Therapy Fact Sheet Acarbose (Glucobay®) Unique mode of action
Acarbose (Glucobay®*, Bayer HealthCare AG) is in a class of oral antidiabetes drugs (OADs)
called alpha-glucosidase inhibitors. Acarbose is active in the small intestine, where it reversibly
inhibits enzymes called alpha-glucosidases, which are responsible for the breakdown of complex
carbohydrates into simpler sugars such as glucose. In this way, acarbose slows the digestion of
carbohydrates and therefore extends the period over which glucose is absorbed into the blood
stream.1 Consequently, acarbose reduces postprandial hyperglycaemia – or the rapid elevation
of blood glucose levels directly after a meal – and lowers HbA1c levels. Postprandial
hyperglycaemia is associated with an increased risk of developing type 2 diabetes in individuals
with prediabetes, and also with an increased risk of cardiovascular disease (CVD) in individuals
Indications for type 2 diabetes and prediabetes
Acarbose is approved for the treatment of type 2 diabetes, and in a number of countries also for
the treatment of prediabetes. The drug was launched worldwide as a type 2 diabetes
monotherapy and combination therapy in 1990. Acarbose was first approved as a prediabetes
therapy in China in 2002, and is now licensed for this use in 25 countries.** Acarbose is currently
the only OAD approved for prediabetes treatment.
Proven treatment for type 2 diabetes
In the 16 years since launch, a large number of clinical trials and surveillance studies have
confirmed the good efficacy and safety profiles of acarbose in type 2 diabetespatients.
Acarbose can be prescribed as a monotherapy in patients receiving lifestyle modification (diet
* In some countries acarbose is available as Prandase® or Glucor®.
** Aruba, Botswana, Brazil, China, Dominican Republic, Ecuador, El Salvador, Finland, Guatemala, Honduras, India,
Kenya, Mexico, Namibia, Nicaragua, Pakistan, Paraguay, Philippines, Portugal, South Africa, Tanzania,
Trinidad/Tobago, Turkey, Venezuela, Uganda.
and exercise). The drug significantly reduces postprandial blood glucose levels, and lowers
overall blood glucose levels, or HbA1c levels.2,3 A recent meta-analysis by the independent
Cochrane group confirmed the efficacy of acarbose and reported a 0.8% reduction in HbA1c
levels.4 In addition, acarbose remains effective during long-term therapy for up to 5 years.5
Acarbose can also be prescribed as a combination therapy in patients receiving lifestyle
modification advice and another OAD or insulin.2
Acarbose has an excellent safety profile because it acts in the small intestine and is minimally
absorbed into the body. ‘Start low, go slow’ dosing, where the drug dosage is increased gradually
over time, is recommended for optimal success.
An analysis of seven type 2 diabetes trials found that acarbose also significantly reduced the risk
of any cardiovascular event by 35% (p=0.0061 vs placebo) and myocardial infarction (MI) by
64% (p=0.0120).6 Glycaemic control, triglyceride levels, body weight and systolic blood pressure
also improved significantly during acarbose treatment.
Only approved treatment for prediabetes
The effectiveness of acarbose as a prediabetes treatment was demonstrated in the Study to
Prevent Non-Insulin Dependent Diabetes Mellitus (STOP-NIDDM). Data from this randomised,
placebo-controlled trial were released in 2002, and showed that acarbose significantly reduced
the risk of progressing from prediabetes to type 2 diabetes by 36% (p=0.0003).7 Furthermore,
patients in the acarbose group were more likely to recover to normal glucose tolerance than those
in the placebo group (p<0.0001). Supporting data have been reported by other studies, including
a trial conducted in China, where acarbose was shown to be a more effective prediabetes therapy
than metformin.8 The safety profile of acarbose in prediabetic individuals was similar to that in
STOP-NIDDM also demonstrated that acarbose therapy reduced the risk of any prespecified
cardiovascular events by 49% (p=0.03 vs placebo.9 Additionally, the risk of acute MI decreased
by 91% (1 vs 12; p=0.02). Acarbose therapy also decreased systolic (p<0.001) and diastolic
(p=0.008) blood pressures, and was associated with a 34% reduction in the risk of new
A new outcome trial will extend the findings of STOP-NIDDM by investigating the ability of
acarbose to prevent cardiovascular events in prediabetic individuals with existing CVD.
The trial will start in 2007 and be conducted by an independent research group co-chaired by
Professor Rury Holman (University of Oxford Diabetes Trials Unit, UK) and Professor Pan
Chang-Yu (University of Beijing, China); final results are expected in 2012. The trial will be
sponsored by Bayer HealthCare. The primary endpoint is the first occurrence of a specified
cardiovascular event (cardiac arrest, MI or stroke) or cardiovascular death. A secondary endpoint
is the diagnosis of new-onset type 2 diabetes.
The findings from this new outcome study are expected to have worldwide implications for future CVD management and prediabetes treatment. References
1. Bischoff H. The mechanism of alpha-glucosidase inhibition in the management of diabetes. Clin Invest
2. 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;41:421–40.
3. Phillips P, et al. Acarbose improves glycemic control in overweight type 2 diabetic patients insufficiently
treated with metformin. Diabetes Care 2003;26:269–73.
4. 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;28:166–75.
5. 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.
6. Hanefeld M, 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;25:10–6.
7. Chiasson JL, et al. Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised
8. Yang WY, et al. [The preventative effect of acarbose and metformin on the IGT population from diabetes
mellitus: a 3-year multicentre prospective trial.] Chin J Endocrinol Metab 2001;17:131–6.
9. Chiasson JL, et al. Acarbose treatment and the risk of cardiovascular disease and hypertension in
patients with impaired glucose tolerance: the STOP-NIDDM trial. JAMA 2003;290:486–94.
Counterfeit and Adulterated Prescription Drugs | Attention-Deficit/Hype. http://www.pharmacytimes.com/issues/articles/2003-09_697.asp?mode=. Pharmacy Times - Attention-Deficit/Hyperactivity Disorder Normal Version Counterfeit and Adulterated Prescription Drugs Several years ago, I attended the annual conference of the National Association of Drug Diversion Investigators (NADDI) in
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