figure 2).

Step 5. Expedite the deepest breath, at the same time press a cylinder bottom before release of one inhalation dose.

Step 6. For several seconds hold the breath, then take out a mouthpiece from a mouth and slowly exhale.

Step 7. To put on a protective cap an inhaler mouthpiece.

Repeat steps 3-6 for receiving the second inhalation dose if it is necessary. After inhalation it is recommended to rinse a mouth and a throat water. Not to swallow of water!

Cleaning of an inhaler. Regularly (weekly) it is necessary to clear an inhaler mouthpiece, as shown in the figure 3.

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 up, but do not use for this purpose heating devices. Place a barrel back in a case and put on a cap. Do not dip a metal barrel into water.

Features of use:

Use at pregnancy and during breastfeeding. At pregnancy and during breastfeeding of Beklometazon-aeronativ it is possible to appoint only if the estimated advantage for mother exceeds any possible risk for a fruit or the child.

Before purpose of inhalation drugs it is necessary to instruct the patient about the rules of their use providing the fullest hit of medicine to the necessary sites of lungs. For prevention of candidiasis of an oral cavity after inhalation it is necessary to rinse an oral cavity and a throat water. For treatment of candidiasis it is possible to use antifungal drugs of local action at simultaneous continuation of therapy of Beklometazonom-aeronativ.

If patients accept GKS inside, then Beklometazon-aeronativ is appointed against the background of reception of a former dose of GKS, at the same time patients have to be in rather stable state. Approximately in 1 – 2 weeks the daily dose of peroral GKS begins to be reduced gradually. The scheme of a dose decline depends 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, an injury, surgical intervention or an infection).

At transfer of patients from reception of system GKS on inhalation therapy allergic reactions (for example, allergic rhinitis, eczema) which were suppressed with system drugs earlier can be shown.

The patients with reduced function of bark of adrenal glands transferred to inhalation treatment have to have a stock of GKS and always carry with themselves the warning card in which it has to be specified that they in stressful situations need additional system purpose of GKS (after elimination of a stressful situation the dose of GKS can be lowered again). The sudden and progressing deterioration in symptoms of asthma is potentially dangerous state, quite often life-threatening patients, and demands increase in a dose of GKS. An indirect indicator of inefficiency of therapy is more frequent, than before, use of b2-adrenostimulyator of short action.

Beklometazon-aeronativ it is intended not for stopping of attacks, and for regular daily use. B2-adrenostimulyator 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 the drug "Beklometazon-aeronativ" and in case of need to appoint system GKS and/or an antibiotic at development of an infection.
At development of a paradoxical bronchospasm it is necessary to stop at once use of Beklometazon-aeronativ, to estimate the patient's condition, to conduct examination and if necessary to appoint therapy other medicines. 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 reception 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. In a dose of 1500 mkg/days drug does not cause essential suppression of functions of adrenal glands in most of patients. Due to the possible adrenal insufficiency it is necessary to observe extra care and to regularly control indicators of function of bark of adrenal glands at transfer of the patients accepting GKS inside on treatment by the drug "Beklometazon-aeronativ".

Sharp drug withdrawal of "Beklometazon-aeronativ" is not recommended. It is necessary to observe extra care at treatment by inhalation GKS of patients with active or inactive forms of a pulmonary tuberculosis.

It is necessary to protect eyes from drug hit. Washing after inhalation it is possible to prevent damage of skin a century and a nose.

The barrel with Beklometazonom-aeronativ cannot be punctured, sorted or thrown into fire even if it is empty. As well as the majority of other means for inhalations in aerosol packages, Beklometazon-aeronativ can be less effective at low temperatures. When cooling a barrel it is recommended to get it from the plastic case and to warm hands within several minutes.

Features of effect of medicine at its cancellation. Because of danger of development of an aggravation it is necessary to avoid sudden drug withdrawal of "Beklometazon-aeronativ". The dose of drug should be reduced gradually under control of the doctor.

Influence on ability to driving of motor transport and to control of mechanisms. Beklometazon-aeronativ does not influence ability to driving of motor transport and control of mechanisms.

Side effects:

Determination of frequency: very often (> 1/10), it is frequent (from 1/100 to 1/10), infrequently (from 1/1000 to 1/100), is rare (from 1/10000 to 1/000), is very rare (<1/10000).

From a metabolism: seldom – a hypercorticoidism; very seldom – symptoms of system glucocorticosteroid effects (including a hypoadrenalism, Cushing's syndrome).

From immune system: seldom – hypersensitivity reactions, rash, urticaria, a Quincke's disease, an itch.

From a musculoskeletal system: decrease in mineral density of a bone tissue.

From respiratory system: often – cough; seldom – a paradoxical bronchospasm, irritation of a throat, the dysphonia disappearing after the termination of therapy or a dose decline of drug.

Others: often – candidiasis of a mucous membrane of an oral cavity and throat. Systemic action of inhalation GKS can be observed at administration of drug in high doses for an appreciable length of time.

Interaction with other medicines:

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

Contraindications:

• Age up to 4 years.
• Hypersensitivity to any component of drug.

With care it is necessary to apply Beklometazon-aeronativ at glaucoma, system infections (bacterial, virus, fungal, parasitic), osteoporosis, a pulmonary tuberculosis, cirrhosis, a hypothyroidism, pregnancy, in the period of a lactation.

Overdose:

The acute overdose of drug can lead to temporary depression of function of bark of adrenal glands that does not demand the emergency therapy as function of bark of adrenal glands 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 similar cases it is recommended to carry out monitoring of reserve function of bark of adrenal glands.

At overdose treatment by beclomethasone can be continued by Dipropionas in the doses sufficient for maintenance of therapeutic effect. In order to avoid overdose patients should not apply Beklometazon-aeronativ in the doses exceeding recommended. Regular assessment of efficiency of therapy and a dose decline of Beklometazona-aeronativ to the minimum level which provides effective control of symptoms of a disease is of great importance.

Storage conditions:

In the place protected from light, at a temperature not above 25 °C, far from heating devices. Not to freeze. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Aerosol for inhalations dosed, 50 mkg / a dose, 100 mkg / a dose, 250 mkg / a dose. On 200 doses of drug in a cylinder aluminum with a raspylitelny nozzle of the dosing action. Each cylinder together with the application instruction is placed in a pack from a cardboard bandbox.