How aminosalicylates reduce autoimmune inflammation

Aminosalicylate (also known as 5-aminosalicylic acid or 5-ASA) is a disease-modifying antirheumatic drug (DMARD) used to control inflammation. They have been used for decades to treat inflammatory bowel disease (IBD) and rheumatoid arthritis (RA).

These drugs are chemically related to aspirin. The drugs in this class contain 5-aminosalicylic acid and other ingredients that have the desired anti-inflammatory effect.

This article will discuss which conditions are treated with aminosalicylates, when they can be used, side effects, and how well they work.

What does 5-ASA medication treat?

5-ASA drugs are used to treat ulcerative colitis, rheumatoid arthritis, and in some specific cases Crohn’s disease.

Ulcerative colitis is a form of IBD. It causes inflammation of the bowel (colon or large intestine) and rectum, as well as internal sores called ulcers. 5-ASA is used to treat colon ulcers and inflammation caused by disease.

Guidelines outlined by the American College of Gastroenterology (ACG) recommend oral 5-ASA medications for mild or moderate ulcerative colitis. For proctitis, rectal ulcerative colitis, rectal administration of 5-ASA in the form of an enema is recommended.

For ulcerative colitis affecting the left side of the colon, both oral and rectal forms of 5-ASA are recommended.

Rheumatoid arthritis is an autoimmune disease that affects joints and other tissues. The 5-ASA drug Azulfidine (sulfasalazine) was used as one of the first drugs to control the disease. It may be prescribed at the same time as other DMARDs, including Plaquenil (hydroxychloroquine), Arava (leflunomide), or Trexall (methotrexate).

Sulfasalazine can be used to treat mild to moderate Crohn’s disease in the colon. Crohn’s disease affects all parts of the digestive tract, including the small and large intestines. According to ACG guidelines, sulfasalazine is not recommended for Crohn’s disease causing extracolonic inflammation.

Other forms of 5-ASA medicines, such as Asacol (mesalazine), are not recommended for Crohn’s disease. This is an important distinction to understand because, with the exception of Azulfidine, 5-ASA drugs have not been shown to be effective in treating Crohn’s disease. Using them may mean delayed remission from Crohn’s disease.

Effects on Inflammation

5-ASA drugs have anti-inflammatory effects. They act locally to reduce inflammation in the colon. 5-ASA directly affects intestinal wall tissue along with beneficial bacteria in the colon.

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As the drug works in the colon, it tends to have less of an effect on the rest of the body. There are potential side effects and adverse effects, but they can be mitigated by delivery methods in the colon.

These drugs are most useful for mild to moderate ulcerative colitis. For more severe disease, other medications may be needed to control inflammation, in which diarrhea and deeper ulcers in the colon often occur.

5-ASA Drug List

There are several forms of 5-ASA medication available, including those in the list below. They are used for various types of diseases. The delivery method used is most likely to affect the site of inflammation in the body.

Colazal (balsalazide disodium): This form of 5-ASA comes in capsule form. It is chemically bonded to inert ingredients. The binding between the two chemicals breaks down in the colon, where 5-ASA is released to act on intestinal tissue.

Azulfidine (sulfasalazine): This type of 5-ASA is the one that has been used for the longest time. It contains an ingredient called sulfanilamide. Sulfonamides are a type of antibiotic.

In the colon, enzymes break down sulfasalazine into its constituent parts. Therefore, it acts locally on the colon. That’s why it may help fight inflammation of the colon caused by ulcerative colitis.

It comes in oral form, with or without an enteric coating (which prevents it from being absorbed or broken down in the stomach). It is usually taken several times a day.

Asacol, Apriso, Pentasa, Salofalk (mesalazine): The oral form of mesalamine is designed to work when it reaches the gut. 5-ASA is located inside components that are broken down in the gut, so it can act on inflamed tissue there.

This drug is available in both extended-release and extended-release forms. This formula helps the drug pass through the esophagus, stomach and small intestine before being broken down in the colon where it works.

Mesalamine is also available in enema form. They are inserted into the rectum and act directly on the site of inflammation, the lining of the rectum and/or colon.

