Diabetes MV - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 71.36 mg, maltodextrin 22.0 mg, hypromellose 100 cP. 160.0 mg, magnesium stearate 1.6 mg, silicon dioxide colloidal anhydrous 5.04 mg.

Description:

White, biconcave, oval tablets with a notch and engraving "DIA" "60" on both sides.

Pharmacotherapeutic group:hypoglycemic agent for oral use of the second-generation sulfonylurea group

ATX: & nbsp

A.10.B.B.09 Gliclazide

Pharmacodynamics:

Gliklazid is a derivative of sulfonylurea, a hypoglycemic preparation for ingestion, which differs from similar drugs in the presence N- containing heterocyclic ring with an endocyclic linkage.

Gliclazide reduces blood glucose levels by stimulating insulin secretion with beta cells from 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 glycazide has hemovascular effects.

Influence on secretion of insulin

With 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 food intake or 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 activating factors (beta-thromboglobulin, thromboxane B2), as well as restoration of fibrinolytic activity of the vascular endothelium and increase in activity of tissue activator plasminogen.

Pharmacokinetics:

Suction

After oral administration glycazide fully is absorbed. The concentration of gliclazide in plasma increases gradually in During the first 6 hours, the plateau level is maintained from 6 to 12 hours.

Individual variability is low. Eating does not affect speed or degree of absorption of gliclazide.

Distribution

With plasma proteins binds about 95% of the gliclazide. Scope distribution - about 30 liters. Reception of the drug Diabeton® MV in a dose of 60 mg once daily ensures effective concentrations of glycazide in blood plasma more than 24 hours.

Metabolism

Gliclazide is metabolized mainly in the liver. There are no active metabolites in the plasma.

Excretion

Gliclazide is excreted mainly by the kidneys: excretion is carried out in the form of metabolites, less than 1% is excreted by the kidneys in an unchanged form. The half-life of the glyclazide averages from 12 to 20 hours.

Linearity

The relationship between the dose taken (up to 120 mg) and the area under the pharmacokinetic curve "concentration-time" is linear.

Special Populations Aged people

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

Indications:

Diabetes mellitus type 2 with insufficient effectiveness of diet therapy, physical activity 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:

hypersensitivity to glycazide, other derivatives of sulfonylurea, sulfonamides or to the auxiliary substances included in the preparation;
diabetes mellitus type 1;
Diabetic ketoacidosis, diabetic precoma, diabetic coma;
severe renal or hepatic insufficiency (in these cases it is recommended to use insulin);
taking miconazole (see section "Interaction with other drugs");
pregnancy and the period of breastfeeding (see the section "Pregnancy and the period of lactation");
age to 18 years.
Due to the fact that lactose is included in the formulation, Diabeton® MB is not recommended for patients with congenital lactose intolerance, galactosemia, glucose-galactose malabsorption.

It is not recommended to use in combination with phenylbutazone or danazol (see section "Interaction with other drugs").

Carefully:Elderly age, irregular and / or unbalanced diet, insufficiency of glucose-6-phosphate dehydrogenase, severe cardiovascular disease, hypothyroidism, adrenal or pituitary insufficiency, renal and / or hepatic insufficiency, long-term glucocorticosteroid (GCS) therapy, alcoholism.

Pregnancy and lactation:

Pregnancy

Experience with glycazide during pregnancy is absent.Data on the use of other derivatives of sulfonylurea during 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 intake of oral hypoglycemic drugs with insulin therapy, both in the case of a planned pregnancy, and if the pregnancy has occurred while taking the drug.

Lactation

Taking into account the lack of data on the intake of glycazide in breast milk and the risk of developing neonatal hypoglycemia, it is contraindicated during therapy with the drug.

Dosing and Administration:

PREPARATION IS INTENDED FOR ADULT TREATMENT.

The recommended dose should be taken orally, 1 time preferably at breakfast time.

