Tablets for type 2 diabetes Amaryl. Amaryl tablets: instructions for use. Effect on platelet aggregation

1 tablet contains:

Active ingredients: glimepiride - 2 mg.

Excipients: lactose monohydrate, sodium carboxymethyl starch (type A), povidone 25,000, microcrystalline cellulose, magnesium stearate, indigo carmine (E132).

Description of the dosage form

Amaryl 1 mg: pink, oblong, flat tablets with a score line on both sides. Engraved "NMK" and stylized "h" on both sides.

Amaryl 2 mg: green, oblong, flat tablets with a score line on both sides. Engraved "NMM" and stylized "h" on both sides.

Amaryl 3 mg: pale yellow, oblong, flat tablets with a score line on both sides. Engraved "NMN" and stylized "h" on both sides.

Amaryl 4 mg: blue, oblong, flat tablets with a score line on both sides. Engraved "NMO" and stylized "h" on both sides.

Pharmacokinetics

When comparing data obtained with single and multiple (1 time/day) administration of glimepiride, no significant differences in pharmacokinetic parameters were revealed, and their variability between different patients was very low. There is no significant accumulation of the drug.

Suction

With repeated oral administration of the drug at a daily dose of 4 mg, Cmax in the blood serum is achieved in approximately 2.5 hours and is 309 ng/ml. There is a linear relationship between dose and Cmax of glimepiride in plasma, as well as between dose and AUC. When taken orally, the bioavailability of glimepiride is 100%. Food intake does not have a significant effect on absorption, except for a slight slowdown in its rate.

Distribution

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

Glimepiride is excreted in breast milk and penetrates the placental barrier.

Metabolism

Glimepiride is metabolized in the liver (mainly with the participation of the CYP2C9 isoenzyme) with the formation of 2 metabolites - hydroxylated and carboxylated derivatives, which are found in urine and feces.

Removal

T1/2 at plasma concentrations of the drug in serum corresponding to multiple dosing regimens is approximately 5-8 hours. After taking glimepiride in high doses, T1/2 increases slightly. After a single oral dose, 58% of glimepiride is excreted by the kidneys and 35% through the intestines. Unchanged active substance is not detected in urine.

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

Pharmacokinetics in special clinical situations

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

Pharmacodynamics

An oral hypoglycemic drug is a third generation sulfonylurea derivative.

Glimepiride reduces blood glucose concentrations, mainly by stimulating the release of insulin from pancreatic β-cells. Its effect is primarily associated with improving the ability of pancreatic β-cells to respond to physiological stimulation with glucose. Compared with glibenclamide, low doses of glimepiride cause the release of less insulin while achieving approximately the same reduction in blood glucose concentrations. This fact indicates that glimepiride has extrapancreatic hypoglycemic effects (increased tissue sensitivity to insulin and insulinomimetic effect).

Insulin secretion. Like all other sulfonylureas, glimepiride regulates insulin secretion through interaction with ATP-sensitive potassium channels on β-cell membranes. Unlike other sulfonylurea derivatives, glimepiride selectively binds to a protein with a molecular weight of 65 kilodaltons located in the membranes of pancreatic β-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 β-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 through exocytosis.

Glimepiride binds and is released from the binding protein much faster and, accordingly, more often than glibenclamide. It is assumed that this property of the high rate of exchange of glimepiride with the protein that binds to it determines its pronounced effect of sensitization of β-cells to glucose and their protection from desensitization and premature exhaustion.

The effect of increasing tissue sensitivity to insulin. Glimepiride enhances the effects of insulin on glucose uptake by peripheral tissues.

Insulinomimetic effect. Glimepiride has effects similar to those of insulin on glucose uptake into peripheral tissues and glucose output from the liver.

Glucose is absorbed by peripheral tissues by transporting it into muscle cells and adipocytes. Glimepiride directly increases the number of glucose transport molecules in the plasma membranes of muscle cells and adipocytes. An increase in the entry of glucose into cells leads to the activation of glycosylphosphatidylinositol-specific phospholipase C. As a result, the intracellular calcium concentration decreases, causing a decrease in the activity of protein kinase A, 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.

Effect on platelet aggregation. Glimepiride reduces platelet aggregation in vitro and in vivo. This effect appears to be due to selective inhibition of COX, which is responsible for the formation of thromboxane A, an important endogenous platelet aggregation factor. Antiatherogenic effect. Glimepiride helps normalize lipid levels, reduces the level of malonaldehyde in the blood, which leads to a significant reduction 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 type 2 diabetes. Glimepiride increases the level of endogenous α-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase.

Cardiovascular effects. Sulfonylureas also have effects on the cardiovascular system through ATP-sensitive potassium channels. Compared with traditional sulfonylurea derivatives, glimepiride has a significantly lesser effect on the cardiovascular system, which may 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 physical activity (decreased insulin secretion) is preserved when taking glimepiride.

There are no significant differences in the effect depending on whether the drug was taken 30 minutes before meals or immediately before meals. In patients with diabetes mellitus, sufficient metabolic control can be achieved within 24 hours with a single dose of the drug. Moreover, in a clinical study, 12 of 16 patients with renal failure (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. Two studies demonstrated improved metabolic control with combination therapy compared with either drug alone.

Combination therapy with insulin. In patients with insufficient metabolic control while taking maximum doses of glimepiride, concomitant insulin therapy may be initiated. Two studies found that this combination achieved the same improvement in metabolic control as insulin alone. However, combination therapy requires a lower dose of insulin.

Indications for use Amaryl

Type 2 diabetes mellitus (as monotherapy or as part of combination therapy with metformin or insulin).

Contraindications to the use of Amaryl

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

With caution: the drug should be used in the first weeks of treatment (increased risk of hypoglycemia); if there are risk factors for the development of hypoglycemia (adjustment of the dose of glimepiride or the entire therapy may be required); for intercurrent diseases during treatment or when changing the lifestyle of patients (changing diet and meal times, increasing or decreasing physical activity); with glucose-6-phosphate dehydrogenase deficiency; in cases of impaired absorption of food and drugs from the gastrointestinal tract (intestinal obstruction, intestinal paresis).

Amaryl Use during pregnancy and children

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

It has been established that glimepiride is excreted in breast milk. During lactation, the woman should be switched to insulin or breastfeeding should be stopped.

