Glimepiride instructions for use reviews. Glimepiride: instructions for use

In this article, you can read the instructions for use medicinal product Glimepiride. Reviews of site visitors - consumers are presented this medicine, as well as the opinions of medical specialists on the use of glimepiride in their practice. A big request to actively add your reviews about the drug: did the medicine help or not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Glimepiride analogs, if available structural analogues. Use to treat non-insulin-dependent type 2 diabetes mellitus and lower blood sugar levels in adults, children, and pregnancy and lactation. The composition of the drug.

Glimepiride- oral hypoglycemic agent, a sulfonylurea derivative. Stimulates the secretion of insulin by the beta cells of the pancreas, increases the release of insulin. Increases the sensitivity of peripheral tissues to insulin.

Compound

Glimepiride + Excipients.

Glimepiride + Metformin + excipients (Amaryl M).

Pharmacokinetics

Eating does not significantly affect absorption. Plasma protein binding is over 99%. undergoes metabolism. The hydroxylated and carboxylated metabolites of glimepiride appear to be formed as a result of hepatic metabolism and are found in urine and feces. After a single oral dose of radiolabeled glimepiride, 58% of the radioactivity was found in the urine and 35% in the feces. Unmodified active substance was not found in the urine.

Indications

type 2 diabetes mellitus (insulin-independent) in case of failure of diet therapy and physical activity.

Release form

Tablets 1 mg, 2 mg, 3 mg and 4 mg.

Instructions for use and dosage

The initial and maintenance dose is set individually based on the results of regular monitoring of blood and urine glucose levels.

The initial dose is 1 mg 1 time per day. If necessary, the daily dose can be gradually increased (by 1 mg in 1-2 weeks) up to 4-6 mg.

The maximum dose is 8 mg per day.

Side effect

hypoglycemia;
hyponatremia;
nausea, vomiting;
feeling of discomfort in the epigastrium;
stomach ache;
diarrhea;
increased activity of hepatic transaminases;
cholestasis;
jaundice;
hepatitis (up to development liver failure);
thrombocytopenia, leukopenia, erythropenia, granulocytopenia, agranulocytosis, pancytopenia, hemolytic anemia;
transient visual impairment;
hives;
skin rash;
drop in blood pressure;
anaphylactic shock;
allergic vasculitis;
photosensitivity.

Contraindications

type 1 diabetes mellitus (insulin-dependent);
ketoacidosis;
precoma, coma;
liver failure;
renal failure (including patients on hemodialysis);
pregnancy;
lactation;
hypersensitivity to glimepiride, other sulfonylurea derivatives and sulfonamides.

Use during pregnancy and lactation

Glimepiride is contraindicated for use in pregnancy. In the event of a planned pregnancy or when pregnancy occurs, the woman should be transferred to insulin.

During lactation, a woman should be transferred to insulin.

In experimental studies, it was found that glimepiride is excreted with breast milk.

Use in children

Not marked.

special instructions

Use with caution in patients with comorbidities endocrine system that affect carbohydrate metabolism(including dysfunction thyroid gland, adenohypophyseal or adrenocortical insufficiency).

AT stressful situations(for trauma, surgical intervention, infectious diseases accompanied by fever) it may be necessary to temporary transfer patient on insulin.

It should be borne in mind that the symptoms of hypoglycemia may be smoothed or completely absent in elderly patients, patients with NCD or receiving simultaneous treatment beta-blockers, clonidine, reserpine, guanethidine or other sympatholytics.

At achievement of compensation of a diabetes mellitus sensitivity to insulin increases; in this regard, the need for glimepiride may decrease during treatment. In order to avoid the development of hypoglycemia, it is necessary to reduce the dose or cancel glimepiride in a timely manner. Dose adjustment should also be carried out when the patient's body weight changes or when his lifestyle changes, or when other factors appear that contribute to the development of hypo- or hyperglycemia.

When switching to glimepiride from another drug, it is necessary to take into account the degree and duration of the effect of the previous hypoglycemic agent. It may be necessary to temporarily stop treatment in order to avoid an additive effect.

In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly strict monitoring of the patient. Factors contributing to the development of hypoglycemia include: irregular, malnutrition; changes in the usual diet; drinking alcohol, especially when combined with skipping meals; change in routine physical activity; simultaneous use of other drugs. Hypoglycemia can be quickly controlled by immediate intake of carbohydrates.

During the treatment period, regular monitoring of blood and urine glucose levels, as well as the concentration of glycated hemoglobin, is necessary.

Influence on the ability to drive vehicles and control mechanisms

During the treatment period, you should refrain from potentially dangerous species activities requiring heightened attention and speed of psychomotor reactions.

drug interaction

Strengthening the hypoglycemic effect of glimepiride is possible with simultaneous application 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, isophosphamides, MAO inhibitors, miconazole, PAS, pentoxifylline (with injection 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 prolonged use), nicotinic acid (in high doses), estrogens and progestogens, phenothiazine , phenytoin, rifampicin, thyroid hormones.

With simultaneous use of histamine H2 receptor blockers, clonidine and reserpine can both potentiate and reduce the hypoglycemic effect of glimepiride.

Against the background of the use of glimepiride, an increase or decrease in the action of coumarin derivatives is possible.

Ethanol (alcohol) may increase or decrease the hypoglycemic effect of glimepiride.

Analogues of the drug Glimepiride

Structural analogues for the active substance:

Amaryl;
Glyme;
Glemaz;
Glemauno;
Glimepiride Canon;
Glimepiride Teva;
Glumedex;
Diameride;
Meglimide.

Analogues for therapeutic effect(Means for the treatment of non-insulin-dependent diabetes mellitus type 2):

Avandamet;
Actrapid;
Amalvia;
Amaryl M;
Anvist;
Antidiab;
Bahomet;
Berlinsulin;
Betanaz;
Biosulin R;
Victoza;
Vipidia;
Galvus;
Galvus Met;
Gensulin;
Glybamide;
Glibenez;
Glibenez retard;
Glibenclamide;
Glibomet;
Glimecomb;
Glitizol;
Gliformin;
Glucophage;
Glucophage Long;
Depot insulin C;
diabeton;
Diabeton MV;
Dibikor;
Isophane insulin ChM;
Invokana;
Insulin C;
Xenical;
Listat;
Maninil;
Metfogamma;
Metformin;
Mixtard;
Monotard;
NovoMix;
NovoNorm;
Onglise;
Pensulin;
Protafan;
Reduxin Met;
Siofor;
Trikor;
Ultratard;
Formetin;
Formin Pliva;
Chlorpropamide;
Humalog;
Humulin;
Euglucon;
Januvia.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.

