Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat

inflammatory bowel disease Inflammatory bowel disease (IBD) is a group of inflammation, inflammatory conditions of the colon (anatomy), colon and small intestine, Crohn's disease and ulcerative colitis being the principal types. Crohn's disease affects the small intestine a ...

, including ulcerative colitis and

Crohn's disease Crohn's disease is a type of inflammatory bowel disease (IBD) that may affect any segment of the gastrointestinal tract. Symptoms often include abdominal pain, diarrhea (which may be bloody if inflammation is severe), fever, abdominal distension ...

. It is generally used for mildly to moderately severe disease. It is taken by mouth or rectally. The formulations which are taken by mouth appear to be similarly effective. Common side effects include headache, nausea, abdominal pain, and fever. Serious side effects may include

pericarditis Pericarditis is inflammation of the pericardium, the fibrous sac surrounding the heart. Symptoms typically include sudden onset of sharp chest pain, which may also be felt in the shoulders, neck, or back. The pain is typically less severe when sit ...

, liver problems, and kidney problems. Use in pregnancy and breastfeeding appears safe. In people with a

sulfa allergy Sulfonamide is a functional group (a part of a molecule) that is the basis of several groups of drugs, which are called sulphonamides, sulfa drugs or sulpha drugs. The original antibacterial sulfonamides are synthetic (nonantibiotic) antimi ...

certain formulations may result in problems. Mesalazine is an

aminosalicylate An aminosalicylate is a class of medications that is often used to treat ulcerative colitis and Crohn's disease. The class includes among others: * 4-Aminosalicylic acid * Balsalazide * Olsalazine *Sulfasalazine *Mesalazine (5-Aminosalicylic acid) ...

and anti-inflammatory. It works by direct contact with the intestines. Mesalazine was approved for medical use in the United States in 1987. It is on the World Health Organization's List of Essential Medicines. It is available as a

generic medication A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active ch ...

and sold under many brand names worldwide. In 2020, it was the 184th most commonly prescribed medication in the United States, with more than 2million prescriptions.

Medical uses

It is used to treat

, including ulcerative colitis and

(effective only in colonic diseases). It is generally used for mildly to moderately active disease. It is taken by mouth or rectally. The formulations which are taken by mouth appear to be similarly effective.

Side effects

There are no data on use in pregnant women, but the drug does cross the placenta and is excreted in

breast milk Breast milk (sometimes spelled as breastmilk) or mother's milk is milk produced by mammary glands located in the breast of a human female. Breast milk is the primary source of nutrition for newborns, containing fat, protein, carbohydrates ( lacto ...

. The drug should not be used in children under two years of age, people with

kidney disease Kidney disease, or renal disease, technically referred to as nephropathy, is damage to or disease of a kidney. Nephritis is an inflammatory kidney disease and has several types according to the location of the inflammation. Inflammation can ...

, or people who are allergic to aspirin. Side effects are primarily gastrointestinal but may also include headache; GI effects include nausea, diarrhea and abdominal pain. There have been scattered reports of various problems when the oral form is used, including: problems caused by myelosuppression ( leukopenia,

neutropenia Neutropenia is an abnormally low concentration of neutrophils (a type of white blood cell) in the blood. Neutrophils make up the majority of circulating white blood cells and serve as the primary defense against infections by destroying bacteria ...

agranulocytosis Agranulocytosis, also known as agranulosis or granulopenia, is an acute condition involving a severe and dangerous lowered white blood cell count (leukopenia, most commonly of neutrophils) and thus causing a neutropenia in the circulating blood. ...

, aplastic anaemia, and thrombocytopenia), as well as hair loss, peripheral neuropathy, pancreatitis, liver problems,

myocarditis Myocarditis, also known as inflammatory cardiomyopathy, is an acquired cardiomyopathy due to inflammation of the heart muscle. Symptoms can include shortness of breath, chest pain, decreased ability to exercise, and an irregular heartbeat. The ...

and

, allergic and fibrotic lung reactions, lupus erythematosus-like reactions and rash (including urticaria),

drug fever Drug-induced fever is a symptom of an adverse drug reaction wherein the administration of drugs intended to help a patient causes a hypermetabolic state resulting in fever. The drug may interfere with heat dissipation peripherally, increase the ra ...

, interstitial nephritis and

nephrotic syndrome Nephrotic syndrome is a collection of symptoms due to kidney damage. This includes protein in the urine, low blood albumin levels, high blood lipids, and significant swelling. Other symptoms may include weight gain, feeling tired, and foamy ...

, usually reversible on withdrawal. Very rarely, use of mesalazine has been associated with an exacerbation of the symptoms of colitis, Stevens Johnson syndrome and erythema multiforme.

Chemistry

Mesalazine is the active

moiety Moiety may refer to: Chemistry * Moiety (chemistry), a part or functional group of a molecule ** Moiety conservation, conservation of a subgroup in a chemical species Anthropology * Moiety (kinship), either of two groups into which a society is ...

of sulfasalazine, which is metabolized to sulfapyridine and mesalazine. It is also the active component of the prodrug

balsalazide Balsalazide is an anti-inflammatory drug used in the treatment of inflammatory bowel disease. It is sold under the brand names Giazo, Colazal in the US and Colazide in the UK. It is also sold in generic form in the US by several generic manufactu ...

along with the inert carrier molecule 4-aminobenzoyl-beta-alanine. It is in the category of disease-modifying antirheumatic drugs (DMARDs) family of medications. It is unclear exactly how it works. Mesalazine is claimed to be a PPAR-γ agonist.

Mechanism of action

Exact mechanism of mesalazine is unknown, but is speculated that mesalazine decreases synthesis of

prostaglandin The prostaglandins (PG) are a group of physiologically active lipid compounds called eicosanoids having diverse hormone-like effects in animals. Prostaglandins have been found in almost every tissue in humans and other animals. They are derive ...

and leukotriene, modulating the inflammatory response derived from the cyclooxygenase and lipooxygenase pathways. It appears to act locally on colonic mucosa.

Society and culture

Brand names

Mesalazine is sold under various names including Apriso, Asacol, Asacol HD, Canasa, Delzicol, Fivasa, Lialda, Pentasa, Rowasa, and Sfrowasa.

References

External links

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