Release form, composition and packing Benacort
Powder for inhalation fine grained, white or nearly white. 1 dose of budesonide 200 mcg * Excipients: sodium benzoate.
Solution for inhalation is colorless or slightly yellow, to light opalescence. 1 ml of budesonide * 250 mcg. Excipients: Nipagin, succinic acid, Trilon B, polyethylene 400, propylene glycol, purified water.
Solution for inhalation is colorless or slightly yellow, to light opalescence. 1 ml of budesonide 500 mcg. Excipients: Nipagin, succinic acid, Trilon B, polyethylene 400, propylene glycol, purified water. Generic international name, recommended by WHO, the Russian Federation agreed to write the international name - budesonide.
Clinico-pharmacological group: corticosteroids for inhalation.
Pharmacological action
Corticosteroids for inhalation use. Has anti-inflammatory, antiallergic and immunosuppressive effect. Increases the production lipomodulina, an inhibitor of phospholipase A, inhibits the synthesis of arachidonic acid and products of its metabolism (cyclic endoperoksidov and prostaglandins).
Warns edge aggregation of neutrophils, reduces inflammatory exudation and production of cytokines, inhibits the migration of macrophages, reduces the intensity of infiltration and granulation formation of chemotactic substances, inhibits the release of mast cell inflammatory mediators. Increases the number of active Ī²-adrenergic receptors, eliminating their desensitization (restores the patient response to bronchodilators, can reduce the frequency of their use), reduces swelling of bronchial mucosa, mucus production and reduces airway hyperresponsiveness. Improves mucociliary transport. Well tolerated for prolonged use, has no mineralocorticoid activity, almost no resorptive action. Improved lung function after a few hours after a single dose solution for inhalation (using an inhaler). However, the therapeutic effect develops only after several days of regular use at recommended doses (average 5-7 days). The drug is designed to prevent asthma attacks, and not for acute bronchospasm.
Pharmacokinetics
Absorption and distribution
Systemic absorption of the drug is low. After inhalation of 20-25% reaches the small bronchi, part of the dose that gets into the digestive tract, and almost completely absorbed (90%), biotransformed in the liver to inactive metabolites. Bioavailability of the powder for inhalation is 10% for that part of the dose, which reached the gastrointestinal tract, and 28% - for a fraction of the lung. Bioavailability solution for inhalation is 38%, and 1 / 6 of this magnitude is formed due to ingestion of the drug. Cmax of budesonide in plasma is reached 15-45 minutes and is 0.01 mg / dL. Plasma protein binding is 88%. Vd is 3 L / kg.
Breeding
Has a high plasma clearance - 84 l / h. T1 / 2 inhalation route of administration is 2.8 h. Write up to 10% - through the gut in the form of metabolites, 70% - kidneys.
Pharmacokinetics in special clinical situations
Patients with impaired liver function may increase the time spent budesonide in the body.
Statement
asthma (as an antiinflammatory therapy, with lack of effectiveness of bronchodilators and / or cromoglicic acid to reduce the dose of oral corticosteroids);
chronic obstructive pulmonary disease with the proven efficacy of SCS.
Dosing regimen
Powder for inhalation
Inhalation Benakorta conduct by an individual portable inhaler Tsiklohaler. The daily dose is determined individually according to the severity of bronchial asthma and the maintenance dose of oral corticosteroids. The recommended starting dose is 400-1600 mg / day maintenance - 200-800 mcg. During exacerbation of bronchial asthma dose can be increased to 800-1600 mg / day. The maximum daily dose - 2000 mg. The daily dose is administered over 2-4 inhalations. The duration of treatment to 3-12 months, depending on the severity of asthma. When hormone-dependent asthma with oral corticosteroids to move to the therapy.
Benakortom should be in a stable phase of the disease, with the first 14-20 days should be combined with the continuation of inhalation Benakorta GCS inside. Then a dose of oral corticosteroids is gradually reduced, until the complete withdrawal (if available).
