Acarbose

Acarbose: What is it and how does it work in the body?

• Acarbose is an alpha-glucosidase inhibitor. It competitively binds to α-glucosidase, which acts on the absorption of carbohydrates in the small intestine. It causes optimal inhibition of postprandial increases in glucose, insulin, and triglycerides.

What is it used for and at what dosage?

• Although most commonly known for its use in type 2 diabetes, other studies have its cardioprotective effects as well as helping patient with metabolic

  syndrome.

• Acarbose is typically dispensed in 25, 50, and 100 mg tablets its maximum dose is 50 mg q8hr for individuals weighing less than 60 kg and 100 mg for those weighing greater than 100 mg q8hr. With its most commonly prescribed to treat type 2 DM.

Evidence for or against its different uses:

• The STOP-NIDDM randomized trial showed evidence that acarbose significantly increased reversion of impaired glucose tolerance to normal glucose tolerance 

• Acarbose could be used, either as an alternative or in addition to changes in lifestyle, to delay development of type 2 diabetes in patients with impaired glucose tolerance. Acarbose monotherapy was also shown to be beneficial in reducing triglyceride levels in obese or overweight patients and did not result in hypoglycemia during medication. Participants with metabolic syndrome treated with acarbose experienced a decrease in weight and abdominal obesity as well as the inflammatory and cardiovascular markers, including flow-­ mediated dilation (FMD), intima media thickness (IMT), epicardial fat thickness (EFT), and C-reactive protein (CRP) levels.

Safety concerns, side effects, and precautions:

• No serious side effects have been reported during treatment with acarbose although it is associated with a high incidence of troublesome gastrointestinal symptoms such as flatulence, abdominal distension, and diarrhea. The incidence of these reactions usually decreases with time.

Interactions with medications:

• Acarbose administered during excessive alcohol consumption has shown to affect glycemic control and produce a disulfaram-like reaction. Digoxin absorption can be lowered by approximately 57–62% when coadministered with Acarbose, regardless of its dosing [4]. Multiple dose of acarbose impacts the peak concentration of metformin and lowers the value 30% and extent of absorption by over 35%

Key Web Sources

•  Chiasson JL, Josse RG, Gomis R, Hanefeld M, Karasik A, Laakso M, STOPNIDDM

  Trail Research Group.

• Acarbose for prevention of type 2 diabetes mellitus: the STOP-

  NIDDM randomised trial. Lancet. 2002;359(9323):2072–7. https://doi.org/10.1016/

  S0140-6736(02)08905-5. PMID: 12086760

• Yu AQ, Le J, Huang WT, Li B, Liang HX, Wang Q, Liu YT, Young CA, Zhang MY, Qin

  SL. The effects of acarbose on non-diabetic overweight and obese patients: a meta-analysis.

  Adv Ther. 2021;38(2):1275–89. https://doi.org/10.1007/s12325-020-01602-9. Epub 2021

  Jan 9. Erratum in: Adv Ther. 2021 Aug;38(8):4603-4604. PMID: 33421022

• Khalili N, Safavipour A. Evaluation of the effects of acarbose on weight and metabolic,

  inflammatory, and cardiovascular markers in patients with obesity and overweight [J]. Int J

  Prev Med. 2020;11:140.

• Serrano JS, Jiménez CM, Serrano MI, et al. A possible interaction of potential clinical interest between digoxin and acarbose. Clin Pharmacol Ther. 1996;60:589–92.

• Gerard J, Lefebvre PJ, Luyckx AS. Glibenclamide pharmacokinetics in acarbose-treated type

  2 diabetics. Eur J Clin Pharmacol. 1984;27:233–6.

• Scheen AJ, de Magalhaes AC, Salvatore T, Lefebvre PJ. Reduction of the acute bioavailability of metformin by the alpha-glucosidase inhibitor acarbose in normal man. Eur J Clin

  Invest. 1994;24:50–4.