The drug Amaryl for diabetes mellitus: a third-generation hypoglycemic agent. Amaryl - instructions for use Treatment of type 2 diabetes with the drug Amaryl

Type 2 diabetes mellitus is a common disease in which the blood sugar level exceeds the required level. Modern medicines successfully fight the disease. One of them is Amaryl, the instructions for use of which are discussed in the article. Experts classify the drug Amaryl as a group of hypoglycemic drugs that can reduce the glucose content in the blood lymph of people with type 2 diabetes.

Amaryl is usually prescribed by an endocrinologist as the main remedy for lowering glucose levels in the blood lymph. Sometimes diabetes pills are prescribed as part of complex therapy, together with insulin and metmorphine, according to indications.

According to the instructions for use, Amaryl is based on a substance that has an international nonproprietary name (INN) - glimepiride. It is responsible for the necessary production of insulin, so that it, in turn, begins to perform its main function - lowering sugar levels. This happens due to the release of insulin from pancreatic cells, which react to the action of glucose itself. More precisely, insulin production occurs due to its interaction with groups of potassium channel proteins (ATP channels), which are located on the surface of cells. Glimepiride is able to selectively bind to proteins and regulate the activity of ATP channels, they open and close in a controlled manner.

Glimepiride can have another important effect. It releases calcium from the blood, which enters tissue cells and prevents the formation of atherosclerotic plaques on the walls of blood vessels.

If the maximum dose is not sufficient for the patient, then metmorphine is added to therapy. The latter inhibits the process of gluconeogenesis in the liver and reduces the absorption of glucose from the intestine. It also increases glucose utilization and the sensitivity of the tissues themselves. As prescribed by a doctor, insulin can be added to therapy together with metmorphine or separately from it.

The active component is completely absorbed in the body. Food has a slight effect on absorption and may slightly slow down its speed. Glimepiride, like most drugs of the latest generation, is excreted through the intestines and kidneys. It was found that the substance does not remain unchanged in the urine. Studies do not determine the accumulation of glimepiride in the body.

Amaryl M is a combination of two active ingredients metformin and glimepiride, the instructions for its use indicate all the necessary characteristics of the drug. In pharmacies, the drug is usually sold: 1 mg of glimepiride + 250 mg of metformin, 2 mg of glimepiride + 500 mg of metformin.

Release forms

The medicine is available in the form of oval tablets (1–4 mg). On one side of the tablet the inscription HD125 is read. There are 15 pieces in one blister. The blisters themselves are packaged in cardboard boxes. You can buy the drug in packages of two, four, six or eight blisters. The tablets vary in color: pinkish ones contain 1 mg; green 2 mg, Amaryl 3 mg – orange in color and Amaryl 4 mg – pale blue tablets.

One tablet contains:

third generation glimepiride is the main component that lowers glucose, a substance isolated from sulfonamide;
povidone – chemical element, enterosorbent;
lactose with a water molecule (monohydrate);
microcrystalline cellulose;
sodium carboxymethyl starch – food additive, thickener, increasing stickiness;
indigo carmine is a safe food coloring
magnesium stearate (stabilizing defoamer).

Amaryl is easy to use; you just need to take the tablet once in the morning. Instructions for use, as well as the price, are quite affordable for anyone suffering from this endocrine disease.

Contraindications

For all its effectiveness, Amaryl has a number of contraindications when taking pills, this must be taken into account.

Diabetes mellitus type 1. Unlike type 2 diabetes, it is characterized by absolute insulin deficiency, which occurs due to the destruction of pancreatic cells.
Diabetic ketoacidosis is a complication of diabetes mellitus, usually type 1. Disturbances in carbohydrate metabolism due to acute lack of insulin.
Diabetic coma or precoma occurs due to insulin deficiency or poor diet, abuse of fatty foods, carbohydrates and alcoholic beverages.
Significant metabolic disorder.
Severe diseases of the liver, as well as kidneys, with impaired functionality of these vital organs. In particular, conditions that lead to disruption of these functions are taken into account - infections, shock, etc.
Carrying out hemodialysis.
Ischemia, respiratory dysfunction, myocardial infarction, coronary heart disease. These conditions can lead to tissue hypoxia.
Lactic acidosis is a rare complication of diabetes that causes excess lactic acid in the body.
Injuries, burns, surgeries, septicemia (one of the types of blood poisoning).
Exhaustion of the body, deliberate fasting - consumption of food and drinks containing less than 1000 calories per day.
Intestinal obstruction, intestinal paresis, diarrhea, vomiting.
Alcohol abuse, acute alcohol poisoning.
Lactase deficiency (an enzyme necessary for the production of lactose), galactose intolerance (one of the sugars).
Expecting a baby, breastfeeding.
Age up to 18 years, due to insufficient research on this issue.
Individual intolerance to one or more components of Amaryl.

