Diamerid - instructions for use, indications, doses, analogues

Release form and composition

Dosage form of release Diamerida - tablets: flat-cylindrical, with a chamfer, minor inclusions are acceptable; 1 and 3 mg - pink with a brownish tint, 2 and 4 mg - from yellow or light yellow to cream color (in blister packs of 10 pcs., in a cardboard pack 3 or 6 packs).

Composition of 1 tablet:

active substance: glimepiride – 1, 2, 3 or 4 mg (calculated as 100% substance);
auxiliary components (1/2/3/4 mg): magnesium stearate – 0.6/0.6/1.2/1.2 mg; lactose monohydrate – 78.68/77.67/156.36/155.34 mg; croscarmellose sodium – 4.7/4.7/9.4/9.4 mg; povidone – 2.5/2.5/5/5 mg; poloxamer – 0.5/0.5/1/1/ mg; microcrystalline cellulose – 12/12/24/24 mg; yellow dye iron oxide – 0/0.03/0/0.06 mg; red dye iron oxide – 0.02/0/0.04/0 mg.

Contraindications

Absolute:

lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
leukopenia;
diabetic ketoacidosis, diabetic coma and precoma;
type 1 diabetes mellitus;
conditions accompanied by impaired absorption of food and the development of hypoglycemia (including infectious diseases);
functional disorders of the kidneys/liver in severe cases (including patients on hemodialysis);
pregnancy and breastfeeding;
age under 18 years;
individual intolerance to the components of the drug, including hypersensitivity to other sulfonylurea derivatives or sulfonamide drugs (associated with the likelihood of developing hypersensitivity reactions).

Prescribing Diameride requires caution in the presence of conditions that require transferring the patient to insulin therapy, including extensive burns, major surgical interventions, multiple severe injuries, impaired absorption of food and drugs from the gastrointestinal tract (gastric paresis, intestinal obstruction).

When pregnancy occurs or when it is planned, the woman must be switched to insulin therapy.

Diamerid tab 2mg No. 30

Compound

Active substance: glimepiride - 2 mg. Excipients: lactose monohydrate - 77.67 mg, povidone - 2.5 mg, poloxamer - 0.5 mg, croscarmellose sodium - 4.7 mg, microcrystalline cellulose - 12 mg, magnesium stearate - 0.6 mg, red iron oxide dye - 0.04 mg.

Pharmacokinetics

With repeated oral administration at a dose of 4 mg/day, Cmax in the blood serum is achieved in approximately 2.5 hours and is 309 ng/ml; There is a linear relationship between dose and Cmax, as well as between dose and AUC. Food intake does not have a significant effect on absorption.

Vd about 8.8 l. Plasma protein binding is more than 99%.

Clearance - about 48 ml/min.

Metabolized. The hydroxylated and carboxylated metabolites of glimepiride appear to be formed as a result of metabolism in the liver and are found in urine and feces.

T1/2 is 5-8 hours. After taking glimepiride in high doses, T1/2 increases. After a single oral dose of radiolabeled glimepiride, 58% of the radioactivity was detected in urine and 35% in feces. No unchanged active substance was detected in the urine.

T1/2 of the hydroxylated and carboxylated metabolites of glimepiride were about 3-6 hours and 5-6 hours, respectively.

In patients with impaired renal function (with low creatinine clearance), there was a trend toward increased clearance of glimepiride and a decrease in its mean serum concentrations. Thus, in this category of patients there is no additional risk of accumulation of glimepiride.

Indications for use

Type 2 diabetes mellitus with ineffectiveness of previously prescribed diet and physical activity.

If monotherapy with glimepiride is ineffective, it can be used in combination therapy with metformin or insulin.

Contraindications

type 1 diabetes mellitus;
diabetic ketoacidosis, diabetic precoma and coma;
conditions accompanied by impaired absorption of food and the development of hypoglycemia (including infectious diseases);
leukopenia;
severe liver dysfunction;
severe renal impairment (including patients on hemodialysis);

hypersensitivity to glimepiride or to any inactive component of the drug, to other sulfonylurea derivatives or to sulfonamide drugs (risk of developing hypersensitivity reactions);

pregnancy and breastfeeding;
lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
children up to 18 years of age.

With caution:
In the first weeks of taking the drug (increased risk of hypoglycemia); in the presence of risk factors for the development of hypoglycemia; when changing the lifestyle of patients (changing diet and meal times, increasing or decreasing physical activity); for intercurrent diseases and during the recovery period of the body after stressful situations; glucose-6-phosphate hydrogenase deficiency; conditions requiring transfer of the patient to insulin therapy (extensive burns, severe multiple injuries, major surgical interventions, as well as impaired absorption of food and drugs in the gastrointestinal tract - intestinal obstruction, gastric paresis, etc.).

Directions for use and doses

As a rule, the dose of Diamerid® is determined by the target blood glucose concentration. The lowest dose sufficient to achieve the required metabolic control should be used.

During treatment with Diamerid®, it is necessary to regularly determine the concentration of glucose in the blood. In addition, regular monitoring of glycated hemoglobin levels is recommended.

Incorrect use of the drug, such as missing a dose, should never be made up for by taking a subsequent higher dose.

The patient's actions in case of errors when taking the drug Diamerid® (in particular, when missing a dose or skipping a meal) or in situations where it is not possible to take the drug should be discussed between the patient and the doctor in advance.

Taking Diamerid®

Diamerid tablets are taken orally, without chewing, with a sufficient amount of liquid (about 0.5 cups).

Initial dose and dose selection

The starting dose is 1 mg glimepiride once daily. If necessary, the daily dose can be gradually (at intervals of 1-2 weeks) increased. It is recommended that the dose be increased under regular monitoring of blood glucose concentrations and in accordance with the following dose increase step: 1 mg - 2 mg - 3 mg - 4 mg - 6 mg (- 8 mg).

