Amaryl
Amaryl: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Amaryl
ATX code: A10BB12
Active ingredient: glimepiride (glimepiride)
Producer: Aventis Pharma Deutschland GmbH (Germany)
Description and photo update: 2019-16-09
Prices in pharmacies: from 301 rubles.
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Amaryl is a drug designed to lower blood sugar in type 2 diabetes.
Release form and composition
Amaryl is available in oval tablets with a dosage of 1, 2, 3 and 4 mg. The active ingredient of the drug is glimepiride.
Pharmacological properties
Pharmacodynamics
Glimepiride helps to lower blood glucose (mainly by stimulating the release of insulin by the β-cells of the pancreas). This effect is mainly based on the fact that the β-cells of the pancreas improve their ability to respond to physiological glucose stimulation. In comparison with glibenclamide, low doses of glimepiride cause the release of lower doses of insulin with approximately the same decrease in glucose content, which indicates an extrapancreatic hypoglycemic effect of glimepiride (increased tissue sensitivity to insulin, insulinomimetic effect).
Insulin secretion
Similar to other sulfonylurea derivatives, glimepiride affects insulin secretion by acting on ATP-sensitive potassium channels on the membranes of β-cells of the pancreas.
The difference from other sulfonylurea derivatives is the selective bond of glimepiride with a protein having a molecular weight of 65 kilodaltons and contained in β-cell membranes. This effect of glimepiride regulates the process of closing / opening of ATP-sensitive potassium channels. Amaryl closes potassium channels, which leads to depolarization of β-cells, opening of voltage-sensitive calcium channels and the flow of calcium into the cell. With an increase in the intracellular calcium concentration, insulin secretion is activated by exocytosis. In comparison with glibenclamide, glimepiride binds faster and more often and is released from bonds with the corresponding protein. Presumably, the high rate of exchange of glimepiride with protein contributes to the pronounced sensitization of β-cells to glucose, and also protects them from desensitization and rapid depletion.
Increased insulin sensitivity
Taking glimepiride increases the effect of insulin on the absorption of glucose by the peripheral tissues of the body.
Insulinomimetic effect
The effect of glimepiride is similar to the effect of insulin on the absorption of glucose by peripheral tissues and its release from the liver.
Peripheral tissues absorb glucose by transporting it to muscle cells and adipocytes. Glimepiride increases the number of glucose transporting molecules and activates glycosylphosphatidylinositol-specific phospholipase C. As a result, the intracellular calcium concentration decreases, which leads to a decrease in the activity of protein kinase A and stimulation of glucose metabolism. Under the influence of glimepiride, the release of glucose from the liver is inhibited (due to an increase in the content of fructose-2,6-bisphosphate, which inhibits gluconeogenesis).
Effects on platelet aggregation
In vivo and in vitro, glimepiride reduces platelet aggregation. This effect is likely due to the selective inhibition of cyclooxygenase, which is responsible for the formation of thromboxane A, which is considered an important endogenous factor of platelet aggregation.
Antiatherogenic effect
Glimepiride normalizes the lipid content, reduces the concentration of malonic aldehyde in the blood, as a result of which lipid peroxidation is significantly reduced. In animal studies, it was found that taking glimepiride significantly reduces the formation of atherosclerotic plaques.
Glimepiride provides a decrease in the severity of oxidative stress characteristic of type 2 diabetes mellitus, increases the concentration of endogenous alpha-tocopherol, as well as the activity of catalase, superoxide dismutase and glutathione peroxidase.
Cardiovascular effects
Sulfonylurea derivatives affect the state of the cardiovascular system by affecting ATP-sensitive potassium channels. In comparison with other sulfonylurea derivatives, glimepiride is characterized by a significantly lower effect on the cardiovascular system, which may be due to the specific process of its association with proteins of ATP-sensitive potassium channels.
The minimum effective dose in healthy volunteers is 0.6 mg. The effect of glimepiride is reproducible and dose-dependent.
When taking Amaril, physiological reactions to physical activity are preserved (decrease in insulin secretion).
There are no reliable data on the differences in the effect of the time of taking the drug (when taken directly before meals or 0.5 hours before meals). With diabetes mellitus, a single dose of Amaril allows you to provide sufficient metabolic control for 1 day. In a clinical study involving 16 volunteers suffering from renal insufficiency (creatinine clearance 4 to 79 ml / min), sufficient metabolic control was achieved in 12 patients.
