Mesalazine

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient mesalazine is an anti-inflammatory agent used to treat chronic inflammatory bowel disease. It is derived from salicylic acid - like the well-known pain reliever acetylsalicylic acid (ASA). Preparations with mesalazine have fewer side effects than those with the previously used active ingredient sulfasalazine, but they are more complex to manufacture. Read more about the effects and uses of mesalazine, side effects and interactions here.

This is how mesalazine works

The active ingredient mesalazine, like acetylsalicylic acid, inhibits various enzymes that form inflammatory tissue hormones (prostaglandins, leukotrienes, thromboxanes, etc.). Often, acute inflammatory reactions ("relapses"), such as those that occur in chronic inflammatory bowel diseases (Crohn's disease, ulcerative colitis), can be alleviated or completely suppressed.

In addition, mesalazine can neutralize reactive oxygen species (ROS). These aggressive oxygen compounds, also known as “free radicals”, are often present in increased quantities during inflammatory processes and damage the tissue. The fact that mesalazine reduces the risk of long-term effects such as colon cancer in patients with inflammatory bowel disease may be due to this ability to render ROS harmless.

Chronic inflammatory diseases can often be traced back to an overactive immune system through which the immune system attacks the body's own tissue. Mesalazine also counteracts this mechanism: It inhibits the formation and function of certain white blood cells and the release of interleukins, which stimulate the immune system and promote inflammation.

Mesalazine uptake, breakdown and excretion

After ingestion or topical application (as a suppository or rectal foam), the active ingredient is absorbed in the intestine and inactivated in the intestinal mucosa or the liver. The ineffective degradation product is then largely excreted via the kidneys with the urine.

When is mesalazine used?

The active ingredient mesalazine is approved for:

• Treatment of an acute flare-up in Crohn's disease

Outside of the approval area (so-called "off-label" use), the active ingredient is also used against other, less common chronic inflammatory bowel diseases.

In the case of acute attacks, the treatment is carried out briefly until improvement. To prevent relapse, the active ingredient can also be taken over a longer period of time.

This is how mesalazine is used

The anti-inflammatory agent is used in different dosage forms depending on the type of disease. If - as is often the case with ulcerative colitis - the rectum and the rectum are more likely to be affected by the inflammation, mesalazine can be used in the form of suppositories, rectal foam and enema (solution for an enema). If higher-lying parts of the intestine are affected, the active ingredient is usually taken in the form of enteric-coated tablets, prolonged-release tablets (tablets with delayed or slowed-down release of active ingredients) or sustained-release granules. As a normal tablet, mesalazine would be absorbed into the blood at the beginning of the small intestine and would not reach the inflamed sections of the intestine.

Depending on the disease and stage of the disease, different doses are taken. Two to four grams of mesalazine are usually divided into several single doses that are taken throughout the day. If necessary, different dosage forms are used in combination.

In severe cases, a highly effective glucocorticoid ("cortisone") is often also prescribed for acute attacks.

What are the side effects of mesalazine?

In general, treatment with mesalazine has few side effects. The most common mesalazine side effects are headache, high blood pressure, abdominal pain, indigestion, abnormal liver function tests, skin rash, itching, muscle and joint pain, fever and weakness.

What should be considered when using mesalazine?

As a derivative of salicylic acid, the active ingredient can possibly affect blood clotting. Excessive anticoagulant conditions have been reported, particularly in combination with coumarin-type anticoagulants (warfarin and phenprocoumon).

The immune-suppressing effects of immunosuppressants such as azathioprine and mercaptopurine may be increased when these drugs are combined with mesalazine.

In addition, the kidney-damaging effect of non-steroidal anti-inflammatory drugs (NSAIDs such as ibuprofen, diclofenac, acetylsalicylic acid) and immunosuppressants (such as azathioprine and methotrexate = MTX) can be increased if mesalazine is taken at the same time or promptly.

There are limited data on the use of the active substance during pregnancy and breastfeeding. Although these data do not indicate a risk to mother and child, a doctor should decide on an application on a case-by-case basis.

The active ingredient can also be used in children aged six years and over and in older patients without kidney dysfunction.

How to get medication with mesalazine

Preparations with the active ingredient mesalazine require a prescription. So they can only be bought in the pharmacy according to a doctor's prescription.

How long has mesalazine been known?

As early as the 1950s, active ingredients such as sulfasalazine were used against chronic inflammatory bowel diseases that release mesalazine locally in the intestine. After it was proven that the main effect is based on mesalazine, this was also used individually in a suitable dosage form - with the result that the side effect profile of the active ingredient was also significantly improved. Today there are numerous preparations with the active ingredient mesalazine on the German market.

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