Immediately after prescribing Amaryl, initial monitoring of the effect of the drug and the general condition of the patient is required.

At first, without control, hypoglycemia may occur, which can cause serious health consequences.

However, patients may not be available for medical supervision. For example, some are unwilling or unable to contact a doctor. This is especially true for older people. This also includes patients who do not monitor their diet for various reasons, and alcoholics. People who perform monotonous hard physical work.

Amaryl should be taken under the supervision of a physician in patients with dysfunction of the thyroid gland, as well as the adrenal glands, and other common endocrine disorders. In this case, strict monitoring of blood glucose levels and diagnosing signs of hypoglycemia is necessary; some dose adjustment may be required.

Particular attention should be paid to taking Amaryl in a situation where patients are simultaneously taking other medications. The doctor must understand their compatibility and advise patients on the rules of admission.

Dosage

The diabetes medicine Amaryl is prescribed exclusively by a specialist - an endocrinologist. He makes appointments only after determining the patient’s blood glucose level. Endocrinologists take into account how a person lives - his diet, physical activity, age, side diseases and many other factors.

The minimum dose is considered to be 1 mg. One tablet should be taken once a day in the morning before or during the first breakfast. It is not recommended to chew the tablets; however, you should take them with water (at least half a glass). If necessary, the doctor may prescribe a larger dose - from 2 to 3 mg; 4 mg is considered a standard high dose, 6 and 8 mg are prescribed in extremely rare cases. The dose should not be increased sharply; the interval between new prescriptions should be at least seven days. While taking the diabetes drug Amaryl and especially adjusting doses, it is necessary to take control tests.

Adjustment is usually required when there are changes in the patient's lifestyle. For example, drinking alcohol, breaking a diet, sudden weight gain or loss. These include carbohydrate metabolism disorders, overdose, complications in the functioning of the kidneys and liver.

When Amaryl M is prescribed, the same principle is used to determine the dosage. Usually this drug is also taken once a day. Particular attention is paid to the selection of doses for patients over 65 years of age. The medicine is prescribed after carefully studying the side diseases of older people, especially with regard to the functioning of the liver and kidneys.

The dose of Amaryl is not increased at subsequent doses if the patient has forgotten to take the daily pill. This day is left without taking the medicine, and the next day you need to take the standard dose.

After taking the pills, the patient must eat, otherwise the sugar level will drop below normal. The following meals should also not be skipped, otherwise the opposite effect of therapy may be observed. Drugs of this type are indicated for use over a long period of time. If the diabetes medication does not have the desired effect, the combined Amaryl M is prescribed, or other glucose-lowering medications are administered - metformin and insulin.

Side effects

Recent clinical studies of glimepiride, the main active ingredient in Amaryl, have revealed side effects. They can manifest themselves in metabolism, digestion, vision, cardiovascular and immune systems. In addition, photosensitivity (increased sensitivity of the body to ultraviolet rays) and hyponatremia (decrease in the amount of sodium ions in the blood) are possible.

Hypoglycemia can manifest itself for a long time; in case of metabolic disorders, its symptoms are:

migraines, dizziness, loss of consciousness, sometimes to the development of coma;
constant desire to eat;
nausea and vomiting;
weakness, insomnia or constant desire to sleep;
sudden manifestation of aggression;
decreased attentiveness, slowdown of basic reactions;
delirium (mental disorder with impaired consciousness);
depression;
confusion;
speech disorders (aphasia)
blurred vision;
tremor, convulsions;
impaired sensitivity of organs;
loss of self-control;
difficulty breathing;
severe sweating, sticky skin;
anxiety attacks;
increased heart rate;
increased blood pressure;
heart rhythm disturbances, sinus rhythm disturbances.

Vision. Significant deterioration of vision, usually at the beginning of taking Amaryl. This occurs due to impaired swelling of the lenses; this process directly depends on the amount of glucose in the blood. The refractive index of the lenses is disrupted, and vision becomes worse.

Digestion. The patient may feel nauseous, vomiting, a feeling of fullness in the stomach, acute pain in the stomach, bloating, and diarrhea. You may develop aversion to food.

