Comparative Pharmacology
Head-to-head clinical analysis: ASACOL HD versus DELZICOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASACOL HD versus DELZICOL.
ASACOL HD 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) derivative that acts locally in the colon to reduce inflammation by inhibiting prostaglandin production and leukotriene synthesis, likely through scavenging free radicals and blocking cytokine release.
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.
2 tablets (1600 mg) once daily with or without food.
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 is 5-10 hours for 5-ASA and 5-10 hours for acetyl-5-ASA; clinically, it supports 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.
Primarily renal excretion of acetyl-5-ASA (about 80% of absorbed dose) and unchanged 5-ASA; minor fecal elimination (<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