From the Guidelines
Mesalamine works by reducing inflammation in the intestines through its active ingredient, 5-aminosalicylic acid, which inhibits the production of inflammatory chemicals called prostaglandins and leukotrienes, as stated in the 2019 AGA clinical practice guidelines on the management of mild-to-moderate ulcerative colitis 1. The mechanism of action of mesalamine involves the delivery of its active compound to the inflamed areas of the intestinal lining, where it blocks the cyclooxygenase and lipoxygenase pathways involved in inflammation.
Key Points
- Mesalamine is an aminosalicylate anti-inflammatory drug that acts locally in the gut to reduce inflammation.
- It inhibits the production of prostaglandins and leukotrienes, which are inflammatory chemicals.
- The medication comes in various formulations, including oral tablets, capsules, and rectal suppositories or enemas.
- Typical oral doses range from 800 mg to 4.8 g daily, depending on the specific condition and severity, as seen in the guidelines 1.
- Mesalamine has a targeted action that minimizes systemic absorption, which helps reduce potential side effects compared to systemic anti-inflammatory medications.
Mechanism of Action
The active ingredient in mesalamine, 5-aminosalicylic acid, is believed to be the compound responsible for its therapeutic effects, as mentioned in the guidelines 1.
- It is converted to its active form by colonic bacteria.
- The exact mechanism of action is not fully understood, but it is thought to involve the inhibition of inflammatory chemicals and the modulation of the immune response.
Clinical Use
Mesalamine is commonly used to treat conditions like ulcerative colitis and Crohn's disease, as discussed in the 2019 guidelines 1.
- It is effective in reducing symptoms like diarrhea and abdominal pain, and in maintaining remission in inflammatory bowel diseases.
- The medication is generally well-tolerated, with minimal systemic side effects due to its targeted action.
From the FDA Drug Label
The mechanism of action of mesalamine is not fully understood, but it appears to have a topical anti-inflammatory effect on the colonic epithelial cells Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase and lipoxygenase pathways, is increased in patients with ulcerative colitis, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
The mechanism of action of mesalamine (5-aminosalicylic acid) is not fully understood. However, it is believed to have a topical anti-inflammatory effect on the colonic epithelial cells. It may work by:
- Blocking cyclooxygenase
- Inhibiting prostaglandin production in the colon This helps to reduce inflammation in patients with ulcerative colitis 2.
From the Research
Mechanism of Action of Mesalamine
The mechanism of action of mesalamine (5-aminosalicylic acid) is not explicitly described in the provided studies. However, its therapeutic effects and uses are well-documented.
Therapeutic Effects and Uses
- Mesalamine is used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease 3, 4, 5, 6, 7.
- It is effective in inducing and maintaining remission in patients with mild to moderately active ulcerative colitis 3, 4, 5, 7.
- Mesalamine is also effective in reducing disease activity and inducing remission in patients with Crohn's disease 3, 4, 6, 7.
- The drug is available in various formulations, including oral delayed-release and sustained-release formulations, topical formulations, and prodrugs 7.
Pharmacokinetics and Pharmacodynamics
- Mesalamine is released in the small and large intestine in a diffusion-dependent manner 3, 4.
- The drug is designed to release continuously throughout the small and large bowel, largely unaffected by intestinal pH 4.
- Mesalamine is the therapeutically active moiety of sulfasalazine, and its formulations are designed to avoid the need for the carrier, sulphapyridine, which is responsible for many of the adverse effects associated with sulfasalazine 5.