Advanced search
Publication Cover
Expert Review of Endocrinology & Metabolism Volume 7, 2012 - Issue 4
Submit an article Journal homepage
51
Views
1
CrossRef citations to date
0
Altmetric
Drug Profile

Acarbose revisited for efficacy, safety and cardiovascular benefits: a key role for controlling glycemic variability

Markolf Hanefeld Center for Clinical Studies, GWT – Technical University Dresden, Fiedlerstrasse 34, 01307 Dresden, Germany. [email protected]
Pages 395-405 | Published online: 10 Jan 2014

References

  • Ray KK, Seshasai SR, Wijesuriya S et al. Effect of intensive control of glucose on cardiovascular outcomes and death in patients with diabetes mellitus: a meta-analysis of randomised controlled trials. Lancet 373(9677), 1765–1772 (2009).
  • Ma J, Yang W, Fang N, Zhu W, Wei M. The association between intensive glycemic control and vascular complications in Type 2 diabetes mellitus: a meta-analysis. Nutr. Metab. Cardiovasc. Dis. 19(9), 596–603 (2009).
  • The Diabetes Control and Complications Trial/Epidemiology of Diabetes Interventions and Complications Research Group. Retinopathy and nephropathy in patients with Type 1 diabetes four years after a trial of intensive therapy. N. Engl. J. Med. 342, 381–389 (2000).
  • UK Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with Type 2 diabetes (UKPDS 33). Lancet 352, 837–853 (1998).
  • DECODE Study Group on behalf of the European Diabetes Epidemiology Group. Glucose tolerance and cardiovascular mortality. Comparison of fasting and 2-hour diagnostic criteria. Arch. Intern. Med. 161, 397–404 (2001).
  • Woerle HJ, Neumann C, Zschau S et al. Impact of fasting and postprandial glycemia on overall glycemic control in Type 2 diabetes. Importance of postprandial glycemia to achieve target HbA1c levels. Diabetes Res. Clin. Pract. 77(2), 280–285 (2007).
  • Kageyama S, Nakamichi N, Sekino H, Nakano S. Comparison of the effects of acarbose and voglibose in healthy subjects. Clin. Ther. 19(4), 720–729 (1997).
  • Hanefeld M. Cardiovascular benefits and safety profile of acarbose therapy in prediabetes and established Type 2 diabetes. Cardiovasc. Diabetol. 6, 20 (2007).
  • Brownlee M. Biochemistry and molecular cell biology of diabetic complications. Nature 414(6865), 813–820 (2001).
  • Esposito K, Nappo F, Marfella R et al. Inflammatory cytokine concentrations are acutely increased by hyperglycemia in humans: role of oxidative stress. Circulation 106(16), 2067–2072 (2002).
  • Ceriello A, Falleti E, Motz E et al. Hyperglycemia-induced circulating ICAM-1 increase in diabetes mellitus: the possible role of oxidative stress. Horm. Metab. Res. 30(3), 146–149 (1998).
  • Chittari MV, McTernan P, Bawazeer N et al. Impact of acute hyperglycaemia on endothelial function and retinal vascular reactivity in patients with Type 2 diabetes. Diabet. Med. 28(4), 450–454 (2011).
  • Hanefeld M, Koehler C, Henkel E, Fuecker K, Schaper F, Temelkova-Kurktschiev T. Post-challenge hyperglycaemia relates more strongly than fasting hyperglycaemia with carotid intima–media thickness: the RIAD Study. Risk factors in impaired glucose tolerance for atherosclerosis and diabetes. Diabet. Med. 17(12), 835–840 (2000).
  • Hanefeld M, Fischer S, Julius U et al. Risk factors for myocardial infarction and death in newly detected NIDDM: the Diabetes Intervention Study, 11-year follow-up. Diabetologia 39(12), 1577–1583 (1996).
