Active substanceBudesonideBudesonide
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  • Dosage form: & nbsppowder for inhalation dosed
    Composition:

    Each dose contains:

    active substance: budesonide 0.2 mg;

    auxiliary substance: lactose monohydrate 7.8 mg.

    Description:

    Inhaler made of polymer material. At the dosing part of the device is put on the lid with a lock. On the front side of the device there is an inscription "Easyhaler®". Side is the counter of the number of remaining doses. The contents of the inhaler are a uniform powder of white or almost white color.

    Pharmacotherapeutic group:Glucocorticosteroid for topical application
    ATX: & nbsp

    R.03.B.A.02   Budesonide

    Pharmacodynamics:

    Budesonide refers to non-halogenated glucocorticosteroids.

    When topically applied, it has a local anti-inflammatory effect on the mucous membrane of the respiratory tract.

    Improvement in the control of bronchial asthma, after budesonide inhalation, can develop within 24 hours after initiation of therapy, although the maximum effect is achieved after several weeks of continuous use of the drug.

    Mechanisms of action of glucocorticosteroids on inflammation in bronchial asthma have not been accurately studied. Shown, that budesonide has a number of inhibitory effects on cells (including eosinophils, macrophages, mast cells, lymphocytes, neutrophils) and mediators (incl.on cytokines, leukotrienes, eicosanoids, histamine), involved in the development of allergic and non-allergic inflammation of the respiratory tract. These effects of glucocorticosteroids may have a value to ensure their clinical effect in bronchial asthma.

    Pharmacokinetics:

    Budesonide, the active substance of the preparation, is a mixture of two isomers (22R and 22S). In studies on the affinity of glucocorticosteroid receptors, it was shown that isomer 22R is 2 times more active than isomer 22S. These two dosage forms, budesonide, do not undergo a mutual transformation. The final half-life period for both isomers is the same (2-3 hours).

    In patients with bronchial asthma, about 15-25% of the dose of budesonide inhaled as part of Isichheiler's preparation reaches the bronchi. The most significant part of the inhaled dose remains in the area of ​​the oropharynx and is swallowed (if not rinse the mouth cavity).

    After budesonide is administered, the maximum plasma concentration in the plasma is reached after approximately 1-2 hours, and the absolute system bioavailability is 6-13%. In plasma, 85-95% of budesonide is bound to a protein.The maximum concentration in the plasma is reached after approximately 30 minutes, after inhalation. The bulk of budesonide entering the lungs is absorbed into the systemic circulation.

    Budesonide is rapidly and largely metabolized in the liver by the cytochrome P4503A4 system with the formation of two major metabolites.

    Glucocorticosteroid activity of these metabolites in vitro is less than 1% of the activity of the starting material. In small amounts, it is metabolized in the lungs and serum.

    Allocation:

    Budesonide is excreted in urine and feces in the form of conjugated and unconjugated metabolites.

    Individual patient groups

    In patients with liver disease, the degree of bioavailability of budesonide may increase.

    In children, the half-life of plasma is significantly lower than in adults.

    Indications:

    Bronchial asthma of mild, moderate and severe course, treatment of chronic obstructive pulmonary disease (COPD).

    Contraindications:

    Hypersensitivity to budesonide, children under 6 years of age, and rare hereditary diseases such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption (since the drug contains lactose).

    Carefully:

    Tuberculosis, fungal, bacterial and viral infections of the respiratory system, cirrhosis, glaucoma, hypothyroidism, osteoporosis.

    Pregnancy and lactation:

    The results of the extensive prospective epidemiological study and the world experience of post-marketing use indicate that the inhalation budesonide, taken during pregnancy, does not have a harmful effect on the health of the fetus / newborn baby.

    During pregnancy, budesonide inhalation should be given only in cases where the potential benefit to the mother exceeds the potential risk to the fetus. It should be used the minimum dose of budesonide necessary to ensure adequate control of the course of bronchial asthma.

    Budesonide is excreted into breast milk. However, in therapeutic doses, it is assumed that it has no effect on the infant breastfed. It is allowed to use inhaled budesonide during the breastfeeding period. Supportive therapy of nursing mothers with inhaled budesonide (200 or 400 μg twice daily) leads to a negligible systemic effect of budesonide on the infant.

    Prescribe budesonide inhalation to lactating mothers only if the expected positive effect on the woman's body exceeds any possible risks to the child.

