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