Latest Guide: Usage and Precautions of Acarbose, Miglitol, and Voglibose

α-glucosidase inhibitors (AGI) are classic hypoglycemic agents and are one of the recommended combination therapies in the Chinese T2DM prevention and treatment guidelines (2020 edition). AGI drugs have been widely used in China for nearly 30 years, based on their increasingly rich clinical applications and scientific research evidence. The Endocrine and Metabolism Branch of the Chinese Geriatrics Society organized domestic experts to compile the “Clinical Application of α-glucosidase Inhibitors: Chinese Expert Consensus”. Here, we summarize the main recommendations for reference and study.

Mechanism of Action

α-glucosidase belongs to the hydrolase class, mainly including sucrase, maltase, isomaltase, and lactase, which can convert oligosaccharides into glucose.

AGI can mimic polysaccharides in the body, competitively binding to α-glucosidase on the brush border of the small intestine with a binding capacity far exceeding that of polysaccharides, inhibiting carbohydrate breakdown, reducing glucose production and absorption, and slowing postprandial increases. AGI drugs are suitable for patients whose postprandial blood glucose (PPG) increases due to carbohydrates in food.

Other Effects

1. Adjusting Incretin Secretion

Mainly manifested as increased postprandial GLP-1 secretion, possibly through the following mechanisms:

(1) Altering the distribution of carbohydrates in different parts of the intestine. After using AGI, carbohydrates cannot be fully absorbed in the upper small intestine, leading to an increase in carbohydrates reaching the lower small intestine, stimulating L cells to secrete more GLP-1.

(2) Inhibiting DPP-4 activity.

2. Adjusting Gut Microbiota

AGI can increase carbohydrates in the distal small intestine, thereby altering gut microbial fermentation, affecting the composition and function of gut microbiota, promoting the growth of probiotics, inhibiting the reproduction of harmful bacteria, helping to maintain intestinal microecological balance, and improving metabolic health and immune function.

3. Improving Insulin Resistance (IR)

Studies show that for patients with diabetes and abnormal glucose tolerance, AGI reduces PPG and postprandial insulin, thereby alleviating hyperinsulinemia. Its mechanisms include reducing inflammation factor secretion, increasing intestinal bile acid secretion, and other pathways.

4. Weight Reduction

Voglibose has little effect on weight improvement, while Acarbose and Miglitol have a slight weight-reducing effect.

5. Improving Oxidative Stress

PPG fluctuations are a major cause of oxidative stress. AGI can reduce oxidative stress by lowering PPG and increasing blood glucose stability. Additionally, Miglitol can inhibit oxidative stress by activating AMP-activated protein kinase and increasing nitric oxide synthase activity.

6. Reducing Cardiovascular Events (MACE) in Prediabetic and Diabetic Patients

The main mechanisms include that AGI drugs can reduce the hemodynamic effects of blood glucose fluctuations on diabetic patients and autonomic nervous system, which can reduce the progression of atherosclerosis, activate GLP-1 receptors, open mitochondrial ATP-sensitive potassium channels, prevent the production of hydroxyl radicals, and reduce the production of inflammatory factors such as monocyte chemotactic protein 1 and soluble adhesion molecule sE-selectin.

7. Other Hypoglycemic Effects

(1) Improving Metabolic Associated Fatty Liver Disease (MAFLD)

(2) Potential Anti-COVID-19 Effects

(3) Inhibiting Melanin Formation

Types and Usage

Currently, the AGIs available in China include Acarbose, Miglitol, and Voglibose.

The AGI drugs currently on the market in China mainly include ordinary tablets and orally disintegrating tablets. Among them, Miglitol orally disintegrating tablets are the first approved and currently the only new formulation of AGI orally disintegrating tablets, which are bioequivalent to Miglitol tablets.

>> Consensus Recommendations:

AGI drugs can be used to prevent the progression of prediabetic patients to diabetes, with reliable efficacy.
In newly diagnosed T2DM patients in China, the efficacy of AGI monotherapy is comparable to that of Metformin and can be used as one of the first-choice drugs.
Due to the unique mechanism of action of AGI, it can be combined with insulin, Metformin, sulfonylurea insulin secretagogues, DPP-4 inhibitors, and other classes of hypoglycemic drugs, which can better control blood glucose, reduce blood glucose fluctuations, and minimize hypoglycemic events.
AGI drugs, especially Miglitol, can effectively treat functional hypoglycemia and can be used for the treatment of dumping syndrome, reactive hypoglycemia, etc.

Adverse Reactions and Management

(1) Common adverse reactions include gastrointestinal reactions (bloating, gas, diarrhea, etc.). Starting with a low dose and gradually increasing is an effective method to reduce adverse reactions.

(2) AGI can induce rare colonic gas accumulation in patients with underlying diseases (such as cirrhosis, emphysema, malnutrition, or those taking glucocorticoids). Related pathological changes can completely disappear after discontinuation of the drug.

(3) Acarbose and Voglibose can cause elevated transaminases, requiring regular monitoring of liver function.

(4) AGI alone does not cause hypoglycemia; if hypoglycemia occurs during treatment, glucose or honey should be used to correct it. The effect of sucrose or starchy foods is poor for correcting hypoglycemia.

Contraindications

Patients with acute diabetic complications such as DKA;

Patients allergic to drug components;

Patients whose condition may worsen due to intestinal gas accumulation, such as inflammatory bowel disease, colon ulcers, intestinal obstruction, and severe abdominal hernias;

Patients with chronic intestinal diseases accompanied by digestive and absorption disorders;

Individuals under 18 years old;

Pregnant or breastfeeding patients, as the three AGI drugs can enter breast milk in small amounts, and there are no safety studies for pregnant patients.

Other Precautions

AGI drugs should be taken immediately before starting a carbohydrate-containing meal.

It is not recommended for patients with eGFR < 25 mL/(min·1.73m²) to use AGI.

The liver safety of different AGIs varies, and routine monitoring of liver function is not required when using Miglitol.

Antibiotic use and concomitant medications can affect AGI efficacy, which should be noted during use.

✩ This article is for reference only for medical and health professionals

Planning | Dai Dongjun

Submission Address | [email protected]

Cover Image | Zcool Hailuo

References: Chinese Expert Consensus on Clinical Application of α-glucosidase Inhibitors

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