    Dosing and Administration:

    Inhalation.

    To ensure an optimal response to treatment, Budesonide Ishihler should be taken regularly.

    When transferring patients to inhaled Budesonide Ishihler inhaler therapy from other inhalers, the treatment regimen should be selected individually. In this case, it is necessary to take into account the characteristics of previously used drugs, treatment regimens, the way the drug is used.

    Patients should be given an initial dose of inhaled budesonide, corresponding to the severity or level of control of the course of the disease.

    The therapeutic effect comes in a few days after the start of the drug and reaches its maximum after a few weeks of treatment.

    The dose should be adjusted until complete control of the disease, and then begin its gradual reduction to a minimal dose, ensuring the maintenance of effective control of asthma.

    Initial dose in adults (including the elderly and children / adolescents over 12 years of age) with bronchial asthma of mild course (stage 2) and in children 6-12 years of age is 200-400 mcg / day. If necessary, the dose can be increased to 800 μg / day. In adults with moderate to severe bronchial asthma (stage 3) and severe (stage 4), the initial dose may be up to 1600 μg / day.

    The maintenance dose should be selected in accordance with the severity of the disease and clinical response.

    The dose should be adjusted before the control of the disease progression, then gradually reduce to a minimum, at which effective control of the disease course is still maintained.

    Dosing twice a day

    Adult patients with bronchial asthma of the lung, moderate and severe course (including the elderly and children / adolescents over 12 years of age): the usual maintenance dose is 200-400 μg twice a day. During periods of increased severity of bronchial asthma, the daily dose can be increased to 1600 μg, administered for several (two) doses, and then reduced after stabilizing the course of asthma.

    Dosing once a day

    Adult patientswith bronchial asthma of the lung and moderate course (including the elderly and children / adolescents over 12 years of age): in patients who have not previously received inhaled glucocorticosteroids, the maintenance dose is usually 200-400 μg once a day. In patients who have already controlled the course of the disease with inhaled glucocorticosteroids (for example, budesonide or beclomethasone dipropionate), administered twice a day, 800 μg inhalation can be used once a day.

    Children 6-12 years with bronchial asthma of mild or moderate course: in patients who have not previously received steroids, as well as patients who have inhaled glucocorticosteroids (for example, budesonide or beclomethasone dipropionate), administered twice a day, previously allowed to monitor the course of the disease, the maintenance dose is usually 200-400 μg once a day.

    The patient should be transferred to the inhalation of the drug once a day at the same daily dose (taking into account the characteristics of the drug and the method of administration). After that, the dose should be reduced to the minimum necessary to ensure effective control of the course of bronchial asthma. Patients should be trained to take the drug once a day in the evenings.It is important that the drug is taken continuously and carried out at the same time in the evenings.

    Data for the development of recommendations on the transfer of patients without prior inhalation therapy with glucocorticosteroids on inhalation of the drug Budesonide Pisichler is not enough once a day.

    Patients receiving the medication once a day should be recommended with a worsening of the course of bronchial asthma (for example, with an increase in the frequency of using bronchodilators or with the preservation of symptoms from the respiratory organs) to double the dose of glucocorticosteroids taken by them by switching to their inhalation twice a day. In this case, patients should be advised to see a doctor as soon as possible.

    The patient is constantly at hand should be inhaled bronchodilators of short action, designed to stop the attacks of bronchial asthma.

    When COPD dose is selected by a doctor individually depending on the severity of the disease. Recommended initial doses are 100-400 mcg twice daily. The highest recommended dose is 800 mcg twice daily.

    Operation and Maintenance Manual

    The Ishidler inhaler is controlled by a flow of inhaled air. This means that when the patient inhales air through the mouthpiece, the drug enters the respiratory tract along with the inhaled air.

    Carefully read the instructions for using the inhaler!

    Note

    It is important to pay attention to the following:

    - after opening the laminated package it is recommended to store the device in a protective case to prevent damage to Ishihler during use and increase its resistance to external influences;

    - shake the device and test the powder before first use;

    - in the sitting or standing position, inhale through the mouthpiece quite actively and deeply, to ensure that the optimal dose of the substance enters the bronchi;

    - do not exhale through the mouthpiece, as this will lead to a decrease in the dose to the body. If this still happens, you need to tap the inhaler on a hard surface or on the palm of your hand to extract the powder from the mouthpiece, and then repeat the procedure for taking the drug. In the same way, it is necessary to act if the patient unintentionally turns on the inhaler without a subsequent inhalation.

