Aminosalicylates: Uses, common brands, and safety info

Inflammatory bowel disease (IBD), notably ulcerative colitis or Crohn’s disease, are conditions of long-term inflammation of the gastrointestinal (GI) tract. Symptoms of IBDs may include abdominal pain, diarrhea, rectal bleeding, fatigue, and weight loss. While there is no cure for IBDs, there are several classes of medications that can help treat and manage the symptoms: 

• Anti-inflammatory drugs (e.g., corticosteroids and aminosalicylates)

• Immunosuppressant drugs (e.g., azathioprine and methotrexate)

• Biologics (e.g., Remicade and Humira)

Aminosalicylates, also known as 5-aminosalicylic acids or 5-ASAs, are often the first treatment option for IBDs. Aminosalicylates may also be used to treat some forms of arthritis, however, this article will focus on their use in the treatment of inflammatory bowel diseases.

The following table lists commonly used aminosalicylates followed by information on how they work, what conditions they treat, safety, and cost. 

What are aminosalicylates?

Aminosalicylates (5-ASAs) are a category of drugs that exert an anti-inflammatory effect in the large and small intestines. 5-ASAs are often the first-line treatment option for mild to moderate ulcerative colitis. They may also be given to help prevent flare-ups of ulcerative colitis and maintain remission of symptoms on a long-term basis. 5-ASAs are used less frequently in the management of Crohn’s disease but may be effective in milder cases or to help manage symptoms following surgery.

How do aminosalicylates work?

During a flare-up of ulcerative colitis or Crohn's disease, the intestinal wall becomes inflamed. 5-ASA drugs, chemically related to aspirin, are thought to work directly on the lining of the large and small intestine by inhibiting the production of molecules produced in the body that activates the acute inflammatory response. As a result of reducing the flare-ups, damaged tissue is given time to heal. 

5-ASAs can be administered orally, as tablets or capsules, or rectally, as enemas or suppositories. 5-ASA drugs tend to get absorbed quickly, so the different 5-ASA medications are formulated in different ways to make sure the active ingredient reaches the area of the digestive tract where the inflammation is occurring.  

The oral 5-ASAs that have mesalamine as the active ingredient may be in time-released formulations, such as Pentasa, or release the active ingredient by using acidity in the colon, such as Asacol does. Dipentum releases mesalamine by allowing bacteria in the colon to activate it from its carrier. An advantage of newer 5-ASA medications, such as Apriso, Asacol HD, and Lialda, is that they don’t need to be taken as often as the older 5-ASAs and have delivery formulations that allow the drug to the entire colon.

Combination therapy using both oral and rectal treatments has been shown to be more effective to induce remission of IBDs and improve quality of life than either treatment used alone.

What are aminosalicylates used for?

Individual aminosalicylates (5-ASAs) are approved by the U.S. Food and Drug Administration (FDA) to treat the following medical conditions:

• Active ulcerative colitis

• Maintenance of ulcerative colitis remission

• Ulcerative proctitis (inflammation in the rectum)

Although no 5-ASA is FDA-approved to treat Crohn's disease they are often used off-label as a treatment option.

Types of aminosalicylates by route of administration 

Orally administered aminosalicylates

Oral formulations of 5-ASA medicines, taken by mouth as a tablet or capsule, have different types of formulations or coatings which allow the active drug to be released at different places along the digestive tract where the drug is most needed. Oral 5-ASAs include:

• Azulfidine and Azulfidine EN-tabs (sulfasalazine)

• Asacol, Asacol HD, Delzicol, Pentasa, Lialda, and Apriso (mesalamine)

• Colazal (balsalazide)

• Dipentum (olsalazine)

Rectally administered aminosalicylates

Rectal formulations of 5-ASA medicines, given as suppositories or enemas, allow for the delivery of high-strength therapy while greatly reducing absorption and systemic exposure resulting in few, if any, side effects. Rectal administration also allows for targeting the therapy exactly where it is needed. Rectal therapies are commonly used in conjunction with oral medicines for additional symptom improvement. Rectal 5-ASAs include:

• Rowasa (mesalamine enema)

• Canasa (mesalamine suppositories)

Who can take aminosalicylates?

