Overview
If the above symptoms begin to bother, then it is urgent to interrupt treatment with budesonide and seek the advice of a doctor.
Drug overdose
Toxic reactions in case of an overdose of budesonide are rarely noted. But with prolonged use of the drug in high doses, a systemic reaction to glucocorticosteroids may occur:
- susceptibility to infections;
- the development of hypercorticism;
- decreased adrenal function;
- atrophy of the adrenal cortex.
Compatibility of budesonide for inhalation with other drugs and alcohol
Information on the interaction of drugs with the inhaled form of budesonide is not available. Although it should be expected that Phenobarbital, Phenytoin, Rifampicin and other similar drugs reduce the effectiveness of Budesonide. Estrogens and methandrostenolone enhance the effects of budesonide.
Storage conditions and expiration dates
Budesonide for inhalation should be stored in a dry place away from children. Air temperature should not exceed 30 degrees Celsius. Protect spray can from freezing or direct sunlight. Shelf life - 3 years from the date of release, after opening it is necessary to use the drug for 6 months.
Budesonide Inhalation Analogs
Structural analogues of the drug Budesonide powder for inhalation: Benacort, Pulmacort Turbuhaler, Cyclocaps, Tafen Novolizer, Cycortide, Novopulmon E Novolizer.
Budesonide price
The average price of the drug Budesonide powder for inhalation is 1100 rubles.
International name: Budesonide
1. Dosage form: metered-dose aerosol for inhalation, capsules with powder for inhalation, metered-dose powder for inhalation, metered-dose suspension for inhalation
Chemical name:
(11 beta, 16 alpha) - 16, 17 - (butylidene - bis (oxy) - 11, 21 - dihydroxypregn - 1, 4 - diene - 3, 20 - dion
Pharmachologic effect:
GCS for local use, has anti-inflammatory, anti-allergic and immunosuppressive effects. It increases the production of lipocortin, which is an inhibitor of phospholipase A2, inhibits the release of arachidonic acid, inhibits the synthesis of arachidonic acid metabolism products - cyclic endoperoxides and Pg. Prevents marginal accumulation of neutrophils, reduces inflammatory exudation and cytokine production, inhibits macrophage migration, reduces the severity of processes of infiltration and granulation, the formation of chemotaxis substance (which explains the effectiveness in the 'late' allergy reactions); inhibits the release of inflammatory mediators from mast cells ('immediate' allergic reaction). It increases the number of 'active' Butacort receptors, restores the patient's reaction to bronchodilators, allowing them to be reduced in frequency, reduces swelling of the bronchial mucosa, mucus production, sputum formation and reduces airway hyperresponsiveness. Increases mucociliary transport. It has a fungicidal effect. It is well tolerated with long-term treatment, does not have ISS activity, practically does not have a resorptive effect. The therapeutic effect develops on average after 5-7 days. Inhalation of budesonide can prevent an attack of bronchial asthma, but does not reduce acute bronchospasm.
Pharmacokinetics:
Absorption is low. After inhalation, the alveoli reaches 25% of the dose, about 1/3 of the budesonide entering the alveoli is absorbed (a significant part is deposited on the mucous membrane of the oropharynx and is swallowed, bioavailability is 10% of the amount received in the stomach). TCmax - 15-45 min. After inhalation using a turbuhaler, the alveoli reaches about 40% of the total dose. After inhalation, 800 μg of budesonide Cmax - 4 nmol / L, TCmax - 30 min. After inhalation using a nebulizer, bioavailability is 15% of the total dose and 40-70% of the delivered dose. After inhalation of 1 and 2 mg of budesonide Cmax, respectively, 2.4 and 4 nmol / L, TCmax - 10-30 minutes. The systemic clearance of an inhaled drug is 0.5 l / min. Distribution volume - 3 l / kg. Communication with plasma proteins - 88%. Part of the gastrointestinal tract undergoes significant (about 90%) metabolism during the 'first passage' through the liver (with the participation of microsomal enzymes) to 6-beta-hydroxybudesonide and 16-alpha-hydroxyprednisolone (systemic clearance - 1.4 l / min). Metabolites are practically devoid of biological activity (100 times less than budesonide). T1 / 2 - 2-2.8 hours. It is excreted through the intestines in the form of metabolites - 10%, by the kidneys - 70%. The concentration of budesonide in blood plasma increases in patients with liver disease.
Indications:
Bronchial asthma (as a basic therapy; with insufficient effectiveness of beta2-adrenostimulants, cromoglycelic acid and ketotifen; to reduce the dose of oral corticosteroids), COPD.
Contraindications:
Hypersensitivity; children up to 3 months (suspension), up to 6 years (powder), up to 16 years (solution for inhalation). With caution. Tuberculosis, fungal, bacterial and viral infections of the respiratory system, pregnancy, lactation.
