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Diseases of the Colon & Rectum

, Volume 39, Issue 7, pp 788–793 | Cite as

Distribution and concentrations of 5-aminosalicylic acid in rectosigmoid biopsy specimens after rectal administration

  • R. Schoonjans
  • M. De Vos
  • A. -M. Schelfhout
  • M. Praet
  • A. Elewaut
Original Contributions

Abstract

PURPOSE: Using the autofluorescent properties of 5-aminosalicylic acid (5-ASA), we studied the penetration and distribution of this molecule in human colonic biopsies at different time intervals after administration of 5-ASA enemas. METHODS: Fluorescence scores of rectosigmoidal biopsy specimens were compared with 5-ASA and acetyl-5-aminosalicylic (Ac-5-ASA) concentrations, determined by high-performance liquid chromatography, in adjacent biopsies and in serum samples. RESULTS: 5-ASA penetrates into the rectal mucosa and into the epithelial cells after local application by means of an enema. We found a characteristic 5-ASA staining of two intramucosal structures that need further identification: intraepithelial triangular configurations and “5-ASA scavengers” in the lamina propria. Fluorescence scores correlate well with 5-ASA concentrations in adjacent biopsies (r=0.67;P<0.005) and correlate even better with serum concentrations of 5-ASA (r=0.84;P<0.005) and Ac-5-ASA (r=0.80;P<0.005), hence reflecting the amount of systemically absorbed and metabolized 5-ASA. CONCLUSION: 5-ASA penetrates into the rectal mucosa after local application. Local availability, assessed by means of fluorescence microscopy, correlates well with serum concentrations.

Key words

5-Aminosalicylic acid Enema Autofluorescence Rectosigmoid 

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References

  1. 1.
    Azad Khan AK, Piris J, Truelove SC. An experiment to determine the active moiety of sulphasalazine. Lancet 1977;2:892–5.PubMedGoogle Scholar
  2. 2.
    Van Hees PA, Bakker JH, Van Tongeren JH. Effect of sulphapyridine, 5-amino-salicylic acid and placebo in patients with idiopathic proctitis: a study to determine the active therapeutic moiety of sulphasalazine. Gut 1980;21:632–5.PubMedGoogle Scholar
  3. 3.
    Sutherland LR, Martin F, Greer S,et al. 5-Aminosalicylic acid enema in the treatment of distal ulcerative colitis, proctosigmoiditis and proctitis. Gastroenterology 1987;92:1894–8.PubMedGoogle Scholar
  4. 4.
    Klotz U, Maier K, Fischer C, Heinkel K. Therapeutic efficacy of sulfasalazine and its metabolites in patients with ulcerative colitis and Crohn's disease. N Engl J Med 1980;303:1499–502.CrossRefPubMedGoogle Scholar
  5. 5.
    De Vos M, Verdievel H, Schoonjans R, Beke R, De Weerdt GA, Barbier F. High-performance liquid chromatographic assay for the determination of 5-aminosalicylic acid and acetyl-5-amino-salicylic acid concentrations in endoscopic intestinal biopsy in humans. J Chromatog 1991;564:296–302.Google Scholar
  6. 6.
    De Vos M, Verdievel H, Schoonjans R, Praet M, Bogaert M, Barbier F. Concentrations of 5-ASA and Ac-5-ASA in human ileocolonic biopsy homogenates after the intake of oral 5-ASA preparations. Gut 1992;33:1338–42.PubMedGoogle Scholar
  7. 7.
    Ireland A, Priddle JD, Jewell DP. Acetylation of 5-aminosalicylic acid by isolated human colonic epithelial cells. Clinical Science 1990;78:105–11.PubMedGoogle Scholar
  8. 8.
    Allgayer H, Ahnfelt NO, Kruis W,et al. ColonicN-acetylation of 5-aminosalicylic acid in inflammatory bowel disease. Gastroenterology 1989;97:38–41.PubMedGoogle Scholar
  9. 9.
    Ireland A, Priddle JD, Jewell DP. Comparison of 5-aminosalicylic acid and N-acetyl aminosalicylic acid uptake by the isolated human colonic epithelial cell. Gut 1992;33:1343–7.PubMedGoogle Scholar
  10. 10.
    Pullman WE, Elsbury S, Kobayashi M, Hapel AJ, Doe WF. Enhanced mucosal cytokine production in inflammatory bowel disease. Gastroenterology 1992;102:529–37.PubMedGoogle Scholar
  11. 11.
    Greenfield SM, Hamblin AS, Punchard NA, Thompson RP. 5-amino-salicylic acid inhibits tumour necrosis factor α (TNFα) induced adhesion molecule upregulation on monocytes and granulocytes. Gastroenterology 1992;102:A632.Google Scholar
  12. 12.
    Jacobsen BA, Abildgaard K, Rasmussen HH,et al. Availability of mesalazine(5-aminosalicylic acid) from enemas and suppositories during steady-state conditions. Scand J Gastroenterol 1991;26:374–8.PubMedGoogle Scholar

Copyright information

© American Society of Colon and Rectal Surgeons 1996

Authors and Affiliations

  • R. Schoonjans
    • 1
  • M. De Vos
    • 1
  • A. -M. Schelfhout
    • 1
  • M. Praet
    • 1
  • A. Elewaut
    • 1
  1. 1.Departments of Gastroenterology and PathologyUniversity Hospital GentGentBelgium

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