Comparative Pharmacology
Head-to-head clinical analysis: AZATHIOPRINE versus CEQUA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZATHIOPRINE versus CEQUA.
AZATHIOPRINE vs CEQUA
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.
Immunosuppressant; binds to cyclophilin D in mitochondria, inhibiting opening of mitochondrial permeability transition pore (mPTP), which reduces T-lymphocyte activation and cytokine release. Also forms complex with cyclophilin A to inhibit calcineurin, suppressing IL-2 production and T-cell 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.
Instill one drop of 0.09% ophthalmic solution in each eye twice daily, approximately 12 hours apart.
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 is approximately 8.4 hours (range 6-10 hours) in healthy adults; prolonged in hepatic impairment and pediatric patients.
Renal (approximately 2% as unchanged drug, 30% as 6-thiouric acid and other metabolites); biliary/fecal (minor, <10% as metabolites).
Primarily fecal (90%) with minor renal excretion (<1% unchanged drug). Biliary excretion is the major route for elimination of cyclosporine metabolites.
Category D/X
Category C
Immunosuppressant
Immunosuppressant