Comparative Pharmacology
Head-to-head clinical analysis: ASACOL versus DELZICOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASACOL versus DELZICOL.
ASACOL vs DELZICOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Asacol (mesalamine) is an aminosalicylate that exerts anti-inflammatory effects in the colon via inhibition of prostaglandin and leukotriene synthesis, particularly by blocking cyclooxygenase and lipoxygenase pathways, and by scavenging reactive oxygen species. It also inhibits cytokine production and reduces mucosal inflammation.
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.
800 mg orally three times daily or 1600 mg three times daily for 6 weeks; maintenance: 1.6 g daily in divided doses.
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 half-life: 0.6-1.4 hours for 5-ASA; 6-12 hours for N-acetyl-5-ASA. Clinical context: short t1/2 necessitates multiple daily dosing for sustained colonic exposure.
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 (80% as 5-ASA and N-acetyl-5-ASA), 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