Beclomethasone

General characteristics. Structure:

Active ingredient: 0,05 mg, 0,1 mg or 0,25 mg of beclomethasone of Dipropionas (in terms of 100% substance) in 1 dose.

Excipients: ethanol of 96%, norflurana (тетрафторэтан).

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. In pulmonary fabric of beclomethasone Dipropionas is quickly hydrolyzed to beclomethasone of monopropionate which is in turn hydrolyzed to beclomethasone. A part of a dose which is accidentally swallowed is substantially inactivated at "the first passing" through a liver. In a liver there is Dipropionas beclomethasone transformation process into beclomethasone monopropionate and then - in polar metabolites. Linkng with proteins of plasma of the active agent which is in a system blood-groove makes 87%. The main part of drug (35-76%) is removed during 96 h a GIT, 10-15% - kidneys are preferential in the form of polar metabolites.

Indications to use:

Basic therapy of various forms of bronchial asthma at adults and children is more senior than 4 years.

Route of administration and doses:

Beclomethasone is intended only for inhalation use.

Beclomethasone is applied regularly (even in the absence of disease symptoms), the dose of beclomethasone of Dipropionas is selected taking into account clinical effect in each case.

At the easy course of bronchial asthma the volume of the forced breath (VFB) or the peak expiratory rate (PER) make more than 80% of due sizes with dispersion of indicators of PSV less than 20%.

At a medium-weight current of OFV or PSV makes 60-80% of due sizes, daily dispersion of indicators of PSV of 20-30%.

At a heavy current of OFV or PSV makes 60% of due sizes, daily dispersion of indicators of PSV more than 30%.

Upon transition to a high dose of inhalation beclomethasone of Dipropionas many patients receiving system glucocorticosteroids will be able to reduce their dose, to cancel them absolutely.

The initial dose of Beclomethasone is defined by severity of bronchial asthma. The daily dose is divided into several receptions. 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.

Children aged from 4 up to 12 years. The initial dose makes 50 mkg 2 times a day. If necessary the nachalkny dose can be increased to 100 mkg 2 times a day. Maximum single dose of 200 mkg.

The maximum daily dose - 400 mkg. The daily dose is divided into 2-4 receptions.

Adults and children at the age of 12 years are also more senior. 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.

Treatment of bronchial asthma is based on step approach - therapy is begun according to a step, the corresponding disease severity. Inhalation GKS are appointed at the second step of therapy.

Step 2. Basic therapy. Beclomethasone Dipropionas of 100-400 mkg 2 times a day.

Step 3. Basic therapy. Apply inhalation GKS in a high dose or in a standard dose, but in combination with inhalation p-2-adrenomimetikami long actions. Beclomethasone Dipropionas in a high dose - 800-1600 mkg/days, in some cases megadoses to 2000 mkg/days.

Step 4. Heavy asthma. Beclomethasone Dipropionas in a high dose - 800-1600 mkg/days, in some cases megadoses to 2000 mkg/days.

Step 5. Heavy asthma. Beclomethasone Dipropionas in a high dose (see steps 3 and 4).

Special groups of patients. There is no need to adjust the Beclomethasone dose at elderly people, at patients with a renal or 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.

The instruction for the patient on use of an inhaler. Check work of an inhaler before its first use, and also if you did not use it any time or if the cylinder was cooled up to the low temperature, and then you warmed it to room temperature. For check remove a protective cap from a nozzle inhaler, turn a cylinder a bottom up, having put an index finger on a cylinder bottom, and a thumb - on a nozzle inhaler top, stir up a barrel up-down and make 2 pressing big and index fingers, having directed outlet opening of a nozzle inhaler aside. After emergence of an aerosol stream after the second pressing arrive as it is described below, since words: "Make sure that in an output tube there is no dust and dirt".

At regular use of drug it is necessary to arrive thus:

1. Remove a protective cap from a nozzle inhaler. Make sure that in an output tube there is no dust and dirt.
2. You keep a cylinder in vertical position a bottom up, having put an index finger on a cylinder bottom, and a thumb - on a nozzle inhaler top. Stir up a barrel up-down.
3. Make deeper exhalation (without tension). Densely clamp lips an output tube of a nozzle inhaler.
4. Take a slow deep breath. At the time of a breath by means of pressing big and index release fingers a drug dose. Continue to inhale slowly.
5. Take out a tube of a nozzle inhaler from a mouth and hold the breath for 10 seconds or so as far as you will be able without tension. Slowly exhale.
6. Slee is required more than one dose of medicine, wait about a minute and then repeat actions, since a step 2. Put on back protective cap a nozzle inhaler.
7. When performing steps 3 and 4 you do not hurry. At the time of release of a dose of medicine 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 mouth corners, then start over again from a step 2.

