Included in the formulation
Pharmacodynamics:The level of blood glucose depends on many factors, and among them - the intensity of its absorption from the intestine and the concentration of glucose in the lumen of the intestine. Obviously, the more glucose is formed in the digestive tract, the higher the level of glycemia. Inhibition of enzymes that form glucose from poly- and oligosaccharides is the basis of acarbose action. This is an oligosaccharide obtained from a bacterium Actinoplanes utahensis. The drug acts in the lumen of the small intestine, competitively and reversibly inhibits alpha-amylase (hydrolysis of polysaccharides to oligosaccharides), and intestinal membrane-bound alpha-glucosidases (formation of glucose from oligosaccharides). Inhibition of the work of these enzymes leads to a decrease in the concentration of glucose in the intestine, and thus to a decrease in its absorption into the plasma. As a consequence, postprandial glycemia decreases, as well as diurnal fluctuations in blood glucose levels. The drug does not increase the susceptibility of cells to insulin, so it can not cause hypoglycemia.
Pharmacokinetics:About 35% of the injected dose is absorbed from the gastrointestinal tract, bioavailability is 1-2%. The maximum concentration is achieved after 1 hour, metabolites - after 14-24 hours.In patients with renal insufficiency (creatinine clearance less than 25 ml / min), the maximum concentration in the plasma is increased 5-fold, in the elderly-1.5 times. It is absorbed exclusively in the gastrointestinal tract mainly by intestinal bacteria and partly by digestive enzymes, with the formation of about 13 compounds. The main metabolites are derivatives of 4-methylpyrogallol (in the form of sulfate, methyl and glucuronic conjugates), one of which is capable of inhibiting alpha-glucosidase. Unabsorbed acarbose (about 50% of the dose) is excreted by the intestine within 96 hours. Approximately 34% of the dose is excreted in the urine as metabolites, less than 2% in unchanged form. The half-life in the distribution phase is 4 hours, in the elimination phase - 10 hours.
Indications:Diabetes mellitus type 2 with ineffectiveness of diet therapy. The course last must be at least 6 months. Insufficient effectiveness of sulfonylurea derivatives against the background of a low calorie diet; type 1 diabetes mellitus (as part of combination therapy); prevention of type 2 diabetes mellitus (in patients with impaired glucose tolerance in combination with diet and exercise).
IV.E10-E14.E10 Insulin-dependent diabetes mellitus
IV.E10-E14.E11 Non-insulin-dependent diabetes mellitus
Contraindications:- chronic, inflammatory bowel diseases, ulcerative bowel lesions with severe digestion and absorption disorders;- Remkheld syndrome (gastrocardial syndrome, when after eating, overfilling, high standing diaphragm, anginal complaints arise);
large ventral hernias;
- intestinal obstruction (complete, partial, in predisposed patients);
- any other conditions for which flatulence is an aggravating factor;
- a violation of the liver. When using acarbose at a dose of 600 mg per day for more than 6 months, it is recommended to regularly monitor the activity of hepatic transaminases in blood plasma;
- Pregnancy, lactation, age under 18;
- hypersensitivity to acarbose.
Carefully:With fever, infection, injuries, as well as in the pre- and postoperative period, the application is possible only if the expected positive effect exceeds the potential risk.
Pregnancy and lactation:The safety of taking the drug during pregnancy is not proven.The action category for the fetus is FDA-B. Breastfeeding should be stopped for the duration of the drug.
Dosing and Administration:Inside, before eating; the starting dose is 50 mg 3 times a day. An increase to 100-200 mg 3 times a day is carried out every 4-8 weeks, taking into account two factors:- blood glucose level after 1 hour after eating;
- individual tolerance of the drug.
The maximum daily dose is 600 mg per day. The maximum single dose is 200 mg.
Prevention: the initial dose - 50 mg once a day with a gradual increase in a single dose to 100 mg (increasing dose is carried out for 3 months).
Side effects:Polysaccharides, not split in the small intestine due to the action of acarbose, remain unchanged in the large intestine. There, polysaccharides are broken down by bacteria. This causes possible side effects from the gastrointestinal tract: abdominal pain, flatulence, nausea, diarrhea; these effects are dose-dependent, therefore it is recommended to gradually increase the dose of the drug. Rarely observed increase in the level of hepatic transaminases, intestinal obstruction, jaundice, hepatitis (in isolated cases fulminant with fatal outcome). Allergic reactions: skin rash, hyperemia, exanthema, urticaria.
Other: rarely - swelling.
Overdose:Symptoms: increased discomfort in the abdominal area, diarrhea, flatulence. Treatment: To exclude for 4-6 hours from the diet food and beverages containing carbohydrates.
Interaction:With digoxin: the concentration of digoxin in the blood plasma decreases. With insulin, sulfonylureas, metformin: hypoglycemic action is increased.
With colestyramine: it is possible to enhance the effect of acarbose.
With neomycin: it is possible to increase the effectiveness and increase the side effects of acarbose from the digestive tract.
With activated carbon, preparations of digestive enzymes: a decrease in acarbose.
Special instructions:To correct hypoglycemia against acarbose, glucose should be used, and not sucrose. Hypoglycemia is corrected by adding sugar glucose to food, or by intravenous glucose administration, or by glucagon (in severe cases). When acute hypoglycemia occurs, it is advisable to use concentrated (40%) glucose in large doses. During the treatment should be strictly observed diet, intended for patients with diabetes. Products with a high content of carbohydrates, cane sugar can cause intestinal disorders.
The treatment is carried out under the constant control of the following indicators: blood glucose, glycosylated hemoglobin, alanine aminotransferase, aspartate aminotransferase.
With simultaneous use of acarbose with derivatives of sulfonylurea, metformin or insulin, a more pronounced hypoglycemic effect is observed, correction of the dosing regimen of these preparations may be required.