Amaryl appointment. Amaryl tablets: instructions for use. Amaryl side effects

1 tablet contains 4 mg glimepiride

Release form:

Blue tablets for oral administration, 30 pieces per pack

Pharmachologic effect:

Oral hypoglycemic drug - III generation sulfonylurea derivative.

Glimepiride reduces the concentration of glucose in the blood, mainly by stimulating the release of insulin from the β-cells of the pancreas. Its effect is predominantly associated with an improvement in the ability of pancreatic β-cells to respond to physiological glucose stimulation. Compared to glibenclamide, low doses of glimepiride cause less insulin to be released while achieving approximately the same reduction in blood glucose concentration. This fact testifies in favor of the presence of extrapancreatic hypoglycemic effects in glimepiride (increased tissue sensitivity to insulin and insulinomimetic effect).

Indication for use:

Diabetes mellitus type 2 (as monotherapy or in combination therapy with metformin or insulin).

Method of administration and dosage:

Typically, the dose of Amaryl is determined by the target blood glucose concentration. The drug should be used in the minimum dose sufficient to achieve the required metabolic control.

During treatment with Amaryl, it is necessary to regularly determine the level of glucose in the blood. In addition, regular monitoring of the level of glycosylated hemoglobin is recommended.

Violation of the drug intake, for example, skipping the next dose, should not be replenished by taking the drug at a higher dose.

The doctor should instruct the patient in advance about the actions that should be taken in case of errors in taking the drug Amaryl (in particular, when you miss a dose or when you skip a meal), or in situations where it is not possible to take the drug.

Amaryl tablets should be taken whole, without chewing, with a sufficient amount of liquid (about 1/2 cup). If necessary, tablets of the drug Amaryl can be divided along the lines into two equal parts.

The initial dose of the drug Amaryl is 1 mg 1 time / day. If necessary, the daily dose can be gradually increased (at intervals of 1-2 weeks) under regular monitoring of blood glucose and in the following order: 1 mg-2 mg-3 mg-4 mg-6 mg (-8 mg) per day ...

Contraindications:

• type 1 diabetes mellitus;
• diabetic ketoacidosis, diabetic precoma and coma;
• severe liver dysfunction (lack of clinical experience of use);
• severe renal dysfunction, incl. patients on hemodialysis (lack of clinical experience of use);
• pregnancy;
• lactation (breastfeeding);
• children's age (lack of clinical experience of use);
• rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• hypersensitivity to drug components;
• hypersensitivity to other sulfonylurea derivatives and sulfonamide drugs (risk of developing hypersensitivity reactions).

Special instructions:

In special clinical stressful conditions, such as trauma, surgery, infections occurring with febrile temperature, metabolic control may deteriorate in patients with diabetes mellitus, therefore, a temporary transfer to insulin therapy may be required to maintain adequate metabolic control.

In the first weeks of treatment, the risk of hypoglycemia may increase, which requires particularly careful monitoring of the blood glucose concentration.

At the beginning of treatment, after a change in treatment or with irregular intake of glimepiride, there may be a decrease in concentration of attention and speed of psychomotor reactions caused by hypo- or hyperglycemia. This can adversely affect the ability to drive vehicles or operate various machines and mechanisms.

Storage conditions:

The drug should be stored at a temperature not exceeding 25 ° C.

Structure

One tablet of Amarsh 1 mg contains: active substance: glimepiride - 1 mg;

excipients: lactose monohydrate, sodium carboxymethyl starch (t sp A), povidone 25000 (E1201), microcrystalline cellulose (E460), magnesium stearate (E470), iron dye red oxide (E172).

One tablet of Amarsh 2 mg contains: active substance: glimepiride - 2 mg;

auxiliary substances: lactose monohydrate, sodium carboxymethyl starch (type A), povidone 25000 (E1201), microcrystalline cellulose (E460), magnesium stearate (E470), iron dye yellow oxide (E172), indigo carmine aluminum varnish (E132).

One tablet of Amarsh 3 mg contains: active substance: glimepiride - 3 mg.

excipients: lactose monohydrate, sodium carboxymethyl starch (type A), povidone 25000 (E1201), microcrystalline cellulose (E460), magnesium stearate (E470), iron dye yellow oxide (E172).

One tablet of Amarsh 4 mg contains: active substance: glimepiride - 4 mg.

excipients: lactose monohydrate, sodium carboxymethyl starch (type A), povidone 25000 (E1201), microcrystalline cellulose, magnesium stearate (E460), indigo carmine aluminum varnish (E132).

Description

Amarsh 1 mg: oblong, flat on both sides pink tablets with a dividing groove on both sides. Upper stamp: NMK / Brand name. Bottom stamp: Brand name / NMK.

Amarsh 2 mg: Oblong green tablets flat on both sides with a dividing groove on both sides. Upper stamp: NMM / Brand name. Bottom stamp: Brand name / NMM.

Amarsh 3 mg: Oblong, light yellow tablets flat on both sides with a dividing groove on both sides. Upper stamp: NMN / Brand name. Bottom stamp: Brand name / NMN.

Amarsh 4 mg: Oblong, flat blue tablets on both sides with a dividing groove on both sides. Upper stamp: NMO / Brand name. Bottom stamp: Brand name / NMO.

pharmachologic effect

Glimepiride, the active substance of Amaryl, is a hypoglycemic (hypoglycemic) drug for oral administration - a sulfonylurea derivative.

Glimepiride stimulates the secretion and release of insulin from the beta cells of the pancreas (pancreatic action), improves the sensitivity of peripheral tissues (muscle and fat) to the action of their own insulin (extra-pancreatic action).

Insulin release

Sulfonylurea derivatives regulate insulin secretion by closing ATP-dependent potassium channels located in the cytoplasmic membrane of the beta cells of the pancreas. By closing potassium channels, they cause beta-cell depolarization, which helps open calcium channels and increase the flow of calcium into cells. Glimepiride at a high displacement rate attaches to and detaches from a pancreatic beta cell protein (molecular weight 65 kD / SURX), which is associated with ATP-dependent potassium channels, but differs from the usual binding site of traditional derivatives

sulfonylureas (140 kDa / SUR1 protein). ................ - X p\u003e

This process leads to the release of insulin by exocytosis, while. - the quality of the secreted insulin is significantly lower than with the action of traditional sulfonylureas. The least stimulating effect of glimepiride on insulin secretion also provides a lower risk of hypoglycemia.

Extrapankueatic activity

In addition, pronounced extrapancreatic effects of glimepiride (decrease in insulin resistance, less effect on the cardiovascular system, antiatherogenic, antiaggregatory and antioxidant effects) were shown, which are also possessed by traditional sulfonylurea derivatives, but to a much lesser extent.

An increase in the utilization of glucose from the blood by peripheral tissues (muscle and fat) occurs with the help of special transport proteins (GLUT1 and GLUT4) located in the cell membranes. Glucose transport to these tissues in type 2 diabetes mellitus is the rate-limiting step in glucose utilization. Glimepiride very rapidly increases the number and activity of glucose transporting molecules (GLUT1 and GLUT4), which leads to an increase in glucose uptake by peripheral tissues.

Glimepiride has a weaker inhibitory effect on KATf channels of cardiomyocytes. When taking glimepiride, the metabolic adaptation of the myocardium to ischemia remains.

Glimepiride increases the activity of glycosyl phosphatidylinositol-specific phospholipase C, with which drug-induced lipogenesis and glycogenesis can correlate in isolated muscle and fat cells.

Glimepiride inhibits glucose production in the liver by increasing intracellular concentrations of fructose-2,6-bisphosphate, which in turn inhibits gluconeogenesis.

Glimepiride selectively inhibits cyclooxygenase and reduces the conversion of arachidonic acid to thromboxane A2, which promotes platelet aggregation, thus exerting an antithrombotic effect.

Glimepiride contributes to the normalization of lipids, reduces the level of malaldehyde in the blood, which leads to a significant decrease in lipid peroxidation, this contributes to the antiatherogenic effect of the drug. Glimepiride increases the level of endogenous a-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase, which helps to reduce the severity of oxidative stress in the patient's body, which is constantly present in type 2 diabetes.