Liver, bile ducts. The development of hepatitis, cholestasis and jaundice is possible; they can significantly worsen the patient’s health and even threaten life, due to the progression of liver failure. However, after discontinuation of Amaryl, a rapid restoration of liver function may occur.

The immune system. Allergic manifestations (urticaria, rash) are observed. These reactions are usually easily tolerated, however, in some cases severe shortness of breath occurs. Blood pressure decreases, anaphylaxis (acute reaction to an allergen) is possible. Allergic vasculitis (immune pathological inflammation of blood vessels) was detected.

Price

The price of the medicine is low, but may differ at pharmacy outlets of different companies. As an example, prices on some major online pharmacy resources where you can buy Amaryl are shown in the table.

Analogs

The medicine is used to treat type 2 diabetes. However, it may not be suitable for the patient due to his side diseases or other reasons. Amaryl analogues are also based on the active substance glimepiride. They may differ in the number of tablets in a pack, place of production, excipients and individual intolerance to them by patients. Experts consider the following drugs to be analogues of Amaryl.

Glemaz. The active ingredient is similar - glimepiride. The drug is available in tablets and is prescribed when planning long-term treatment, under medical supervision. Unlike Amaryl, only 4 mg tablets are available. Average price – 650 rubles.
Glemauno. The action of the medicine is similar to the action of Amaryl. It does not have a very long list of warnings for use. However, instructions are given not to engage in activities requiring alertness during the appointment. The drug is available only with a prescription. The average price of 2 mg is 476 rubles.
Glimepiride. A drug similar to Amaryl can lower the sugar level in the patient’s blood lymph. Usually the tablets are also taken once a day before a heavy carbohydrate breakfast, washed down with sufficient water. If the effectiveness is insufficient, additional insulin is administered. Reviews about it are positive; the cost of the medicine is cheaper than similar drugs. Average price – 2 mg 139 rubles.

Overdose

An overdose is dangerous due to the occurrence of hypoglycemia - the concentration of glucose in the blood is critically reduced, and a hypoglycemic coma is possible. This condition can last from one day to three days. If symptoms of overdose occur, the patient is offered foods rich in carbohydrates. You can eat a piece of sugar, drink juice or sweet tea. If the patient has lost consciousness, then dextrose and glucagon are administered parenterally, bypassing the gastrointestinal tract.

If the patient’s condition worsens after an overdose, call an ambulance and, if necessary, hospitalize the patient.

Amaryl is a hypoglycemic drug intended for oral use.

Release form and composition

Amaryl tablets are made containing:

1 ml of glimepiride – pink;
2 ml of glimepiride – green;
3 mg glimepiride – light yellow;
4 mg glimepiride – green.

Blisters contain 15 tablets, 2 blisters per package.

Auxiliary components of Amaryl are: polyvidone 25000, lactose monohydrate, magnesium stearate, microcrystalline cellulose, sodium starch glycolate.

Indications for use of Amaryl

According to the instructions, Amaryl is prescribed for type 2 diabetes mellitus as the main treatment or as part of combination therapy in combination with insulin and metformin.

Contraindications

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

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

When using Amaryl, caution should be exercised when:

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);
Impaired absorption of food and drugs from the gastrointestinal tract (intestinal paresis, intestinal obstruction);
Glucose-6-phosphate dehydrogenase deficiency.

Directions for use and dosage of Amaryl

The exact dosage of Amaryl is determined based on the initial concentration of glucose in the blood.

Initially, the drug is prescribed in a minimum dose in order to achieve the required metabolic control.

While using Amaryl, the patient should regularly monitor the level of glucose in the blood, as well as glycosylated hemoglobin.

Amaryl tablets are taken whole with half a glass of water.

The initial dosage of Amaryl is 1 mg per day. The dosage should be increased gradually, at intervals of 1-2 weeks, in the following order: 1mg-2mg-3mg-4mg-6mg-8mg per day.

As a rule, for well-regulated diabetes mellitus, the optimal dosage of Amaryl is 1-4 mg. The use of Amaryl at a dose of 6 mg or more per day is effective only for certain groups of patients.

The frequency and time of use of Amaryl is determined individually by the attending physician, taking into account the age, severity of the disease, the patient’s lifestyle, and nutritional pattern.

The daily dosage of Amaryl should be taken in one dose, preferably before breakfast or another meal. It is important not to skip meals after taking the pills.