10 - blisters (3) - packs of cardboard. 10 - blisters (3) - packs of cardboard. 10 - blisters (6) - packs of cardboard. 10 - blisters (10) - packs of cardboard. 10 pieces. - blisters (3) - packs of cardboard. 10 pieces. - cellular contour packings (3) - packs of cardboard. 30 tabs in cards. a pack of 10, 20 or 30 tablets in a blister pack made of PVC film and printed lacquered aluminum foil. tab. 2 mg: 30 tab. 3 mg: 30 tab. 4 mg: 30 pieces Tablets 1 mg - 30 pieces per pack. Tablets 2 mg - 30 pcs per pack. Tablets 3 mg - 30 pcs per pack. Tablets

Description of the dosage form

Tablets Tablets white or almost white color, round, biconvex, with risk, on one side; Tablets are white or almost white, round, flat-cylindrical, scored on one side and chamfered. Tablets are white or almost white, flat-cylindrical, with a chamfer and a cruciform risk. Tablets are white or almost white, flat-cylindrical, with a bevel. Tablets white, oblong, with beveled edges, with a break line on one side Tablets from white to white with a creamy tint, round, flat-cylindrical, with a bevel. oblong tablets yellow color with beveled edges and notch on one side of the tablet light yellow with a brownish tint, with a marble surface, oblong, with beveled edges, with a fault line on one side. Tablets light yellow, round, flat-cylindrical, chamfered Tablets light pink, round, flat-cylindrical, chamfered; marbling is allowed. Tablets

pharmachologic effect

Glimepiride reduces the concentration of glucose in the blood, mainly by stimulating the release of insulin from pancreatic beta cells. Its effect is predominantly associated with an improvement in the ability of pancreatic beta cells to respond to physiological glucose stimulation. Compared with glibenclamide, low-dose glimepiride causes less insulin to be released while achieving approximately the same reduction in blood glucose. This fact testifies in favor of the presence of extrapancreatic hypoglycemic effects in glimepiride (increased sensitivity of tissues to insulin and insulinomimetic effect). secretion of insulin. Like all other sulfonylurea derivatives, glimepiride regulates insulin secretion by interacting with ATP-sensitive potassium channels on beta cell membranes. Unlike other sulfonylurea derivatives, glimepiride selectively binds to a protein with a molecular weight of 65 kDa, located in the membranes of pancreatic beta cells. This interaction of glimepiride with its binding protein regulates the opening or closing of ATP-sensitive potassium channels. Glimepiride closes potassium channels. This causes depolarization of beta cells and leads to the opening of voltage-sensitive calcium channels and the entry of calcium into the cell. As a result, an increase in intracellular calcium concentration activates insulin secretion by exocytosis. Glimepiride binds to and is released from its binding protein much more rapidly and therefore more frequently than glibenclamide. It is assumed that this property high speed the exchange of glimepiride with its binding protein causes its pronounced effect of sensitizing beta cells to glucose and protecting them from desensitization and premature exhaustion. The effect of increasing the sensitivity of tissues to insulin. Glimepiride enhances the effects of insulin on glucose uptake peripheral tissues. insulinomimetic effect. Glimepiride has effects similar to those of insulin on glucose uptake by peripheral tissues and glucose output from the liver. Absorption of glucose by peripheral tissues is carried out by its transport inside muscle cells and adipocytes. Glimepiride directly increases the number of glucose-transporting molecules in the plasma membranes of muscle cells and adipocytes. Increased intake of glucose into cells leads to the activation of glycosylphosphatidylinositol-specific phospholipase C. As a result, intracellular calcium concentration decreases, causing a decrease in protein kinase A activity, which in turn leads to stimulation of glucose metabolism. Glimepiride inhibits the release of glucose from the liver by increasing the concentration of fructose-2,6-bisphosphate, which inhibits gluconeogenesis. Influence on platelet aggregation. Glimepiride reduces platelet aggregation in vitro and in vivo. This effect appears to be due to selective inhibition of cyclooxygenase, which is responsible for the formation of thromboxane A, an important endogenous platelet aggregation factor. Antiatherogenic effect of the drug. Glimepiride contributes to the normalization of lipid levels, reduces the content of malonic aldehyde in the blood, which leads to a significant decrease in lipid peroxidation. In animals, glimepiride leads to a significant reduction in the formation of atherosclerotic plaques. Reducing the severity of oxidative stress, which is constantly present in patients with diabetes 2 types. Glimepiride increases the content of endogenous alpha-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase. cardiovascular effects. Through ATP-sensitive potassium channels (see above), sulfonylurea derivatives also affect cardiovascular system. Compared with traditional sulfonylurea derivatives, glimepiride has a significantly lower effect on the cardiovascular system, which can be explained by the specific nature of its interaction with the ATP-sensitive potassium channel protein that binds to it. In healthy volunteers, the minimum effective dose of glimepiride is 0.6 mg. The effect of glimepiride is dose-dependent and reproducible. The physiological response to exercise (decrease in insulin secretion) while taking glimepiride is preserved. There are no significant differences in the effect depending on whether the drug was taken 30 minutes before a meal or immediately before a meal. In patients with diabetes mellitus, sufficient metabolic control can be achieved for 24 hours with a single dose of the drug. In a clinical study, 12 out of 16 patients with renal insufficiency (creatinine clearance 4-79 ml / min) also achieved sufficient metabolic control. Combination therapy with metformin. In patients with insufficient metabolic control when using the maximum dose of glimepiride, combination therapy with glimepiride and metformin may be initiated. In two studies, when conducting combination therapy improved metabolic control compared with that of treatment with each of these drugs alone has been shown. Combination therapy with insulin. In patients with insufficient metabolic control when using maximum doses glimepiride, concomitant insulin therapy may be initiated. Two studies show that this combination achieves the same improvement in metabolic control as insulin alone; however, combination therapy requires a lower dose of insulin. Application in children. Available an insufficient amount data on the long-term efficacy and safety of the drug in children.

Pharmacokinetics

Absorption With repeated administration of glimepiride in daily dose 4 mg, the maximum concentration (Cmax) in the blood plasma is reached after about 2.5 hours and is 309 ng / ml. There is a linear relationship between dose and Cmax of glimepiride in plasma, as well as between dose and area under the concentration-time curve (AUC). When administered orally, glimepiride has a complete absolute bioavailability. Eating does not have a significant effect on absorption, with the exception of a slight slowdown in its rate. Distribution Glimepiride has a very low volume of distribution (about 8.8 L), approximately equal to that of albumin, a high degree of plasma protein binding (greater than 99%), and a low clearance (about 48 ml/min). Metabolism Glimepiride is metabolized in the liver (mainly with the participation of the CYP2C9 isoenzyme) with the formation of two metabolites - hydroxylated and carboxylated derivatives, which are found in urine and feces. Withdrawal After a single oral dose of glimepiride, 58% of the dose is excreted by the kidneys and 35% of the dose is excreted through the intestines. Unchanged glimepiride is not detected in the urine. The average half-life (T1 / 2), determined by serum concentrations under conditions of repeated administration of the drug, is approximately 5-8 hours. After taking high doses, there is a slight increase in T1 / 2. The average T1 / 2 of the hydroxylated and carboxylated metabolites of glimepiride is 3-5 and 5-6 hours, respectively. Glimepiride passes into breast milk and through the placental barrier. Comparison of single and multiple (once a day) administration of glimepiride did not reveal significant differences in pharmacokinetic parameters; very low variability between different patients. There is no significant accumulation of the drug. Pharmacokinetics in special clinical cases Pharmacokinetic parameters are similar in patients of different sexes and different age groups. In patients with impaired renal function (with low creatinine clearance), there is a trend towards an increase in the clearance of glimepiride and a decrease in its mean serum concentrations, which, in all likelihood, is due to faster elimination of the drug due to its lower protein binding. Thus, in this category of patients there is no additional risk drug accumulation.

