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. 1990 Aug;49(8):587–590. doi: 10.1136/ard.49.8.587

Comparison of the single dose pharmacokinetics of sulphasalazine in rheumatoid arthritis and inflammatory bowel disease.

C Astbury 1, A J Taggart 1, L Juby 1, L Zebouni 1, H A Bird 1
PMCID: PMC1004169  PMID: 1975737

Abstract

The pharmacokinetics of sulphasalazine and its principal metabolites in rheumatoid arthritis (RA) and inflammatory bowel disease (IBD) were compared. Patients with RA had a significantly greater concentration of plasma sulphapyridine than patients with IBD (medians 14.0 micrograms/ml and 7.4 micrograms/ml respectively). Patients with RA also tended to maintain a higher plasma sulphapyridine concentration with time, as determined by the area under the curve (AUC), but a lower plasma sulphasalazine AUC than patients with IBD. It is suggested that more sulphasalazine may be presented to the lower bowel for cleavage to sulphapyridine and 5-aminosalicylic acid in patients with RA than in IBD. Patients with RA may also have impaired metabolism of sulphapyridine as a consequence of their disease. Together these factors may contribute to higher peak circulating sulphapyridine concentrations and may be responsible for the higher incidence of side effects of sulphasalazine treatment in patients with RA than in patients with IBD.

