What is the role of cyclosporine in immunosuppression after solid organ transplantation?

Updated: Jan 04, 2016
  • Author: Bethany Pellegrino, MD; Chief Editor: Mary C Mancini, MD, PhD, MMM  more...
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Answer

Answer

Calcineurin inhibitors

Cyclosporine

Cyclosporine has been a keystone of immunosuppression in transplantation for 4 decades. This agent is used for induction and maintenance immunosuppression. It is a polypeptide of 11 amino acids of fungal origin and a prodrug that binds to cyclophilin; complex inhibits calcineurin phosphatase and T-cell activation by dephosphorylation of inactive nuclear factor of activated T cells (NF-AT). Therefore, it prevents the production of IL-2 via calcineurin inhibition.

Cyclosporin trough level or checking levels 2 hours after administration is required. Multiple drug interactions are possible, primarily with agents affecting the cytochrome P-450 system.

Adverse effects of cyclosporin include nephrotoxicity (immediate, secondary to renal ischemia; 2-3 weeks after transplantation, secondary to renal vasoconstriction; and chronic, secondary to interstitial nephritis). Other adverse effects include hyperkalemia, hypomagnesemia, nausea, vomiting, diarrhea, hypertrichosis, hirsutism, gingival hyperplasia, skin changes, hyperlipidemia, glucose intolerance, infection, malignancy, hyperuricemia, and hemolytic uremic syndrome. Hypertrichosis and hirsutism can be alleviated by switching from cyclosporine to tacrolimus.

The adverse consequences (eg, hypertension, renal impairment) of long-term cyclosporine use for solid organ transplant rejection have prompted exploration of various treatment regimens.


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