Mesalazine
Encyclopedia
Mesalazine also known as Mesalamine (USAN
) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory
drug
used to treat inflammation of the digestive tract ulcerative colitis
and mild-to-moderate Crohn's disease
. Mesalazine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects. As a derivative of salicylic acid
, 5-ASA is also thought to be an antioxidant
that traps free radicals, which are potentially damaging byproducts of metabolism.
5-ASA is considered the active moiety
of sulfasalazine, which is metabolized to sulfapyridine and 5_ASA.
, suspension or enema
s. It is marketed under a variety of brand names:
The newest of these is Apriso (Salofalk granules in Europe), approved by the U.S. Food and Drug Administration (FDA) in October 2008 for the induction and maintenance of remission in ulcerative colitis. Its main benefit is that it needs to be taken only once a day, which provides convenient dosing regimen for patients. Several formulations of mesalazine have published data to suggest that once-daily dosing is sufficient in ulcerative colitis.
Lialda (Mesavant XL in Europe) contains the highest mesalamine dose per tablet (1.2 g).
Dosing depends on the preparation used; in particular, slow-release tablets may have quite different drug delivery characteristics and are not interchangeable.
Preparations that lower stool pH (such as lactulose
, a laxative) will possibly affect the binding of mesalazine in the bowel and will therefore reduce its efficacy.
Uncommonly:
Rarely:
Mesalazine avoids the sulphonamide side effects of sulfasalazine (which contains additional sulfapyridine
), but carries additional rare risks of:
United States Adopted Name
United States Adopted Names are unique nonproprietary names assigned to pharmaceuticals marketed in the United States. Each name is assigned by the USAN Council, which is co-sponsored by the American Medical Association , the United States Pharmacopeial Convention , and the American Pharmacists...
) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory
Anti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....
drug
Medication
A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...
used to treat inflammation of the digestive tract ulcerative colitis
Ulcerative colitis
Ulcerative colitis is a form of inflammatory bowel disease . Ulcerative colitis is a form of colitis, a disease of the colon , that includes characteristic ulcers, or open sores. The main symptom of active disease is usually constant diarrhea mixed with blood, of gradual onset...
and mild-to-moderate Crohn's disease
Crohn's disease
Crohn's disease, also known as regional enteritis, is a type of inflammatory bowel disease that may affect any part of the gastrointestinal tract from mouth to anus, causing a wide variety of symptoms...
. Mesalazine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects. As a derivative of salicylic acid
Salicylic acid
Salicylic acid is a monohydroxybenzoic acid, a type of phenolic acid and a beta hydroxy acid. This colorless crystalline organic acid is widely used in organic synthesis and functions as a plant hormone. It is derived from the metabolism of salicin...
, 5-ASA is also thought to be an antioxidant
Antioxidant
An antioxidant is a molecule capable of inhibiting the oxidation of other molecules. Oxidation is a chemical reaction that transfers electrons or hydrogen from a substance to an oxidizing agent. Oxidation reactions can produce free radicals. In turn, these radicals can start chain reactions. When...
that traps free radicals, which are potentially damaging byproducts of metabolism.
5-ASA is considered the active moiety
Functional group
In organic chemistry, functional groups are specific groups of atoms within molecules that are responsible for the characteristic chemical reactions of those molecules. The same functional group will undergo the same or similar chemical reaction regardless of the size of the molecule it is a part of...
of sulfasalazine, which is metabolized to sulfapyridine and 5_ASA.
Formulations
Mesalazine is formulated for oral ingestion as tablets or granules, and for rectal administration as a rectal suppositorySuppository
A suppository is a drug delivery system that is inserted into the rectum , vagina or urethra , where it dissolves.They are used to deliver both systemically-acting and locally-acting medications....
, suspension or enema
Enema
An enema is the procedure of introducing liquids into the rectum and colon via the anus. The increasing volume of the liquid causes rapid expansion of the lower intestinal tract, often resulting in very uncomfortable bloating, cramping, powerful peristalsis, a feeling of extreme urgency and...
s. It is marketed under a variety of brand names:
- UK: Asacol, Ipocal, Pentasa, Salofalk, Mezavant XL
- Ireland: Asacolon, Pentasa, Salofalk, Mezavant XL
- France: Asacol, Pentasa, Mezavant
- US: Canasa, Rowasa, Pentasa, Asacol, Lialda, Apriso,Salofalk
- Canada: Asacol, Pentasa, Salofalk, Mezavant
- India: Mesacol
- Mexico: Salofalk
The newest of these is Apriso (Salofalk granules in Europe), approved by the U.S. Food and Drug Administration (FDA) in October 2008 for the induction and maintenance of remission in ulcerative colitis. Its main benefit is that it needs to be taken only once a day, which provides convenient dosing regimen for patients. Several formulations of mesalazine have published data to suggest that once-daily dosing is sufficient in ulcerative colitis.
