Mesalazine

Mesalazine

Clinical data
Routes of administration	oral rectal
ATC code	A07EC02 (WHO)
Pharmacokinetic data
Bioavailability	orally: 20-30% absorbed rectally: 10-35%
Metabolism	Rapidly & extensively metabolised intestinal mucosal wall and the liver.
Elimination half-life	5 hours after initial dose. At steady state 7 hours
Identifiers
IUPAC name 5-amino-2-hydroxybenzoic acid
CAS Number	89-57-6
PubChem CID	4075
DrugBank	APRD01098
CompTox Dashboard (EPA)	DTXSID5024506
ECHA InfoCard	100.001.745
Chemical and physical data
Formula	C7H7NO3
Molar mass	153.135 g/mol g·mol−1

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.

As a derivative of salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism.

5-ASA is considered the active moiety of Sulfasalazine, which is metabolized to it.

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 and Lialda). The newest of these is Lialda, approved by the FDA in January 2007 for induction of remission in ulcerative colitis. Its main benefit is that it needs to be taken only once a day, which improves convenience and treatment compliance.

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.

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:

• 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:

• Allergic lung reactions
• Allergic myocarditis
• 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.

References

• British National Formulary 45 March 2003
• Edited by Sean C. Sweetman, ed. (November 30, 2004). Martindale: The complete drug reference (34th edition ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4. {{cite book}}: |edition= has extra text (help); |editor= has generic name (help)

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.
• Side effects and Dosages of cansa