Dipentum (olsalazine): This form of the drug contains two molecules of 5-ASA chemically bonded together. This bond is broken by enzymes in the colon, releasing 5-ASA.

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side effect

Various 5-ASA drugs may have some side effects. These may include abdominal pain and cramps, fever, headache, nausea, loss of appetite, rash or vomiting. Diarrhea is uncommon, but it is possible and can be challenging for those who already have IBD.

When to try 5-ASA drugs

5-ASA drugs are used at different stages of the disease process.

For ulcerative colitis, 5-ASA drugs are so-called first-line therapy. This means using them before trying other types of medicines.

This is in cases of mild to moderate disease when oral or rectal 5-ASA drugs may be effective in reducing inflammation. More serious illnesses require treatment with other types of drugs.

In Crohn’s disease, sulfasalazine may be used for mild to moderate disease affecting the colon. For inflammation of the small intestine or other parts of the body, or for severe disease, other medications are recommended.

In rheumatoid arthritis, sulfasalazine is the first-line therapy that may be used with other drugs. If this drug combination does not have the desired effect on inflammation, other treatments may be tried.

who should not use them

Before taking a 5-ASA drug, tell your healthcare provider your medical history of:

  • Allergy to sulfonamides (for sulfasalazine)
  • Allergy to aspirin (for sulfasalazine)
  • Asthma (airway constriction and inflammation)
  • blood disease
  • Myocarditis (swelling of the heart muscle)
  • Pericarditis (cysts around the heart)
  • liver disease
  • kidney disease
  • intestinal obstruction
  • Phenylketonuria (a genetic disorder in which amino acids are not broken down and cause damage to the nervous system)

Do 5-ASA drugs work?

5-ASA drugs do help with mild to moderate types of inflammation. They are often used as the first drug to control inflammation. They may be less effective in severe disease, or they may no longer be effective over time. In these cases, other drugs may be used when disease activity returns.


5-ASA drugs can be used to treat ulcerative colitis, rheumatoid arthritis, or some cases of Crohn’s disease. These drugs are available in oral and topical forms and are used to treat ulcerative colitis. Oral sulfasalazine is used to treat Crohn’s disease (Crohn’s colitis) and rheumatoid arthritis in the colon.

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VigorTip words

5-ASA drugs have been used for decades, so there’s plenty of evidence for when they work and when they don’t, and have a good effect on inflammation. Some people cannot take these drugs or cannot tolerate them, but this is not common.

There are more drugs available to treat IBD and RA, but 5-ASA drugs are still the first to be prescribed because they are effective, often have fewer side effects, and are less expensive.

However, it is important to recognize when these drugs are not doing a good job of stopping inflammation and move on to another treatment.

Frequently Asked Questions

  • How similar are aminosalicylates and NSAIDs?

    NSAIDs (NSAIDs such as Advil or Motrin, which are a type of ibuprofen, Aleve, a type of naproxen, and their strong prescriptions), which can treat pain and inflammation throughout the body (whole body). Aminosalicylates are also locally acting anti-inflammatory drugs (where they are applied). Although there is some overlap in their mechanisms of action, they are different classes of drugs.

  • Do 5-ASA drugs affect immune function?

    5-ASA drugs are not considered immunosuppressive. Other drugs used to treat IBD or rheumatoid arthritis do have an effect on the immune system. However, 5-ASA drugs act directly on inflammation rather than the immune system.

  • What is the best aminosalicylate for Crohn’s disease?

    Various forms of 5-ASA drugs have been used to treat Crohn’s disease in the past. However, they are now known to be less effective than other drugs. In some cases, sulfasalazine may be used to treat mild to moderate Crohn’s disease (Crohn’s colitis) in the large intestine.

  • What is the price of aminosalicylates?

    Sulfasalazine is an older drug and tends to be cheaper at $20 a month. Colazal (balsalazide) may cost less than $100 per month. Oral mesalamines (eg, Asacol, Lialda, Delzicol) can range in price from $100 to $300 per month, but some brands (eg, Pentasa) can cost $1,500 or more per month.

    Mesalamine enemas can cost about $200 a month. Dipentum (olsalazine) may be $1,600 per month. Contacting drug manufacturers may offer patient assistance programs.