testosterone cypionate

Cyclosporine is a cyclic polypeptide consisting of 11 amino acids. Testosterone cypionateis a selective immunosuppressant that inhibits lymphocyte activation kaltsiynevrina in  phase of the cell cycle. This prevents activation of T lymphocytes and, at a cellular level, the antigen-dependent release of lymphokines, including interleukin . Tacrolimus acts on lymphocytes specifically and reversibly. Unlike cytotoxic drugs, it does not suppress hematopoiesis and does not affect the function of phagocytes.

Increases the lifetime of allogeneic transplants of skin, heart, kidney, pancreas, bone marrow, small intestine, lung. Cyclosporine also inhibits development of cellular responses against an allograft, cutaneous delayed-type hypersensitivity, experimental allergic encephalomyelitis, arthritis caused by  adjuvant, disease “graft versus host” () and dependent on antibody formation. Sandimmun efficacy of bone marrow transplantation has been shown and solid organs in humans for the prevention and treatment of rejection , and in the treatment of various conditions which are inherently autoimmune or may be treated as such.

Pharmacokinetics of
Is distributed largely outside the blood stream. At 33-47% blood plasma are cyclosporine, 9.4% – in the lymphocytes, 5-12% – in granulocytes and 41-58% – in erythrocytes. Plasma protein binding (mostly lipoproteins) is approximately 90%.

Largely biotransformation in the liver by hydroxylation to form approximately 15 metabolites. There is no single major metabolic pathway. The drug is excreted mainly in the bile and only 6% of the administered oral dose is excreted in the urine (and less than 1% excreted unchanged).

The values testosterone cypionate of terminal half-life of cyclosporine is very variable, depending on the method used and the local population of patients. The final half-life of unchanged when the liver is about 6.3 hours; in patients with severe liver disease – about 20.4 hours.

Indications

 

  • prevention of transplant rejection after bone marrow transplantation;
  • prevention of allograft rejection of solid organs: kidney, liver, heart, combined heart-lung transplant, lung or pancreas (when receiving the drug inside is impossible, or absorption of the drug when administered disrupted by diseases of the gastrointestinal ;
  • prevention and treatment of graft vs. host disease (in cases where the ingestion of the drug is not possible, or absorption of the drug when administered disrupted due gastrointestinal diseases).

 

Contraindications
Hypersensitivity to cyclosporin or any other component of the preparation, including polyoxyethylated castor oil.

With care use during pregnancy and breastfeeding In experimental studies have shown toxic effects of the drug on reproductive function.

Experience with Sandimmun in pregnant women is limited.

Pregnant women who have undergone organ transplantation and receiving immunosuppressive treatment with cyclosporine or combination therapy including cyclosporine, there is a risk of preterm delivery (occurring during pregnancy up to 37 weeks). A limited number of observations of the children (up until the age of 7 years), exposed to cyclosporine in utero. Renal function and blood pressure in these children were normal.

However, adequate and well-controlled studies in pregnant women have not been conducted, therefore, Sandimmun should not be used during pregnancy unless the expected benefit to the mother justifies the potential risk to the fetus.

Cyclosporin passes into breast milk. Mothers receiving Sandimmun should not breast-feed.

Dosing and Administration
The drug is administered intravenously testosterone cypionate drip.

The mode set individually. Selection of the initial dose and dosage regimen in the treatment of correction performed based on clinical and laboratory parameters as well as values of the concentration of cyclosporine in the blood plasma determined daily.

Adults with a bone marrow transplant in the day before the transplant, Sandimmun is introduced into / in the drip in the dose of 3-5 mg / kg / day. The introduction of this dose continued during the immediate post-transplant period, for up to 2 weeks; then move on to maintenance therapy with oral forms of ciclosporin. In cases where the impaired absorption of the drug may be necessary to continue the on / in. In solid organ transplant, for 4-12 hours prior to surgery, a single dose administered 5.3 mg / kg body weight. Within 1-2 weeks after the operation the preparation is prescribed daily at the same dose, after which the dose was gradually reduced under the control of the concentration of cyclosporine in the blood.

In the appointment of Sandimmun in combination with corticosteroids or other immunosuppressants can be used smaller doses of Sandimmun.

The use in children
in the pediatric dose Sandimmun applied 3.5 mg / kg / day; dosing regimen the same as that of adults.

Use in elderly patients
Experience with Sandimmun in the elderly is limited.

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