Comparative Pharmacology
Head-to-head clinical analysis: AZATHIOPRINE SODIUM versus MYFORTIC.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZATHIOPRINE SODIUM versus MYFORTIC.
AZATHIOPRINE SODIUM vs MYFORTIC
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Azathioprine is a prodrug of 6-mercaptopurine. It inhibits purine synthesis by interfering with the synthesis of DNA, RNA, and cellular proteins, thereby suppressing immune responses.
Mycophenolic acid inhibits inosine monophosphate dehydrogenase (IMPDH), thereby depleting guanosine nucleotides in T and B lymphocytes, suppressing their proliferation and antibody production.
1-2 mg/kg/day IV or oral, initially; maintenance 0.5-1 mg/kg/day IV or oral. For severe organ rejection: 3-5 mg/kg/day IV.
720 mg orally twice daily, on an empty stomach, 1 hour before or 2 hours after meals.
None Documented
None Documented
Terminal elimination half-life of azathioprine is approximately 3-5 hours; its active metabolite 6-mercaptopurine has a half-life of 0.5-1.5 hours. However, the pharmacodynamic effect (immunosuppression) persists longer due to intracellular accumulation of thioguanine nucleotides.
Terminal elimination half-life is approximately 12-18 hours (mean 17 hours) in healthy volunteers; longer in hepatic impairment (up to 40 hours).
Primarily renal: approximately 50% as unchanged drug and metabolites (6-mercaptopurine, thiouric acid) within 24 hours. Biliary/fecal excretion accounts for minor fraction (<5%).
Primarily renal (approximately 95% as metabolites, <3% as unchanged drug); biliary/fecal excretion accounts for <5%.
Category D/X
Category C
Immunosuppressant
Immunosuppressant