From the Guidelines
Mesalamine is recommended as a first-line treatment for mild-to-moderate ulcerative colitis, with a standard dose of 2-3 grams/day, due to its effectiveness in reducing inflammation and inducing remission, as supported by the most recent guidelines from the American Gastroenterological Association (AGA) in 2019 1. The AGA guidelines suggest that mesalamine is a preferred treatment option for patients with extensive mild-moderate ulcerative colitis, and that it should be used instead of low-dose mesalamine, sulfasalazine, or no treatment. Some key points to consider when using mesalamine include:
- The use of standard-dose mesalamine (2-3 grams/day) is recommended for patients with extensive mild-moderate ulcerative colitis, as it has been shown to be effective in inducing remission 1.
- The addition of rectal mesalamine to oral 5-ASA may be beneficial for patients with extensive or left-sided mild-moderate ulcerative colitis, as it has been shown to improve outcomes 1.
- High-dose mesalamine (>3 grams/day) may be considered for patients with moderate disease activity or those who have not responded to standard-dose mesalamine, although the evidence for this is moderate to low quality 1.
- Once-daily dosing of mesalamine is suggested, rather than multiple times per day dosing, as it has been shown to be effective and improve patient adherence 1. It's worth noting that while older guidelines from 2004 also support the use of mesalamine for the treatment of ulcerative colitis, the most recent guidelines from 2019 provide the strongest and most up-to-date evidence for its use 1. Overall, mesalamine is a well-established treatment option for mild-to-moderate ulcerative colitis, and its use is supported by strong evidence from recent guidelines.
From the FDA Drug Label
Mesalamine delayed-release tablets are an aminosalicylate indicated for the: (1) induction and maintenance of remission in adult patients with mildly to moderately active ulcerative colitis. (1) treatment of mildly to moderately active ulcerative colitis in pediatric patients weighing at least 24 kg.
The primary use of mesalamine is for the treatment of ulcerative colitis. It is indicated for:
- Induction and maintenance of remission in adult patients with mildly to moderately active ulcerative colitis.
- Treatment of mildly to moderately active ulcerative colitis in pediatric patients weighing at least 24 kg 2, 2.
From the Research
Mesalamine Overview
- Mesalamine, also known as mesalazine, is a 5-aminosalicylic acid compound used in the treatment of mild to moderate ulcerative colitis 3.
- It is the first-line treatment for patients with mild-to-moderate ulcerative colitis, with multiple formulations available, primarily differentiated by their means of delivering active mesalamine to the colon 3.
Efficacy in Ulcerative Colitis
- Mesalamine has been demonstrated in randomized controlled trials to induce both clinical response and remission, and maintain clinical remission, in patients with ulcerative colitis 3, 4.
- It has few serious adverse effects and is generally well tolerated by patients 3.
- The therapeutic effect of mesalazine occurs topically at the site of diseased colonic mucosa, with high rates of efficacy in induction and maintenance of remission 5.
Efficacy in Crohn's Disease
- Aminosalicylates, including mesalamine, have been advocated for several decades in Crohn's disease, but the evidence base is not as firmly established as for ulcerative colitis 4, 6.
- Sulfasalazine has modest efficacy compared to placebo and is inferior to corticosteroids for the treatment of mild to moderately active Crohn's disease 6.
- High dose mesalamine (3 to 4.5 g/day) is not more effective than placebo for inducing response or remission in Crohn's disease 6.
Formulations and Delivery Methods
- A myriad of oral mesalazine preparations have been formulated with various drug delivery methods to minimize systemic absorption and maximize drug availability at the inflamed colonic epithelium 5.
- It remains unclear whether different oral mesalazine formulations are bioequivalent, and factors that may influence the selection of one agent above another are still being explored 5.