Carbadox
Carbadox - General Information
Carbadox is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease. It is sold under the name "Colazal" in the US and "Colazide" in the UK.
The chemical name is (E)-5-[[-4-(2-carboxyethyl) aminocarbonyl] phenyl]azo] -2-hydroxybenzoic acid. It is usually administered as the disodium salt.
Carbadox releases mesalazine, also known as 5-aminosalicylic acid, or 5-ASA, in the large intestine. Its advantage over that drug in the treatment of Ulcerative colitis is believed to be the delivery of the active agent past the small intestine to the large intestine, the active site of ulcerative colitis.
Pharmacology of Carbadox
Carbadox 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. Carbadox 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.
Carbadox for patients
Carbadox Interactions
No drug interaction studies have been conducted for COLAZAL, however the use of orally administered antibiotics could, theoretically, interfere with the release of mesalamine in the colon.
Carbadox Contraindications
COLAZAL is contraindicated in patients with hypersensitivity to salicylates or to any of the components of COLAZAL capsules or balsalazide metabolites.
Additional information about Carbadox
Carbadox Indication: For the treatment of mildly to moderately active ulcerative colitis.
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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Balsalazide
Synonyms: Balsalazido [Spanish]; Balsalazida [Spanish]; Balsalazide disodium; Balsalazidum [Latin]
Drug Category: Anti-Ulcer Agents; Gastrointestinal Agents; Anti-Inflammatory Agents, Non-Steroidal
Drug Type: Small Molecule; Approved
Other Brand Names containing Balsalazide: Carbadox; Colazal;
Absorption: Low and variable, intact balsalazide is poorly absorbed systemically.
Toxicity (Overdose): 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.
Protein Binding: ≥99%
Biotransformation: Cleaved in the colon via bacterial azoreduction to 5–aminosalicylic acid (5–ASA) and 4–aminobenzoyl-beta-alanine, the inactive carrier moiety.
Half Life: Half-life could not be determined.
Dosage Forms of Carbadox: Capsule Oral
Chemical IUPAC Name: (3Z)-3-[[4-(2-carboxyethylcarbamoyl)phenyl]hydrazinylidene]-6-oxocyclohexa-1,4-diene-1-carboxylic acid
Chemical Formula: C17H15N3O6
Balsalazide on Wikipedia: https://en.wikipedia.org/wiki/Balsalazide
Organisms Affected: Humans and other mammals