During the use of Amaryl, dosage adjustment may be required due to improved metabolic control. Dose adjustment of Amaryl may also be required if:

Lifestyle changes;
Losing body weight;
The emergence of factors leading to the development of hyperglycemia or hypoglycemia.

According to the instructions, Amaryl is taken for a long time.

Side effects of Amaryl

Amaryl can cause the following side effects from various vital systems of the body:

Metabolism: hypoglycemia, symptoms of which include fatigue, drowsiness, nausea, vomiting, headache, hunger, sleep disturbances, aggressiveness, anxiety, depression, impaired concentration, speech disorders, confusion, visual disturbances, cerebral spasms, bradycardia ;
Visual organs: transient visual impairment due to changes in blood glucose levels;
Digestive system: abdominal pain, feeling of heaviness in the epigastrium, diarrhea, increased activity of liver enzymes, hepatitis, jaundice;
Hematopoietic system: leukopenia, thrombocytopenia, erythrocytopenia, hemolytic anemia, agranulocytosis, pancytopenia, granulocytopenia;
Allergies: skin rash, itching, urticaria, severe allergic reactions accompanied by shortness of breath, a sharp decrease in blood pressure, allergic vasculitis;
Other adverse reactions: photosensitivity, hyponatremia.

special instructions

During the first time using Amaryl, there is a high risk of developing hypoglycemia, so the patient must carefully monitor blood glucose levels.

Glimepiride, the active component of Amaryl, is a sulfonylurea derivative and can lead to the development of hemolytic anemia. Therefore, caution should be exercised when prescribing the drug to patients with glucose-6-phosphate dehydrogenase deficiency. It is preferable to prescribe hypoglycemic agents that are not sulfonylurea derivatives to such patients.

By quickly taking easily digestible carbohydrates, hypoglycemia can be quickly eliminated. However, taking Amaryl is characterized by the resumption of a stopped attack of hypoglycemia. Therefore, it is recommended that patients remain under the supervision of doctors or relatives. In case of severe hypoglycemia, the patient must be taken to the hospital.4.8 - 25 votes

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 may cause 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

Name:

Amaryl

Pharmachologic effect:

Amaryl is a sulfonylurea drug, an oral hypoglycemic agent. Has a primarily prolonged effect. The mechanism of action is to stimulate the secretion and release of insulin from the beta cells of the pancreas (pancreatic effect). It also increases the sensitivity of adipose and muscle tissue to the action of insulin (extrapancreatic effect). It acts by blocking the cytoplasmic ATP-dependent potassium channels of pancreatic beta cells. This is accompanied by the opening of calcium channels in the beta cell membranes and increased penetration of calcium into them (depolarization).

Amaryl's active ingredient, glimepiride, quickly detaches and binds to beta-cell protein, which has a molecular weight of 65 kDa/SURX and is associated with adenosine triphosphate-dependent potassium channels. It differs from other sulfonylurea derivatives in that it does not interact with the beta cell protein with a molecular weight of 140 kDa/SUR1. This leads to exocytosis of insulin, and the content of released insulin is much less than with the influence of other traditional drugs. The slight stimulating effect of amaryl on insulin secretion by beta cells leads to a lower risk of hypoglycemia.

The extrapancreatic effect of amaryl leads to a decrease in insulin resistance and a slight effect on the cardiovascular system. It has antiplatelet, antiatherogenic and antioxidant effects.

Increased utilization of glucose by adipose and muscle tissue is due to the presence of specific transport proteins in cell membranes. In non-insulin-dependent diabetes, the penetration of glucose into these tissues is limited at the disposal stage. Amaryl quickly increases the activity of transport proteins, due to which glucose is absorbed better. There is also an increase in the number of transport proteins with the use of amaryl. There is virtually no blocking effect on ATP-dependent potassium channels of cardiac myocytes. The possibility of metabolic adaptation of cardiomyocytes to ischemic conditions remains. The activity of specific glycosyl-phosphatidylinositol phospholipase C increases, due to which glycogenesis and lipogenesis, correlated with amaryl intake, are observed.

Amaryl blocks hepatic glucose production by increasing the content of fructose-2,6-bisphosphate in hepatocytes (the latter also blocks gluconeogenesis).

While taking the drug, there is a blocking of COX secretion and a decrease in the transformation of arachidonic acid into thromboxane A2, due to which platelet aggregation (antithrombotic effect) decreases. Under the influence of amaryl, an increase in the concentration of alpha-tocopherol, which is formed endogenously, is observed. There is also an increase in the activity of superoxide dismutase, catalase and glutathione peroxidase, which is manifested by a decrease in the severity of oxidative reactions in diabetes mellitus.

