Acarbose

Acarbose is a prescription drug used to treat type 2 diabetes. It is a pseudo-oligosaccharide that was originally isolated from the bacterium Actinoplanes utahensis. Acarbose belongs to the drug class of alpha-glucosidase inhibitors and is usually administered orally in tablet form. The active ingredient is known in many countries under the trade name Glucobay®.

Acarbose is not absorbed by the body but acts locally in the small intestine, where it delays the breakdown of complex carbohydrates into simple sugars. As a result, blood sugar levels after a meal (postprandial blood sugar) rise more slowly. This targeted action makes Acarbose an important component of blood sugar control – especially in patients with isolated elevated postprandial blood sugar spikes.

What health benefits does Acarbose offer?

Various studies have examined the effects of Acarbose. Here is a selection of various possible effects. As always, however, these should be viewed critically, as they cannot simply be transferred without further ado. Acarbose should always be taken under the supervision of a physician.

  • Blood sugar regulation: Acarbose slows carbohydrate digestion and thereby effectively reduces the postprandial rise in blood sugar (1,2,3).
  • Lower likelihood of diabetes: Results of scientific research suggest that Acarbose could reduce the risk of developing diabetes (1,4).
  • Weight reduction: Studies point to a possible weight-reducing effect that could accompany the intake of Acarbose (1,5,6).
  • Low risk of hypoglycemia: Since Acarbose does not have an insulinotropic effect, the risk of low blood sugar (hypoglycemia) is very low, especially when used alone. There are, moreover, even studies that classify Acarbose as a useful addition to the treatment of reactive hypoglycemia in non-diabetic patients (1,7).
  • Possible cardiovascular benefits: Studies suggest that Acarbose can lower the risk of cardiovascular events in diabetics – possibly by stabilizing postprandial blood sugar levels (8).

How does Acarbose work?

Acarbose specifically blocks the enzyme alpha-glucosidase, which is responsible in the small intestine for breaking down complex carbohydrates into glucose. Through this inhibition, the absorption of glucose into the blood is delayed and the blood sugar level after eating becomes flatter and more even. As a result, insulin secretion is stimulated less strongly. Since Acarbose does not act systemically (hardly enters the bloodstream), it essentially remains active locally in the intestine, where it is largely broken down by intestinal bacteria.

Dosage forms and dosage

Acarbose is available as 25 mg, 50 mg, or 100 mg oral tablets and should be taken three times daily with the first bite of a meal.

The starting dose for adults is 25 mg orally, three times daily. However, initially limiting intake to 25 mg once daily can limit gastrointestinal side effects. From a dose of 25 mg per day, it can be increased step by step to 3 doses per day. Starting from 25 mg orally, three times daily, the dose can be titrated every 4 to 8 weeks to achieve the desired blood sugar control while limiting gastrointestinal side effects. The maximum daily dose is 100 mg, three times daily (1).

Side effects, usage notes, and risks (1)

  • Common side effects: Flatulence, abdominal pain, and diarrhea are common, especially at the beginning of therapy – caused by carbohydrates that remain undigested and are fermented in the large intestine.
  • Contraindications: Acarbose is unsuitable in cases of chronic intestinal diseases, impaired liver function, or severe renal insufficiency.
  • Diet matters: A carbohydrate-rich diet can intensify side effects – adjusting the diet significantly improves tolerability.
  • Body weight: At a body weight below 60 kg, a dose of 50 mg three times daily should not be exceeded.
  • Pediatric patients: Safety and efficacy in pediatric patients have not been studied.
  • Pregnancy and breastfeeding: Studies have not established the safety of Acarbose in pregnant patients. Breastfeeding mothers should not use Acarbose.

Conclusion

Acarbose is an interesting active ingredient for postprandial blood sugar control in type 2 diabetes – especially for patients who do not tolerate systemic antidiabetic drugs or wish to avoid them. Its action in the digestive tract, the low risk of hypoglycemia, and its possible weight-reducing effect potentially make it an interesting alternative or addition in diabetes therapy. However, the therapy requires patience and a mindful diet to minimize side effects, and it should only be taken under medical supervision.

Sources:

  1. McIver, L. A., Preuss, C. V., & Tripp, J. (2024, February 12). Acarbose. In StatPearls. StatPearls Publishing. https://www.ncbi.nlm.nih.gov/books/NBK493214/
  2. Isman, A., Nyquist, A., Moel, M., Zhang, X., & Zalzala, S. (2023). The efficacy and tolerability of intermittent prandial acarbose to reduce glucose spikes in healthy individuals. Translational Medicine of Aging, 7, 12–19. https://doi.org/10.1016/j.tma.2023.04.002
  3. Yang, H. K., Lee, S. H., Shin, J., Choi, Y. H., Ahn, Y. B., Lee, B. W., Rhee, E. J., Min, K. W., & Yoon, K. H. (2019). Acarbose add-on therapy in patients with type 2 diabetes mellitus with metformin and sitagliptin failure: A multicenter, randomized, double-blind, placebo-controlled study. Diabetes & Metabolism Journal, 43(3), 287–301. https://doi.org/10.4093/dmj.2018.0054
  4. Holman, R. R., Coleman, R. L., Chan, J. C. N., Chiasson, J. L., Feng, H., Ge, J., Gerstein, H. C., Gray, R., Huo, Y., Lang, Z., McMurray, J. J., Rydén, L., Schröder, S., Sun, Y., Theodorakis, M. J., Tendera, M., Tucker, L., Tuomilehto, J., Wei, Y., Yang, W., … ACE Study Group (2017). Effects of acarbose on cardiovascular and diabetes outcomes in patients with coronary heart disease and impaired glucose tolerance (ACE): a randomised, double-blind, placebo-controlled trial. The lancet. Diabetes & endocrinology, 5(11), 877–886. https://doi.org/10.1016/S2213-8587(17)30309-1
  5. Wolever, T., Chiasson, JL., Josse, R. 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 21, 756–763 (1997). https://doi.org/10.1038/sj.ijo.0800468
  6. Li, Y., Tong, Y., Zhang, Y., Huang, L., Wu, T., & Tong, N. (2014). Acarbose monotherapy and weight loss in Eastern and Western populations with hyperglycaemia: an ethnicity-specific meta-analysis. International journal of clinical practice, 68(11), 1318–1332. https://doi.org/10.1111/ijcp.12467
  7. Lefebvre, P. J., & Scheen, A. J. (1994). The use of acarbose in the prevention and treatment of hypoglycaemia. European journal of clinical investigation, 24 Suppl 3, 40–44. https://doi.org/10.1111/j.1365-2362.1994.tb02255.x
  8. Chiasson J, 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. doi:10.1001/jama.290.4.486