Pharmacological properties of the drug Beclomethasone
Locally acting GCS is used as a basic therapy for asthma and has anti-inflammatory and antiallergic effects. Inhibits the release of inflammatory mediators, increases the production of lipomodulin - an inhibitor of phospholipase A, reduces the formation of arachidonic acid and its metabolic products - cyclic endoperoxides, prostaglandins. Under the influence of beclomethasone, the number of mast cells in the bronchial mucosa decreases, epithelial edema decreases, mucus secretion by bronchial glands, bronchial hyperreactivity, marginal accumulation of neutrophils, inflammatory exudate and lymphokine production, macrophage migration is inhibited, the intensity of infiltration and granulation processes decreases, which ultimately improves indicators of external respiration function. Increases the number of active β-adrenergic receptors, restores the patient’s response to bronchodilators, and allows to reduce the frequency of their use. It has virtually no mineralocorticosteroid activity and no resorptive effect after inhalation administration. In therapeutic doses, it has an active local effect without the development of side effects characteristic of systemic corticosteroids. It does not relieve bronchospasm; the therapeutic effect develops gradually, usually after 5–7 days of course use of beclomethasone dipropionate. Absorption is low; when administered by inhalation in recommended doses, it does not have significant systemic activity. 10–20% of the dose enters the lungs, where beclomethasone dipropionate is hydrolyzed into its active metabolite, beclomethasone monopropionate. Most of the beclomethasone that enters the digestive tract is inactivated during its first passage through the liver. Connection with blood plasma proteins - 87%. The main part (35–76%) is excreted within 96 hours in feces, mainly in the form of polar metabolites, 10–15% in urine.
Beclomethasone ds 50 µg/dose 200 doses nasal dosed aerosol
pharmachologic effect
GKS.
Has anti-inflammatory and anti-allergic effects. Inhibits the release of inflammatory mediators, increases the production of lipomodulin - an inhibitor of phospholipase A, reduces the release of arachidonic acid, and inhibits the synthesis of prostaglandins. Prevents the marginal accumulation of neutrophils, reducing the formation of inflammatory exudate and the production of lymphokines, inhibits the migration of macrophages, which leads to a slowdown in the processes of infiltration and granulation.
Increases the number of active β-adrenergic receptors, neutralizes their desensitization, restores the patient's response to bronchodilators, allowing them to be used less frequently.
Under the influence of beclomethasone, the number of mast cells in the bronchial mucosa decreases, the swelling of the epithelium and the secretion of mucus by the bronchial glands decreases. Causes relaxation of bronchial smooth muscles, reduces their hyperreactivity and improves external respiration function.
Does not have mineralocorticoid activity.
In therapeutic doses it does not cause side effects characteristic of systemic corticosteroids.
When used intranasally, it eliminates swelling and hyperemia of the nasal mucosa.
The therapeutic effect usually develops after 5-7 days of course use of beclomethasone.
When applied externally and locally, it has antiallergic and anti-inflammatory effects.
Composition and release form Beclomethasone ds 50 µg/dose 200 doses nasal dosed aerosol
Aerosol – 1 dose:
- Active substance: beclomethasone 50 mcg.
- Excipients: ethanol 96%, norflurane.
200 doses - aluminum cylinders (1) with a spray nozzle - cardboard packs.
Description of the dosage form
Dosed aerosol for inhalation; in the form of a colorless or almost colorless solution, under pressure in an aluminum cylinder with a metering valve, equipped with a spray nozzle with a protective cap; At the exit of the cylinder, the drug is sprayed in the form of an aerosol jet.
Directions for use and doses
When administered by inhalation, the average dose for adults is 400 mcg/day, the frequency of use is 2-4 times/day. If necessary, the dose can be increased to 1 g/day. For children, a single dose is 50-100 mcg, frequency of use is 2-4 times a day.
When administered intranasally, the dose is 400 mcg/day, the frequency of use is 1-4 times/day.
For external and local use, the dose depends on the indications and the dosage form of the drug used.
Pharmacokinetics
After inhalation administration, part of the dose that enters the respiratory tract is absorbed in the lungs. In lung tissue, beclomethasone dipropionate is rapidly hydrolyzed to beclomethasone monopropionate, which in turn is hydrolyzed to beclomethasone.
The portion of the dose that is inadvertently ingested is largely inactivated on first pass through the liver. In the liver, the process of converting beclomethasone dipropionate into beclomethasone monopropionate and then into polar metabolites occurs.
The binding of the active substance in the systemic circulation to plasma proteins is 87%.
With intravenous administration, T1/2 of beclomethasone 17,21-dipropionate and beclomethasone is approximately 30 minutes. Excreted up to 64% in feces and up to 14% in urine within 96 hours, mainly in the form of free and conjugated metabolites.
