Comparative Pharmacology
Head-to-head clinical analysis: CAPECITABINE versus TREXALL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CAPECITABINE versus TREXALL.
CAPECITABINE vs TREXALL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Capecitabine is a prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in the body, which inhibits thymidylate synthase and incorporates into RNA and DNA, leading to cytotoxic effects.
Methotrexate is a folate analog that inhibits dihydrofolate reductase, preventing the conversion of folic acid to tetrahydrofolate, thereby inhibiting DNA synthesis, repair, and cellular replication. It also has immunomodulatory and anti-inflammatory effects through inhibition of purine and pyrimidine synthesis and release of adenosine.
Oral, 1250 mg/m2 twice daily for 2 weeks followed by a 1-week rest period.
Oral: 7.5-15 mg once weekly; subcutaneous: 7.5-15 mg once weekly for rheumatoid arthritis; may be increased up to 25-30 mg weekly based on response and tolerability.
None Documented
None Documented
Clinical Note
moderateCapecitabine + Digoxin
"Capecitabine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateCapecitabine + Digitoxin
"Capecitabine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateCapecitabine + Deslanoside
"Capecitabine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateCapecitabine + Acetyldigitoxin
"Capecitabine may decrease the cardiotoxic activities of Acetyldigitoxin."
The terminal elimination half-life of capecitabine is approximately 0.75 hours. For its active metabolite 5-fluorouracil, the half-life is about 0.7 hours. Clinically, this short half-life necessitates twice-daily dosing to maintain therapeutic levels.
Terminal elimination half-life is 3-10 hours; for high-dose methotrexate, half-life is 8-15 hours. Clinically, monitoring at 24, 48, and 72 hours is standard to guide leucovorin rescue
Capecitabine is predominantly eliminated renally. Approximately 95.5% of the administered dose is recovered in urine, with 61% as unchanged capecitabine and its metabolites. Fecal excretion accounts for about 2.6%. Biliary elimination is minimal (<1%).
Renal excretion of unchanged drug accounts for 80-90% of elimination; biliary/fecal elimination is minor (<10%)
Category D/X
Category C
Antimetabolite
Antimetabolite