Amaryl Side effects

Metabolic: hypoglycemia is possible, which, as with the use of other sulfonylurea derivatives, can be prolonged. Symptoms of hypoglycemia - headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbances, anxiety, aggressiveness, impaired concentration, alertness and reaction speed, depression, confusion, speech disorders, aphasia, visual disturbances, tremor, paresis , sensory disturbances, dizziness, loss of self-control, delirium, cerebral spasms, drowsiness or loss of consciousness up to coma, shallow breathing, bradycardia. In addition, manifestations of adrenergic counterregulation in response to hypoglycemia may occur, such as the appearance of cold clammy sweat, anxiety, tachycardia, hypertension, angina, palpitations and cardiac arrhythmias. The clinical picture of severe hypoglycemia may resemble a stroke. Symptoms of hypoglycemia almost always disappear once it is corrected.

On the part of the organ of vision: transient visual impairment is possible (especially at the beginning of treatment), caused by 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 change in the refractive index of the lenses.

From the digestive system: rarely - 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 reverse when the drug is discontinued.

From the hematopoietic system: rarely - thrombocytopenia; in some cases - leukopenia, hemolytic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia. Cases of severe thrombocytopenia with platelet counts have been reported during post-marketing use of the drug.< 10 000/мкл и тромбоцитопенической пурпуре (частота неизвестна).

Allergic reactions: rarely - allergic and pseudo-allergic reactions, such as itching, urticaria, skin rash. Such reactions are almost always mild, but can develop into severe reactions with shortness of breath, a sharp decrease in blood pressure, which sometimes progress to anaphylactic shock; in some cases - allergic vasculitis.

Other: in some cases - hyponatremia, photosensitivity.

If symptoms of hives appear, you should consult a doctor immediately.

Drug interactions

Glimepiride is metabolized with the participation of the CYP2C9 isoenzyme, which should be taken into account when using the drug simultaneously with inducers (for example, rifampicin) or inhibitors (for example, fluconazole) of CYP2C9.

Potentiation of the hypoglycemic effect and, in some cases, the associated possible development of hypoglycemia can be observed when Amaryl is combined with one of the following drugs: insulin, other oral hypoglycemic agents, ACE inhibitors, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide , disopyramide, fenfluramine, pheniramidol, fibrates, fluoxetine, guanethidine, ifosfamide, MAO inhibitors, fluconazole, PAS, pentoxifylline (high parenteral doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, clarithromycin, sulfonamides, tetracyclines, tritoqualine , trophosfamide.

A decrease in the hypoglycemic effect and an associated increase in blood glucose concentration is possible when combined with one of the following drugs: acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, sympathomimetic agents (including epinephrine), glucagon, laxatives (with long-term use ), nicotinic acid (in high doses), estrogens and progestogens, phenothiazines, phenytoin, rifampicin, iodine-containing thyroid hormones.

Histamine H2 receptor blockers, beta-blockers, clonidine and reserpine can both enhance and reduce the hypoglycemic effect of glimepiride.

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

While taking glimepiride, the effect of coumarin derivatives may be enhanced or weakened.

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

Bile acid sequestrants: Colesevelam binds to glimepiride and reduces the absorption of glimepiride from the gastrointestinal tract. When glimepiride is administered at least 4 hours before colesevelam is administered orally, no interaction is observed. Therefore, glimepiride should be taken at least 4 hours before taking colesevelam.

Amaryl dosage

As a rule, 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 necessary metabolic control.

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

Violations in taking the drug, for example, missing a dose, should not be compensated for by subsequent administration of 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 missing a dose or skipping 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, Amaryl tablets can be divided lengthwise into two equal parts.

The initial dose of 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 .

In patients with well-controlled type 2 diabetes mellitus, the daily dose of the drug is usually 1-4 mg. A daily dose of more than 6 mg is more effective in only a small number of patients.

The doctor determines the time of taking Amaryl and the distribution of doses during the day, taking into account the patient’s lifestyle (time of meals, amount of physical activity). The daily dose is prescribed in 1 dose, usually immediately before a full breakfast or, if the daily dose has not been taken, immediately before the first main meal. It is very important not to skip meals after taking Amaryl tablets.

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

Conditions that may also require dose adjustment of glimepiride:

weight loss;
lifestyle changes (changes in diet, meal times, amount of physical activity);
the occurrence of other factors that lead to a predisposition to the development of hypoglycemia or hyperglycemia.

Treatment with glimepiride is usually long-term.

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

There is no exact relationship between the doses of Amaryl and other oral hypoglycemic drugs. When transferring from such drugs to Amaryl, the recommended initial daily dose of the latter is 1 mg (even if the patient is transferred to Amaryl from the maximum dose of another oral hypoglycemic drug). Any dose increase should be done in stages based on response to glimepiride, as recommended above. It is necessary to take into account the intensity and duration of the effect of the previous hypoglycemic agent. Interruption of treatment may be necessary to avoid additive effects that increase the risk of hypoglycemia.

Use in combination with metformin

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

Use in combination with insulin

In patients with poorly controlled diabetes mellitus, insulin may be prescribed concomitantly when taking glimepiride at the maximum daily dose. In this case, the last dose of glimepiride prescribed to the patient remains unchanged. In this case, insulin treatment begins with low doses, which are gradually increased under the control of blood glucose concentrations. Combined treatment is carried out under close medical supervision.

Patients with impaired renal function may be more sensitive to the hypoglycemic effect of glimepiride. Data on the use of Amaryl in patients with renal failure are limited.

Data on the use of Amaryl in patients with liver failure are limited.

Overdose

Symptoms: in case of acute overdose, as well as long-term treatment with glimepiride in excessively high doses, severe life-threatening hypoglycemia may develop.

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

Until the doctor decides that the patient is out of danger, the patient requires careful medical observation. It should be borne in mind that hypoglycemia may recur after the initial restoration of blood glucose concentrations.

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

Sometimes it may be necessary to hospitalize the patient, even if only as a precaution. Significant overdose and severe reactions with manifestations such as loss of consciousness or other serious neurological damage are medical emergencies and require immediate treatment and hospitalization.

