Active ingredient: Gliclazide (Gliclazide) Concentration of active ingredient (mg): 60
Gliclazide is a sulfonylurea derivative, an oral hypoglycemic drug that differs from similar drugs by the presence of an N-containing heterocyclic ring with an endocyclic bond. Gliclazide lowers the concentration of glucose in the blood, stimulating insulin secretion by β-cells of Langerhans islets. Increased postprandial insulin and C-peptide levels persist after 2 years of therapy. In addition to the effect on carbohydrate metabolism, gliclazide has hemovascular effects. Effect on insulin secretion In diabetes mellitus type 2, the drug restores the early peak of insulin secretion in response to glucose intake and enhances the second phase of insulin secretion. A significant increase in insulin secretion is observed in response to stimulation caused by food intake and glucose administration. Hemovascular effects Gliclazide reduces the risk of small vessel thrombosis, affecting the mechanisms that can cause complications in diabetes mellitus: partial inhibition of aggregation and adhesion of platelets and a decrease in activation factors. (beta-thromboglobulin, thromboxane B2), as well as to restore the fibrinolytic activity of the vascular endothelium and increase activity and tissue plasminogen activator. Intensive glycemic control, based on the use of the drug Diabeton MB (glycosylated hemoglobin (HbA1c <6.5%), reliably reduces micro- and macrovascular complications of type 2 diabetes, compared to standard glycemic control (ADVANCE study). Intensive strategy glycemic control included the appointment of the drug Diabeton MB and increasing its dose against (or instead of) standard therapy before adding to it another hypoglycemic drug media Twa (e.g., metformin, alpha-glucosidase inhibitor, a thiazolidinedione derivative or insulin). The average daily dose of Diabeton MB in patients in the intensive control group was 103 mg,the maximum daily dose was 120 mg. Against the background of the use of the drug Diabeton MB in the intensive glycemic control group (average observation duration 4.8 years, average HbA1c 6.5%) compared with the standard control group (average HbA1c 7.3%) a significant decrease of 10% was shown relative risk of the combined frequency of macro-and microvascular complications. The advantage was achieved due to a significant reduction in the relative risk: the main microvascular complications by 14%, the occurrence and progression of not phropathy by 21%, the occurrence of microalbuminuria by 9%, macroalbuminuria by 30% and the development of renal complications by 11%. The benefits of intensive glycemic control while taking Diabeton MB did not depend on the benefits achieved against antihypertensive therapy.
AbsorptionAfter ingestion, gliclazide is completely absorbed. Plasma gliclazide concentration increases gradually during the first 6 hours, the plateau level is maintained from 6 to 12 hours. Individual variability is low. Food intake does not affect the speed or extent of absorption of gliclazide. Distribution Plasma protein binding is approximately 95% of glyclycide. Vd - about 30 liters. Taking the drug Diabeton MB at a dose of 60 mg 1 time / day ensures the maintenance of an effective concentration of gliclazide in the blood plasma for more than 24 hours. Metabolism Gliclazide is metabolized mainly in the liver. Plasma active metabolites are absent. Excretion of T1 / 2 averages from 12 to 20 hours. Gliclazide is excreted mainly by the kidneys, excretion is in the form of metabolites, less than 1% is excreted by the kidneys unchanged. Linearity Relationship between the dose taken (up to 120 mg) and AUC is linear. The pharmacokinetics in special clinical situations of the elderly do not show significant changes in pharmacokinetic parameters.
The recommended dose of the drug should be taken orally, 1 time per day, preferably at breakfast. The daily dose may be 30-120 mg (1/2 –2 pills) in a single dose. It is recommended to swallow a pill or half of the pill whole, without chewing or crushing. When you skip one or more doses of the drug should not take a higher dose in the next dose, the missed dose should be taken the next day.As with other hypoglycemic drugs, the dose of the drug in each case must be selected individually, depending on the concentration of blood glucose and HbA1c.
type 1 diabetes; diabetic ketoacidosis, precoma, coma; simultaneous use of miconazole; these pills are especially harmful for slender and thin people, read the LADA-diabetes article for more details; severe renal and hepatic impairment (in these cases, you need to prick insulin, and not take pills for diabetes); simultaneous use of miconazole; pregnancy and breastfeeding; age up to 18 years; hypersensitivity to gliclazide, other sulfonylurea derivatives, tablet auxiliaries. To appoint with caution: severe diseases of the cardiovascular system (heart failure, heart attack, etc.); hypothyroidism - reduced thyroid function; adrenal or pituitary insufficiency; diseases of the liver or kidneys, including diabetic nephropathy; irregular or unbalanced diet, alcoholism; elderly people.
