Comparative Pharmacology
Head-to-head clinical analysis: CANASA versus DELZICOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CANASA versus DELZICOL.
CANASA vs DELZICOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Mesalamine (5-aminosalicylic acid) is an anti-inflammatory agent that inhibits prostaglandin and leukotriene synthesis, scavenges reactive oxygen species, and inhibits cytokine production and nuclear factor-kappa B (NF-κB) activation in colonic mucosa.
Delzicol is a prodrug of mesalamine (5-aminosalicylic acid). It is converted to mesalamine in the colon by bacterial azoreduction. Mesalamine reduces inflammation in the colon by inhibiting prostaglandin production via cyclooxygenase inhibition and decreasing leukotriene synthesis via lipoxygenase pathway. It also scavenges reactive oxygen species and inhibits cytokine production.
Mesalamine 1000 mg rectally once daily at bedtime, or 500 mg rectally twice daily (morning and evening). Administered as suppository for ulcerative colitis.
800 mg orally 3 times daily for ulcerative colitis; mesalamine 4 g retention enema once daily or 4 g foam once daily for proctosigmoiditis.
None Documented
None Documented
Terminal elimination half-life of mesalamine is approximately 0.5-2 hours; however, the N-acetyl metabolite has a half-life of 5-10 hours. Due to the sustained-release formulation, clinical effects persist beyond the plasma half-life.
The terminal elimination half-life of mesalamine is approximately 0.5-1.5 hours after oral administration. For the acetylated metabolite, it is 5-10 hours. The short half-life necessitates multiple daily dosing for sustained colonic anti-inflammatory effect.
Renal (approximately 20-30% as unchanged drug and metabolites, primarily N-acetyl-5-aminosalicylic acid); biliary/fecal (the remainder, with extensive enterohepatic circulation).
Approximately 40-50% of the absorbed dose is excreted renally as mesalamine (5-ASA) and its acetylated metabolite (N-Ac-5-ASA). Fecal excretion accounts for the remainder, including unabsorbed drug and biliary elimination.
Category C
Category C
Aminosalicylate
Aminosalicylate