In case of loss of consciousness, it is necessary to administer a concentrated solution of dextrose (glucose) intravenously (for adults, starting with 40 ml of a 20% solution). As an alternative, adults can administer glucagon IV, SC or IM, for example at a dose of 0.5-1 mg.

When treating hypoglycemia due to accidental ingestion of Amaryl® in infants or young children, the dextrose dose should be carefully adjusted to avoid the possibility of dangerous hyperglycemia; administration of dextrose should be carried out under constant monitoring of blood glucose concentrations.

In case of an overdose of Amaryl®, gastric lavage and activated charcoal may be required.

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

As soon as an overdose is detected, you must immediately inform your doctor.

Precautionary measures

In specific clinical stress conditions, such as trauma, surgery, infections, and febrile fever, metabolic control may deteriorate in patients with diabetes, so temporary switching to insulin therapy may be necessary to maintain adequate metabolic control.

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

Factors that contribute to the risk of developing hypoglycemia include:

the patient's reluctance or inability (more often observed in elderly patients) to cooperate with the doctor;
malnutrition, irregular eating or skipping meals;
diet change;
drinking alcohol, especially in combination with skipping meals;
severe renal dysfunction;
severe liver dysfunction (in patients with severe liver dysfunction, transfer to insulin therapy is indicated, at least until metabolic control is achieved);
overdose of glimepiride;
some decompensated endocrine disorders that impair carbohydrate metabolism or adrenergic counterregulation in response to hypoglycemia (for example, some disorders of the thyroid gland and anterior pituitary gland, adrenal insufficiency);
simultaneous use of certain medications;
taking glimepiride in the absence of indications for its use.

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

If the above risk factors for hypoglycemia are present, as well as if intercurrent diseases occur during treatment or changes in the patient's lifestyle, adjustment of the dose of glimepiride or the entire therapy may be necessary.

Symptoms of hypoglycemia, resulting from adrenergic counterregulation of the body in response to hypoglycemia, may be mild or absent when hypoglycemia develops gradually, in elderly patients, in patients with disorders of the autonomic nervous system, or in patients receiving beta-blockers, clonidine, reserpine , guanethidine and other sympatholytic agents.

Hypoglycemia can be quickly corrected by immediate administration of rapidly digestible carbohydrates (glucose or sucrose). As with other sulfonylureas, despite initial successful relief of hypoglycemia, hypoglycemia may recur. Therefore, patients should remain under constant monitoring. Severe hypoglycemia additionally requires immediate treatment and medical supervision, and in some cases, hospitalization of the patient.

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

Side effects such as severe hypoglycemia, serious changes in blood count, severe allergic reactions, liver failure can be life-threatening, therefore, in the event of such reactions, the patient should immediately inform the attending physician about them, stop taking the drug and not resume taking it without a doctor’s recommendation .

Use in pediatrics

There are no data on the long-term effectiveness and safety of the drug in children.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

At the beginning of treatment, after changing treatment, or when taking glimepiride irregularly, a decrease in concentration and speed of psychomotor reactions due to hypo- or hyperglycemia may be observed. This may adversely affect the ability to drive vehicles or operate various machines and mechanisms.

Elevated sugar levels are the cause of decreased quality of life in type 2 diabetes. Amaryl is designed to correct blood glucose due to the action of glimepiride. This substance is a sulfonylurea derivative.

Amaryl is a long-acting drug that not only reduces blood glucose concentrations, but also stimulates the beta cells of the pancreas.

This is a medicine that has passed all stages of testing and clinical trials, and not a dietary supplement.

In contact with

Amaryl for diabetes

Amaryl is prescribed by an endocrinologist for elevated blood sugar levels and diagnosed type 2 diabetes.

Compound

Contains different amounts of glimepiride:

Pink tablets contain 1 g of active ingredient;
Greens – 2 g;
Yellow – 3g;
Blue – 4 g

Additionally, markings are applied to the packaging. In addition to glimepiroid, the composition contains a negligible amount of lactose, sodium starch, microcrystalline cellulose and polyvidione, as well as a dye corresponding to the drug labeling.

All substances in the composition are suitable for use in type 2 diabetes in the dosages contained in the tablet.

The release form is tablets, the international name is Glimepiride, the price of Amaryl starts from 617 rubles.

Advantages and disadvantages

Advantages of the drug:

use of third generation derivatives;
speed of action;
protection against hypoglycemia;
ease of use;
prolonged action.

the dosage is selected by the doctor;
relatively high price;
In case of overdose, side effects are possible;
not suitable for diabetics with ketoacidosis;
not suitable for lactose intolerance;
not compatible with alcohol.

Indications

Amaryl is designed to “restart” the functioning of the pancreas in type 2 diabetes, and correct tissue sensitivity to insulin to normal.

It is used as a drug to lower blood sugar levels. Diagnosis is carried out individually, and the doctor makes a decision on prescribing the drug if the fasting sugar level is more than 6.9.

Usually the drug is prescribed along with lifestyle correction and a rational diet, and not as a pill that will “even the chances” of a diabetic and an ordinary person in the process of eating sweet foods.

The drug is not prescribed for prediabetes and temporary increases in glucose levels. It is contraindicated in type 1 diabetes.

For patients with concomitant type 2 diabetes, the drug can be prescribed along with Metformin; the doctor makes the choice between them based on the condition of the patient’s pancreas.

Operating principle

This is a “double action” drug:

Stimulates the production of its own insulin by the pancreas.
Reduces insulin resistance and normalizes the absorption of glucose by tissues.

Amaryl was developed as an alternative to cheaper drugs with a greater risk of hypoglycemia. Due to the active substance, it allows the pancreas to produce insulin in small doses. The risk increases if the dosage is selected incorrectly, or the dose of the drug is too high.

Amaryl has an antithrombotic and antiacidotic effect, it blocks neoglucogenesis in the liver, and corrects lipogenesis and glycogenesis.

Important: Obese diabetics must adhere to a diet. The product is not a “fat blocker” and any excess calories consumed will be stored as normal.

Instructions for use

Amaryl is taken before breakfast or together with it, without chewing and with a sufficient amount of water. The initial dosage is 1 mg.

A glucometer should be used to monitor your condition throughout the day. If the drug does not bring the desired reduction in blood sugar, an increase in dosage is required. In this case, additional doses of Amaryl may be prescribed.