General information

In healthy individuals, the minimum effective oral dose of glimepiride is approximately 0.6 mg. The effect of glimepiride is dose dependent and reproducible. The physiological response to heavy physical activity and a decrease in insulin secretion while taking glimepiride is preserved.

There is no significant difference in effect depending on whether the drug was taken 30 minutes before meals or just before meals. In diabetic patients, satisfactory metabolic control over 24 hours can be achieved by taking a single daily dose.

Despite the fact that glimepiride hydroxymetabolite caused a small but significant decrease in blood glucose concentration in healthy patients, this metabolite is responsible for only a small part of the overall effect of the drug.

Combination therapy with metformin

In one clinical study, it was proved that in patients with unsatisfactory treatment results, despite the maximum doses of metformin, the simultaneous use of glimepiride with metformin provides better metabolic control compared to metformin monotherapy.

Combination therapy with insulin

There are few data on the combination of glimepiride with insulin. Patients with unsatisfactory results of treatment with maximum doses of glimepiride can begin simultaneous insulin therapy. In two clinical trials, combination treatment provided the same metabolic improvement as insulin monotherapy, however, in the case of combination therapy, lower doses of insulin were required.

Special groups of patents

Children and adolescents

A clinical study with active control (glimepiride up to 8 mg per day or metformin up to 2,000 mg per day) for 24 weeks was conducted in 285 children (8-17 years old) with type 2 diabetes. Both glimepiride and metformin showed a significant decrease in HbAlc relative to baseline [glimepiride -0.95 (serum 0.41); metformin -1.39 (serum 0.40)]. Despite this, glimepiride did not meet the criteria of “no worse than metformin” status, judging by the average change in HbAlc relative to baseline. The difference was 0.44% in favor of metformin. Upper Limit (1.05) 95% Confidence

the interval for the difference was above the permissible limit of not less efficiency equal to 0.3%,

Glimepiride treatment did not reveal any additional safety concerns for children compared with those available for adult patients with type 2 diabetes. Long-term efficacy and safety data for pediatric patients are lacking.

Pharmacokinetics

Suction

When taken orally glimepiride, its bioavailability is complete. Food intake has no significant effect on absorption, with the exception of a slight slowdown in the rate of absorption. With repeated administration of glimepiride in a daily dose of 4 mg, the maximum concentration in the serum (C max) is reached after about 2.5 hours and is 309 ng / ml; there is a linear relationship between dose and Cmax and between dose and AUC (area under the concentration-time curve).

Distribution

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

Biotpansformatsh and excretion

After a single oral dose of glimepiride, 58% are excreted in the urine and 35% in the feces. No unchanged substance was found in the urine. The half-life at plasma concentrations of the drug in serum corresponding to a multiple dosing regimen is 5-8 hours. After taking high doses, the half-life increases slightly.

In urine and feces, two inactive metabolites are detected, formed as a result of metabolism in the liver, one of them is a hydroxy derivative, and the other is a carboxy derivative. After oral administration of glimepiride, the terminal half-life of these metabolites is 3-5 hours and 5-6 hours, respectively.

Glimepiride is excreted in breast milk and crosses the placental barrier. The drug poorly penetrates the blood-brain barrier.

Comparison of single and multiple (once a day) administration of glimepiride did not reveal significant differences in pharmacokinetic parameters, and their very low variability was observed between different patients. There was no significant accumulation of the drug.

Special groups of patents

Pharmacokinetic parameters are similar in patients of different sexes and different age groups. In patients with impaired renal function (with low creatinine clearance), there was a tendency to an increase in the clearance of glimepiride and to a decrease in its average concentrations in the blood serum, which is most likely due to a more rapid excretion of the drug due to its lower binding to protein. Thus, this category of patients does not have an additional risk of drug accumulation.

A trial to study the pharmacokinetics, safety and tolerance of a single 1 mg dose of glimepiride in 30 pediatric patients (4 children aged 10-12 years and 26 children aged 12-17 years) with type 2 diabetes mellitus showed that the average AUCo -i as t, C max and X \\ a analogs chny values \u200b\u200bpreviously observed in adults.

Indications for use

Diabetes mellitus type 2 (in monotherapy or as part of combination therapy with metformin or insulin) if adequate control is not possible only through diet, exercise or weight loss.

Contraindications

Glimepiride should not be used when:

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

Insulin-dependent diabetes mellitus;

Diabetic ketoacidosis, diabetic precoma and coma;

Severe liver dysfunction;

Severe renal dysfunction (including patients on hemodialysis);

Pregnancy and lactation.

Pregnancy and lactation

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

Since glimepiride appears to pass into breast milk, it should not be given to women during lactation. In this case, it is necessary to switch to insulin therapy or stop breastfeeding.

Method of administration and dosage

Intended for oral administration.

Adequate diet, regular exercise, and regular monitoring of blood and urine counts are key to successful diabetes management. Deviations from dietary recommendations cannot be compensated for by either pills or insulin.

Initial dose and dose selection

The dosage of glimepiride is determined by the results of the analysis of glucose in the blood and urine.

The initial dose is 1 mg glimepiride per day, if successful metabolic control is achieved, this dose should be maintained during treatment.

For other dosage regimens, tablets with appropriate dosages are available.

If necessary, the daily dose can be gradually increased under regular monitoring of the concentration of glucose in the blood (at intervals of 1-2 weeks) and in the following order: 1 mg - 2 mg - 3 mg - 4 mg glimepiride per day.

A dose of glimepiride in excess of 4 mg per day leads to better results 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. As a rule, it is sufficient to prescribe a daily dose in 1 reception immediately before or during a hearty breakfast or, if the daily dose is not

was taken immediately before or during the first large meal. The missed dose should not be corrected by the subsequent administration of a higher dose. Amaril tablets are taken whole, without chewing, with a sufficient amount of liquid (about 0.5 cups). It is very important not to skip a meal after taking Amaril.

Use in combination with metformin

In the case of insufficient stabilization of blood glucose concentration in patients taking metformin, concomitant therapy with glimepiride may be initiated. While maintaining the dose of metformin at the same level, treatment with glimepiride begins with a minimum dose, and then its dose is gradually increased depending on the desired level of glycemic control, up to a maximum daily dose of 6 mg. The combination therapy should be carried out under close medical supervision.

Use in combination with insulin

In cases where normalization of blood glucose concentration cannot be achieved by taking the maximum dose of glimepiride in monotherapy or in combination with the maximum dose of metformin, a combination of glimepiride with insulin is possible. In this case, the last dose of glimepiride prescribed to the patient remains unchanged. In this case, insulin treatment begins with a minimum dose, with a possible subsequent gradual increase in the insulin dose under the control of the blood glucose concentration. Combined treatment requires mandatory medical supervision. While maintaining long-term glycemic control, this combination therapy can reduce insulin requirements by up to 40%.

Transfer of a patient from another oral hypoglycemic drug to glimepiride There is no exact relationship between the doses of glimepiride and other oral hypoglycemic drugs. When switching from such drugs to glimepiride, the initial daily dose of the latter should be 1 mg (even if the patient is transferred to glimepiride from the maximum dose of another oral hypoglycemic drug). Any dose escalation of glimepiride should be done in stages, taking into account the response to glimepiride in accordance with the recommendations above. The dose used and the duration of the effect of the previous hypoglycemic agent must be taken into account. In some cases, especially when taking hypoglycemic drugs with a long half-life (for example, chlorpropamide), it may be necessary to temporarily (over several days) discontinue treatment in order to avoid an additive effect that increases the risk of hypoglycemia.

Transfer of a patient from insulin to glimepiride

In exceptional cases, if patients with type 2 diabetes mellitus receive insulin therapy, then with compensation for the disease and with the preserved secretory function of the beta cells of the pancreas, they may be shown transfer to glimepiride. The translation must be carried out under the close supervision of a physician. In this case, the transfer of the patient to glimepiride begins with a minimum dose of glimepiride of 1 mg.

Application for renal and hepatic insufficiency

There is insufficient information on the use of the drug in patients with renal and hepatic insufficiency (see section Contraindications).

