Pharmacological properties
Pharmacodynamics. Beclomethasone dipropionate is a precursor of the active substance with weak affinity for GCS receptors.
When inhaled, systemic absorption of unchanged beclomethasone dipropionate occurs in the lungs with little oral absorption of the dose delivered to the gastrointestinal tract. Before absorption, beclomethasone dipropionate undergoes extensive transformation into its active metabolite, beclomethasone-17-monopropionate. Systemic absorption of beclomethasone-17-monopropionate consists of absorption in the lungs and in the gastrointestinal tract. Absolute bioavailability when inhaled is approximately 60% of the administered dose for beclomethasone-17-monopropionate.
Beclomethasone dipropionate is rapidly eliminated from the systemic circulation by esterase-mediated metabolism. The main metabolic product is the active beclomethasone-17-monopropionate.
The volume of distribution of beclomethasone dipropionate in the plateau phase is moderate (20 L), but that of beclomethasone-17-monopropionate is greater (424 L). Protein binding is moderately high (87%).
Beclomethasone dipropionate and beclomethasone-17-monopropionate have high plasma clearance (150 and 120 l / h), T ½ are 0.5 and 2.7 hours. Approximately 60% of the drug dose is excreted in the feces, 12% - in the urine in the form of free and conjugated polar metabolites. Renal clearance of beclomethasone dipropionate and its metabolites is insignificant.
Indication
Treatment of severe BA in adults, as well as the treatment of patients who require the use of systemic steroids for adequate control of BA symptoms.
Application
The drug Becloforte Evohaler is prescribed only for oral inhalation.
Patients should be aware that Becloforte Evohaler should be used for the prevention of the disease and therefore should be taken regularly, even during the absence of asthma attacks.
The dose is adjusted depending on the individual response.
If improvement after use of short-acting bronchodilators becomes less effective or there is a need for more inhalations than usual, treatment should be reviewed.
Patients who have difficulty synchronizing breathing with the use of an inhaler are recommended to additionally use a spacer - a device to facilitate inhalation of inhaled medications.
The initial dose of the drug should correspond to the severity of the disease. For patients who require high doses of inhaled corticosteroids, the initial dose should be 1000 mcg/day. In the future, the dose of the drug can be adjusted until control of asthma symptoms is achieved or reduced to the minimum effective dose, depending on the individual patient's response.
Adults and children over 12 years of age (including the elderly) 1000 mcg/day; the dose may be increased to 2000 mcg/day. After stabilization of the patient's condition, the dose should be reduced. The daily dose may be divided into 2, 3, or 4 doses.
To obtain optimal results, Becloforte Evohaler must be taken regularly, even in the absence of symptoms.
Patients who have difficulty synchronizing breathing with the use of an inhaler are recommended to additionally use a spacer.
As with other inhalation medications, the therapeutic effect may be reduced if the canister cools. The canister should not be broken, punctured or burned, even when empty.
Before using the inhaler for the first time or after a break in use of 3 days or more, remove the mouthpiece cap by lightly pressing on it from the sides, shake the inhaler well and spray it into the air twice to make sure it is working properly.
Rules for using an inhaler
1. Remove the mouthpiece cap by pressing lightly on the sides.
2. Make sure that there are no foreign objects inside and outside the inhaler, including the mouthpiece.
3. Shake the inhaler well to remove any foreign object from the inhaler and to evenly mix its contents.
4. Hold the inhaler vertically in your hand, placing it between your thumb and the rest of your fingers, with your thumb on the inhaler body below the mouthpiece. Use your other fingers to hold the bottle from below.
5. Exhale as deeply as possible, then place the mouthpiece between your teeth and clasp it with your lips without biting.
6. While breathing in through your mouth, press the top of the inhaler to spray the medication, while continuing to breathe in slowly and deeply (this releases 1 dose of aerosol).
7. Hold your breath, remove the inhaler from your mouth and remove your finger from the top of the inhaler. Continue to hold your breath for as long as possible.
