Medications for Ulcerative Colitis Treatment
For the treatment of ulcerative colitis, aminosalicylates (5-ASA) are the first-line therapy for mild to moderate disease, with oral mesalamine 2-4g daily being the most effective option, while corticosteroids are indicated when 5-ASA therapy fails or for moderate to severe disease. 1, 2
First-Line Medications for Mild to Moderate Ulcerative Colitis
Aminosalicylates (5-ASA)
- Standard dose mesalamine (2-3g/day) is recommended over low-dose mesalamine, sulfasalazine, or no treatment for extensive mild-moderate ulcerative colitis 1
- Mesalamine formulations include:
- Once-daily dosing with mesalamine is as effective as multiple times per day dosing 1, 2
- For distal disease (proctitis or left-sided colitis), combining oral and topical mesalamine therapy is more effective than either alone 2
- Topical mesalamine (suppositories or enemas) is more effective than topical corticosteroids for distal disease 2
Dosing Considerations
- For mild-moderate disease, standard dose mesalamine (2-3g/day) is recommended 1
- For suboptimal response or moderate disease activity, high-dose mesalamine (>3g/day) with rectal mesalamine is suggested 1
- For maintenance therapy, 2.4g/day is generally sufficient 3
- Dose-dependent efficacy has been observed with 4.8g/day being optimal for active disease and 2.4g/day for maintenance 3
Second-Line Medications
Corticosteroids
- Prednisolone 40mg daily is appropriate for patients requiring prompt response or those with mild-moderate disease who failed mesalamine therapy 1
- Budesonide MMX or controlled ileal-release budesonide may be used but are less effective than standard-dose mesalamine for induction of remission 1
- Prednisolone should be tapered gradually over approximately 8 weeks according to patient response 1
- Long-term treatment with steroids is undesirable due to side effects 1
Immunomodulators
- For steroid-dependent disease, azathioprine (1.5-2.5mg/kg/day) or mercaptopurine (0.75-1.5mg/kg/day) are recommended 1
- These agents help reduce steroid dependency and maintain remission 4
Treatment Based on Disease Location
Extensive or Left-Sided Colitis
- First-line: Oral mesalamine 2-4g daily 1
- Consider adding topical mesalamine for left-sided disease 1, 2
- For inadequate response: Prednisolone 40mg daily 1
Distal Colitis/Proctitis
- First-line: Mesalamine suppositories (for proctitis) or enemas (for more proximal disease) combined with oral mesalamine 1, 2
- Mesalamine enemas are preferred over rectal corticosteroids 1
- For proctitis, mesalamine suppositories are strongly recommended over other therapies 1
Severe Ulcerative Colitis
- Requires hospital admission and intensive treatment 2
- Intravenous corticosteroids are the mainstay of treatment 1
- Ciclosporin may be effective for severe, steroid-refractory colitis 1
Common Side Effects and Monitoring
Aminosalicylates
- Generally well-tolerated with fewer side effects than sulfasalazine 5
- Potential adverse reactions include headache, flatulence, abnormal liver function tests, and pruritus 6
- Rare but serious side effects include renal impairment, mesalamine-induced acute intolerance syndrome, and hypersensitivity reactions 6
Corticosteroids
- Side effects include mood changes, insomnia, hyperglycemia, fluid retention, and with long-term use: osteoporosis, cataracts, and adrenal suppression 4
- Not recommended for long-term maintenance therapy 1
Important Clinical Considerations
- Treatment should be tailored based on disease extent, severity, and patient preference 2
- Combination of oral and topical therapy is more effective than either alone for distal disease 2
- Proximal constipation should be treated with stool bulking agents or laxatives 1
- Sulfasalazine has a higher incidence of side effects compared to newer 5-ASA drugs but may benefit patients with reactive arthropathy 1
- Treatment goals have shifted from achieving clinical response to achieving biochemical, endoscopic, and histological remission 1, 2