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5-Aminosalicylic Acid or Sulphapyridine

Which is the Active Moiety of Sulphasalazine in Rheumatoid Arthritis?

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Summary

Thirty patients with active rheumatoid arthritis participated in an open study of 6 months’ treatment with either 5-aminosalicylic acid or sulphapyridine, the two moieties of sulphasalazine. Patients were assessed at regular intervals using a number of clinical and biochemical tests designed to detect specific antirheumatic activity.

Patients taking sulphasalazine showed significant improvement in most parameters of disease activity, but those taking 5-aminosalicylic acid did not improve despite the fact that high serum concentrations of 5-aminosalicylic acid and acetyl 5-aminosalicylic acid were achieved. These results suggest that sulphapyridine is the active moiety of sulphasalazine. Its possible mode of action is discussed.

Nausea was a frequent problem in patients taking sulphapyridine. Unless this problem can be overcome, sulphapyridine is unlikely to offer any therapeutic advantages over sulphasalazine in the treatment of rheumatoid arthritis.

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Enteric-coated sulphasalazine was used in this study; marketed by Pharmacia Ltd as Salazopyrin® EN-tabs, Azulfidine® EN-tabs® (USA), Azulfidine RA® (Germany).

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Taggart, A.J., Neumann, V.C., Hill, J. et al. 5-Aminosalicylic Acid or Sulphapyridine. Drugs 32 (Suppl 1), 27–34 (1986). https://doi.org/10.2165/00003495-198600321-00006

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  • DOI: https://doi.org/10.2165/00003495-198600321-00006

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