Products
Mesalazine is commercially available as film-coated tablets, enteric-coated sustained-release tablets, granules, sustained-release granules, clysms, and suppositories (e.g., Asacol, Mezavant, Pentasa, Salofalk). It has been approved in many countries since 1984.
Structure and properties
Mesalazine (C7H7NO3, Mr = 153.1 g/mol) corresponds to 5-aminosalicylic acid (5-ASA). The active ingredient exists as powders or crystals that are white to light gray or light pink in color and are very sparingly soluble in water. Olsalazine (Dipentum) and sulfasalazine (Salazopyrin) are prodrugs of mesalazine.
Effects
Mesalazine (ATC A07EC02) has anti-inflammatory and antioxidant properties. The dosage forms are designed to exert their effects only in the intestine. They are not only effective locally in the intestine but are also absorbed into the body to a certain extent.
Indications
Mesalazine is used to treat inflammation of the mucosa of the rectum and colon. Potential indications include chronic inflammatory colonic diseases such as ulcerative colitis and Crohn’s disease, rectal inflammation (proctitis), and proctosigmoiditis. Another area of use is complications of hemorrhoids.
Dosage
According to the SmPC. Mesalazine is used either orally, for example, as film-coated tablets or granules, or locally in the form of an enema or suppository.
Contraindications
- Hypersensitivity, including to salicylates.
- Severe liver and kidney dysfunction
- Stomach or intestinal ulcer
- Increased bleeding tendency
- Children under 2 years
Full precautions can be found in the drug label.
Interactions
Potential drug-drug interactions have been described with digoxin, NSAIDs, 6-mercaptopurine, and azathioprine.
Adverse effects
The most common possible adverse effects include diarrhea, nausea, abdominal pain, headache, vomiting, rash, hypersensitivity reactions, and drug fever.
