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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References
Azad Khan AK, Piris J, Truelove SC. An experiment to determine the active therapeutic moiety of sulphasalazine. Lancet 2: 892–895, 1977
Bax DE, Amos RS. Sulphasalazine: a safe, effective agent for prolonged control of rheumatoid arthritis. A comparison with sodium aurothiomalate. Annals of the Rheumatic Diseases 44: 194–198, 1985
Bickers DR, Hazen PG, Lynch WS (Eds). Clinical pharmacology of skin disease. Sulfones and sulphapyridine, Chapter 10, pp. 217–234, Churchill Livingstone, London, 1984
Bird HA, Rhind V, Leathern P, Saunders A, Wright V. Enteric-coated aspirin in rheumatoid arthritis. Rheumatology and Rehabilitation 20: 116–121, 1981
Bird HA, Dixon JS, Pickup ME, Rhind VM, Lowe JR, Lee MR, Wright V. A biochemical assessment of sulphasalazine in rheumatoid arthritis. Journal of Rheumatology 9: 36–45, 1982
Das KM, Eastwood MA, McManus JPA, Sircus W. Adverse reactions during salicylazosulfapyridine therapy and the relation with drug metabolism and acetylator phenotype. New England Journal of Medicine 289: 491–495, 1973
Das KM, Eastwood MA, McManus JPA, Sircus W. The role of the colon in the metabolism of salicylazosulphapyridine. Scandinavian Journal of Gastroenterology 9: 137–141, 1974
Dew MJ, Hughes P, Harries AD, Williams G, Evans BK, Rhodes J. Maintenance of remission in ulcerative colitis with oral preparation of 5-aminosalicylic acid. British Medical Journal 285: 1012, 1982
Dixon JS. Biochemical and clinical changes in rheumatoid arthritis: their relation to the action of antirheumatoid drugs. Seminars in Arthritis and Rheumatism 12: 191–207, 1982
Dixon JS, Bird HA, Pickup ME, Wright V. A human model system for the detection of specific antirheumatic activity. Seminars in Arthritis and Rheumatism 12: 185–190, 1982
Evans DAP. An improved and simplified method of detecting the acetylator phenotype. Journal of Medical Genetics 6: 405–407, 1969
Fischer C, Klotz U. High performance liquid Chromatographic determination of aminosalicylate, sulphapyridine and their metabolites. Journal of Chromatography 162: 237–243, 1979
McConkey B, Crockson RA, Crockson AP. The assessment of rheumatoid arthritis. A study based on measurements of the serum acute-phase reactants. Quarterly Journal of Medicine 162: 115–125, 1972
McConkey B, Amos RS, Butler EP, Crockson RA, Crockson AP. Walsh L. Salazopyrin in rheumatoid arthritis. Agents and Actions 8: 438–441, 1978
Misiewicz JJ, Lennard-Jones JE, Connell AM, Baron JH, Avery Jones F. Controlled trial of sulphasalazine in ulcerative colitis. Lancet 1: 185–188, 1965
Neumann VC, Grindulis K, Hubball S, McConkey B, Wright V. Comparison between penicillamine and sulphasalazine in rheumatoid arthritis: Leeds-Birmingham trial. British Medical Journal 287: 1099–1102, 1983
Olhagen B, Mansson I. Intestinal Clostridium perfringens in rheumatoid arthritis and other collagen diseases. Acta Medica Scandinavica 184: 395–402, 1968
Pullar T, Capell HA. Sulphasalazine: a ‘new’ antirheumatic drug. British Journal of Rheumatology 23: 26–34, 1984
Pullar T, Hunter JA, Capell HA. Sulphasalazine in rheumatoid arthritis: a double-blind comparison of sulphasalazine with placebo and sodium aurothiomalate. British Medical Journal 287: 1102–1104, 1983
Pullar T, Hunter JA, Capell HA. Which component of sulphasalazine is active in rheumatoid arthritis? British Medical Journal 290: 1535–1538, 1985
Schroder H, Campbell DES. Absorption, metabolism and excretion of salicylazosulfapyridine in man. Clinical Pharmacology and Therapeutics 13: 539–555, 1972
Shinebaum R, Neumann V, Wright V, Cooke EM. Comparison of faecal flora of patients with rheumatoid arthritis and controls. Journal of Medical Microbiology 18(3): Abstr. IV, 1984
Situnayake RD, McConkey B. Resin-coated 5-aminosalicylic acid (‘Asacol’) in rheumatoid arthritis. British Journal of Rheumatology 24: 226–227, 1985
Svartz N. Salazopyrin, a new sulfanilamide preparation. Acta Medica Scandinavica 60: 577–598, 1942
West B, Lendrum R, Hill MJ, Walker G. Effects of sulphasalazine (salazopyrin) on faecal flora in patients with inflammatory bowel disease. Gut 15: 960–965, 1974
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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