The drug can be used together with, if the latter does not reduce sugar levels to normal. In this case, the dosage of Metformin is left the same, and Amaryl is increased.

Compatibility

Amaryl increases the effect of all drugs that lower sugar levels. It is not recommended to independently add any dietary supplements of a similar effect to the treatment plan.

The effect of Amaryl is enhanced by anabolic steroids, MAO inhibitors, fluoxetine, tetracyclines and sulfonamides, as well as fenfluramine.

The effectiveness of the drug is reduced by laxatives, various sorbents, thyroid hormones, adrenaline, glucagon and thiazide diuretics.

The drug is not used with alcohol. Amaryl together with alcohol can cause unexpected hypoglycemia and a toxic effect. It is recommended to take a pill 18-24 hours before drinking alcohol, and the same amount after, which means that for most people it is easier to give up alcohol.

There is no scientifically based information on non-alcoholic beer and Amaryl.

Contraindications to drinking alcohol are due to the fact that Amaryl increases the toxic effect on the liver and can provoke gastric ulcers and bleeding. If dizziness, tinnitus and other symptoms of poisoning occur after drinking alcohol, call an ambulance, wash the stomach, take sorbents, and then follow the treatment plan.

How to reduce the dosage and discontinue the drug

Independent dosage reduction is not allowed. The doctor must analyze the dynamics of blood glucose levels, conduct a study of the pancreas, and take into account all the patient’s health parameters.

The patient should not discontinue the medication under any circumstances. Reducing dosages, selecting other drugs - only according to the instructions of the attending physician.

Amaryl's analogs

The cheapest analogue is the Russian-made drug Glimepiride Pharmstandard.

In addition to it, there is Diameride and Glimepiride Canon on the market.

All analogues contain the same active ingredient and are cheaper.

Contraindications, side effects

Amaryl is contraindicated:

for lactose intolerance, severe liver damage and ketoacidosis.
The drug is not prescribed for type 1 diabetes.
It is not used during pregnancy and lactation.

A side effect may be hypoglycemia. It manifests itself when there is an overdose of the active substance, or the wrong combination of Amaryl with other sugar-lowering drugs.

– dizziness, cold sweat, confusion, in severe cases – loss of consciousness. At the first appearance of dizziness, you should eat 20 g of sugar, or administer glucose, and call an ambulance.

Amaryl is a modern remedy designed to improve the quality of life of a diabetic. It is used for type 2 diabetes. The dosage is selected by the doctor; regarding changes in diet, and the possibility of using the drug together with other substances, as well as withdrawal, it is better to consult an endocrinologist. The drug has available analogues and can be used for a long time.

Compound

One Amarsha 1 mg tablet contains: active substance: glimepiride - 1 mg;

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

One Amarsha 2 mg tablet contains: active substance: glimepiride - 2 mg;

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

One Amarsha 3 mg tablet contains: active substance: glimepiride - 3 mg.

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

One Amarsha 4 mg tablet 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. Top stamp: NMK/Brand mark. Bottom stamp: Brand/NMK.

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

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

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

pharmachologic effect

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

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

Insulin release

Sulfonylureas regulate insulin secretion by closing ATP-dependent potassium channels located in the cytoplasmic membrane of pancreatic beta cells. By closing potassium channels, they cause depolarization of beta cells, which promotes the opening of calcium channels and increased calcium entry into the cells. Glimepiride binds and dissociates at a high displacement rate to pancreatic beta cell protein (MW 65 kDa/SURX), which associates with ATP-dependent potassium channels but differs from the usual binding site of traditional derivatives

sulfonylureas (protein with a molecular weight of 140 kD / SUR1). ................ - X p>

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

Extrapancueal activity

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

Increased 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 cell membranes. Transport of glucose into these tissues in type 2 diabetes mellitus is the rate-limiting step in glucose utilization. Glimepiride very quickly increases the number and activity of glucose transport molecules (GLUT1 and GLUT4), which leads to increased glucose uptake by peripheral tissues.

Glimepiride has a weaker inhibitory effect on the K A tf channels of cardiomyocytes. When taking glimepiride, the ability of myocardial metabolic adaptation to ischemia is preserved.

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 hepatic glucose production 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 helps normalize lipid levels, reduces the level of minor aldehyde in the blood, which leads to a significant reduction in lipid peroxidation, this contributes to the antiatherogenic effect of the drug. Glimepiride increases the level of endogenous α-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase, which helps reduce the severity of oxidative stress in the patient’s body, which is constantly present in type 2 diabetes mellitus.

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 decreased insulin secretion with glimepiride is maintained.

There is no significant difference in effect depending on whether the drug is taken 30 minutes before a meal or immediately before a meal. In patients with diabetes, satisfactory metabolic control for 24 hours can be achieved by taking a single daily dose.

Although the hydroxy metabolite of glimepiride caused a small but significant decrease in blood glucose concentrations in healthy patients, this metabolite is responsible for only a small portion of the overall effect of the drug.

Combination therapy with metformin

One clinical trial showed that in patients with unsatisfactory treatment results despite maximum doses of metformin, the simultaneous use of glimepiride with metformin provided better metabolic control compared with metformin monotherapy.

Combination therapy with insulin

Data on the combination of glimepiride with insulin are scarce. Patients with unsatisfactory results of treatment with maximum doses of glimepiride can begin simultaneous insulin therapy. In two clinical studies, combination therapy provided similar metabolic improvements as insulin monotherapy, but the combination therapy required lower doses of insulin.

Special groups of patents

Children and teenagers

A 24-week active-controlled clinical trial (glimepiride up to 8 mg per day or metformin up to 2,000 mg per day) was conducted in 285 children (8-17 years) with type 2 diabetes. Both compounds, glimepiride and metformin, showed a significant reduction in HbAlc relative to baseline [glimepiride -0.95 (serum 0.41); metformin -1.39 (serum 0.40)]. Despite this, glimepiride did not achieve non-inferiority criteria for metformin status, as measured by mean change in HbAlc from 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 noninferiority margin of 0.3%,

Treatment with glimepiride did not reveal any additional safety concerns in children compared with those for adult patients with type 2 diabetes. There are no long-term studies of efficacy and safety in pediatric patients.