Special conditions

Glimepiride-Teva should be taken at the recommended doses and at the scheduled times. Errors in the use of the drug, such as skipping a dose, can never be eliminated by a subsequent dose of a higher dose. The doctor and patient should discuss in advance the measures to be taken in case of such errors (for example, skipping a drug or meal) or in situations where it is impossible to take the next dose of the drug in set time. The patient should immediately inform the doctor in case of taking too high a dose of the drug. If a patient develops a hypoglycemic reaction when taking 1 mg Glimepiride-Teva per day, this indicates that in this patient, normalization of blood glucose levels can be achieved using diet alone. When compensation for type 2 diabetes mellitus is achieved, insulin sensitivity increases. In this regard, the need for Glimepiride-Teva may decrease during treatment. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or cancel Glimepiride-Teva. Dose adjustment should also be carried out with a change in the patient's body weight, with a change in his lifestyle, or with the appearance of other factors that increase the risk of developing hypo- or hyperglycemia. Adequate diet, regular and sufficient physical exercises and, if necessary, weight loss have the same importance to achieve optimal control of blood glucose levels, as well as the regular intake of Glimepiride-Teva. Clinical symptoms hyperglycemia (insufficient lowering of blood glucose levels) are: increased frequency of urination, intense thirst, dry mouth and dryness skin. In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly careful monitoring of the patient. Against the background of treatment with Glimepiride-Teva, hypoglycemia may develop with irregular meals or skipping meals. Her possible symptoms are: headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbances, anxiety, aggressiveness, concentration, attention and reaction disorders, depression, confusion, speech and visual disorders, aphasia, tremor, paresis, sensory disturbances, dizziness, delirium, cerebral twitching, confusion or loss of consciousness, including coma, shallow breathing, bradycardia. In addition, as a result of the adrenergic mechanism feedback sweating, restlessness, tachycardia, increased blood pressure, angina and disorders heart rate. Factors contributing to the development of hypoglycemia include: unwillingness or (especially in old age) insufficient ability of the patient to cooperate with the doctor; inadequate, irregular nutrition, skipping meals, fasting, changes in the usual diet; imbalance between exercise and carbohydrate intake; drinking alcohol, especially when combined with skipping meals; impaired renal function; severe violation liver function; overdose of Glimepiride-Teva; some uncompensated diseases of the endocrine system that affect carbohydrate metabolism (for example, thyroid dysfunction, pituitary failure or insufficiency of the adrenal cortex); simultaneous use of drugs that enhance the effect of Glimepiride-Teva (see section "Interaction with other medicines"). The physician should be informed about the above factors and episodes of hypoglycemia, since they require particularly strict monitoring of the patient. In the presence of such factors that increase the risk of developing hypoglycemia, the dose of Glimepiride-Teva or the entire treatment regimen should be adjusted. This should also be done in the case of an intercurrent disease or a change in the patient's lifestyle. Symptoms of hypoglycemia may be smoothed out or completely absent in elderly patients, in patients suffering from autonomic neuropathy or receiving simultaneous treatment with ?-blockers, clonidine, reserpine, guanethidine, or other sympatholytic agents. Hypoglycemia can almost always be quickly controlled 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 pieces of sugar) with him. Sweeteners are ineffective in the treatment of hypoglycemia. From experience with other sulfonylurea drugs, it is known that, despite the initial success in stopping hypoglycemia, its recurrence is possible. In this regard, continuous and careful monitoring of the patient is necessary. Severe hypoglycemia requires immediate treatment under the supervision of a physician, and under certain circumstances, hospitalization of the patient. If a diabetic patient is treated by different doctors (for example, during a stay in the hospital after an accident, when sick on weekends), he must necessarily inform them about his disease and previous treatment. During treatment with Glimepiride-Teva, regular monitoring of liver function and picture is required. peripheral blood(especially the number of leukocytes and platelets). 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-Teva in patients with severely impaired liver and kidney function or patients on hemodialysis. Patients with severely impaired renal and hepatic function are shown to be transferred to insulin therapy. During treatment with Glimepiride-Teva, regular monitoring of the concentration of glucose in the blood, as well as the concentration of glycosylated hemoglobin, is necessary. At the beginning of treatment, when switching from one drug to another, or when taking Glimepiride-Teva irregularly, there may be a decrease in the concentration of attention and the speed of the patient's psychomotor reactions due to hypo- or hyperglycemia. This may adversely affect the ability to drive vehicles or to control various machines and mechanisms. Overdose Symptoms: hypoglycemia (nausea, vomiting and pain in epigastric region, restlessness, tremor, visual disturbances, incoordination, drowsiness, coma and convulsions). Treatment: if the patient is conscious - induction of vomiting, plentiful drink, Activated carbon and laxative. In case of severe overdose - intravenous bolus administration of a dextrose solution (50 ml of a 40% solution), then - infusion administration 10% solution. Necessary constant surveillance for the patient, maintaining vital functions and monitoring the concentration of glucose in the blood (recurrence of episodes of hypoglycemia is possible). AT further treatment symptomatic.

Compound

glimepiride 4 mg Excipients: lactose monohydrate 237.5 mg, microcrystalline cellulose 36 mg, sodium carboxymethyl starch 15 mg, povidone 3 mg, polysorbate 80 1.5 mg, magnesium stearate 3 mg. 1 tab. Glimepiride (in terms of 100% substance) 3 mg - 0.002 mg. 1 tab. glimepiride 2 mg 1 tab. glimepiride 2 mg Excipients: lactose monohydrate - 150.8 mg, corn starch - 4.66 mg, sodium carboxymethyl starch - 10 mg, povidone - 6 mg, polysorbate 80 - 1.34 mg, talc - 2 mg, magnesium stearate - 1.2 mg. 1 tab. glimepiride 3 mg Excipients: lactose monohydrate - 149.5 mg, corn starch - 4.66 mg, sodium carboxymethyl starch - 10 mg, povidone - 7 mg, polysorbate 80 - 1.34 mg, talc - 2 mg, magnesium stearate - 1.2 mg, iron oxide yellow dye (E172) - 0.3 mg. 1 tab. glimepiride 4 mg 1 tab. glimepiride (in terms of 100% substance) 2 mg Excipients: lactose monohydrate - 107.8 mg, microcrystalline cellulose - 14 mg, pregelatinized starch - 3.9 mg, sodium lauryl sulfate - 1.3 mg, magnesium stearate - 1 mg. 1 tab. glimepiride (in terms of 100% substance) 4 mg Excipients: lactose monohydrate - 104.498 mg, microcrystalline cellulose - 14 mg, pregelatinized starch - 3.9 mg, sodium lauryl sulfate - 2.6 mg, magnesium stearate - 1 mg, azorubine (E122) - 0.002 mg. glimepiride 2 mg; excipients: calcium hydrogen phosphate dihydrate 30 mg, croscarmellose sodium 3.7 mg, corn starch 16 mg, mannitol 55 mg, magnesium stearate 0.8 mg, povidone-K30 2.5 mg. Glimepiride 2mg; Auxiliary substances: lactose, MCC, pregelatinized starch, sodium lauryl sulfate, magnesium stearate, yellow dye glimepiride 3 mg magnesium stearate 1.5 mg. glimepiride 3 mg; excipients: calcium hydrogen phosphate dihydrate 40.5 mg, croscarmellose sodium 5 mg, corn starch 22.1 mg, mannitol 75 mg, magnesium stearate 1 mg, povidone-K30 3.4 mg. Glimepiride 3mg; Auxiliary in-va: lactose, MCC, pregelatinized starch, sodium lauryl sulfate, magnesium stearate, yellow dye glimepiride 4 mg; excipients: calcium hydrogen phosphate dihydrate 53.3 mg, croscarmellose sodium 6.7 mg, corn starch 30 mg, mannitol 100 mg, magnesium stearate 1.5 mg, povidone-K30 4.5 mg. Glimepiride 4mg; Auxiliary in-va: lactose, MCC, pregelatinized starch, sodium lauryl sulfate, magnesium stearate, dye yellow limepiride 1 mg; excipients: calcium hydrogen phosphate dihydrate 24.4 mg, croscarmellose sodium 3 mg, corn starch 14 mg, mannitol 45 mg, magnesium stearate 0.6 mg, povidone-K30 2 mg.

