Ulcerative Colitis in Children Medication

Class Summary

These drugs are used to maintain remission and to induce remission of mild flares of disease. The mainstay of outpatient management is anti-inflammatory therapy with 5-a minosalicylic acid (5-ASA) preparations.

Sulfasalazine (Azulfidine)

Sulfasalazine was the first 5-aminosalicylic acid preparation available for the treatment of ulcerative colitis (UC). It is useful in the management of ulcerative colitis and acts locally in the colon to decrease the inflammatory response and systemically inhibits prostaglandin synthesis

Mesalamine (Asacol, Pentasa, Rowasa)

Mesalamine is DOC to maintain remission. Mesalamine is provided as a controlled-release capsule (Pentasa) or enteric-coated tablet (Asacol). Begin with a low dose, and increase the dose if adverse effects (eg, headache, diarrhea) do not develop. It is also available as an enema or suppository for rectal administration.

The currently approved PO mesalamine products in the United States differ only in the mechanism of drug delivery. Asacol has mesalamine within a Eudragit-S coating that dissolves and releases the mesalamine at pH 7, which typically occurs in the terminal ileum. Pentasa is 5-ASA in ethylcellulose and has a time-release coating. Its release begins at the pylorus. Rectal dosage forms deliver high concentrations of mesalamine to the left colon as high as the splenic flexure (enema with 30 min retention) or to the rectum for use in proctitis (supp). Although effective, mesalamine is associated with a relatively high relapse rate upon discontinuation.

Balsalazide (Colazal)

Balsalazide is a prodrug that is converted into 5-aminosalicyclic acid through bacterial azoreduction. Metabolites of the drug may decrease inflammation by blocking production of arachidonic acid metabolites in the colon mucosa.

Class Summary

These drugs are used in steroid-refractory or steroid-dependent patients.

6-Mercaptopurine (Purinethol)

6-Mercaptopurine is a purine analog that inhibits purine ribonucleotide synthesis and cell proliferation. It alters immune response through effects on natural killer cells and cytotoxic T cells.

Azathioprine (Imuran)

Azathioprine is rapidly converted to 6-mercaptopurine in vivo. It antagonizes purine metabolism and inhibits synthesis of DNA, RNA, and proteins. It may decrease proliferation of immune cells, which lowers autoimmune activity.

Cyclosporine (Sandimmune, Neoral)

Cyclosporine, also called cyclosporin A, is used to treat severe colitis refractory to corticosteroids. One must strongly consider surgical colectomy. It may cause irreversible nephrotoxicity, seizures, and opportunistic infections.

Class Summary

These drugs are used to induce the remission of acute exacerbations. Acute flares of moderate-to-severe ulcerative colitis in the pediatric population tend to respond well to corticosteroids, but numerous adverse effects limit long-term use.

Prednisone (Deltasone, Orasone)

Used for short-term exacerbations. It has a direct effect on inflammation, including decreased release of inflammatory cytokines; inhibition of phospholipase, which, in turn, inhibits arachidonic acid liberation from membranes; and inhibition of neurofibromatosis (NF)–kappa-beta function.

Methylprednisolone (Solu-Medrol)

Methylprednisolone decreases inflammation by suppressing migration of polymorphonuclear leukocytes and reversing increased capillary permeability. This agent is administered intravenously in severe cases.

Class Summary

Tumor necrosis factor (TNF) is a cytokine; 2 forms with similar biologic properties have been identified. TNF-alpha, or cachectin, is produced predominantly by macrophages. TNF-beta, or lymphotoxin, is produced by lymphocytes. TNF is but one of many cytokines involved in the inflammatory cascade that may contribute to symptoms.

Infliximab (Remicade)

Infliximab neutralizes cytokine TNF-alpha and inhibits its binding to TNF-alpha receptor. Mix in 250 mL 0.9% NaCl and infuse IV over 2 hours. A low-protein-binding filter (1.2 µm or smaller) must be used. It is indicated to reduce signs and symptoms, to induce and maintain clinical remission and mucosal healing, and to eliminate corticosteroid use in adults with moderate-to-severe active UC who have had an inadequate response to conventional therapy. In September 2011, the FDA approved infliximab for UC in children.