Olsalazine

Olsalazine Uses, Dosage, Side Effects, Food Interaction and all others data.

Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Olsalazine 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.

Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Olsalazine reduces the bowel inflammation, diarrhea (stool frequency), rectal bleeding, and abdominal pain. Olsalazine is thought to work like balsalazide, delivering mesalazine or 5-aminosalicylic acid past the small intestine to the large intestine to act on the site of disease.

Trade Name Olsalazine
Availability Prescription only
Generic Olsalazine
Olsalazine Other Names Olsalazine
Related Drugs Entyvio, Humira, Zeposia, Colazal, prednisone, dexamethasone, methylprednisolone, hydrocortisone, hydrocortisone topical, budesonide
Weight 250mg
Type Oral capsule
Formula C14H10N2O6
Weight Average: 302.239
Monoisotopic: 302.053886062
Protein binding

Olsalazine and olsalazine-S are more than 99% bound to plasma proteins. Mesalamine (5-ASA) is 74% bound to plasma proteins.

Groups Approved
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Olsalazine
Olsalazine

Uses

Olsalazine is an anti-inflammatory agent used in the treatment of inflammatory bowel disease and ulcerative colitis.

For the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.

Olsalazine is also used to associated treatment for these conditions: Ulcerative Colitis

How Olsalazine works

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.

Toxicity

Maximum single oral doses of 5g/kg in mice and rats and 2 g/kg in dogs were not lethal.

Food Interaction

  • Take with food.

Olsalazine Disease Interaction

Moderate: renal dysfunction

Elimination Route

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.

Half Life

Olsalazine has an elimination half-life of 0.9 hours, however, olsalazine-S has a half-life of 7 days.

Elimination Route

Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S).The remaining 5-ASA is partially acetylated and is excreted in the feces.

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