Glimepiride
Glimepiride: 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: Glimepiride
ATX code: A10BB12
Active ingredient: Glimepiride (Glimepiride)
Manufacturer: Vertex (Russia), Rafarma (Russia), Pharmstandard-Leksredstva (Russia), Pharmproject (Russia), Pliva Hrvatska (Croatia)
Description and photo update: 2018-24-10
Prices in pharmacies: from 60 rubles.
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Glimepiride is a third generation hypoglycemic drug of the sulfonylurea group.
Release form and composition
Dosage form Glimepiride - tablets: white or almost white, flat-cylindrical; for dosages of 1 mg, 2 mg, 3 mg - with a bevelling, for a dosage of 4 mg - with a chamfer and a cross-shaped line, for a dosage of 6 mg - with a beveled carton box 3 or 6 packs of 10 tablets each, or 2 or 4 packs of 15 tablets, or 3 packs of 20 tablets, or 1 or 2 packs of 30 tablets; 30 or 60 tablets each in a HDPE jar, in a cardboard box 1 bank).
Composition of 1 tablet:
- active substance: glimepiride - 1/2/3/4/6 mg;
- auxiliary components: lactose monohydrate, microcrystalline cellulose, sodium carboxymethyl starch (sodium starch glycolate), povidone K-30, polysorbate 80, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Glimepiride is a hypoglycemic agent, a sulfonylurea derivative of a new (third) generation. Stimulates the release of insulin from the beta cells of the pancreas (pancreatic action), improving their ability to respond to glucose stimulation, while the amount of insulin secreted is significantly less than with the action of other sulfonylurea derivatives, which reduces the risk of hypoglycemia.
In addition, glimepiride has an extra-pancreatic effect - it increases the sensitivity of peripheral tissues (fat and muscle) to the action of its own insulin, reduces the absorption of insulin by the liver, and inhibits the production of glucose in the liver. Also, the drug has an antithrombotic effect, selectively inhibiting cyclooxygenase and reducing the conversion of arachidonic acid to thromboxane A2, which promotes platelet aggregation.
Glimepiride normalizes the lipid content, lowers the level of malonic aldehyde in the blood, leading to a decrease in lipid peroxidation, which contributes to the antiatherogenic effect of the drug.
In addition, the drug reduces the severity of oxidative stress present in the body of a patient with type 2 diabetes mellitus by increasing the level of endogenous α-tocopherol, catalase, glutathione peroxidase and superoxide dismutase activity.
Pharmacokinetics
The maximum concentration (C max) of glimepiride after repeated administration in a daily dose of 4 mg is reached in about 2.5 hours and is 309 ng / ml. There is a linear relationship between the dose and C max of glimepiride in blood plasma, as well as between the dose and the area under the concentration-time curve (AUC). The bioavailability of glimepiride is complete. Eating only insignificantly slows down the absorption of the drug.
The degree of binding of glimepiride to plasma proteins is 99%. The volume of distribution is 8.8 liters. The clearance of the drug is 48 ml / min. The average elimination half-life is 5-8 hours. Taking high doses increases the half-life slightly.
With a single dose of glimepiride, 58% of its dose is excreted by the kidneys and 35% by the intestine. The drug is excreted in the form of metabolites formed as a result of metabolism in the liver (mainly with the help of the isoenzyme CYP2C9), one of them was a hydroxy derivative, and the other was a carboxy derivative. The half-life of these metabolites is 3-5 hours and 5-6 hours, respectively.
The drug crosses the placental barrier and is also found in breast milk.
In patients with impaired renal function (with reduced creatinine clearance), the clearance of the drug increases, and its average plasma concentrations decrease due to the rapid elimination of the drug caused by its lower binding to protein.
Indications for use
Glimepiride is indicated for type 2 diabetes mellitus (in monotherapy or as part of combination therapy with metformin or insulin).
Contraindications
Absolute:
- type 1 diabetes mellitus;
- diabetic ketoacidosis, diabetic precoma and coma;
- glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- severe renal dysfunction, including in patients on hemodialysis;
- severe liver dysfunction;
- childhood;
- pregnancy and lactation;
- hypersensitivity to drug components, as well as to other sulfonylurea derivatives or sulfonamide drugs.