Indications for use Beclomethasone ds 50 µg/dose 200 doses nasal dosed aerosol
For inhalation use: treatment of bronchial asthma (including those with insufficient effectiveness of bronchodilators and/or sodium cromoglycate, as well as severe hormone-dependent bronchial asthma in adults and children).
For intranasal use: prevention and treatment of year-round and seasonal allergic rhinitis, including hay fever rhinitis, vasomotor rhinitis.
For external and local use: in combination with antimicrobial agents - infectious and inflammatory diseases of the skin and ear.
Contraindications
For inhalation and intranasal use: severe attacks of bronchial asthma requiring intensive care, tuberculosis, candidomycosis of the upper respiratory tract, first trimester of pregnancy, hypersensitivity to beclomethasone.
Application of Beclomethasone ds 50 µg/dose 200 doses nasal aerosol dosed during pregnancy and breastfeeding
Contraindicated in the first trimester of pregnancy.
Use in the second and third trimesters of pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus. Infants whose mothers received beclomethasone during pregnancy should be closely monitored for adrenal insufficiency.
If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.
Use in children
Preparations for inhalation containing 250 mcg of beclomethasone in 1 dose are not intended for children under 12 years of age. For inhalation administration for children, a single dose is 50-100 mcg, frequency of use is 2-4 times a day.
special instructions
Beclomethasone is not intended for the relief of acute asthmatic attacks. It should also not be used for severe asthma attacks requiring intensive care. The recommended route of administration for the dosage form used should be strictly followed.
Beclomethasone should be used with extreme caution and under close medical supervision in patients with adrenal insufficiency.
The transfer of patients who constantly take GCS orally to inhaled forms can be done only if their condition is stable.
If there is a possibility of developing paradoxical bronchospasm, bronchodilators (for example, salbutamol) are inhaled 10-15 minutes before the administration of beclomethasone.
With the development of candidiasis of the oral cavity and upper respiratory tract, local antifungal therapy is indicated without stopping treatment with beclomethasone. Infectious and inflammatory diseases of the nasal cavity and paranasal sinuses, if appropriate therapy is prescribed, are not a contraindication for treatment with beclomethasone.
Preparations for inhalation containing 250 mcg of beclomethasone in 1 dose are not intended for children under 12 years of age.
Side effects Beclomethasone ds 50mcg/dose 200 doses nasal dosed aerosol
From the respiratory system: hoarseness, feeling of irritation in the throat, sneezing; rarely - cough; in isolated cases - eosinophilic pneumonia, paradoxical bronchospasm, with intranasal use - perforation of the nasal septum. Candidiasis of the oral cavity and upper respiratory tract is possible, especially with long-term use, which resolves with local antifungal therapy without stopping treatment.
Allergic reactions: rash, urticaria, itching, erythema and swelling of the eyes, face, lips and larynx.
Effects due to systemic action: decreased function of the adrenal cortex, osteoporosis, cataracts, glaucoma, growth retardation in children.
Drug interactions
With simultaneous use of beclomethasone with other corticosteroids for systemic or intranasal use, increased suppression of adrenal cortex function is possible. Previous inhaled use of beta-agonists may increase the clinical effectiveness of beclomethasone.
Use of the drug Beclomethasone
Inhalation use Adults (including elderly patients) and children over 12 years of age with mild asthma (forced expiratory volume (FEV) or peak expiratory flow (PEF) - more than 80%, daily variation in PEF indicators - less than 20%) - 200 each –600 mcg/day for 2 inhalations; for moderate asthma (FEV or PEF - 60-80%, daily variation in PEF - 20-30%) - 600-1000 mcg/day for 2-4 inhalations; Severe BA (FEV or PEF - 60%, daily variation in PEF - 30%) - 1000-2000 mcg/day for 2-4 inhalations. The maximum daily dose of the drug in adults should not exceed 1 mg, in very severe cases - 1.5–2 mg/day in 3–4 doses. Children aged 6 to 12 years are prescribed an initial dose of 50–100 mcg 2 times a day. If necessary, the dose can be increased to 400 mcg. The daily dose is divided into 2–4 doses. The maximum daily dose of the drug in children should not exceed 500 mcg. After each inhalation, it is recommended to rinse your mouth with water. Beclomethasone dipropionate, containing 250 mcg per dose, is not intended for use in pediatrics. Intranasal use The recommended dose for adults and children over 12 years of age is 200 mcg (2 inhalations, with the first inhalation directed to the upper and the second to the lower part of the nasal passage) 2 times a day in each nasal passage or 100 mcg in each nasal passage stroke 3–4 times a day; the maximum daily dose is 1000 mcg. Children aged 6–12 years: 42–50 mcg in each nasal passage 3–4 times a day. The total daily dose is 252–400 mcg, the maximum is 500 mcg.