Rules of the inhaler "Tsiklohaler"
Remove the protective cover, shake the inhaler, push dispenser from the housing inhaler to stop and knock on the grounds dispenser palm, then push the dispenser into the body. Make a full exhalation. Insert the mouthpiece into your mouth and make him a deep and strong breath. Remove the inhaler from the mouth and hold your breath for 10 seconds. When you exhale the exhaled air must pass through an inhaler. If necessary, make repeated inhalation through an inhaler. After the procedure, the inhaler wear a protective boot.
Solution for inhalation
Benakort in the form of solution for inhalation use only through the nebulizer. The dosage regimen set individually. The recommended starting dose for adults is 1-2 mg / day maintenance dose - 0.5-4 mg / day. On reaching effect dose is gradually reduced to the minimum effective, needed to maintain a stable state. In some cases it is possible to use the drug in higher doses (if necessary, a more rapid achievement of therapeutic effect).
Go to the GCS inside to therapy
Benakortom possible in a stable phase of disease (in this case within 10-14 days of combined inhalation and GCS in, then gradually reduce the dose of oral corticosteroids up to a full withdrawal). 1 vial contains a single dose.
Rules of the nebulizer
Open the vial. Fill in the nebulizer through the upper hole necessary amount of the drug. Nebulirovanie produced in accordance with the instructions for the type of nebulizer. Solution for inhalation can be diluted with 0.9% sodium chloride. Volume of the solution of budesonide delivered to the patient's lungs using the nebulizer, is variable and depends on several factors (including time of inhalation, the level of filling chamber specifications nebulizer, individual characteristics of the patient's respiratory function, the use of a mouthpiece or mask).
If you use a mask, make sure that the inhalation mask fits snugly to the face, the face should be washed after inhalation. After each inhalation should rinse your mouth with water. Nebulizer chamber and mouthpiece or mask, wash with warm water using mild detergent (or in accordance with the manufacturer's instructions).
Side effect
From the respiratory system: possible irritation of the mouth and throat, coughing, hoarseness, sore throat, dry mouth, thrush, rarely - paradoxical bronchospasm (usually due to incorrect inhalation technique).
From the digestive system: rarely - nausea, changes in taste sensations, oesophageal candidiasis.
CNS: Rarely - headache, anxiety, motor restlessness, depression, changes in behavior.
Other: rarely - petechiae.
When used in high doses (more than 2000 micrograms) may develop systemic effects of corticosteroids.
Contraindications
pulmonary tuberculosis in an active form;
fungal, bacterial and viral infections of the respiratory system;
acute bronchospasm, asthmatic status (as a means of emergency care);
neastmatichesky bronchitis;
childhood and adolescence to 16 years;
hypersensitivity to the drug.
With caution is prescribed for cirrhosis of the liver, glaucoma, hypothyroidism, other bacterial and parasitic infections (including at amebiaze), osteoporosis.
Pregnancy and lactation
If necessary, use Benakorta during pregnancy and lactation (breastfeeding) should be related to the expected benefit to the mother and the potential risk to the fetus. Data on the allocation of budesonide in breast milk are not available.
Use in hepatic dysfunction
Patients with impaired liver function may increase the time spent budesonide in the body.
Designate caution in liver cirrhosis.
Cautions
Pre-inhalation agonists (salbutamol and its derivatives) expands the bronchi and improves intake of budesonide in the airways, thereby increasing its therapeutic effect. In bronchial asthma Benakort can be used in combination with beta2-agonists, cromoglicic nedokromilom acid or sodium, methylxanthines, and ipratropium bromide. Avoid getting solution for inhalation in the eye. Benakort in the form of solution for inhalation can be used in patients who can not apply the other formulations for inhaled corticosteroids (elderly and senile).
One dose of powder for inhalation contains 9.8 milligrams of sodium benzoate, used as a carrier of the active substance, it has antifungal activity and reduces the risk of respiratory tract candidiasis.
In the transition from inside the GCS on drug therapy Benakort as a solution to decrease the dose of inhaled corticosteroids for systemic use should be made very slowly and in small doses, because patients may initially experience symptoms not associated with asthma (such as rhinitis, eczema, sore muscles and joints) as well as fatigue, headaches, nausea, and vomiting.