  • Meigs JB, Nathan DM, D’Agostino RB Sr, Wilson PW; Framingham Offspring Study. Fasting and postchallenge glycemia and cardiovascular disease risk: the Framingham Offspring Study. Diabetes Care 25(10), 1845–1850 (2002).
  • Levitan EB, Song Y, Ford ES, Liu S. Is nondiabetic hyperglycemia a risk factor for cardiovascular disease? A meta-analysis of prospective studies. Arch. Intern. Med. 164(19), 2147–2155 (2004).
  • Nakagami T; DECODA Study Group. Hyperglycaemia and mortality from all causes and from cardiovascular disease in five populations of Asian origin. Diabetologia 47(3), 385–394 (2004).
  • Monnier L, Colette C, Boniface H. Contribution of postprandial glucose to chronic hyperglycaemia: from the ‘glucose triad’ to the trilogy of ‘sevens’. Diabetes Metab. 32, 2S11–2S16 (2006).
  • Wang JS, Tu ST, Lee IT et al. Contribution of postprandial glucose to excess hyperglycaemia in Asian Type 2 diabetic patients using continuous glucose monitoring. Diabetes Metab. Res. Rev. 27(1), 79–84 (2011).
  • Ning F, Tuomilehto J, Pyörälä K, Onat A, Söderberg S, Qiao Q; DECODE Study Group. Cardiovascular disease mortality in Europeans in relation to fasting and 2-h plasma glucose levels within a normoglycemic range. Diabetes Care 33(10), 2211–2216 (2010).
  • Marfella R, Nappo F, De Angelis L, Siniscalchi M, Rossi F, Giugliano D. The effect of acute hyperglycaemia on QTc duration in healthy man. Diabetologia 43(5), 571–575 (2000).
  • Hyvärinen M, Tuomilehto J, Mähönen M et al.; DECODE Study Group. Hyperglycemia and incidence of ischemic and hemorrhagic stroke comparison between fasting and 2-hour glucose criteria. Stroke 40(5), 1633–1637 (2009).
  • Zhou XH, Qiao Q, Zethelius B et al.; DECODE Study Group. Diabetes, prediabetes and cancer mortality. Diabetologia 53(9), 1867–1876 (2010).
  • Peter R, Okoseime OE, Rees A, Owens DR. Postprandial glucose – a potential therapeutic target to reduce cardiovascular mortality. Curr. Vasc. Pharmacol. 7(1), 68–74 (2009).
  • Hanefeld M, Fischer S, Schmechel H et al. Diabetes Intervention Study. Multi-intervention trial in newly diagnosed NIDDM. Diabetes Care 14(4), 308–317 (1991).
  • Stratton IM, Adler AI, Neil HA et al. Association of glycaemia with macrovascular and microvascular complications of Type 2 diabetes (UKPDS 35): prospective observational study. BMJ 321(7258), 405–412 (2000).
  • American Diabetes Association. Standards of Medical Care in Diabetes-2011. Diabetes Care 34(Suppl. 1), S11–S61 (2011).
  • Rodbard HW, Jellinger PS, Davidson JA et al. Statement by an American Association of Clinical Endocrinologists/American College of Endocrinology consensus panel on Type 2 diabetes mellitus: an algorithm for glycemic control. Endocr. Pract. 15(6), 540–559 (2009).
  • Brownlee M, Hirsch IB. Glycemic variability: a hemoglobin A1c-independent risk factor for diabetic complications. JAMA 295(14), 1707–1708 (2006).
  • Alberti KG, Zimmet P, Shaw J. International Diabetes Federation: a consensus on Type 2 diabetes prevention. Diabet. Med. 24(5), 451–463 (2007).
  • van de Laar FA, Lucassen PL, Akkermans RP et al. Alpha-glucosidase inhibitors for Type 2 diabetes mellitus. Cochrane Database Syst. Rev. CD003639 (2005).
