Azatioprin
Brand names,
Azatioprin
Analogs
Azatioprin
Brand Names Mixture
Azatioprin
Chemical_Formula
C9H7N7O2S
Azatioprin
RX_link
http://www.rxlist.com/cgi/generic/azathioprine.htm
Azatioprin
fda sheet
Azatioprin
msds (material safety sheet)
Azatioprin
Synthesis Reference
No information avaliable
Azatioprin
Molecular Weight
277.264 g/mol
Azatioprin
Melting Point
243.5 oC
Azatioprin
H2O Solubility
272 mg/L
Azatioprin
State
Solid
Azatioprin
LogP
1.001
Azatioprin
Dosage Forms
Powder for solution and tablets for oral administration (25 mg, 75 mg and 100 mg)
Azatioprin
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.
Azatioprin
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.
Azatioprin
Absorption
Well absorbed following oral administration.
Azatioprin
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.
Azatioprin
Patient Information
Azatioprin
Organisms Affected
Humans and other mammals