    - always close the protective cover after using the inhaler to prevent accidental spraying of the powder from the device (which can lead to either an overdose or inhalation of an insufficient amount of the drug when the inhaler is subsequently used);

    - Wash your mouth with water or brush your teeth after inhalation, to minimize the risk of candidiasis of the mouth and throat, and hoarseness of the voice;

    - Regularly clean the mouthpiece with a dry cloth. For purification, water can not be used, since the powder is hygroscopic;

    - replace the Budesonid Ishihler inhaler when a zero appears on the meter, even if some powder is still visible inside the device.

    Side effects:

    Possible undesirable actions are presented according to organ systems and are distributed according to the frequency of development.

    Very Frequent

    (>1/10)

    Frequent

    (>1/100 - <1/10)

    Infrequent

    (>1/1000)

    Rare

    (>1/10000 - <1/1000)

    Very rare

    (<1/10000, including individual cases)

    Bacterial and parasitic infections

    Candidiasis of the pharynx and oral cavity

    Diseases of the immune system

    Hypersensitivity reactions (including rash, contact dermatitis, urticaria, angioedema and anaphylactic shock)

    Endocrine diseases

    Hypocorticism, hypercorticism

    hypofunction of the adrenal glands

    Mental diseases

    Depression, increased aggression, excitability, anxiety, psychosis, behavioral changes in children, anxiety, increased motor activity

    Nervousness, sleep disturbance, irritability

    Eye Diseases

    cataract, glaucoma

    Diseases of the respiratory tract, chest and mediastinal organs

    Hoarseness, cough, irritation in the pharynx

    Bronchospasm

    Gastrointestinal diseases

    Difficulty swallowing

    Nausea, changes in taste

    Diseases of the skin and subcutaneous tissue

    Rash, hives, itching, dermatitis, erythema, angioedema, hematoma

    Musculoskeletal diseases, connective tissue diseases

    Slow growth (in children and adolescents)

    Decreased bone density

    Treatment with inhaled budesonide can lead to the development of candidal infection of the pharynx and oral cavity. Clinical experience shows that candidal infection develops less often if inhalations are carried out before meals and / or rinse the oral cavity after inhalation. In most cases, local antifungal drugs are effective in this disease, and treatment with inhaled budesonide is not necessary.

    Inhaled glucocorticosteroids, especially with prolonged use of high doses, can lead to systemic side effects. Possible systemic side effects include suppression of adrenal function, slowing of growth in children and adolescents, reduction of bone mineral density, cataracts, glaucoma, and susceptibility to various infectious diseases. The ability to adapt to stress can be impaired. Nevertheless, the likelihood of developing the described systemic side effects for the inhaled dosage form of budesonide is significantly lower than for oral glucocorticosteroids.

    Lactose - the filler of this drug - contains small amounts of milk proteins, and therefore can cause allergic reactions.

    In view of the danger of growth retardation in children and adolescents, the growth of patients must be regularly monitored.

    Overdose:

    Overdose Symptoms

    The frequency of acute toxic reactions to budesonide low. With prolonged use of excessively high doses of the drug, systemic reactions to glucocorticosteroids may develop,for example: increased sensitivity to infections, the development of giercercorticism and suppression of adrenal function. There may be atrophy of the adrenal cortex.

    Drug therapy with drug overdose

    In acute overdose, specific emergency treatment is not required. Treatment with inhaled budesonide should be continued at the dose recommended for monitoring the course of bronchial asthma. The function "hypothalamus - pituitary - adrenal cortex" is restored after a few days.

    In stressful situations, it may be necessary, as a precaution, to prescribe glucocorticosteroids (for example, high doses of hydrocortisone) systemically. Patients with atrophy of the adrenal cortex are considered steroid-dependent and, before achieving stabilization of the condition, they are selected with adequate maintenance therapy with a systemic glucocorticosteroid.

    Interaction:

    Metabolic transformation of budesonide is disturbed by substances interacting with the isoenzyme CYP3A4 (eg, itraconazole, ketoconazole, ritonavir, nelfinavir, cyclosporine, ethinyl estradiol and oleandomycin).Simultaneous administration of these inhibitors of the CYP3A4 isoenzyme may lead to an increase in the concentration of budesonide in the plasma. In short courses of therapy (1-2 weeks), this increase has little clinical significance, but with long-term admission it should be considered. Since there is no data to ensure the proper dosage in such cases, combinations of these drugs with budesonide should be avoided. If combination of these drugs is impossible, maximize the time interval between taking these medications and consider reducing the dose of budesonide.

