Mesalazine

Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease.<ref name=AHFS2019/> It is generally used for mildly to moderately severe disease.<ref name=AHFS2019/> It is taken by mouth or rectally.<ref name=AHFS2019/> The formulations which are taken by mouth appear to be similarly-effective.<ref name=BNF76/>

Common side-effects include headache, nausea, abdominal pain, and fever.<ref name=AHFS2019/> Serious side-effects may include pericarditis, liver problems, and kidney problems.<ref name=AHFS2019/><ref name=BNF76/> Use in pregnancy and breastfeeding appears safe.<ref name=BNF76/> In people with a sulfa allergy certain formulations may result in problems.<ref name=AHFS2019/> Mesalazine is an aminosalicylate and anti-inflammatory.<ref name=AHFS2019/><ref name=BNF76>Template:Cite book</ref> It works by direct contact with the intestines.<ref name=AHFS2019/>

Mesalazine was approved for medical use in the United States in 1987.<ref name=AHFS2019>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref name="Asacol FDA label">{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> It is on the World Health Organization's List of Essential Medicines.<ref name="WHO22nd">Template:Cite book</ref> It is available as a generic medication.<ref name=AHFS2019/><ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> In 2021, it was the 239th most commonly prescribed medication in the United States, with more than 1Template:Nbspmillion prescriptions.<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref>

Medical uses

Template:See also It is used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease (effective only in colonic diseases).<ref name=AHFS2019/>

In 2022 Germany introduced guidance to use mesalamine to treat acute uncomplicated diverticulitis.<ref>Template:Cite journal</ref>

Side-effects

Most often reported side-effects are gastrointestinal (GI) (but may also include headache), including: nausea, diarrhea, and abdominal pain.<ref name="Asacol SmPC" />

Very rarely, use of mesalazine has been associated with an exacerbation of the symptoms of colitis, Stevens Johnson syndrome, and erythema multiforme.<ref name="Asacol SmPC">{{#invoke:citation/CS1|citation |CitationClass=web }}</ref>

Pregnancy

There is no data on use in pregnant women, but the drug does cross the placenta and is excreted in breast milk. The drug should not be used in children under two years of age,<ref name="Asacol SmPC" /> people with kidney disease,<ref name="Asacol SmPC" /> or people who are allergic to aspirin.<ref name="Asacol SmPC" />

Chemistry

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.<ref>Template:Cite book</ref> It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.<ref>Template:Cite journal</ref> It is in the category of disease-modifying antirheumatic drugs (DMARDs) family of medications.<ref name=AHFS2016>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> It is unclear exactly how it works.<ref name=AHFS2016/> Mesalazine is claimed to be a PPAR-γ agonist.<ref>Template:Cite journal</ref>

Mechanism of action

Exact mechanism of mesalazine is unknown, but is speculated that mesalazine decreases synthesis of prostaglandin and leukotriene, modulating the inflammatory response derived from the cyclooxygenase and lipooxygenase pathways.<ref>Template:Cite book</ref> It appears to act locally on colonic mucosa.<ref>Template:Cite journal</ref>

Society and culture

Brand names

Mesalazine is sold under various names including Apriso, Asacol, Asacol HD, Canasa, Delzicol, Fivasa, Lialda, Salofalk, Pentasa, Rowasa, Octasa, and Sfrowasa. In Europe, it is sold under the name Salofalk (rectal suppository). <ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref>