Comparative Pharmacology
Head-to-head clinical analysis: ASTAGRAF XL versus AZATHIOPRINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASTAGRAF XL versus AZATHIOPRINE.
ASTAGRAF XL vs AZATHIOPRINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).
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.
Initial oral dose of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/day.
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.
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 is approximately 43 hours (range 15.8–68.6 hours) in adult kidney transplant recipients. This long half-life supports once-daily dosing. In liver transplant patients, half-life ranges from 12 to 42 hours.
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.
Primarily fecal (94.6%) via biliary elimination. Renal excretion accounts for approximately 2.4% of the dose, mainly as metabolites. Less than 1% is excreted unchanged in urine.
Renal (approximately 2% as unchanged drug, 30% as 6-thiouric acid and other metabolites); biliary/fecal (minor, <10% as metabolites).
Category C
Category D/X
Immunosuppressant, Calcineurin Inhibitor
Immunosuppressant