Diabeton MB 60mg #30

Diabeton MB instruction

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Clinical and pharmacological group

Oral hypoglycemic drug

Form of release, composition and packaging

Modified-release tablets are white, oval, biconvex, with a notch and engraved "DIA" "60" on both sides.
1 tab.
Gliclazide 60 mg
Excipients: lactose monohydrate - 71.36 mg, maltodextrin - 22 mg, hypromellose 100 cp - 160 mg, magnesium stearate - 1.6 mg, silicon dioxide colloidal anhydrous - 5.04 mg.
30 pcs. - blisters (1) - packs of cardboard.

pharmachologic effect

Gliclazide is a sulfonylurea derivative, a hypoglycemic preparation for oral administration, which differs from similar preparations by the presence of an N-containing heterocyclic ring with an endocyclic linkage.
Gliklazid reduces the concentration of glucose in the blood, stimulating the secretion of insulin β-cells of the islets of Langerhans. The increase in postprandial insulin and C-peptide levels persists after 2 years of therapy. In addition to the effect on carbohydrate metabolism, gliclazide exerts hemovascular effects.

Influence on secretion of insulin

In type 2 diabetes, the drug restores the early peak of insulin secretion in response to the intake of glucose and enhances the second phase of insulin secretion. A significant increase in insulin secretion is observed in response to stimulation caused by eating and the introduction of glucose.

Hemovascular effects

Gliklazid reduces the risk of thrombosis of small vessels, affecting the mechanisms that can cause complications in diabetes mellitus: partial inhibition of platelet aggregation and adhesion and a decrease in the concentration of platelet activation factors (beta-thromboglobulin, thromboxane B2), as well as restoration of fibrinolytic activity of the vascular endothelium and increase in activity of tissue activator plasminogen.
Intensive glycemic control, based on the use of Diabeton MB (glycosylated hemoglobin (HbA1c <6.5%), significantly reduces micro- and macrovascular complications of type 2 diabetes, compared to standard glycemic control (ADVANCE study).
The strategy of intensive glycemic control included the appointment of the drug Diabeton MB and an increase in its dose against a background (or instead of) standard therapy before adding to it another hypoglycemic drug (eg, metformin, alpha-glucosidase inhibitor, thiazolidinedione or insulin derivative). 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 backdrop of the use of Diabeton MB in the intensive glycemic control group (mean follow-up of 4.8 years, mean HbA1c of 6.5%), compared to the standard control group (mean HbA1c 7.3%), a significant 10% reduction in the relative risk of the combined frequency of macro- and microvascular complications.
The advantage was achieved due to a significant reduction in the relative risk: major microvascular complications by 14%, the onset and progression of nephropathy by 21%, the occurrence of microalbuminuria by 9%, macroalbuminuria by 30% and the development of renal complications by 11%.
The advantages of intensive glycemic control against the background of taking Diabeton MB did not depend on the advantages achieved against the background of antihypertensive therapy.

Pharmacokinetics

Suction

After oral administration, the glycazide is completely absorbed. The concentration of glycazide in the blood plasma increases gradually during the first 6 hours, the plateau level is maintained from 6 to 12 hours. Individual variability is low.
Eating does not affect the rate or degree of absorption of the glycazide.

Distribution

The binding to plasma proteins is approximately 95% of the gliclazide. Vd - about 30 liters. Admission of the drug Diabeton MB in a dose of 60 mg 1 time / day provides maintenance of an effective concentration of gliclazide in the blood plasma for more than 24 hours.

Metabolism

Gliklazid is metabolized primarily in the liver. There are no active metabolites in the plasma.

Excretion

T1 / 2 averages from 12 to 20 hours. Gliklazid is excreted mainly by the kidneys, excretion is carried out in the form of metabolites, less than 1% is excreted by the kidneys unchanged.

Linearity

The relationship between the dose taken (up to 120 mg) and AUC is linear.

Pharmacokinetics in special clinical cases

In elderly people, there are no significant changes in pharmacokinetic parameters.

Indications

- Type 2 diabetes mellitus with insufficient effectiveness of diet therapy, physical exertion and weight loss;
- Prevention of complications of diabetes mellitus: reducing the risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke) in patients with type 2 diabetes by intensive glycemic control.