Relative:
- the presence of risk factors for the development of hypoglycemia;
- intercurrent diseases during treatment;
- changes in the patient's lifestyle (changes in diet and meal times, increase or decrease in physical activity);
- insufficiency of glucose-6-phosphate dehydrogenase;
- diseases that impair the absorption of food and drugs from the gastrointestinal tract (intestinal obstruction, intestinal paresis).
Also, special care is needed at the beginning of treatment due to the increased risk of hypoglycemia.
Instructions for the use of Glimepiride: method and dosage
Glimepirid tablets are taken orally, without chewing, with half a glass of water. If necessary, the tablets are divided into equal parts along the lines.
Usually, the minimum dose of the drug is prescribed, sufficient to achieve the desired blood glucose concentration. The starting dose is 1 mg per day. Further, if necessary, it can gradually increase (with an interval of 1–2 weeks). As the dose is increased, the patient needs to monitor the blood glucose concentration. Recommended dosage increments: 1 mg - 2 mg - 3 mg - 4 mg - 6 mg.
In well-controlled diabetes mellitus, the dose of Glimepiride is usually 1–4 mg / day. The maximum daily dose is 6 mg; only in a small number of patients, increasing the daily dose to 8 mg was more effective.
The time of taking the drug is prescribed by the doctor and depends on the patient's daily regimen. In normal cases, a single dose of Glimepiride during the day is sufficient, before a full breakfast or the first main meal. Do not skip meals after taking the pill.
Improving metabolic control is accompanied by an increase in insulin sensitivity, so the need for glimepiride during treatment may decrease, and therefore it is necessary to adjust its dose in a timely manner to avoid hypoglycemia.
Also, a dose adjustment of glimepiride may be required when the patient's body weight is reduced, his lifestyle changes (meal time, amount of physical activity, diet change), the occurrence of factors leading to the development of hypoglycemia or hyperglycemia.
Treatment with glimepiride is usually long-term.
When transferring a patient from another oral hypoglycemic agent to Glimepiride, its usual initial dose (1 mg / day) is recommended, even if the patient took the maximum dose of the previous drug. Further, the dose can be gradually increased. Given the strength and duration of the effect of the previous hypoglycemic agent, a break in treatment may be required to avoid an increase in the effect of the drugs.
Combination therapy with metformin
If the effect of taking the maximum daily doses of glimepiride or metformin is insufficient, it is possible to use a combination of these substances under strict medical supervision. In this case, the previously taken drug continues to be used at the same dose, and the additional one begins to be used at the lowest dose, which then increases depending on the clinical effect.
Combination therapy with insulin
If the effect of taking the maximum daily dose of glimepiride is insufficient, additional insulin administration is possible. In this case, Glimepiride continues to be used at the same dose, and insulin begins to be used at the lowest dose, which then increases under the control of the blood glucose concentration. Combination therapy should be carried out under medical supervision.
Side effects
- metabolism and nutrition: hypoglycemia, including severe (its symptoms are described in the subheading "Overdose"), the clinical picture of which may be similar to a stroke. After elimination of hypoglycemia, its symptoms disappear;
- organ of vision: transient visual impairments (especially at the beginning of treatment) associated with a change in the concentration of glucose in the blood, which leads to a temporary change in the swelling of the lens and, as a consequence, a distortion of the refractive index of the lens;
- Gastrointestinal tract: rarely - nausea, vomiting, abdominal pain, diarrhea, feeling of heaviness or fullness in the epigastrium, sometimes - hepatitis, increased activity of liver enzymes, cholestasis and jaundice, which can progress to life-threatening liver failure (if the drug is discontinued, reverse development is possible);
- blood and lymphatic system: in rare cases - thrombocytopenia, leukopenia, hemolytic anemia, erythrocytopenia, granulocytopenia, agranulocytosis, pancytopenia;
- immune system: rarely - allergic and pseudo-allergic reactions (itching, rash, urticaria), sometimes - vasculitis, photosensitivity. Usually, allergic reactions are mild, but sometimes severe complications can develop with a sharp decrease in blood pressure, shortness of breath, in some cases anaphylactic shock is possible. At the first symptoms of hives, you should consult a doctor;
- laboratory indicators: a decrease in the concentration of sodium in the blood plasma.