Pharmacokinetics

Suction

When glimepiride is taken orally, its bioavailability is complete. Food intake does not have a significant effect on absorption, with the exception of a slight slowdown in the rate of absorption. With repeated doses of glimepiride in a daily dose of 4 mg, the maximum concentration in the blood serum (Cmax) is reached after approximately 2.5 hours and is 309 ng/ml; There is a linear relationship between dose and Cmax, as well as between dose and AUC (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 low clearance (about 48 ml/min).

Biopanformation and excretion

After a single oral dose of glimepiride, 58% is excreted in urine and 35% in feces. No unchanged substance was detected in the urine. The half-life at plasma serum concentrations of the drug corresponding to multiple dosing regimens 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 penetrates the placental barrier. The drug penetrates the blood-brain barrier poorly.

Comparison of single and multiple (once daily) doses of glimepiride did not reveal significant differences in pharmacokinetic parameters, and their variability was very low 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 trend towards increased clearance of glimepiride and a decrease in its mean serum concentrations, which is likely due to more rapid elimination of the drug due to its lower protein binding. Thus, in this category of patients there is no additional risk of drug accumulation.

A trial examining the pharmacokinetics, safety and tolerability 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 AUC -i as t, C max and X\a analogues chny values previously observed in adults.

Indications for use

Type 2 diabetes mellitus (in monotherapy or as part of combination therapy with metformin or insulin) if it is impossible to adequately control it with diet, exercise or weight loss alone.

Contraindications

Glimepiride should not be used if:

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 case of planned pregnancy or if pregnancy occurs, the woman should be transferred to insulin therapy.

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

Directions for use and doses

Intended for oral use.

The basis for successful treatment of diabetes is proper diet, systematic exercise, and regular monitoring of blood and urine counts. Deviations from dietary recommendations cannot be compensated for by pills or insulin.

Initial dose and dose selection

The dosage of glimepiride is determined based on the results of an analysis of glucose levels 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.

Tablets with appropriate dosages are available for other dosage regimens.

If necessary, the daily dose can be gradually increased under regular monitoring of blood glucose concentrations (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 exceeding 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 administer the daily dose in 1 dose immediately before or during a large breakfast or, if the daily dose is not

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

Use in combination with metformin

In case of insufficient stabilization of blood glucose concentrations in patients taking metformin, concomitant therapy with glimepiride can be started. 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. Combination therapy should be carried out under close medical supervision.

Use in combination with insulin

In cases where it is not possible to achieve normalization of blood glucose concentrations 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 dose of insulin under the control of blood glucose concentrations. Combined treatment requires mandatory medical supervision. While maintaining long-term glycemic control, this combination therapy can reduce insulin requirements by up to 40%.

Transferring 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 transferring 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 increase in the dose 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 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 discontinue treatment for several days to avoid additive effects that increase the risk of hypoglycemia.

Transferring a patient from insulin to glimepiride

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

Use for renal and liver failure

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

Children and teenagers

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

Side effect

Below are data obtained from clinical studies on adverse reactions caused by taking glimepiride and other sulfonylurea derivatives. Adverse reactions are grouped by organ system class and distributed into groups in order of decreasing frequency of occurrence (very common: > 1/10; common: > 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)).

Disorders of the lymphatic and hematopoietic systems

Rarely: thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis,

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

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: Possible cross-allergic reactions with other sulfonylureas, sulfonamide drugs and similar substances.

Metabolic disorders Rare: hypoglycemia.

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

Visual disorders

Frequency unknown: temporary visual disturbances 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, which in rare cases leads to discontinuation of treatment.

From the hepatobiliary system

Frequency unknown - increased levels of liver enzymes.

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

Skin and subcutaneous tissue disorders

Frequency unknown," skin hypersensitivity reactions such as itching, rash, urticaria and photosensitivity may occur.

Laboratory results

Very rare: decreased sodium concentration 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 concentrations. Hypoglycemia can almost always be quickly reversed by immediate intake of carbohydrates (glucose or sugar, for example in the form of a sugar cube, sweet fruit juice or tea). In this regard, the patient should always have at least 20 g of glucose (4 lumps of sugar) with him. Sweeteners are ineffective in treating hypoglycemia. In most cases, observation in a hospital setting is recommended. Treatment includes induction of vomiting, fluid intake (water or lemonade with activated carbon (adsorbent) and sodium sulfate (laxative). When taking a large amount of the drug, gastric lavage is indicated, followed by the administration of activated carbon and sodium sulfate. The clinical picture of severe hypoglycemia may be similar to 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 blood glucose concentration.Further treatment should be symptomatic.

Symptoms of hypoglycemia may be smoothed out or completely absent in elderly patients, in patients suffering from autonomic neuropathy or receiving concomitant treatment with p-blockers, clonidine, reserpine, guanethidine or other sympatholytic agents.

When treating hypoglycemia that has developed as a result of accidental administration of Amaryl to infants or small children, the indicated dose of dextrose (50 ml of a 40% solution) should be carefully monitored in order to avoid dangerous hyperglycemia. In this regard, continuous and careful monitoring of blood glucose concentrations is necessary.

Interaction with other drugs

In the case of concomitant use of certain other drugs with glimepiride, both an undesirable decrease and an undesirable increase in the hypoglycemic effect of glimepiride may occur. In this regard, other medications can only be taken with the permission (or as prescribed) by 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 sulfonylureas, the following interactions should be noted.

An increase in the hypoglycemic effect and the associated possible development of hypoglycemia can be observed with 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 inhibitors (MAOIs),

Allopurinol, probenecid, sulfinpyrazone,

Sympatholytics,

Cyclo-, tro- and ifosfamides,

Miconazole, fluconazole,

Pentoxifylline (when administered parenterally in high doses),

Tritoqualine.

A weakening of the hypoglycemic effect and an associated increase in blood glucose concentration can be observed when glimepiride is used simultaneously 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.

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

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

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

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

Features of application

Glimepiride should be taken immediately before or during meals.

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

hypoglycemia. Possible symptoms of hypoglycemia include: headache, extreme hunger, nausea, vomiting, feeling tired, drowsiness, sleep disturbances, anxiety, aggressiveness, problems with 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 spasms, 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, hypertension, palpitations, angina pectoris and heart rhythm disturbances may occur.

