Composition
Active ingredient:
glimepiride 3 mg;
Auxiliary substances:
lactose monohydrate 150.80 mg,
corn starch 4.66 mg,
sodium carboxymethyl starch 10.00 mg,
Povidone 6.00 mg,
Polysorbate 1.34 mg,
talc 2.00 mg,
magnesium stearate 1.20 mg,
iron dye (E 172) 0.30 mg
Pharmacological action
Glimepiride is a hypoglycemic drug for oral use-a new (third) generation sulfonylurea derivative. Glimepiride works mainly by stimulating the secretion and release of insulin from pancreatic beta cells (pancreatic action). As with other sulfonylurea derivatives, this effect is based on an increase in the response of pancreatic beta cells to physiological glucose stimulation, while the amount of insulin secreted is significantly lower than with traditional drugs-sulfonylurea derivatives. The lowest stimulating effect of glimepiride on insulin secretion also provides a lower risk of hypoglycemia. In addition to this, glimepiride has an extra-pancreatic effect – the ability to improve the sensitivity of peripheral tissues (muscle, fat) to the action of its own insulin, reduce the absorption of insulin by the liver; inhibits glucose production in the liver.
Glimepiride selectively inhibits cyclooxygenase and reduces the conversion of arachidonic acid to thromboxane a2, which promotes platelet aggregation, thus having an antithrombotic effect.
Glimepiride helps to normalize the lipid content, reduces the level of malic aldehyde in the blood, which leads to a significant decrease in lipid peroxidation, this contributes to the anti-atherogenic effect of the drug.
Glimepiride increases the level of endogenous alpha-tocopherol, catalase, glutathione peroxidase and superoxide dismutase activity, which helps to reduce the severity of oxidative stress in the patient’s body, which is constantly present in type 2 diabetes mellitus.
Indications
Type 2 diabetes mellitus.
Contraindications
Hypersensitivity, type 1 diabetes mellitus, diabetic ketoacidosis, diabetic precoma and coma, severe liver and kidney dysfunction, leukopenia, pregnancy, breast-feeding.
Side effects
Cardiovascular and blood disorders (hematopoiesis, hemostasis):  rarely — downgrade Blood pressure, thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis, erythropenia, pancytopenia, hemolytic and aplastic anemia.
Nervous system and sensory disorders: Â dizziness, headache, temporary visual impairment.
From the digestive tract: Â nausea, vomiting, abdominal pain, heaviness in the epigastric region, diarrhea, intrahepatic cholestasis.
From the side of metabolism: Â hypoglycemia.
Other services: Â increased transaminase levels, hyponatremia, allergic skin reactions, late cutaneous porphyria, asthenia; rarely-shortness of breath, hepatitis, allergic vasculitis, photosensitization.
Interaction
The hypoglycemic effect of glimepiride may be enhanced when used concomitantly with insulin or other hypoglycemic drugs, ACE inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, phenyramidol, fibrates, fluoxetine, guanethidine, isophosphamides, MAO inhibitors, miconazole, PASC, pentoxifylline (when injected in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, sulfonamides, tetracyclines.
Weakening of the hypoglycemic effect of glimepiride is possible when used simultaneously with acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine (epinephrine) and other sympathomimetics, glucagon, laxatives (after prolonged use), nicotinic acid (in high doses), estrogens and progestogens, phenothiazine, phenytoin, rifampicin, thyroid hormones.
When used concomitantly, histamine H2-receptor blockers, clonidine and reserpine can both potentiate and reduce the hypoglycemic effect of glimepiride.
When using glimepiride, the effect of coumarin derivatives may increase or decrease.
Ethanol may increase or decrease the hypoglycemic effect of glimepiride.
How to take, course of use and dosage
The drug is used internally. The initial and maintenance doses of Glimepiride are determined individually based on the results of regular monitoring of blood glucose concentrations.
Starting dose and dose selection At the beginning of treatment,1 mg of Glimepiride is prescribed once a day. When the optimal therapeutic effect is achieved, it is recommended to take this dose as a maintenance dose. In the absence of glycemic control, the daily dose should be gradually increased under regular monitoring of blood glucose concentration (at intervals of 1-2 weeks) to 2 mg,3 mg or 4 mg per day. Doses above 4 per day are effective only in exceptional cases. The maximum recommended daily dose is 6 mg.
Use in combination with metformin In the absence of glycemic control in patients taking metformin, concomitant therapy with Glimepiride may be initiated. If the metformin dose is maintained at the same level, treatment with Glimepiride begins with the minimum dose, and then the dose gradually increases depending on the desired level of glycemic control, up to the maximum daily dose. Combination therapy should be performed under close medical supervision.
Use in combination with insulin In cases where it is not possible to achieve glycemic control 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 Glimepiridaa prescribed to the patient remains unchanged. In this case, treatment with insulin begins with a minimum dose, with a possible subsequent gradual increase in its dose under the control of blood glucose concentration. Combined treatment requires mandatory medical supervision.
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 prescribe a single daily dose immediately before or during a full breakfast or the first main meal. Glimepiride 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 Glimepiride.
Duration of treatmentas a rule, treatment with Glimepiride is long.
Transfer of the patient from another oral hypoglycemic drug to glimepiride. When transferring a patient from another oral hypoglycemic drug to Glimepiride, the initial daily dose of the latter should be 1 mg (even if the patient is transferred to Glimepiridt from the maximum dose of another oral hypoglycemic drug). Any increase in the dose of Glimepiride should be carried out in stages in accordance with the recommendations given above. It is necessary to take into account the effectiveness, dose and duration of action of the hypoglycemic agent used. In some cases, especially when taking hypoglycemic drugs with a long half-life (for example, chlorpropamide), it may be necessary to temporarily (for several days) stop treatment in order to avoid an additive effect that increases the risk of hypoglycemia.
Transfer of a patient from insulin to glimepiridein exceptional cases, when conducting insulin therapy in patients with type 2 diabetes mellitus, when the disease is compensated and when the secretory function (3-cells of the pancreas) is preserved, it is possible to replace insulin with Glimepiride. The transfer should be carried out under the close supervision of a doctor. In this case, the transfer of the patient to Glimepiride begins with a minimum dose of 1 mg.
Overdose
Symptoms: Â hypoglycemia (nausea, vomiting and epigastric pain, restlessness, tremor, visual disturbances, coordination disorders, drowsiness, coma and convulsions).
Treatment: Â if the patient is conscious – induction of vomiting, heavy drinking, activated charcoal and laxatives. In case of severe overdose-intravenous bolus use of dextrose solution (50 ml of 40% solution), followed by infusion of 10% solution. It is necessary to constantly monitor the patient, maintain vital functions and monitor the concentration of glucose in the blood (possible recurrence of episodes of hypoglycemia). Further treatment is symptomatic.
Tablet Form of production
Storage conditions
In a place protected from light, at a temperature not exceeding 25 °C, in a tightly sealed container.
Shelf life
5 years
Active ingredient
Glimepiride
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For adults as directed by your doctor
Indications
Type 2 Diabetes
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