Comparative Pharmacology
Head-to-head clinical analysis: AZATHIOPRINE versus CELLCEPT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZATHIOPRINE versus CELLCEPT.
AZATHIOPRINE vs CELLCEPT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Azathioprine is a purine analog that inhibits purine nucleotide synthesis, thereby suppressing DNA replication and cell proliferation. It is converted to 6-mercaptopurine, which acts as a purine antagonist, inhibiting de novo purine synthesis and interfering with RNA and DNA synthesis, particularly in rapidly dividing cells such as T-lymphocytes.
Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), inhibiting de novo purine synthesis in T and B lymphocytes, thereby suppressing lymphocyte proliferation.
1.5 to 2.5 mg/kg orally once daily; typical adult dose 50-150 mg/day orally. Intravenous dose is 3-5 mg/kg/day as a slow infusion over 30-60 minutes.
Oral: 1-2 g daily in two divided doses. Intravenous: 1-2 g daily in two divided doses as a 2-hour infusion.
None Documented
None Documented
Clinical Note
moderateAzathioprine + Digoxin
"Azathioprine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateAzathioprine + Digitoxin
"Azathioprine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateAzathioprine + Deslanoside
"Azathioprine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateAzathioprine + Acetyldigitoxin
"Azathioprine may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life of azathioprine is approximately 2–5 hours; its active metabolite 6-mercaptopurine has a half-life of 1–2 hours, but 6-thioguanine nucleotides accumulate in red blood cells with a half-life of several days, correlating with myelosuppression.
Terminal elimination half-life of MPA is approximately 17.9 ± 6.5 hours in renal transplant patients. Clinical significance: dosing interval of 12 hours maintains therapeutic levels.
Renal (approximately 2% as unchanged drug, 30% as 6-thiouric acid and other metabolites); biliary/fecal (minor, <10% as metabolites).
Mycophenolic acid (MPA) is primarily excreted in urine as mycophenolic acid glucuronide (MPAG) (87% of dose); <1% excreted as unchanged MPA. Fecal excretion accounts for approximately 6% of dose.
Category D/X
Category C
Immunosuppressant
Immunosuppressant