The clinical picture of severe hypoglycemia may resemble that of a stroke.

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

As is known from experience with other sulfonylureas, despite the initial success of countermeasures, hypoglycemia may subsequently recur.

Severe or prolonged hypoglycemia that is only temporarily controlled by taking normal amounts of sugar requires immediate medical attention or even hospitalization.

Factors contributing to the development of hypoglycemia include:

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

Changes in your usual diet

Imbalance between physical activity and carbohydrate intake,

Drinking alcohol, especially in combination with skipping meals,

Renal dysfunction, severe liver dysfunction,

Overdose of glimepiride,

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

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

Also, during treatment with glimepiride, regular liver function tests and blood cell 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 the use of glimepiride in patients with severe renal impairment or patients requiring hemodialysis. Patients with severe renal or liver failure are advised to switch to insulin.

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

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

The effect of glimepiride on the ability to drive vehicles and operate machinery has not been studied. 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 operating a car or machinery).

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 have little or no awareness of the early signs of hypoglycemia. In these cases, the advisability of driving a vehicle or operating equipment should be considered.

One of the most common antidiabetic drugs from the sulfonylurea group is Amaryl.

Thanks to the active and additional components, the drug helps lower glucose concentrations and effectively reduces the severity of symptoms of diabetes.

The antidiabetic drug Amaryl is accepted for oral use. The generally accepted international name of the drug is Amaryl. The drug is produced in Germany, manufactured by Aventis Pharma Deutschland GmbH.

On this page you will find all the information about Amaryl: complete instructions for use for this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Amaryl. Would you like to leave your opinion? Please write in the comments.

Clinical and pharmacological group

Oral hypoglycemic drug.

Conditions for dispensing from pharmacies

Dispensed with a doctor's prescription.

Prices

How much does Amaryl cost? The average price in pharmacies depends on the form of release:

Amaryl tablets 1 mg, 30 pcs. – from 262 rub.
Amaryl tablets 2 mg, 30 pcs. – from 498 rub.
Amaryl tablets 3 mg, 30 pcs. – from 770 rub.
Amaryl tablets 4 mg, 30 pcs. – from 1026 rub.

Release form and composition

Amaryl is available in tablet form in several dosages: 1, 2, 3 and 4 mg. Its properties are due to the active substance – glimepiride, a sulfonylurea derivative. Lactose monohydrate, povidone, magnesium stearate, microcrystalline cellulose and dyes E172 or E132 are used as excipients.

Regardless of the dosage, all tablets have a dividing line and engraving. As a distinctive feature, the color of the tablet itself: 1 mg is pink, 2 mg is green, 3 mg is pale yellow and 4 mg is blue.

pharmachologic effect

Glimepiride, the active substance of the drug, has a positive effect on the pancreas, helps regulate insulin production and its entry into the blood. In turn, insulin lowers the amount of sugar in the blood.

Thanks to the effects of glimepiride, calcium from the blood enters tissue cells and helps prevent the formation of atherosclerotic plaques on the walls of blood vessels.

Metformin also helps reduce blood glucose, but in a different way: it improves hepatic circulation and converts blood sugar into glycogen, a substance safe for patients with diabetes. In addition, metmorphine promotes better absorption of glucose by muscle cells.

It has been established that glimepiride is more effective in combination with metformin. For this reason, Amaryl M was created - a drug convenient for both patients and doctors.

Indications for use

According to the instructions, Amaryl is prescribed for type 2 diabetes mellitus (non-insulin-dependent diabetes).

The active substance glimepiride stimulates the production of insulin by the pancreas and its release into the blood. Insulin, in turn, reduces the amount of sugar in the blood. Glimepiride improves potassium metabolism in cells and also helps prevent the formation of atherosclerotic plaques on the walls of blood vessels.

Contraindications

According to the instructions, Amaryl is contraindicated in the following cases:

Rare hereditary diseases (lactase deficiency, galactose intolerance, glucose-galactose malabsorption);
Hypersensitivity to the active or auxiliary components of the drug;
Diabetes mellitus type 1;
Severe liver dysfunction;
Diabetic precoma and coma, diabetic ketoacidosis;
Pregnancy and breastfeeding;
Severe liver dysfunction (including patients on hemodialysis);
Childhood.

When using Amaryl, caution should be exercised when:

Impaired absorption of food and drugs from the gastrointestinal tract (intestinal paresis, intestinal obstruction);
The presence of risk factors for the development of hypoglycemia;
Intercurrent diseases during therapy or when the patient’s lifestyle changes (changes in diet or meal times, decrease or increase in physical activity);
Glucose-6-phosphate dehydrogenase deficiency.

Use during pregnancy and lactation

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

It has been established that glimepiride is excreted in breast milk. During lactation, the woman should be switched to insulin or breastfeeding should be stopped.

Instructions for use Amaryl

The instructions for use indicate that Amaryl tablets are taken orally, do not chew them, and are washed down with about 150 ml of water. It is important not to forget to eat after taking the drug. The starting and maintenance dosage is set by the doctor individually, depending on the level of glucose in the blood serum and its excretion in the urine.

First, the drug is used at 1 mg/day; if necessary, you can gradually increase the daily dose to 6 mg. The dose is increased at intervals of 1-2 weeks according to the following scheme: 1 mg/day-2 mg/day-3 mg/day-4 mg/day-6 mg/day of amaryl. It is recommended not to exceed amaryl doses of more than 6 mg/day. The frequency and time of use of the drug is determined individually by the doctor, which depends on the patient’s lifestyle. As a rule, the daily dose of Amaryl is prescribed 1 time per day during or before the first large meal (breakfast). If the morning dose was not taken, then during or before the second meal. The therapy is long-term.

Using a combination of amaryl-metformin. For patients taking metformin who experience insufficient reductions in serum glucose levels, supplemental amaryl can be started. If the daily dosage of metformin does not change, then Amaryl therapy is started with a dose of 1 mg/day. Subsequently, the dose of Amaryl can be increased to achieve the desired reduction in serum glucose levels to a maximum of 6 mg/day.

