Amaryl pills 4 mg №90

Amaryl

Pills

Composition

1 pill Amaryl contains Glimepiride 4 mg;
Excipients: lactose, sodium starch glycolate, polyvidone 25 000, microcrystalline cellulose, Magnesium stearate, indigo carmine (E132)

Packing

90 pcs.

Mechanism of action

Oral hypoglycemic drug Amaryl is a sulfonylurea derivative of primary prolonged action. Stimulates the secretion and release of insulin from pancreatic b-cells (pancreatic action), increases the sensitivity of peripheral tissues (muscle and fat) to insulin (extrapancreatic action).
The sulfonylurea derivatives regulate insulin secretion by closing the ATP-dependent potassium channels located in the cytoplasmic membrane of pancreatic b-cells. Closing the potassium channels, they cause b-cell depolarization, which promotes the opening of Calcium channels and an increase in calcium intake into the cells. Glimepiride connects and detaches from the pancreatic b-cell protein (molecular weight 65 kD / SURX), which is associated with ATP-dependent potassium channels, but differs from the usual binding site of traditional sulfonylurea derivatives (protein 140 kD / SUR1 ).This process leads to the release of insulin by exocytosis, while the amount of secreted insulin is much less than under the action of traditional sulfonylurea derivatives. The least stimulating effect of glimepiride on insulin secretion provides a lower risk of hypoglycemia.
In addition, the drug Amaryl has an extrapancreatic effect, which includes a decrease in insulin resistance, a lesser effect on the cardiovascular system, anti-atherogenic, antiaggregant, antioxidant effect.
Increased utilization of glucose from the blood by peripheral tissues (muscle and fat) occurs with the help of special transport proteins located in the cell membranes. The transport of glucose to these tissues in non-insulin dependent diabetes mellitus is a speed-limited glucose utilization step. Amaryl very quickly increases the amount and activity of transport proteins, which leads to an increase in glucose uptake by peripheral tissues.
Amaryl has a weaker inhibitory effect on the ATP-dependent potassium channels of cardiomyocytes. When receiving Amaryl retained the ability of metabolic myocardial adaptation to ischemia.
Amaryl increases the activity of glycosyl-phosphatidylinositol-specific phospholipase C, with which lipogenesis and glycogenesis caused by the preparation can correlate in isolated muscle and fat cells.
Amaryl inhibits glucose production in the liver by increasing the intracellular concentrations of fructose 2,6-bisphosphate, which in turn inhibits gluconeogenesis.
Amaryl selectively inhibits cyclooxygenase and reduces the conversion of arachidonic acid to thromboxane A₂which promotes platelet aggregation, thus exerting an antithrombotic effect.
Amaryl increases the level of endogenous alpha-tocopherol, the activity of catalase, glutathion peroxidase and superoxide dismutase, which helps reduce the severity of oxidative stress in the body of a patient who is constantly present in diabetes mellitus.

Indications and usage

Type 2 diabetes as monotherapy or in combination with Metformin or insulin.

Contraindications

- diabetes mellitus type 1;
- diabetic ketoacidosis, diabetic precoma and coma;
- severe abnormal liver function;
- severe renal dysfunction (including patients on hemodialysis);
- pregnancy;
- lactation;
- hypersensitivity to glimepiride or other components of the drug, other sulfonylurea derivatives and sulfanilamide preparations.

Pregnancy and Breastfeeding

Amaryl is contraindicated for use in pregnancy. In the case of a planned pregnancy or if the pregnancy occurs, the woman should be transferred to insulin.
It is established that glimepiride is excreted in breast milk.During lactation, you should transfer a woman to insulin or stop breastfeeding.

Dosage and administration

The initial and maintenance dose is set individually based on the results of regular monitoring of blood glucose and urine levels.
At the beginning of treatment prescribed Amaryl 1 mg 1 time / day. If necessary, the daily dose can be gradually increased (at intervals of 1-2 weeks) and in the following order: 1 mg-2 mg-3 mg-4 mg-6 mg Amaryl per day. The maximum recommended daily dose is 6 mg.
The time and frequency of taking the drug Amaryl is determined by the doctor taking into account the lifestyle of the patient. The daily dose is prescribed in 1 reception, as a rule, before or during a hearty breakfast or, if the daily dose has not been taken, immediately before or during the first heavy meal. The treatment is long.
Amaryl use in combination with metformin
With insufficient stabilization of the glucose concentration in the blood of patients taking metformin, concomitant Amaryl therapy may be initiated. While maintaining the dose of metformin at the same level, treatment with Amaryl begins with a minimum dose of 1 g, and then its dose gradually increases depending on the desired level of glycemic control, up to a maximum daily dose of 6 mg.
Amaryl use in combination with insulin
In the case when it is not possible to achieve normalization of the concentration of glucose in the blood by taking the maximum dose of Amaryl 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 Amaryl assigned to the patient remains unchanged. In this case, insulin treatment begins with a minimum dose, with the possible subsequent gradual increase in insulin dose under the control of glucose concentration in the blood. Combined treatment requires mandatory medical supervision. While maintaining long-term glycemic control, this combination therapy can reduce the need for insulin by up to 40%.
Transfer of a patient from another oral hypoglycemic drug to Amaryl
There is no exact relationship between doses of Amaryl and other oral hypoglycemic drugs. When transferring from such drugs to Amaryl, the initial daily dose of the latter should be 1 mg (even if the patient is transferred to Amaryl from the maximum dose of another oral hypoglycemic drug). Any increase in the dose of Amaryl should be carried out in stages, taking into account the response to glimepiride in accordance with the above recommendations. It is necessary to take into account the dose used and the duration of the effect of the previous hypoglycemic agent. In some cases, especially when taking hypoglycemic drugs with a long half-life (for example, chlorpropamid), it may be necessary to temporarily (within a few days) discontinue treatment in order to avoid an additive effect that increases the risk of hypoglycemia.
Transfer of the patient from insulin to Amaryl
In exceptional cases, if patients with type 2 diabetes mellitus (non-insulin-dependent) receive insulin therapy, they can be shown a transfer to Amaryl when compensating for the disease and when the secretory function of the b-cells of the pancreas is preserved. Translation must be carried out under the close supervision of a physician. In this case, the transfer of the patient to Amaryl begins with a minimum dose of glimepiride 1 mg.
pills should be taken whole, without chewing, drinking plenty of liquid (about 1/2 cup). It is very important not to skip meals after taking Amaryl.

