Cyclosporine Soft Gel Capsules

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.

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

ABSORPTION:
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.
METABOLISM:
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.
Pregnancy 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-feeding
Hypersensitivity to the active substance or to any of the excipients.
Very rare but the common side effects are:
  • Shaking
  • Headache
  • Dizziness
  • Unusual growth of body hair,
  • Nausea/vomiting
  • Diarrhea
  • Stomach upset