Children and adolescents

There are no data on the use of glimepiride in patients under 8 years of age. For children aged 8 to 17 years, there are limited data on the use of glimepiride as monotherapy (see section Pharmacokinetics and Pharmacodynamics). The available efficacy and safety data are insufficient for the use of glimepiride in pediatrics, and therefore such use is not recommended.

Side effect

The following are data obtained during clinical studies on adverse reactions caused by taking glimepiride and other sulfonylurea derivatives. Adverse reactions are grouped by classes of organ systems and divided into groups in decreasing order of frequency of occurrence (very common:\u003e 1/10; often:\u003e 1/100,< 1/10, нечасто: > 1/1000, < 1/100, редко: > 1/10000, < 1/1000, очень редко: < 1/10000; частота неизвестна (частота встречаемости не может быть оценена на основании имеющихся данных)).

Lymphatic and hematopoietic disorders

Rarely: thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis,

erythrocytopenia, hemolytic anemia, and pancytopenia, which are usually reversible when the drug is discontinued.

Immune system disorders

Very rare: leukocytoplastic vasculitis, moderate hypersensitivity reactions that can progress to life-threatening conditions, accompanied by a drop in blood pressure, dyspnea, and sometimes anaphylactic shock.

Frequency unknown: It is possible to develop cross-allergic reactions with other sulfonylurea derivatives, sulfonamide drugs and similar substances.

Metabolic disorders Rare: hypoglycemia.

These reactions mainly occur soon after taking the drug, can become dangerous, and cannot always be easily controlled. The occurrence of such reactions depends, as in the case of other types of hypoglycemic therapy, on a number of individual factors, such as dietary habits and drug dosage (for more information, see section. Special instructions and precautions for use).

Violations of the organs of vision

Frequency unknown: temporary visual impairment may occur, especially at the beginning of treatment, due to changes in glucose concentration.

From the digestive system

Very rare: nausea, vomiting, diarrhea, feeling of pressure, heaviness or discomfort in the abdomen, abdominal pain, in rare cases leading to discontinuation of treatment.

From the hepatobiliary system

The frequency is unknown - an increase in the level of liver enzymes.

Very rare: abnormal hepatic function (eg, cholestasis or bile leakage), hepatitis, and liver failure.

Skin and subcutaneous tissue disorders

Frequency not known ", skin hypersensitivity reactions may occur in the form of itching, rash, urticaria and photosensitivity.

Laboratory results

Very rare: a decrease in the concentration of sodium in the blood.

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 concentration. Hypoglycemia can almost always be quickly relieved by immediate intake of carbohydrates (glucose or sugar, such as 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. Sugar substitutes are ineffective in the treatment of hypoglycemia. In most cases, inpatient monitoring is recommended. Treatment includes induction of vomiting, fluid intake (water or lemonade with activated carbon (adsorbent) and sodium sulfate (laxative). When taking large amounts of the drug, gastric lavage is indicated, followed by the introduction of activated charcoal and sodium sulfate. The clinical picture of severe hypoglycemia may be similar to the clinical picture of stroke, therefore, it requires immediate treatment under the supervision of a doctor, and under certain circumstances, hospitalization of the patient.As soon as possible, begin the administration of glucose, if necessary in the form of an intravenous jet injection of 50 ml of a 40% solution, followed by an infusion of 10% solution with careful monitoring of the concentration of glucose in the blood.In further treatment should be symptomatic.

Symptoms of hypoglycemia may be mitigated or completely absent in elderly patients, in patients with autonomic neuropathy or receiving concomitant treatment with β-blockers, clonidine, reserpine, guanethidine or other sympatholytic agents.

If a patient with diabetes is treated by different doctors (for example, during a hospital stay after an accident, during an illness on weekends), he must inform them of his illness and previous treatment.

In the treatment of hypoglycemia resulting from the accidental intake of Amaril in infants or young children, the indicated dose of dextrose (50 ml of a 40% solution) should be carefully controlled in order to avoid dangerous hyperglycemia. In this regard, continuous and careful monitoring of blood glucose concentration is necessary.

Interaction with other medicinal products

In the case of concomitant administration of some other drugs with glimepiride, both an undesirable decrease and an undesirable increase in the hypoglycemic effect of glimepiride may occur. In this regard, other drugs can only be taken with the permission (or prescription) of a doctor.

Glimepiride is metabolized by cytochrome P4502C9, which should be taken into account when used simultaneously with inducers (for example, rifampicin) or inhibitors (for example, fluconazole).

Based on experience with glimepiride and other sulfonylurea derivatives, the following interactions should be noted.

An increase in the hypoglycemic effect and the associated possible development of hypoglycemia can be observed with the simultaneous use of glimepiride with the following drugs:

Phenylbutazone, Azapropazone, Oxyphenbutazone,

Insulin and other hypoglycemic drugs such as metformin

Salicylates and aminosalicylic acid,

Anabolic steroids and male sex hormones,

Chloramphenicol, some long-acting sulfonamides, tetracyclines, quinolones and clarithromycin,

Coumarin anticoagulants,

Fenfluramine,

Disopyramide,

Fibrates,

Angiotensin-converting enzyme (ACE) inhibitors,

Fluoxetine, monoamine oxidase (MAO) inhibitors,

Allopurinol, Probenicid, Sulfinpyrazone,

Sympatholytics,

Cyclo-, tro- and ifosfamides,

Miconazole, fluconazole,

Pentoxifylline (for parenteral administration in high doses),

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 the following drugs:

Estrogens and progestogens,

Saluretics and thiazide diuretics,

Thyroid hormones, glucocorticosteroids

Phenothiazines, chlorpromazines,

Epinephrine and other sympathomimetic drugs,

Nicotinic acid (in high doses) and nicotinic acid derivatives,

Laxatives (with long-term use)

Phenytoin, diazoxide,

Glucagon, barbiturates and rifampicin

Acetazolamide.

Blockers of H 2 -receptors, clonidine and reserpine are capable of both increasing and weakening the hypoglycemic effect of glimepiride.

Under the influence of sympatholytic agents such as beta-blockers, clonidine, guanethidine and reserpine, the signs of adrenergic counterregulation in response to hypoglycemia may diminish or be absent.

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

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

Application features

Glimepiride should be taken immediately before or during meals.

If meals are taken at irregular intervals or are skipped altogether, the patient receiving glimepiride therapy may develop

hypoglycemia. Possible symptoms of hypoglycemia include: headache, severe hunger, nausea, vomiting, tired feeling, drowsiness, sleep disturbances, anxiety, aggressiveness, impaired concentration, attention and reaction, depression, confusion, speech and visual disturbances, aphasia, tremors, paresis , sensory disturbances, dizziness, feelings of helplessness, loss of self-control, delirium, cerebral convulsions, confusion and loss of consciousness, including coma, shallow breathing, bradycardia. In addition, as a result of the adrenergic feedback mechanism, symptoms such as cold, clammy sweat, anxiety, tachycardia, arterial hypertension, heart palpitations, angina pectoris, and heart rhythm disturbances can occur.

The clinical picture of severe hypoglycemia may resemble the clinical picture of stroke.

In almost all cases, symptoms can be promptly controlled by immediate intake of carbohydrates (sugar). Artificial sweeteners are not effective in this case.

As is known from the experience of using other sulfonylurea derivatives, despite the successful application of countermeasures at the beginning, hypoglycemia may subsequently reappear.

Severe or prolonged hypoglycemia, which is only temporarily controlled by the intake of normal amounts of sugar, requires immediate medical attention or even hospitalization.

Factors contributing to the development of hypoglycemia include:

Unwillingness or (usually in old age) insufficient ability of patients to cooperate with a doctor, inadequate, irregular nutrition, skipping meals, fasting,

Changes in your diet

An imbalance between exercise and carbohydrate intake

Drinking alcohol, especially when combined with skipping meals,

Renal dysfunction, severe liver dysfunction,

Glimepiride overdose

Certain uncompensated diseases of the endocrine system that affect carbohydrate metabolism, or feedback hypoglycemia (for example, some thyroid dysfunction, pituitary insufficiency, or adrenal cortex insufficiency), concomitant use of certain other drugs (see Interaction with other drugs) ...

