Acarbose

Acarbose，called  Carbopine, which is a kind of glycosidase inhibitor.

Acarbose, which is an oral drug for the treatment of diabetic patients with elevated blood glucose after meals, can significantly reduce the level of blood glucose after meals.

Indications

1. It is suitable for patients with type 2 diabetes who are not satisfied with the curative effect after 2-3 months of diet control and physical exercise (without acute complications such as infection, trauma, ketoacidosis, hyperosmolar coma, etc.), without pregnancy. This product can be used alone or in combination with other diabetes medications such as sulfonylureas, metformin or insulin.

2. For type 1 diabetic patients with unstable blood sugar, this product can be used in combination with insulin to reduce the amount of insulin, so that the increase in blood sugar after a meal is more synchronized with the increase in blood concentration after subcutaneous injection of regular insulin, which can make blood sugar throughout the day The volatility is reduced. This product alone is not effective for patients with type 1 diabetes.

Pharmacology

1. Mechanism of Action

The most obvious effect of acarbose is to reduce postprandial hyperglycemia.

Carbohydrates in food, such as starch with a large molecular weight and oligosaccharides (oligosaccharides) with a small molecular weight, must be digested first, that is, decomposed into oligosaccharides under the action of saliva and pancreatic juice alpha amylase, and then brushed in the small intestinal mucosal cells The shape border is decomposed into monosaccharides (glucose, fructose) by alpha glycosidase before it can be absorbed by epithelial cells of the upper small intestine and enter the blood circulation, causing postprandial blood sugar to rise.

Acarbose, because of its structure similar to oligosaccharides (pseudo-oligosaccharides), can be combined with α-glycosidase. Its active center contains nitrogen in its structure, and its ability to bind to enzymes is much stronger than that of partially digested and decomposed oligosaccharides in food. Therefore, it can competitively inhibit the rapid absorption of carbohydrates in the upper part of the small intestine, and are gradually absorbed in the entire small intestine, so that the hydrolysis and absorption of disaccharides to monosaccharides are reduced, thereby delaying the intestinal lumen of disaccharides, oligosaccharides and polysaccharides. Glucose release; delay and reduce postprandial blood sugar and insulin levels.

Long-term use of this product can reduce fasting blood sugar and glycosylated hemoglobin. At the beginning of treatment, especially when a larger dose is used, part of the carbohydrate reaches the colon, is fermented by the colon flora, produces gas-containing products, and causes changes in the osmotic pressure of the intestinal tract, thereby causing flatulence and diarrhea.

2. Pharmacokinetics

After the volunteers took the radioactive 14C-labeled acarbose orally, only 1.7%±0.52% was absorbed in the active form of the drug, and the rest was degraded by bacteria or digestive enzymes in the intestine. The degraded fragments are mainly 4-methylpyrogallol derivatives. 34% of this decomposition product is absorbed within 96 hours, and is quickly and completely excreted in the urine after absorption. Therefore, the total radioactivity excreted in the urine is about 35.4%±6.0%. The radiation dose of the active drug is less than 2%. The remaining 51.3±19.5% was eliminated from feces. After oral administration of acarbose, the peak radioactivity time is 14-24 hours after taking the drug, but the peak plasma peak of the active drug is about 1 hour. This may be caused by the absorption of metabolites formed by the hydrolysis of intestinal bacteria or intestinal enzymes. After intravenous injection, 89% of the amount is excreted in urine within 48 hours, which is consistent with low bioavailability.

The half-life of acarbose is 2 hours in healthy subjects. Three oral doses a day did not produce drug accumulation. The peak concentration of acarbose and the area under the drug curve of patients with severe renal insufficiency were 5 and 6 times higher than those of healthy volunteers, respectively.

Adverse reactions

1. Adverse reactions caused by acarbose are more common in the gastrointestinal tract, including stomach bloating, abdominal distension, diarrhea, gastrointestinal cramps, stubborn constipation, hyperintestinal sounds, and increased exhaust. The main reason for these adverse reactions is the presence of undigested carbohydrates in the lower intestines, and the prolonged residence time in the intestines due to the breakdown and absorption of carbohydrates in the small intestine, resulting in increased gas production by intestinal bacteria. Most of the reactions can be reduced or disappeared with the prolonged medication time.

2. Other adverse reactions such as fatigue, headache, dizziness, skin pruritus, etc. are rare. Individual cases may have skin allergic reactions such as erythema, rash, and urticaria.

3. Individuals may also have hypoglycemia.