Combination treatment with metformin
With insufficient metabolic control in patients taking the maximum dose of glimepiride, there is the possibility of combination therapy with metformin and glimepiride. In two studies, combination therapy showed a significant increase in metabolic control compared with separate treatment with each of these drugs.
Combined treatment with insulin
With insufficient metabolic control in patients taking the maximum dose of glimepiride, there is the possibility of combination therapy with metformin and insulin. In two studies, combination therapy has shown an increase in metabolic control, similar to insulin monotherapy. However, combination therapy requires a lower dose of insulin.
Therapy in children
There is insufficient data on the long-term safety and effectiveness of the use of Amaril in childhood.
Pharmacokinetics
In cases of repeated administration of glimepiride at a dose of 4 mg per day, the time to reach the maximum concentration in the serum is about 2.5 hours, and the maximum plasma concentration of the active substance is 309 ng / ml. The maximum plasma concentration of glimepiride and the area under the concentration-time pharmacokinetic curve linearly depend on the dose of Amaril. With oral administration of glimepiride, complete absolute bioavailability is observed. Absorption does not significantly depend on food intake (except for a slight slowdown in the rate of absorption). Glimepiride has a very low volume of distribution (~ 8.8 L), which is approximately equal to the volume of distribution of albumin. The active substance is characterized by a high degree of binding to plasma proteins (over 99%) and a low clearance (~ 48 ml / min). Determined by serum concentration with repeated administration of Amaril, the average elimination half-life is 5 to 8 hours. In the case of taking high doses, the half-life is slightly increased.
As a result of a single oral administration of glimepiride, 58% of the dose is excreted by the kidneys, and 35% of the dose through the intestines. In urine, unchanged glimepiride is not detected.
In feces and urine, two metabolites formed in the liver (mainly with the participation of the CYP2C9 isoenzyme) were identified, one of which is a carboxy derivative, and the other is a hydroxy derivative. After oral administration, the terminal half-life of these metabolites was 5–6 and 3–5 hours, respectively.
The active substance crosses the placental barrier and is excreted into breast milk.
When comparing single and multiple doses of glimepiride, there were no significant differences in pharmacokinetic parameters, and there was also very low variability in different patients. There is no significant accumulation of the active substance.
The pharmacokinetic parameters are similar in patients of different age groups and different sexes. In case of impaired renal function (with low creatinine clearance), an increase in the clearance of glimepiride and a decrease in its average concentration in the blood serum are possible. In all likelihood, this is due to the higher rate of elimination of the drug due to the lower degree of protein binding. Accordingly, patients in this category do not have a risk of accumulation of Amaril.
Indications for use
According to the instructions, Amaryl is prescribed for type 2 diabetes mellitus (non-insulin dependent diabetes).
The active ingredient glimepiride stimulates the production of insulin by the pancreas and its entry into the blood. Insulin, in turn, reduces the amount of sugar in the blood. Glimepiride improves potassium metabolism in cells, and also helps to prevent the formation of atherosclerotic plaques on the walls of blood vessels.
Contraindications
Amaryl is contraindicated in the following diseases:
- Type 1 diabetes mellitus (insulin dependent);
- Diabetic ketoacidosis (complication of type 1 diabetes)
- Severe kidney and liver diseases;
- Diabetic coma and precoma preceding it;
- Glucose-galactose malabsorption, lactase deficiency, galactose intolerance;
- Childhood;
- Individual intolerance to any component of Amaril;
- Pregnancy and lactation.
Instructions for the use of Amaril: method and dosage
According to the instructions, Amaryl should be taken orally without chewing, immediately before or during breakfast, washed down with plenty of water (at least ½ glass). Taking medicine must necessarily be tied to food intake, otherwise a critical decrease in blood sugar levels is possible.
The dosage for each patient is selected by the attending physician individually, depending on the blood sugar level.
Treatment is usually started with a minimum dose of Amaril - 1 mg per day. Depending on the patient's condition, the doctor can gradually (once every 1-2 weeks) increase the dosage of Amaril, following the scheme: 1-2-3-4-6 mg. The most common dosages are 1-4 mg per day.
