Mesalazine

 {{#switch:  

 }}(AU) 

 {{#switch:  

}}(US) 

 {{#switch: 

 }}(AU) 

  {{#switch: 

 }}(CA) 

 {{#switch: 

 }}(UK) 

 {{#switch: 

 }}(US) 

 {{#switch: 

 }}

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 provides convenient dosing regimen for patients.

Once-daily LIALDA with MMX technology contains the highest mesalamine dose per tablet (1.2 g), so patients can take as few as two tablets once daily. Other currently available mesalamines require three to four times daily dosing and 6 to 16 pills a day. ^[1] Whether convenience leads to improved compliance and adherence to therapy long term remains to be proven. Adherence to IBD therapy is multifactorial.

Dosing depends on the preparation used, in particular, slow-release tablets may have quite different drug delivery characteristics and are not interchangeable.

Safety and effectiveness of Lialda has been established for up to 8 weeks. ^[2]

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
• Flatulence ^[2]

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

1. ↑ {{
   1. if: {{#if: http://www.rxdrugnews.com/site/more/fda-approves-lialda-mesalamine/ | {{#if: FDA approves LIALDA™ (mesalamine) |1}}}}
   ||You must specify title = and url = when using {{cite web}}. {{#if: ||}} }}{{
   1. if:
   | {{#if: {{#if: | {{#if: |1}}}} ||You must specify archiveurl = and archivedate = when using {{cite web}}. {{#if: ||}} }} }}{{#if: | {{#if: | [[{{{authorlink}}}|{{#if: | {{{last}}}{{#if: | , {{{first}}} }} | {{{author}}} }}]] | {{#if: | {{{last}}}{{#if: | , {{{first}}} }} | {{{author}}} }} }} }}{{#if: | {{#if: | ; {{{coauthors}}} }} }}{{#if: | {{#if: | ({{#ifeq:{{#time:Y-m-d|{{{date}}}}}|{{{date}}}|[[{{{date}}}]]|{{{date}}}}}) | {{#if: 2007 | {{#if: Jan 17 | (Jan 17 2007) | (2007) }} }} |}} }}{{#if: | . }}{{ #if: | {{{editor}}}: }}{{#if: | {{#if: | {{#if: FDA approves LIALDA™ (mesalamine) | [{{{archiveurl}}} FDA approves LIALDA™ (mesalamine)] }}}} | {{#if: http://www.rxdrugnews.com/site/more/fda-approves-lialda-mesalamine/ | {{#if: FDA approves LIALDA™ (mesalamine) | FDA approves LIALDA™ (mesalamine) }}}} }}{{#if: | () }}{{#if: | ({{{language}}}) }}{{#if: FDA approves LIALDA | . FDA approves LIALDA }}{{#if: | {{{pages}}} }}{{#if: | . {{{publisher}}}{{#if: | | {{#if: 2007Jan 17 || }} }} }}{{#if: ||{{#if: | ({{#ifeq:{{#time:Y-m-d|{{{date}}}}}|{{{date}}}|[[{{{date}}}]]|{{{date}}}}}) | {{#if: 2007 | {{#if: Jan 17 | (Jan 17 2007) | (2007) }} }} }} }}.{{#if: | Archived from the original on [[{{{archivedate}}}]]. }}{{#if: | DOI:{{{doi}}}. }}{{#if: 2008-01-07 | Retrieved on 2008-01-07{{#if: | , [[{{{accessyear}}}]] }}. }}{{#if: | Retrieved on {{{accessmonthday}}}, {{{accessyear}}}. }}{{#if: | Retrieved on {{{accessdaymonth}}} {{{accessyear}}}. }}{{#if: |  “{{{quote}}}” }}
2. ↑ ^{2.0 2.1} {{
   1. if: {{#if: http://www.lialda.com/aboutLialda/sideEffect.asp | {{#if: Safety Information about Lialda |1}}}}
   ||You must specify title = and url = when using {{cite web}}. {{#if: ||}} }}{{
   1. if:
   | {{#if: {{#if: | {{#if: |1}}}} ||You must specify archiveurl = and archivedate = when using {{cite web}}. {{#if: ||}} }} }}{{#if: | {{#if: | [[{{{authorlink}}}|{{#if: | {{{last}}}{{#if: | , {{{first}}} }} | {{{author}}} }}]] | {{#if: | {{{last}}}{{#if: | , {{{first}}} }} | {{{author}}} }} }} }}{{#if: | {{#if: | ; {{{coauthors}}} }} }}{{#if: | {{#if: | ({{#ifeq:{{#time:Y-m-d|{{{date}}}}}|{{{date}}}|[[{{{date}}}]]|{{{date}}}}}) | {{#if: 2007 | {{#if: Oct | (Oct 2007) | (2007) }} }} |}} }}{{#if: | . }}{{ #if: | {{{editor}}}: }}{{#if: | {{#if: | {{#if: Safety Information about Lialda | [{{{archiveurl}}} Safety Information about Lialda] }}}} | {{#if: http://www.lialda.com/aboutLialda/sideEffect.asp | {{#if: Safety Information about Lialda | Safety Information about Lialda }}}} }}{{#if: | () }}{{#if: | ({{{language}}}) }}{{#if: Lialda Side Effects | . Lialda Side Effects }}{{#if: | {{{pages}}} }}{{#if: | . {{{publisher}}}{{#if: | | {{#if: 2007Oct || }} }} }}{{#if: ||{{#if: | ({{#ifeq:{{#time:Y-m-d|{{{date}}}}}|{{{date}}}|[[{{{date}}}]]|{{{date}}}}}) | {{#if: 2007 | {{#if: Oct | (Oct 2007) | (2007) }} }} }} }}.{{#if: | Archived from the original on [[{{{archivedate}}}]]. }}{{#if: | DOI:{{{doi}}}. }}{{#if: 2008-01-07 | Retrieved on 2008-01-07{{#if: | , [[{{{accessyear}}}]] }}. }}{{#if: | Retrieved on {{{accessmonthday}}}, {{{accessyear}}}. }}{{#if: | Retrieved on {{{accessdaymonth}}} {{{accessyear}}}. }}{{#if: |  “{{{quote}}}” }}