Treatment with glimepiride requires regular monitoring of blood and urine glucose concentrations. In addition, the determination of the level of glycosylated hemoglobin is recommended.

Also, during treatment with glimepiride, regular liver function tests and blood counts (especially leukocytes and platelets) are necessary.

In stressful situations (for example, after accidents, urgent operations, febrile infections, etc.), a temporary switch to insulin may be indicated.

There is no experience with glimepiride in patients with severe renal insufficiency or in patients requiring hemodialysis. For patients with severe renal or hepatic impairment, a switch to insulin is indicated.

Treatment with sulfonylurea derivatives can lead to hemolytic anemia in patients with glucose-6-phosphate dehydrogenase deficiency. Since glimepiride belongs to the class of sulfonylurea derivatives, it should be used with caution in patients with glucose-b-phosphate dehydrogenase deficiency. In addition, treatment options should be considered with alternatives that do not contain sulfonylurea derivatives.

Amaryl contains lactose monohydrate, so it should not be taken by patients with hereditary lactose intolerance, lactase deficiency or glucose-lactose malabsorption.

The study of the effect of glimepiride on the ability to drive vehicles and mechanisms has not been conducted. The patient's response or ability to concentrate may be reduced as a result of hypoglycemia or hyperglycemia, or, for example, due to visual impairment. These effects can be dangerous in situations where these abilities are of particular importance (for example, when driving a car or equipment).

Patients should be informed of the need to take precautions to avoid hypoglycemia while driving. This is especially important for patients with frequent episodes of hypoglycemia, or patients who are insufficiently or completely unaware of the early signs of hypoglycemia. In these cases, the advisability of driving or operating machinery should be considered.

Amaryl is a pill from a German manufacturer with hypoglycemic action.

Designed for type 2 diabetics.

Helps to reduce the concentration of glucose in the blood.

General characteristics, release form and composition

The drug is commercially available in 4 dosages, depending on the amount of active substance:

• pink tablets - 1 mg
• greenish - 2 mg
• light yellow - 3 mg
• bluish - 4 mg

The active ingredient is glimepiride. In addition to this form, there is a combined Amaryl M, which contains metformin.

Amaryl M is commercially available in 2 dosages, represented by the following component composition of glimepiride / metformin:

• 2 mg / 500 mg
• 1 mg / 200 mg

In contrast to the previous form, Amaryl M is presented in white and biconvex.

Subject to the correct diet, a complex of gymnastic exercises aimed at weight loss, a high effectiveness of treatment for type 2 diabetes is guaranteed in the following cases:

• non-insulin dependent type 2 diabetes (as monotherapy or combination treatment with metformin or insulin);
• if it is impossible to achieve glycemic control with monotherapy with glimepiride or metformin;
• when replacing combination therapy with the use of one combined Amaryl M.

Amaryl is an essential drug for type 2 diabetics who do not use insulin.

Instructions for use

Amaryl is used according to the scheme prescribed by the attending physician. The dose is selected on a personal basis and depends on the stage of the disease.

Taking Amaril begins with a minimum daily dosage of 1 mg. It is consumed in the morning during the breakfast period or after it. The tablets are washed down with 1⁄2 glass of water.

In the absence of side effects, taking into account the patient's condition, the further treatment regimen with Amaril is as follows: once every 7-14 days (the rate of increase in dosage will be determined by the doctor), the intake increases by 1 mg and reaches 6-8 mg.

The last 2 dosages are used very rarely. The period from the initial to the next dosage ranges from 7-14 days. During the use of the drug, daily monitoring of blood glucose levels is mandatory.

If you miss a pill, an additional dose is not recommended, and the next day the dose remains the same.

Attention! Amaril is taken on a full stomach, otherwise fluctuations in blood sugar levels below the permissible norms are possible.

Application features

Amaryl is prohibited for pregnant and lactating women. This is due to the penetration of glimepiride into breast milk. The patient should follow insulin therapy.

The effect of the drug on children with type 2 diabetes is not fully understood. That is why Amaryl is contraindicated in children under 18 years of age.

It is known that the active component is excreted from the body through the kidneys. Therefore, the drug is not recommended for elderly people suffering from kidney disease. For healthy patients, the dosage is selected individually, which is associated with the risk of reduced renal function.

Patients should be prepared for a long course of treatment.

In addition, it is worth considering some features:

• skipping medication is not recommended;
• taken with food and washed down with a significant amount of liquid;
• swallowed whole;
• if necessary, it is divided into two equal parts;
• the distribution of the dosage is carried out by the doctor, taking into account the metabolic processes in the body;
• dose adjustment depends on body weight, standard of living and risks of hypoglycemia;
• the initial dosage is 1 mg, even with other medications at higher doses.

If necessary, the doctor can prescribe a combined treatment regimen, which will increase the effectiveness of the active substance of the drug.

Side effects and overdose

One of the most undesirable effects is a decrease in blood sugar concentration to a minimum, the symptoms of which are:

• feeling weak;
• dizziness;
• numbness of the limbs;
• overexcitation;
• feeling hungry;
• tachycardia or slow heartbeat;
• problems with visual functions.

The stronger the attack of hypoglycemia, the more pronounced the symptoms. Sometimes symptoms resemble a stroke, accompanied by unconsciousness and blurred consciousness.

The main task of this stage is to quickly bring blood glucose levels back to normal.

Other side effects of Amaril:

1. Nervous system... The patient feels dizzy, trouble sleeping, or excessive sleepiness. Feeling tired or suddenly aggressive is anxiety-provoking. Concentration is lost, psycho-motor reactions slow down. The patient feels helpless. Anxiety, loss of self-control, profuse sweating, seizures, depression can lead to coma.
2. Gastrointestinal tract... The negative effect of Amaril on the gastrointestinal tract is manifested by gag reflexes, sensations of pain in the epigastric region, nausea, diarrhea, discoloration of the skin to yellow, liver failure and hepatitis.
3. Vision... The side effects of the pills are felt early in the treatment. The patient experiences a weakening of vision, which is associated with abrupt changes in blood sugar levels.
4. Heart... Cardiac problems are indicated by attacks of sudden tachycardia, angina pectoris, bradycardia, arterial hypertension, or cardiac arrhythmias.
5. Blood... The blood formula changes. Anemia, leukopenia, thrombocytopenia, erythrocytopenia, granulocytopenia, pancytopenia, or agranulocytosis are possible.
6. Hypersensitivity of the skin... It is manifested by the occurrence of urticaria, an allergic rash. In this case, an allergic reaction can quickly turn into anaphylactic shock.

If these signs of an overdose or side effects occur, the patient must urgently seek help from a doctor. Self-first aid is to quickly take a lump of sugar, candy or sweet tea.

Drug interactions and analogues

When prescribing other drugs to a patient together with amaril, their interaction is taken into account:

• insulin and other hypoglycemic tablets lead to an increase in the hypoglycemic effectiveness of Amaril;
• adrenaline, sympathomimetics - a decrease in the hypoglycemic effect is possible;
• reserpine, clonidine, histamine H2 receptor blockers - instability of the hypoglycemic effect is possible;
• ethyl-containing products - depending on the concentration of ethanol in the blood, an increase or decrease in the hypoglycemic effect is possible.

Available analogues that have a similar effect, have the same active ingredient and are sold at an affordable price:

1. Glimepiride Canon... A cheap analogue of Amaril, which is prescribed when the therapeutic diet and physical activity are ineffective.
2. Glimepiride... A drug similar to Canon with the same active ingredient. Has contraindications. Independent use is prohibited. Production of the Russian Federation.
3. Diamerid... Type 2 diabetes pills. Recommended when diet and exercise are not effective. Forbidden in type 1 diabetes.

The selection of analogs should be entrusted to a specialist. The drugs are used according to the scheme. Spontaneous violation of dosages can lead to irreversible consequences for the body.

Patient opinion

From patient reviews, it can be concluded that Amaryl is quite effective, but requires precise adherence to dosages, since it has a lot of side effects.