If the patient has forgotten to take the daily dose of the drug, then the next time the dose is taken, the dosage should not be increased. Actions in case of accidental violation of the treatment regimen should be discussed with the doctor in advance.
During the use of Amaryl, control over blood sugar levels is necessary.
Side effects
The most common side effect of taking the drug is hypoglycemia (a drop in blood sugar levels below normal). In addition, the use of Amaril can cause the following negative effects:
- From the side of the cardiovascular system: arterial hypertension, tachycardia, angina pectoris, bradycardia;
- From the hematopoietic system: thrombocytopenia, leukopenia, anemia, pancytopenia, granulocytopenia, agranulocytosis;
- From the nervous system: drowsiness or insomnia, headache, increased aggressiveness, decreased reaction rate, anxiety, loss of consciousness, speech disorders, convulsions, tremors in the limbs;
- From the digestive system: vomiting, nausea, diarrhea, feeling of heaviness in the stomach, cholestasis, jaundice, hepatitis;
- Allergic reactions: itching, urticaria, allergic vasculitis, skin rash;
- Visual impairment.
Overdose
Symptoms
In cases of acute overdose or with prolonged therapy with high doses of glimepiride, there is a risk of developing severe hypoglycemia with a threat to life.
Treatment
When diagnosing an overdose, you should immediately seek medical attention. Almost always, hypoglycemia can be quickly stopped by immediate intake of carbohydrates (a lump of sugar, glucose, tea or sweet fruit juice), so the patient should always have 4 lumps of sugar (20 g of glucose) with him. Sugar substitutes are ineffective in the treatment of hypoglycemia.
The patient must be under close medical supervision until the moment when the doctor decides that there is no danger of complications. Consideration should be given to the possibility of resumption of hypoglycemia after restoration of blood glucose.
When treating a patient with diabetes mellitus with different doctors (for example, on weekends or when admitted to the hospital as a result of an accident), he must definitely inform about his illness, as well as about previous treatment.
In some cases, hospitalization may be required. A significant overdose with a severe reaction (loss of consciousness or other serious neurological disorders) is a medical emergency and requires immediate hospitalization and therapy.
When the patient is unconscious, a concentrated solution of glucose (dextrose) 20% is injected intravenously (for adults, a dose of 40 ml of solution is indicated). In adults, an alternative treatment option is intravenous, intramuscular, or subcutaneous glucagon (0.5 to 1 mg).
If Amaril is accidentally taken by young children or infants, the dose of dextrose administered for hypoglycemia should be carefully adjusted taking into account the likelihood of dangerous hyperglycemia. The introduction of dextrose must be carried out under constant monitoring of blood glucose levels.
In case of overdose, gastric lavage and administration of activated charcoal may be required.
The rapid restoration of blood glucose requires the mandatory intravenous administration of a lower concentration of dextrose solution in order to prevent the recurrence of hypoglycemia. In such patients, the concentration of glucose in the blood should be constantly monitored for 1 day. In severe cases, with a prolonged course of hypoglycemia, the risk of lowering the glucose content to a hypoglycemic level persists for several days.
special instructions
In case of side effects after taking Amaril and deterioration of the general condition, you should immediately seek the advice of your doctor.
During the course of drug treatment, it is recommended to regularly monitor blood glucose levels and liver function.
The use of the drug requires increased caution when working with complex mechanisms and transport control.
Application during pregnancy and lactation
During pregnancy, the use of Amaril is contraindicated. With a planned pregnancy or with the onset of pregnancy during drug therapy, a woman should be transferred to insulin therapy.
Since glimepiride is excreted in breast milk, the use of Amaril when breastfeeding is contraindicated. In this case, the transition to insulin therapy or the cessation of breastfeeding is indicated.
Pediatric use
Amaryl is contraindicated for the treatment of patients in childhood.
With impaired renal function
In severe renal impairment, the use of Amaril is contraindicated.
For violations of liver function
In severe liver dysfunction, the use of Amaril is contraindicated.