Powder for inhalation fine grained, white or nearly white. 1 dose of budesonide 200 mcg * Excipients: sodium benzoate.
Solution for inhalation is colorless or slightly yellow, to light opalescence. 1 ml of budesonide * 250 mcg. Excipients: Nipagin, succinic acid, Trilon B, polyethylene 400, propylene glycol, purified water.
Solution for inhalation is colorless or slightly yellow, to light opalescence. 1 ml of budesonide 500 mcg. Excipients: Nipagin, succinic acid, Trilon B, polyethylene 400, propylene glycol, purified water. Generic international name, recommended by WHO, the Russian Federation agreed to write the international name - budesonide.
Clinico-pharmacological group: corticosteroids for inhalation.
Pharmacological action
Corticosteroids for inhalation use. Has anti-inflammatory, antiallergic and immunosuppressive effect. Increases the production lipomodulina, an inhibitor of phospholipase A, inhibits the synthesis of arachidonic acid and products of its metabolism (cyclic endoperoksidov and prostaglandins).
Warns edge aggregation of neutrophils, reduces inflammatory exudation and production of cytokines, inhibits the migration of macrophages, reduces the intensity of infiltration and granulation formation of chemotactic substances, inhibits the release of mast cell inflammatory mediators. Increases the number of active Ī²-adrenergic receptors, eliminating their desensitization (restores the patient response to bronchodilators, can reduce the frequency of their use), reduces swelling of bronchial mucosa, mucus production and reduces airway hyperresponsiveness. Improves mucociliary transport. Well tolerated for prolonged use, has no mineralocorticoid activity, almost no resorptive action. Improved lung function after a few hours after a single dose solution for inhalation (using an inhaler). However, the therapeutic effect develops only after several days of regular use at recommended doses (average 5-7 days). The drug is designed to prevent asthma attacks, and not for acute bronchospasm.
Pharmacokinetics
Absorption and distribution
Systemic absorption of the drug is low. After inhalation of 20-25% reaches the small bronchi, part of the dose that gets into the digestive tract, and almost completely absorbed (90%), biotransformed in the liver to inactive metabolites. Bioavailability of the powder for inhalation is 10% for that part of the dose, which reached the gastrointestinal tract, and 28% - for a fraction of the lung. Bioavailability solution for inhalation is 38%, and 1 / 6 of this magnitude is formed due to ingestion of the drug. Cmax of budesonide in plasma is reached 15-45 minutes and is 0.01 mg / dL. Plasma protein binding is 88%. Vd is 3 L / kg.
Breeding
Has a high plasma clearance - 84 l / h. T1 / 2 inhalation route of administration is 2.8 h. Write up to 10% - through the gut in the form of metabolites, 70% - kidneys.
Pharmacokinetics in special clinical situations
Patients with impaired liver function may increase the time spent budesonide in the body.
Statement
asthma (as an antiinflammatory therapy, with lack of effectiveness of bronchodilators and / or cromoglicic acid to reduce the dose of oral corticosteroids);
chronic obstructive pulmonary disease with the proven efficacy of SCS.
Dosing regimen
Powder for inhalation
Inhalation Benakorta conduct by an individual portable inhaler Tsiklohaler. The daily dose is determined individually according to the severity of bronchial asthma and the maintenance dose of oral corticosteroids. The recommended starting dose is 400-1600 mg / day maintenance - 200-800 mcg. During exacerbation of bronchial asthma dose can be increased to 800-1600 mg / day. The maximum daily dose - 2000 mg. The daily dose is administered over 2-4 inhalations. The duration of treatment to 3-12 months, depending on the severity of asthma. When hormone-dependent asthma with oral corticosteroids to move to the therapy.
Benakortom should be in a stable phase of the disease, with the first 14-20 days should be combined with the continuation of inhalation Benakorta GCS inside. Then a dose of oral corticosteroids is gradually reduced, until the complete withdrawal (if available).