More recently, as prescribed by a doctor, he began to take Amaryl. I believe that in order to obtain the desired effect, it is necessary to strictly observe the dosage and treatment regimen. Initially, I thought that the pills were not suitable for me, because my blood sugar levels were too high even after taking Amaril. But after increasing the dosage, Amaryl did the trick and proved effective.

Oleg, 39 years old, Voronezh

On taking Amaryl tablets, I want to say the following. I do not recommend conducting experiments on glucose levels using Amaril, since the harm done to the body can be irreparable. Take the tablets under the supervision of a doctor. For example, in addition to the recommendations of a specialist, I was trained at a diabetes school, which gave me the opportunity to evaluate and feel the effect of the drug on the body.

Inna, 36 years old, Moscow

Amaryl is taken according to the scheme. My dosage prescribed by my doctor is 2 mg. In addition, I drink siaphor 2 times a day. The blood count is 6-6.5, by the evening it drops to 3.9. I feel great, but the doctor has reduced the dosage of Amaril. You can't joke with these pills - there are many side effects and contraindications.

Igor, 45 years old, Chelyabinsk

Video material about the signs of type 2 diabetes:

Where is the medicine sold?

Amaryl is a drug that is sold in the pharmacy chain of any city. The price ranges from 238 rubles. up to 2550 rubles, which depends on the dosage of the active substance glimepiride and the number of tablets in the package.

You can buy quality pills at a price lower than in pharmacies through the online store. When buying medicines, pay attention to its originality, since there are many facts of acquiring counterfeit products.

INN: Glimepiride

Manufacturer: Sanofi S.P.A.

Anatomical-therapeutic-chemical classification: Glimepiride

Registration number in the RK: No. RK-LS-5 No. 011904

Registration period: 16.05.2017 - 16.05.2022

KNF (drugs are included in the Kazakhstan National Formulary of Medicines)

ALO (Included in the List of Free Outpatient Drug Provision)

UNIT (Included in the List of Medicines under the guaranteed volume of medical care to be purchased from a Single Distributor)

Maximum purchase price in the Republic of Kazakhstan: 66.67 KZT

Instructions

Tradename

International non-proprietary name

Glimepiride

Dosage form

4 mg tablets

Structure

One 4 mg tablet contains

active substance -glimepiride 4 mg,

excipients: lactose monohydrate, sodium starch glycolate (type A), povidone 25000, microcrystalline cellulose, magnesium stearate, indigo carmine aluminum varnish (E 132).

Description

4 mg tablets

Tablets, oblong, with a flat surface on both sides, light blue with a break line on both sides and marked NMO / company logo or company logo / NMO.

Amaril tablets 4 mg can be divided into equal doses.

Pharmacotherapeutic group

Sugar-lowering drugs for oral administration.

Sulfonylurea derivatives. Glimepiride.

ATX code А10ВВ12

Pharmacological properties

Pharmacokinetics

Suction

Glimepiride is fully bioavailable after oral administration. Food intake does not significantly affect the absorption of the drug, accompanied by only a slight decrease in the rate of absorption. Maximum serum concentrations (Cmax) are reached approximately 2.5 hours after oral administration (averaging 0.3 μg / ml with repeated doses of 4 mg per day), demonstrating a linear relationship between dose and Cmax and AUC ( area under the concentration versus time curve).

Distribution

Glimepiride has a very low volume of distribution (approximately 8.8 liters), approximately corresponding to the volume of distribution of albumin; high degree of protein binding (\u003e 99%) and low clearance (approx. 48 ml / min.). In preclinical studies, glimepiride is excreted in breast milk. Glimepiride is able to cross the placenta. The penetration rate through the blood-brain barrier is low.

Biotransformation and excretion

The mean dominant serum half-life, which is important for serum concentrations under repeated use conditions, is approximately 5-8 hours. After taking the drug in high doses, slightly longer half-lives were noted. After a single dose of glimepiride labeled with a radioactive isotope, 58% of the radioactivity was detected in the urine and 35% in the feces. No unchanged substance was found in the urine. In urine and faeces, two metabolites were identified, most likely products of hepatic metabolism (the main enzyme CYP2C9): a hydroxy derivative and a carboxy derivative. After oral administration of glimepiride, the terminal elimination half-lives of these metabolites were 3-6 and 5-6 hours, respectively.

Comparison of the results obtained with a single and multiple doses in the once a day regimen did not reveal significant differences in the parameters of pharmacokinetics, characterized by very low intraindividual variability of values. No significant accumulation of glimepiride was observed.

Special populations

The values \u200b\u200bof pharmacokinetic parameters were similar in men and women, as well as in young and elderly (over 65 years old) patients. In patients with low creatinine clearance, there was a tendency towards an increase in glimepiride clearance and a decrease in mean serum concentrations, most likely due to a faster excretion due to a lower degree of protein binding. In addition, impairment of renal excretion of two major metabolites was noted. In general, no additional risk of drug accumulation is expected in these patients.

Pharmacokinetic parameter values \u200b\u200bin five non-diabetic patients after bile duct surgery were similar to those observed in healthy individuals.

Pediatric population

A study evaluating the pharmacokinetics, safety and tolerability of glimepiride taken as a single dose of 1 mg in 30 pediatric patients (4 children aged 10-12 years and 26 children aged 12-17 years) with type 2 diabetes mellitus demonstrated average AUC values \u200b\u200b(0 -last.), Cmax and t1 / 2, similar to those previously observed in adults.

Pharmacodynamics

Glimepiride is an orally active hypoglycemic agent belonging to the group of sulfonylurea derivatives. It can be used for non-insulin dependent diabetes mellitus.

The action of glimepiride is mainly to stimulate the secretion of insulin by the beta cells of the pancreas.

As with other sulfonylureas, this effect is based on an increase in the response of pancreatic beta cells to stimulation by physiological glucose levels. In addition, glimepiride appears to have a pronounced extrapancreatic effect, also characteristic of other sulfonylurea derivatives.

Insulin secretion

Sulfonylurea derivatives regulate insulin secretion by closing the ATP-sensitive potassium channels of beta-cell membranes. Closing the potassium channels causes the beta cells to depolarize and by opening the calcium channels leads to an increase in the flow of calcium into the cells. This leads to the release of insulin by exocytosis.

Glimepiride binds with a high displacement rate to a beta-cell membrane protein that associates with ATP-sensitive potassium channels, but differs from the usual site of sulfonylurea binding.

Extrapancreatic activity

Extrapancreatic effects include, for example, improving the sensitivity of peripheral tissues to insulin and reducing the rate of insulin consumption by the liver.

The assimilation of glucose coming from the blood by peripheral muscle and adipose tissues occurs due to special transport proteins located in the cell membranes. The transport of glucose in these tissues is the step that limits the rate at which glucose is used by tissues. Glimepiride very rapidly increases the number of active glucose transporter molecules in the cell membranes of muscle and fat cells, which leads to stimulated glucose uptake.

Glimepiride enhances the activity of specific glycosyl phosphatidylinositol phospholipase C, which may be correlated with drug-induced lipogenesis and glycogenesis in individual fat and muscle cells. Glimepiride inhibits the production of glucose in the liver by increasing intracellular concentrations of fructose-2,6-bisphosphate, which, in turn, inhibits the processes of gluconeogenesis.

General properties

In healthy individuals, the minimum effective oral dose is approximately 0.6 mg. Glimepiride is dose-dependent and reproducible. The physiological response to strong physical activity, a decrease in insulin secretion, while using glimepiride, persists.

There were no significant differences in the nature of the action when the drug was taken 30 minutes before and immediately before meals. In patients with diabetes mellitus, sufficient metabolic control within 24 hours can be achieved with the drug once a day.

The hydroxymetabolite glimepiride, although it caused a small but significant decrease in serum glucose levels in healthy individuals, is responsible for only a small part of the overall effect of the drug.

Combination therapy with metformin

In one study in patients with insufficient control on metformin at maximum doses with concomitant use of glimepiride, an improvement in metabolic control was demonstrated compared to metformin monotherapy.