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Selected References

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  1. Astbury C., Dixon J. S. Rapid method for the determination of either plasma sulphapyridine or sulphamethoxazole and their acetyl metabolites using high-performance liquid chromatography. J Chromatogr. 1987 Feb 20;414(1):223–227. doi: 10.1016/0378-4347(87)80045-2. [DOI] [PubMed] [Google Scholar]
  2. Ayesh R., Mitchell S. C., Waring R. H., Withrington R. H., Seifert M. H., Smith R. L. Sodium aurothiomalate toxicity and sulphoxidation capacity in rheumatoid arthritic patients. Br J Rheumatol. 1987 Jun;26(3):197–201. doi: 10.1093/rheumatology/26.3.197. [DOI] [PubMed] [Google Scholar]
  3. Azad Khan A. K., Howes D. T., Piris J., Truelove S. C. Optimum dose of sulphasalazine for maintenance treatment in ulcerative colitis. Gut. 1980 Mar;21(3):232–240. doi: 10.1136/gut.21.3.232. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Azad Khan A. K., Truelove S. C. Circulating levels of sulphasalazine and its metabolites and their relation to the clinical efficacy of the drug in ulcerative colitis. Gut. 1980 Aug;21(8):706–710. doi: 10.1136/gut.21.8.706. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Bax D. E., Amos R. S. Sulphasalazine: a safe, effective agent for prolonged control of rheumatoid arthritis. A comparison with sodium aurothiomalate. Ann Rheum Dis. 1985 Mar;44(3):194–198. doi: 10.1136/ard.44.3.194. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Bird H. A., Dixon J. S., Pickup M. E., Rhind V. M., Lowe J. R., Lee M. R., Wright V. A biochemical assessment of sulphasalazine in rheumatoid arthritis. J Rheumatol. 1982 Jan-Feb;9(1):36–45. [PubMed] [Google Scholar]
  7. Dinarello C. A. Biology of interleukin 1. FASEB J. 1988 Feb;2(2):108–115. [PubMed] [Google Scholar]
  8. Dissanayake A. S., Truelove S. C. A controlled therapeutic trial of long-term maintenance treatment of ulcerative colitis with sulphazalazine (Salazopyrin). Gut. 1973 Dec;14(12):923–926. doi: 10.1136/gut.14.12.923. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Farr M., Tunn E., Crockson A. P., Bacon P. A. The long term effects of sulphasalazine in the treatment of rheumatoid arthritis and a comparative study with penicillamine. Clin Rheumatol. 1984 Dec;3(4):473–481. doi: 10.1007/BF02031270. [DOI] [PubMed] [Google Scholar]
  10. Grindulis K. A., McConkey B. Outcome of attempts to treat rheumatoid arthritis with gold, penicillamine, sulphasalazine, or dapsone. Ann Rheum Dis. 1984 Jun;43(3):398–401. doi: 10.1136/ard.43.3.398. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Leden I., Hanson A., Melander A., Sturfelt G., Svensson B., Wàhlin-Boll E. Varying distribution of acetylation phenotypes in RA patients with and without Sjögren's syndrome. Scand J Rheumatol. 1981;10(3):253–255. doi: 10.3109/03009748109095308. [DOI] [PubMed] [Google Scholar]
  12. Madhok R., Capell H. A., Waring R. Does sulphoxidation state predict gold toxicity in rheumatoid arthritis? Br Med J (Clin Res Ed) 1987 Feb 21;294(6570):483–483. doi: 10.1136/bmj.294.6570.483. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. McConkey B., Amos R. S., Durham S., Forster P. J., Hubball S., Walsh L. Sulphasalazine in rheumatoid arthritis. Br Med J. 1980 Feb 16;280(6212):442–444. doi: 10.1136/bmj.280.6212.442. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Neumann V. C., Grindulis K. A., Hubball S., McConkey B., Wright V. Comparison between penicillamine and sulphasalazine in rheumatoid arthritis: Leeds-Birmingham trial. Br Med J (Clin Res Ed) 1983 Oct 15;287(6399):1099–1102. doi: 10.1136/bmj.287.6399.1099. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Panayi G. S., Huston G., Shah R. R., Mitchell S. C., Idle J. R., Smith R. L., Waring R. H. Deficient sulphoxidation status and D-penicillamine toxicity. Lancet. 1983 Feb 19;1(8321):414–414. doi: 10.1016/s0140-6736(83)91526-x. [DOI] [PubMed] [Google Scholar]
  16. Pinals R. S., Kaplan S. B., Lawson J. G., Hepburn B. Sulfasalazine in rheumatoid arthritis. A double-blind, placebo-controlled trial. Arthritis Rheum. 1986 Dec;29(12):1427–1434. doi: 10.1002/art.1780291202. [DOI] [PubMed] [Google Scholar]
  17. Pullar T., Hunter J. A., Capell H. A. Sulphasalazine in rheumatoid arthritis: a double blind comparison of sulphasalazine with placebo and sodium aurothiomalate. Br Med J (Clin Res Ed) 1983 Oct 15;287(6399):1102–1104. doi: 10.1136/bmj.287.6399.1102. [DOI] [PMC free article] [PubMed] [Google Scholar]
  18. Pullar T., Hunter J. A., Capell H. A. Sulphasalazine in the treatment of rheumatoid arthritis: relationship of dose and serum levels to efficacy. Br J Rheumatol. 1985 Aug;24(3):269–276. doi: 10.1093/rheumatology/24.3.269. [DOI] [PubMed] [Google Scholar]
  19. Schröder H., Campbell D. E. Absorption, metabolism, and excretion of salicylazosulfapyridine in man. Clin Pharmacol Ther. 1972 Jul-Aug;13(4):539–551. doi: 10.1002/cpt1972134539. [DOI] [PubMed] [Google Scholar]
  20. Schröder H., Evans D. A. Acetylator phenotype and adverse effects of sulphasalazine in healthy subjects. Gut. 1972 Apr;13(4):278–284. doi: 10.1136/gut.13.4.278. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Schröder H., Evans D. A. The polymorphic acetylation of sulphapyridine in man. J Med Genet. 1972 Jun;9(2):168–171. doi: 10.1136/jmg.9.2.168. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. van Hees P. A., Tuinte J. H., van Rossum J. M., van Tongeren J. H. Influence of intestinal transit time on azo-reduction of salicylazosulphapyridine (Salazopyrin). Gut. 1979 Apr;20(4):300–304. doi: 10.1136/gut.20.4.300. [DOI] [PMC free article] [PubMed] [Google Scholar]

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