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Acarbose (Glucobay®)

Acarbose (Glucobay® *) belongs to the class of oral antidiabetic drugs (OAD) called alpha-glucosidase inhibitors. With over one hundred studies examining its role as a treatment for type 2 diabetes and accumulating evidence of its efficacy in prediabetes, acarbose is an important intervention option throughout the hyperglycaemic disease continuum. In addition, in several trials acarbose shows cardiovascular benefits at all stages of hyperglycaemia.
Mode of Action
  • Acarbose is active in the small intestine, where it reversibly inhibits enzymes called alpha-glucosidases responsible for the breakdown of complex carbohydrates into simpler sugars such as glucose.
  • Acarbose thereby slows the digestion of carbohydrates and extends the period over which glucose is absorbed into the blood stream.1
  • By delaying the absorption of glucose from the gut, acarbose primarily reduces post-meal hyperglycaemia, which contributes to the lowering of HbA1c levels – an indicator of overall glycaemic control.
  • Prevention of post-meal hyperglycaemia is associated with additional benefits, limiting oxidative stress, prevention of beta-cell dysfunction2, reduction of hyperinsulinaemia and an improvement of insulin sensitivity3.
  • It has been demonstrated4 recently that lowering post-meal plasma glucose with acarbose treatment is associated with a significant reduction in:
    • urinary 11-dehydro-thromboxane (TBX2) – a marker of platelet activation
    • 8-iso-prostaglandin (PGF2α) – a marker of oxidative stress
  • Down-regulation of abnormal oxidative stress and of platelet activation in early type 2 diabetes may contribute to cardio-protection in this setting.
  • In 1990, acarbose was launched worldwide as a type 2 diabetes mono- and combination therapy.
  • There are further indications for acarbose in individual countries.
Efficacy and Safety**

Type 2 Diabetes

  • Acarbose can be effective as monotherapy in patients receiving lifestyle modification advice, i.e. diet and exercise
    • Acarbose significantly reduces post-meal blood glucose levels and lowers overall blood glucose levels or HbA1c levels.5,6
    • A recent meta-analysis of the independent Cochrane Group confirmed the efficacy of acarbose and reported a 0.8% reduction in HbA1c levels.7
    • In addition, acarbose remains effective during long-term therapy for at least 5 years.8
  • Acarbose can also be effective as a combination therapy with another OAD or insulin in patients receiving lifestyle modification advice.5
  • Acarbose has an excellent safety profile because it acts in the small intestine and is minimally absorbed into the body.
  • A ‘start low, go slow’ dosing regimen, with the drug dosage increased gradually over time, is recommended for optimal success. This will manage and usually decrease over time the tolerability aspects such as flatulence.
*In some countries available as Prandase® or Glucor®
**Note: Due to national registration procedure for acarbose, the product information may vary in different countries. Please refer to the product information available in your country.

1 Bischoff H. The mechanism of alpha-glucosidase inhibition in the management of diabetes, Clin Invest Med 1995;18:303-311
2 Rosak C et al. Modification of ß-cell response to different postprandial blood glucose concentrations by prandial repaglinide and combined acarbose/repaglinide application. Diab. Nutr. Metab. 17: 137-142, 2004
3 Meneilly GS et al. Effect of acarbose on insulin sensitivity in elderly patients with diabetes. Diabetes care 23: 1162-1167, 2000
4 Santilli F, Formoso G, Sbraccia P, Averna M, Miccoli R, di Fulvio P, Ganci A, Pulizzi N, Ciabattoni G, Consoli , Lauro R, Patrono C, Davì G. Effects of Acarbose on in Vivo Markers of Oxidative Stress and Platelet Activation in Early Type 2 Diabetes, JACC 2008;51(10):292-293
sup>5 Breuer HW. Review of acarbose therapeutic strategies in the long-term treatment and in the prevention of type 2 diabetes, Int J Clin Pharmacol Ther 2003;41:421-440
6 Phillips P et al. Acarbose improves glycaemic control in overweight type 2 diabetic patients insufficiently treated with metformin, Diabetes Care 2003;26:269-273
7 Van de Laar F et al. Alpha-glucosidase inhibitors for patients with type 2 diabetes mellitus: results from a Cochrane systematic review and meta-analysis, Diabetes Care 2005;28:166-175
8 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 2001;52:193-204


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