The Role of Alpha-Glucosidase Inhibitors (Acarbose)

  • Markolf Hanefeld
  • Frank Schaper

Keywords: acarbose, pharmacology, diabetes, metabolic syndrome, primary prevention, cardiovascular disease.


Postprandial Glucose Postprandial Hyperglycemia Gastric Inhibitory Polypeptide Oral Antidiabetic Insulin Secretagogue 
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. 1.
    Wallander M, Bartnik M, Efendic S et al. Beta cell dysfunction in patients with acute myocardial infarction but without previously known type 2 diabetes: a report from the GAMI study. Diabetologia 2005;48(11):2229–2235.CrossRefPubMedGoogle Scholar
  2. 2.
    Hanefeld M, Fischer S, Julius U et al. Risk factors for myocardial infarction and death in newly detected NIDDM: The Diabetes Intervention Study, 11 years follow-up. Diabetologia 1996;39(12):1577–1583.CrossRefPubMedGoogle Scholar
  3. 3.
    Ceriello A, Hanefeld M, Leiter L et al. Postprandial glucose regulation and diabetic complications. Arch Intern Med 2004;164(19):2090–2095.CrossRefPubMedGoogle Scholar
  4. 4.
    Burchfiel CM, Curb JD, Rodriguez BL et al. Glucose intolerance and 22-year stroke incidence. The Honolulu Heart Program. Stroke 1994;25(5): 951–957.PubMedGoogle Scholar
  5. 5.
    DECODE Study Group, European Diabetes Epidemiology Group. Is the current definition for diabetes relevant to mortality risk from all causes and cardiovascular and noncardiovascular diseases? Diabetes Care 2003;26(3):688–696.CrossRefGoogle Scholar
  6. 6.
    Kawano H, Motoyama T, Hirashima O et al. Hyperglycemia rapidly suppresses flow-mediated endothelium-dependent vasodilation of brachial artery. J Am Coll Cardiol 1999;34(1):146–154.CrossRefPubMedGoogle Scholar
  7. 7.
    Scognamiglio R, Negut C, De Kreutzenberg SV et al. Postprandial myocardial perfusion in healthy subjects and in type 2 diabetic patients. Circulation 2005; 112(2):179–184.CrossRefPubMedGoogle Scholar
  8. 8.
    Rudofsky G, Reismann P, Schiekofer S et al. Reduction of postprandial hyperglycemia in patients with type 2 diabetes reduces NF-kB activation in PBMCs. Horm Met Res 2004;36:630–638.CrossRefGoogle Scholar
  9. 9.
    Monnier L, Mas E, Ginet C et al. Activation of oxidative stress by acute glucose fluctuations compared with sustained chronic hyperglycemia in patients with type 2 diabetes. JAMA 2006;295(14):1681–1687.CrossRefPubMedGoogle Scholar
  10. 10.
    Woerle HJ, Szoke E, Meyer C et al. Mechanisms for abnormal postprandial glucose metabolism in type 2 diabetes. Am J Physiol Endocrinol Metab 2006; 290(1):E67–E77.CrossRefPubMedGoogle Scholar
  11. 11.
    Coutinho M, Gerstein HC, Wang Y et al. The relationship between glucose and incident cardiovascular events. A meta-regression analysis of published data from 20 studies of 95, 783 individuals followed for 12.4 years. Diabetes Care 1999;22(2):233–240.CrossRefPubMedGoogle Scholar
  12. 12.
    UK Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulfonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 1998; 352:837–853.CrossRefGoogle Scholar
  13. 13.
    Kahn SE, Haffner SM, Heise MA et al. Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med 2006;355(23):2427–2443.CrossRefPubMedGoogle Scholar
  14. 14.
    Salsburg DS. The UGDP study. JAMA 1971;218(11):1704–1705.CrossRefPubMedGoogle Scholar
  15. 15.
    Goke B, Herrmann C, Goke R et al. Intestinal effects of alpha-glucosidase inhibitors: absorption of nutrients and enterohormonal changes. Eur J Clin Invest 1994;24(Suppl 3):25–30.PubMedGoogle Scholar
  16. 16.
    Puls W. Pharmacology of glucosidase inhibitors. Oral Antidiabetics. Berlin: Springer, 1996;119:497–525.Google Scholar
  17. 17.
    Puls W, Keup U, Krause HP et al. Glucosidase inhibition. A new approach to the treatment of diabetes, obesity and hyperlipoproteinemia. Naturwissenschaften 1977;64:536–537.CrossRefPubMedGoogle Scholar
  18. 18.
    Schmidt DD, Frommer W, Junge B et al. Alpha-glucosidase inhibitors. New complex oligosaccharides of microbial origin. Naturwissenschaften 1977;64: 535–536.CrossRefPubMedGoogle Scholar
  19. 19.
    Krause HP, Ahr HJ. Pharmacokinetics and metabolism of glucosidase inhibitors. In: Kuhlmann J, Puls W, editors. Handbook of Experimental Pharma–cology: Oral Antidiabetics. Vol. 119. Berlin: Springer, 1996;541–545.Google Scholar
