Evolution of Olsalazine

Sc, Truelove

doi:10.3109/00365528809101538

Cited by 13 publications

(7 citation statements)

References 17 publications

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“…Reductive metabolism of these, and a range of 5-aminosalicylic acid pro-drugs used in the treatment of ulcerative colitis and inflammatory bowel conditions, is mediated largely by the gut microbiota. So, the therapeutic activity of compounds such as sulfasalazine19,20, olsalazine21, ipsalazide and balsalazide22 depends upon the release of aminosalicylic acid to treat the inflammation. This ability to perform reductive metabolism on azo dyes and nitropolycyclic aromatic hydrocarbons was shown for bacteria of the genera Clostridia and Eubacteria by Rafii and Cerniglia23.…”

Section: Direct Drug Metabolism By the Gut Microbiotamentioning

confidence: 99%

Gut microbiome interactions with drug metabolism, efficacy, and toxicity

Wilson

Nicholson

2017

Translational Research

486

327

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The gut microbiota have both direct and indirect effects on drug and xenobiotic metabolism and this can have consequences for both efficacy and toxicity. Indeed microbiome-driven drug metabolism is essential for the activation of certain prodrugs such as e.g., azo drugs such as prontosil and neoprontosil resulting in the release of sulphanilamide. In addition to providing a major source of reductive metabolizing capability the gut microbiota provide a suite of additional reactions including acetylation/deacylation decarboxylation, dehydroxylation, demethylation, dehalogenation and importantly, in the context of certain types of drug-related toxicity, conjugate hydrolysis reactions. In addition to direct effects the gut microbiota can affect drug metabolism and toxicity indirectly via e.g., the modulation of host drug metabolism and disposition and competition of bacterial-derived metabolites for xenobiotic metabolism pathways. And, of course, the therapeutic drugs themselves can have effects, both intended and unwanted, which can impact on the health and composition of the gut microbiota with unforeseen consequences.

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Section: Direct Drug Metabolism By the Gut Microbiotamentioning

confidence: 99%

Gut microbiome interactions with drug metabolism, efficacy, and toxicity

Wilson

Nicholson

2017

Translational Research

486

327

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“…Since it is a colonic disease that is treated by 5-ASA clinically, it is better to deliver 5-ASA directly to the diseased site. However instead of reaching the colon, free 5-ASA is absorbed in the upper small intestine after oral administration 66 . So it is a great idea to conjugate 5-ASA to a moiety which acts as a carrier to target it specifically to colon 23 .…”

Section: The Gut Microbial Enzyme Activitymentioning

confidence: 99%

The influence of the gut microbiota on the bioavailability of oral drugs

Zhang

Han

Huang

et al. 2021

Acta Pharmaceutica Sinica B

137

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Due to its safety, convenience, low cost and good compliance, oral administration attracts lots of attention. However, the efficacy of many oral drugs is limited to their unsatisfactory bioavailability in the gastrointestinal tract. One of the critical and most overlooked factors is the symbiotic gut microbiota that can modulate the bioavailability of oral drugs by participating in the biotransformation of oral drugs, influencing the drug transport process and altering some gastrointestinal properties. In this review, we summarized the existing research investigating the possible relationship between the gut microbiota and the bioavailability of oral drugs, which may provide great ideas and useful instructions for the design of novel drug delivery systems or the achievement of personalized medicine.

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“…2 The drug consists of two molecules of 5-aminosalicylic acid (5-ASA) joined by an azo bond that is split by bacterial azoreductase to release 5-ASA in the colon. 3 Olsalazine is now well established in the treatment of ulcerative colitis.…”

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confidence: 99%

Optimum dose of olsalazine for maintaining remission in ulcerative colitis.

Travis

Tysk

Silva

et al. 1994

Gut

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To evaluate the optimum dose of olsalazine for maintaining remission in ulcerative colitis, 198 patients in remission for more than three months were randomly assigned to receive 0.5 g, 1.0 g, or 2.0 g/day for 12 months. A dose-ranging effect was detected in the per protocol analysis, with remission rates of 60% (0.5 g), 70% (1.0 g), and 78% (2.0 g) (p=0.03, trend in proportions). The higher dose was most effective in patients with proctitis (90Gb remission on 2 g/day, p=0.03) or those in remission for less than 12 months before the trial (88% remission on 2 g/day, p=0.0006). There was little dose-ranging effect in patients with extensive colitis or those in remission for more than 12 months. Diarrhoea necessitated treatment withdrawal in 12%. The optimal dose of olsalazine for maintaining remission in ulcerative colitis is 1 g/day. For patients with proctitis or recent relapse, 2 g/day may be preferabJle, although the dose seems to be less important in patients with more extensive disease or those in long term remission.

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Evolution of Olsalazine

Cited by 13 publications

References 17 publications

Gut microbiome interactions with drug metabolism, efficacy, and toxicity

Gut microbiome interactions with drug metabolism, efficacy, and toxicity

The influence of the gut microbiota on the bioavailability of oral drugs

Optimum dose of olsalazine for maintaining remission in ulcerative colitis.

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