Aminosalicylates (under construction)

Aminosalicylates (5-aminosalicylate or 5-ASA drugs)

The anti-inflammatory action of these drugs is effective for inducing and maintaining remission in mild to moderate ulcerative colitis and other forms of inflammatory bowel disease and some forms of arthritis (e.g. rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, and juvenile idiopathic arthritis). They appear to work (at least in part) by inhibiting the production of pro-inflammatory mediators including prostaglandin, leukotriene, thromboxane and interleukin-1, thereby reducing the acute inflammatory response.

Sulfasalazine for treatment and maintenance of remission of acute mild/moderate and severe ulcerative colitis, active Crohn's disease and sometimes prescribed by clinical specialists for active rheumatoid arthritis. Sulfasalazine’s side-effects are largely caused by the sulfapyridine component of the molecule, so newer 5-ASA only drugs have been developed. These are not effective for rheumatoid arthritis, where the beneficial effects reside with the sulfapyridine component.

5-ASA only drug formulations are equally efficacious and safety is comparable.  The prescriber’s choice of oral 5-ASA drug will be driven by several factors including the indication (e.g. induction or maintenance of remission in ulcerative colitis), disease location, the patient’s preference and their ability to comply with the required dosing regimen, and availability of the drug.

Mesalazine is unconjugated 5-ASA, delivered orally for treatment and maintenance of remission in mild to moderate ulcerative colitis. Available in delayed- and controlled-release formulations which resist gastric breakdown, delivering the drug more effectively to the gut.

Balsalazide (PubChem CID 6335412) consists of one 5-ASA molecule linked to an inert unabsorbed carrier molecule. It is administered orally two to three times a day depending on which formulation is prescribed. Prescribed for treating acute attacks of mild/moderate ulcerative colitis, and maintenance of remission of ulcerative colitis.

Olsalazine (PubChem CID 6003770) is a dimerised 5-ASA prodrug administered orally twice daily for treatment and maintenance of remission of acute mild ulcerative colitis.