Dosage regimen:
Inhalation, using a special inhaler (turbuhaler, cyclohaler, etc.). Each capsule of the inhaler contains 200 doses, one portion of the powder separated from the capsule by the inhaler dispenser contains 200 μg of budesonide. Inhaled 200-800 mcg / day for 2-4 breaths. Powder for inhalation. If the previous treatment of bronchial asthma was carried out only by beta2-adrenostimulants or inhaled GCS - 200-400 mcg (1-2 inhalations) 2 times a day; if systemic corticosteroids were used, 400-800 mcg (2-4 inhalations) 2 times a day. The maximum dose for patients receiving only beta2-adrenostimulants is 800 mcg / day; for patients previously treated with inhaled or systemic corticosteroids, 1600 mcg / day. Children over 6 years: 1 inhalation (200 mcg / day), maximal - 2 inhalations 2 times a day (400 mcg / day). Suspension for inhalation. Adults - 1-2 mg, children 3 months-12 years old - 0.25-1 mg, if necessary previously diluted with 2-4 ml of NaCl solution, 2 times a day. After receiving the effect, the dose is reduced to the effective lowest dose necessary to maintain a stable state. In cases where the patient was taking GCS orally, transfer to treatment with budesonide is possible in the stable phase of the disease (for 10-14 days, inhalation and taking GCS are combined inside, then the doses prescribed by mouth are gradually reduced until it is completely canceled).
Side effects:
Coughing, dry oral mucosa, dysphonia, pharyngeal mucosal irritation, candidal stomatitis, dry pharyngeal mucosa, headache, nausea (suspension and aerosol for inhalation), vomiting (capsules with powder for inhalation), bruising or thinning of the skin, unpleasant taste sensations (aerosol for inhalation), bronchospasm, oropharyngeal candidiasis, mental changes (nervousness, motor anxiety, depression or behavior change), allergic reactions (skin rash, contact dermatitis, urticaria). Nasal spray: irritation of the mucous membrane of the nasal cavity and pharynx, nosebleeds, cough, dryness of the mucous membrane of the nasal cavity, sneezing, fatigue, dizziness, allergic reactions (dermatitis, urticaria, skin rash, angioedema), perforation of the nasal septum, anosmia, tachycardia growth retardation in children.
Special instructions:
Avoid contact with eyes. Children under 6 years of age: safety and efficacy not determined. High doses of the drug can lead to a slowdown in the growth rate and a decrease in the secretion of hydrocortisone in children, so it is recommended that these indicators be constantly monitored during treatment. After using the drug, it is recommended to rinse your mouth with water to reduce the risk of candidal stomatitis. When skipping doses, the drug should be used as soon as possible and all remaining doses should be used on the same day at regular intervals. The drug should not be frozen and exposed to direct sunlight. The spray can not be punctured, disassembled or thrown into the fire, even if it is empty. When cooling the can, it is recommended to remove it from the plastic case and warm it with your hands (at low temperatures, the effectiveness of the drug is reduced). For patients also receiving systemic glucocorticosteroids, dosage reduction should be carried out very slowly and in small doses if the patient was on long-term therapy with systemic glucocorticosteroids (pseudo-rheumatism syndrome is possible). After complete cancellation, prolonged monitoring of the patient (adrenal insufficiency), as well as an assessment of the function of external respiration, is recommended.
Interaction:
Pre-inhalation of beta-adrenostimulants expands the bronchi, improves the intake of budesonide in the Thalomid tract and enhances its therapeutic effect. Taking 200 mg of ketoconazole once a day increases the plasma concentration of orally taken budesonide in a dose of 3 mg on average 6 times. With the appointment of ketoconazole 12 hours after taking budesonide, the concentration in the plasma of the latter increases 3 times. There is no information on such an interaction with inhaled dosage forms of budesonide, however, a noticeable increase in the concentration of the drug in plasma should be expected. Phenobarbital, phenytoin, rifampicin and other microsomal oxidation inducers reduce the effectiveness of GCS systemic action (induction of microsomal oxidation enzymes). Methandrostenolone, estrogens enhance the effect of budesonide.
2. Dosage form: nasal spray dosage
Chemical name:
(11 beta, 16 alpha) - 16, 17 - (butylidene - bis (oxy) - 11, 21 - dihydroxypregn - 1, 4 - diene - 3, 2 0 - dion
Pharmachologic effect:
GCS for local use, has anti-inflammatory and anti-allergic effects. It increases the production of lipocortin, which is an inhibitor of phospholipase A2, inhibits the release of arachidonic acid, inhibits the synthesis of arachidonic acid metabolism products - cyclic endoperoxides and Pg. Prevents marginal accumulation of neutrophils, reduces inflammatory exudation and cytokine production, inhibits macrophage migration, reduces the Butacort of infiltration and granulation processes, the formation of chemotaxis substance (which explains the effectiveness in the 'late' allergy reactions); inhibits the release of inflammatory mediators from mast cells ('immediate' allergic reaction), which plays a significant role in the occurrence of nasal symptoms of allergic genesis and the development of chronic rhinitis. It is well tolerated with long-term treatment, does not have ISS activity, practically does not have a resorptive effect. The therapeutic effect develops after 2-21 days.
