Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
GCS. Has anti-inflammatory and anti-allergic effect.
It inhibits the release of inflammatory mediators, increases the production of lipomodulin, an inhibitor of phospholipase A, reduces the release of arachidonic acid, inhibits the synthesis of prostaglandins. It prevents the accumulation of neutrophils, reducing the formation of inflammatory exudates and production of lymphokines, inhibits the migration of macrophages, which leads to a slowing of the processes of infiltration and granulation.
Increases the number of active? -adrenoceptors, neutralizes their desensitization, restores the patient's reaction to bronchodilators, allowing to reduce the frequency of their application.
Under the action of beclomethasone, the number of mast cells in the mucous membrane of the bronchi decreases, the epithelial edema decreases and the mucus secretion by the bronchial glands. It causes relaxation of the smooth muscles of the bronchi, reduces their hyperreactivity and improves the function of external respiration.
Does not have mineralocorticoid activity.
In therapeutic doses does not cause side effects, characteristic of systemic GCS.
With intranasal application, it eliminates edema, hyperemia of the nasal mucosa.
The therapeutic effect usually develops after 5-7 days of course use of beclomethasone.
With external and local application has anti-allergic and anti-inflammatory effect.
PHARMACOKINETICS
After inhalation, a portion of the dose that enters the respiratory tract is absorbed into the lungs. In the lung tissue of beclomethasone, dipropionate is rapidly hydrolyzed to beclomethasone monopropionate, which in turn hydrolyses to beclomethasone.
Part of the dose, which is unintentionally swallowed, is largely inactivated by "first passing" through the liver. In the liver, beclomethasone dipropionate converts into beclomethasone monopropionate and then into polar metabolites.
The binding with plasma proteins of the active substance in the systemic circulation is 87%.
With iv injection of Tl 1/2 beclomethasone 17,21-dipropionate and beclomethasone are approximately 30 min. Output is up to 64% with feces and up to 14% in urine for 96 h mainly in the form of free and conjugated metabolites.
INDICATIONS
For inhalation application: treatment of bronchial asthma (including with insufficient effectiveness of bronchodilators and / or cromoglycate sodium, as well as hormone-dependent bronchial asthma of severe course in adults and children).
For intranasal use: the prevention and treatment of year-round and seasonal allergic rhinitis, including rhinitis in hay fever, vasomotor rhinitis.
For external and topical application: in combination with antimicrobial agents - infectious and inflammatory diseases of the skin and ear.
DOSING MODE
With inhalation, the average dose for adults is 400 Ојg / day, the frequency of application is 2-4 times / day. If necessary, the dose may be increased to 1 g / day. For children, a single dose of 50-100 Ојg, the frequency of application - 2-4 times / day.
With intranasal administration, the dose is 400 Ојg / day, the frequency of application is 1-4 times / day.
For external and local administration, the dose depends on the indications and the drug dosage form used.
SIDE EFFECT
On the part of the respiratory system: hoarseness, sensation of irritation in the throat, sneezing; rarely - cough; in isolated cases - eosinophilic pneumonia, paradoxical bronchospasm, with intranasal application - perforation of the nasal septum. Possible candidiasis of the oral cavity and upper respiratory tract, especially with prolonged use, taking place with local antifungal therapy without discontinuing treatment.
Allergic reactions: rashes, hives, itching, erythema and swelling of the eyes, face, lips and throat.
Effects caused by systemic action: decreased function of the adrenal cortex, osteoporosis, cataract, glaucoma, growth retardation in children.
CONTRAINDICATIONS
For inhalation and intranasal use: severe attacks of bronchial asthma requiring intensive care, tuberculosis, candidomycosis of the upper respiratory tract, I trimester of pregnancy, hypersensitivity to beclomethasone.
PREGNANCY AND LACTATION
Contraindicated in the first trimester of pregnancy.
Application in the II and III trimesters of pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. Newborns, whose mothers received beclomethasone during pregnancy, should be carefully screened for the lack of adrenal function.
If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.
APPLICATION FOR CHILDREN
Preparations for inhalation use, containing 1 dose of 250 Ојg beclomethasone, are not intended for children under 12 years of age. When inhaled for children, a single dose of 50-100 Ојg, the frequency of application - 2-4 times / day.
SPECIAL INSTRUCTIONS
Beclomethasone is not intended for relief of acute asthmatic attacks. It should also not be used in severe asthma attacks requiring intensive care. The recommended route of administration for the dosage form to be used should be strictly observed.
With special care and under close supervision of the doctor, beclomethasone should be used in patients with adrenal insufficiency.
The transfer of patients permanently taking GCS inside, on inhalation forms can be performed only in a stable state.
If there is a possibility of developing paradoxical bronchospasm for 10-15 min before the administration of beclomethasone, bronchodilators (for example, salbutamol) are inhaled.
With the development of candidiasis of the oral cavity and upper respiratory tract, local antifungal therapy is indicated without discontinuing beclomethasone treatment. Infectious and inflammatory diseases of the nasal cavity and paranasal sinuses in the appointment of appropriate therapy are not a contraindication for treatment with beclomethasone.
Preparations for inhalation use, containing 1 dose of 250 Ојg beclomethasone, are not intended for children under 12 years of age.
DRUG INTERACTION
With the simultaneous use of beclomethasone with other GCS for systemic or intranasal use, it is possible to enhance the suppression of adrenal cortex function. The previous inhalation use of beta-adrenostimulants may increase the clinical efficacy of beclomethasone.
