Active ingredient: Balsalazide - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anti-ulcer Agents

Dosage Forms

• Capsule (750 mg)

Brands / Synonyms

Balsalazida [Spanish]; Balsalazide disodium; Balsalazido [Spanish]; Balsalazidum [Latin]; Carbadox; Colazal; Colazal

Indications

For the treatment of mildly to moderately active ulcerative colitis.

Pharmacology

Balsalazide is a prodrug that is enzymatically cleaved in the colon to produce mesalamine (5-aminosalicylic acid), an anti inflammatory drug indicated for the treatment of mildly to moderately active ulcerative colitis. Balsalazide disodium is delivered intact to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalamine, which is the therapeutically active portion of the molecule, and 4-aminobenzoyl-(beta)-alanine.

Mechanism of Action

The mechanism of action of 5-aminosalicylic acid is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that 5-aminosalicylic acid diminishes inflammation by blocking production of arachidonic acid metabolites in the colon.

Absorption

Low and variable, intact balsalazide is poorly absorbed systemically.

Toxicity

A single oral dose of balsalazide disodium at 5 grams/kg or 4-aminobenzoyl-(beta)-alanine, a metabolite of balsalazide disodium, at 1 gram/kg was non-lethal in mice and rats. No symptoms of acute toxicity were seen at these doses.

Biotrnasformation / Drug Metabolism

Cleaved in the colon via bacterial azoreduction to 5–aminosalicylic acid (5–ASA) and 4–aminobenzoyl-beta-alanine, the inactive carrier moiety.

Contraindications

COLAZAL ô is contraindicated in patients with hypersensitivity to salicylates or to any of the components of COLAZAL ô capsules or balsalazide metabolites.

Drug Interactions

No drug interaction studies have been conducted for COLAZAL ô, however the use of orally administered antibiotics could, theoretically, interfere with the release of mesalamine in the colon.