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Azathioprine Brand names, Azathioprine Analogs

Azathioprine Brand Names Mixture

  • No information avaliable

Azathioprine Chemical_Formula

C9H7N7O2S

Azathioprine RX_link

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

Azathioprine fda sheet

Azathioprine msds (material safety sheet)

Azathioprine MSDS

Azathioprine Synthesis Reference

No information avaliable

Azathioprine Molecular Weight

277.264 g/mol

Azathioprine Melting Point

243.5 oC

Azathioprine H2O Solubility

272 mg/L

Azathioprine State

Solid

Azathioprine LogP

1.001

Azathioprine Dosage Forms

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

Azathioprine Indication

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 Pharmacology

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.

Azathioprine Absorption

Well absorbed following oral administration.

Azathioprine side effects and Toxicity

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.

Azathioprine Patient Information

Azathioprine Organisms Affected

Humans and other mammals