  • Pan C, Yang W, Barona JP et al. Comparison of vildagliptin and acarbose monotherapy in patients with Type 2 diabetes: a 24-week, double-blind, randomized trial. Diabet. Med. 25(4), 435–441 (2008).
  • Pan CY, Gao Y, Li GW, Zhu XX, Gao X, Liu X. [A comparison of efficacy and tolerance of nateglinide and acarbose monotherapy in Type 2 diabetes mellitus]. Zhonghua Nei Ke Za Zhi 48(4), 304–307 (2009).
  • Hoffmann J, Spengler M. Efficacy of 24-week monotherapy with acarbose, glibenclamide, or placebo in NIDDM patients. The Essen Study. Diabetes Care 17(6), 561–566 (1994).
  • Hoffmann J, Spengler M. Efficacy of 24-week monotherapy with acarbose, metformin, or placebo in dietary-treated NIDDM patients: the Essen-II Study. Am. J. Med. 103(6), 483–490 (1997).
  • Matsumura M, Monden T, Miyashita Y et al. Effects of changeover from voglibose to acarbose on postprandial triglycerides in Type 2 diabetes mellitus patients. Adv. Ther. 26(6), 660–666 (2009).
  • Rathmann W, Kostev K, Haastert B. Glycemic durability of monotherapy for diabetes. N. Engl. J. Med. 356(13), 1378–1379; author reply 1380 (2007).
  • Mertes G. Safety and efficacy of acarbose in the treatment of Type 2 diabetes: data from a 5-year surveillance study. Diabetes Res. Clin. Pract. 52(3), 193–204 (2001).
  • Li C, Hung YJ, Qamruddin K, Aziz MF, Stein H, Schmidt B. International noninterventional study of acarbose treatment in patients with Type 2 diabetes mellitus. Diabetes Res. Clin. Pract. 92(1), 57–64 (2011).
  • Schnell O, Mertes G, Standl E; Acarbose-Insulin Combination Study Group. Acarbose and metabolic control in patients with Type 2 diabetes with newly initiated insulin therapy. Diabetes. Obes. Metab. 9(6), 853–858 (2007).
  • Rosak C. The role of acarbose in Type 2 diabetes combination therapy. Diabetes Metab. Heart 16, 119–126 (2007).
  • Jayaram S, Hariharan RS, Madhavan R, Periyandavar I, Samra SS. A prospective, parallel group, open-labeled, comparative, multi-centric, active controlled study to evaluate the safety, tolerability and benefits of fixed dose combination of acarbose and metformin versus metformin alone in Type 2 diabetes. J. Assoc. Physicians India 58, 679–682, 687 (2010).
  • Halimi S, Le Berre MA, Grangé V. Efficacy and safety of acarbose add-on therapy in the treatment of overweight patients with Type 2 diabetes inadequately controlled with metformin: a double-blind, placebo-controlled study. Diabetes Res. Clin. Pract. 50(1), 49–56 (2000).
  • Phillips P, Karrasch J, Scott R, Wilson D, Moses R. Acarbose improves glycemic control in overweight Type 2 diabetic patients insufficiently treated with metformin. Diabetes Care 26(2), 269–273 (2003).
  • Rosenstock J, Brown A, Fischer J et al. Efficacy and safety of acarbose in metformin-treated patients with Type 2 diabetes. Diabetes Care 21(12), 2050–2055 (1998).
  • Rosak C, Haupt E, Walter T, Werner J. The effect of combination treatment with acarbose and glibenclamide on postprandial glucose and insulin profiles: additive blood glucose lowering effect and decreased hypoglycaemia. Diabetes Nutr. Metab. 15(3), 143–151 (2002).
  • Rosak C, Hofmann U, Paulwitz O. Modification of beta-cell response to different postprandial blood glucose concentrations by prandial repaglinide and combined acarbose/repaglinide application. Diabetes Nutr. Metab. 17(3), 137–142 (2004).