• British National Formulary 45 March 2003
• {{

 #if: 
 | {{
   #if: 
   | [[{{{authorlink}}}|{{
     #if: 
     | {{{last}}}{{ #if:  | , {{{first}}} }}
     | {{{author}}}
   }}]]
   | {{
     #if: 
     | {{{last}}}{{ #if:  | , {{{first}}} }}
     | {{{author}}}
   }}
 }}

}}{{

 #if: 
 | {{ #if:  | ; {{{coauthors}}} }}

}}{{

 #if: 
 |  [{{{origdate}}}]
 | {{
   #if: 
   | {{
     #if: 
     |  [{{{origmonth}}} {{{origyear}}}]
     |  [{{{origyear}}}]
   }}
 }}

}}{{

 #if: November 30, 2004
 |  (November 30, 2004)
 | {{
   #if: 
   | {{
     #if: 
     |  ({{{month}}} {{{year}}})
     |  ({{{year}}})
   }}
 }}

}}{{ #if: | . }}{{

 #if: 
 |  "{{
   #if: 
   | [{{{chapterurl}}} {{{chapter}}}]
   | {{{chapter}}}

}}",}}{{

 #if: Edited by Sean C. Sweetman
 |  in Edited by Sean C. Sweetman: 

}} {{

 #if:  | [{{{url}}} Martindale: The complete drug reference] | Martindale: The complete drug reference

}}{{

 #if:  |  ({{{format}}})

}}{{

 #if:  | , {{{others}}}

}}{{

 #if: 34th edition | , 34th edition

}}{{

 #if:  | , {{{series}}}

}}{{

 #if:  |  (in {{{language}}})

}}{{

 #if: Pharmaceutical Press
 | {{#if: 34th edition | ,  | .  }}{{ 
   #if: London 
   | London: 
 }}Pharmaceutical Press

}}{{

 #if:  | , {{{page}}}

}}{{

 #if:  | . DOI:{{{doi}}}

}}{{

 #if: ISBN 0-85369-550-4 | . ISBN 0-85369-550-4

}}{{

 #if:  | . ISBN {{{isbn}}}

}}{{

 #if:  | . OCLC {{{oclc}}}

}}{{

 #if:  | {{
 #if:  | 
 . Retrieved on [[{{{accessdate}}}]]
 | {{
   #if: 
   | . Retrieved {{
     #if: 
     | on [[{{{accessmonth}}} {{{accessyear}}}]]
     | during [[{{{accessyear}}}]]
 }}}}
 }}

}}.{{ #if: |  “{{{quote}}}” }} 

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.
• Asacol Official Site

Template:Antidiarrheals, intestinal anti-inflammatory/anti-infective agentsde:Mesalazin fr:Mésalazine hr:Mesalazin pl:Mesalazyna pt:Aminosalicilato