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Cyclosporine

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Information about Cyclosporine

Cyclosporine is a calcineurin inhibitor and potent immunosuppressive agent used largely as a means of prophylaxis against cellular rejection after solid organ transplantation.

Liver safety of Cyclosporine

Cyclosporine therapy can be associated with mild elevations in serum bilirubin and transient serum enzyme elevations, and to rare instances of clinically apparent cholestatic liver injury.

Mechanism of action of Cyclosporine

Cyclosporine (sye" kloe spor' in), also called cyclosporin A, is a cyclic polypeptide of 11 amino acids produced by a fungal species (Beaveria nivea) which has profound immunosuppressive properties, particularly affecting T cells and the cellular immune response. Cyclosporine acts as a inhibitor of calcineurin which is responsible for activating an important signal transduction pathway of T cell activation. The result of the inhibition is a decrease in maturation of T lymphocytes and reduction in lymphokine production, including IL-2.

FDA approval information for Cyclosporine

Cyclosporine was introduced into use in the United States in the early 1980s and rapidly became part of the primary regimen of immunosuppression after allogenic, solid organ transplantation. Current indications are for prevention of organ rejection after transplantation and for therapy of active and recalcitrant rheumatoid arthritis and psoriasis.

Dosage and administration for Cyclosporine

Cyclosporine is available as capsules of 25 and 100 mg in generic forms and under the brand name of Sandimmune, and as a more reliably absorbed microemulsion formulation of 25 and 100 mg in generic forms and under the brand name of Neoral (2003). Cyclosporine is also available in solution for oral and for intravenous use. Because of variable absorption, the usual maintenance dose of cyclosporine varies greatly and proper dosing requires monitoring for drug levels, which is also important because of its many dose dependent side effects and drug-drug interactions.

Side effects of Cyclosporine

Common side effects of cyclosporine include headache, dizziness, paresthesias, neuropathy, tremor, hypertension, hyperlipidemia, nephropathy, acne, hirsutism and gum hyperplasia.

The following drugs used to prevent transplant rejection.

Immunosuppressants

Monoclonal Antibodies

Antithymocyte Globulin

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