Dipentum
Dipentum - General Information
Dipentum is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Dipentum is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Mesalamine works as an anti-inflammatory agent in treating inflammatory diseases of the intestines.
Pharmacology of Dipentum
Dipentum is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Dipentum reduces the bowel inflammation, diarrhea (stool frequency), rectal bleeding, and abdominal pain. Like Balsalazide, Dipentum is believed to deliver Mesalazine, or 5-aminosalicylic acid (5-ASA), past the small intestine, directly to the large intestine, which is that active site of disease in ulcerative colitis.
Additional information about Dipentum
Dipentum Indication: For the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.
Mechanism Of Action: Orally administered olsalazine is converted to mesalamine which is thought to be the therapeutically active agent in the treatment of ulcerative colitis. The mechanism of action of mesalamine (and sulfasalazine) is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid (AA) metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes (LTs) and hydroxyelcosatetraenoic acids (HETEs) is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin (PG) production in the colon.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Olsalazine
Synonyms: Olsalazine sodium
Drug Category: Anti-Inflammatory Agents, Non-Steroidal; Gastrointestinal Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Olsalazine: Dipentum;
Absorption: After oral administration, olsalazine, has limited systemic bioavailability. 98-99% of the dose is converted to mesalamine (5-ASA) in the colon, which is absorbed slowly resulting in very high local concentrations in the colon.
Toxicity (Overdose): Maximum single oral doses of 5g/kg in mice and rats and 2 g/kg in dogs were not lethal.
Protein Binding: Olsalazine and olsalazine-S are more than 99% bound to plasma proteins. Mesalamine (5-ASA) is 74% bound to plasma proteins.
Biotransformation: Most (98 to 99%) of an oral dose is rapidly converted into two molecules of 5-aminosalicylic acid (5-ASA) by colonic bacteria and the low prevailing redox potential found in this environment. The conversion of olsalazine to mesalamine in the colon is similar to that of sulfasalazine, which is converted into sulfapyridine and mesalamine. Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S)
Half Life: Olsalazine has an elimination half-life of 0.9 hours, however, olsalazine-S has a half-life of 7 days.
Dosage Forms of Dipentum: Capsule Oral
Chemical IUPAC Name: 5-[(2Z)-2-(3-carboxy-4-oxo-1-cyclohexa-2,5-dienylidene)hydrazinyl]-2-hydroxybenzoic acid
Chemical Formula: C14H10N2O6
Olsalazine on Wikipedia: https://en.wikipedia.org/wiki/Olsalazine
Organisms Affected: Humans and other mammals