Combination therapy with insulin

At the moment, there are quite limited data on combination therapy in combination with insulin. Patients with insufficient disease control at the maximum dose of glimepiride may be prescribed concomitant insulin therapy. In two studies, combination therapy was accompanied by an improvement in metabolic control similar to that observed with insulin monotherapy; however, the combination therapy required the use of a lower mean insulin dose.

Special populations

Pediatric population

A 24-week study was conducted with active control (glimepiride at doses up to 8 mg per day or metformin at doses up to 2000 mg per day) in 285 children (aged 8-17 years) with type 2 diabetes mellitus.

The intake of glimepiride and metformin was accompanied by a significant decrease in HbA1c compared to the baseline level (glimepiride - 0.95 (SD 0.41); metformin -1.39 (SD 0.40)). However, the mean HbA1c change from baseline in the glimepiride group did not meet the metformin-like efficacy criterion. The difference between the treatment groups was 0.44% in favor of metformin. The upper limit (1.05) of the 95% confidence interval of the difference in values \u200b\u200bwas higher than the 0.3% limit of no less efficiency.

On the background of glimepiride therapy, no signals of new adverse reactions were observed in children compared with those observed in adult patients with type 2 diabetes. There are no data on the effectiveness and safety of long-term use of the drug in pediatric patients.

Indications for use

For the treatment of type 2 diabetes when diet, exercise and weight loss alone do not provide sufficient control of the disease.

Method of administration and dosage

For oral administration.

A good diet, regular exercise, and regular blood and urine tests are essential to successfully treating diabetes. Pills or insulin do not replace the need to follow the patient's recommended diet. Dosage is determined based on blood and urine glucose tests.

The starting dose is 1 mg glimepiride per day. If the appropriate level of control is achieved, this dosage should be used for maintenance therapy.

For various modes of use of the drug, there are appropriate release forms.

In case of insufficient control, it is necessary to gradually increase the dose, with an interval of 1-2 weeks between stages, based on the indicators of glycemic control, to 2, 3 or 4 mg of glimepiride per day.

A dosage of more than 4 mg of glimepiride per day gives better results only in exceptional cases. The maximum recommended dose is 6 mg glimepiride per day.

Patients whose disease cannot be adequately controlled at maximum daily doses of metformin may be prescribed concomitant therapy with glimepiride.

While maintaining the dose of metformin used, glimepiride therapy should be started at the lowest dose followed by titration up to the maximum daily dose, depending on the level of metabolic control desired. Such combination therapy should only be started under close medical supervision.

Patients who do not achieve a sufficient level of control when using Amaril at the maximum daily dose may, if necessary, be prescribed concomitant insulin therapy. While maintaining the dose of glimepiride used, insulin therapy should be started at a low dose and then increased, depending on the desired level of metabolic control. Such combination therapy should only be started under close medical supervision.

As a rule, a single daily dose of glimepiride is sufficient for the patient. It is recommended to take this dose immediately before or during a hearty breakfast, and if breakfast is skipped, then immediately before or during the first main meal.

If the patient forgets to take a dose, it should not be compensated for by increasing the next dose.

The tablets should be swallowed without chewing, with a little liquid.

If, while taking 1 mg of glimepiride once a day, a patient develops a hypoglycemic reaction, this indicates that only a proper diet can be enough for this patient to control the disease.

During treatment, as the control of diabetes mellitus improves, accompanied by an increase in insulin sensitivity, the need for glimepiride may decrease. Therefore, in order to avoid hypoglycemia, it should be remembered about the need for a timely dose reduction or discontinuation of therapy in such cases. A dose adjustment may also be required in case of changes in body weight or lifestyle, as well as other factors that increase the risk of developing hypo- or hyperglycemia.

- Going to Amaryl® with other oral hypoglycemic agents

Switching to Amaryl® from other oral hypoglycemic agents is generally allowed. When switching to Amaryl®, it is necessary to take into account the dosage and half-life of the previous drug. In some cases, in particular when taking antidiabetic agents with a long half-life (for example, chlorpropamide), a washout period of several days is recommended in order to minimize the risk of hypoglycemic reactions due to the additive effect.

- Switching from insulin to Amaryl®

In exceptional cases, when patients with type 2 diabetes mellitus are treated with insulin, a switch to treatment with Amaryl® may be indicated. Such a transition should be carried out under the close supervision of a physician.

- Special populations

Patients with impaired renal or hepatic function: see section "Contraindications".

- Pediatric population

There are no data on the use of glimepiride in patients under the age of 8 years. As for children aged 8 to 17 years, there are only limited data on the use of glimepiride as monotherapy (see sections "Pharmacokinetics" and "Pharmacodynamics"). Currently, insufficient data have been obtained on the safety and efficacy of the drug in the pediatric population, so such use is not recommended.

Side effects

Below is a list of adverse reactions noted in clinical trials with the use of Amaryl and other sulfonylurea derivatives. The corresponding reactions are listed in descending order of frequency of occurrence (very often: ≥ 1/10; often: from ≥ 1/100 to< 1/10; нечасто: от ≥ 1/1000 до < 1/100; редко: от ≥ 1/10 000 до < 1/1000; очень редко: < 1/10 000; с неизвестной [не поддающейся оценке по имеющимся данным] частотой возникновения).

Rarely

Thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis, erythropenia, hemolytic anemia and pancytopenia, which are usually reversible and disappear after the drug is stopped.

Hypoglycemia; such hypoglycemic reactions are generally immediate, may be severe, and not always easy to correct. The development of these reactions, as in the case of other hypoglycemic therapy regimens, depends on individual factors, such as dietary habits and dosage (for more details, see the "Special instructions" section).

Very rarely

Leukocytoclastic vasculitis, mild hypersensitivity reactions that can develop into serious reactions with difficulty breathing, a drop in blood pressure, and sometimes even shock

Nausea, vomiting, diarrhea, bloating, discomfort and pain in the abdominal area, which in rare cases lead to discontinuation of treatment

Liver dysfunction (eg, with cholestasis and jaundice), hepatitis, and liver failure

Decreased blood sodium levels

Frequency unknown

Possible development of cross-allergenicity with sulfonylurea derivatives, sulfonamides or related substances

Temporary visual disturbances may occur, particularly at the start of treatment, due to changes in blood glucose levels

Severe thrombocytopenia with a platelet count of less than 10,000 / μL and thrombocytopenic purpura

Elevated levels of liver enzymes

Skin hypersensitivity reactions, manifested in the form of itching, rash, urticaria and photosensitivity.

Reporting suspected adverse reactions

It is important to report suspected adverse reactions following drug registration. This allows you to continue monitoring the benefit / risk ratio of the drug. Health workers are asked to report any suspected adverse reactions through the national reporting system.

Contraindications

Hypersensitivity to glimepiride, other sulfonylurea drugs, sulfonamides, or any of the excipients

Insulin-dependent diabetes mellitus

Diabetic coma

Ketoacidosis

Severe renal or liver dysfunction. In case of severe impairment of kidney or liver function, it is necessary to transfer the patient to insulin

Children and adolescents up to 18 years old

Drug interactions

If glimepiride is taken concomitantly with certain other drugs, it may be accompanied by an undesirable increase or decrease in its hypoglycemic effect. In this regard, other drugs should be used only after informing the doctor (or on his prescription).

Glimepiride is metabolized by cytochrome P450 2C9 (CYP2C9). It is known that its metabolism is affected by the concomitant use of inducers (eg, rifampicin) or CYP2C9 inhibitors (eg, fluconazole).

Published results of a study of interactions under conditions in vivo show that the use of fluconazole, one of the most potent inhibitors of CYP2C9, is accompanied by an approximately 2-fold increase in the area under the concentration-time curve (AUC) of glimepiride.

Taking into account the experience of using glimepiride and other sulfonylurea derivatives, it seems necessary to point out the following interactions.