Use during pregnancy and lactation
Hypoglycemia When taking sulfonylurea derivatives, incl. and gliclazide, hypoglycemia can develop, and in some cases it can be severe and prolonged, requiring hospitalization and IV administration of dextrose for several days (see the Adverse Effects section). The drug can be prescribed only to those patients whose food is regularly and includes breakfast. It is very important to maintain adequate intake of carbohydrates from food, because the risk of hypoglycemia increases with irregular or malnutrition, as well as with the consumption of food, poor in carbohydrates. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol or taking several hypoglycemic drugs at the same time. As a rule, the symptoms of hypoglycemia disappear after a meal rich in carbohydrates (for example, sugar). It should be borne in mind that taking sweeteners does not contribute to the elimination of hypoglycemic symptoms.Experience with other sulfonylurea derivatives suggests that hypoglycemia can recur, despite effective initial relief of this condition. If the hypoglycemic symptoms have a pronounced nature or are long, even in the case of a temporary improvement after a meal rich in carbohydrates, emergency medical care is required, including hospitalization. In order to avoid hypoglycemia, careful individual selection of drugs and dosage regimen is necessary, and also providing the patient with full information about the treatment being conducted. The increased risk of hypoglycemia may occur in the following cases: - refusal or not the ability of the patient (especially the elderly) to follow the doctor's prescriptions and control his condition; - insufficient and irregular nutrition, skipping meals, fasting and changing the diet; - an imbalance between exercise and the amount of carbohydrates; - renal failure; - severe liver failure; - overdose of Diabeton MB; some endocrine disorders (diseases of the thyroid gland, pituitary and adrenal insufficiency); - simultaneous administration of certain drugs Hepatic / renal insufficiency In patients with hepatic insufficiency and / or severe renal insufficiency, the pharmacokinetic and / or pharmacodynamic properties of gliclazide may be changed. Hypoglycemia that develops in such patients can be quite long, in such cases it is necessary to immediately conduct appropriate therapy. Information for patients It is necessary to inform the patient and his family about the risk of developing hypoglycemia, its symptoms and conditions conducive to its development. The patient must be informed of the potential risks and benefits of the proposed treatment. The patient needs to clarify the importance of dieting, the need for regular exercise and monitoring blood glucose concentrations. Insufficient glycemic controlGlycemic control in patients receiving hypoglycemic therapy may be impaired in the following cases: fever, trauma, infectious diseases, or large surgical procedures.In these conditions, it may be necessary to discontinue therapy with Diabeton MB and prescribe insulin therapy. In many patients, the effectiveness of oral hypoglycemic agents, including gliclazide tends to decrease after a long period of treatment. This effect may be due to both the progression of the disease and a decrease in the therapeutic response to the drug. This phenomenon is known as secondary drug resistance, which must be distinguished from the primary, in which the drug does not give the expected clinical effect at the first appointment. Before diagnosing a patient's secondary drug resistance, it is necessary to evaluate the adequacy of the dose selection and patient compliance with the prescribed diet. Monitoring of laboratory parameters To assess glycemic control, it is recommended to regularly determine fasting blood glucose and glycated hemoglobin HbA1c. In addition, it is advisable to regularly monitor blood glucose concentrations. Sulfonylurea derivatives can cause hemolytic anemia in patients with glucose-6-phosphate dehydrogenase deficiency. Since gliclazide is a sulfonylurea derivative, care must be taken when prescribing it to patients with glucose-6-phosphate dehydrogenase deficiency. The possibility of prescribing a hypoglycemic drug of another group should be assessed. Effect on the ability to drive motor vehicles and control mechanisms In connection with the possible development of hypoglycemia when using Diabeton MB, patients should be aware of the symptoms of hypoglycemia and should be careful when driving high rate of physical and mental reactions, especially at the beginning of therapy.
Dosage and administration
Indications for use: Sugar diabetes type 2, if diet and exercise do not help. Prevention of diabetes complications: reducing the risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke) by intensive control of blood sugar.
