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Aminosalicylates 5-aminosalicylic acid, mesalamine

Pharmacology Olsalazine sodium is a sodium salt of a salicylate compound that is effectively bioconverted to 5-aminosalicylic acid (mesalamine 5-ASA), which has anti-inflammatory activity in ulcerative colitis. Approximately 98% to 99% of an oral dose will reach the colon, where each molecule is rapidly converted into 2 molecules of 5-ASA by colonic bacteria. The liberated 5-ASA is absorbed slowly, resulting in very high local concentrations in the colon. [Pg.1425]

Sulfasalazine is a prodrug of which 70% is converted by colon bacteria to two active metabolites, sulfapyri-dine and 5-aminosalicylic acid (mesalamine). Sulfa-pyridine has antibacterial activities, and 5-aminosali-... [Pg.433]

Pharmacology Balsalazide is delivered intact to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalamine, which is the therapeutically active portion of the molecule and 4-aminobenzoyl- -alanine. The recommended dose of 6.75 g/day for the treatment of active disease provides 2.4 g of free 5-aminosalicylic acid (5-ASA) to the colon. [Pg.1426]

Drugs that contain 5-aminosalicylic acid (5-ASA) have been used successfully for decades in the treatment of inflammatory bowel diseases (Figure 62-8). 5-ASA differs from salicylic acid only by the addition of an amino group at the 5 (meta) position. Aminosalicylates are believed to work topically (not systemically) in areas of diseased gastrointestinal mucosa. Up to 80% of unformulated, aqueous 5-ASA is absorbed from the small intestine and does not reach the distal small bowel or colon in appreciable quantities. To overcome the rapid absorption of 5-ASA from the proximal small intestine, a number of formulations have been designed to deliver 5-ASA to various distal segments of the small bowel or the colon. These include sulfasalazine, olsalazine, balsalazide, and various forms of mesalamine. [Pg.1326]

The active ingredient in the rectal suspension enema, a disposable (60 mL) unit, is mesalamine, also known as 5-aminosalicylic acid. Each rectal suspension enema unit contains 4 g of mesalamine. In addition to mesalamine, the preparation contains the inactive ingredients carbomer 934P, edetate disodium, potassium acetate, potassium met-... [Pg.149]

Acetylsalicylic acid Angettes , Arthrisin , 5-Aminosalicylic acid see Mesalamine... [Pg.369]

Sulfasalazine, an agent that combines a sulfonamide (sulfapyridine) antibiotic and mesalamine (5-aminosalicylic acid) in the same molecule, has been used for many years to treat IBD. Mesalamine-based products are listed in Table 26-5. [Pg.286]

Chemical modification is also used to a limited extent to facilitate a dnig reaching its desired target (sec Chapter 3). An example is olsalazine. used in the treatment of ulcerative colitis. This drag is a dimer of (he pharmacologically active mesalamine (3-aminosalicylic acid). The latter is not effective orally because it is metabolized to inactive forms... [Pg.4]


See other pages where Aminosalicylates 5-aminosalicylic acid, mesalamine is mentioned: [Pg.608]    [Pg.138]    [Pg.1575]    [Pg.813]    [Pg.835]    [Pg.841]    [Pg.842]    [Pg.555]    [Pg.25]    [Pg.1422]    [Pg.176]    [Pg.374]    [Pg.657]    [Pg.416]    [Pg.416]    [Pg.660]   


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5-Aminosalicylate

Aminosalicylates

Mesalamine

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