Contraindications

- Type 1 diabetes mellitus;
- diabetic ketoacidosis, diabetic precoma, diabetic coma;
- severe renal or hepatic insufficiency (in these cases it is recommended to use insulin);
- simultaneous administration of miconazole (see section "Drug Interactions");
- pregnancy and the period of breastfeeding (see the section "Pregnancy and lactation");
- age up to 18 years;
- Hypersensitivity to gliclazide or any of the auxiliary substances of the drug, other derivatives of sulfonylurea, sulfonamides.
Due to the fact that lactose is included in the preparation, Diabeton MB is not recommended for patients with congenital lactose intolerance, galactosemia, glucose / galactose malabsorption syndrome.
It is not recommended to use the drug in combination with phenylbutazone or danazol (see section "Drug Interactions").
Precautions should be taken with irregular and / or unbalanced diet, insufficiency of glucose-6-phosphate dehydrogenase, severe cardiovascular disease, hypothyroidism, adrenal or hypophysial insufficiency, renal and / or hepatic insufficiency, prolonged therapy with GCS, alcoholism, in elderly patients age.

Dosage

The drug is intended only for the treatment of adults.
The recommended dose of the drug should be taken orally, 1 time / day, preferably during breakfast.
The daily dose is 30-120 mg (1 / 2-2 tab.) In 1 dose. It is recommended to swallow a pill or half of the whole tablet without chewing or grinding.
If you skip one or more doses of the drug, you can not take a higher dose to 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.
The initial recommended dose for adults (including for elderly patients ≥65 years) is 30 mg (1/2 table) / day.
In case of adequate control, the drug in this dose can be used for maintenance therapy. With inadequate glycemic control, the daily dose of the drug can be sequentially increased to 60 mg, 90 mg or 120 mg. Increase in the dose is possible not earlier than after 1 month of therapy with the drug at a previously prescribed dose. Exception is made by patients, in whom the blood glucose concentration did not decrease after 2 weeks of therapy. In such cases, the dose of the drug may be increased 2 weeks after the start of the treatment.
The maximum recommended daily dose of the drug is 120 mg.
1 tab. drug Diabeton MB tablets with a modified release of 60 mg is equivalent to 2 tablets. drug Diabeton MB tablets with a modified release of 30 mg. The presence of a notch on tablets of 60 mg allows you to divide the tablet and take a daily dose of 30 mg (1/2 tablets 60 mg) and, if necessary, 90 mg (1 tablets 60 mg and 1/2 tablets 60 mg).
Transition from taking the drug Diabeton tablets 80 mg to the preparation Diabeton MB tablets with a modified release of 60 mg
1 tablet of the drug Diabeton 80 mg can be replaced with 1/2 modified-release tablets Diabeton MB 60 mg. When transferring patients from the drug Diabeton 80 mg to the drug Diabeton MV recommended careful glycemic control.
Transition from taking another hypoglycemic drug to the drug Diabeton MB tablets with a modified release of 60 mg
The drug Diabeton Mint MB tablets with a modified release of 60 mg can be used in place of another hypoglycemic agent for oral administration. When transferring to MB of patients receiving other hypoglycemic drugs for oral administration, their dose and T1 / 2 should be taken into account. As a rule, a transition period is not required. The initial dose should be 30 mg and then should be titrated depending on the concentration of blood glucose.
When Diabeton MB is replaced with sulfonylureas with long T1 / 2 in order to avoid hypoglycemia caused by the additive effect of two hypoglycemic agents, you can stop taking them for several days. The initial dose of Diabeton MB preparation is also 30 mg (1/2 tablets 60 mg) and, if necessary, can be further increased as described above.

Combination with another hypoglycemic drug

Diabeton MB can be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.
With inadequate glycemic control, additional insulin therapy should be prescribed with careful medical supervision.