Adverse reactions

Metabolism: rarely - the development of hypoglycemic reactions. These reactions mainly occur shortly after taking the drug, and they are not always easy to stop. Headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbances, anxiety, aggression, concentration disorders and reactions, depression, confusion, speech and visual disturbances, aphasia, tremor, paresis, sensory disturbances, dizziness , lack of coordination, helpless state, loss of self-control, delirium, cerebral seizures, confusion or loss of consciousness, including coma, shallow breathing, bradycardia. In addition, as a result of the adrenergic feedback mechanism, symptoms such as cold, clammy sweat, anxiety, tachycardia, arterial hypertension, angina pectoris, and heart rhythm disturbances can occur.
On the part of the organ of vision: during treatment (especially at the beginning of treatment) transient visual disturbances due to a change in glucose concentration in the blood may occur.
From the digestive system: sometimes nausea, vomiting, feeling of heaviness or discomfort in the epigastrium, abdominal pain, diarrhea (very rarely leading to discontinuation of treatment); rarely - increased activity of hepatic transaminases, cholestasis , jaundice, hepatitis (up to the development of liver failure).
From the hemopoietic system: rarely, thrombocytopenia (moderate to severe), leukopenia, hemolytic or aplastic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia.
Allergic reactions: sometimes itching, hives, skin rash. Such reactions are, as a rule, moderately pronounced, but can progress, accompanied by a fall in blood pressure, dyspnea, up to the development of anaphylactic shock. Possible cross-allergy with other sulfonylurea derivatives, sulfonamides, or similar substances, the development of allergic vasculitis is also possible.
Other: in isolated cases - photosensitivity, hyponatremia.

Special attention should be paid to conditions requiring the transfer of the patient to insulin therapy: extensive burns, severe multiple injuries, extensive surgical interventions, impaired absorption of food and drugs in the gastrointestinal tract (intestinal obstruction, intestinal paresis).
In stressful situations (with injury, surgery, infectious diseases, accompanied by fever), it may be necessary to temporarily transfer the patient to insulin.
It should be borne in mind that in patients with inadequately controlled type 2 diabetes mellitus, when maximized doses of metformin are used in monotherapy, there is a significant improvement in metabolic control when joining glimepiride.
It should be borne in mind that in patients with insufficiently controlled type 2 diabetes mellitus, when taking maximum doses of glimepiride and metformin, combination therapy of glimepiride with insulin can be started. When using this combination there is a significant improvement in metabolic control.
In the first weeks of treatment, irregular eating or skipping meals may increase the risk of hypoglycemia, which requires particularly strict monitoring of the patient. The factors contributing to the development of hypoglycemia include: the reluctance or (especially in old age) lack of the patient's ability to cooperate with a doctor; irregular, inadequate food, skipping meals, fasting, changes in the usual diet; drinking alcohol, especially when combined with skipping meals; imbalance between exercise and carbohydrate intake; renal dysfunction; severe abnormal liver function; overdose of Amaryl; uncompensated concomitant diseases of the endocrine system affecting carbohydrate metabolism (includingthyroid dysfunction, pituitary or adrenal insufficiency); simultaneous intake of other drugs.
It should be borne in mind that the symptoms of hypoglycemia may be smoothed out or absent altogether in elderly patients, patients with NCD or who are receiving simultaneous treatment with beta-blockers, clonidine, reserpine, guanethidine, or other sympatholytics.
The doses of Amaryl are determined by the level of glucose in the blood. Amaryl should be taken in prescribed doses and at the appointed time. The skip of the drug should never be corrected by the subsequent reception of a higher dose. The patient should immediately inform the doctor in case of receiving too high a dose of the drug.
Upon attaining the compensation of type 2 diabetes mellitus, insulin sensitivity increases; therefore, the need for glimepiride may decrease during the treatment process. In order to avoid the development of hypoglycemia, it is necessary to reduce the dose in time or to stop Amaryl. Dose adjustment should also be carried out when the patient's body weight changes or when their lifestyle changes, or when other factors appear that contribute to the development of hypo- or hyperglycemia.
Adequate diet, regular exercise and, if necessary, weight loss are just as important for achieving optimal control of blood glucose levels as regular glimepiride intake.
When switching to Amaryl from another drug, it is necessary to take into account the degree and duration of the effect of the preceding hypoglycemic drug. It may be necessary to temporarily discontinue treatment in order to avoid an additive effect.
If a patient has developed a hypoglycemic reaction while taking glimepiride in a dose of 1 mg / day, this indicates that the patient's normalization of blood glucose can be achieved using a single diet.
Currently, there is no experience with glimepiride in patients with severe impaired liver and kidney function or in patients on hemodialysis. Patients with severe impaired hepatic or renal function are shown to switch to insulin therapy.
The patient should be informed that when severe adverse reactions develop, one should immediately consult a doctor and not continue taking the drug without his recommendations.
The patient should be informed not only about the symptoms of hypoglycemia, but also about the symptoms of hyperglycemia (frequent urination, severe thirst, dry mouth, dry skin).
Control of laboratory parameters
During treatment, Amaryl requires regular monitoring of blood glucose and urine levels, as well as the concentration of glycated hemoglobin. Monitor observation of the above indicators helps to establish the primary or secondary resistance to the drug.
Also during treatment with glimepiride, it is necessary to monitor the function of the liver and the picture of peripheral blood (especially the number of platelets and leukocytes).
Influence on ability to drive motor transport and control mechanisms
At the beginning of treatment, when switching from one hypoglycemic drug to another or when taking glimepiride on an irregular basis, there may be a decrease in the concentration of attention and speed of the psychomotor reactions of the patient caused by hypo- or hyperglycemia. Therefore, in such situations, you should refrain from engaging in potentially hazardous activities that require increased attention and quickness of psychomotor reactions.