Dose range in patients with well-controlled diabetes mellitus

The usual daily dose in patients with well-controlled diabetes mellitus is 1-4 mg glimepiride. A daily dose of more than 6 mg is more effective in only a small number of patients.

Dosage regimen

The time for taking Diamerid and the distribution of doses during the day is determined by the doctor, depending on the patient’s lifestyle at a given time (time of eating, amount of physical activity).

Usually, a single dose of Diamerid during the day is sufficient. It is recommended that in this case the entire dose of Diamerid® be taken immediately before a full breakfast or, if not taken at this time, immediately before the first main meal.

It is very important not to skip meals after taking Diamerid.

Since improved metabolic control is associated with increased insulin sensitivity, the need for glimepiride may decrease during treatment. In order to avoid the development of hypoglycemia, it is necessary to promptly reduce the dose or stop taking the drug Diamerid.

Conditions that may also require dose adjustment of glimepiride:

weight loss in the patient;
changing the patient’s lifestyle (changes in diet, meal times, amount of physical activity);
the occurrence of other factors that lead to a predisposition to the development of hypoglycemia or hyperglycemia (see section “Special instructions”).

Duration of treatment

Treatment with glimepiride is usually long-term.

Transferring a patient from taking another oral hypoglycemic drug to taking Diameride

There is no exact relationship between the doses of Diamerid and other oral hypoglycemic agents. When another oral hypoglycemic agent is replaced by Diameride®, it is recommended that the administration procedure be the same as for the original administration of Diameride®, that is, treatment should begin with an initial dose of 1 mg (even if the patient is transferred to the drug Diamerid® with the maximum dose of another hypoglycemic drug for oral administration). Any dose increase should be done in stages, taking into account the response to glimepiride, in accordance with the above recommendations.

The strength and duration of the effect of the previous oral hypoglycemic agent must be taken into account. Interruption of treatment may be necessary to avoid any additive effects that could increase the risk of hypoglycemia.

Use in combination with metformin

In patients with inadequately controlled diabetes mellitus who are taking maximum daily doses of either glimepiride or metformin, treatment with a combination of these two drugs may be initiated. In this case, previous treatment with either glimepiride or metformin is continued at the same dose level, and additional metformin or glimepiride is started at a low dose, which is then titrated depending on the target level of metabolic control up to the maximum daily dose. Combination therapy should be initiated under close medical supervision.

Use in combination with insulin

In patients with inadequately controlled diabetes mellitus, insulin may be administered concomitantly when taking maximum daily doses of glimepiride. In this case, the last dose of glimepiride prescribed to the patient remains unchanged. In this case, insulin treatment begins with low doses, which are gradually increased under the control of blood glucose concentrations. Combination treatment requires careful medical supervision.

Use in patients with renal failure

There is a limited amount of information on the use of Diamerid® in patients with renal failure. Patients with impaired renal function may be more sensitive to the hypoglycemic effect of glimepiride (see sections “Pharmacokinetics”, “Contraindications”),

Use in patients with liver failure

There is a limited amount of information on the use of the drug in liver failure (see sections “Contraindications”),

Use in children

There is insufficient data on the use of the drug in children.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25°C.

Keep out of the reach of children.

Best before date

2 years. Do not use after the expiration date.

special instructions

Glimepiride should be taken at the recommended doses and at the prescribed times. The patient should immediately inform the doctor if the dose of the drug is too high.

The development of hypoglycemia in a patient after taking 1 mg of glimepiride per day means that glycemia can be controlled solely through diet.

When compensation for type 2 diabetes mellitus is achieved, insulin sensitivity increases. In this regard, the need for glnmepiride may decrease during treatment. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or discontinue glimepiride. Dose adjustment should also be carried out if the patient’s body weight changes, his lifestyle changes, or if other factors appear that increase the risk of developing hypo- or hyperglycemia.

Adequate diet, regular and sufficient exercise and, if necessary, weight loss are as important for achieving optimal control of blood glucose concentrations as regular use of glimepiride.

Clinical symptoms of hyperglycemia are: increased frequency of urination, extreme thirst, dry mouth and dry skin.

In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly careful monitoring of the patient. During treatment with glimepiride, hypoglycemia may develop if you eat irregularly or skip meals. Factors contributing to the development of hypoglycemia include:

reluctance or (especially in old age) insufficient ability of the patient to cooperate with the doctor;
inadequate, irregular nutrition, skipping meals, fasting, changing the usual diet;
imbalance between physical activity and carbohydrate intake;
drinking alcohol, especially in combination with skipping meals;
dysfunction of the night;
severe liver dysfunction;
overdose of glimepiride;
some uncompensated diseases of the endocrine system that affect carbohydrate metabolism (for example, dysfunction of the thyroid gland and anterior pituitary gland or adrenal insufficiency);

simultaneous use of certain other drugs (see section “Interaction with other drugs”).

The doctor should be informed about the above factors and about episodes of hypoglycemia, since they require particularly strict monitoring of the patient. If such factors are present that increase the risk of hypoglycemia, the dose of glimepiride or the entire treatment regimen should be adjusted. This must also be done in the case of an intercurrent illness or a change in the patient’s lifestyle. Symptoms of hypoglycemia may be smoothed out or completely absent in the elderly, in patients with autonomic neuropathy or receiving concomitant treatment with beta-blockers, clonidine, reserpine, guanethidine. Hypoglycemia can almost always be quickly reversed by immediate intake of carbohydrates (glucose or sugar, for example in the form of a sugar cube, sweet fruit juice or tea). In this regard, the patient should always have at least 20 g of glucose (4 lumps of sugar) with him. Sweeteners are ineffective in treating hypoglycemia.

From the experience of using other sulfonylurea drugs, it is known that despite the initial success in relieving hypoglycemia, its relapse is possible. In this regard, continuous and careful monitoring of the patient is necessary. Severe hypoglycemia requires immediate treatment under medical supervision, and under certain circumstances, hospitalization of the patient.

