Aminosalicylates contain the compound 5-aminosalicylic acid, or 5-ASA, which helps reduce inflammation. These drugs are used to prevent relapses and maintain remission in mild-to-moderate ulcerative colitis.
The standard aminosalicylate drug is sulfasalazine (Azulfidine, generic). This drug combines the 5-ASA drug mesalamine with sulfapyridine, a sulfa antibiotic. While sulfasalazine is inexpensive and effective, the sulfa component of the drug can cause unpleasant side effects, including headache, nausea, and rash.
Patients who cannot tolerate sulfasalazine or who are allergic to sulfa drugs have other options for aminosalicylate drugs, including mesalamine (Asacol, Pentasa, Lialda, Delzicol, generic), olsalazine (Dipentum), and balsalazide (Colazal, generic). These drugs, like sulfasalazine, are taken as pills several times a day. Lialda is a once-daily mesalamine pill for patients with ulcerative colitis. Mesalamine is also available in enema (Rowasa, generic) and suppository (Canasa, generic) forms.
Common side effects of aminosalicylate drugs include:
- Abdominal pain and cramps (mesalamine, balsalazide)
- Diarrhea (mesalamine, olsalazine)
- Gas (mesalamine)
- Nausea (mesalamine)
- Hair loss (mesalamine)
- Headache (mesalamine, balsalazide)
- Dizziness (mesalamine)
Mesalamine can cause kidney problems and should be used with caution by patients with kidney disease. All mesalamine preparations, including sulfasalazine, appear to be safe for children, and for women who are pregnant or nursing.
Corticosteroids (commonly called steroids) are powerful anti-inflammatory drugs. They are used only for active ulcerative colitis. Steroids are frequently combined with other drugs to produce more rapid symptom relief and to allow quicker withdrawal, although such combinations do not improve remission time. Because the oral form has serious long-term effects, they are not useful for maintenance therapy. Patients who have a poor response to steroids are also less likely to do well with repeat therapy.
Corticosteroid Types. Prednisone (Deltasone, generic), methylprednisolone (Medrol, generic), and hydrocortisone (Cortef, generic) are the most common oral corticosteroids. Newer steroids, such as budesonide (Entocort), are given via enema and affect only local areas in the intestine and do not circulate throughout the body. Such drugs may avoid the widespread side effects that are a serious problem with long-term treatment using older conventional steroids. They are only helpful for milder ulcerative colitis involving the rectum and sigmoid colon.
Administering Corticosteroids. Most corticosteroids can be taken as a pill. For patients who cannot take oral forms, methylprednisolone and hydrocortisone may also be given intravenously or rectally as a suppository, enema, or foam. The severity or location of the condition often determines the form.
Side Effects of Corticosteroids. Oral steroids can have distressing and sometimes serious long-term side effects, including:
- Susceptibility to infection
- Weight gain (particularly increased fatty tissue on the face and upper trunk and back)
- Excess hair growth
- High blood pressure (hypertension)
- Weakened bones (osteoporosis)
- Cataracts and glaucoma
- Muscle wasting
- Menstrual irregularities
- Upper gastrointestinal ulcers
- Personality change, including irritability, insomnia, depression, and psychosis
Withdrawing from Corticosteroids. Once the intestinal inflammation has subsided, steroids must be withdrawn very gradually. Withdrawal symptoms, including fever, malaise, and joint pain, may occur if the dosage is lowered too rapidly. If this happens, the dosage is increased slightly and maintained until symptoms are gone. More gradual withdrawal is then resumed.
Immunosuppressant drugs are used for long-term therapy, especially for very active inflammatory bowel disease that does not respond to milder treatments. Such drugs suppress or limit actions of the immune system and therefore the inflammatory response that causes ulcerative colitis. Immunosuppressants can prevent relapse, even when used alone, and they can help maintain remissions of ulcerative colitis for several years.
Azathioprine (Imuran, Azasan, generic) and mercaptopurine ([6-MP], Purinethol, generic) are the standard oral immunosuppressant drugs. However, it can take 3 - 6 months for these drugs to have an effect. To speed up the response, they are sometimes prescribed along with a corticosteroid drug. Lower steroid doses are then needed, resulting in fewer side effects. Corticosteroids may also be withdrawn more quickly. For this reason, immunosuppressants are sometimes referred to as steroid-sparing drugs.
Other pill forms of immunosuppressants include cyclosporine A (Sandimmune, Neoral) and tracrolimus (Prograf). Cyclosporine A is also given intravenously to patients with severe ulcerative colitis. These drugs are quicker-acting than azathiopine and 6-mercaptopurine. Cyclosporine A generally takes 1 - 2 weeks to take effect. Methotrexate (MTX, Rheumatrex) is another fast-acting type of injectable immunosuppressant that is effective for Crohn’s disease but not for ulcerative colitis. Antibiotics, which are used to treat Crohn's disease, are also not helpful for ulcerative colitis.
General side effects of immunosuppressants may include nausea, vomiting, and liver or pancreatic inflammation. Patients should receive frequent blood tests to monitor bone marrow, liver, and kidneys. Patients who take cyclosporine A or tacrolimus need to have their blood pressure and kidney function checked regularly. Children and young adults who take azathioprine or mercaptopurine should be monitored for signs of cancer as these drugs have been associated with increased risk of an aggressive form of T-cell lymphoma. Immunosuppressants are usually not recommended for women who are pregnant or breast-feeding.
Biologic response modifiers are genetically engineered drugs that target specific proteins involved with the body’s inflammatory response. Three biologic drugs are approved for treatment of moderate-to-severe ulcerative colitis in patients who have not responded to other drugs:
- Infliximab (Remicade), which is given by intravenous infusion in a doctor’s office or hospital clinic (after the first three doses, the drug is administered every 8 weeks)
- Adalimumab (Humira), which you can give by injection at home (after the first two doses, you give yourself an injection every other week)
- Golimumab (Simponi) is given by self-injection at home once a month
Infliximab, adalimumab, and golimumab target and block an inflammatory immune factor known as tumor necrosis factor (TNF). These drugs are described as anti-TNF drugs, TNF blockers, or TNF inhibitors. Studies indicate that anti-TNF drugs may reduce ulcerative colitis symptoms and help patients achieve and maintain remission.
Common side effects of TNF inhibitors include respiratory infections (sinus infections and sore throat), headache, rash, cough, and stomach pain. All anti-TNF drugs can potentially cause serious severe side effects, including increased susceptibility to viral, fungal, and bacterial infections (including tuberculosis).
Your doctor should carefully monitor you for any signs of infection. Symptoms of fungal infections include fever, malaise, weight loss, sweating, cough, and shortness of breath. If you experience any of these symptoms, contact your doctor.
Anti-TNF drugs can increase the risk for cancer, particularly lymphomas, in children and adolescents. They can also increase the risk for leukemia in patients of all ages. Other severe side effects may include psoriasis, heart failure, liver failure, aplastic anemia, nervous system disorders, and allergic reactions.
Investigational Drugs. Vendolizumab (Entyvio) is a new biologic drug that is being investigated for treatment of moderate-to-severe ulcerative colitis and Crohn’s disease. The FDA is considering this drug for approval in 2014. In clinical trials, the drug was particularly effective for ulcerative colitis.