Pharmacodynamics of Acarbose: Clinical Investigations

  • B. Lembcke
Conference paper


The pharmacodynamics of the microbial α-glucosidase inhibitor acarbose (Fig. 1) (BAY g 5421; Glucobay) have been investigated in a large number of clinical studies. Several of these have already been reported on at the first international symposium on acarbose (Creutzfeldt 1982), others have been carried out more recently. Both theoretical and practical aspects of the pharmacodynamics of acarbose have been investigated in volunteers and diabetics, the number of studies of theoretical aspects decreasing with time and of practical aspects increasing with time.


Gastric Inhibitory Polypeptide Postprandial Blood Glucose Maltase Activity Small Bowel Transit Time Enteroinsular Axis 
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  1. Anderson IH, Levine AS, Levitt MD (1981) Incomplete absorption of the carbohydrate in allpurpose wheat flour. N Engl J Med 304:891–892PubMedCrossRefGoogle Scholar
  2. Bedine MS, Bayless TM (1973) Intolerance of small amounts of lactose by individuals with low lactase levels. Gastroenterology 65:735–743PubMedGoogle Scholar
  3. Caspary WF (1978) Sucrose malabsorption in man after ingestion of α-glucosidase-hydrolase inhibitor. Lancet ii: 1231–1233CrossRefGoogle Scholar
  4. Caspary WF, Graf S (1979) Inhibition of human intestinal α-glucosidehydrolases by a new complex oligosaccharide. Res Exp Med 75:1–6CrossRefGoogle Scholar
  5. Caspary WF, Kalisch H (1978) Effect of α-glucosidehydrolase inhibition on intestinal absorption of sucrose, water, and sodium in man. Gut 20:750–755CrossRefGoogle Scholar
  6. Christopher NL, Bayless TM (1971) Role of the small bowel and colon in lactose-induced diarrhea. Gastroenterology 60:845–852PubMedGoogle Scholar
  7. Creutzfeldt W (ed) (1982) First international symposium on acarbose. Excerpta Medica, AmsterdamGoogle Scholar
  8. Creutzfeldt W, Ebert R (1986) The enteroinsular axis. In: Go VLW, Gardner JP, DiMagno EP, Scheele GA (eds) The exocrine pancreas: biology, pathobiology, and diseases. Raven, New York, pp 279–286Google Scholar
  9. DeFronzo R, Ferrannini E, Hendler R, Wahren J, Felig P (1978) Influence of hyperinsulinaemia, hyperglycemia, and the route of glucose administration on splanchnic glucose exchange. Proc Natl Acad Sci USA 75:5173–5177PubMedCrossRefGoogle Scholar
  10. Dimitriadis G, Tessari P, Go V, Gerich J (1982) Effects of the disaccharidase inhibitor acarbose on meal and intravenous glucose tolerance in normal man. Metabolism 31:841–843PubMedCrossRefGoogle Scholar
  11. Fölsch UR, Ebert R, Creutzfeldt W (1981) Response of serum levels of gastric inhibitory polypeptide and insulin to sucrose ingestion during long-term application of acarbose. Scand J Gastroenterol 16:629–632PubMedCrossRefGoogle Scholar
  12. Fölsch UR, Lembcke B, Börger D, v Baumbach A, Kirchhoff S, Creutzfeldt W (1987) Dosisvergleich zwischen den α-Glukosidaseinhibitoren BAYg5421 (Acarbose) und BAYml099 (Miglitol) nach wiederholter Stärke- oder Saccharosebelastung (Abstract). Aktuel Endokrinol Stoffw 8:77Google Scholar
  13. Gerard J, Jandrain B, Pirnay F, Pallikarakis N, Krzentowski G, Lacroix M, Mosora F, Luyckx AS, Lefebvre PJ (1986) Utilization of oral sucrose load during exercise in humans. Effect of the α-glucosidase inhibitor acarbose. Diabetes 35:1294–1301PubMedCrossRefGoogle Scholar
  14. Groop P-H, Groop L, Tötterman KJ, Fyhrquist F (1986) Effects of acarbose on the relationship between changes in GIP and insulin responses to meals in normal subjects. Acta Endocrinol 112:361–366PubMedGoogle Scholar
  15. Hagel HJ, Ruppin H, Pichel J, Feuerbach W, Bloom S, Domschke W (1985) Mode of action of the α-glucosidase inhibitor acarbose (BAY g 5421) in the small bowel. A perfusion study in man (Abstract). Diabetes Res Clin Pract Suppl 1:215Google Scholar
  16. Hayakawa T, Noda A, Kondo T, Okumura N (1984) Effects of acarbose, an α-glucosidase inhibitor (BAY g 5421), on orally loaded glucose, maltose and sucrose and on blood glucose control in non-insulin-dependent diabetics. Nagoya J Med Sci 47:35–41Google Scholar
  17. Hillebrand I, Boehme K, Frank G, Fink H, Berchtold P (1979 a) The effects of the α-glucosidase inhibitor BAY g 5 421 (Acarbose) on meal-stimulated elevations of circulating glucose, insulin, and triglyceride levels in man. Res Exp Med (Berl) 175:81–86CrossRefGoogle Scholar