If a patient with diabetes is treated by different doctors (for example, while staying in the hospital after an accident, when sick on the weekend), he must inform them about his illness and previous treatment.

Treatment with sulfonylurea derivatives, which include glimepiride, can lead to the development of hemolytic anemia, therefore, in patients with glucose-6-phosphate dehydrogenase deficiency, special care should be taken when prescribing glimepiride, and it is better to use hypoglycemic agents that are not sulfonylurea derivatives.

During treatment with glimepiride, regular monitoring of liver function and peripheral blood patterns (especially the number of leukocytes and platelets) is required.

In stressful situations (for example, trauma, surgery, infectious diseases accompanied by fever), it may be necessary to temporarily transfer the patient to insulin therapy.

There is no experience with the use of glimepiride in patients with severely impaired liver and kidney function or patients on hemodialysis. Patients with severely impaired renal and liver function are advised to switch to insulin therapy. During treatment with glimepiride, regular monitoring of blood glucose concentrations, as well as the concentration of glycosylated hemoglobin, is necessary.

Certain side effects (severe hypoglycemia, serious changes in the blood picture, severe allergic reactions, liver failure) may, under certain circumstances, pose a threat to the patient's life. In the event of the development of undesirable or severe reactions, the patient must immediately inform the attending physician about them and in no case continue to take the drug without his recommendation.

Description

Oral hypoglycemic drug.

Dosage form

Tablets are pink with a brownish tint, flat-cylindrical, with a bevel; Minor inclusions are allowed.

Use in children

Contraindicated for use in children and adolescents under 18 years of age.

Pharmacodynamics

Oral hypoglycemic agent, sulfonylurea derivative. Stimulates insulin secretion by pancreatic β-cells, increases insulin release. Increases the sensitivity of peripheral tissues to insulin.

Side effects

Metabolic: hypoglycemia, hyponatremia.

From the digestive system: nausea, vomiting, discomfort in the epigastrium, abdominal pain, diarrhea, increased activity of liver transaminases, cholestasis, jaundice, hepatitis (up to the development of liver failure).

From the hematopoietic system: thrombocytopenia, leukopenia, erythropenia, granulocytopenia, agranulocytosis, pancytopenia, hemolytic anemia.

From the organ of vision: transient visual impairment.

Allergic reactions: itching, urticaria, skin rash; rarely - dyspnea, drop in blood pressure, anaphylactic shock, allergic vasculitis, photosensitivity.

Use during pregnancy and breastfeeding

Contraindicated for use during pregnancy. In case of planned pregnancy or pregnancy, the woman should be switched to insulin.

During lactation, a woman should be switched to insulin.

Experimental studies have shown that glimepiride is excreted in breast milk.

Interaction

Strengthening the hypoglycemic effect of glimepiride is possible with simultaneous use with insulin or other hypoglycemic drugs, ACE inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, pheniramidol, fibrates, fluoxetine, guanethidine, isophosphamide ami, MAO inhibitors , miconazole, PAS, pentoxifylline (when administered in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, sulfonamides, tetracyclines.

Weakening of the hypoglycemic effect of glimepiride is possible with simultaneous use with acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine (adrenaline) and other sympathomimetics, glucagon, laxatives (after long-term use), nicotinic acid (in high doses), estrogens and progestogens, phenothiazine , phenytoin, rifampicin, thyroid hormones.

When used simultaneously, histamine H2 receptor blockers, clonidine and reserpine can both potentiate and reduce the hypoglycemic effect of glimepiride.

The use of glimepiride may enhance or weaken the effect of coumarin derivatives.

Ethanol may enhance or weaken the hypoglycemic effect of glimepiride.

Overdose

After ingestion of a large dose of glimepiride, hypoglycemia may develop, lasting from 12 to 72 hours, which may recur after the initial restoration of blood glucose concentrations. Acute overdose, as well as long-term treatment with too high doses of glimepiride, can lead to the development of severe life-threatening hypoglycemia.

Symptoms of hypoglycemia: increased sweating, anxiety, tachycardia, increased blood pressure, palpitations, pain in the heart, arrhythmia, headache, dizziness, sudden increase in appetite, nausea, vomiting, apathy, sniffling, anxiety, aggressiveness, impaired concentration, depression, tremor, paresis, sensory disturbances, convulsions of central origin. In addition, symptoms such as cold clammy sweat, shallow breathing, bradycardia, speech and visual disturbances, aphasia, delirium, impaired self-control, vigilance and reaction speed, impaired consciousness or loss of consciousness, even coma, may occur. Sometimes the clinical picture of hypoglycemia can resemble a stroke.

Treatment: Hypoglycemia can be relieved by immediate intake of carbohydrates (glucose or a lump of sugar, sweet fruit juice or tea). In most cases, observation in a hospital setting is recommended.

Treatment includes inducing vomiting, drinking plenty of activated charcoal (an adsorbent) and sodium picosulfate (a laxative). When taking a large amount of the drug, gastric lavage is indicated, followed by sodium picosulfate and activated charcoal. Dextrose is started as soon as possible, if necessary in the form of an intravenous bolus of 50 ml of a 40% solution, followed by an infusion of a 10% solution, with careful monitoring of blood glucose concentrations. As an alternative for adults, glucagon can be administered intravenously, subcutaneously or intramuscularly at a dose of 0.5-1 mg. Further treatment should be symptomatic.

When treating hypoglycemia due to accidental ingestion of glimepiride in infants or young children, the dose of dextrose administered should be carefully adjusted to reflect the potential for dangerous hyperglycemia; administration of dextrose should be carried out under constant monitoring of blood glucose concentrations.

After rapid restoration of blood glucose concentrations, an intravenous infusion of a dextrose solution at a lower concentration is imperative to prevent the resumption of hypoglycemia. Blood glucose concentrations in such patients should be continuously monitored over a 24-hour period. In severe cases with prolonged hypoglycemia, the risk of reducing blood glucose concentrations to hypoglycemic levels may persist for several days.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Directions for use and dosage

Diameride is taken orally.