8. If further spraying is required, wait approximately 30 seconds, holding the inhaler vertically. Then follow steps 3-7.
9. Put the cap on the mouthpiece, pressing it gently until you hear a characteristic click.
IMPORTANTLY!
Perform steps 5, 6 and 7 slowly. Inhale as slowly as possible just before pressing. Practice in front of a mirror the first few times. If a "cloud" appears at the tip of the inhaler or at the corners of your mouth, start over from step 2.
If your doctor has given you other instructions on how to use your inhaler, follow them and seek advice if you have any difficulties.
In general, there is no need to clean the inhaler, but if this occurs, the following recommendations should be followed.
1. Remove the metal canister from the plastic inhaler case and remove the mouthpiece cap.
2. Rinse the plastic case and mouthpiece cap with warm water.
3. Dry them inside and out.
4. Place the metal cylinder and mouthpiece cap back in place.
DO NOT PUT THE METAL CYLINDER IN WATER.
Contraindication
Hypersensitivity to any of the components of the drug.
Side effects
Adverse reactions are classified by organ system and frequency: very common (≥1/10), common (≥1/100 to 1/10), uncommon (≥1/1000 to 1/100), rare (≥1/10,000 to 1/1000) and very rare (<1/10,000), including isolated reports. Data on adverse reactions occurring very often, often and infrequently are mainly based on clinical studies. Data on adverse reactions occurring rarely and very rarely are mainly obtained spontaneously.
Infections and infestations: very common - candidiasis of the mouth and throat.
Immune system: Hypersensitivity reactions such as: uncommon - skin rash, urticaria, pruritus, erythema; very rare - angioedema, respiratory symptoms (dyspnea and/or bronchospasm with increased wheezing, cough) and anaphylactoid/anaphylactic reactions have been reported.
Endocrine system. Systemic effects are possible, including (see Precautions): very rarely - Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, decreased bone mineralization, cataracts and glaucoma.
Psychiatric disorders: very rarely - anxiety, sleep disturbances, depression, aggression, behavioral changes, including hyperactivity and agitation (mainly in children).
Respiratory system: often - hoarseness, sore throat; very rarely - paradoxical bronchospasm (see Features of use).
Special instructions
Treatment for BA should be carried out according to a phased program, the patient's condition should be regularly monitored both clinically and by determining indicators of external respiratory function.
Increasing the frequency of use of inhaled short-acting β2-adrenergic agonists signals a gradual loss of asthma control. In these conditions, it is necessary to review therapy. Sudden and progressive deterioration of asthma control is potentially life-threatening, so the dose of GCS should be increased. In patients at risk, peak flowmetry should be performed.
Becloforte Evohaler is not intended for the relief of acute asthma attacks, but for long-term preventive treatment. For the relief of acute asthma attacks, fast-acting and short-acting inhaled bronchodilators should be used.
It is necessary to use the inhaler correctly in order to ensure that the drug reaches the bronchi.
Insufficient response to treatment or severe exacerbation of asthma requires an increase in the dose of Becloforte Evohaler and, if necessary, the use of systemic steroids and/or antibiotics in the presence of infection.
Systemic effects may occur with inhaled corticosteroids, especially at high doses and over long periods of time, but to a lesser extent than with oral steroids. Systemic effects may include Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, decreased bone mineralization, cataracts, and glaucoma. It is therefore important that the dose of inhaled corticosteroids be reduced to the lowest dose at which effective control of asthma symptoms is maintained (see Adverse Reactions).
It is recommended to regularly monitor the growth of children who are receiving long-term treatment with inhaled corticosteroids.
There is individual hypersensitivity to inhaled corticosteroids.
Due to the possibility of adrenal suppression, transferring patients from oral GCS to Becloforte Evohaler requires special attention and constant monitoring of adrenal function.
The process of switching to Becloforte Evohaler and discontinuation of systemic therapy should be gradual and patients should carry a special card with a warning about the need for additional administration of systemic steroid during stressful periods, for example, during a severe asthma attack, severe intercurrent diseases, surgical interventions, injuries.