    Phenobarbital, phenytoin, rifampicin and other inducers of microsomal oxidation reduce the effectiveness of systemic glucocorticosteroids (induction of microsomal oxidation enzymes).

    Methandrostenolone, estrogens strengthen the action of budesonide. An increase in the concentration of glucocorticosteroids in the blood plasma and an increase in their activity were observed in women who were given estrogen and steroid contraceptives simultaneously with glucocorticosteroids, but no effect was observed with budesonide and concomitant administration of low doses of combined oral contraceptives.

    In view of the possibility of suppression of adrenal function, a test with stimulation of ACTH in the diagnosis of pituitary insufficiency can give false results (low values).

    Special instructions:

    Inhaler Budesonid Isihayler is not intended for the treatment of acute bronchospasm or asthmatic status. These conditions should be treated in accordance with current recommendations.

    Patients should remember that budesonide Isihheler inhalation powder is a prophylactic drug, and therefore, to ensure optimal performance, it must be used regularly, even in the absence of symptoms of bronchial asthma, and do not stop taking it abruptly.

    The transfer of patients receiving glucocorticosteroids by ingestion to inhaled glucocorticosteroids and their further treatment require additional therapeutic measures.

    Before starting therapy with a high dose of inhaled glucocorticosteroids taken twice a day, the patient's asthma should be quite stable, and inhalations should be performed in addition to the usual maintenance dose of systemic glucocorticosteroids.

    Approximately 10 days later start cancellation systemic glucocorticosteroids, gradually reducing their daily dose (e.g., monthly, reducing the dose to 2.5 mg of prednisolone or another drug - the equivalent value) to the minimum possible level. Sometimes it is possible to completely replace the intake of glucocorticosteroids by inhalation.

    When transferring to inhaled glucocorticosteroids patients with impaired function of the adrenal cortex, in times of stress, such as during surgery, the development of infections weighting asthma attacks may require supplemental assignment systemic glucocorticosteroids. This also applies to patients receiving long-term therapy with high doses of inhaled glucocorticosteroids.

    When translated from the receiving glucocorticosteroid budesonide inwards on inhalation may develop symptoms which previously suppressed systemic glucocorticoid therapy, e.g., the symptoms of allergic rhinitis, eczema, muscle and joint pains. To stop such symptoms, specific treatment methods should be added to the therapy.

    In some patients, the development of a general malaise due to cancellation of the systemic intake of glucocorticosteroids is possible, despite the preservation or even improvement of the respiratory function. In such cases, patients should be instructed to continue treatment with budesonide inhalations and to stop taking glucocorticosteroids internally, despite the presence of clinical indications for cancellation of inhalations, for example, symptoms indicative of adrenal insufficiency.

    As with other methods of inhalation therapy, paradoxical bronchospasm may develop, manifested by the immediate increase in wheezing and the feeling of lack of air after inhalation of the dose of the drug. Paradoxical bronchospasm is stopped with high-speed inhaled bronchodilators, and treatment should be carried out immediately. You must immediately cancel budesonide, conduct a patient examination and, if necessary, prescribe alternative methods of treatment.

    If, despite proper control of the treatment, there was an episode of acute dyspnea, you need to apply a high-speed inhalation bronchodilator and revise the prescribed treatment.In cases where, despite the maximum dose of inhaled glucocorticosteroids, asthma symptoms can not be properly controlled, patients may need a short-term course of systemic glucocorticosteroids. In such situations, therapy with inhaled glucocorticosteroids should be supplemented with systemic drug preparations.

    Systemic consequences of ingestion of inhaled glucocorticosteroids can be observed, in particular, when high doses are prescribed for a long period of time. These consequences are much less likely than the effects of taking oral glucocorticosteroids. Possible Cushing's effects include Cushing's syndrome, Cushingoid appearance, adrenal suppression, growth retardation in children and adolescents, a decrease in bone mineral density, cataracts, glaucoma and, much less often, various psychological and behavioral abnormalities, including psychomotor hyperactivity, sleep disorders, anxiety, depression or aggressiveness (especially in children).