Drug interactions
Glimepiride is metabolized by the CYP2C9 isoenzyme of the cytochrome P4502C9 system, which should be taken into account when used together with inducers (for example, rifampicin) or inhibitors (for example, fluconazole) CYP2C9. When combined with the drugs listed below, potentiation of the hypoglycemic action can develop, and in some cases the development of hypoglycemia resulting from this: insulin and other hypoglycemic drugs for oral administration, angiotensin-converting enzyme inhibitors, male sex hormones, anabolic steroids, coumarin derivatives, chloramphenicol, disloopyramide, feniramidol, fenfluramine, fluoxetine, fibrates, ifosfamide, guanethidine, monoamine oxidase inhibitors, fluconazole, pentoxifylline (in high parenteral doses), para-aminosalicylic acid, azapropazone, phenylbutazone, probenecid,oxyphenbutazone, salicylates, quinolones, clarithromycin, sulfinpyrazone, tetracyclines, sulfonamides, trophosphamide, tritoqualin.
When combined with the drugs listed below, a weakening of the hypoglycemic effect may be observed, as well as an increase in blood glucose associated with this: acetazolamide, glucocorticosteroids, barbiturates, diuretics, epinephrine, other sympathomimetic drugs, glucagon, nicotinic acid (high doses), laxatives (in cases of long-term use), progestogens, estrogens, rifampicin, phenytoin, phenothiazines, iodine-containing thyroid hormones.
When used together with beta-blockers, blockers of H 2 -histamine receptors, clonidine and reserpine, both weakening and strengthening of the hypoglycemic effect of glimepiride are possible.
When taking sympatholytic drugs (beta-blockers, guanethidine, reserpine and clonidine), signs of adrenergic counterregulation may be absent or decreased in hypoglycemia.
The combined use of glimepiride and coumarin derivatives can enhance or weaken the effect of the latter.
In the case of a single or chronic consumption of alcohol, the hypoglycemic effect of glimepiride can both increase and decrease.
Use with sequestrants of bile acids: colesevelam, binding with glimepiride, reduces its absorption from the gastrointestinal tract; when using glimepiride 4 hours before taking colesevelam, no interaction was recorded.
Analogs
Structural analogs of Amaril include the following drugs: Glemaz, Glyumedex, Meglimid, Diamerid, Glemauno.
Storage conditions and periods
The drug should be stored in a dry, dark place at an air temperature not exceeding 25 ° C.
The shelf life of Amaril is 3 years from the date of production.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Amaril
Reviews of Amaril indicate that the key to the effectiveness of the drug is the correct selection of the dose and treatment regimen. At the same time, some reports contain information that at the initial stage of taking Amaril in patients, the blood sugar level changed sharply. According to experts, this phenomenon can be dealt with by adjusting the dose by the doctor (if the drug is taken illiterately, the risk of developing complications of the disease increases).
Amaryl price in pharmacies
The approximate price for Amaryl is: 30 tablets 1 mg - 330 rubles, 30 tablets 2 mg - 620 rubles, 30 tablets 3 mg - 940 rubles, 30 tablets 4 mg - 1200 rubles, 90 tablets 2 mg - 1700 rubles., 90 tablets 3 mg - 2200 rubles, 90 tablets 4 mg - 2900 rubles.
Amaryl: prices in online pharmacies
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Drug name Price Pharmacy |
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Amaryl 1 mg tablets 30 pcs. 301 RUB Buy |
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Amaryl tablets 1mg 30 pcs. 336 r Buy |
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Amaryl 2 mg tablets 30 pcs. 428 r Buy |
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Amaryl 3 mg tablets 30 pcs. 573 r Buy |
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Amaryl 2mg tablets 30 pcs. 601 RUB Buy |
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Amaryl M 2 mg + 500 mg film-coated tablets 30 pcs. 698 r Buy |
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Amaryl M tablets p.p. 2mg + 500mg 30 pcs. 746 RUB Buy |
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Amaryl 3mg tablets 30 pcs. 857 r Buy |
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Amaryl 4 mg tablets 30 pcs. 1098 RUB Buy |
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Amaryl tablets 4mg 30 pcs. 1169 RUB Buy |
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Amaryl 3 mg tablets 90 pcs. 1627 RUB Buy |
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Amaryl 3mg tablets 90 pcs. RUB 2166 Buy |
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Amaryl 4 mg tablets 90 pcs. 2400 RUB Buy |
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Amaryl 4mg tablets 90 pcs. 2873 RUB Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