Lialda (Mesavant XL in Europe) contains the highest mesalamine dose per tablet (1.2 g).
Dosing depends on the preparation used; in particular, slow-release tablets may have quite different drug delivery characteristics and are not interchangeable.
Preparations that lower stool pH (such as lactulose
Lactulose
Lactulose is a synthetic, non-digestible sugar used in the treatment of chronic constipation and hepatic encephalopathy, a complication of liver disease. It is a disaccharide formed from one molecule each of the simple sugars fructose and galactose...
, a laxative) will possibly affect the binding of mesalazine in the bowel and will therefore reduce its efficacy.
Side effects
Commonly:- Diarrhea
- Nausea
- Cramping
- Flatulence
Uncommonly:
- HeadacheHeadacheA headache or cephalalgia is pain anywhere in the region of the head or neck. It can be a symptom of a number of different conditions of the head and neck. The brain tissue itself is not sensitive to pain because it lacks pain receptors. Rather, the pain is caused by disturbance of the...
- Exacerbation of the colitis
- Hypersensitivity reactions (including rash, urticariaUrticariaUrticaria is a kind of skin rash notable for pale red, raised, itchy bumps. Hives is frequently caused by allergic reactions; however, there are many non-allergic causes...
aka hives, interstitial nephritisInterstitial nephritisInterstitial nephritis is a form of nephritis affecting the interstitium of the kidneys surrounding the tubules...
and lupus erythematosusLupus erythematosusLupus erythematosus is a category for a collection of diseases with similar underlying problems with immunity . Symptoms of these diseases can affect many different body systems, including joints, skin, kidneys, blood cells, heart, and lungs...
-like syndrome) - Hair Loss
- Interstitial nephritisInterstitial nephritisInterstitial nephritis is a form of nephritis affecting the interstitium of the kidneys surrounding the tubules...
Rarely:
- Acute pancreatitisPancreatitisPancreatitis is inflammation of the pancreas. It occurs when pancreatic enzymes that digest food are activated in the pancreas instead of the small intestine. It may be acute – beginning suddenly and lasting a few days, or chronic – occurring over many years...
- HepatitisHepatitisHepatitis is a medical condition defined by the inflammation of the liver and characterized by the presence of inflammatory cells in the tissue of the organ. The name is from the Greek hepar , the root being hepat- , meaning liver, and suffix -itis, meaning "inflammation"...
- Nephrotic syndromeNephrotic syndromeNephrotic syndrome is a nonspecific disorder in which the kidneys are damaged, causing them to leak large amounts of protein from the blood into the urine....
- Blood disorders (including agranulocytosisAgranulocytosisGranulopenia, also known as Agranulosis or Agranulocytosis, is an acute condition involving a severe and dangerous leukopenia , most commonly of neutrophils causing a neutropenia in the circulating blood. It represents a severe lack of one major class of infection-fighting white blood cells...
, aplastic anaemia, leukopeniaLeukopeniaLeukopenia is a decrease in the number of white blood cells found in the blood, which places individuals at increased risk of infection....
, neutropeniaNeutropeniaNeutropenia, from Latin prefix neutro- and Greek suffix -πενία , is a granulocyte disorder characterized by an abnormally low number of neutrophils, the most important type of white blood cell...
, thrombocytopeniaThrombocytopeniaThrombocytopenia is a relative decrease of platelets in blood.A normal human platelet count ranges from 150,000 to 450,000 platelets per microliter of blood. These limits are determined by the 2.5th lower and upper percentile, so values outside this range do not necessarily indicate disease...
)
Mesalazine avoids the sulphonamide side effects of sulfasalazine (which contains additional sulfapyridine
Sulfapyridine
Sulfapyridine, original UK spelling Sulphapyridine, is a sulfonamide antibacterial. At one time it was commonly referred to as M&B....
), but carries additional rare risks of:
- Allergic lung reactions
- Allergic myocarditisMyocarditisMyocarditis is inflammation of heart muscle . It resembles a heart attack but coronary arteries are not blocked.Myocarditis is most often due to infection by common viruses, such as parvovirus B19, less commonly non-viral pathogens such as Borrelia burgdorferi or Trypanosoma cruzi, or as a...
- Methaemoglobinaemia
Monitoring
As a result of the small risks of kidney, liver and blood disorders, blood tests should be taken before and after starting treatment. Patients are advised to report any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that occurs during treatment so that a full blood count can be urgently taken.External links
- Optimal Dosing of 5-Aminosalicylic Acid: 5 Decades of Choosing Between Politicians
- "Novel formulation increases efficacy of mesalamine for treating ulcerative colitis" Reuters article on Lialda/Mezavant trial success.
- Once daily mesalazine effective in active ulcerative colitis: study
- Pentasa Official Site
- Asacol Official Site
- Lialda Official Site
- Apriso Official Site
- Asacol Side Effects