An increase in the effect of lowering blood glucose levels and, accordingly, the development of hypoglycemia in some cases can be observed with the use of one of the following drugs:

phenylbutazone, azapropazone and oxyphenbutazone

insulin and oral antidiabetic drugs such as metformin

salicylic acid salts and paraaminosalicylic acid preparations

anabolic steroids and male sex hormones

chloramphenicol, certain long-acting sulfonamides, tetracyclines, quinolone antibiotics, and clarithromycin

coumarin anticoagulants

fenfluramine

disopyramid

fibrates

aCE inhibitors

fluoxetine, MAO inhibitors

allopurinol, probenecid, sulfinpyrazone

sympatholytic agents

cyclophosphamide, trophosphamide and ifosfamides

miconazole, fluconazole

pentoxifylline (parenteral, high doses)

tritoqualine

The weakening of the effect of lowering blood glucose levels and, accordingly, increased blood glucose levels can be observed with the use of one of the following drugs:

estrogens and progestogens

saluretics and thiazide diuretics

thyrotropic drugs, glucocorticoids

derivatives of phenothiazine, chlorpromazine

adrenaline and sympathomimetics

nicotinic acid (in high doses) and nicotinic acid derivatives

laxatives (with prolonged use)

phenytoin, diazoxide

glucagon, barbiturates and rifampicin

acetazolamide

H2 receptor antagonists, beta-blockers, clonidine and reserpine can both increase and decrease the effect of lowering blood glucose levels.

Under the influence of sympatholytic drugs such as beta-blockers, clonidine, guanethidine, and reserpine, signs of adrenergic counterregulation in response to hypoglycemia may be reduced or absent.

Alcohol consumption can cause an unpredictable increase or decrease in the hypoglycemic effect of glimepiride.

Glimepiride is able to both enhance and weaken the action of coumarin derivatives.

Kolesevelam binds to glimepiride and reduces the absorption of glimepiride from the gastrointestinal tract. No interaction was observed when taking glimepiride, at least 4 hours before taking colesevelam. Therefore, glimepiride should be taken at least 4 hours before taking colesevelam.

special instructions

Amaryl® should be taken immediately before or with meals.

With irregular meals or skipping regular meals, treatment with Amaril can lead to the development of hypoglycemia. Possible symptoms of hypoglycemia include: headache, insatiable hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbances, agitation, aggressiveness, deterioration in concentration, weakening of attention and reaction, depression, confusion, speech and visual impairment, aphasia, tremor, paresis, sensory disturbances, dizziness, a state of helplessness, loss of self-control, delirium, cerebral cramps, drowsiness and loss of consciousness up to coma, shallow breathing and bradycardia. In addition, signs of adrenergic counterregulation such as sweating, clammy skin, anxiety, tachycardia, hypertension, palpitations, angina pectoris, and cardiac arrhythmias may be present.

The clinical picture of an attack of severe hypoglycemia may resemble the picture of a stroke.

Symptoms can almost always be stopped immediately by taking carbohydrates (sugar) immediately. Sugar substitutes are not effective in this case.

The practice of using other sulfonylurea derivatives shows that the re-development of hypoglycemia is possible, even despite the initial success of the measures taken.

Severe or prolonged hypoglycemia, only temporarily controlled by the use of normal amounts of sugar, requires immediate medical attention, and in some cases even hospitalization.

Factors contributing to the development of hypoglycemia include:

reluctance or (more often in older patients) inability of the patient to interact with healthcare professionals

undernutrition, irregular eating, skipping meals, or periods of fasting

diet changes

lack of balance between exercise and carbohydrate intake

drinking alcohol, especially when combined with skipping meals

renal dysfunction

serious liver dysfunction

amaril overdose

some uncompensated endocrine system disorders affecting carbohydrate metabolism or counter-regulation of hypoglycemia (as, for example, with certain thyroid dysfunctions and insufficiency of the adenohypophysis or adrenal cortex)

simultaneous use of some other drugs (see section "Drug interactions").

During treatment with Amaril, regular monitoring of blood and urine glucose levels is required. In addition, the determination of the level of glycated hemoglobin is recommended.

During treatment with Amaril, regular monitoring of hepatic and hematological parameters (in particular, the number of leukocytes and platelets) is required.

In stressful situations (for example, in accidents, emergency operations, infectious diseases with fever, etc.), a temporary switch to insulin may be indicated.

To date, no experience has been accumulated in the use of Amaril in patients with severe liver dysfunction or in patients on dialysis. For patients with severely impaired renal or hepatic function, a switch to insulin is indicated.

In patients with G6PD (glucose-6-phosphate dehydrogenase) deficiency, treatment with sulfonylurea derivatives can lead to the development of hemolytic anemia. Since glimepiride belongs to the class of sulfonylurea derivatives, it should be used with caution in patients with G6PD deficiency and an alternative non-sulfonylurea drug should be considered.

Amaryl® contains lactose monohydrate. Patients with rare congenital disorders such as galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this drug.

Amaryl® 6 mg tablets contains FCF (E110), an aluminum dye-color, sunset yellow, which may cause allergic reactions.

Pregnancy

Risks associated with diabetes

During pregnancy, abnormalities in blood glucose levels are accompanied by an increased incidence of congenital anomalies and perinatal mortality. Therefore, in order to avoid the risk of teratogenicity, blood glucose levels should be carefully monitored throughout pregnancy. In such circumstances, the use of insulin is necessary. Patients planning a pregnancy should inform their doctor about this.

Risks associated with glimepiride

At the moment, there is no relevant data on the use of glimepiride in pregnant women. Preclinical studies have demonstrated the presence of reproductive toxicity, which appears to be related to the pharmacological action (hypoglycemia) of glimepiride.

Accordingly, glimepiride should not be taken throughout pregnancy.

If during the treatment with glimepiride the patient plans to become pregnant or the fact of pregnancy is established, it is necessary to transfer her to insulin therapy as soon as possible.

Lactation

It is not known whether the drug is excreted in breast milk in breastfeeding women. In preclinical studies, it has been established that glimepiride is excreted in breast milk. Since other sulfonylurea derivatives can be excreted into human breast milk, and given the risk of hypoglycemia in breastfed infants, it is recommended to refrain from breastfeeding during glimepiride treatment.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Studies of the effect of the drug on the ability to drive vehicles and work with mechanisms have not been conducted.

As a result of hypoglycemia or hyperglycemia, or, for example, due to visual disturbances, the patient may experience a deterioration in concentration and response. This can pose a risk in situations where these abilities are especially important (for example, when driving or operating machinery).

Patients should receive appropriate advice on the precautions to be taken to avoid hypoglycemia while driving. This is especially important for individuals with little or no knowledge of the predictive symptoms of hypoglycemia, as well as for patients with frequent episodes of hypoglycemia. In such circumstances, it may be advisable to advise the patient to refrain from driving or operating machinery.

Overdose

Symptoms: after ingestion of an excessive dose, hypoglycemia may develop lasting from 12 to 72 hours, which may recur after the initial recovery. Symptoms of hypoglycemia may be absent for up to 24 hours after administration. Inpatient monitoring is usually recommended. The patient may have symptoms such as nausea, vomiting, and epigastric pain. In addition, hypoglycemia is often accompanied by a number of neurological symptoms such as restlessness, tremors, visual disturbances, coordination problems, drowsiness, coma, and seizures.

Treatment: is mainly to prevent absorption by stimulating vomiting, followed by drinking water or lemonade with activated carbon (adsorbent) and sodium sulfate (laxative). In case of ingestion of large amounts of the drug, gastric lavage is indicated, followed by the intake of activated carbon and sodium sulfate. In the event of a severe (severe) overdose, hospitalization in the intensive care unit is indicated. It is necessary to start administering glucose to the patient as soon as possible: if necessary, by bolus intravenous injection of 50 ml of a 50% solution, followed by an infusion of a 10% solution with careful monitoring of blood glucose levels. In the future, symptomatic treatment is prescribed.

In the treatment of hypoglycemia, caused, in particular, by the accidental intake of Amaril in infants or young children, it is necessary to carefully monitor the administered dose of glucose in order to avoid the possible development of dangerous hyperglycemia. Continuous monitoring of blood glucose levels is required.