  20. 20.
    Junge B, Matzke M, Stoltefuss J. Chemistry and structure–activity relationships of glucosidase inhibitors. In: Kuhlmann J, Puls W, editors. Handbook of Experimental Pharmacology: Oral Antidiabetics. Vol. 119. Berlin: Springer, 1996;541–545.Google Scholar
  21. 21.
    Joubert PH, Venter HL, Foukaridis GN. The effect of miglitol and acarbose after an oral glucose load: a novel hypoglycaemic mechanism. Br J Clin Pharmacol 1990;30:391–396.PubMedGoogle Scholar
  22. 22.
    Toeller M. Modulation of intestinal glucose absorption: postponement of glucose absorption by alpha-glucosidase inhibitors. In: Mogensen CE, Standl E, editors. Pharmacology of Diabetes. Berlin: De Gruyter, 1991;93–112.Google Scholar
  23. 23.
    Meneilly G, Ryan EA, Radziuk J et al. Effect of acarbose on insulin sensitivity in elderly patients with diabetes. Diabetes Care 2000;23:1162–1167.CrossRefPubMedGoogle Scholar
  24. 24.
    Hillebrand I, Boehme K, Frank G et al. Effects of the glycoside hydrolase inhibitor (BAY g 5421) on post-prandial blood glucose, serum insulin and triglycerides levels in man. In: Creutzfeldt W, editor. Frontiers of Hormone Research, the Entero-insular Axis. Basel: Karger, 1979;7:290–291.Google Scholar
  25. 25.
    Hanefeld M, Fischer S, Schulze J et al. Therapeutic potentials of acarbose as first-line drug in NIDDM insufficiently treated with diet alone. Diabetes Care 1991;14:732–737.CrossRefPubMedGoogle Scholar
  26. 26.
    Chiasson JL, Josse RG, Leiter LA et al. The effect of acarbose on insulin sensitivity in subjects with impaired glucose tolerance. Diabetes Care 1996;19:1190–1193.CrossRefPubMedGoogle Scholar
  27. 27.
    Laube H, Linn T, Heyen P. The effects of acarbose on insulin sensitivity and proinsulin in overweight subjects with impaired glucose tolerance. Exp Clin Endocrinol Diabetes 1998;106:231–233.CrossRefPubMedGoogle Scholar
  28. 28.
    Hanefeld M, Haffner SM, Menschikowski M et al. Different effects of acarbose and glibenclamide on proinsulin and insulin profiles in people with type 2 diabetes. Diabetes Res Clin Pract 2002;55:221–227.CrossRefPubMedGoogle Scholar
  29. 29.
    Chiasson JL, Josse RG, Gomis R et al. Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised trial. Lancet 2002;359(9323): 2072–2077.CrossRefPubMedGoogle Scholar
  30. 30.
    Goke B, Fuder H, Wieckhorst G et al. Voglibose is an efficient alpha-glucosidase inhibitor and mobilize the endogenous GLP-1 reserve. Digestion 1995;56: 493–501.CrossRefPubMedGoogle Scholar
  31. 31.
    Qualmann C, Nauck MA, Hoist JJ et al. Glucagon-like peptide 1 (GLP-1) [17–36 amide] secretion in response to luminal sucrose from the upper and lower gut: a study using a-glucosidase inhibition (acarbose). Scand J Gastroenterol 1995;30:892–896.CrossRefPubMedGoogle Scholar
  32. 32.
    Holman RR, Turner RC, Cull CA et al. A randomised double-blind trial of acarbose in type 2 diabetes shows improved glycemic control over 3 years (UK Prospective Diabetes Study 44). Diabetes Care 1999;22:960–964.CrossRefPubMedGoogle Scholar
  33. 33.
    Wolever TMS, Chiasson JL, Josse RG et al. Small weight loss on long-term acarbose therapy with no change in dietary pattern or nutrient intake of individuals with non-insulin-dependent diabetes. Int J Obes Relat Metab Disord 1997;21:756–763.CrossRefPubMedGoogle Scholar
  34. 34.
    Lindström J, Tuomilehto J, Spengler M. Acarbose treatment does not change the habitual diet of patients with type 2 diabetes mellitus. The Finnish Acarbose Study Group. Diabet Med 2000;17(1):20–25.CrossRefPubMedGoogle Scholar
  35. 35.
    Rosenthal JH, Mauersberger H. Effects on blood pressure of the alpha-glucosidase inhibitor acarbose compared with the insulin enhancer glibenclamide in patients with hypertension and type 2 diabetes mellitus. Clin Drug Invest 2002;22(10):695–701.CrossRefGoogle Scholar
  36. 36.
    Hanefeld M, Cagatay M, Petrowitsch T et al. Acarbose reduces the risk for myocardial infarction in type 2 diabetic patients: meta-analysis of seven long-term studies. Eur Heart J 2004;25(1):10–16.CrossRefPubMedGoogle Scholar
  37. 37.