Similarly, switching from systemic steroid therapy to inhaled steroid therapy can sometimes unmask allergic conditions, such as allergic rhinitis or eczema, that were previously controlled by systemic steroids. These allergic manifestations should be treated with antihistamines and/or topical medications, including corticosteroids.
As with other inhaled corticosteroids, special caution is required when prescribing Becloforte Evohaler to patients with active and latent pulmonary tuberculosis. Treatment with corticosteroids may mask the symptoms of pulmonary tuberculosis and other bacterial, viral and fungal infections of the respiratory tract. Reactivation of pulmonary tuberculosis is possible. If the drug is prescribed to patients with concomitant respiratory tract infections, they should be treated appropriately. The drug should be used with restrictions for the treatment of patients with lung abnormalities, such as bronchiectasis and pneumoconiosis, due to the possibility of fungal infection. After using the drug, the oral cavity should be rinsed with water.
The drug should not be prescribed to patients with herpes simplex and asthmatic status.
As with other inhaled medications, paradoxical bronchospasm with rapidly progressive dyspnea after inhalation may occur. In such cases, rapid-acting inhaled bronchodilators should be used immediately, Becloforte Evohaler inhalation should be discontinued immediately, the patient should be examined and, if necessary, alternative therapy should be instituted.
Patients should be warned that the drug contains small amounts of ethanol and glycerin. In therapeutic doses, the amount of ethanol and glycerin is extremely small and does not pose a risk to patients.
Use during pregnancy and breastfeeding. The safety of Becloforte Evohaler during pregnancy has not been definitively established. When deciding whether to use the drug during pregnancy, the ratio of the expected benefit to the mother and the potential risk to the fetus should be assessed. Inhalation of beclomethasone may be accompanied by intrauterine growth retardation of the fetus.
The drug penetrates into breast milk, but in very small quantities. The appointment of the drug during breastfeeding should be considered taking into account the fact that the therapeutic benefit of the drug should be higher than the possible risk to the fetus.
Children: Not recommended for use in children under 12 years of age.
Ability to influence the reaction rate when driving vehicles or operating other mechanisms. Becloforte Evohaler does not affect the ability to drive vehicles and operate other mechanisms.
Interactions
Becloforte Evohaler contains a very small amount of ethanol, so theoretically, in patients with hypersensitivity, an interaction is possible when taken simultaneously with disulfiram or metronidazole.
Overdose
When using Becloforte Evohaler in doses exceeding the recommended ones, temporary suppression of the function of the adrenal cortex is possible. This condition does not require emergency care, since the function of the adrenal cortex will recover after a few days, which is confirmed by the level of cortisol in the blood plasma. However, when using the drug in doses exceeding the recommended ones, some suppression of the adrenal function is possible for a long time. In such cases, it is necessary to check the reserve of adrenal function. Treatment with Becloforte Evohaler should be continued at doses approved for the control of BA.
There is no specific treatment for overdose with beclomethasone dipropionate. In case of overdose, supportive therapy should be provided with appropriate monitoring as necessary. Further treatment should be according to the clinical situation or local recommendations, if available.
Storage conditions
At a temperature not exceeding 30 °C.
Immediately after use, close the mouthpiece with the cap, pressing it gently until a characteristic click appears. Avoid exposure to direct sunlight. Do not freeze.
You can report an adverse event to GlaxoSmithKline Pharmaceuticals Ukraine LLC by phone: (044) 585-51-85 or e-mail: oax70065@gsk.com. You can complain about the quality of the drug by phone: (044) 585-51-85, +38 (050) 381-43-49 or e-mail: ua.complaints@gsk.com
For additional information, please contact GlaxoSmithKline Pharmaceuticals Ukraine LLC: 02152, Kyiv, Pavla Tychyny Ave., 1V.
Tel. : (044) 585-51-85, fax: (044) 585-51-92.
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UA / RESP / 0053 / 18.11.20