Release form and packaging

Amaryl tablets for type 2 diabetes: learn everything you need to know. Below is an instruction manual written in clear language. Study the indications, contraindications, dosages, side effects, the ratio of benefits and harms to the body. Understand how to take Amaryl correctly, after how many hours the drug begins to act, whether it is compatible with alcohol. In the article, this remedy is compared with the tablets Diabeton, Glukofazh and Yanumet. Also listed are inexpensive analogues of domestic production. The drug Amaryl is not cheap in pharmacies, but it is convenient, because it is enough to drink it once a day. The active ingredient is glimepiride.

Medication for type 2 diabetes Amaryl: detailed article

Instructions for use

pharmachologic effect

Glimepiride causes the pancreas to vigorously produce insulin and release it into the bloodstream. Thanks to this, sugar decreases, especially after eating. In the liver, the active substance is oxidized with the participation of cytochrome P450 IIC9. Problems can arise when you are taking other drugs that compete for the same enzyme, such as rifampicin or fluconazole. It is excreted by 60% by the liver and 40% by the kidneys.

Indications for use

Type 2 diabetes - for patients who are not adequately supported by diet and physical activity to maintain normal blood sugar. Official medicine says glimepiride can be used in combination with metformin and insulin shots. claims that this drug is harmful and should be discarded. Read more why Amaryl is harmful and how to replace it.

Taking Amaryl, like any other pill for diabetes, you need to follow a diet.

Read more about healthy eating:

Contraindications	Type 1 diabetes mellitus, diabetic ketoacidosis, coma. Severe liver and kidney disease. Intolerance to the active substance glimepiride or other sulfonylurea derivatives. Malnutrition, irregular nutrition, impaired absorption of food in the gastrointestinal tract, restriction of calorie intake to 1000 kcal per day or less. Age under 18.
special instructions	You need to beware of hypoglycemia. Read the article "" carefully. Learn the symptoms of this acute complication, how to provide urgent care. In the first weeks of taking glimepiride, it is better not to do work that requires a quick physical and mental response. Treatment may increase the risk when driving.
Dosage	The appropriate dose of Amaryl is prescribed by the doctor. Diabetics should not do this on their own. The drug is available in various dosages - tablets of 1, 2, 3 and 4 mg. It is taken once a day before breakfast or the first main meal. The tablets can be divided in half, but cannot be chewed, they should be washed down with liquid.
Side effects	- a frequent and dangerous side effect. Other problems are rare. These are nausea, vomiting, a feeling of fullness in the stomach, diarrhea, itching, rash. The sensitivity of the skin to the sun's rays may increase, and sodium deficiency in the body may develop. Due to the rapid drop in blood sugar, vision may temporarily deteriorate.

Pregnancy and breastfeeding	Glimepiride and other sulfonylurea derivatives should not be taken during pregnancy and breastfeeding. If you are experiencing high blood sugar during pregnancy, read the "" and "" articles. Treat as written in them. Do not spontaneously take any glucose lowering pills.
Interaction with other medications	Amaryl can interact negatively with blood pressure pills, non-steroidal anti-inflammatory drugs, and many other popular medications. Read more in the instructions for use, which is in the package with the drug. Consult your doctor! Tell him about all the medications you are taking.

Overdose

Severe, life-threatening hypoglycemia may develop. Her symptoms, home and hospital treatment are described. Emergency medical attention is required for people who accidentally or knowingly swallow glimepiride or other sulfonylurea tablets.

Release form, shelf life, composition

The color of Amaryl tablets differs depending on the dosage. Tablets with the active ingredient glimepiride 1 mg are pink. 2 mg - green, 3 mg - pale yellow, 4 mg - blue. Excipients: lactose monohydrate, sodium carboxymethyl starch (type A), povidone 25,000, microcrystalline cellulose, magnesium stearate, and dyes. Keep out of reach of children at a temperature not exceeding 30 ° C. The shelf life is 3 years.

Read about preventing and treating complications:

Below are the answers to questions that people with type 2 diabetes often ask.

How to take Amaryl: before or after meals?

Amaryl is taken before meals, so that he has time to start acting by the time when the food eaten is absorbed. Typically, the doctor instructs the diabetic to take this medicine before breakfast. And if the patient usually does not eat breakfast, then take a pill before dinner. Analogs containing the active ingredient glimepiride should be taken in the same way.

Do not try to skip a meal after taking Amaryl. You must definitely eat, otherwise the medicine will lower your blood sugar too much and will. This is an acute complication that can cause symptoms of varying severity. From nervousness and palpitations to coma and death. The risk of hypoglycemia is one of the reasons why glimepiride is not recommended. You have a safe and effective one at your disposal.

Is this medication compatible with alcohol?

Instructions for the use of Amaryl tablets require diabetics to completely abstain from alcohol during the entire period of treatment with this drug. Because drinking alcohol increases the risk of hypoglycemia and liver problems. The incompatibility of the drug glimepiride with alcohol is a serious problem. Because it is a long-term, lifelong drug, not a short-term course of treatment.

At the same time, patients with type 2 diabetes who do not take harmful pills and are treated according to the law are not prohibited from drinking alcohol in moderation. Read more in the article “”. You can keep perfectly normal sugar and sometimes allow yourself to drink a glass or two without harm to your health.

How long does it take after taking it?

Unfortunately, there is no exact data on how long after taking Amaryl begins to act. Blood sugar goes down as much as possible after 2-3 hours. Most likely, the action of the drug begins much earlier, after 30-60 minutes. So do not delay eating to avoid hypoglycemia. The effect of each dose of glimepiride taken lasts more than a day.

Read about products for diabetics:

Which is better: Amaryl or Diabeton?

Both of these drugs are included in. It is better to refrain from taking them ..

Try to familiarize the doctor who prescribed Amaryl or Diabeton with the materials on this page. The original drug Diabeton dramatically increased mortality among patients who took it. Therefore, it was quietly removed from the sale. Now you can only buy pills. They act more gently, but are still harmful.

What is better to drink: Amaryl or Glucophage?

Amaryl is a harmful medicine .. - another matter. It is the original metformin drug and is an important part of the step-by-step treatment for type 2 diabetes. - the medicine is not harmful, but rather very useful. For good diabetes control, you must first switch to. A healthy diet is complemented by taking Glucophage medication, and, if necessary, also with insulin injections in low doses.

Can Yanumet and Amaryl be taken at the same time?

Amaryl and other tablets containing glimepiride should not be taken for the reasons listed above. Janumet is a combination medicine that contains metformin. At the time of this writing, it is very expensive and has no cheap analogues. In principle, you can take it. But you can try switching from it to pure metformin, best of all. If you can do this without compromising diabetes control, you will be saving a lot of money every month.

Analogs of the drug Amaryl

At the time of writing, only Glimepirid-Teva manufactured by Pliva Hrvatska, Croatia, was sold in pharmacies from imported analogues. At the same time, Amaryl has many Russian substitutes that are much cheaper than the original drug.

Russian analogues of the drug Amaryl

Each manufacturer produces all dosage options for the glimepiride drug - 1, 2, 3 and 4 mg. Check the availability of drugs and prices in pharmacies.

The original drug Amaryl or cheap analogues: what to choose

Read why Amaryl and its analogues are harmful why you need to refuse to accept them and what is better to replace. The site teaches the site to get to the norm and keep it stably normal without fasting, taking harmful and expensive drugs, injections of large doses of insulin.

Amaryl M: combination medicine

Amaryl M is a combination drug for type 2 diabetes. It contains two active ingredients in one tablet - glimepiride and. As you read above, glimepiride is harmful and shouldn't be taken. But metformin is not at all harmful, but on the contrary is very useful for diabetics. It lowers blood sugar, protects against diabetes complications, helps you lose weight and prolongs life.

What are the analogues of Amaryl M tablets?

Amaryl M is a combination tablet containing two active ingredients: glimepiride and metformin. All drugs that contain glimepiride are harmful. They can lower blood glucose levels for several years, and then the disease turns into severe type 1 diabetes. For diabetics who are treated with these pills, the risk of death from heart attack and stroke does not decrease, but rather even increases.

Instead of looking for analogues of Amaryl M, switch to pure metformin. Best of all is the original imported drug Glucophage. It is known to be of good quality and at an affordable price. Use also. You will be able to keep sugar consistently in the norm, like in healthy people, without a "hungry" diet and strenuous exercise.