Side effects of the drug Beclomethasone
Dysphonia, throat irritation, cough, sneezing, paradoxical bronchospasm, eosinophilic pneumonia, allergic reactions, candidiasis of the oral cavity and upper respiratory tract (with long-term use and/or when used in high doses). With long-term use in doses of more than 1.5 mg/day, systemic side effects of GCS, headache, dizziness, cataracts, increased intraocular pressure, leukocytosis, lymphopenia, eosinopenia are possible. With a single inhalation of beclomethasone dipropionate in high doses (more than 1 mg), there may be a slight decrease in the function of the hypothalamic-pituitary-adrenal system, which does not require any emergency measures, and treatment should be continued. The function of the hypothalamic-pituitary-adrenal system is restored after 1-2 days.
Beclomethasone, 1 piece, 250 mcg/dose, dosed aerosol for inhalation
Before prescribing inhaled drugs, it is necessary to instruct the patient on the rules for their use, ensuring the most complete delivery of the drug to the desired areas of the lungs. The development of oral candidiasis is most likely in patients with high levels of precipitating antibodies in the blood against the Candida fungus, which indicates a previous fungal infection. After inhalation, you should rinse your mouth and throat with water. To treat candidiasis, topical antifungal drugs can be used while continuing Beclomethasone therapy.
If patients take GCS orally, then Beclomethasone is prescribed while taking the previous dose of GCS, and the patients should be in a relatively stable condition. After about 1–2 weeks, the daily dose of oral corticosteroids begins to be gradually reduced. The dose reduction scheme depends on the duration of previous therapy and the size of the initial dose of GCS. Regular use of inhaled corticosteroids allows, in most cases, to cancel oral corticosteroids (patients who need to take no more than 15 mg of prednisolone can be completely transferred to inhaled therapy). However, in the first months after the transition, the patient's condition should be carefully monitored until his pituitary-adrenal system has recovered sufficiently to ensure an adequate response to stressful situations (for example, injury, surgery or infection).
When transferring patients from taking systemic corticosteroids to inhalation therapy, allergic reactions (for example, allergic rhinitis, eczema) that were previously suppressed by systemic drugs may occur.
Patients with reduced function of the adrenal cortex who are transferred to inhalation treatment should have a supply of GCS and always carry a warning card with them, which should indicate that in stressful situations they need additional systemic administration of GCS (after eliminating the stressful situation, the dose of GCS can be repeated reduce). A sudden and progressive worsening of asthma symptoms is a potentially dangerous condition, often life-threatening for the patient, and requires an increase in the dose of GCS. An indirect indicator of the ineffectiveness of therapy is the more frequent use of short-acting β2-agonists than before.
Beclomethasone dipropionate for inhalation is not intended for the relief of attacks, but for regular daily use. Short-acting β2-adrenergic agonists (for example, salbutamol) are used to relieve attacks. In case of severe exacerbation of bronchial asthma or insufficient effectiveness of the therapy, the dose of inhaled beclomethasone dipropionate should be increased and, if necessary, a systemic corticosteroid and an antibiotic should be prescribed if the infection develops.
If paradoxical bronchospasm develops, you should immediately stop using Beclomethasone, assess the patient's condition, conduct an examination and, if necessary, prescribe therapy with other drugs. With long-term use of any inhaled corticosteroids, especially in high doses, systemic effects may be observed (see “Side effects”), but the likelihood of their development is much lower than when taking corticosteroids orally. Therefore, it is especially important that when a therapeutic effect is achieved, the dose of inhaled corticosteroids is reduced to the minimum effective dose that controls the course of the disease. At a dose of 1500 mcg/day, the drug does not cause significant suppression of adrenal function in most patients. Due to possible adrenal insufficiency, special care should be taken and regular monitoring of adrenal function indicators when transferring patients taking oral corticosteroids to treatment with beclomethasone.
It is recommended to regularly monitor the growth dynamics of children receiving inhaled corticosteroids for a long time.
Administration can be carried out using special dispensers (spacers), which improve the distribution of the drug in the lungs and reduce the risk of side effects.
Abrupt withdrawal of Beclomethasone aerosol is not recommended.
It is necessary to protect the eyes from contact with the drug. By washing after inhalation you can prevent damage to the skin of the eyelids and nose.
The Beclomethasone canister should not be pierced, disassembled or thrown into fire, even if it is empty. Like most other inhalation aerosol products, Beclomethasone may be less effective at low temperatures. When cooling the cylinder, it is recommended to remove the inhaler nozzle from it and warm it with your hands for a few minutes.
Information about the possible effect of the drug on the ability to drive vehicles and machinery
No data.