Special patient groups

Correction of the dose of the drug for patients over 65 years is not required.
The results of clinical studies showed that correction of the dose of the drug in patients with mild and moderate renal insufficiency is not required. It is recommended that a thorough medical check is carried out.
In patients who are at risk for developing hypoglycemia (inadequate or unbalanced nutrition, severe or poorly compensated endocrine disorders - pituitary and adrenal insufficiency, hypothyroidism, cancellation of GCS after prolonged use and / or reception in high doses, severe cardiovascular disease - severe ischemic heart disease, severe atherosclerosis of the carotid arteries, widespread atherosclerosis), it is recommended to use the minimum dose (30 mg) of the drug Diabeton MB.
To achieve intensive glycemic control, you can gradually increase the dose of Diabeton MB to 120 mg / day in addition to diet and exercise before reaching the target level of HbA1c. It should be remembered about the risk of developing hypoglycemia. In addition, other hypoglycemic drugs may be added to the therapy, for example, metformin, an alpha-glucosidase inhibitor, a thiazolidinedione derivative or insulin.
Data on the efficacy and safety of the drug in children and adolescents under the age of 18 are not available.

Side effects

Considering the experience of using glycazide, one should remember about the possibility of developing the following side effects.
Hypoglycaemia
Like other sulfonylureas, Diabeton MB may cause hypoglycemia in the event of an occasional meal and especially if the meal is missed. Possible symptoms of hypoglycemia: headache, severe hunger, nausea, vomiting, fatigue, sleep disturbance, irritability, agitation, decreased concentration, slowed reaction, depression, confusion, impaired vision and speech, aphasia, tremor, paresis, loss of self-control , feelings of helplessness, impaired perception, dizziness, weakness, convulsions, bradycardia, delirium, shallow breathing, drowsiness, loss of consciousness with possible development of coma, up to a lethal outcome.
Adrenergic reactions can also be noted: increased sweating, "sticky" skin, anxiety, tachycardia, increased blood pressure, palpitations, arrhythmia and angina.
As a rule, the symptoms of hypoglycemia are stopped by the intake of carbohydrates (sugar). The intake of sugar substitutes is ineffective. Against the background of other derivatives of sulfonylureas, there were relapses of hypoglycemia after its successful cupping.
With severe or prolonged hypoglycemia, emergency medical care is indicated, possibly with hospitalization, even if there is an effect of taking carbohydrates.

Other side effects

On the part of the digestive system: abdominal pain, nausea, vomiting, diarrhea, constipation. Taking the drug during breakfast allows you to avoid these symptoms or minimize them.
Less common are the following side effects.
From the skin and subcutaneous tissue: rash, itching, hives, Quincke's edema, erythema, maculopapular rash, bullous reactions (such as Stevens-Johnson syndrome and toxic epidermal necrolysis).
On the part of the organs of hematopoiesis and lymphatic system: hematological disorders (anemia, leukopenia, thrombocytopenia, granulocytopenia) develop rarely. As a rule, these phenomena are reversible in the event of discontinuation of therapy.
From the liver and bile ducts: increased activity of liver enzymes (AST, ALT, APF); in isolated cases - hepatitis. When cholestatic jaundice occurs, therapy should be discontinued. These phenomena are usually reversible in the event of discontinuation of therapy.
From the side of the organ of vision: transient visual disturbances caused by changes in blood glucose level can occur, especially at the beginning of therapy.
Side effects inherent in the derivatives of sulfonylureas: as against the background of taking other sulfonylurea derivatives, erythrocytopenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia were noted. There was an increase in the activity of hepatic enzymes, a violation of liver function (for example, with the development of cholestasis and jaundice) and hepatitis. These manifestations decreased with time after the withdrawal of sulfonylureas, but in some cases led to life-threatening liver failure.

Side effects noted during clinical trials

In the ADVANCE study, there was a slight difference in the incidence of various serious adverse events between the two groups of patients. No new safety data was received. A small number of patients experienced severe hypoglycemia, but the overall incidence of hypoglycemia was low. The frequency of hypoglycemia in the group of intensive glycemic control was higher than in the group of standard glycemic control. Most episodes of hypoglycemia in the group of intensive glycemic control were noted against the background of concomitant insulin therapy.