The daily dose can be 30-120 mg (1/2 -2 tablets) in one 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 it is necessary to select in dependence of the concentration of blood glucose and HbAlc.

Initial dose

The initial recommended dose (including for elderly patients 30 mg per day (1/2 tablet).

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, 90 or 120 mg.

Increase in the dose is possible not earlier than after 1 month of therapy with the drug in the 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 tablet of the preparation Diabeton® MV tablets with a modified release of 60 mg is equivalent to 2 tablets 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 tablet 60 mg) and, if necessary, 90 mg (1 and 1/2 tablets 60 mg).

Transition from the drug Diabeteston ® tablets 80 mg per drug

Diabeton MB tablets modified release 60 mg

1 tablet of the preparation Diabetes 80 mg can be replaced with 1/2 modified Diabeteson® MB 60 mg tablet. When transferring patients from Diabetes 80 mg to Diabeton® MV, careful glycemic control is recommended.

Transition from taking another hypoglycemic drug to the preparation Diabeton® MV tablets with a modified release of 60 mg

Diabetes ® preparation: The modified-release 60 mg tablet can be used in place of another hypoglycemic drug for ingestion. When transferring to Diabeton® MV patients receiving other hypoglycemic drugs for ingestion, their dose and half-life period should be considered. 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 sulfonylurea derivatives with a prolonged half-life period, 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 is 30 mg (1/2 tablet, 60 mg) and, if necessary, can be further increased as described above.

Combined reception with another hypoglycemic drugmeans of

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.

Elderly patients

Correction of the dose of the drug for patients over 65 years is not required.

Patients with renal insufficiency

The results of clinical studies have shown that correction of the dose of the drug in patients with renal insufficiency in addition to mild and moderate severity is required.It is recommended that a thorough medical check is carried out.

Patients at risk of developing hypoglycemia

Patients at risk for developing hypoglycemia (inadequate or unbalanced diet, severe or poorly compensated endocrine disorders: pituitary adrenal insufficiency, hypothyroidism; elimination of glucocorticosteroids (GCS) after long-term administration and / or administration in high doses; severe cardiovascular disease - severe ischemic heart disease, severe atherosclerosis carotid arteries, widespread atherosclerosis), it is recommended to use the minimum dose (30 mg) of the drug Diabeton® MB.

Prevention of complications of diabetes mellitus

To achieve glycemic intensive control, you can gradually increase the dose of Diabeton® MV to 120 mg / day supplement to diet and exercise until the target level of HbAlc is reached. It should be remembered about the risk of developing hypoglycemia. In addition, other hypoglycemic drugs may be added to therapy, for example, metformin, an alpha-glucosidase inhibitor, a hyazolidinedione derivative or insulin.

Children and adolescents under the age of 18.

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 drugs, drug Diabeton CF can cause hypoglycemia in the case of the irregular reception are poor, and particularly when cooking reception omitted. Possible symptoms of hypoglycemia include 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.

Also may be noted andrenergic reactions: increased sweating, "sticky" skin, anxiety, tachycardia, increased blood pressure, heartbeat, arrhythmia and angina pectoris.

As a rule, the symptoms of hypoglycemia are stopped by the intake of carbohydrates (sugar).

The intake of sugar substitutes is ineffective. On background of other derivatives sulfonylureas, there were relapses hypoglycemia after its successful cupping.

With severe or prolonged hypoglycemia emergency medical care is shown, possibly with hospitalization, even with the presence of the effect of taking carbohydrates.

Other side effects

- From the gastrointestinal side tract: abdominal pain, nausea, vomiting, diarrhea, constipation. Taking the drug in The breakfast time allows to avoid these symptoms or minimize them.

Less common are the following secondary effects:

- From the skin and subcutaneous tissue: rash. itching. urticaria, Quincke's edema, erythema, maculopapular rash, bullous reactions (such as, Stevens-Jones syndrome and toxic epidermal necrolysis).

