Mesalazine

Mesalazine is an active ingredient for the treatment of inflammatory mucosal diseases of the rectum and colon. It has anti-inflammatory and antioxidant properties and belongs to the group of aminosalicylates. Mesalazine is available in the form of enemas or suppositories, but is also available in the form of film-coated tablets, granules, depot granules or prolonged-release tablets. Mesalazine is a white to light pink powder. Olsalazine and sulfasalazine are prodrugs of mesalazine and are converted into the active mesalazine in the body.

Mesalazine is used to treat chronic inflammatory bowel diseases such as Crohn's disease or ulcerative colitis. It is chemically related to the non-steroidal anti-inflammatory drugs (NSAIDs). The dosage forms are designed in such a way that mesalazine only develops its effect in the intestine. Like its close relatives, the NSAIDs, mesalazine also interferes with arachidonic acid metabolism by inhibiting cyclooxygenase 1&2 in a similar way to aspirin.

Mesalazine also acts as a radical scavenger. Radicals are single electrons. Electrons usually occur in pairs, if they do not, they are called radicals. Radicals are characterized by the fact that they are very reactive and can therefore cause cell damage in the body. Inflammatory bowel disease leads to a higher concentration of damaging oxygen and nitrogen radicals. Mesalazine lowers the concentration of these radicals.

Mesalazine also lowers the activity of the immune system by inhibiting the production of antibodies and disrupting the function of lymphocytes and macrophages. All three are responsible for various inflammations in the body. If their work is disrupted, the inflammatory reaction is also weakened.

Mesalazine is broken down by the liver and excreted by the kidneys in the urine. The half-life of mesalazine, i.e. the time the body needs to excrete half of the active ingredient, is around 25 hours on average. As mesalazine is also available as a prolonged-release tablet, the half-life can be significantly longer.

Always take mesalazine exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose for adults in acute attacks is between 0.8 g and 4.8 g per day.

During remission, the usual dose for adults is between 1.5 g and 2.4 g per day.

The recommended dose for children aged 5 years and over or weighing 17 kg or more is between 1.2 g and 2.4 g per day.

The duration of therapy should not exceed 6 weeks for both children and adults.

The following side effects may occur:

• Allergic reactions

Rarely:

• Abdominal pain
• Diarrhea
• Flatulence
• Nausea and vomiting
• Headache
• dizziness
• chest pain
• Increased sensitivity of the skin to UV radiation

Very rare:

• Renal dysfunction
• pancreatitis
• fever
• sore throat
• malaise
• shortness of breath
• cough
• Skin rash or skin inflammation
• muscle and joint pain
• jaundice
• hair loss
• Numbness and tingling in hands and feet
• Decrease in semen production

Frequency unknown:

• Kidney stones

Interactions may occur if the following medicines are taken at the same time:

• with azathioprine
• with 6-mercaptopurine
• with tioguanine
• with digoxin
• with NSAR
• with drugs that inhibit blood clotting (e.g. warfarin)

Mesalazine must NOT be taken in the following cases:

• in case of allergy to mesalazine or other salicylates
• liver or kidney dysfunction

Mesalazine can be taken from the age of 5 or a weight of 17 kg.

Mesalazine can be taken during pregnancy. No increased risks to the unborn child have been identified in studies. Mesalazine is the drug of choice during pregnancy.

Mesalazine can also be taken during breastfeeding. Mesalazine does pass into breast milk, but only in minimal traces, even at very high doses. There is a single case report of watery diarrhea in a 6-week-old child, but this subsided immediately when therapy was discontinued. Mesalazine is also the drug of choice during breastfeeding.