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The clinical investigator

, Volume 71, Issue 4, pp 286–289 | Cite as

Effect of olsalazine and mesalazine on human ileal and colonic (Na+ + K+)-ATPase

A possible diarrhogenic factor?
  • C. Scheurlen
  • H. Allgayer
  • W. Kruis
  • E. Erdmann
  • T. Sauerbruch
Original Article

Summary

Olsalazine (azodisalicylate) and mesalazine (5-aminosalicylic acid) have recently been developed as new treatment modalities for inflammatory bowel disease to avoid sulfasalazine-related side effects. However, there are reports regarding new and hitherto unexpected side effects in some patients receiving olsalazine or mesalazine, such as watery diarrhea. Since sodium pump activities play an important role in the pathogenesis of water and electrolyte disturbances, we investigated the influence of olsalazine and mesalazine on human ileal and colonic (Na+ + K+)-ATPase and its specific [3H]-ouabain binding. We found a concentration-dependent inhibition of ileal and colonic (Na+ + K+)-ATPase by olsalazine with an IC50 of 4.1 mM and 4.8 mM, respectively. Mesalazine inhibited this enzyme in the ileum with an IC50 of 4.5 mM and in the sigmoid colon with an IC50 3.5 mM. In addition, [3H]-ouabain binding was inhibited by mesalazine with an IC50 of 3.6 mM. The maximal inhibition, however, did not exceed 80% under any conditions (up to 10 mM drug concentration). Olsalazine and mesalazine induce inhibition of the ileal and colonic sodium pump activities that may (in addition to other possible mechanisms) mediate impaired water and electrolyte absorption. This is possibly of clinical relevance in patients with severely damaged mucosa. In patients with milder forms of mucosal inflammation, this inhibition most likely is of minor importance because of the great capacitiy of the (Na+ + K+)-ATPase and the incomplete inhibition leaving at least 20% of the enzyme activity intact.

Key words

(Na+ + K+)-ATPase Inflammatory bowel disease Diarrhea 5-Aminosalicyclic acid Olsalazine Mesalazine 

Abbreviations

5-ASA

5-aminosalicylic acid

EDTA

ethylenediaminetetracetic acid

IBD

inflammatory bowel disease

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Copyright information

© Springer-Verlag 1993

Authors and Affiliations

  • C. Scheurlen
    • 1
    • 5
  • H. Allgayer
    • 2
  • W. Kruis
    • 3
  • E. Erdmann
    • 4
  • T. Sauerbruch
    • 1
  1. 1.Allgemeine Innere Medizinische Klinik (Schwerpunkt Gastroenterologie-Hepatologie)Rheinische Friedrich-Wilhelms-UniversitätBonn
  2. 2.Medizinische Klinik, Städtisches Krankenhaus KarlsruheGermany
  3. 3.Abteilung für Innere Medizin, Evangelisches Krankenhaus Köln-KalkGermany
  4. 4.Medizinische Klinik I, Klinikum Gro\hadernLudwig-Maximilians-Universität MünchenGermany
  5. 5.Allgemeine Innere Medizin der RheinFriedrich-Wilhelm-Universität BonnBonn - VenusbergGermany

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