Mesalazine (INN, BAN), also known as Mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract (Crohn's disease) and mild to moderate ulcerative colitis. Mesalazine is a bowel-specific aminosalicylate drug that is metabolized in the gut and has its predominant actions there, thereby having fewer systemic side effects. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... The posterior aspect of the rectum exposed by removing the lower part of the sacrum and the coccyx. ... An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ... A British Approved Name (BAN) is the official non-proprietary or generic name given to a pharmaceutical substance, as defined in the British Pharmacopoeia (BP). ... United States Adopted Names are unique nonproprietary names assigned to pharmaceuticals marketed in the United States. ... Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. ... Oral medication A medication is any drug taken to cure or reduce the symptoms of an illness or ongoing medical condition. ... Crohns disease (also known as regional enteritis) is a chronic, episodic, inflammatory condition of the gastrointestinal tract characterized by transmural inflammation (affecting the entire wall of the involved bowel) and skip lesions (areas of inflammation with areas of normal lining in between). ... Aminosalicylic acid (C7H7NO3) is also known as para-aminosalicylic acid, p-aminosalicylic acid or 4-aminosalicylic acid; abbreviated 4-ASA, PAS or P. It is sold in the US by Jacobus Pharmaceutical as Paser®. 5-aminosalicylic acid is a closely related compound that also has medical uses. ...

As a derivative of salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism. Salicylic acid is the chemical compound with the formula C6H4(OH)CO2H, where the OH group is adjacent to the carboxyl group. ... Space-filling model of the antioxidant metabolite glutathione. ... In chemistry free radicals are uncharged atomic or molecular species with unpaired electrons or an otherwise open shell configuration. ...

5-ASA is considered the active moiety of Sulfasalazine, which is metabolized to it. Look up moiety in Wiktionary, the free dictionary. ... Sulfasalazine is a sulfa drug, a derivative of Mesalazine (5-aminosalicylic acid abbreviated as 5-ASA), used primarily as an anti-inflammatory agent in the treatment of inflammatory bowel disease as well as for rheumatoid arthritis. ...

Formulations

It is formulated for oral ingestion as tablets or granules, and for rectal administration as rectal suppository, suspension or enemas. It is sold under a variety of brand names (UK: Asacol®, Ipocal®, Pentasa® & Salofalk®. US: Canasa®, Rowasa®, Pentasa® & Asacol®). Four 500mg acetaminophen/paracetamol suppositories A suppository is a medicine that is inserted either into the rectum (rectal suppository) or into the vagina (vaginal suppository) where it melts. ... This 2qt (about 2 liters) enema bag, or fountain syringe, equipped with a rectal nozzle, is to be filled with water or a solution, then suspended near the patient using the hook. ...

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 affect the binding of Mesalazine in the bowel and will therefore reduce its efficacy. Lactulose is a synthetic sugar used in the treatment of constipation and hepatic encephalopathy, a complication of liver disease. ...

Side effects

Commonly:

• Diarrhea
• Nausea
• Cramping

Uncommonly:

• Headache
• Exacerbation of the colitis
• Hypersensitivity reactions (including rash, urticaria, interstitial nephritis and lupus erythematosus-like syndrome)
• Hair Loss
• Interstitial nephritis

Rarely: Interstitial nephritis (or Tubulo-interstitial nephritis) is a form of nephritis affecting the interstititum of the kidneys surrounding the tubules. ... Interstitial nephritis (or Tubulo-interstitial nephritis) is a form of nephritis affecting the interstititum of the kidneys surrounding the tubules. ...

• Acute pancreatitis,
• Hepatitis
• Nephrotic syndrome
• Blood disorders (including agranulocytosis, aplastic anaemia, leukopenia, neutropenia, thrombocytopenia)

Mesalazine avoids the sulphonamide side effects of Sulfasalazine (which contains additional (sulfapyridine), but carries additional rare risks of: Pancreatitis is inflammation of the pancreas. ... Hepatitis (plural hepatitides) implies injury to liver characterised by presence of inflammatory cells in the liver tissue. ... Aplastic anemia is a condition where the bone marrow does not produce enough, or any, new cells to replenish the blood cells. ... Leukopenia or leukocytopenia refers to a decrease in the number of circulating white blood cells (leukocytes) in the blood. ... Neutropenia (or neutropaenia, adjective neutrop(a)enic) is a hematological disorder characterized by an abnormally low number of neutrophil granulocytes (a type of white blood cell). ... Thrombocytopenia (or -paenia, or thrombopenia in short) is the presence of relatively few platelets in blood. ... Sulfasalazine is a sulfa drug, a derivative of Mesalazine (5-aminosalicylic acid abbreviated as 5-ASA), used primarily as an anti-inflammatory agent in the treatment of inflammatory bowel disease as well as for rheumatoid arthritis. ...

• Allergic lung reactions
• Allergic myocarditis
• Methaemoglobinaemia

In medicine (cardiology), myocarditis is inflammation of the myocardium, the muscular part of the heart. ...

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. A full blood count (FBC) or complete blood count (CBC) is a test requested by a doctor or other medical professional that gives information about the cells in a patients blood. ...

References

• British National Formulary 45 March 2003
• (November 30, 2004) in Edited by Sean C. Sweetman: Martindale: The complete drug reference, 34th edition, London: Pharmaceutical Press. ISBN 0-85369-550-4. 

Otherwise known as the doctors prescribing Bible the British National Formulary (BNF) contains a wide spectrum of information on prescribing and pharmacology, among others indications, side effects and costs of the prescription of all medication drugs available on the National Health Service. ...

External links

General Information

• Optimal Dosing of 5-Aminosalicylic Acid: 5 Decades of Choosing Between Politicians

• Links to external chemical sources