Overdose
Overdose of the drug (both acute and in the case of long-term use of high doses) can lead to severe, life-threatening hypoglycemia, which is characterized by the following symptoms: headache, nausea, vomiting, feeling of hunger and fatigue, impaired concentration, alertness and reaction speed, visual disturbances, sleep disturbances, drowsiness, aggressiveness, sensory disturbances, anxiety, confusion, depression, speech disorders, tremor, aphasia, paresis, dizziness, loss of self-control, delirium, cerebral cramps, somnolence or loss of consciousness up to coma, shallow breathing, bradycardia. In addition, manifestations of adrenergic counterregulation are possible, such as the appearance of cold clammy sweat, anxiety, tachycardia, increased blood pressure, angina pectoris,feeling of palpitations and heart rhythm disturbances.
An overdose of the drug must be immediately reported to the doctor. Hypoglycemia is quickly stopped by the use of carbohydrates (sweet tea, juice, sugar cube, etc.), therefore it is recommended to always have 20 g of glucose (4 sugar cubes) with you. Sweeteners are ineffective.
The patient needs close medical supervision until the doctor decides that he is out of danger. After initial recovery of blood glucose concentration, hypoglycemia may resume. When a patient is being treated by different doctors, he must inform each of them about his illness and previous treatment.
As a precaution, the patient may need to be hospitalized. The indication for hospitalization is a severe overdose with loss of consciousness and other serious neurological disorders.
If the patient is unconscious, an intravenous administration of a glucose solution (dextrose) is necessary. For adult patients, a concentrated solution (20%) is administered starting from 40 ml; an alternative is intravenous, subcutaneous, or intramuscular glucagon in a dose of 0.5–1 mg.
If Glimepiride is accidentally taken by infants and young children, the dose of dextrose administered must be carefully adjusted to avoid the occurrence of dangerous hyperglycemia. During the administration of dextrose, it is necessary to constantly monitor the concentration of glucose in the blood.
In some cases, after an overdose of Glimepiride, gastric lavage and the appointment of activated carbon may be required.
To prevent recurrence of hypoglycemia after an initial rapid recovery of blood glucose concentration, it is advisable to administer an intravenous infusion of a dextrose solution at a lower concentration. In such patients, the blood glucose concentration should be monitored for 24 hours. In the case of prolonged hypoglycemia, the risk of lowering blood glucose levels to hypoglycemic levels may persist for several days.
special instructions
In some situations, for example, trauma, surgery, infections occurring with a febrile temperature, metabolic control in patients with diabetes may deteriorate, in which case it may be necessary to temporarily transfer the patient to insulin therapy.
During the first weeks of taking the drug, more careful monitoring of the concentration of glucose in the blood is necessary, since during this period the risk of developing hypoglycemia increases.
Factors contributing to the risk of developing hypoglycemia:
- unwillingness or inability of the patient to cooperate with the doctor;
- irregular food intake, malnutrition;
- diet change;
- imbalance between exercise and carbohydrate intake;
- alcohol intake, especially while skipping meals;
- severe renal dysfunction;
- severe liver dysfunction (such patients are shown switching to insulin therapy, at least until metabolic control is achieved);
- overdose of glimepiride;
- some decompensated endocrine disorders that disrupt carbohydrate metabolism or adrenergic counterregulation in response to hypoglycemia (some disorders of the thyroid gland and anterior pituitary gland, adrenal insufficiency);
- joint administration with some drugs;
- taking the drug without indications for it.
Patients with deficiency of glucose-6-phosphate dehydrogenase should be approached with extreme caution when taking Glimepiride, as it can lead to the development of hemolytic anemia. In such cases, it is better to use hypoglycemic agents that are not sulfonylurea derivatives.
In the presence of these factors in the development of hypoglycemia, it may be necessary to adjust the dose of Glimepiride or the entire therapy.
Symptoms of hypoglycemia, reflecting adrenergic counterregulation of the body in elderly patients, patients with autonomic neuropathy, as well as in patients taking beta-blockers, clonidine, reserpine and other symptomatic drugs, may be mild or absent.
Immediate intake of rapidly digestible carbohydrates (glucose, sucrose) can quickly eliminate hypoglycemia.
