• Antimetabolites
• Antimetabolites, Antineoplastic
• Antirheumatic Agents
• Immunosuppressive Agents
• ATC:L04AX01

• ATP
• Azamun
• Azanin
• Azasan
• Azathioprin
• Azathioprine Sodium
• Azatioprin
• Azothioprine
• Ccucol
• Imuran
• Imurek
• Imurel
• Muran
• Rorasul

C₉H₇N₇O₂S

http://www.rxlist.com/cgi/generic/azathioprine.htm

No information avaliable

277.264 g/mol

243.5 ^oC

272 mg/L

Solid

1.001

Powder for solution and tablets for oral administration (25 mg, 75 mg and 100 mg)

For use as an adjunct in the prevention of rejection in renal homotransplantation. Also for the management of severe, active rheumatoid arthritis unresponsive to rest, aspirin or other nonsteroidal anti-inflammatory drugs, or to agents in the class of which gold is an example.

Azathioprine is a chemotherapy drug, now rarely used for chemotherapy but more for immunosuppression in organ transplantation and autoimmune disease such as rheumatoid arthritis or inflammatory bowel disease or Crohn's disease. It is a pro-drug, converted in the body to the active metabolite 6-mercaptopurine. Azathioprine acts to inhibit purine synthesis necessary for the proliferation of cells, especially leukocytes and lymphocytes. It is a safe and effective drug used alone in certain autoimmune diseases, or in combination with other immunosuppressants in organ transplantation. Its most severe side effect is bone marrow suppression, and it should not be given in conjunction with purine analogues such as allopurinol. The enzyme thiopurine S-methyltransferase (TPMT) deactivates 6-mercaptopurine. Genetic polymorphisms of TPMT can lead to excessive drug toxicity, thus assay of serum TPMT may be useful to prevent this complication.

Well absorbed following oral administration.

The oral LD₅₀ for single doses of azathioprine in mice and rats are 2500 mg/kg and 400 mg/kg, respectively. Very large doses of this antimetabolite may lead to marrow hypoplasia, bleeding, infection, and death.

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Humans and other mammals