Glimepiride indications for use

The drug is indicated for the treatment of type 2 diabetes mellitus with the ineffectiveness of a previously prescribed diet and exercise. If monotherapy with glimepiride-Teva is ineffective, it can be used in combination therapy with metformin or insulin

Glimepiride contraindications

Type 1 diabetes mellitus (insulin-dependent), ketoacidosis, precoma, coma, liver failure, renal failure (including patients on hemodialysis), pregnancy, lactation, hypersensitivity to glimepiride, other sulfonylurea derivatives and sulfonamides. Use during pregnancy and lactation Contraindicated for use during pregnancy. In the event of a planned pregnancy or when pregnancy occurs, the woman should be transferred to insulin. During lactation, a woman should be transferred to insulin. In experimental studies, it was found that glimepiride is excreted in breast milk. Application for violations of liver function Contraindicated in liver failure. Application for violations of kidney function Contraindicated in kidney failure(including patients on hemodialysis).

Glimepiride dosage

1 mg 2 mg 3 mg 4 mg

Glimepiride side effects

From the side of metabolism: as a result of the hypoglycemic effect of the drug, hypoglycemia may develop, which, as with other sulfonylurea derivatives, can be prolonged. Symptoms of hypoglycemia are: headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbance, anxiety, aggressiveness, impaired concentration, vigilance and reaction speed, depression, confusion, speech disorders, aphasia, visual disorders, tremor, paresis, sensory disturbances, dizziness, loss of self-control, delirium, cerebral convulsions, somnolence or loss of consciousness, up to coma, shallow breathing, bradycardia. In addition, there may be manifestations of adrenergic counterregulation in response to hypoglycemia, such as the appearance of cold clammy sweat, anxiety, tachycardia, increased blood pressure (BP), angina pectoris, palpitations and heart rhythm disturbances. Clinical picture severe hypoglycemia may be similar to a stroke. Symptoms of hypoglycemia almost always disappear after it is eliminated. On the part of the organ of vision: during treatment (especially at its beginning), there may be transient disorders vision due to changes in the concentration of glucose in the blood. Their cause is a temporary change in the swelling of the lenses, depending on the concentration of glucose in the blood, and due to this - a change in the refractive index of the lenses. From the gastrointestinal tract: in rare cases- nausea, vomiting, feeling of heaviness or fullness in the epigastrium, abdominal pain, diarrhea. In some cases - hepatitis, increased activity of "liver" enzymes and / or cholestasis and jaundice, which can progress to life threatening liver failure, but may be subject to reverse development upon discontinuation of the drug. From the blood and lymphatic system: rarely - thrombocytopenia. In some cases, leukopenia, hemolytic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia. In post-marketing use of the drug, cases of severe thrombocytopenia with a platelet count of less than 10,000 / µl and thrombocytopenic purpura have been reported (frequency unknown). Violations by immune system: in rare cases, allergic and pseudo-allergic reactions are possible, such as itching, urticaria, skin rash. Such reactions are almost always light form, but may progress to severe reactions with shortness of breath, sharp decline AD, which sometimes progress to anaphylactic shock. If symptoms of hives appear, you should immediately consult a doctor. General disorders and disorders at the injection site: in some cases, there may be a decrease in the concentration of sodium in the blood plasma, allergic vasculitis, photosensitivity.

drug interaction

Interaction with other drugs Glimepiride is metabolized by cytochrome P450 2C9 (CYP2C9). With simultaneous use with inducers of the CYP2C9 isoenzyme, for example, rifampicin, it is possible to reduce the hypoglycemic effect of glimepiride and increase the risk of developing hypoglycemia if they are canceled without dose adjustment of glimepiride. With simultaneous use with inhibitors of the CYP2C9 isoenzyme, for example, fluconazole, it is possible to increase the hypoglycemic effect of glimepiride and increase the risk of developing hypoglycemia and side effects glimepiride, and it is also possible to reduce its hypoglycemic effect when they are canceled without dose adjustment of glimepiride. Increased hypoglycemic effect and related possible development hypoglycemia can be observed with the simultaneous use of glimepiride with insulin or other oral hypoglycemic drugs, metformin, angiotensin-converting enzyme (ACE) inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclo-, tro- and isophosphamides, fenfluramine, disopyramide, fibrates, fluoxetine, sympatholytics (guanethidine), monoamine oxidase (MAO) inhibitors, miconazole, fluconazole, pentoxifylline (with parenteral administration in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenicide, quinolones, salicylates and aminosalicylic acid, sulfinpyrazone, some sulfonamides long-acting, tetracyclines, tritoqualin. The weakening of the hypoglycemic effect and the associated increase in the concentration of glucose in the blood can be observed with the simultaneous use of glimepiride with acetazolamide, barbiturates, glucocorticosteroids, glucagon, laxatives (with long-term use), nicotinic acid (in high doses) and derivatives nicotinic acid, estrogens and progestogens, phenothiazines, chlorpromazine, phenytoin, rifampicin, thyroid hormones, lithium salts. Blockers of H2-histamine receptors, clonidine and reserpine, can both potentiate and weaken the hypoglycemic effect of glimepiride. Under the influence of such sympatholytic agents like beta-blockers, clonidine, guanethidine and reserpine, possibly weakening or absence clinical signs hypoglycemia. Against the background of taking glimepiride, an increase or decrease in the action of coumarin derivatives may be observed. With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases. Single or chronic alcohol consumption can both enhance and weaken the hypoglycemic effect of glimepiride.