Drugs and substances that increase the risk of hypoglycemia (enhancing the effect of gliclazide) Combinations are contraindicated Mikonazol (with systemic administration and using the gel on the oral mucosa): enhances the hypoglycemic effect of gliclazide (hypoglycemia may develop to coma). introduction) enhances the hypoglycemic effect of sulfonylurea derivatives, since displaces them from their association with plasma proteins and / or slows their elimination from the body. Preferably the use of another anti-inflammatory drug. If taking phenylbutazone is necessary, the patient should be warned about the need for glycemic control. If necessary, the dose of Diabeton MB should be adjusted while taking phenylbutazone and after it. When used simultaneously with gliclazide, ethanol enhances hypoglycemia, inhibiting compensatory reactions, and may contribute to the development of hypoglycemic coma. It is necessary to refuse to take medicines that contain ethanol and to use alcohol. Combinations that require precautions Glyclaside in combination with certain drugs (for example, other hypoglycemic agents - insulin, acarbose, metformin, thiazolidinedione, dippeptidyl peptidase-4 inhibitors, agonist GLP-1); beta adrenoblockers, fluconazole; ACE inhibitors - captopril, enalapril; histamine H2 receptor blockers; MAO inhibitors; sulfonamides, clarithromycin, NSAIDs) is accompanied by increased hypoglycemic effect and the risk of hypoglycemia. Preparations that increase the blood glucose (weaken the effect of gliclazide). Combinations are not recommended. Danazole has a diabetogenic effect. If taking this drug is necessary, the patient is recommended to thoroughly monitor blood glucose. If necessary, joint medication, it is recommended to select a dose of a hypoglycemic agent both during danazol intake and after discontinuation. Combinations that require precautions Combined use of gliclazide with chlorpromazine (neuroleptic) in high doses (more than 100 mg / day) can lead to an increase in glucose concentration in the blood by reducing insulin secretion. A thorough glycemic control is recommended.If necessary, joint medication, it is recommended that the dose of a hypoglycemic agent be selected both during neuroleptic intake and after it is discontinued. the development of ketoacidosis (reduced tolerance to carbohydrates). A careful glycemic control is recommended, especially at the beginning of treatment. If necessary, joint medication, it may be necessary to adjust the dose of the hypoglycemic agent both during the intake of GCS, and after their cancellation. special attention to the importance of self-glycemic control. If necessary, it is recommended to transfer the patient to insulin therapy. Combinations that should be taken into accountSulfonylurea derivatives can enhance the effect of anticoagulants (for example, warfarin) when taken together. May require dose adjustment of the anticoagulant.
The most dangerous side effect is low blood sugar, hypoglycemia. Her symptoms: headache, fatigue, irritability, nightmares, palpitations. In severe cases, the patient may lose consciousness. Read the article "Hypoglycemia - Symptoms, Treatment and Prevention." Diabeton MV causes severe hypoglycemia less frequently than other sulfonylurea derivatives. Other side effects - abdominal pain, nausea, vomiting, diarrhea, constipation, rash, skin itches, increased activity of liver enzymes (AST, ALT, alkaline phosphatase). At the beginning of taking Diabeton, there may be temporary visual impairment - due to the fact that blood sugar quickly drops. Hepatitis and jaundice are also possible, but rarely. Adverse changes in the composition of the blood - extremely rare.
Interaction with other drugs
Do not exceed recommended doses.
With an overdose of sulfonylurea derivatives, hypoglycemia may develop. Treatment: If you experience mild symptoms of hypoglycemia, you should increase your carbohydrate intake with food, reduce the dose of the drug and / or change the diet.Careful monitoring of the patient’s condition should be continued until the attending physician is confident that the patient’s health is not in danger. Severe hypoglycemic states may develop, accompanied by coma, convulsions or other neurological disorders. If these symptoms appear, emergency medical care and immediate hospitalization are necessary. In case of hypoglycemic coma or suspicion of a coma, 50 ml of a 20-30% dextrose (glucose) solution is injected into the patient. Then in / in drip 10% dextrose solution to maintain the concentration of glucose in the blood above 1 g / l. Careful monitoring of blood glucose levels and patient monitoring should be carried out for at least the next 48 hours. Then, depending on the patient’s condition, the need for further monitoring should be resolved. Dialysis is ineffective due to the pronounced binding of gliclazide to plasma proteins.