- On the part of the organs of hematopoiesis and lymphatic system: hematologic disorders (anemia, leukopenia, thrombocytopenia, granulocytopenia) are rare.

As a rule, these phenomena are reversible in discontinuation of therapy.

- From the liver and bile excretory ways: increased activity "hepatic" enzymes (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), alkaline phosphatase), hepatitis (isolated cases). When a cholestatic jaundice should stop therapy.

These phenomena are usually reversible in the case of discontinuation of therapy.

- From the side of the organ of vision: can transient visual disorders caused by change concentration of blood glucose, especially in beginning of therapy.

- Side effects. inherent derivatives of sulfonylureas were noted following side effects: erythrocytopenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia. 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; manifestations decreased with time after the withdrawal of sulfonylureas, but in some cases led to life-threatening liver failure.

Side effects noted during the clinical trial

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.

If mild symptoms of hypoglycemia occur without a loss of consciousness or neurological symptoms, you should increase the intake of carbohydrates with food, reduce the dose of the drug and / or change the diet. Close medical surveillance of the patient's condition should continue until there is no certainty that his 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 if it is suspected, 50 ml of 20-30% dextrose solution (glucose) is injected intravenously. Then 10% dextrose solution is administered intravenously dropwise to maintain a glucose concentration in the blood above 1 g / l. Careful monitoring of blood glucose and monitoring of the patient should be carried out for at least 48 consecutive hours. After this period of time, depending on the patient's condition, the attending physician decides on the need for further monitoring.

Dialysis is ineffective due to the expressed binding of glycazide to plasma proteins.

Interaction:

1) Preparations and substances that increase the risk of developing hypoglycemia:

(enhancing the action of gliclazide)

Contraindications

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).

Unrecommended combinations

Phenylbutazone (systemic administration): enhances the hypoglycemic effect of sulfonylurea derivatives (displaces them from the bond with plasma proteins and / or slows their elimination from the body).

It is more preferable to use another anti-inflammatory drug. 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 Diabetes MW should be adjusted during the administration of phenylbutazone and after its completion.

Ethanol: increases hypoglycemia, inhibiting compensatory reactions, can contribute to the development of hypoglycemic coma. It is necessary to refuse from taking medicines, which include ethanol and drinking alcohol.

Combinations that require precautions

Admission gliclazide in combination with certain drugs: other hypoglycemic agents (insulin, acarbose, metformin, thiazolidinidiones, inhibitors

dipeptidyl peptidase-4, agonists of GLP-1); beta-adrenoblockers, fluconazole; inhibitors of angiotensin-converting enzyme - captopril,enalapril; H2-histamine receptor blockers; monoamine oxidase inhibitors; sulfonamides; clarithromycin and non-steroidal anti-inflammatory drugs drugs)

accompanied by increased hypoglycemic effect and risk of hypoglycemia.

2) Drugs that promote an increase in blood glucose: (weakening the action of gliclazide)

Unrecommended combinations

- 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 as during the administration of danazol. hack and after its cancellation.

Combinations that require precautions

Chlorpromazine (antipsychotic): in high doses (more than 100 mg per day) increases the concentration of glucose in the blood, reducing the secretion of insulin. Careful glycemic control is recommended. If it is necessary to take drugs together, it is recommended that a dose of a hypoglycemic agent be chosen, both during the administration of the neuroleptic and after its withdrawal.

SCS (systemic and topical application: intraarticular, skin, rectal administration) and tegrakozaktid: increase the concentration of blood glucose 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 the administration of the GCS and after their withdrawal.

Ritodrin, salbutamol, terbutaline (intravenous administration): beta-2 adrenomimetics contribute to increased blood glucose concentrations.

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.

3) Combinations that must be taken into account

Anticoagulants (for example, warfarin) Derivatives of sulfonylureas can enhance the effect of anticoagulants when taken together. You may need to adjust the dose of anticoagulant.

