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Aminosalicylic Acid

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H. A. Bird – One of the best experts on this subject based on the ideXlab platform.

  • Sulphasalazine, Sulphapyridine or 5-Aminosalicylic Acid—which is the Active Moiety in Rheumatoid Arthritis?
    Rheumatology, 1995
    Co-Authors: H. A. Bird

    Abstract:

    Sulphasalazine is cleaved into 5-Aminosalicylic Acid and sulphapyridine by colonic bacteria. The bulk of evidence favours sulphapyridine rather than 5-Aminosalicylic Acid as the active moiety (as well as the main producer of side-effects) though a therapeutic action from the 30% of sulphasalazine that is absorbed unaltered also cannot be excluded.

  • Sulphasalazine, sulphapyridine or 5-Aminosalicylic Acid–which is the active moiety in rheumatoid arthritis?
    British journal of rheumatology, 1995
    Co-Authors: H. A. Bird

    Abstract:

    Sulphasalazine is cleaved into 5-Aminosalicylic Acid and sulphapyridine by colonic bacteria. The bulk of evidence favours sulphapyridine rather than 5-Aminosalicylic Acid as the active moiety (as well as the main producer of side-effects) though a therapeutic action from the 30% of sulphasalazine that is absorbed unaltered also cannot be excluded.

Subrata Ghosh – One of the best experts on this subject based on the ideXlab platform.

  • Review article: mode of action and delivery of 5‐Aminosalicylic Acid – new evidence
    Alimentary Pharmacology & Therapeutics, 2006
    Co-Authors: Pierre Desreumaux, Subrata Ghosh

    Abstract:

    The effectiveness of sulfasalazine depends on the splitting of the diazo bond in the molecule by the action of bacteria in the large bowel, releasing the pharmacologically active moiety, 5-Aminosalicylic Acid. The development of pH-dependent, delayed-release formulations of 5-Aminosalicylic Acid abolished the toxicity associated with the sulfapyridine part of sulfasalazine. 5-Aminosalicylic Acid is now believed to act by activating a class of nuclear receptors involved in the control of inflammation, cell proliferation, apoptosis and metabolic function, the gamma form of peroxisome proliferator-activated receptors. These receptors are expressed at particularly high levels in colon epithelial cells, where their expression appears to be at least in part stimulated by gut bacteria. Other drugs known to act via peroxisome proliferator-activated receptor-gamma, such as rosiglitazone and the selective peroxisome proliferator-activated receptor-gamma ligand GW1929, can be displaced from their binding sites on the peroxisome proliferator-activated receptor-gamma molecule by 5-Aminosalicylic Acid at concentrations of 5-Aminosalicylic Acid that correspond with the concentrations found in the lumen of ulcerative colitis patients taking oral mesalazine. Genetically engineered heterozygous knockout mice (peroxisome proliferator-activated receptor-gamma+/-) are particularly susceptible to colonic inflammation, and inflammation is more severe in these mice, in response to chemicals that induce experimental colonic ulcers. In these experimental models, 5-Aminosalicylic Acid is ineffective in peroxisome proliferator-activated receptor-gamma+/- mice. This new insight provides a mechanistic foundation for the possibility that long-term treatment with 5-Aminosalicylic Acid can reduce the risk of colorectal cancer in patients with ulcerative colitis.

  • Review article: mode of action and delivery of 5-Aminosalicylic Acid – new evidence.
    Alimentary pharmacology & therapeutics, 2006
    Co-Authors: Pierre Desreumaux, Subrata Ghosh

    Abstract:

    The effectiveness of sulfasalazine depends on the splitting of the diazo bond in the molecule by the action of bacteria in the large bowel, releasing the pharmacologically active moiety, 5-Aminosalicylic Acid. The development of pH-dependent, delayed-release formulations of 5-Aminosalicylic Acid abolished the toxicity associated with the sulfapyridine part of sulfasalazine. 5-Aminosalicylic Acid is now believed to act by activating a class of nuclear receptors involved in the control of inflammation, cell proliferation, apoptosis and metabolic function, the gamma form of peroxisome proliferator-activated receptors. These receptors are expressed at particularly high levels in colon epithelial cells, where their expression appears to be at least in part stimulated by gut bacteria. Other drugs known to act via peroxisome proliferator-activated receptor-gamma, such as rosiglitazone and the selective peroxisome proliferator-activated receptor-gamma ligand GW1929, can be displaced from their binding sites on the peroxisome proliferator-activated receptor-gamma molecule by 5-Aminosalicylic Acid at concentrations of 5-Aminosalicylic Acid that correspond with the concentrations found in the lumen of ulcerative colitis patients taking oral mesalazine. Genetically engineered heterozygous knockout mice (peroxisome proliferator-activated receptor-gamma+/-) are particularly susceptible to colonic inflammation, and inflammation is more severe in these mice, in response to chemicals that induce experimental colonic ulcers. In these experimental models, 5-Aminosalicylic Acid is ineffective in peroxisome proliferator-activated receptor-gamma+/- mice. This new insight provides a mechanistic foundation for the possibility that long-term treatment with 5-Aminosalicylic Acid can reduce the risk of colorectal cancer in patients with ulcerative colitis.

Chaim M. Bell – One of the best experts on this subject based on the ideXlab platform.

  • Safety of topical 5-Aminosalicylic Acid in pregnancy.
    The American journal of gastroenterology, 1997
    Co-Authors: Chaim M. Bell

    Abstract:

    Objective: To assess the safety and efficacy of topical 5-Aminosalicylic Acid preparations for therapy of distal colitis during pregnancy. Methods: Nineteen pregnancies in sixteen consecutive patients with proven distal colitis were identified prospectively at a tertiary care center. All patients were given trials of weaning off medication and all failed. All subjects were on maintenance topical 5-Aminosalicylic Acid therapy at the time of conception. They were followed throughout their pregnancy and thereafter. Their children were also closely examined and followed by a pediatrician. Results: The mean age at delivery was 25.8 yr, and the mean duration of illness was 4.6 yr. After taking topical therapy, there were no relapses during the pregnancy. There were 19 successful full-term pregnancies with no fetal abnormalities. The mothers and children were followed for more than 6 months. Conclusion: In this series, topical 5-Aminosalicylic Acid appears safe, effective, and well tolerated in the management of pregnant patients with distal colitis.