Absorption Metabolism and Excretion

After oral administration, cyclosporine is absorbed slowly and incompletely, with great variation among in dividuals. Peak plasma concentrations are reached in 3 to 4 hours, and the plasma half-life is 10 to 27 hours. The drug is extensively metabolized by hepatic mixed-function oxidase enzymes and is excreted principally via the bile into the feces. Metabolism results in inactiva-tion of the immunosuppressive activity. Agents that enhance or inhibit the mixed-function oxidase enzymes will alter the therapeutic response to cyclosporine.

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