Using a combination of amaryl-insulin. To stabilize blood serum glucose levels in cases where monotherapy or the use of the amaryl-metformin combination is ineffective, a combination of insulin and amaryl is used. In this case, the dose of Amaryl is left the same, and insulin therapy is started with small doses. In the future, it is possible to increase the administered insulin. Therapy should be accompanied by monitoring of serum glucose concentrations. Treatment is carried out under the supervision of the attending physician. An insulin-amaryl regimen can reduce insulin requirements by approximately 40%.

Replacing another antidiabetic drug with amaryl. Initial treatment begins with 1 mg/day of amaryl, regardless of the dose of the previous drug (even if it was the maximum). Depending on the therapeutic effect of amaryl, you can increase the dose according to the above rules. In some cases, it is necessary to discontinue Amaryl due to possible hypoglycemia (especially if a drug with a high half-life, chlorpropramide, was used before Amaryl). Therapy is stopped for several days (due to the likely additive effect).

Replacing insulin with amaryl. In cases where patients with type 2 diabetes are prescribed insulin, but their insulin-secreting function of pancreatic beta cells remains intact, the patient can be switched to taking Amaryl with the exception of insulin. In this case, Amaryl therapy begins with a dose of 1 mg/day.

Side effects

The use of Amaryl may cause the following adverse reactions:

Digestive system: rarely - abdominal pain, attacks of nausea, diarrhea, vomiting, feeling of fullness and heaviness in the epigastrium; in some cases - increased activity of cholestasis and/or liver enzymes, hepatitis, jaundice, life-threatening liver failure.
Organ of vision: at the beginning of therapy, transient visual disturbances are possible, triggered by changes in blood glucose levels.
Hematopoietic system: in some cases - granulocytopenia, leukopenia, pancytopenia, hemolytic anemia, agranulocytosis and erythrocytopenia; rarely - thrombocytopenia. Cases of severe thrombocytopenia and thrombocytopenic purpura have been reported during post-marketing use of Amaryl.
Allergic manifestations: rarely - pseudo-allergic and allergic reactions (urticaria, skin rashes and itching). Such reactions are usually mild, but can develop into severe reactions with a sharp decrease in blood pressure, shortness of breath, anaphylactic shock, and allergic vasculitis (in rare cases).
Metabolism: as with other sulfonylurea derivatives, prolonged hypoglycemia is possible. Signs of this disorder are nausea, headache, vomiting, feelings of hunger and fatigue, impaired concentration, drowsiness, paresis, sleep disturbances, loss of self-control, anxiety, bradycardia, aggressiveness, sensory disturbances, loss of vigilance and reaction speed, visual disturbances, depression , delirium, confusion, speech disorders, aphasia, tremor, dizziness, cerebral spasms, shallow breathing, loss of consciousness up to coma. In addition, signs of adrenergic counterregulation in response to hypoglycemia may be observed (restlessness, the appearance of sticky cold sweats, angina pectoris, tachycardia, cardiac arrhythmias, palpitations and arterial hypertension). The clinical picture of severe hypoglycemia resembles a stroke.
Other: in some cases – photosensitivity, hyponatremia.

Symptoms of overdose: severe, life-threatening hypoglycemia (with long-term treatment with glimepiride in high doses and acute overdose of the drug).

Overdose

In case of an overdose of Amaryl, nausea, abdominal pain, and vomiting may occur. Hypoglycemia may occur, which may cause tremors, anxiety, visual disturbances, drowsiness, coordination problems, convulsions, and coma.

In case of overdose, gastric lavage is indicated, followed by the use of enterosorbents. Glucose administration should be started as soon as possible. Further therapy is symptomatic. In case of severe overdose, hospitalization in the intensive care unit is required.

special instructions

When prescribing Amaryl or Amaryl M to a patient, a doctor must warn about the possibility of side effects, and most importantly, about the occurrence of hypoglycemia if the patient takes the medicine but forgets to eat. In this case, the patient is recommended to always carry candy or sugar pieces with him in order to be able to quickly raise his blood sugar level.

In addition to systematically checking blood and urine glucose levels, during treatment with Amaryl and Amaryl M, blood composition and liver function are also regularly monitored.

In stressful circumstances, accompanied by the release of adrenaline into the blood, the effectiveness of Amaryl and Amaryl M is reduced. Such situations can be accidents, conflicts in the family or at work, illnesses with a high rise in temperature. In such cases, the practice is to temporarily transfer the patient to insulin.

Drug interactions

The hypoglycemic effect is enhanced by the simultaneous use of amaryl with insulin, other hypoglycemic drugs, some antibiotics (tetracyclines, sulfonamides, clarithromycin), high doses of pentoxifylline, fluoxetine, fluconazole, anabolic steroids, ACE inhibitors (captopril, enalapril, ramipril, perindopril, lisinopril, etc.) . A combination of amaryl with barbiturates, laxatives, diuretics, high doses of nicotinic acid, and rifampicin will have the opposite effect.

Beta-blockers (carvedilol, atenolol, bisoprolol, metoprolol, etc.), reserpine, clonidine, coumarin derivatives and alcohol can increase or decrease the hypoglycemic effect of amaryl.

One tablet of the drug contains the active substance - glimepiride – 1-4 mg and auxiliary components: lactose monohydrate, povidone, sodium carboxymethyl starch, microcrystalline cellulose, indigo carmine and magnesium stearate.

Release form

Amaryl is available in tablets containing 1-4 mg, which are packaged in 15 pieces per blister. One pack of the drug may include 2, 4, 6 or 8 blisters.

pharmachologic effect

Amaryl tablets have a hypoglycemic effect.

Pharmacodynamics and pharmacokinetics

Contraindications for use

There is a fairly large list of contraindications for taking Amaryl:

1 type;
severe disorders of the liver and kidneys;
, precoma and coma;
, ;
the presence of rare hereditary diseases, for example, galactose intolerance, glucose-galactose malabsorption or lactase deficiency;
childhood;
intolerance or sensitivity to the drug, and so on.

Caution is required during the initial treatment of patients, as at this time there is a risk of developing hypoglycemia. If hypoglycemia remains a possibility, dosage adjustments often have to be made. glimepiride or therapeutic regimen. In addition, the presence of intercurrent and other diseases, lifestyle, nutrition, and so on requires special attention.

