- Discovered in soil fungus in 1970, it has tremendously improved graft survival in all areas of transplantation.
The cyclosporine compound is soluble only in organic solvents or lipids, it is insoluble in water. It enters the cell passively and binds to cyclophilin causing inactivation of calcium dependent activation of the cell.
Blocks the signal to lymphocytes to produce IL-1, IL-2, IL-3, IL-4, and interferon gamma.
Dosage given based on trough (lowest) blood levels. Target trough level depends on the organ transplanted and the time since transplant. Multiple different assays are available for cyclosporine trough levels, actual values will vary depending on the assay used.
Cyclosporine metabolism is in the liver by the cytochrome p-450 system. Drugs that induce this system will decrease the level of cyclosporine, drugs that block this system will increase cyclosporine blood levels
Side effects include high blood pressure, kidney damage, tremors, headaches, seizures, excessive hair growth, excessive gum growth, confusion, coma, and gout.