Drug Discovery pp 365-376 | Cite as


  • Robert A. Maxwell
  • Shohreh B. Eckhardt


Peptic ulcers are circumscribed lesions of the alimentary mucosa that penetrate through to its muscular layer. They occur most commonly in the proximal duodenum and also in the lesser curvature of the stomach. These ulcers are always associated with acid and pepsin secretion, and seem to result from a disturbance in the balance between the ulcerogenic potential of such secretions and the protective effects of mucus production, membrane barriers to the acid and pepsin, and the regeneration of mucosal cells (Stedman, 1982; Shearman and Finlayson, 1982; Berkow, 1982; Lampe, 1986). Venables et al. (1978) noted that 10% of the population is said to suffer peptic ulceration at some time in their lives.


Peptic Ulcer Peptic Ulcer Disease Gastric Acid Secretion Histamine Receptor Thio Ether 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Ash, A. S. F. and Schild, H. O.: Receptors mediating some actions of histamine. Br. J. Pharmacol. Chemother. 27:427–439, 1966.PubMedGoogle Scholar
  2. Berkow, R., ed.: The Merck Manual, 14th Ed., Merck Sharp & Dohme Research Laboratories, Rahway, NJ, 1982.Google Scholar
  3. Black, J., Gerskowitch, V. P., and Leff, P.: Reflections on the classification of histamine receptors, in Pharmacology of Histamine Receptors, C. R. Ganellin and M.E. Parsons, eds. pp. 1–9, Wright, PSG, Bristol, UK, 1982.Google Scholar
  4. Black, J.W., Duncan, W. A. M., Durant, C. J., Ganellin, C. R., and Parsons, E. M.: Definition and antagonism of histamine H2-receptors. Nature 236: 385–390, 1972.PubMedCrossRefGoogle Scholar
  5. Black, J.W., Duncan, W. A. M., Emmett, J. C., Ganellin, C. R., Hesselbo, T., Parsons, M. E.,and Wyllie, J.H.: Metiamide: An orally active histamine H2-receptor antagonist. Agents Actions 3:133–137, 1973.PubMedCrossRefGoogle Scholar
  6. Blackwood, W. S., Maudgal, D. P., Pickard, R. G., Lawrence, D., and Northfield, T. C: Cimetidine in duodenal ulcer: Controlled trial. Lancet 2:174–176, 1976.PubMedCrossRefGoogle Scholar
  7. Bodemar, G. and Walan, A.: Cimetidine in the treatment of active duodenal and prepyloric ulcers. Lancet 2:161–164, 1976.PubMedCrossRefGoogle Scholar
  8. Bradshaw, J., Brittain, R.T., Clitherow, J. W., Daly, M. J., Jack, D., Price, B. J., and Stables, R.: Ranitidine (AH 19065): A new potent, selective histamine H2-receptor antagonist. Br. J. Pharmacol. 66:464P, 1979.Google Scholar
  9. Brimblecombe, R. W., Duncan, W. A. M., Durant, G.J., Emmett, J. G, Ganellin, C. R., and Parsons, M. E.: Cimetidine: A non-thiourea H2-receptor antagonist.J. Int. Med. Res. 3:86–92, 1975a.Google Scholar
  10. Brimblecombe, R.W., Duncan, W. A. M., Durant, G. J., Ganellin, C. R., Parsons, M. E. and Black, J.W.: The pharmacology of cimetidine, a new histamine H2-receptor antagonist. Br. J. Pharmacol. 53:435,436,1975b.Google Scholar
  11. Brimblecombe, R. W., Duncan, W. A. M., Durant, G. J., Emmett, J. C., Ganellin, C. R., Leslie, G. B., and Parsons, M. E.: Characterization and development of cimetidine as a histamine H2-receptor antagonist. Gastroenterology, 74:339–347, 1978.PubMedGoogle Scholar
  12. Brogden, R. N., Heel, R. C., Speight, T. M., and Avery, G. S.: Cimetidine: A review of its pharmacological and therapeutic efficacy in peptic ulcer disease. Drugs 15:93–131, 1978.PubMedCrossRefGoogle Scholar
  13. Brogden, R. N., Carmine, A. A., Heel, R. C., Speight, T. M. and Avery, G. S.: Ranitidine: A review of its pharmacology and therapeutic use in peptic ulcer disease and other allied diseases. Drugs 24:267–303, 1982.PubMedCrossRefGoogle Scholar
  14. Burland, W. L., Duncan, W. A. M., Hesselbo, T., Mills, J. G., Sharpe, P. G, Haggie, S. J., and Wyllie, J. H.: Pharmacological evaluation of cimetidine, a new histamine H2-receptor antagonist, in healthy man. Br. J. Clin. Pharmacol. 2:481–486, 1975.PubMedCrossRefGoogle Scholar
  15. Code, G F.: Histamine and gastric secretion: A later look, 1955-1965. Fed. Proc. 24:1311–1321, 1965.PubMedGoogle Scholar
  16. Duncan, W. A. M. and Parsons, M. E.: Reminiscences of the development of cimetidine. Gastroenterology 78:620–625, 1980.PubMedGoogle Scholar