Side effects

When treated with Amaryl, a wide variety of undesirable phenomena can develop, one way or another affecting the activity of almost all body systems. Quite often, side effects are manifested by hypoglycemia, the symptoms of which are expressed by: , feeling of hunger, nausea , vomiting , , , , and many other symptoms. Sometimes the severe clinical picture of hypoglycemia resembles a stroke. After its elimination, the unwanted symptoms completely disappear.

At the initial stage of treatment, problems with vision, the functioning of the digestive system, and hematopoiesis may occur. It is also possible to develop which can lead to complications. Therefore, if unwanted symptoms appear, you should immediately consult a doctor.

Instructions for Amaryl (Method and dosage)

The tablets are intended for internal use in their entirety, without chewing and with plenty of liquid.

Typically, the dose of the drug is determined by the concentration of glucose in the blood. For treatment, the lowest dose is prescribed that helps achieve the necessary metabolic control

Also, the instructions for use of Amaryl indicate that during treatment, regular determination of the concentration of glucose in the blood and the level of glycosylated hemoglobin is required.

It is not recommended to make up for any incorrect intake of tablets, as well as missing the next dose, with an additional dosage. Such situations should be discussed in advance with your doctor.

At the beginning of treatment, patients are prescribed a daily dose of 1 mg. If the need arises, the dosage is gradually increased, regularly monitoring the concentration of glucose in the blood according to the following scheme: 1 mg−2 mg−3 mg−4 mg−6 mg−8 mg. The usual daily dosage in well-controlled patients is 1–4 mg of the active substance. A daily dose of 6 mg or more produces an effect in only a small number of patients.

The daily dosage regimen of the drug is established by the doctor, since various factors must be taken into account, for example, meal times, amount of physical activity, etc.

A single daily dose of the drug is often prescribed, before a full breakfast or the first main meal. It is important that you do not skip meals after taking the pills.

It is known that improved metabolic control is related to increased insulin sensitivity, and during treatment the need for glimepiride may decrease. The development of hypoglycemia can be avoided by timely reducing the dosage or stopping taking Amaryl.

During the therapeutic process, dosage adjustment glimepiride can be performed when:

reducing the patient's weight;
lifestyle changes;
the occurrence of other factors leading to a predisposition to hypoglycemia or hyperglycemia.

As a rule, treatment with Amaryl is carried out for a long time.

Overdose

In cases of acute overdose or prolonged use of high doses glimepiride severe hypoglycemia may develop, which is life-threatening.

If an overdose is detected, you should immediately consult a doctor. Hypoglycemia can be stopped by taking carbohydrates, for example, glucose or a small piece of any sweets. Until the symptoms of hypoglycemia are completely eliminated, the patient requires careful medical monitoring, as undesirable manifestations may recur. Further therapy depends on the symptoms.

Interaction

Concomitant use of glimepiride with certain drugs can cause the development of hypoglycemia, for example, with Insulin and other hypoglycemic agents, ACE inhibitors, anabolic steroids And male sex hormones, derivatives Coumarin, Cyclophosphamide, Disopyramide, Fenfluramine, Pheniramidol, fibrates, Fluoxetine, Guanethidine, Ifosfamide, MAO inhibitors, para-aminosalicylic acid, Phenylbutazone, Azapropazone, Oxyphenbutazone, salicylates, Sulfinpyrazone, sulfonamides, tetracyclines and others.

Reception , barbiturates, GKS, diazoxides, diuretics, and other sympathomimetic drugs, laxatives (with long-term use), (in high dosages), estrogen And progestogens, phenothiazines, phenytoins, rifampicins,iodine-containing thyroid hormones causes a weakening of the hypoglycemic effect, and accordingly, increases the concentration of glucose in the blood.

H2-histamine receptor blockers can enhance or weaken the hypoglycemic effect of glimepiride. , and beta blockers.

Terms of sale

The drug is available in pharmacies with a prescription.

Storage conditions

To store Amaryl, you need a dark place, protected from children, with a temperature of up to 30 C.

Best before date

Amaryl's analogs

Level 4 ATX code matches:

Modern pharmacology offers many means of similar action. However, the most common analogues of Amaryl are , Glemaz, Glemauno, Diamerid And Meglimid .

Alcohol and Amaryl

During treatment with this drug, especially at first, you must stop drinking alcohol. The fact is that both single and chronic alcohol consumption can significantly enhance or weaken the hypoglycemic effect glimepiride .

Reviews about Amaril

Numerous reviews from patients and specialists indicate that in the treatment of diabetes mellitus, proper selection of dosage and therapeutic regimen is of particular importance.

At the same time, reviews of Amaryl show that this drug is not suitable for all diabetics. Quite often, at the initial stage of treatment, patients experience a sharp change in blood sugar levels. However, experts are confident that in such cases it is necessary to adjust the dose upward and this is not at all an indicator of the ineffectiveness of the drug.

Of course, any adjustments associated with either increasing or decreasing the dosage should be carried out under the close supervision of a specialist. It has been established that improper use of Amaryl can cause complications of the disease.

Amaryl price, where to buy

In pharmacies, this drug is offered in several versions, with different contents of the active substance. The average price of the drug is 238-286 rubles, the price of Amaryl 4 mg is 868-1080 rubles, 3 mg is 633-829 rubles. and 2 mg – 453-562 rubles.

Online pharmacies in Russia Russia
Online pharmacies in Ukraine Ukraine
Online pharmacies in Kazakhstan Kazakhstan

ZdravCity

Amaryl tablets 4 mg 30 pcs.Sanofi-Aventis S.P.A.

Amaryl tablets 1 mg 30 pcs.Sanofi-Aventis S.P.A.

Amaryl tablets 2 mg 90 pcs.Sanofi-Aventis S.P.A.

Amaryl tablets 3 mg 30 pcs.Sanofi-Aventis S.P.A.

Amaryl tablets 3 mg 90 pcs.Sanofi-Aventis S.P.A.

Pharmacy Dialogue

Amaryl (tablet 3 mg No. 30) Sanofi-Aventis

Amaryl (tablet 1 mg No. 30) Sanofi-Aventis

Amaryl (tablet 3 mg No. 90) Sanofi-Aventis

Amaryl (tab. 2 mg No. 90) Sanofi-Aventis

Amaryl (tab. 4 mg No. 30) Sanofi-Aventis