Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn’s disease.
It is in the category of disease-modifying antirheumatic drugs (DMARDs) family of medications.
It is effective only in colonic diseases.
Mesalazine is an aminosalicylate and anti-inflammatory agent.
It works by direct contact with the intestines.
It is taken by mouth or rectally.
The formulations which are taken by mouth appear to be similarly effective.
Bioavailability
orally: 20–30% absorbed
rectally: 10–35%
Metabolism-Rapidly & extensively metabolized intestinal mucosal wall and the liver
Elimination half-life 5 hours after initial dose.
Use in pregnancy and breastfeeding appears safe, but the drug does cross the placenta and is excreted in breast milk.
The drug should not be used in children under two years of age, in people with kidney disease, or people who are allergic to aspirin.
Patients with a sulfa allergy may have problems.
It is generally used for mildly to moderately active disease.
The formulations which are taken by mouth appear to be similarly effective.
Side effects are primarily gastrointestinal but may also include headache; GI effects include nausea, diarrhea, abdominal pain, and fever.
Serious side effects may include pericarditis, liver problems, and kidney problems.
Reports of various problems when the oral form is used, including: problems caused by myelosuppression, as well as hair loss, peripheral neuropathy, pancreatitis, liver problems, myocarditis and pericarditis, allergic and fibrotic lung reactions, lupus erythematosus-like reactions and rash, drug fever, interstitial nephritis and nephrotic syndrome.
Rarely, use of mesalazine has been associated with an exacerbation of colitis, Stevens Johnson syndrome and erythema multiforme.
Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.
It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.
It is speculated that mesalazine decreases synthesis of prostaglandin and leukotriene, modulating the inflammatory response derived from the cyclooxygenase and lipooxygenase pathways.
It acts locally on colonic mucosa.