Comparative Pharmacology
Head-to-head clinical analysis: APRISO versus ASACOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APRISO versus ASACOL.
APRISO vs ASACOL
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).
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.
1.5 g (3 capsules) orally once daily in the morning. Each capsule contains 0.5 g mesalamine.
800 mg orally three times daily or 1600 mg three times daily for 6 weeks; maintenance: 1.6 g daily in divided doses.
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.
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.
Renal (primarily as acetylated metabolite, ~80%) and fecal (~20%).
Renal (80% as 5-ASA and N-acetyl-5-ASA), fecal (20%)
Category C
Category C
Aminosalicylate
Aminosalicylate