The tablets are taken without chewing, whole, with a sufficient amount of liquid (about 100 ml). After taking the drug, skipping meals is not recommended.

The doctor determines the dosage regimen individually, based on the results of regular monitoring of blood glucose concentrations.

At the beginning of therapy, Diameride is prescribed 1 mg per day. After achieving the optimal therapeutic effect, this dose is recommended to be taken as a maintenance dose.

In cases of lack of glycemic control, the daily dose should be increased gradually (with intervals of 1–2 weeks) under regular monitoring of blood glucose concentrations to 2, 3 or 4 mg per day. Higher doses are effective only in exceptional cases. Maximum – 6 mg per day.

The time and frequency of taking the drug are determined by the doctor. The regimen for using Diameride should take into account the patient’s lifestyle. The daily dose should be taken in 1 dose immediately before or during a hearty breakfast or the first main meal.

Diameride is intended for long-term therapy, which should be carried out under the control of blood glucose levels.

In cases of lack of glycemic control in patients taking metformin, Diameride may be additionally prescribed.

The dose of metformin usually does not change; Diameride at the beginning of therapy should be prescribed at a minimum dose, which is gradually increased up to the maximum. Combination therapy should be carried out under the close supervision of a specialist.

If it is not possible to achieve glycemic control when taking the maximum dose of Diameride as monotherapy, additional insulin may be prescribed, which is prescribed in a minimum dose at the beginning of therapy. If necessary, it can be gradually increased. Combination therapy should be carried out under the close supervision of a specialist.

When transferring a patient from another oral hypoglycemic drug to Diamerid, its initial daily dose should be 1 mg (even in cases where the patient is transferred from the maximum dose of another oral hypoglycemic drug). Any increase in the dose of Diameride should be carried out in stages in accordance with the above recommendations. The effectiveness, dose and duration of action of the hypoglycemic agent used should be taken into account. In some cases, especially when taking hypoglycemic drugs with a long half-life, it may be necessary to temporarily discontinue therapy over several days to avoid additive effects that increase the likelihood of hypoglycemia.

When carrying out insulin therapy in patients with type 2 diabetes mellitus, with compensation of the disease and with preserved secretory function of pancreatic β-cells, in exceptional cases it is possible to replace insulin with Diameride (minimum doses are used at the beginning of therapy). Translation must be carried out under the close supervision of a specialist.

Diamerid tablets 2mg bl N10x3 Akrikhin

As a rule, the dose of Diamerid is determined by the target blood glucose concentration. The lowest dose sufficient to achieve the required metabolic control should be used. During treatment with Diamerid, it is necessary to regularly determine the concentration of glucose in the blood. In addition, regular monitoring of the level of glycosylated hemoglobin is recommended. Incorrect use of the drug, such as missing a dose, should never be made up for by taking a subsequent higher dose. The patient’s actions in case of errors when taking the drug Diamerid (in particular, when missing a dose or skipping a meal) or in situations where it is not possible to take the drug should be discussed between the patient and the doctor in advance. Taking the drug Diamerid. Diamerid tablets are taken orally, without chewing, with a sufficient amount of liquid (about 0.5 cups). Initial dose and dose selection. The starting dose is 1 mg glimepiride once daily. If necessary, the daily dose can be gradually (at intervals of 1-2 weeks) increased. It is recommended that the dose be increased under regular monitoring of blood glucose concentrations and in accordance with the following dose increase step: 1 mg - 2 mg - 3 mg - 4 mg - 6 mg (- 8 mg). Dose range in patients with well-controlled diabetes mellitus. The usual daily dose in patients with well-controlled diabetes mellitus is 1-4 mg glimepiride. A daily dose of more than 6 mg is more effective in only a small number of patients. Dosage regimen. The time for taking Diamerid and the distribution of doses during the day is determined by the doctor, depending on the patient’s lifestyle at a given time (time of meals, amount of physical activity). Usually, a single dose of Diamerid during the day is sufficient. It is recommended that in this case the entire dose of Diamerid be taken immediately before a full breakfast or, if not taken at this time, immediately before the first main meal. It is very important not to skip meals after taking Diamerid. Since improved metabolic control is associated with increased insulin sensitivity, the need for glimepiride may decrease during treatment. In order to avoid the development of hypoglycemia, it is necessary to promptly reduce the dose or stop taking the drug Diamerid. Conditions that may also require dose adjustment of glimepiride: • weight loss in the patient; • changing the patient's lifestyle (changes in diet, meal times, amount of physical activity); • the occurrence of other factors that lead to a predisposition to the development of hypoglycemia or hyperglycemia. Duration of treatment. Treatment with glimepiride is usually long-term. Transferring the patient from taking another oral hypoglycemic drug to taking Diamerid. There is no exact relationship between the doses of Diamerid and other oral hypoglycemic agents. When another oral hypoglycemic agent is replaced by Diameride, it is recommended that the administration procedure be the same as for the initial administration of Diameride, that is, treatment should begin with an initial dose of 1 mg (even if the patient is switched to the drug Diameride with the maximum dose of another hypoglycemic drug for oral administration). Any dose increase should be done in stages, taking into account the response to glimepiride, in accordance with the above recommendations. The strength and duration of the effect of the previous oral hypoglycemic agent must be taken into account. Interruption of treatment may be necessary to avoid any additive effects that could increase the risk of hypoglycemia. Use in combination with metformin. In patients with inadequately controlled diabetes mellitus who are taking maximum daily doses of either glimepiride or metformin, treatment with a combination of these two drugs may be initiated. In this case, previous treatment with either glimepiride or metformin is continued at the same dose level, and additional metformin or glimepiride is started at a low dose, which is then titrated depending on the target level of metabolic control up to the maximum daily dose. Combination therapy should be initiated under close medical supervision. Use in combination with insulin. In patients with inadequately controlled diabetes mellitus, insulin may be administered concomitantly when taking maximum daily doses of glimepiride. In this case, the last dose of glimepiride prescribed to the patient remains unchanged. In this case, insulin treatment begins with low doses, which are gradually increased under the control of blood glucose concentrations. Combination treatment requires careful medical supervision. Use in patients with renal failure. There is a limited amount of information on the use of Diamerid in patients with renal failure. Patients with impaired renal function may be more sensitive to the hypoglycemic effect of glimepiride. Use in patients with liver failure. There is limited information on the use of the drug in liver failure. Use in children. There is insufficient data on the use of the drug in children.

