Ulcerative Colitis Medication
- Author: Marc D Basson, MD, PhD, MBA, FACS; Chief Editor: BS Anand, MD more...
The goals of pharmacotherapy are to reduce morbidity and to prevent complications. The treatment of ulcerative colitis relies on initial medical management with corticosteroids and anti-inflammatory agents, such as sulfasalazine, in conjunction with symptomatic treatment with antidiarrheal agents and rehydration.
5-aminosalicylic Acid Derivative
These agents have anti-inflammatory effects. They are used to maintain remission and to induce remission of mild flares of disease.
Sulfasalazine is useful in treating mild-to-moderate ulcerative colitis and maintaining remission. It acts locally in the colon to reduce the inflammatory response and systemically inhibits prostaglandin synthesis.
Balsalazide is a prodrug that is converted into 5-aminosalicylic acid through bacterial azo reduction. Metabolites of drug may decrease inflammation by blocking the production of arachidonic acid metabolites in colon mucosa.
Mesalamine is the drug of choice for maintaining remission. It is useful for the treatment of mild-to-moderate ulcerative colitis. It is better tolerated and has less adverse effects than sulfasalazine. Enema and suppository forms are typically used in patients with distal colitis.
Tumor Necrosis Factor Inhibitor
These agents prevent the endogenous cytokine from binding to the cell surface receptor and exerting biological activity. These agents adversely affect normal immune responses and allow development of superinfections; reactivation of latent TB has been reported in patients with previous exposure to TB.
Infliximab is a chimeric mouse-human monoclonal antibody to TNF. It binds free and membrane-bound TNF and thus prevents the cytokine from binding to its cell surface receptor and exerting biological activity. Infliximab is indicated for the treatment of moderate-to-severe active ulcerative colitis in patients who have experienced inadequate response to conventional therapy. It has been shown to reduce signs and symptoms, to achieve clinical remission and mucosal healing, and to eliminate corticosteroid use.
Adalimumab is a recombinant human anti-TNF-alpha IgG1 monoclonal antibody that blocks inflammatory activity of TNF-alpha. It specifically binds to TNF-alpha and blocks its interaction with p55 and p75 cell surface TNF receptors. It also lyses surface TNF expressing cells in vitro and modulates the biological responses responsible for leukocyte migration. This agent is indicated for patients with ulcerative colitis unresponsive to immunosuppressant medicines (eg, corticosteroids, azathioprine, 6-mercaptopurine).
Golimumab is a human anti-TNF-alpha monoclonal antibody that blocks the inflammatory activity of TNF-alpha. It is indicated for induction and maintenance treatment of adults with moderate-to-severe ulcerative colitis that is resistant to prior treatment or requires continuous corticosteroid therapy. Following a brief induction dosage regimen, the maintenance dose is given SC once each month.
These agents regulate key factors of the immune system. Agents such as tacrolimus and cyclosporine are often effective in bringing steroid-resistant disease under control.
Azathioprine is effective as a steroid-sparing or steroid-reducing agent and for use in maintenance therapy. Administration is oral. Onset of action can be delayed up to 3-6 months.
Cyclosporine is effective as a means of avoiding surgery in patients with severe ulcerative colitis refractory to intravenous corticosteroids. It is given as an intravenous infusion, but can be switched to PO qd dose as "bridge" therapy for outpatient use.
6-Mercaptopurine is effective as a steroid-reducing or steroid-sparing agent and for use in maintaining remission. Administration is oral. Onset of action can be delayed up to 3-6 months.
Immunomodulator produced by the bacteria Streptomyces tsukubaensis. Mechanism of action of tacrolimus is similar to cyclosporine. It is effective in bringing steroid-resistant disease under control. Tacrolimus should not be used for long-term therapy, owing to the risk of nephrotoxicity.
Corticosteroids decrease inflammation by suppressing the migration of polymorphonuclear leukocytes and reversing increased capillary permeability. They are used for induction of remission in moderate-to-severe active ulcerative colitis. They have no role in maintaining remission; long-term use can cause adverse effects.
Methylprednisolone is administered intravenously in severe cases.
Given orally, is effective for the treatment of active moderate-to-severe ulcerative colitis.
High dose corticosteroids such as hydrocortisone are used in the treatment of acute, severe ulcerative colitis. Hydrocortisone decreases inflammation by suppressing migration of polymorphonuclear leukocytes and reversing increased capillary permeability.
Budesonide is a potent glucocorticoid that has poor oral absorption and extensive first-pass metabolism. These properties make it ideal for reducing gastrointestinal inflammation. It is indicated for remission induction of active, mild-to-moderate ulcerative colitis.
Budesonide rectal is a corticosteroid available as a 20 mg/metered-dose rectal foam. It is indicated for the induction of remission in adults with active mild-to-moderate distal ulcerative colitis extending up to 40 cm from the anal verge.
Alpha 4 Integrin Inhibitors
Integrin inhibitors are emerging as options for moderate-to-severe active IBD in patients who have had an inadequate response with, lost response to, or were intolerant to a TNF blocker or immunomodulator; or had an inadequate response with, were intolerant to, or demonstrated dependence on corticosteroids.
Vedolizumab is a recombinant humanized monoclonal antibody that binds specifically to α4β7 integrin. It blocks the interaction of α4β7 integrin with mucosal addressin cell adhesion molecule-1 (MAdCAM-1) and inhibits the migration of memory T-lymphocytes across the endothelium into inflamed gastrointestinal parenchymal tissue. It is indicated for both ulcerative colitis and Crohn disease.
In several controlled, trials, antibiotics have not been shown to provide consistent benefits for the treatment of active ulcerative colitis. Thus, they are usually administered on an empiric basis in patients with severe colitis in whom they may help by averting a life-threatening infection. They have been shown to be effective for the treatment of pouchitis after an IPAA procedure
A fluoroquinolone, ciprofloxacin has activity against pseudomonads, streptococci, MRSA, Staphylococcus epidermidis, and most gram-negative organisms but no activity against anaerobes. Inhibits bacterial DNA synthesis and, consequently, growth.
Metronidazole is an imidazole ring–based antibiotic active against various anaerobic bacteria and protozoa. Used in combination with other antimicrobial agents but as monotherapy for C difficile enterocolitis.
These agents are nonabsorbable synthetic opioids that provide symptomatic relief in the treatment of ulcerative colitis. They prolong GI transit time and decrease secretion via peripheral mu-opioid receptors. They reduce visceral nociception via afferent pathway inhibition.
This drug combination consists of 2.5 mg of diphenoxylate, which is a constipating meperidine congener, and 0.025 mg of atropine to discourage abuse. The preparation inhibits excessive GI propulsion and motility, but it may exacerbate constipation.
Loperamide, which is available over the counter, acts on intestinal muscles to inhibit peristalsis and to slow intestinal motility. It prolongs the movement of electrolytes and fluid through bowel and increases viscosity and loss of fluids and electrolytes. Loperamide improves stool frequency and consistency, reduces abdominal pain and fecal urgency, and may exacerbate constipation.
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|Ulcerative Colitis||Crohn Disease|
|Only colon involved||Panintestinal|
|Continuous inflammation extending proximally from rectum||Skip-lesions with intervening normal mucosa|
|Inflammation in mucosa and submucosa only||Transmural inflammation|
|No granulomas||Noncaseating granulomas|
|Perinuclear ANCA (pANCA) positive||ASCA positive|
|Bleeding (common)||Bleeding (uncommon)|
|Fistulae (rare)||Fistulae (common)|