Comparative Pharmacology
Head-to-head clinical analysis: APRISO versus DELZICOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APRISO versus DELZICOL.
APRISO vs DELZICOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Mesalamine, the active ingredient, is a 5-aminosalicylic acid (5-ASA) that acts locally in the colon to reduce inflammation by inhibiting prostaglandin and leukotriene synthesis, scavenging free radicals, and activating peroxisome proliferator-activated receptor-gamma (PPAR-γ).
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.
1.5 g (3 capsules) orally once daily in the morning. Each capsule contains 0.5 g mesalamine.
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
8.6 ± 4.2 hours for mesalamine; after multiple dosing, effective half-life ~12 hours. Clinical context: allows twice-daily dosing.
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 (primarily as acetylated metabolite, ~80%) and fecal (~20%).
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