Special instructions:

When taking derivatives: sulfonylureas, including glycazide, hypoglycemia may develop,in some cases - in severe and prolonged form, requiring hospitalization and intravenous: administration of a solution of dextrose for several days (see section "Side effect").

The drug can be assigned only to those patients who eat regularly and include breakfast. It is very important to maintain sufficient intake of carbohydrates with food, since the risk of developing hypoglycemia: increases with an irregular or malnutrition, as well as consumption of food, poor carbohydrates. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after ingestion of hypoglycemic drugs at the same time.

Typically, the symptoms of hypoglycemia go away after eating a meal rich in carbohydrates (such as sugar). Should keep in mind that the intake of sugar substitutes is not promotes eliminating hypoglycemic symptoms. Experience with other derivatives sulfonylureas indicates that hypoglycaemia 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 medical care, up to hospitalization.

To avoid avoiding the development of hypoglycemia requires a careful individual selection of drugs and dosing regimens, and also 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) follow the doctor's appointments to control one's condition;

insufficient and irregular nutrition, skipping meals, fasting and changing rations;
an imbalance between the load and the amount of carbohydrates taken;
some endocrine disorders: thyroid disease, pituitary and adrenal insufficiency;
drug overdose Diabetes MB;
kidney failure; severe hepatic impairment;
simultaneous administration of certain medicines (see section "Interaction with other drugs").

Renal and hepatic impairment

In patients with hepatic and / or severe renal insufficiency to change the pharmacokinetic and / or pharmacodynamic properties of the pharmacodynamic properties of glycazide. The state of hypoglycemia, developing in such patients, it may be sufficient that such cases require immediate appropriate means, including gliclazide, has therapies.

Information for patients

It is necessary to inform the patient, as well as members of his family about the risk of developing hypoglycemia, its symptoms and conditions conducive 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 glucose control.

Insufficient glycemic control

Glycemic control in patients receiving therapy with hypoglycemic agents may be weakened in the following cases: -fever, trauma, infectious diseases or major surgical interventions.In these conditions, it may be necessary to discontinue therapy with Diabeton® MV and prescribe insulin therapy.

Many patients the effectiveness of oral hypoglycemic agents, including gliclazide, tends to decline after a prolonged period of treatment. This effect can be caused both by the progression of the bloating and by 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 a patient with secondary drug resistance, adequacy of dose selection and patient compliance with the prescribed diet.

Laboratory Tests

For evaluation of glycemic control

it is recommended to regularly check the fasting blood glucose level and the level of glycosylated hemoglobin; HALC. 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.

Because the 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.

Effect on the ability to drive transp. cf. and fur:

In connection with possible development hypoglycemia with the use of the drug Diabetes MB, patients should be are aware of the symptoms of hypoglycemia and care must be taken during vehicle management or performance of work that requires high the speed of physical and mental reactions, especially at the beginning of therapy.

Form release / dosage:

Modified release tablets 60 mg.

Packaging:

For 30 tablets per blister (PVC / Al), 1 or 2 blisters with instructions for medical use in a pack of cardboard.

When packaging (packaging) at the Russian enterprise LLC

"Serdiks": 30 tablets per blister (PVC / Al), 1 or 2 blisters with instructions for medical use in a pack of cardboard.

For 15 tablets per blister (PVC / Al), 2 or 4 blisters with instruction on

medical use in a pack of cardboard.

When manufacturing at the Russian enterprise LLC "Serdiks"

For 15 tablets in a blister of PVC / Al. For 2 or 4 blisters with instructions for medical use in a pack of cardboard.

Storage conditions:

Special storage conditions are not required.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006030/09

Date of registration:23.07.2009 / 30.04.2013

The owner of the registration certificate:Servier LaboratoriesServier Laboratories France

Manufacturer: & nbsp

Laboratories Servier France

Information update date: & nbsp18.01.2016

Illustrated instructions

Instructions

Diabeton® MB (Diabeton® MR)