  • Derosa G, Salvadeo SA, D’Angelo A et al. Metabolic effect of repaglinide or acarbose when added to a double oral antidiabetic treatment with sulphonylureas and metformin: a double-blind, cross-over, clinical trial. Curr. Med. Res. Opin. 25(3), 607–615 (2009).
  • Su JB, Wang XQ, Chen JF, Wu G, Jin Y. Glycemic variability in insulin treated Type 2 diabetes with well-controlled hemoglobin A1c and its response to further treatment with acarbose. Chin. Med. J. 124(1), 144–147 (2011).
  • Lin SD, Wang JS, Hsu SR et al. The beneficial effect of α-glucosidase inhibitor on glucose variability compared with sulfonylurea in Taiwanese Type 2 diabetic patients inadequately controlled with metformin: preliminary data. J. Diabetes Complicat. 25(5), 332–338 (2011).
  • Bao YQ, Zhou J, Zhou M et al. Glipizide controlled-release tablets, with or without acarbose, improve glycaemic variability in newly diagnosed Type 2 diabetes. Clin. Exp. Pharmacol. Physiol. 37(5–6), 564–568 (2010).
  • Chiasson JL, Josse RG, Gomis R, Hanefeld M, Karasik A, Laakso M; STOP-NIDDM Trail Research Group. Acarbose for prevention of Type 2 diabetes mellitus: the STOP-NIDDM randomised trial. Lancet 359(9323), 2072–2077 (2002).
  • Chiasson JL, Josse RG, Gomis R, Hanefeld M, Karasik A, Laakso M; STOP-NIDDM Trial Research Group. Acarbose treatment and the risk of cardiovascular disease and hypertension in patients with impaired glucose tolerance: the STOP-NIDDM trial. JAMA 290(4), 486–494 (2003).
  • Wenying Y, Lixiang L, Jinwu Q et al. The Chinese Diabetes Prevention Trial: preventive effect of metformin on the progression to diabetes mellitus in the IGT population: a 3-year multicenter prospective study. Chin. J. Endocrinol. Metab. 17, 131–136 (2001).
  • Hanefeld M, Cagatay M, Petrowitsch T, Neuser D, Petzinna D, Rupp M. Acarbose reduces the risk for myocardial infarction in Type 2 diabetic patients: meta-analysis of seven long-term studies. Eur. Heart J. 25(1), 10–16 (2004).
  • Chaisson JL. Acarbose for the prevention of diabetes, hypertension, and cardiovascular disease in subjects with impaired glucose tolerance: the Study to Prevent Non-Insulin-Dependent Diabetes Mellitus (STOP-NIDDM) Trial. Endocr. Pract. 12(Suppl. 1), 25–30 (2006).
  • Hanefeld M, Pistrosch F, Koehler C, Chiasson JL. Conversion of IGT to Type 2 diabetes mellitus is associated with incident cases of hypertension: a post-hoc analysis of the STOP-NIDDM trial. J. Hypertens. 30(7), 1440–1443 (2012).
  • Hanefeld M, Schaper F. Drug therapy for the prevention of Type 2 diabetes – is there a medical rationale. Br. J. Diab. Vasc. Dis. 11, 168–174 (2012).
  • Karunakaran S, Hammersley MS, Morris RJ, Turner RC, Holman RR. The Fasting Hyperglycaemia Study: III. Randomized controlled trial of sulfonylurea therapy in subjects with increased but not diabetic fasting plasma glucose. Metab. Clin. Exp. 46(12 Suppl. 1), 56–60 (1997).
  • NAVIGATOR Study Group. Effect of nateglinide on the incidence of diabetes and cardiovascular events. N. Engl. J. Med. 362, 1463–1476 (2010).
  • 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. 35(9), 551–557 (2005).
  • Kato T, Inoue T, Node K. Postprandial endothelial dysfunction in subjects with new-onset Type 2 diabetes: an acarbose and nateglinide comparative study. Cardiovasc. Diabetol. 9, 12 (2010).
