Azathioprine
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 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