Indications for use:

Non-insulin-dependent diabetes mellitus (type 2) - as monotherapy or in combination with insulin (or metformin).

Method of application:

Amaryl is taken orally. The tablets are not chewed, 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.

Adverse events:

Metabolism:

the occurrence of hypoglycemic reactions soon after taking amaryl (such reactions are very difficult to correct).

Nervous system:

headache, sleep disturbances, drowsiness, feeling tired, aggressiveness, anxiety, changes in concentration and speed of psycho-motor reactions, visual and speech disorders, dizziness, confusion, depression, sensory disturbances, aphasia, coordination disorders, paresis, helpless state, cerebral spasms, loss of self-control, tremors, loss or confusion, delirium, coma, restlessness, cold, clammy sweat.

Gastrointestinal tract:

vomiting, epigastric discomfort, hunger, abdominal pain, diarrhea, jaundice, cholestasis, increased liver transaminases, hepatitis, liver failure, nausea.

The cardiovascular system:

tachycardia, heart rhythm disturbances, arterial hypertension, bradycardia, angina pectoris.

Organ of vision:

transient visual impairment as a result of changes in blood glucose levels (especially at the beginning of therapy).

Respiratory system:

shallow breathing.

Hematopoietic system:

leukopenia, thrombocytopenia (moderate or severe), erythrocytopenia, aplastic or hemolytic anemia, granulocytopenia, pancytopenia, agranulocytosis.

Hypersensitivity reactions:

urticaria, itching, skin rash, allergic vasculitis. Allergic reactions are usually mild, but sometimes progression to anaphylactic shock is possible. A cross-reaction is possible with sulfonylureas and sulfonamides.

Other:

hyponatremia, photosensitivity.

Contraindications:

Ketoacidosis of diabetic origin, diabetic coma and precoma,

Insulin-dependent diabetes mellitus (type 1),

Severe renal dysfunction (including patients on hemodialysis),

Severe liver dysfunction,

Individual hypersensitivity to amaryl (glimepiride) or other components of the drug, other sulfonylureas, sulfonamides.

During pregnancy:

Amaryl should not be prescribed to pregnant women or breastfeeding women. If the patient is planning a pregnancy, then she must be switched to insulin administration with the exception of Amaryl. If the patient is breastfeeding, then insulin administration is continued or breastfeeding is stopped (since amaryl passes into breast milk).

Interaction with other drugs:

In combination with insulin, other drugs for the treatment of hypoglycemia, allopurinol, angiotensin-converting factor inhibitors, male sex hormones, anabolic steroids, coumarin derivatives, chloramphenicol, fenfluramine, fluoxetine, fibrates, pheniramidol, MAO inhibitors, guanethidine, pentoxifylline (when administered parenterally in large doses ), miconazole, azapropazone, phenylbutazone, quinolones, probenecid, oxyphenbutazone, salicylates, sulfinpyrazone, tetracyclines, long-acting sulfonamides, tritoqualine, tro-, cyclo-, and isophosphamide may increase the hypoglycemic effect of amaryl.

In combination with adrenaline (epinephrine) and sympathomimetics, acetazolamide, glucocorticosteroids, glucagon, diazoxide, barbiturates, saluretics, laxatives (with prolonged use), thiazide diuretics, nicotinic acids in large doses, phenytoine, phenotiazin, rifacein , progestagenes and estrogens, chlorpromazine , thyroid hormones, lithium salts may reduce the hypoglycemic effect of amaryl.

When amaryl is combined with reserpine, clonidine and histamine H2 receptor blockers, both a decrease and an increase in the hypoglycemic effect are possible.

It is possible to reduce or weaken the effects of coumarin and its derivatives in combination with amaryl. Long-term or single use of enthanol-containing drugs and drinks can either weaken or enhance the hypoglycemic effect of Amaryl.