Overdose

When an overdose of sulfonylurea derivatives may develop hypoglycemia.
Treatment: if mild symptoms of hypoglycemia occur, you should increase the intake of carbohydrates 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 sure that the patient's health is not threatened.
Possible development of severe hypoglycemic conditions, accompanied by coma, seizures or other neurological disorders. If such symptoms appear, emergency medical care and immediate hospitalization are necessary.
In the case of hypoglycemic coma or suspected of it, a 50 ml 20-30% solution of dextrose (glucose) is injected intravenously into the patient. Then I / drip a 10% dextrose solution to maintain blood glucose levels above 1 g / l. Careful monitoring of blood glucose and monitoring of the patient should be carried out at least for the next 48 hours. Then, depending on the patient's condition, the need for further monitoring should be decided.
Dialysis is ineffective due to the expressed binding of glycazide to plasma proteins.

Drug Interactions

Drugs and substances that increase the risk of developing hypoglycemia (enhancing the action of Gliclazide)

Combinations are contraindicated

Miconazole (with systemic administration and with the use of gel on the oral mucosa): increases the hypoglycemic effect of glycazide (hypoglycemia may develop up to the state of coma).

Combinations are not recommended

Phenylbutazone (systemic administration) enhances the hypoglycemic effect of sulfonylurea derivatives, displaces them from the bond with plasma proteins and / or slows their excretion from the body. Preferably, another anti-inflammatory drug is used. If the reception of phenylbutazone is necessary, the patient should be warned about the need for glycemic control. If necessary, the dose of the drug Diabeton MB should be adjusted during the administration of phenylbutazone and after its completion.
When used simultaneously with glycazide, ethanol enhances hypoglycemia, inhibiting compensatory reactions, and may contribute to the development of hypoglycemic coma. It is necessary to refuse to take medicines containing ethanol, and from drinking alcohol.

Combinations that require precautions

The use of gliclazide in combination with certain drugs (for example, other hypoglycemic agents - insulin, acarbose, metformin, thiazolidinediones, dipeptidyl peptidase-4 inhibitors, GLP-1 agonists, beta-adrenoblockers, fluconazole, ACE inhibitors - captopril, enalapril, histamine H2 blockers, receptors, MAO inhibitors, sulfonamides, clarithromycin, NSAIDs) is accompanied by an increase in the hypoglycemic effect and a risk of hypoglycemia.
Drugs that promote an increase in blood glucose (weakening the effect of gliclazide)

Combinations are not recommended

Danazol has a diabetic effect. If the drug is needed, the patient should be carefully monitored for blood glucose. If it is necessary to take joint medications, it is recommended that a dose of a hypoglycemic agent be selected at the time of danazol administration and after its withdrawal.

Combinations that require precautions

The combined use of gliclazide with chlorpromazine (neuroleptic) in high doses (more than 100 mg / day) can lead to an increase in the concentration of glucose in the blood by reducing the secretion of insulin. Careful glycemic control is recommended. If it is necessary to take joint medications, it is recommended that a dose of a hypoglycemic agent be chosen at the time of taking the neuroleptic, and after its withdrawal.
With simultaneous application of GCS (for systemic and topical application - intraarticular, cutaneous, rectal administration) and tetracosactide increase the concentration of glucose in the blood with the possible development of ketoacidosis (reduced tolerance to carbohydrates). Careful glycemic control is recommended, especially at the beginning of treatment. If it is necessary to take medications together, it may be necessary to correct the dose of the hypoglycemic agent both during administration of the GCS and after their withdrawal.
With the combined use of beta2-adrenomimetics (ritodrin, salbutamol, terbutaline intravenously) contribute to an increase in the concentration of glucose in the blood.
It is necessary to pay special attention to the importance of independent glycemic control. If necessary, it is recommended to transfer the patient to insulin therapy.

Combinations that should be taken into account

Derivatives of sulfonylureas can enhance the action of anticoagulants (eg, warfarin) when taken together. You may need to adjust the dose of anticoagulant.