Side effects

organ of vision: transient visual impairment (observed, as a rule, at the beginning of therapy; caused by changes in the concentration of glucose in the blood);
metabolism: hypoglycemic reactions (develop mainly soon after taking Diameride and can occur in severe forms; they are not always easy to stop; their occurrence is largely determined by individual factors, especially nutrition and the dose used);
hematopoietic system: thrombocytopenia (moderate/severe), leukopenia, granulocytopenia, erythrocytopenia, aplastic/hemolytic anemia, pancytopenia, agranulocytosis;
digestive system: vomiting, nausea, feeling of discomfort/heaviness in the epigastrium, abdominal pain, diarrhea (this leads to discontinuation of the drug in very rare cases), increased activity of liver enzymes, jaundice, cholestasis, hepatitis (sometimes with the development of liver failure);
dermatological reactions: in some cases - porphyria cutanea tarda, photosensitivity;
allergic reactions: urticaria (in the form of itching, skin rash; is usually moderate in nature, but can progress, accompanied by shortness of breath, a drop in blood pressure, up to the development of anaphylactic shock; requires immediate contact with a specialist), cross-allergy with other sulfonamides, sulfonylurea derivatives or other sulfonamides, allergic vasculitis;
others: in some cases – hyponatremia, asthenia, headache.

special instructions

Patients must adhere to the prescribed dosage regimen. Missing a single dose cannot be compensated for by subsequent doses of a higher dose.

The occurrence of hypoglycemia after taking 1 mg of Diameride means that glycemia can be controlled solely through diet.

When compensation for type 2 diabetes mellitus is achieved, an increase in insulin sensitivity is observed. In this regard, during therapy the need for Diameride may decrease. To avoid the development of hypoglycemia, you need to temporarily reduce the dose or discontinue treatment. Dose adjustment is also required in cases of changes in the patient’s weight, lifestyle, or when other factors appear that increase the likelihood of hyper- or hypoglycemia.

To achieve optimal blood glucose control, as well as taking the drug regularly, it is important to maintain an adequate diet and perform regular and sufficient exercise.

Clinical symptoms of hyperglycemia include extreme thirst, increased frequency of urination, dry skin, and dry mouth.

In the first weeks of using Diameride, the likelihood of hypoglycemia may increase (in these cases, particularly careful monitoring of the patient's condition is required). Hypoglycemia may occur if you eat irregularly or skip meals.

The main factors contributing to the occurrence of hypoglycemia:

unwillingness/insufficient ability (especially in old age) of the patient to cooperate with the doctor;
eating disorders, including changes in the usual diet, fasting, irregular/poor nutrition, skipping meals;
drinking alcohol, especially in combination with skipping meals;
imbalance between carbohydrate intake and physical activity;
severe liver dysfunction;
overdose of Diameride;
impaired renal function;
combined use with certain other drugs;
some uncompensated diseases of the endocrine system that affect carbohydrate metabolism, including thyroid dysfunction, adrenal insufficiency or pituitary insufficiency.

The presence/appearance of the above factors, as well as episodes of hypoglycemia, should be reported to the doctor, since in these cases particularly careful monitoring of the patient’s condition is required. If these factors are present, dose adjustment/entire treatment regimen may be required. Similar measures are taken in cases of intercurrent illness or when the patient’s lifestyle changes.

In elderly patients, in patients with autonomic neuropathy or in patients receiving simultaneous therapy with guanethidine, beta-blockers, reserpine, clonidine, symptoms of hypoglycemia may be smoothed out or absent altogether.

Hypoglycemia can in almost all cases be quickly reversed by immediate intake of carbohydrates (sugar or glucose). In this regard, the patient should always have at least 20 g of glucose (4 lumps of sugar) with him. Sweeteners are ineffective in treating hypoglycemia.

Despite the initial success of relieving hypoglycemia, its relapse may occur, which requires constant monitoring of the patient's condition. Severe hypoglycemia requires immediate treatment under specialist supervision and sometimes hospitalization.

During therapy, it is necessary to regularly monitor liver function and peripheral blood patterns (this especially applies to the number of platelets and leukocytes).

In stressful situations (for example, injuries, surgery, infectious diseases accompanied by fever), it may be necessary to transfer the patient to insulin.

There is no experience with the use of Diameride in patients with severe renal/hepatic dysfunction or in patients on hemodialysis (the use of insulin is indicated).

During therapy, the concentration of glucose in the blood, as well as the concentration of glycosylated hemoglobin, should be regularly monitored.

Some adverse reactions (in the form of severe hypoglycemia, serious changes in the blood picture, severe allergic reactions, liver failure) under certain circumstances can be life-threatening. In cases of severe/undesirable reactions, the patient should immediately inform the specialist about them. You should not continue taking the drug on your own.

At the beginning of the course, when switching from one drug to another or when taking Diameride irregularly, a decrease in concentration and speed of psychomotor reactions due to hyper- or hypoglycemia may occur, which affects the ability to drive vehicles. Patients should take measures to prevent the occurrence of these conditions. Patients who have no/reduced severity of warning symptoms are advised to stop driving.

