Upon receiving Cyclosporine hexane stable absorption observed and almost no influence food intake, which ensures low variability expressed pharmacokinetics and effect relationship between the drug and the highest dose. Absorption: After primo steroid oral administration, the maximum concentration of cyclosporine in the blood plasma is achieved in the time interval 95.0 . ± 42,1 minutes distribution: Cyclosporine is primarily distributed in the bloodstream to the magnitude of the apparent volume of distribution of 3 – 5 l / kg. The plasma is determined by 33 to 47%, in granulocytes – from 5 to 12% in the lymphocytes – 4 to 9% of the erythrocytes and – from 41 to 58% of the injected drug. Plasma protein binding is approximately 90%.
Metabolism: The biotransformation process produces up to 15 metabolites.Major metabolic pathways are mono- and dihydroxylation in different parts of the molecule. Active metabolites of either one does not exceed by more than 10% of the activity of “parent” substance.Excretion: The primo steroid elimination of the organism occurs mainly in the bile, only about 6% of the administered dose excreted in urine as metabolites, and approximately 0.1% – in the form of unchanged substance.Half-life values are significant fluctuations and make up about 6.3 hours in healthy volunteers, approximately 20.4 hours in patients with severe liver diseases and an average 11 hours (from 2 to 25 hours) in renal transplantation. The magnitude of clearance of cyclosporine in children is about 2 times higher than in adults. Capsules and solution for internal use bioequivalent.
Indications for use:
- Immune suppression and prevention of transplant rejection after kidney, liver, heart, combined heart-lung transplant, lung, or pancreas.
- Prevention of graft rejection after bone marrow transplantation.
- Prevention and treatment primo steroid of graft – versus – host.
- Endogenous uveitis (after exclusion of infectious etiology): active, sight-threatening uveitis middle or rear portion of the eye; Behçet uveitis with recurrent attacks of inflammation affecting the retina.
- Severe psoriasis is usually in cases of resistance to prior treatment.
- Nephrotic syndrome, dependent on corticosteroids and resistant to them (impaired renal function with a pronounced loss of protein) caused by disorders of the vascular glomerulus (diseases such as minimal change nephropathy, focal and segmental glomerulonephritis).
- Severe forms of rheumatoid primo steroid arthritis of the active current (in those cases where the classical slow-acting antirheumatic drugs are ineffective, or their application is impossible).
- Severe form of atopic dermatitis when systemic therapy is shown.