Cleaning of an inhaler. The nozzle inhaler should be cleaned, at least, weekly. Remove a nozzle - an inhaler from a cylinder and rinse it and a protective cap warm water. Do not use hot water. Carefully dry up, but do not use for this purpose heating devices. Put on back protective cap a nozzle inhaler, and it is on a cylinder. Do not dip a cylinder into water.

 

Features of use:

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. Development of candidiasis of an oral cavity is most probable at patients with the high level of precipitant antibodies in blood against Candida fungus that indicates earlier postponed fungal infection. 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 by Beclomethasone.

If patients accept GKS inside, then Beclomethasone 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 gipofizarnoknadpochechnikovy 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, not seldom 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 0-2 adrenostimulyator of short action.

Beclomethasone Dipropionas for inhalations is intended not for stopping of attacks, and for regular daily use. Apply to stopping of attacks (3-2-adrenostimulyatory short actions (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 an antibiotic at development of an infection.

At development of a paradoxical bronchospasm it is necessary to stop at once Beclomethasone use, 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 function 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 into treatment by beclomethasone.

It is recommended to watch dynamics of growth of the children receiving inhalation GKS for a long time regularly.

Introduction can be carried out by means of the special dosers (spacers) improving distribution of drug in lungs and reducing risk of development of side effects.

Sharp drug withdrawal Beclomethasone an aerosol is not recommended.

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

The barrel with Beclomethasone 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, Beclomethasone can be less effective at low temperatures. When cooling a cylinder it is recommended to remove from it a nozzle inhaler and to warm hands within several minutes.

Side effects:

Undesirable reactions are listed depending on anatomokfiziologichesky classification and occurrence. Frequency of occurrence is defined thus: very often 1/10, it is frequent 1/100 and <1/10, infrequently 1/1000 and <1/100, is rare 1/10000 and <1/1000 and is very rare <1/10000.

Infections: very often - candidiasis of a mouth and throat. Use of a spacer and rinsing of a mouth and throat water after inhalation reduces probability of development of these side effects.

From immune system: infrequently - skin reactions of hypersensitivity, including rash, urticaria, the itch, reddening also swelled an eye, persons, lips and a mucous membrane of a mouth and a throat; very seldom - a Quincke's disease, anaphylactic reactions.

From endocrine system: system effects are possible: very seldom - oppression of function of bark of adrenal glands, a growth inhibition at children and teenagers, a cataract, glaucoma.

From respiratory system: often a dysphonia (hoarseness of a voice) or irritation of a mucous membrane of a throat, it is very rare - a paradoxical bronchospasm which needs to be stopped immediately by means of inhalation 3-2-adrenostimulyatora short actions. In case of a paradoxical bronchospasm it is necessary to stop at once use of drug in inhalations, to estimate the patient's condition, to conduct necessary examination and to appoint necessary treatment.

From skin and a hypodermic fatty tissue: often - bruises, thinning of skin.

Interaction with other medicines:

Beclomethasone recovers reaction of the patient to beta-adrenergic agonists, allowing to reduce the frequency of their use.

At combined use with inductors of a microsomal oxidation (including phenobarbital, Phenytoinum, rifampicin, etc.) decrease in efficiency of beclomethasone is possible.

At simultaneous use with metandiyenony, estrogen, beta2-adrenomimetika, theophylline, and also system GKS efficiency of beclomethasone increases.

At simultaneous use beclomethasone strengthens effect of beta adrenomimetik.

Contraindications:

- Hypersensitivity to any component of drug.

- Pulmonary tuberculosis.

- Children's age up to 4 years. The beclomethasone containing 250 mkg in 1 dose is not intended for use in pediatrics (i.e. at children up to 18 years).

With care to apply: at glaucoma, system infections (bacterial, virus, fungal, parasitic), osteoporosis, cirrhosis, a hypothyroidism, pregnancy, in the period of a lactation.

Overdose:

Symptoms: 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 concentration of cortisol in plasma. At chronic overdose permanent suppression of function of bark of adrenal glands can be observed.

Treatment: in similar cases it is recommended to carry out monitoring of reserve function of bark of adrenal glands. At overdose beclomethasone treatment by Dipropionas can be continued in the doses sufficient for maintenance of therapeutic effect.

Storage conditions:

To store at a temperature not above 25 °C. To store far from heating system and direct sunshine. To store in the place, unavailable to children! To protect from falling and blows. A period of validity - 3 years. Not to use after expiry date of the validity.

Issue conditions:

According to the recipe

Packaging:

Aerosol for inhalations dosed 50 mkg / a dose, 100 mkg / a dose or 250 mkg / a dose. On 200 doses in cylinders aluminum with a sheeting, pressurized by the dosing valve and supplied with a nozzle sprayer with a protective cap. Each cylinder together with a nozzle - the sprayer and a protective cap, and also the application instruction is placed in a pack.