Overdose

Overdose symptoms Acute overdose, as well as long-term treatment too much high doses glimepiride can lead to the development of severe life-threatening hypoglycemia. Treatment of overdose As soon as an overdose of glimepiride is detected, the doctor should be informed immediately. Hypoglycemia can almost always be quickly controlled by immediate intake of carbohydrates (glucose or sugar cubes, sweet fruit juice, or tea). In this regard, the patient should always have at least 20 g of glucose (4 pieces of sugar) with him. Sweeteners are ineffective in the treatment of hypoglycemia. Until the doctor decides that the patient is out of danger, the patient needs careful medical supervision. It should be remembered that hypoglycemia may recur after the initial recovery of blood glucose levels. If a diabetic patient is being treated by different physicians (for example, during a hospital stay after an accident, when sick at the weekend), he should

Storage conditions

store at room temperature 15-25 degrees
keep away from children
store in a place protected from light

Information provided

Glimepiride (in the prescription in Latin - Glimepiride)- this is an unfairly forgotten medicine today. Of all the antidiabetic agents that make up the sulfonylurea class of drugs, this is a very convenient medication. When the pills first appeared in pharmacy network, they were one of the most sought after medicines. But after the discovery of a new class of drugs (incretins), they began to undeservedly forget it.

Glimepiride - very high quality hypoglycemic agent and quite safe. Its main function as a secretagogue is to stimulate the pancreas.

The drug also has extra-pancreatic possibilities: increasing the sensitivity of tissues to endogenous insulin, reducing the production of glucose in the liver, preventing the formation of blood clots, and reducing the level of free radicals.

Dosage form

The domestic manufacturer PHARMSTANDART produces Glimepiride in the form of 4 types of capsule tablets:

Light pink color - 1 mg each;
Light green shade - 2 mg;
Light yellow tone - 3 mg each;
Light blue color - 4 mg.

Capsules are packaged in aluminum blisters of 10 pieces, the plates are placed in paper packaging. Store the medicine in the original box at room temperature for no more than 3 years. For Glimepiride, the price in online pharmacies is from 153 rubles. up to 355 rubles depending on dosage. The category of drug dispensing is by prescription.

Glimepiride - analogues and synonyms

The original medicine, the very first, most studied, is Amaryl from Sanofi Aventis. All other drugs, including glimepiride, are analogues, pharmaceutical companies produce them under a patent. Among the most famous:

Glimepiride (Russia);
Diamerid (Russia);
Diapiride (Ukraine);
Glimepiride-Teva (Croatia);
Glemaz (Argentina);
Glianov (Jordan);
Glibetik (Poland);
Amaril M (Korea);
Glairi (India).

Ingredients of Glimepiride

Glimepiride is an oral antidiabetic agent with hypoglycemic potential. The drug belongs to the group of sulfonamides, urea derivatives.

The basic active ingredient of the drug is glimepiride. In one tablet, its mass is 1 - 4 mg. complement active substance auxiliary components: sodium starch, povidone, polysorbate, microcrystalline cellulose, lactose, magnesium stearate, indigo aluminum lacquer.

Pharmacology

Glimepiride is an antidiabetic drug from the group of sulfonylurea derivatives, active when taken orally. It was developed to control SD type 2. The mechanism of action of the drug is based on the stimulation of β-cells responsible for the production of endogenous insulin. The drug binds to the membrane protein of these cells very quickly.

Like all medicines in this group, the drug increases the sensitivity of tissues to glucose stimulation. It has a drug and an extrapancreatic effect. The production of insulin under the influence of the drug occurs due to improved access to calcium channels: increased influx of calcium promotes the release of insulin.

Of the extra-pancreatic effects, one can note a decrease in cell resistance to the hormone, a decrease in the rate of its utilization in the liver. Glucose is burned in muscles and fat by transport proteins, the activity of which increases significantly after the use of the drug.

Pharmacokinetics

The bioavailability of glimepiride is 100%. Parallel arrival nutrients slightly slows down absorption. The maximum content in plasma is observed 2.5 hours after the drug enters the gastrointestinal tract. The volume of distribution of the drug is low (8.8 l), it binds to serum proteins to the maximum (by 99%), the clearance of the drug is 48 ml / min.

With a repeated dosing regimen, the average half-life is 5-8 hours. With an increase in the therapeutic dose, this time increases. Metabolites are eliminated naturally: 58% marked radioactive isotope a single dose was found in the urine and 35% in the feces. The half-life of decay products is 3-6 hours.

Fundamental differences in the pharmacokinetics of glimepiride in young or younger diabetics middle age, female or male is not recorded. In diabetics with low creatinine clearance, there is no danger of drug accumulation. Pharmacokinetic parameters in 5 patients after cholecystectomy were similar to those in healthy diabetics.

In 26 adolescents aged 12-17 years, as well as 4 children aged 10-12 years with type 2 diabetes, a single dose of the minimum (1 mg) dose of the drug showed results similar to adults.

Who is prescribed the drug

Tablets are prescribed for type 2 diabetes if glycemic control through lifestyle modification is not enough. It is possible to prescribe the drug as an additional, in complex therapy with other hypoglycemic agents.

Who should not take glimepiride

The medicine is not suitable for diabetics with type 1 disease, do not use it for diabetic ketoacidosis, coma and precoma, as well as with severe dysfunctions of the kidneys and liver.

As with any drug, glimepiride is not prescribed for diabetics with high sensitivity to the ingredients of the formula, as well as to other sulfonamide medicines.

The drug is prescribed only for adults, since the efficacy and safety of Glimepiride in children has not been sufficiently established.

Glimepiride is contraindicated during pregnancy and lactation.

How to use Glimepiride correctly

To ensure 100% glycemic control, drug therapy not enough.

Only if you follow the principles of low-carbohydrate nutrition, control emotional state, constant monitoring of their glycemic profile, as well as physical activity adequate for age and health status, you can count on the effectiveness of any hypoglycemic agents, including glimepiride.

indicative plan muscle loads with DM 2 light type and medium shape could be like this:

Strength exercises - 2-3 rubles / week;
Energetic walk - 3 rubles / week;
Swimming, cycling, tennis or dancing;
Walking up the stairs, quiet walks - daily.

If such a complex is not suitable, you can do exercise therapy every day. AT sitting position a diabetic can stay without a break for no more than 30 minutes.

Optimal therapeutic dose the doctor selects taking into account the stage of the disease, concomitant pathologies, general condition, the age of the patient, the reaction of his body to the drug.

Glimepiride instructions for use recommends the use of 1 mg / day. (at starting dose). With a frequency of 1-2 weeks, when it is already possible to evaluate the result, it can be titrated if the previous treatment regimen was not effective enough. The norm is more than 4 mg / day. applied in special occasions. Maximum amount drugs - up to 6 mg / day.

If the maximum dose of metformin does not provide 100% glycemic control, glimepiride can be taken in parallel as maintenance therapy, it combines perfectly with this drug, even combined medicines with these two active ingredients. Comprehensive treatment is started with a minimum dose of glimepiride (1 g), daily monitoring of glucometer readings will help to correct the norm. All changes to the algorithm are made only under medical supervision.

Perhaps the combination of glimepiride and insulin preparations. The dosage of tablets in this case should also be minimal at first. Based on the results of the tests, every two weeks the dose of the drug can be adjusted.

Usually, the drug is taken once. Combine it with a solid breakfast or the next meal, if the diabetic's breakfast is symbolic.

“Jumping” the medicine is very important, the only way to count on its maximum effectiveness, to avoid hypoglycemia and other side effects.