Instructions:

Clinical and pharmacological group

15.014 (Oral hypoglycemic drug)

Release form, composition and packaging

Tablets of pink color with a brown tint, flat-cylindrical, with a bevel; Minor inclusions are allowed.

1 tab.
glimepiride	1 mg

Excipients: lactose monohydrate, povidone, poloxamer, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, red iron oxide dye.

10 pieces. — cellular contour packages (3) — cardboard packs.

Tablets from cream to light yellow or yellow, flat-cylindrical, chamfered; Minor inclusions are allowed.

1 tab.
glimepiride	2 mg

Excipients: lactose monohydrate, povidone, poloxamer, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, iron oxide yellow dye.

10 pieces. — cellular contour packages (3) — cardboard packs.

Tablets of pink color with a brown tint, flat-cylindrical, with a bevel; Minor inclusions are allowed.

1 tab.
glimepiride	3 mg

Excipients: lactose monohydrate, povidone, poloxamer, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, red iron oxide dye.

10 pieces. — cellular contour packages (3) — cardboard packs.

Tablets from cream to light yellow or yellow, flat-cylindrical, chamfered; Minor inclusions are allowed.

1 tab.
glimepiride	4 mg

Excipients: lactose monohydrate, povidone, poloxamer, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, iron oxide yellow dye.

10 pieces. — cellular contour packages (3) — cardboard packs.

pharmachologic effect

An oral hypoglycemic drug is a third generation sulfonylurea derivative.

Glimepiride acts primarily by stimulating the secretion and release of insulin from the beta cells of the pancreas (pancreatic action). As with other sulfonylureas, this effect is based on an increase in the response of pancreatic β-cells to physiological stimulation by glucose, while the amount of insulin secreted is significantly less than with the action of traditional sulfonylurea drugs. The least stimulating effect of glimepiride on insulin secretion also provides a lower risk of developing hypoglycemia.

In addition to this, glimepiride has an extrapancreatic effect - the ability to improve the sensitivity of peripheral tissues (muscle, fat) to the action of its own insulin, reduce the absorption of insulin by the liver; inhibits glucose production in the liver. Glimepiride selectively inhibits COX and reduces the conversion of arachidonic acid to thromboxane A2, which promotes platelet aggregation, thus exerting an antiplatelet effect.

Glimepiride helps normalize lipid levels, reduces the concentration of malonaldehyde in the blood, which leads to a significant reduction in lipid peroxidation, which contributes to the antiatherogenic effect of the drug.

Glimepiride increases the level of endogenous α-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase, which helps reduce the severity of oxidative stress in the patient’s body, which is constantly present in type 2 diabetes mellitus.

Pharmacokinetics

Suction

With repeated doses of glimepiride at a daily dose of 4 mg, Cmax in the blood serum is achieved after approximately 2.5 hours and is 432 ng/ml; There is a linear relationship between dose and Cmax, as well as between dose and AUC. When glimepiride is taken orally, its bioavailability is approximately 100%. Food intake does not have a significant effect on absorption, with the exception of a slight slowdown in the rate of absorption.

Distribution

Glimepiride is characterized by a very low Vd (about 8.8 l), approximately equal to the Vd of albumin, a high degree of binding to plasma proteins (more than 99%) and low clearance (about 48 ml/min).

Glimepiride passes into breast milk and through the placental barrier. The drug does not penetrate the BBB well.

Removal

After a single dose of glimepiride, 58% is excreted orally by the kidneys and 35% through the intestines. No unchanged substance was detected in the urine. T1/2 at plasma concentrations of the drug in serum corresponding to multiple doses is 5-8 hours. After administration in high doses, T1/2 increases slightly.

Pharmacokinetics in special clinical situations

In patients with impaired renal function, there is a tendency for the clearance of glimepiride to increase and for its mean serum concentrations to decrease, which is likely due to more rapid elimination of the drug due to its lower binding to plasma proteins. Thus, in this category of patients there is no additional risk of drug accumulation.

Dosage

The drug is used orally. The initial and maintenance doses of glimepiride are set individually based on the results of regular monitoring of blood glucose concentrations.

Initial dose and dose selection

At the beginning of treatment, the drug is prescribed at a dose of 1 mg 1 time / day. When the optimal therapeutic effect is achieved, it is recommended to take this dose as a maintenance dose.

In the absence of glycemic control, the daily dose should be gradually increased under regular monitoring of blood glucose concentrations (at intervals of 1-2 weeks) to 2 mg, 3 mg or 4 mg per day. Doses above 4 mg/day are effective only in exceptional cases. The maximum recommended daily dose is 6 mg.

The time and frequency of taking the daily dose is determined by the doctor, taking into account the patient’s lifestyle. The daily dose is prescribed in 1 dose immediately before or during a hearty breakfast, or the first main meal. The tablets are taken whole, without chewing, with a sufficient amount of liquid (about 0.5 cups). It is not recommended to skip meals after taking Diameride.

Duration of treatment

Treatment with Diamerid® is long-term, under the control of blood glucose levels.

Use in combination with metformin

In the absence of glycemic control in patients taking metformin, concomitant therapy with Diamerid® may be started. While maintaining the dose of metformin at the same level, treatment with Diamerid® begins with a minimum dose, and then gradually increases it depending on the desired level of glycemic control, up to the maximum daily dose. Combination therapy should be carried out under close medical supervision.

Use in combination with insulin

In cases where it is not possible to achieve glycemic control by taking the maximum dose of Diameride alone or in combination with the maximum dose of metformin, a combination of glimepiride with insulin is possible. In this case, the last prescribed dose of glimepiride remains unchanged. In this case, insulin treatment should begin with a minimum dose, with a possible subsequent gradual increase in its dose under the control of blood glucose concentrations. Combined treatment requires mandatory medical supervision.