    Therefore, it is very important that the dose of an inhaled glucocorticosteroid is brought to a minimum level, at which the effectiveness of asthma control remains.

    If, despite the use of maximum doses of inhaled glucocorticosteroids, asthma symptoms are not adequately controlled, patients may require a short course of treatment with systemic glucocorticosteroids. In such cases it is necessary to continue therapy with inhaled glucocorticosteroids in combination with treatment with systemic glucocorticosteroids.

    There may be an increased risk of developing pneumonia in patients with newly diagnosed COPD who begin treatment with inhaled glucocorticosteroids.

    In children receiving long-term therapy with inhaled glucocorticosteroids, it is recommended to regularly measure growth. If growth slows down, a treatment regimen should be revised to reduce the dose of an inhaled glucocorticosteroid, if possible, to a minimum, ensuring the maintenance of effective control of the course of bronchial asthma. In addition, it is necessary to send the patient to the pediatrician-pulmonologist.

    In the period of therapy with inhaled glucocorticosteroids, oral candidiasis can be observed. In order to reduce the risk of oral candidiasis and hoarseness, patients should rinse the mouth well or brush their teeth after every intake of an inhaled glucocorticosteroid.Oral candidiasis may require treatment with appropriate antifungal drugs, and some patients may even need to interrupt treatment with inhaled glucocorticosteroids.

    Patients who have a history of dependence on ingested glucocorticosteroids, caused by long-term systemic therapy of glucocorticosteroids, develop adrenocortical dysfunction. To restore it after therapy with glucocorticosteroids inside may take a long time, and therefore, when transferring patients with the dependence on orally taken glucocorticosteroids on budesonide the risk of dysfunction of the adrenal cortex may persist for a fairly long time. In such cases, the function "hypothalamus-hypophysis-adrenal cortex" should be regularly monitored.

    Exacerbation of clinical manifestations of bronchial asthma may be due to acute bacterial infections of the respiratory tract, and this may require treatment with appropriate antibiotics. In such cases, patients sometimes have to increase the dose of inhaled budesonide and conduct a short course of glucocorticosteroid therapy inside.As a first-line therapy for relief of asthma attacks, high-speed inhaled bronchodilators should be used.

    Before starting therapy with budesonide Ishihler inhaler, patients with active or inactive form of pulmonary tuberculosis should conduct specific diagnostic and adequate specific treatment measures to ensure control of this disease. Similarly, in patients with fungal, viral or other respiratory infections, careful observation and specific therapy should be provided and Budesonide Isihairer inhaler used only when adequate therapy for these infections is provided.

    Patients with excessive mucus secretion in the respiratory tract may need a short course of glucocorticosteroid therapy inside.

    In patients with severe impairment of liver function, treatment with inhaled budesonide can lead to a decrease in the rate of excretion of the drug, and, consequently, to an increase in its systemic bioavailability. In this case, the systemic effects of the drug may develop,so these patients should regularly monitor the function of the "hypothalamus - pituitary - adrenal cortex" system.

    Simultaneous administration of ketoconazole and other potent inhibitors of the CYP3A4 isoenzyme should be avoided. If this is not possible, the time intervals between receptions of interacting drugs should be set as large as possible.

    Patients with rare hereditary lactose intolerance syndromes, lactase deficiency (Lapp syndrome) or impaired absorption of glucose and galactose, this drug can not be taken.

    Effect on the ability to drive transp. cf. and fur:In connection with the possibility of developing neuropsychiatric symptoms, care should be taken when operating vehicles and mechanisms.
    Form release / dosage:

    Powder for inhalation dosed, 0.2 mg / dose.

    Packaging:

    2.5 g of the powder of the preparation is placed in an inhaler from a polymeric material.

    Each inhaler packed in a foil bag made of aluminum laminated, together with the instructions for use, is placed in a pack of cardboard.

    Storage conditions:

    Store at a temperature not exceeding 30 ° C, in a dry place inaccessible to children.

    Shelf life:

    3 years.

    After opening the aluminum bag, use it for 6 months.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002227
    Date of registration:20.10.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Orion Corporation Orion Pharma Orion Corporation Orion Pharma Finland
    Manufacturer: & nbsp
    Representation: & nbspOrion Pharma LLCOrion Pharma LLC
    Information update date: & nbsp19.04.2017
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