It is best to take the tablet a few minutes before meals as it needs time to work. If the time of taking glimepiride is missed, the medicine should be taken at the first opportunity, without changing the dosage.

If a minimum dose Glimepiride causes symptoms of hypoglycemia, the drug is discontinued, since it is enough for the patient to control his sugar proper nutrition, good mood, observance of the regime of sleep and rest, adequate physical activity.

When complete control of diabetes is achieved, resistance to the hormone may decrease, which means that over time, the need for the drug will decrease. It is also necessary to revise the dose with a sharp weight loss, a change in the nature of physical activity, an increased stress background and other factors provoking glycemic crises.

Possibility of switching from other antidiabetic agents to glimepiride

When moving from alternative options treatment of type 2 diabetes by oral means take into account the parameters of the half-life of previous drugs. If this period is too long for a drug (such as chlorpropamide), a pause of several days must be allowed before switching to glimepiride. This will reduce the chances of developing hypoglycemia due to the additive effects of the 2 agents. When replacing drugs, the starting dose is recommended to be minimal - 1 mg / day. Titration is carried out under similar conditions.

Glimepiride insulin replacement in type 2 diabetics is extreme cases and under constant medical supervision.

Side effects

Glimepiride, like other sulfa drugs, has accumulated a solid evidence base their effectiveness. AT clinical research their safety has also been studied. According to WHO recommendations, the risk of developing undesirable consequences evaluated on the following scale:

Very often ≥ 0.1;
Often: from 0.1 to 0.01;
Uncommon: 0.01 to 0.001;
Rare: 0.001 to 0.0001;
Very rarely<0, 00001;
It is not known if it is impossible to estimate the degree of risk based on available statistics.

The results of the body's reactions from various organs and systems are presented in the table. Most of them are not permanent and go away on their own after changing the medicine.

Organs and systems	Adverse reactions	Frequency of manifestations
Circulatory system	granulocytopenia, thrombocytopenia, leukopenia, erythropenia, agranulocytosis, anemia, pancytopenia	rarely
Immunity	leukocytoclastic vasculitis, progressive hypersensitivity, dyspnea, blood pressure fluctuations up to shock	very rarely
Metabolic disorders	rapidly developing and difficult to correct hypoglycemic conditions	rarely
Vision	fluctuations in the level of glycemia can provoke a temporary swelling of the lens	unknown
gastrointestinal tract	dyspeptic disorders, epigastric pain, violation of the rhythm of defecation (do not imply discontinuation of the drug)	very rarely
Hepatobiliary system	increase in liver enzymes, dysfunction such as jaundice or choleostasis	unknown very rarely
Leather	itching, rash, urticaria, photosensitivity	unknown
Laboratory data	drop in sodium concentration in the blood - hyponatremia	very rarely

Help with overdose

The main danger of an overdose of glimepiride is hypoglycemia lasting up to 72 hours, after normalization of the condition, relapses are also possible. The first signs of an overdose may appear only a day after the absorption of the drug. With such symptoms (dyspeptic disorders, chest pain), the victim needs to be monitored in a medical facility. With hypoglycemia, neurological disorders are also possible: impaired vision and coordination, hand tremor, anxiety, isomnia, muscle spasms, coma.

First aid for overdose is to prevent the absorption of excess drug by gastric lavage. It is necessary to induce a gag reflex in any way, then drink activated charcoal or another adsorbent and some laxative (for example, sodium sulfate). At the same time, an ambulance must be called for urgent hospitalization.

The victim will be injected with glucose intravenously: first, 50 ml of a 50% solution, then a 10% solution. Plasma sugar levels should be checked as often as possible. In addition to specific therapy, symptomatic therapy is also used.

If a child accidentally takes glimepiride, the dosage of glucose is selected taking into account the likelihood of developing hypoglycemia. The degree of risk is periodically assessed with a glucometer.

Deviations from the norm in the composition of the blood during pregnancy can cause fetal malformations and even perinatal mortality, and glycemic parameters are no exception in this regard. To reduce the teratogenic risk, a woman should regularly monitor her glycemic profile.

If the pregnant woman is a diabetic with type 2 disease, she is temporarily transferred to insulin. Women already at the stage of planning a child should warn their endocrinologist about upcoming changes to correct the treatment regimen.

There is no information on the effect of glimepiride on the human fetus. Based on the results of studies in pregnant animals, the drug has reproductive toxicity related to the hypoglycemic effects of glimepiride.

Therefore, the drug is contraindicated for pregnant women.

Whether the drug enters the mother's milk has not been established, but in rats the drug penetrated into the mother's milk, so the tablets are also canceled for the duration of lactation. Since other sulfonylamide drugs pass into breast milk, the risk of hypoglycemia in an infant is quite real.

Children

There is no information on the use of the drug for diabetic children under 8 years of age. For older people (up to 17 years old), there are some recommendations for using the drug as monotherapy. Published information is not enough for the widespread use of the drug by this category of diabetics, therefore

Features of Glimepiride treatment

Take the tablets a few minutes before meals so that the medicine is absorbed and begins to work. With insufficient compensation for the capabilities of the drug with carbohydrates, it can provoke hypoglycemic conditions. An attack can be recognized by a combination of such signs: headache, wolfish appetite, dyspeptic disorders, isomnia, unusual revival, manifestations of aggression, inhibited reaction, increased anxiety, absent-mindedness, impaired vision and speech, confused consciousness, loss of sensitivity and control, cerebral spasms, fainting , precome and coma. Adrenergic counterregulation is manifested by increased sweating, wet palms, increased anxiety, heart rhythm disorder, hypertension, coronary heart disease.

The clinical picture of a serious condition is similar in signs to a stroke, with the difference that the signs of a hypoglycemic crisis can always be neutralized by urgent administration (orally, subcutaneously, intramuscularly, intravenously - depending on the condition of the victim) of glucose or sweets. Sugar substitutes do not work in this situation.

The experience of treating diabetics with sulfonylamide analogues shows that, despite the obvious effectiveness of measures to stop an attack, there is a risk of its recurrence. A severe and prolonged hypoglycemic state, which periodically normalizes under the influence of ordinary sugar, requires urgent medical treatment, including in a hospital. The following factors increase the risk of hypoglycemia:

Ignoring medical recommendations, inability to cooperate;
Starvation diets, untimely meals, inadequate diet due to poor social conditions;
Failure to follow the principles of low-carbohydrate nutrition;
Lack of balance between the volume of muscle loads and the amount of carbohydrates consumed;
Alcohol abuse, especially with malnutrition;
Renal and hepatic dysfunctions;
Overdose of glimepiride;
Decompensated endocrine pathologies that affect metabolic processes (insufficiency of the pituitary or adrenal glands, thyroid dysfunction);
Parallel use of other medicines.

During drug therapy, constant monitoring of glycemia is required. To avoid complications, it is necessary to regularly undergo other examinations:

Checking the indicators of glycated hemoglobin - 1 time / 3-4 months;
Consultations of an ophthalmologist, nephrologist, cardiologist, neurologist - if necessary;
Microalbuminuria - 2 times / year;
Lipid profile assessment + HD - 1 time / year;
Examination of the legs - 1 time / 3 months;
BP - 1 time / month;
ECG - 1 time / year;
General analyzes - 1 time / year.

