Omnadren 250 cycle is bioequivalent to the respective monotherapies in relation to systemic effects of budesonide and formoterol. Despite this, it was noted a small increase in cortisol suppression after taking Symbicort turbuhaler compared to monotherapy. This difference does not affect the clinical safety. No evidence of pharmacokinetic interactions between budesonide and formoterol.
Pharmacokinetic indices for the respective substances are comparable after administration of budesonide and formoterol as monotherapies and as part turbuhaler. For budesonide, when administered as part of a combined preparation, area under the curve, “concentration-time” is somewhat greater drug absorption is faster and the amount of the maximum plasma concentration above.
For formoterol when administered as part of a combination preparation the maximum concentration in blood plasma It coincides with that of single agent. Inhaled budesonide is rapidly absorbed, reaching peak plasma concentrations within 30 minutes after inhalation. The average dose of budesonide, got into the lungs after inhalation via Turbuhaler is 32-44% of the delivered dose. Systemic bioavailability is about 49% of the delivered dose. In children aged 6 to 16 years, the average dose of budesonide, got into the lungs after inhalation differ from that of adults y (final concentration of drug in blood plasma was not determined). Inhaled formoterol is rapidly absorbed, reaching peak plasma concentrations within 10 minutes after inhalation. The average dose of formoterol, got into the lungs after inhalation via Turbuhaler is 28-49% of the delivered dose. Systemic bioavailability of approximately 61% of the delivered dose.
Distribution and metabolism . The plasma protein binds approximately 50% to 90% of formoterol and budesonide. The volume of distribution for formoterol is about 4 l / kg and budesonide – 3 L / kg. Formoterol is inactivated by conjugation (active form O-demethylated metabolites, mostly in the form of inactivated conjugates). Budesonide undergoes biotransformation intense (about 90%) at the first passage through the liver with the formation of metabolites with low glucocorticosteroid activity. Glucocorticosteroid activity of the major metabolite – 6-β-gidroksibudesonida 16-α-hydroxyprednisolone – less than 1% of similar activity of budesonide. There is no evidence of interaction of metabolites or substitution reaction between budesonide and formoterol. The main part of the dose of formoterol is metabolized in the liver and omnadren 250 cycle then excreted by the kidneys: after inhalation 8-13% delivered dose of formoterol is excreted unchanged. Formoterol has a high systemic clearance (approximately 1.4 L / min); the half-life of the drug is on average 17 hours. Budesonide is metabolized primarily by enzyme. Budesonide metabolites excreted by the kidneys in an unmodified form or in the form of conjugates. In urine found only a small amount of unchanged budesonide. Budesonide has a high systemic clearance (approximately 1.2 L / min). The pharmacokinetics of formoterol and budesonide has not been studied in patients with renal insufficiency. Budesonide and formoterol concentration in blood plasma can be increased in patients with liver disease.
• Bronchial asthma, as maintenance therapy and cupping (insufficiently controlled intake of inhaled corticosteroids and beta2-agonists short-acting as a therapy on demand, or adequately controlled with inhaled corticosteroids and beta2-agonists long-acting).
• omnadren 250 cycle (Symptomatic therapy in patients with severe chronic obstructive pulmonary disease (<50% of the estimated settlement level) and repeated exacerbations in history that have marked symptoms despite treatment with bronchodilators long-acting).