  17. Durant, G. J., Emmett, J. G, and Ganellin, G R.: Some chemical aspects of histamine H2-receptor antagonists, in International Symposium on Histamine H 2-Receptor Antagonists, C. J. Wood and M. A. Simkins, ed., pp. 13–21, SKF, London, 1973.Google Scholar
  18. Durant, G. J., Parsons, M. E., and Black, J.W.: Potential histamine H2-receptor antagonists. 2. Nαguanylhistamine. J. Med. Chem. 18:830–833, 1975.PubMedCrossRefGoogle Scholar
  19. Dyck, W. P.: Cimetidine in management of peptic ulcer disease, in Symposium on New Methods of Treatment of Gastrointestinal Disease. Surg. Clin. North Am. 59:863–867, 1979.PubMedGoogle Scholar
  20. Fleshier, B.: The impact of cimetidine on the treatment of acid-peptic disease. Primary Care 8:195–203, 1981.Google Scholar
  21. Forrest, J. A. H., Shearman, D. J. C., Spence, R., and Celestin, L. R.: Neutropenia associated with metiamide. Lancet 1:392,393,1975.PubMedCrossRefGoogle Scholar
  22. Ganellin, C. R.: Cimetidine, in Chronicles of Drug Discovery, J. S. Bindra and D. Lednicer, eds., pp. 1–38, Wiley, New York, 1982.Google Scholar
  23. Ganellin, C. R., Durant, G. J., and Emmett, J. C: Some chemical aspects of histamine H2-receptor antagonists. Fed. Proc. 35:1924–1930, 1976.PubMedGoogle Scholar
  24. Haggie, S. J., Fermont, D. C., and Wyllie, J. H.: Treatment of duodenal ulcer with cimetidine. Lancet 1:983,984,1976.PubMedCrossRefGoogle Scholar
  25. Hirschowitz, B.I.: H2histamine receptors. Annu. Rev. Pharmacol. Toxkol. 19: 203–244, 1979.CrossRefGoogle Scholar
  26. Lampe, K. F., ed.: Drug Evaluations, 6th Ed., American Medical Association, Chicago, 1986.Google Scholar
  27. Misiewicz, J. J.: Role of cimetidine in gastrointerestinal disease: Present status and future potential. Drugs 15:89–92, 1978.PubMedCrossRefGoogle Scholar
  28. Pounder, R. E., Williams, J. G., Milton-Thompson, G. J., and Misiewicz, J. J.: 24-Hour control of intragastric acidity by cimetidine in duodenal-ulcer patients. Lancet 2:1069–1072, 1975.PubMedCrossRefGoogle Scholar
  29. Pounder, R. E., Hunt, R. H., Stekelman, M., Milton-Thompson, G. J., and Misiewicz, J. J.: Healing of gastric ulcer during treatment with cimetidine. Lancet 1:337–339, 1976.PubMedCrossRefGoogle Scholar
  30. Richardson, C T. and Peterson, W. L.: New agents for peptic ulcer therapy. Drug Ther. 12:145–151, 1982.Google Scholar
  31. Rocha e Silva, M., ed.: Histamine and antihistamines, in Handbook of Experimental Pharmacology, vol. 18, Part 1, pp. 991, Springer-Verlag, New York, 1966.Google Scholar
  32. Shearman, D. J. C. and Finlayson, N. D. G: Diseases of the Gastrointestinal Tract and Liver, Churchill Livingstone, Edinburgh, 1982.Google Scholar
  33. Stedman’s Medical Dictionary, 24th Ed., Williams & Wilkins, Baltimore, 1982.Google Scholar
  34. Thjodleifsson, B. and Wormsley, K. G.: Aspects of the effect of metiamide on pentagastrin-stimulated and basal gastric secretion of acid and pepsin in man. Gut 16:501–508, 1975.PubMedCrossRefGoogle Scholar
  35. Thomas, J. M. and Misiewicz, G.: Histamine H2-receptor antagonists in the short-and long-term treatment of duodenal ulcer. Clin. Gasiroenterol.13: 501–542, 1984.Google Scholar
  36. Venables, C. W., Stephen, J. G., Blair, E. L., Reed, J. D., and Saunders, J. D.: Cimetidine in the treatment of duodenal ulceration and the relationship of this therapy to surgical management, in Cimetidine, The Westminster Hospital Symposium, C. Wastell and P. Lance, eds., pp. 13–27, Churchill Livingstone, London, 1978.Google Scholar
  37. Wyllie, J.H., Hesselbo, T., and Black, J.W.: Effects in man of histamine H2-receptor blockade by burimamide. Lancet 2:1117–1120, 1972.PubMedCrossRefGoogle Scholar
  38. Wyllie, J. H., Ealding, W. D. P., Hesselbo, T., and Black, J. W.: Inhibition of gastric secretion in man by metiamide: A new, orally active histamine H2-receptor antagonist. Gut 14:424, 1973.PubMedGoogle Scholar

Copyright information

© Springer Science+Business Media New York 1990

Authors and Affiliations

  • Robert A. Maxwell
    • 1
  • Shohreh B. Eckhardt
    • 2
  1. 1.The Wellcome Research Laboratories ResearchTriangle ParkUSA
  2. 2.University of Vermont College of MedicineBurlingtonUSA

Personalised recommendations