  • Koyasu M, Ishii H, Watarai M et al. Impact of acarbose on carotid intima–media thickness in patients with newly diagnosed impaired glucose tolerance or mild Type 2 diabetes mellitus: a one-year, prospective, randomized, open-label, parallel-group study in Japanese adults with established coronary artery disease. Clin. Ther. 32(9), 1610–1617 (2010).
  • Hanefeld M, Chiasson JL, Koehler C, Henkel E, Schaper F, Temelkova-Kurktschiev T. Acarbose slows progression of intima–media thickness of the carotid arteries in subjects with impaired glucose tolerance. Stroke 35(5), 1073–1078 (2004).
  • Kado S, Murakami T, Aoki A et al. Effect of acarbose on postprandial lipid metabolism in Type 2 diabetes mellitus. Diabetes Res. Clin. Pract. 41(1), 49–55 (1998).
  • Santilli F, Formoso G, Sbraccia P et al. Postprandial hyperglycemia is a determinant of platelet activation in early Type 2 diabetes mellitus. J. Thromb. Haemost. 8(4), 828–837 (2010).
  • Ceriello A, Taboga C, Tonutti L et al. Post-meal coagulation activation in diabetes mellitus: the effect of acarbose. Diabetologia 39(4), 469–473 (1996).
  • Tsunosue M, Mashiko N, Ohta Y et al. An alpha-glucosidase inhibitor, acarbose treatment decreases serum levels of glyceraldehyde-derived advanced glycation end products (AGEs) in patients with Type 2 diabetes. Clin. Exp. Med. 10(2), 139–141 (2010).
  • 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 [abstract 1634]. Chin. J. Endocrinol. Metab. 19, 254–256 (2003).
  • Hanefeld M, Schaper F, Koehler C et al. Effect of acarbose on postmeal mononuclear blood cell response in patients with early Type 2 diabetes: the AI(I)DA study. Horm. Metab. Res. 41(2), 132–136 (2009).
  • Rudofsky G Jr, Reismann P, Schiekofer S et al. Reduction of postprandial hyperglycemia in patients with Type 2 diabetes reduces NF-kappaB activation in PBMCs. Horm. Metab. Res. 36(9), 630–638 (2004).
  • Spengler M, Schmitz H, Landen H. Evaluation of the efficacy and tolerability of acarbose in patients with diabetes mellitus: a postmarketing surveillance study. Clin. Drug Investig. 25(10), 651–659 (2005).
  • Holstein A, Egberts EH. Risk of hypoglycaemia with oral antidiabetic agents in patients with Type 2 diabetes. Exp. Clin. Endocrinol. Diabetes 111(7), 405–414 (2003).
  • May C. Efficacy and tolerability of stepwise increasing dosage of acarbose in patients with non-insulin-dependent diabetes mellitus (NIDDM), treated with sulphonylureas. Diabetes Stoffwechsel 4, 3–8 (1995).
  • Piccinni C, Motola D, Marchesini G, Poluzzi E. Assessing the association of pioglitazone use and bladder cancer through drug adverse event reporting. Diabetes Care 34(6), 1369–1371 (2011).
  • Suzuki S, Arnold LL, Pennington KL et al. Effects of pioglitazone, a peroxisome proliferator-activated receptor gamma agonist, on the urine and urothelium of the rat. Toxicol. Sci. 113(2), 349–357 (2010).
  • Tseng CH. Diabetes and risk of bladder cancer: a study using the National Health Insurance database in Taiwan. Diabetologia 54(8), 2009–2015 (2011).
  • Bo S, Ciccone G, Rosato R et al. Cancer mortality reduction and metformin: a retrospective cohort study in Type 2 diabetic patients. Diabetes. Obes. Metab. 14(1), 23–29 (2012).
  • Fachinformation. Glucobay® 50 mg, Glucobay® 100 mg. Document 003443-D671. November 2010. DE/28 (2010).

Websites

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.