Rules of the inhaler "Tsiklohaler"
Remove the protective cover, shake the inhaler, push dispenser from the housing inhaler to stop and knock on the grounds dispenser palm, then push the dispenser into the body. Make a full exhalation. Insert the mouthpiece into your mouth and make him a deep and strong breath. Remove the inhaler from the mouth and hold your breath for 10 seconds. When you exhale the exhaled air must pass through an inhaler. If necessary, make repeated inhalation through an inhaler. After the procedure, the inhaler wear a protective boot.
Solution for inhalation
Benakort in the form of solution for inhalation use only through the nebulizer. The dosage regimen set individually. The recommended starting dose for adults is 1-2 mg / day maintenance dose - 0.5-4 mg / day. On reaching effect dose is gradually reduced to the minimum effective, needed to maintain a stable state. In some cases it is possible to use the drug in higher doses (if necessary, a more rapid achievement of therapeutic effect).
Go to the GCS inside to therapy
Benakortom possible in a stable phase of disease (in this case within 10-14 days of combined inhalation and GCS in, then gradually reduce the dose of oral corticosteroids up to a full withdrawal). 1 vial contains a single dose.
Rules of the nebulizer
Open the vial. Fill in the nebulizer through the upper hole necessary amount of the drug. Nebulirovanie produced in accordance with the instructions for the type of nebulizer. Solution for inhalation can be diluted with 0.9% sodium chloride. Volume of the solution of budesonide delivered to the patient's lungs using the nebulizer, is variable and depends on several factors (including time of inhalation, the level of filling chamber specifications nebulizer, individual characteristics of the patient's respiratory function, the use of a mouthpiece or mask).
If you use a mask, make sure that the inhalation mask fits snugly to the face, the face should be washed after inhalation. After each inhalation should rinse your mouth with water. Nebulizer chamber and mouthpiece or mask, wash with warm water using mild detergent (or in accordance with the manufacturer's instructions).
Side effect
From the respiratory system: possible irritation of the mouth and throat, coughing, hoarseness, sore throat, dry mouth, thrush, rarely - paradoxical bronchospasm (usually due to incorrect inhalation technique).
From the digestive system: rarely - nausea, changes in taste sensations, oesophageal candidiasis.
CNS: Rarely - headache, anxiety, motor restlessness, depression, changes in behavior.
Other: rarely - petechiae.
When used in high doses (more than 2000 micrograms) may develop systemic effects of corticosteroids.
Contraindications
pulmonary tuberculosis in an active form;
fungal, bacterial and viral infections of the respiratory system;
acute bronchospasm, asthmatic status (as a means of emergency care);
neastmatichesky bronchitis;
childhood and adolescence to 16 years;
hypersensitivity to the drug.
With caution is prescribed for cirrhosis of the liver, glaucoma, hypothyroidism, other bacterial and parasitic infections (including at amebiaze), osteoporosis.
Pregnancy and lactation
If necessary, use Benakorta during pregnancy and lactation (breastfeeding) should be related to the expected benefit to the mother and the potential risk to the fetus. Data on the allocation of budesonide in breast milk are not available.
Use in hepatic dysfunction
Patients with impaired liver function may increase the time spent budesonide in the body.
Designate caution in liver cirrhosis.
Cautions
Pre-inhalation agonists (salbutamol and its derivatives) expands the bronchi and improves intake of budesonide in the airways, thereby increasing its therapeutic effect. In bronchial asthma Benakort can be used in combination with beta2-agonists, cromoglicic nedokromilom acid or sodium, methylxanthines, and ipratropium bromide. Avoid getting solution for inhalation in the eye. Benakort in the form of solution for inhalation can be used in patients who can not apply the other formulations for inhaled corticosteroids (elderly and senile).
One dose of powder for inhalation contains 9.8 milligrams of sodium benzoate, used as a carrier of the active substance, it has antifungal activity and reduces the risk of respiratory tract candidiasis.
In the transition from inside the GCS on drug therapy Benakort as a solution to decrease the dose of inhaled corticosteroids for systemic use should be made very slowly and in small doses, because patients may initially experience symptoms not associated with asthma (such as rhinitis, eczema, sore muscles and joints) as well as fatigue, headaches, nausea, and vomiting.
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