Azathioprine is a prodrug of 6-mercaptopurine, first synthesized in 1956 by Gertrude Elion, William Lange, and George Hitchings in an attempt to produce a derivative of 6-mercaptopurine with a better therapeutic index. Azathioprine is used to treat inflammatory conditions like rheumatoid arthritis and as an immunosuppressant in the prevention of renal transplant rejection
MODE OF ACTION:
Azathioprine is a purine analogue that converts to its active metabolites, mercaptopurine (6-MP) and thioguanine (6-TGN), by the action of hypoxanthine-guanine phosphoribosyltransferase (HPRT) and thiopurine methyltransferase (TPMT) enzymes. It then inhibits purine synthesis. Its metabolites are incorporated into the replicating DNA and halt division. AZA metabolites may also mediate most of its immunosuppressive and toxic effects.
- Renal Transplant Rejection
Initial dose: 3 to 5 mg/kg orally once a day
Maintenance dose: 1 to 3 mg/kg orally once a day
This information is for registered medical practitioner only. Anyone other than medical practitioner should consult medical practitioner before using this product.