Synthetic glucocorticosteroids (GCS) for the topical (inhaled) applications, has anti-inflammatory, anti-allergic and immunosuppressive effect. Increases production lipomodulina, an inhibitor of phospholipase A, inhibits the synthesis of arachidonic acid and its products of metabolism, cyclic endoperekisey and prostaglandins. It prevents the accumulation of neutrophils boundary, reduces the inflammatory exudation and production of lymphokines inhibits the migration of macrophages, reduces the intensity of infiltration and granulation processes, the formation of chemotactic substances (which explains the efficacy in the “late” reactions, allergies); inhibits the release of mast cell inflammatory mediators ( “immediate” allergic reaction). It increases the number of active beta – adrenergic receptors, eliminating their desensitization (restores the patient’s response to bronchodilators, allowing you to reduce the frequency of their use) reduces the bronchial mucosa swelling, mucus production. It improves mucociliary transport. Well tolerated in long-term treatment has not mineralokortikosteroidnoy activity almost no resorptive action.
Absorption – low. After inhalation of 20-25% reaches the small bronchi, the dose received by the gastro – intestinal tract (GIT), and almost completely absorbed (90%) of biotransformation in the liver to inactive metabolites. Bioavailability – 10% of the amount released to the stomach and 28% – for pulmonary fraction. Time of occurrence of the maximum concentration in plasma -15-45 minutes after inhalation. Relationship to plasma proteins – 88%. It has a high systemic clearance – 84 l / h half-life -. 2.8 hours, maximum plasma concentration of -0.01 mmol / L. Displayed through the intestine in the form of metabolites to 10%, kidneys 70%.
testimony to application :
Benacort prescribed as a basic anti-inflammatory agent in various forms and degrees of severity of asthma (including hormone-dependent – to reduce the dose of oral corticosteroids..); the lack of effectiveness of bronchodilators and / or cromoglicic acid and nedocromil sodium. Chronic obstructive pulmonary disease (COPD) with varying severity of airway obstruction.
Increased sensitivity and idiosyncrasy of the drug. Pulmonary tuberculosis (active form), bacterial and viral infections of the respiratory, acute bronchospasm, asthmatic status (as a priority means), bronchitis neastmaticheskoy nature. Children under 16 years old. Be wary of liver cirrhosis, glaucoma, hypothyroidism, bacterial, fungal, parasitic and viral infections (in Vol. H. Amebiasis, tuberculosis, herpes of the lips and eyes), osteoporosis.
Note : Caution should be exercised when administered to patients during pregnancy and lactation.
process applications and dose :
Benacort used by inhalation, using individual portable inhaler “tsiklohalera”. A single dose contains 200 micrograms of buy andriol testocaps. The daily dose benacort selected individually, taking into account the severity of the asthma and the maintenance dose of oral glucocorticosteroids. As recommended initial daily dose of 2-8 single doses a day (400 mcg of buy andriol testocaps -1600). For maintenance treatment is typically fairly 1-4 individual doses per day (200 – 800 g of buy andriol testocaps). During an exacerbation of asthma benacort dose should be increased to 4 – 8 doses per day. The maximum daily dose is 2,000 mg / day. The daily dose of inhaled benacort in 2- 4 admission. The duration of treatment up to 3 to 12 months, depending on the severity of asthma. In those cases where the patient receives the SCS inwardly move benacort treatment follows in a stable phase of the disease. First, you need to combine the continuation of buy andriol testocaps inhalation receiving corticosteroids orally for 14-20 days.
After that produce a gradual reduction in the dose of drugs taken by mouth, until their complete abolition, if possible. Preliminary inhalation beta -2 adrenoceptor agonists (salbutamol) extends bronchi and improves the flow of buy andriol testocaps in the airways, thereby enhancing its therapeutic effect.
side action :
Hoarseness, cough resulting from settling of the drug in the oropharynx. Irritation of the throat and oral mucosal candidiasis, xerostomia, oral candidiasis, headache, nausea, changes in taste sensations, bruising; rarely paradoxical bronchospasm, zzofagealny candidiasis, mental changes (anxiety, restlessness, depression, behavioral changes). High doses (more than 2,000 mg) may cause the development of systemic side effects of corticosteroids.
Interaction from other drugs means :
In the treatment of asthma benacort well with beta -2 agonists, kromoglitsievoy acid or sodium nedocromil, methylxanthines and iprotropiya bromide.
Phenobarbital, phenytoin, rifampin reduce the effectiveness (induction of enzymes of microsomal oxidation). Methandrostenolone, estrogens increase the effect of buy andriol testocaps.
Information about the interaction of ketoconazole with inhaled buy andriol testocaps is not, however, expect a noticeable increase in drug concentration in blood plasma.
special instructions :
In acute, severe attack of asthma (status asthmaticus) the drug is not a means of “first aid”. instructions must be strictly observed by the use of an inhaler “tsiklohalera”. After inhalation, it is recommended to hold their breath for 10 seconds. The presence of sodium benzoate, the drug reduces the risk of upper respiratory tract candidiasis.