It is important to periodically monitor the performance of the liver and blood composition, in particular the ratio of platelets and leukocytes.

If the body is under severe stress (injuries, burns, surgeries, serious infections), it is possible to temporarily replace the tablets with insulin.

There is no experience of using the drug for the treatment of diabetics with severe hepatic pathologies, as well as patients on hemodialysis. With renal or hepatic dysfunctions, the diabetic is transferred to insulin.

Glimepiride contains lactose. If a diabetic has genetic galactose intolerance, lactase deficiency, malabsorption of galactose-glucose, he is given replacement therapy.

The effect of glimepiride on the ability to control complex mechanisms

Special studies of glimepiride for the ability to drive or work in a high-risk area have not been conducted. But, since the drug has a side effect in the form of hypoglycemia, there is a risk of a decrease in the speed of reactions and concentration due to visual impairment and other hypoglycemic symptoms.

When prescribing a remedy, a diabetic should be warned about the danger of serious consequences when operating complex mechanisms. This is especially true for those who have hypoglycemic situations often, as well as those who are not able to recognize the symptoms of an impending problem.

Results of interaction with other medicines

Parallel use of drugs can cause in a diabetic both an increase in the hypoglycemic capabilities of glimepiride and an inhibition of its properties. Some medicines are neutral when used together. Only a specialist can give an accurate assessment of compatibility, therefore, when drawing up a treatment regimen, it is necessary to warn the endocrinologist about all the medications that the diabetic is already taking to treat concomitant diseases.

Strengthening the hypoglycemic effect of Glimepiride provokes the simultaneous use of phenylbutazone, azapropazone and oxyphenbutazone, insulin and oral hypoglycemic drugs, long-acting sulfonamides, metformin, tetracyclines, MAO inhibitors, salicylates, anabolic steroids and male sex hormones, quinolone antibiotics and clarithromycin, chloramphenicol, probenenicol , miconazole, fenfluramine, disopyramides, pentoxifylline, fibrates, tritoqualian, ACE inhibitors, fluconazole, fluoxetine, allopurinol, sympatholytics, cyclo-, tro- and phosphamides.

Inhibition of the hypoglycemic capabilities of glimepiride is possible with joint therapy with estrogens, saluretics, diuretics, glucocorticoids, thyroid stimulants, phenothiazine derivatives, adrenaline, chlorpromazine, sympathomimetics; nicotinic acid (especially at high dosage), laxatives (with prolonged use), phenytoin, diazoxide, glucagon, barbiturates, rifampicin, acetozolamide.

An unpredictable effect is provided by complex therapy with β-blockers, clonidine and reserpine, as well as alcohol intake.

Glimepiride is able to reduce or increase the effect on the body of coumarin derivatives.

Glimepiride - reviews

Glimepiride, according to doctors and patients, is a highly effective medication. Its safety is ensured by small doses, it also has a number of additional features that cannot but rejoice. But, like all antidiabetic drugs, Amaryl's analogue is effective only if the diabetic himself helps him.

Olga Grigorievna, Moscow region. I drink a tablet of Glimepiride (2 mg) before breakfast, and after meals - also prolonged Metformin in the morning and in the evening, 1000 mg each. If I do not sin with the diet, then the medicines keep sugar. I don’t know whose merit is greater here, but on holidays, when it is difficult to avoid feasts and overeating, I drink 3 mg of Glimepiride. The medicine is prescribed to me at the polyclinic under a preferential prescription, so everything suits me.
Andrey Vitalievich, Yekaterinburg. For 3 years I was prescribed Amaryl, I drank 4 mg in the morning. Then the free Amaryl was gone at the polyclinic, they replaced it with Glimepiride, a budget generic. I tried to take it in the same dose - sugar jumped to 12 mmol / l (it used to be no higher than 8). The doctor increased the dose to 6 mg, everything seemed to be fine, but I still bought Amaryl. And again, 4 mg per day was enough for me. But I will probably have to return to a free analog, because I also buy heart drugs and cholesterol pills. Too bad they canceled the free Amaryl.

Glimepiride is a hypoglycemic drug that is prescribed in the treatment of type 2 diabetes mellitus when a specific diet and exercise do not give a positive result. The main active ingredient is glimepiride, a chemical derivative of a sulfonylurea. When it enters the patient's body, it affects the cellular structures of the pancreas, stimulating the production of insulin. In addition, taking the drug significantly increases the sensitivity of the tissues of the human body to an increased amount of insulin.

1. Pharmacological action

Drug group:

Oral hypoglycemic drug.

Therapeutic effects of glimepiride:

Hypoglycemic;
Extrapancreatic;
Anti-atherogenic;
Antiplatelet;
Antioxidant.

2. indications for use

The drug is used for:

Treatment of non-insulin dependent diabetes mellitus in combination with insulin or Metformin, as well as as monotherapy.

1 mg 1 time per day with a gradual increase in dosage to 6 mg 1 time per day.

Set by the attending physician.

Application Features:

Tablets are taken whole, without chewing, and washed down with 1 glass of warm boiled water;
According to the instructions, the dosage is selected individually for each patient and depends on the initial content of glucose in the blood;
After taking the drug, you must eat.

4. Side effects

Nervous system:

Sleep disturbances, fatigue, anxiety, loss or confusion of consciousness, sensory disturbances, impaired coordination, helplessness, loss of self-control, headaches, drowsiness, aggressiveness, speech disorders, changes in concentration and speed of psycho-motor reactions, dizziness, depression, aphasia, paresis, cerebral convulsions, coma;

Respiratory system:

shallow breathing;

The cardiovascular system:

Heart rhythm disturbances, bradycardia;

Digestive system:

Discomfort in the stomach, abdominal pain, increased levels of liver enzymes, nausea, vomiting, hunger, cholestasis, liver failure;

The immune system:

Skin rash, itching, allergic vasculitis;

Blood system:

Decrease in the number of leukocytes, platelets, erythrocytes, granulocytes, aplastic or, pancytopenia;

Sense organs:

visual disturbances;

Skin lesions:

photosensitivity;

Exchange processes:

Hyponatremia.

5. Contraindications

6. During pregnancy and lactation

Pregnant women and nursing mothers should take the drug contraindicated.

7. Interaction with other drugs

Simultaneous use of glimepiride with:

Insulin, Allopurinol, male sex hormones, coumarin derivatives, Fenfluramine, fibrates, MAO inhibitors, Pentoxifylline, Azapropazone, quinolones, Oxyphenbutazone, Sulfinpyrazone, long-acting sulfonamides, Tro-, Cyclo- and Isofosfamide, other hypoglycemic drugs, angiotensin-anabolic-converting factor inhibitors, , Chloramphenicol, Fluoxetine, Pheniramidol, Guanethidine, Miconazole, Phenylbutazone, Probenecid, salicylates, tetracyclines or Tritoqualine: increased hypoglycemic effect of glimepiride;
Epinephrine, Epinephrine, Acetazolamide, Glucagon, Barbiturates, Laxatives, Laxatives, Nicotinic acid in high doses, Phenothiazine, Progestogens and Estrogens, Thyroid hormones, Sympathomimetics, Glucocorticosteroids, Diazoxide, Saluretics, Thiazide diuretics, Phenytoin, Rifampicin, Chlorpromazine or salts lithium: reduction of the hypoglycemic effect of glimepiride.