special instructions

Hypoglycaemia
When taking sulfonylurea derivatives, incl. and gliclazide, hypoglycemia may develop, and in some cases in severe and prolonged form, requiring hospitalization and / or dextrose administration for several days (see section "Side effect").
The drug can be prescribed only to those patients, whose meals are regular and includes breakfast. It is very important to maintain sufficient intake of carbohydrates with food, because The risk of developing hypoglycemia increases with irregular or inadequate nutrition, as well as when consuming 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.
Typically, the symptoms of hypoglycemia go away after eating a meal rich in carbohydrates (such as sugar). It should be borne in mind that the use of sugar substitutes does not help to eliminate hypoglycemic symptoms. The experience of using other sulfonylurea derivatives suggests that hypoglycemia can recur despite effective initial arrest of this condition. In the event that hypoglycemic symptoms have a pronounced character or are prolonged, even in the case of temporary improvement after a meal rich in carbohydrates, it is necessary to provide emergency medical care, up to hospitalization.
In order to avoid the development of hypoglycemia, careful individual selection of drugs and dosing regimens is necessary, as well as providing the patient with complete information about the treatment.
An increased risk of hypoglycemia may occur in the following cases:
- refusal or inability of the patient (especially the elderly) to follow the doctor's appointments and monitor his condition;
- insufficient and irregular meals, skipping meals, fasting and changing diets;
- an imbalance between physical activity and the amount of carbohydrates taken;
- kidney failure;
severe hepatic impairment;
- an overdose of Diabeton MB;
- Some endocrine disorders (thyroid gland diseases, pituitary and adrenal insufficiency);
- simultaneous intake of certain medicines.
Hepatic / Renal Failure
In patients with hepatic insufficiency and / or severe renal insufficiency, the pharmacokinetic and / or pharmacodynamic properties of the glycazide may change. Hypoglycemia, developing in such patients, can be quite long, in such cases, immediate appropriate therapy is needed.

Information for patients

It is necessary to inform the patient and his family about the risk of developing hypoglycemia, its symptoms and conditions that contribute to its development. The patient should be informed of the potential risks and benefits of the proposed treatment. The patient needs to explain the importance of dieting, the need for regular exercise and control of blood glucose.

Insufficient glycemic control

Glycemic control in patients receiving therapy with hypoglycemic agents may be weakened in the following cases: fever, trauma, infectious diseases or large surgical interventions. With 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, incl. glyclazide, tends to decline after a long treatment period. This effect can be due to both the progression of the disease and the 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 already at the first appointment does not give the expected clinical effect. Before diagnosing the patient for secondary drug resistance, it is necessary to assess the adequacy of dose selection and patient compliance with the prescribed diet.

Control of laboratory indicators

To assess the glycemic control is recommended to determine the fasting blood glucose level and the level of glycosylated hemoglobin HbA1c. In addition, it is advisable to regularly conduct self-monitoring of blood glucose concentration.
Derivatives of sulfonylureas can cause hemolytic anemia in patients with deficiency of glucose-6-phosphate dehydrogenase. Since glycazide is a derivative of sulfonylureas, caution should be exercised when it is administered to patients with deficiency of glucose-6-phosphate dehydrogenase. One should evaluate the possibility of prescribing a hypoglycemic drug of another group.
Impact on the ability to drive vehicles and manage mechanisms
In connection with the possible development of hypoglycemia in the use of the drug Diabeton MB, patients should be aware of the symptoms of hypoglycemia and should be careful when driving vehicles or performing work that requires a high rate of physical and mental reactions, especially at the beginning of therapy.

Pregnancy and lactemia

Experience with glycazide during pregnancy is absent. Data on the use of other derivatives of sulfonylurea in pregnancy are limited.
In studies on laboratory animals teratogenic effects of glycazide were not revealed.
To reduce the risk of developing congenital malformations, optimal control (appropriate therapy) of diabetes mellitus is necessary.
Oral hypoglycemic drugs during pregnancy are not applied. Insulin is the drug of choice for the therapy of diabetes mellitus in pregnant women. It is recommended to replace the use of oral hypoglycemic agents to insulin therapy in the case of a planned pregnancy, and in that case, if the pregnancy while taking the drug.
Given the lack of data on the flow of gliclazide into breast milk and the risk of neonatal hypoglycemia, during therapy with breast-feeding is contraindicated.

Application in childhood

Contraindicated in children and adolescents under 18 years.

In case of violations of kidney function

Contraindicated use of the drug in severe renal failure.
The results of clinical studies showed that correction of the dose of the drug in patients with mild and moderate renal insufficiency is not required.

With violations of liver function

Contraindicated use of the drug in severe hepatic insufficiency.

Application in old age

With caution should be used in elderly patients.

Terms and conditions of storage

The drug should be stored out of the reach of children. Special storage conditions are not required. Shelf life - 2 years. Do not use after the expiration date printed on the package.