    Wascher TC, Schmoelzer I, Wiegratz A et al. Reduction of postchallenge hyperglycaemia prevents acute endothelial dysfunction in subjects with impaired glucose tolerance. Eur J Clin Invest 2005;35(9):551–557.CrossRefPubMedGoogle Scholar
  38. 38.
    Leonhardt W, Hanefeld M, Fischer S et al. Efficacy of alpha-glucosidase inhibitors on lipids in NIDDM subjects with moderate hyperlipidaemia. Eur J Clin Invest 1994;24(Suppl 3):45–49.PubMedGoogle Scholar
  39. 39.
    Inoue I, Shinoda Y, Nakano T et al. Acarbose ameliorates atherogenecity of low-density lipoprotein in patients with impaired glucose tolerance. Metabolism 2006;55(7):946–952.CrossRefPubMedGoogle Scholar
  40. 40.
    Hanefeld M, Fischer S, Schulze J et al. Therapeutic potentials of acarbose as first-line drug in NIDDM insufficiently treated with diet alone. Diabetes Care 1991;14:732–737.CrossRefPubMedGoogle Scholar
  41. 41.
    Heine RJ, Dekker JM. Beyond postprandial hyperglycaemia: metabolic factors associated with cardiovascular disease. Diabetologia 2002;45(4):461–475.CrossRefPubMedGoogle Scholar
  42. 42.
    Tschoepe D. Decreased fibrinogen by treatment with the alpha-glucosidase inhibitor acarbose. Diabetes 2004;53(Suppl 2):A189.Google Scholar
  43. 43.
    Wang X, Lu J, Pan C. Comparison of serum C-reactive protein level in different glucose tolerance subjects and the change in serum CRP level in IGT subjects with acarbose. EASD 2003. Published in Chinese: Lu JM et al. Chin J Endocrinol Metab 2003;19:254–256.Google Scholar
  44. 44.
    Drent ML. Miglitol as single oral hypoglycemic agent in type 2 diabetes [Abstract]. Diabetologia 1994;37(Suppl 1):211.Google Scholar
  45. 45.
    Mertes G. Safety and efficacy of acarbose in the treatment of Type 2 diabetes: data from 5-year surveillance study. Diabetes Res Clin Pract 2001;2:193–204.CrossRefGoogle Scholar
  46. 46.
    Leboritz HE. α-Glucosidase inhibitors as agents in the treatment of diabetes. Diabetes Rev 1998;6:132–145.Google Scholar
  47. 47.
    Hanefeld M, Fischer S, Julius U et al. and the DIS Group. Risk factors for myocardial infarction and death in newly detected NIDDM: the Diabetes Intervention Study, 11-year follow-up. Diabetologia 1996;39:1577–1583.CrossRefPubMedGoogle Scholar
  48. 48.
    Temelkova-Kurktschiev T, Kohler C, Henkel E et al. Post-challenge plasma glucose and glycemic spikes are more strongly associated with atherosclerosis than fasting glucose or HbAlc level. Diabetes Care 2000;23:1830–1834.CrossRefPubMedGoogle Scholar
  49. 49.
    Monnier L, Lapinski H, Colette C. Contributions of fasting and postprandial plasma glucose increments to the overall diurnal hyperglycemia of type 2 diabetic patients: variations with increasing levels of HbA(1c). Diabetes Care 2003;26(3):881–885.CrossRefPubMedGoogle Scholar
  50. 50.
    May C. Efficacy and tolerability of step wise increasing dosage of acarbose in patients with non-insulin-dependent diabetes (NIDDM) treated with sulfonylureas. Diabetes Stoffwechsel 1995;4:3–7.Google Scholar
  51. 51.
    Fischer S, Hanefeld M, Spengler M et al. European study on dose–response relationship of acarbose as a first-line drug in non-insulin-dependent diabetes mellitus: efficacy and safety of low and high doses. 1998;35:34.Google Scholar
  52. 52.
    Knowler WC, Barrett-Connor E, Fowler SE et al. Reduction in the incidence of type 2 diabetes with lifestyle intervention or metformin. N Engl J Med 2002;346(6):393–403.CrossRefPubMedGoogle Scholar
  53. 53.
    Chiasson JL, Josse RG, Gomis R et al. Acarbose treatment and the risk of cardiovascular disease and hypertension in patients with impaired glucose tolerance: the STOP-NIDDM trial. JAMA 2003;290(4):486–494.CrossRefPubMedGoogle Scholar
  54. 54.
    Hanefeld M, Chiasson JL, Koehler C et al. Acarbose slows progression of intima-media thickness of the carotid arteries in subjects with impaired glucose tolerance. Stroke 2004;35(5):1073–1078.CrossRefPubMedGoogle Scholar

Copyright information

© Springer Science+Business Media, LLC 2007

Authors and Affiliations

  • Markolf Hanefeld
    • 1
  • Frank Schaper
    • 1
  1. 1.Science and Technology TransferCentre for Clinical StudiesGermany

Personalised recommendations