Cyclosporine lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader.Cyclosporine is used to prevent organ rejection after a kidney, heart, or liver transplant. Cyclosporine is also used to treat severe psoriasis or severe rheumatoid arthritis. Pharmacology:Pharmacodynamic Properties Of Cyclosporine
Used in immunosuppression for prophylactic treatment of organ transplants, cyclosporine exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited. The T1-helper cell is the main target, although the T1-suppressor cell may also be suppressed. Sandimmune (cyclosporine) also inhibits lymphokine production and release including interleukin-2. Pharmacokinetic Properties Of Cyclosporine
Pregnancy & Lactation Pregnancy
The absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. The extent of absorption is dependent on the individual patient, the patient population, and the formulation.
- Protein Binding:
In the plasma, approximately 90% is bound to proteins, primarily lipoproteins. In blood, the distribution is concentration dependent. Approximately 33% to 47% is in plasma, 4% to 9% in lymphocytes, 5% to 12% in granulocytes, and 41% to 58% in erythrocytes.
Hepatic, extensively metabolized by the cytochrome P450 3A enzyme system in the liver. It is also metabolized in the gastrointestinal tract and kidney to a lesser degree. The metabolites are significantly less potent than the parent compound. The major metabolites (M1, M9, and M4N) result from oxidation at the 1-beta, 9-gamma, and 4-N-demethylated positions, respectively.
- Route Of Elimination:
Elimination is primarily biliary with only 6% of the dose (parent drug and metabolites) excreted in the urine. Only 0.1% of the dose is excreted in the urine as unchanged drug.
Pregnant women receiving immunosuppressive therapies after transplantation, including cyclosporin and cyclosporin-containing regimens, are at risk of premature delivery.Breast-Feeding
Cyclosporin passes into breast milk. The ethanol content of the Neoral formulations should also be taken into account in women who are breast-feedingContraindications
Hypersensitivity to the active substance or to any of the excipients.Side Effects
Very rare but the common side effects are:
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