BRAND NAMES
 MECHANISM OF ACTION
Cyclosporine binds an intracellular receptor, cyclophiline. This complex inhibits calcineurin, an intracellular phosphatase, which involves activation of the promoter region for the gene-encoding cytokine, such as interleukin-2. This results in inhibiting T-cell activation in the early stage of immune response to a foreign antigen such as a graft.
Kidney, Liver, and Heart Transplantation
Cyclosporine is indicated for the prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants. Cyclosporine has been used in combination with azathioprine and corticosteroids.
Cyclosporine is indicated for the treatment of patients with severe active, rheumatoid arthritis where the disease has not adequately responded to methotrexate. Cyclosporine can be used in combination with methotrexate in rheumatoid arthritis patients who do not respond adequately to methotrexate alone.
Cyclosporine is indicated for the treatment of adult, nonimmunocompromised patients with severe (i.e., extensive and/or disabling), recalcitrant, plaque psoriasis who have failed to respond to at least one systemic therapy (e.g., PUVA, retinoids, or methotrexate) or in patients for whom other systemic therapies are contraindicated, or cannot be tolerated. While rebound rarely occurs, most patients will experience relapse with Cyclosporine as with other therapies upon cessation of treatment.
Cyclosporine pharmacokinetics is unpredictable, and many factors such as age, time after transplant , different oral formulation (Neoral® or Sandimmune®), or drugs affect it . Oral bioavailability is about 30%. Neoral and Sandimmune are not bioequivalent and cannot be used interchangeably without physician supervision.
Generally, 8mg/kg/day of oral cyclosporine as two divided doses is used in solid organ transplantat ion and adjusted according to the blood levels. Serum creatinine should be monitored with the blood levels of cyclosporine. The blood levels are useful in the clinical monitoring ( Dose adjustments should be made in transplant patients to minimize possible organ rejection due to low concentrations)
- Hypersensitivity to cyclosporine.
- Rheumatoid arthritis patients with abnormal renal function, uncontrolled hypertension, or malignancies should not receive Cyclosporine.
- Psoriasis patients who are treated with Cyclosporine should not receive concomitant PUVA or UVB therapy, methotrexate or other immunosuppressive agents, coal tar or radiation therapy. Psoriasis patients with abnormal renal function, uncontrolled hypertension, or malignancies should not receive Cyclosporine.
Cyclosporine may increase the susceptibility to infection and the development of neoplasia.
 PREGNANCY AND LACTATION
 SIDE EFFECTS
- Nephrotoxicity is the major side effect.
- Neurotoxicity and hepatotoxicity are also common.
- Facial hair growth (hirsutism) is one of the cumbersome side effects of cyclosporine, which may discourage the patient's compliance.
- Gingival hyperplasia is also cumbersome side effect.
- Hypertension is a common side effect of cyclosporine therapy which may persist. Mild or moderate hypertension is encountered more frequently than severe hypertension and the incidence decreases over time.