Capsule Presentation

Each Soft gelatin Capsule Contains:
Cyclosporine IP 25/50/100 mg


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.

Indications

• Prevention of graft rejection following solid organ transplantation
• Treatment of transplant cellular rejection in patients previously receiving other immunosuppressive agents
• Prevention of graft rejection following allogeneic bone marrow and stem cell transplantation
• Prevention or treatment of graft-versus-host disease

Pharmacology

Pharmacodynamic Properties:

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:

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.

Contraindications

Hypersensitivity to the active substance or to any of the excipients.

Side Effects

• Shaking
• Headache
• Dizziness
• Unusual growth of body hair,
• Nausea/vomiting
• Diarrhea
• Stomach upset