Adults

5-ASAs are an effective treatment option for adults with ulcerative colitis and may help with flare-ups of mild Crohn’s disease. Because there are a number of dosage options healthcare professionals can tailor the type of drug regimen appropriate for each person’s individual situation.  Dosage choices are typically determined by how active the disease is and what part of the intestine or colon is affected

Children

The FDA has approved the following 5-ASAs to treat mild to moderately active ulcerative colitis in pediatric patients:

• Delzicol (mesalamine): 5 years of age and older

• Colazal (balsalazide): 5 years of age and older

The efficacy and safety of the other 5-ASAs have either not been demonstrated or have not been fully evaluated in randomized, placebo-controlled trials and their use is not recommended in children or adolescents.

Seniors

In general, in clinical studies of 5-ASAs, no overall differences in safety or effectiveness were seen between older patients and younger patients however the numbers of trial participants over age 65 were often too low to rule out differences. Elderly patients should be treated with caution, usually starting at the low end of the dosage range, due to the greater likelihood of decreased liver, kidney, or cardiac function, the presence of other disease states, and the increased probability of other drug use.

Reports from some clinical studies and postmarketing experience suggest a higher incidence of blood dyscrasias (an abnormal condition or disease of the blood such as agranulocytosis, neutropenia, or pancytopenia) in patients 65 and older receiving the following mesalamine (also known as mesalazine) medicines:

• Delzicol

• Asacol and Asacol HD 

• Canasa 

Women who are pregnant or breastfeeding

In general, there have been no adequate and well-controlled clinical trials on the use of 5-ASAs in pregnant women and they should not be administered unless the potential benefit justifies the potential risk to the fetus. 

In general, most 5-ASAs show evidence that they may pass into human milk therefore it is not recommended they be given to nursing women. 

A woman’s healthcare provider is the best source of information when deciding to start or continue 5-ASAs during pregnancy or while breastfeeding.

Are aminosalicylates safe?

In general, 5-ASAs have been found to be safe and well tolerated.  

Contraindications

You should not take any 5-ASA if you are allergic to salicylates or any other active or inactive ingredients of the dosage form. Individual 5-ASAS have the following contraindications:

• Azulfidine (sulfasalazine) and Azulfidine EN-tabs (sulfasalazine delayed-release) are contraindicated in patients with intestinal or urinary obstruction 

Recalls

There are no current 5-ASA product recalls as of February 2022. 

Restrictions

Although 5-ASAs very rarely cause kidney injury, patients with known kidney problems should exercise caution when using these drugs. For those taking 5-ASAs with known kidney problems, routine kidney tests should be performed, particularly when initiating therapy. Individual 5-ASAs have the following cautions/warnings:

• Azulfidine (sulfasalazine) and Azulfidine EN-tabs (sulfasalazine delayed-release) should be given with caution to patients with severe allergy or bronchial asthma.

• Delzicol, Asacol, Asacol HD, Apriso, Canasa, Lialda, Pentasa (mesalamine) should be used cautiously in patients with known liver impairment. 

• Rowasa (mesalamine enema) and Canasa (mesalamine suppositories) should be used cautiously when initially administered to patients with a known allergy to sulfasalazine.

Are aminosalicylates controlled substances?

No, aminosalicylates are not controlled substances.

Common aminosalicylates side effects

Common side effects related to oral 5-ASA agents include headache, nausea, abdominal pain and cramping, loss of appetite, vomiting, rash, or fever. Rarely, 5-ASA agents may cause diarrhea. There have been reports of men who take mesalamine experiencing lower sperm counts however sperm counts returned to normal after stopping the medication.

How much do aminosalicylates cost?

Several 5-ASAs are available in generic formulations, therefore the price will vary greatly between the generic and the brand name versions. Cost may also depend on insurance coverage. The best way to find out how much you will pay is to contact your insurance or Medicare prescription plan for up-to-date coverage information. You can always use a free SingleCare discount card to save money on your prescriptions at participating pharmacies.