8. Overdose

Symptoms:

Nervous system:

Dizziness, headaches, aggressiveness, paresis, impaired sensitivity, anxiety, apathy, drowsiness, anxiety, impaired concentration, confusion, depression, convulsions of central origin,;

The cardiovascular system:

Increased blood pressure, pain in the heart, palpitations, arrhythmia,;

Digestive system:

Vomiting, a sharp increase in appetite, nausea;

Exchange processes:

Increased perspiration.

Specific antidote: no data available.

Treatment of overdose with glimepiride:

Intake of sweet food;
Elimination of dehydration;
Symptomatic treatment with constant monitoring of blood glucose levels.

Hemodialysis: no data.

9. Release form

Tablets, 1, 2, 3, 4 or 6 mg - 10, 30, 60, 90, 100 or 120 pcs.

10. Storage conditions

Dry dark place without access to children and strangers.

Should not exceed 25 degrees.

Not longer than 3 years.

11. Composition

1 tablet:

glimepiride - 1, 2, 3, 4 or 6 mg;
Excipients: lactose monohydrate, microcrystalline cellulose, sodium carboxymethyl starch, povidone, polysorbate, magnesium stearate

12. Terms of dispensing from pharmacies

The drug is released according to the prescription of the attending physician.

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* Instructions for medical use for the drug Glimepiride published in free translation. THERE ARE CONTRAINDICATIONS. BEFORE USE, IT IS NECESSARY TO CONSULT WITH A SPECIALIST

Gross formula

C 24 H 34 N 4 O 5 S

Pharmacological group of the substance Glimepiride

Nosological classification (ICD-10)

CAS code

93479-97-1

Characteristics of the substance Glimepiride

White or yellowish-white crystalline powder, almost odorless, practically insoluble in water.

Pharmacology

pharmachologic effect- hypoglycemic.

Stimulates secretion and release of insulin by pancreatic beta cells, improves postprandial insulin/C-peptide response, reduces hyperglycemia without increasing fasting insulin/C-peptide levels. Increases the sensitivity of peripheral tissues to insulin (extrapancreatic action). The hypoglycemic effect reaches a maximum after 2-3 hours; lasts more than 24 hours and stabilizes within 2 weeks. The level of glucose and glycosylated hemoglobin (HbA1c) varies dose-dependently (with the appointment of 1 to 4 mg / day). In a number of patients, especially those with high fasting glucose levels, the effect is achieved at a dose of 6 mg. Reduces the risk of developing retino-, neuro- and nephropathy. With combined use, it can reduce the dose of insulin in obese patients by 38%.

In experiments on animals, there were no cases of mutagenic, carcinogenic and teratogenic effects, effects on fertility.

After oral administration, it is completely absorbed from the gastrointestinal tract. The time to reach C max is 2-3 hours. The volume of distribution is 8.8 l (113 ml / kg), total Cl is 47.8 ml / min, plasma protein binding approaches 100%. In the liver, almost all of it is oxidized to cyclohexylhydroxymethyl derivative (with the participation of cytochrome P450 IIC9), which has 1/3 of the pharmacological activity of glimepiride, and then (with the participation of one or more cytosolic enzymes) to an inactive carboxyl metabolite. T 1/2 - 5-8 hours Excreted mainly as metabolites in the urine (60% of the administered dose) and faeces (40%). Does not accumulate.

Application of the substance Glimepiride

Diabetes mellitus type 2.

Contraindications

Hypersensitivity, type 1 diabetes mellitus, diabetic ketoacidosis, diabetic precoma and coma, severe liver and kidney dysfunction, leukopenia, pregnancy, lactation.

Application restrictions

Conditions requiring the patient to be transferred to insulin therapy: extensive burns, severe multiple trauma, major surgical interventions, malabsorption of food and drugs in the gastrointestinal tract (including intestinal obstruction, intestinal paresis), febrile syndrome, alcoholism, adrenal insufficiency, thyroid disease , hypothyroidism or thyrotoxicosis.

Use during pregnancy and lactation

In the event of pregnancy, it is necessary to transfer the patient to insulin treatment as soon as possible.

At the time of treatment should stop breastfeeding.

Side effects of glimepiride

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): rarely - lowering blood pressure, thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis, erythropenia, pancytopenia, hemolytic and aplastic anemia.

From the nervous system and sensory organs: dizziness, headache, transient blurred vision.

From the digestive tract: nausea, vomiting, abdominal pain, feeling of heaviness in the epigastric region, diarrhea, intrahepatic cholestasis.

From the side of metabolism: hypoglycemia.

Others: increased levels of transaminases, hyponatremia, skin allergic reactions, tardive cutaneous porphyria, asthenia; rarely - shortness of breath, hepatitis, allergic vasculitis, photosensitivity.

Interaction

Hypoglycemia is increased by NSAIDs and other drugs with a high degree of binding to plasma proteins (sulfonamides, chloramphenicol, coumarins, probenecid), MAO inhibitors, insulin, beta-blockers, miconazole, allopurinol, ACE inhibitors, PAS, pentoxifylline (with parenteral administration in high doses) , quinolones, anabolic steroids, male sex hormones, salicylates, tetracyclines, tritoqualin, triphosphamide. Effect weaken (cause hyperglycemia) thiazide diuretics, corticosteroids, phenothiazines, thyroid hormones, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, isoniazid, barbiturates, acetazolamide, rifampicin, laxatives (with prolonged use). Alcohol can either increase or decrease hypoglycemic activity. Propranolol increases C max , AUC and T 1/2 (by an average of 20%). Reduces (slightly) hypocoagulation caused by warfarin. Recombinant alpha-interferons increase the risk of developing thyroid dysfunction.

Overdose

Symptoms: hypoglycemia, up to the development of coma.

Treatment: IV bolus of 50% glucose solution followed by infusion of 10% glucose solution. If the patient is conscious, a sweet hot drink is recommended. It is necessary to constantly monitor and maintain vital functions, blood glucose concentration (at the level of 5.5 mmol / l) for at least 24-48 hours (repeated episodes of hypoglycemia are possible).

Routes of administration

inside

Glimepiride Substance Precautions

Treatment is started only if diet and exercise do not normalize blood glucose levels. At the beginning of therapy, when selecting a dose, it is recommended to determine the concentration of glucose on an empty stomach and every 4 hours; in the future, it is necessary to control the fasting glucose level and the glucose content in the daily urine, periodically (every 3-6 months) to determine glycated hemoglobin. In case of insufficient effect or weakening of action (secondary resistance), a combination with insulin is recommended. Against the background of constant intake, hyperglycemia is possible as a result of various stressful effects - fever, trauma, infectious disease, surgery (in these cases, insulin is temporarily prescribed). A high risk of developing hypoglycemia exists in debilitated and malnourished patients, with adrenal, pituitary or liver failure. The likelihood of hypoglycemia is increased by alcohol, skipping meals, a calorie deficit in the diet, heavy and prolonged physical exertion. Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention.

Interactions with other active substances

Trade names

Name	The value of the Wyshkovsky Index ®