Amplification AMARE hypoglycemic action can be observed while the use of insulin or other hypoglycemic drugs, ACE inhibitors, Allopurinol , anabolic steroids and male sex hormones, chloramphenicol, coumarine derivatives, cyclo-, Trojan and ifosfamide, fenfluramine, feniramidolom, fibrates, Fluoxetine , guanethidine , MAO inhibitors , miconazole, Pentoxifylline (when administered parenterally in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, chi nolones, salicylates, sulfinpyrazone, long-acting sulfonamides, tetracyclines, tritoqualine.
The weakening of the hypoglycemic effect of Amaryl is possible with simultaneous use with acetazolamide,barbiturates, glucocorticosteroids, diazoxide, saluretics, thiazide diuretics, epinephrine (adrenaline) and other sympathomimetics, glucagon, laxatives (with long-term use), nicotinic acid (in high doses) and their derivatives, estrogens, progestogens, and chromosomals; thyroid hormones, lithium salts, chlorpromazine.
With simultaneous use of histamine H blockers₂-receptors, clonidine and reserpine are able to both strengthen and weaken the hypoglycemic effect of Amaryl.
While taking Amaryl, the effect of coumarin derivatives may be enhanced or weakened.
A single or chronic use of ethanol can both strengthen and weaken the hypoglycemic effect of glimepiride.

Symptoms: after taking high-dose glimepiride, hypoglycemia may develop for a period of 12-72 hours, which can be repeated after an initial recovery of blood glucose concentrations, accompanied by such manifestations as increased sweating, anxiety, tachycardia, increased blood pressure, heartbeat, pain in the heart, arrhythmia, headache, dizziness, a sharp increase in appetite, nausea, vomiting, apathy, drowsiness, anxiety, aggressiveness, impaired concentration, depression, confusion, conscious I, tremor, paresis, sensory disorder, seizures of central origin.Sometimes the clinical picture of hypoglycemia may resemble a stroke. Perhaps the development of coma.
Treatment: hypoglycemia can be quickly stopped by the immediate consumption of carbohydrates (glucose or sugar, for example, in the form of a piece of sugar, sweet fruit juice or tea). In this regard, the patient should always carry at least 20 g of glucose (4 pieces of sugar). Sweeteners are ineffective in the treatment of hypoglycemia. In severe cases, the patient must be hospitalized. It is necessary to induce vomiting, to appoint a fluid intake (water or lemonade with Activated carbon / adsorbent / and sodium sulfate / laxative /). The introduction of dextrose is started as soon as possible, if necessary, in the form of IV injection of 50 ml of 40% solution with subsequent infusions of a more diluted (10%) solution with careful monitoring of the level of glucose in the blood. Further treatment should be symptomatic.
In the treatment of hypoglycemia, which has developed as a result of accidental administration of Amaryl by infants or young children, in order to avoid hyperglycemia, the dose of dextrose (50 ml of 40% solution) should be monitored and the glucose concentration in the blood should be continuously monitored.

The preparation Amaryl should be stored at a temperature not higher than 25 ° C.

3 years.