The oral LD₅₀s for single doses of AZASAN® (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. About 30% of AZASAN® (azathioprine) is bound to serum proteins, but approximately 45% is removed during an 8-hour hemodialysis.²⁴ A single case has been reported of a renal transplant patient who ingested a single dose of 7500 mg azathioprine. The immediate toxic reactions were nausea, vomiting, and diarrhea, followed by mild leukopenia and mild abnormalities in liver function. The white blood cell count, SGOT, and bilirubin returned to normal 6 days after the overdose.

AZASAN® (azathioprine) should not be given to patients who have shown hypersensitivity to the drug.

AZASAN® (azathioprine) should not be used for treating rheumatoid arthritis in pregnant women.

Patients with rheumatoid arthritis previously treated with alkylating agents (cyclophosphamide, chlorambucil, melphalan, or others) may have a prohibitive risk of neoplasia if treated with AZASAN® (azathioprine) .

REFERENCES

24. Schusziarra V, Ziekursch V, Schlamp R, et al. Pharmacokinetics of azathioprine under haemodialysis. Int J Clin Pharmacol Biopharm. 1976; 14:298-302.

Last reviewed on RxList: 9/14/2009
This monograph has been modified to include the generic and brand name in many instances.