How does azathioprine contribute to immunosuppression following liver transplantation?

Updated: Dec 31, 2017
  • Author: Lemi Luu, MD, RDMS, FACEP, FAAEM; Chief Editor: Barry E Brenner, MD, PhD, FACEP  more...
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Azathioprine is an imidazolyl derivative of 6-mercaptopurine. The drug inhibits nucleic acid synthesis, suppressing cell-mediated hypersensitivity and altering antibody production. This results in inhibition of T-cell activation, reduction of antibody production, and a decrease in the number of circulating monocytes and granulocytes. It is effective in preventing rejection but does not have a large effect on an immune response already activated.

Azathioprine is metabolized in the liver and erythrocytes. Renal function has minor effects on levels. The drug causes a dose-dependent decrease in leukocyte and platelet counts via bone marrow suppression. It is typically dosed according to white blood cell (WBC) and platelet counts, with an initial dosage of 3-5 mg/kg/day. The maintenance dosage usually is lower, at 1-3 mg/kg/day.

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