Overdose:

In case of an overdose of Amaryl, hypoglycemia is possible for 12-72 hours when taking Amaryl in a high dose. Hypoglycemia may re-develop after blood glucose levels are restored. Hypoglycemia is manifested by the following symptoms: increased blood pressure, increased sweating, nausea, vomiting, arrhythmia, pain in the heart, anxiety, a sharp increase in appetite, apathy, dizziness, drowsiness, headache, anxiety, palpitations, aggressiveness, impaired concentration, tremor , confusion, paresis, depression, sensory disturbances, tachycardia, convulsions of central origin. In some cases, hypoglycemia manifests itself as symptoms of a stroke. There is a risk of developing a coma. Therapy for hypoglycemia should begin with taking a piece of sugar, sweet tea or juice. The patient is warned to keep approximately 20 g of glucose with him at all times (in the form of 4 lumps of sugar, for example). Various sweeteners are ineffective in treatment. In severe cases, hospitalization is necessary. Induction of vomiting is carried out, the patient is dehydrated (water with activated carbon orally, laxative). Dextrose is administered parenterally (40% solution 50 ml intravenously). Subsequently, diluted dextrose (10% solution) is used. Treatment is accompanied by constant monitoring of serum glucose levels. Other symptoms are relieved by symptomatic treatment.

If amaryl is accidentally taken by people without diabetes (children), the development of hyperglycemia must be avoided. The dose of dextrose is carefully selected against the background of monitoring serum glucose levels.

Release form of the drug:

Amaryl - tablets, have a dividing strip, elongated in shape. Glimepiride tablets of 1 ml are pink in color. Amaryl 2 ml – green tablets. Amaryl 3 mg – light yellow tablets. Amaryl 4 mg – green. The package contains 2 blisters, each containing 15 tablets.

Storage conditions:

Amaryl is stored at a temperature of no more than 25°C. Shelf life - 3 years.

Compound:

Active ingredient: glimepiride.

Inactive components: lactose monohydrate, polyvidone 25,000, sodium starch glycolate, microcrystalline cellulose, magnesium stearate, dye (for amaryl 1 mg - iron oxide red (E172), for amaryl 2 mg - iron oxide yellow (E172) and indigo carmine (E132) , for amaryl 3 mg - yellow iron oxide (E172), for amaryl 4 mg - indigo carmine (E132).

Additionally:

When treating with Amaryl, it is necessary to remember about conditions that require transferring the patient to parenteral administration of insulin (polytraumas, surgical treatment, diseases with increased body temperature, extensive burns, changes in the absorption of food from the gastrointestinal tract in diseases - intestinal obstruction, intestinal paresis and others) .

When combining amaryl-metformin, it must be taken into account that taking high doses of metformin and glimepiride is accompanied by a marked improvement in metabolism in patients with uncontrolled diabetes mellitus. In the case of high doses of metformin and amaryl, if control is still insufficient, the patient can be switched to a combination of amaryl-insulin.

Factors that provoke the development of hypoglycemia: low patient compliance, inadequate, irregular nutrition, changes in the usual diet, skipping meals, alcohol consumption, fasting, changes in the balance between carbohydrate intake and physical activity, severe dysfunction of the liver and kidneys, concomitant uncompensated diseases of the endocrine system , amaryl overdose, thyroid dysfunction, adrenal insufficiency, pituitary insufficiency, combination with other drugs.

Signs of hypoglycemia are leveled out in the elderly, patients with neurocirculatory dystonia, patients taking beta-blockers, reserpine, clonidine, guanethidine, and sympatholytics.

The dose of the drug is selected individually depending on the glucose level in the blood. If the next dose is missed, it is strictly forbidden to take a higher next dose. The patient should tell the doctor if they are taking too high a dose of Amaryl. In case of diabetes compensation, an improvement in insulin sensitivity may be observed, so it is possible to reduce the dose of Amaryl (or even discontinue the drug). It is necessary to adjust the dose of Amaryl when various factors appear that can provoke hypoglycemia or hyperglycemia, as well as in case of lifestyle changes. It must be remembered that a proper diet, correction of physical activity, and weight loss are of great importance for the treatment of diabetes mellitus while taking Amaryl.

It is necessary to inform the patient that he should immediately inform the attending physician of all side effects that develop during therapy with amaryl. It is also necessary to inform him about the factors that cause both hyper- and hypoglycemia and the symptoms of these conditions.

Amaryl therapy should be accompanied by regular monitoring of glucose levels in the blood serum and urine, and determination of the concentration of glycosylated hemoglobin. Regular monitoring of these laboratory parameters helps to identify possible primary or secondary drug resistance in a timely manner.

Laboratory control also includes determination of liver function and a clinical blood test. During drug therapy, the speed of psycho-motor reactions may decrease, so working with precision machinery and driving a car is contraindicated. This is especially true for the initial stages of treatment with amaryl.

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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.

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.

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 concentrations 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.