What are the oral (PO) medications for ulcerative colitis?

From the Guidelines

For patients with mild-to-moderate ulcerative colitis, the most effective oral medication is standard-dose mesalamine (2–3 grams/day) or diazo-bonded 5-ASA, as recommended by the AGA guidelines 1. This recommendation is based on the strongest and most recent evidence, which suggests that standard-dose mesalamine or diazo-bonded 5-ASA is more effective than low-dose mesalamine, sulfasalazine, or no treatment for inducing and maintaining remission in patients with extensive mild-to-moderate ulcerative colitis. Some key points to consider when selecting an oral medication for colitis include:

• The use of mesalamine enemas or suppositories may be considered for patients with mild-to-moderate ulcerative proctosigmoiditis or proctitis, as they may be more effective than oral mesalamine for these conditions 1.
• Once-daily dosing of mesalamine may be comparable to multiple times daily administration, and may improve adherence to treatment 1.
• Budesonide formulations, such as budesonide MMX or controlled ileal release budesonide, may be considered for patients with mild-to-moderate ulcerative colitis, but the evidence for their effectiveness is limited 1.
• Sulfasalazine may be considered for patients who are already taking it and are in remission, or for those with prominent arthritic symptoms, but it has a higher rate of intolerance compared to other 5-ASA drugs 1.
• Immunomodulators, such as azathioprine or 6-mercaptopurine, may be considered for patients with chronic active steroid-dependent disease, as they may help to maintain remission and reduce the need for steroids 1. Overall, the choice of oral medication for colitis should be individualized based on the patient's disease severity, extent, and preferences, as well as their medical history and comorbidities. Regular monitoring for medication side effects and disease activity is essential for optimal management of colitis.

From the FDA Drug Label

Sulfasalazine tablets, USP are indicated: in the treatment of mild to moderate ulcerative colitis, and as adjunctive therapy in severe ulcerative colitis; and for the prolongation of the remission period between acute attacks of ulcerative colitis. Mesalamine delayed-release tablets dosages of 2.4 g and 4.8 g once daily demonstrated superiority over placebo in the primary efficacy endpoint, which was to compare the percentage of patients in remission after 8 weeks of treatment for the mesalamine delayed-release tablets treatment groups versus placebo.

PO Medication Options for Colitis:

• Sulfasalazine (PO): indicated for the treatment of mild to moderate ulcerative colitis, and as adjunctive therapy in severe ulcerative colitis; and for the prolongation of the remission period between acute attacks of ulcerative colitis 2.
• Mesalamine (PO): demonstrated superiority over placebo in inducing remission in patients with mildly to moderately active ulcerative colitis, with dosages of 2.4 g and 4.8 g once daily 3.

From the Research

Medications for Colitis

• Mesalamine is a commonly used medication for the treatment of ulcerative colitis, with multiple formulations available, including oral and topical forms 4, 5, 6.
• Sulfasalazine, olsalazine, and balsalazide are also effective first-line therapies for mildly to moderately active ulcerative colitis and for subsequent maintenance of remission 4.
• Azathioprine and 6-mercaptopurine are effective for maintaining remission in patients with ulcerative colitis, particularly for those who have failed or cannot tolerate mesalazine or sulfasalazine 7, 8.

Dosage and Administration

• The optimal dose of mesalamine for induction of response is unclear, but doses above 1.5 g may not provide additional benefits 4, 5.
• Once-daily dosing with multi-matrix system mesalamine 1.2 g tablets may lead to optimal compliance 4.
• Azathioprine has been shown to be significantly superior to placebo for maintenance of remission, with a lower risk of failure to maintain remission compared to placebo 8.

Safety and Efficacy

• Mesalamine has few serious adverse effects and is generally well tolerated by patients 5.
• Azathioprine and 6-mercaptopurine may be effective as maintenance therapy for patients who have failed or cannot tolerate mesalazine or sulfasalazine, but may be associated with adverse events such as acute pancreatitis and bone marrow suppression 8.
• The risk of colorectal cancer may be reduced with mesalamine doses of 1.2 g or higher, and sulfasalazine doses of 2 g or higher 4.