Patients taking Glimepiride should be monitored constantly, as hypoglycemia may recur despite its initial successful relief.
Severe hypoglycemia requires immediate treatment, as well as medical supervision, in some cases, hospitalization is necessary.
During the period of taking Glimepiride, regular monitoring of liver function and peripheral blood patterns (in particular the number of leukocytes and platelets) should be carried out.
Some side effects of the drug can be life-threatening, and therefore, if severe reactions develop, you should immediately inform your doctor about this, stopping the drug until further prescriptions.
Missing one dose of the drug should not be replenished with a subsequent double dose. Actions in case of errors in taking the drug should be discussed with the doctor in advance.
Influence on the ability to drive vehicles and complex mechanisms
At the beginning or after a change in treatment, as well as with irregular use of the drug, there is a risk of hypoglycemia or hyperglycemia, which may lead to a decrease in attention and speed of psychomotor reactions. In this regard, the patient's ability to drive vehicles and other complex mechanisms that require the speed of psychomotor reactions may be impaired.
Application during pregnancy and lactation
According to the instructions, Glimepiride is contraindicated for use in pregnant women. In case of planning or the onset of pregnancy, the patient should be transferred to insulin therapy.
The drug passes into breast milk. During lactation, a woman should be transferred to insulin therapy or breastfeeding should be interrupted.
Pediatric use
The experience of using Glimepiride in children is insufficient.
With impaired renal function
The limited experience with the use of Glimepiride in patients with renal insufficiency suggests that this group of patients may be more sensitive to the hypoglycemic effect of the drug.
For violations of liver function
The experience of using Glimepiride in liver failure is limited.
Drug interactions
Glimepiride is metabolized by cytochrome P450 2C9 (CYP2C9), which should be taken into account when taken together with inducers or inhibitors of the isoenzyme CYP2C9.
- insulin and other oral hypoglycemic drugs, chloramphenicol, angiotensin-converting enzyme (ACE) inhibitors, guanethidine, anabolic steroids and male sex hormones, cyclophosphamide, coumarin derivatives, disopyramide, phenyramidol, pentoxifylline doses, fenyramidol, pentoxifylline doses (high parenteralfuramine) monoamine oxidase (MAO), fluconazole, paraaminosalicylic acid, phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, clarithromycin, sulfonamides, tetracyclines, trofosfamide: can also potentiate hypoglycemic action in some cases;
- diazoxide, acetazolamide, glucocorticosteroids, barbiturates, diuretics, epinephrine and other sympathomimetic drugs, glucagon, laxatives (with prolonged use), nicotinic acid (in high doses), estrogens and progestogens, phenothiazines, phenytoin, rifampicin: reduce the thyroid gland hypoglycemic effect of Glimepiride and, as a result, increase the concentration of glucose in the blood;
- beta-blockers, blockers of H 2 -histamine receptors, clonidine and reserpine: can both enhance and reduce the hypoglycemic effect of the drug;
- beta-blockers, guanethidine and reserpine, clonidine: when taken together with these drugs, the signs of adrenergic counterregulation in response to hypoglycemia may decrease or be absent;
- kolesevelam: reduces the absorption of glimepiride from the gastrointestinal tract. When taking Glimepiride 4 hours before colevelam, interaction does not occur, and therefore, an interval of at least 4 hours must be observed between taking these drugs.
Glimepiride can both enhance and weaken the effect of coumarin derivatives.
Alcohol consumption (both single and chronic) can increase or decrease the effect of glimepiride.
Analogs
Analogs of Glimepiride are: Amapirid, Glibenclamide, Amix, Maninil, Glibetik, Glinova, Diabrex, Dimaril, Amaryl, Glemaz, Glirid, Glimax, Eglim, Oltar, Perinel, Glairi, Glianov, Diabeton.
Terms and conditions of storage
Store away from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Glimepiride
Reviews about Glimepiride are mostly positive, the drug is effective in type 2 diabetes, if you strictly follow the prescription regimen. A plus is also considered a single dose of the drug per day. Among the minuses, it is noted that in some patients it can cause nausea and weight gain.
Price for Glimepiride in pharmacies
The estimated price for Glimepiride is 270 rubles. per package containing 30 tablets of 4 mg.
Glimepiride: prices in online pharmacies
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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!
