Comparative Pharmacology
Head-to-head clinical analysis: DELZICOL versus LIALDA.
Head-to-head clinical analysis: DELZICOL versus LIALDA.
DELZICOL vs LIALDA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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, the active ingredient in Lialda, is an anti-inflammatory agent that inhibits prostaglandin production and leukotriene synthesis, and reduces cytokine production in the colonic mucosa.
800 mg orally 3 times daily for ulcerative colitis; mesalamine 4 g retention enema once daily or 4 g foam once daily for proctosigmoiditis.
2-4 tablets (2.4-4.8 g) orally once daily. Each tablet contains 1.2 g mesalamine.
None Documented
None Documented
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.
Terminal elimination half-life of mesalamine is approximately 12 hours (range 8-15 hours) for the sustained-release formulation; clinical steady-state is reached within 3-5 days.
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.
Renal (primarily, as N-acetyl-5-aminosalicylic acid, about 80%) and fecal (as unchanged mesalamine, about 20%).
Category C
Category C
Aminosalicylate
Aminosalicylate