Comparative Pharmacology
Head-to-head clinical analysis: ABITREXATE versus MERCAPTOPURINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABITREXATE versus MERCAPTOPURINE.
ABITREXATE vs MERCAPTOPURINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Methotrexate, the active ingredient, is a folate analog that inhibits dihydrofolate reductase (DHFR), thereby blocking the conversion of dihydrofolate to tetrahydrofolate, inhibiting DNA synthesis, repair, and cellular replication. It also has immunosuppressive and anti-inflammatory effects via modulation of adenosine and cytokine pathways.
Mercaptopurine is a prodrug that is converted to 6-thioguanine nucleotides, which inhibit de novo purine synthesis and DNA replication by incorporating into DNA and RNA. It also inhibits purine nucleotide interconversions via feedback inhibition of amidophosphoribosyltransferase.
7.5 mg orally once weekly; alternatively, 7.5 mg subcutaneously once weekly. Dose may be increased by 2.5 mg every 1-2 weeks up to 20 mg once weekly based on response and tolerability.
1.5 to 2.5 mg/kg orally once daily; maintenance 1.5 to 2.5 mg/kg orally once daily.
None Documented
None Documented
Clinical Note
moderateMercaptopurine + Digoxin
"Mercaptopurine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateMercaptopurine + Digitoxin
"Mercaptopurine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateMercaptopurine + Deslanoside
"Mercaptopurine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateMercaptopurine + Acetyldigitoxin
"Mercaptopurine may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life is 6-12 hours (mean 7.5 hours) in patients with normal renal function; prolonged in renal impairment.
Terminal elimination half-life: 1.5-3 hours (variable); for active metabolites (e.g., 6-thioguanine nucleotides) half-life is 5-7 days, which correlates with myelosuppression.
Primarily renal (80-90% as unchanged drug) via glomerular filtration and active tubular secretion; biliary/fecal excretion accounts for <10%.
Renal: 20-30% as unchanged drug; biliary/fecal: minor; extensive hepatic metabolism to active and inactive metabolites.
Category C
Category D/X
Antimetabolite
Antimetabolite