Transferring a patient from another oral gynoglycemic drug to glumenuride

When transferring a patient from another oral hypoglycemic drug to Diamerid®, the initial daily dose of the latter should be 1 mg (even if the patient is transferred to Diamerid® from the maximum dose of another oral hypoglycemic drug). Any increase in the dose of Diameride should be carried out in stages in accordance with the recommendations above. It is necessary to take into account the effectiveness, dose and duration of action of the hypoglycemic drug used. In some cases, especially when taking hypoglycemic drugs with a long half-life, it may be necessary to temporarily (for several days) discontinue treatment to avoid additive effects that increase the risk of hypoglycemia.

Transferring a patient from insulin to glumeniride

In exceptional cases, during insulin therapy in patients with type 2 diabetes mellitus, with compensation of the disease and with preserved secretory function of pancreatic β-cells, it is possible to replace insulin with glimepiride. The transfer should be carried out under the close supervision of a physician. In this case, transferring the patient to Diamerid® begins with a minimum dose of 1 mg.

Overdose

Symptoms: after oral administration of glimepiride in a high dose, hypoglycemia may develop, lasting from 12 hours to 72 hours, which may recur after the initial restoration of blood glucose concentrations. In most cases, observation in a hospital setting is recommended.

Treatment: induction of vomiting, drinking plenty of activated carbon (adsorbent) and sodium picosulfate (laxative). When taking a large amount of the drug, gastric lavage is indicated, followed by sodium picosulfate and activated charcoal. The administration of dextrose should be started as soon as possible, if necessary - 50 ml of a 40% solution intravenously, followed by an infusion of a 10% solution, with careful monitoring of blood glucose concentrations. Subsequently, symptomatic therapy is carried out.

Drug interactions

The simultaneous use of glimepiride with certain drugs can cause either an increase or decrease in the hypoglycemic effect of the drug. Therefore, other medications can only be taken after consultation with your doctor.

An increase in hypoglycemic effect and the associated possible development of hypoglycemia can be observed with simultaneous use of glimepiride with insulin, metformin or other oral hypoglycemic drugs, ACE inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, trophosphamide and isofosfamide, fenfluramine , fibrates, fluoxetine, sympatholytics (guanethidine), MAO inhibitors, miconazole, pentoxifylline (when administered parenterally in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolone antibiotics, salicylates and aminosalicylic acid, sulfinpyrazone, some long-acting sulfonamides actions, tetracyclines, tritoqualine, fluconazole.

A weakening of the hypoglycemic effect and an associated increase in the concentration of glucose in the blood can be observed with the simultaneous use of glimepiride with acetazolamide, barbiturates, corticosteroids, diazoxide, saluretics, thiazide diuretics, epinephrine and other sympathomimetic drugs, glucagon, laxatives (with long-term use), nicotinic acid (in high doses) and nicotinic acid derivatives, estrogens and progestogens, phenothiazine derivatives, incl. chlorpromazine, phenytoin, rifampicin, thyroid hormones, lithium salts.

H2-histamine receptor blockers, clonidine and reserpine can both potentiate and weaken the hypoglycemic effect of glimepiride.

Under the influence of beta-blockers, clonidine, guanethidine and reserpine, clinical signs of hypoglycemia may be weakened or absent.

While taking glimepiride, an increase or decrease in the effect of coumarin derivatives may be observed.

When used simultaneously with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.

Single or chronic consumption of alcohol can either enhance or weaken the hypoglycemic effect of glimepiride.

Use during pregnancy and lactation

Glimepiride is contraindicated for use during pregnancy. In case of planned pregnancy or if pregnancy occurs, the woman should be transferred to insulin therapy.

Because Since glimepiride is excreted in breast milk, it should not be prescribed during lactation. In this case, it is necessary to switch to insulin therapy or stop breastfeeding.

Side effects

Metabolism: hypoglycemic reactions may develop. These reactions mainly occur soon after taking the drug, can be severe in form and course, and cannot always be easily controlled. The development of these symptoms depends on individual factors such as diet and dosage.

On the part of the organ of vision: during treatment (especially at the beginning), transient visual impairment may be observed due to changes in the concentration of glucose in the blood.

From the digestive system: nausea, vomiting, feeling of heaviness or discomfort in the epigastrium, abdominal pain, diarrhea, very rarely leading to cessation of treatment; increased activity of liver enzymes, cholestasis, jaundice, hepatitis (up to the development of liver failure).

From the hematopoietic system: thrombocytopenia (moderate to severe), leukopenia, hemolytic or aplastic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia.

Allergic reactions: possible appearance of urticaria (itching, skin rash). Such reactions are usually moderate, but can progress, accompanied by a drop in blood pressure, shortness of breath, and even the development of anaphylactic shock. If hives appear, you should consult a doctor immediately. Cross-allergy with other sulfonylurea derivatives, sulfonamides or other sulfonamides is possible, and the development of allergic vasculitis is also possible.

Dermatological reactions: in some cases - photosensitivity, porphyria cutanea tarda.

Other: in some cases - headache, asthenia, hyponatremia.

Storage conditions and periods

The drug should be stored out of the reach of children, in a dry place, protected from light, at a temperature not exceeding 25°C. Shelf life: 2 years.

Indications

- type 2 diabetes mellitus when the previously prescribed diet and physical activity are ineffective.

If monotherapy with glimepiride is ineffective, it can be used as part of combination therapy with metformin or insulin.

Contraindications

— diabetes mellitus type 1;

- diabetic ketoacidosis, diabetic precoma and coma;

— conditions accompanied by impaired absorption of food and the development of hypoglycemia (including infectious diseases);

- leukopenia;

- severe liver dysfunction;

- severe renal dysfunction (including patients on hemodialysis);

- pregnancy;

- lactation period;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

- children under 18 years of age;

- hypersensitivity to the components of the drug;

- hypersensitivity to other sulfonylurea derivatives or to sulfonamide drugs (risk of developing hypersensitivity reactions).