  18. Hillebrand I, Boehme K, Frank G, Fink H, Berchtold P (1979b) The effects of the α-glucosidase inhibitor BAY g 5 421 (Acarbose) on postprandial blood glucose, serum insulin and triglyceride levels: dose-time-response relationships in man. Res Exp Med (Berl) 175:87–94CrossRefGoogle Scholar
  19. Homma Y, Irie N, Yano Y, Nakaya N, Goto Y (1982) Changes in plasma lipoprotein levels during medication with a glucoside-hydrolase inhibitor (acarbose). Tokai J Exp Clin Med 7:393–396PubMedGoogle Scholar
  20. Jain NK, Rosenberg DB, Ulahannan MJ, Glasser MJ, Pitchumoni CS (1985) Sorbitol intolerance in adults. Am J Gastroenterol 80:678–681PubMedGoogle Scholar
  21. Jandrain B, Gerard J, Verdin E, Luyckx AS, Lefebvre PJ (1985) Effect of acarbose on the hormonal and metabolic response to the simultaneous ingestion of sucrose and ethanol (Abstract). Diabetes Res Clin Pract Suppl 1:267Google Scholar
  22. Jenkins DJA, Taylor RH, Goff DV, Fielden H, Misiewicz JJ, Sarson DL, Bloom SR, Alberti KGMM (1981) Scope and specificity of acarbose in slowing carbohydrate absorption in man. Diabetes 30:951–954PubMedCrossRefGoogle Scholar
  23. Ladas S, Papanikos J, Arapakis G (1982) Lactose malabsorption in greek adults: correlation of small bowel transit time with the severity of lactose intolerance. Gut 23:968–973PubMedCrossRefGoogle Scholar
  24. Lebovitz HE (1987) Type II diabetes mellitus: a treatment dilemma. Am J Med 83 (Suppl 3A): 1–2PubMedCrossRefGoogle Scholar
  25. Lembcke B (1982) Physiologie und Pathophysiologie des Dünn- und Dickdarmes. Ernährungsumschau 29:457–465Google Scholar
  26. Lembcke B (1987) Untersuchungen zur medikamentösen Beeinflussung der intestinalen Kohlenhy-dratassimilation. Ein Beitrag zum Therapieprinzip Resorptionsverzögerung. Habilitationsschrift, Georg-August-University GöttingenGoogle Scholar
  27. Lembcke B, Caspary WF (1983) Atemanalytische Funktionstests. In: Caspary WF (ed) Handbuch der Inneren Medizin, vol 3/3A, Dünndarm. Springer, Berlin Heidelberg New York, pp 488–520Google Scholar
  28. Levitt MD (1983) Malabsorption of starch: a normal phenomenon (Editorial). Gastroenterology 85:769–770PubMedGoogle Scholar
  29. Puls W (1980) Zur Inhibition intestinaler Glukosidasen — Ein neues Prinzip zur Prävention und Therapie von kohlenhydratabhängigen Stoffwechselerkrankungen. Habilitationsschrift, University of DüsseldorfGoogle Scholar
  30. Puls W, Keup U, Krause HP, Thomas G, Hoffmeister F (1977) Glucosidase inhibition. A new approach to the treatment of diabetese, obesity, and hyperlipoproetinaemia. Naturwissenschaften 64:536PubMedCrossRefGoogle Scholar
  31. Radziuk J, Kemmer F, Morishima T, Berchtold P, Vranic M (1984) The effects of an alpha-glucoside hydrolase inhibitor on glycemia and the absorption of sucrose in man determined using a tracer method. Diabetes 33:207–213PubMedCrossRefGoogle Scholar
  32. Raptis S, Dimitriadis G, Etzrodt H, Karaiskos C, Hadjidakis D, Rosenthal J, Zoupas C, Diamantopoulos E (1982) The effects of acarbose treatment on release of pancreatic and gastro-intestinal hormones in man. In: Creutzfeldt W (ed) First international symposium on acarbose. Excerpta Medica, Amsterdam, pp 210–215Google Scholar
  33. Rating D, Gryzewski N, Burger W, Kneer J, Weber B, Helge H (1982) The modification of sucrose absorption by acarbose. In: Creutzfeldt W (ed) First international symposium on acarbose. Excerpta Medica, Amsterdam, pp 252–257Google Scholar
  34. Ravich WJ, Bayless TM, Thomas M (1983) Fructose: incomplete intestinal absorption in humans. Gastroenterology 84:26–29PubMedGoogle Scholar
  35. Suehiro I, Otsuki M, Yamasaki T, Ohki A, Sakamoto C, Yuu H, Maeda M, Baba S (1981) Effect of α-glucosidase inhibitor on human pancreatic and salivary amylase. Clin Chim Acta 117:145–152PubMedCrossRefGoogle Scholar
  36. Taylor RH, Jenkins DJA, Barker HM, Fielden H, Goff DV, Misiewicz JJ, Lee DA, Brian Allen H, MacDonald G, Wallrabe H (1982) Effect of acarbose on the 24-hour blood glucose profile and pattern of carbohydrate absorption. Diabetes Care 5:92–96PubMedCrossRefGoogle Scholar
  37. Uttenthal LO, Ukponmwan OO, Ghiglione M, Bloom SR (1987) Acute and short term effect of intestinal alpha-glucosidase inhibition on gut hormone responses in man. Dig Dis Sci 32:139–144PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1988

Authors and Affiliations

  • B. Lembcke
    • 1
  1. 1.Division of GastroenterologyCentre of Internal Medicine Johann-Wolfgang-Goethe-UniversitätFrankfurt 70Germany

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