The drug is prescribed with caution for conditions that require transferring the patient to insulin therapy (including extensive burns, severe multiple injuries, major surgical interventions, as well as for impaired absorption of food and drugs from the gastrointestinal tract - intestinal obstruction, gastric paresis).

special instructions

Diameride® should be taken in recommended doses and at the prescribed time. Errors in use of the drug, such as missing doses, should never be corrected by subsequent administration of a higher dose. The doctor and the patient should discuss in advance the measures that should be taken in case of such errors (for example, skipping a drug dose or meal) or in situations where it is impossible to take the next dose of the drug at the prescribed time. The patient should immediately inform the doctor if the dose of the drug is too high.

The development of hypoglycemia in a patient after taking Diameride at a dose of 1 mg/day means that glycemia can be controlled solely through diet.

When compensation for type 2 diabetes mellitus is achieved, insulin sensitivity increases. In this regard, the need for glimepiride may decrease during treatment. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or discontinue Diamerid®. Dose adjustment should also be carried out if the patient’s body weight changes, his lifestyle changes, or if other factors appear that increase the risk of developing hypo- or hyperglycemia.

An adequate diet, regular and sufficient exercise and, if necessary, weight loss are as important for achieving optimal blood glucose control as regular use of glimepiride.

Clinical symptoms of hyperglycemia are: increased frequency of urination, extreme thirst, dry mouth and dry skin.

In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly careful monitoring of the patient. During treatment with Diamerid, hypoglycemia may develop if you eat irregularly or skip meals. Factors contributing to the development of hypoglycemia include:

- reluctance or (especially in old age) insufficient ability of the patient to cooperate with the doctor;

- inadequate, irregular nutrition, skipping meals, fasting, changing the usual diet;

— imbalance between physical activity and carbohydrate consumption;

- alcohol consumption, especially in combination with skipping meals;

- renal dysfunction;

- severe liver dysfunction;

- overdose of glimepiride;

- some uncompensated diseases of the endocrine system that affect carbohydrate metabolism (for example, dysfunction of the thyroid gland, pituitary insufficiency or adrenal insufficiency);

- simultaneous use of certain other drugs.

Symptoms of hypoglycemia may be smoothed out or completely absent in elderly patients, in patients with autonomic neuropathy or receiving concomitant treatment with beta-blockers, clonidine, reserpine, guanethidine. Hypoglycemia can almost always be quickly reversed by immediate intake of carbohydrates (glucose or sugar, for example in the form of a sugar cube, sweet fruit juice or tea). In this regard, the patient should always have at least 20 g of glucose (4 lumps of sugar) with him. Sweeteners are ineffective in treating hypoglycemia.

From the experience of using other sulfonylurea drugs, it is known that despite the initial success in relieving hypoglycemia, its recurrence is possible. In this regard, continuous and careful monitoring of the patient is necessary. Severe hypoglycemia requires immediate treatment under medical supervision, and under certain circumstances, hospitalization of the patient.

During treatment with Diamerid®, regular monitoring of liver function and peripheral blood patterns (especially the number of leukocytes and platelets) is required.

In stressful situations (for example, trauma, surgery, infectious diseases accompanied by fever), it may be necessary to temporarily transfer the patient to insulin therapy.

During treatment with glimepiride, regular monitoring of blood glucose concentrations, as well as the concentration of glycosylated hemoglobin, is necessary.

Certain adverse reactions (severe hypoglycemia, serious changes in blood count, severe allergic reactions, liver failure) may, under certain circumstances, pose a threat to the patient's life. In the event of the development of undesirable or severe reactions, the patient should immediately inform the attending physician about them and in no case continue to take the drug without his recommendation.

Impact on the ability to drive vehicles and operate machinery

At the beginning of treatment, when switching from one drug to another, or when taking the drug Diamerid® irregularly, a decrease in concentration and speed of psychomotor reactions of the patient may occur due to hypo- or hyperglycemia. This may adversely affect the ability to drive vehicles or operate various machines and mechanisms. Patients should be advised to take measures to prevent the development of hypoglycemia and hyperglycemia when driving vehicles and operating machinery. This is especially important for patients with no or decreased severity of symptoms that are warning signs of developing hypoglycemia or who suffer from frequent episodes of hypoglycemia. In these cases, the feasibility of performing such work should be considered.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Drug interactions

When Diameride is used in combination with certain drugs/substances, the following effects may develop (before prescribing any drug, medical advice is required):

acetazolamide, barbiturates, glucocorticosteroids, diazoxide, saluretics, thiazide diuretics, epinephrine and other sympathomimetic agents, glucagon, laxatives (with prolonged use), nicotinic acid derivatives, nicotinic acid (in high doses), estrogens, progestogens, phenothiazine derivatives, including chlorpromazine , phenytoin, rifampicin, thyroid hormones, lithium salts: weakening of the hypoglycemic effect and, as a consequence, an increase in the concentration of glucose in the blood;
insulin, metformin or other oral hypoglycemic drugs, angiotensin-converting enzyme inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, trophosphamide and isophosphamide, fenfluramine, fibrates, fluoxetine, sympatholytics (guanethidine), monoamine oxidase inhibitors, miconazole, pentoxifylline (with parenteral administration of high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolone antibiotics, salicylates and aminosalicylic acid, sulfinpyrazones, some long-acting sulfonamides, tetracyclines, tritoqualine, fluconazole: increased hypoglycemic effect and, as a result, the likelihood of hypoglycemia;
reserpine, clonidine, H2-histamine receptor blockers: potentiation/weakening of the hypoglycemic effect of Diameride;
drugs that inhibit bone marrow hematopoiesis: increased likelihood of myelosuppression;
coumarin derivatives: strengthening/weakening of their action;
beta-blockers, clonidine, reserpine, guanethidine: weakening or absence of clinical signs of hypoglycemia;
alcohol (chronic/single use): strengthening/weakening of the hypoglycemic effect of Diameride.