Glimepiride-Vertex pills 3mg, 30pcs

Composition

One tablet contains: Active ingredient

glimepiride – 3 mg

Auxiliary substances:

lactose (milk sugar),

microcrystalline cellulose,

pregelatinized starch,

sodium lauryl sulfate,

magnesium stearate.

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

The drug is indicated for the treatment of type 2 diabetes mellitus if the previously prescribed diet and physical activity are ineffective.

If Glimepiride monotherapy is ineffective, it can be used in combination therapy with metformin or with insulin.

Contraindications

Type 1 diabetes mellitus; diabetic ketoacidosis, diabetic precoma and coma; hyperosmolar coma; hypersensitivity to glimepiride or to any inactive component of the drug, to other sulfonylureas or to sulfonamide preparations (risk of hypersensitivity reactions); severe liver function disorders; severe renal function disorders (including patients on hemodialysis); lactose intolerance, lactase deficiency, glc-galactose malabsorption; children under 18 years of age; glucose-6-phosphate dehydrogenase deficiency; pregnancy and lactation.

With caution – conditions that require transfer of the patient to insulin therapy (extensive burns, severe multiple trauma, extensive surgical interventions); adrenal insufficiency; thyroid diseases (hypothyroidism, thyrotoxicosis); disorders of absorption of food and medicines in the gastrointestinal tract, including intestinal obstruction, intestinal paresis; infectious fever; alcoholism; in the first days of treatment (increased risk of hypoglycemia); when increased risk of hypoglycemia; intercurrent diseases during treatment or when changing the patient’s lifestyle (changing diet and meal times, increasing or decreasing physical activity).

Side effects

Rarely: From the side of metabolism:  development of hypoglycemic reactions. These reactions mainly occur shortly after taking the drug, and they are not always easily stopped.

From the side of the visual organs:  during treatment (especially at the beginning of treatment), there may be a transient decrease in vision due to changes in the concentration of glucose in the blood.

From the digestive system:  increased activity of liver enzymes, cholestasis, jaundice, hepatitis (up to the development of liver failure).

From the hematopoietic system:  thrombocytopenia (moderate to severe), leukopenia, hemolytic or aplastic anemia, erythrocytopenia, granulocytopenia, agranulocytosis, and pancytopenia.

Sometimes:

From the digestive system:  nausea, vomiting, feeling of heaviness or discomfort in the epigastrium, abdominal pain, diarrhea, very rarely leading to discontinuation of treatment.

Allergic reactions:  the appearance of symptoms of urticaria (pruritus, skin rash). Such reactions are usually moderate, but can progress, accompanied by a drop in blood pressure, dyspnoea, up to the development of anaphylactic shock. If you experience symptoms of urticaria, you should immediately consult a doctor. Cross-allergy with other sulfonylurea derivatives, sulfonamides, or similar substances is possible, and allergic vasculitis may also develop.

In exceptional cases:

Other side effects:  photosensitivity and hyponatremia may develop.

Since certain side effects, such as severe hypoglycemia, serious changes in the blood picture, severe allergic reactions, liver failure, can under certain circumstances be life-threatening, in case of undesirable or severe reactions, the patient should immediately inform the attending physician about them and in no case continue taking the drug without his recommendation.

Interaction

Glimepiride is metabolized by cytochrome P4502C9 (CYP2C9). When used concomitantly with inducers of the CYP2C9 isoenzyme, for example, rifampicin, the hypoglycemic effect of glimepiride may decrease and the risk of hypoglycemia may increase if they are discontinued without dose adjustment of glimepiride.

When used concomitantly with inhibitors of the CYP2C9 isoenzyme, for example, fluconazole, it is possible to increase the hypoglycemic effect of glimepiride and increase the risk of hypoglycemia and side effects of glimepiride, and it is also possible to reduce its hypoglycemic effect if they are discontinued without dose adjustment of glimepiride.

Increased hypoglycemic activity and the associated possible development of hypoglycemia can be observed with the simultaneous use of glimepiride with insulin or other oral hypoglycemic drugs, metformin, angiotensin converting enzyme (ACE) inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclo-, tro – and isophosphamides, fenfluramine dizopyramide, fibrates, fluoxetine, sympatholytics (guanethidine), monoamine oxidase inhibitors (MAO), miconazole, fluconazole, pentoxifylline (with high-dose parenteral use), phenylbutazone, azapropazone, oxyphenbutazone, probenicide, quinolones, salicylates and aminosalicylic acid, sulfinpyrazone, some long-acting sulfonamides, tetracyclines, and tritoqualin. Weakening of the hypoglycemic effect and the associated increase in blood glucose concentration can be observed with simultaneous use of glimepiride with acetazolamide, barbiturates, glucocorticosteroids, glucagon, laxatives (with prolonged use), nicotinic acid (in high doses) and nicotinic acid derivatives, estrogens and progestogens, phenothiazines, chlorpromazine, phenytoin, rifampicin, thyroid hormones, lithium salts. H2-histamine receptor blockers, clonidine and reserpine, can both potentiate and weaken the hypoglycemic effect of glimepiride.

Under the influence of sympatholytic agents such as beta-blockers, clonidine, guanethidine and reserpine, there may be a weakening or absence of clinical signs of hypoglycemia. When taking glimepiride, there may be an increase or decrease in the effect of coumarin derivatives. When used concomitantly with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases. Single or chronic alcohol use may either increase or decrease the hypoglycemic effect of glimepiride.

How to take, course of use and dosage

The drug is used internally. Initial and maintenance doses of Glimepiride-Teva 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 metforminIn 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 glycemic control cannot be achieved by taking the maximum dose of Glimepiride alone 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, 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 treatment

As a rule, treatment with Glimepiride can be prolonged.

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 Glimepiride 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.

Switching patients from insulin to Glimepiride

In exceptional cases, when insulin therapy is performed 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:

hypoglycemia (nausea, vomiting and epigastric pain, restlessness, tremor, visual disturbances, coordination disorders, drowsiness, coma and convulsions).

Treatment:

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.

Special instructions

Glimepiride should be taken at the recommended doses and at the prescribed time. Errors in the use of the drug, such as skipping an appointment, can never be eliminated by taking a higher dose later. The doctor and the patient should discuss in advance the measures that should be taken in case of such errors (for example, skipping a drug or meal) or in situations where it is impossible to take the next dose of the drug at the set time. The patient should immediately inform the doctor in case of taking too high a dose of the drug. If a patient develops a hypoglycemic reaction when taking 1 mg of Glimepiride per day, this indicates that this patient can achieve normalization of blood glucose levels with a single diet.

When compensation for type 2 diabetes is achieved, insulin sensitivity increases. In this regard, the need for Glimepiride may decrease during treatment. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or cancel Glimepiride. Dose adjustment should also be carried out if the patient’s body weight changes, if his lifestyle changes, or if other factors appear that contribute to an increased risk of hypo – or hyperglycemia. An adequate diet, regular and sufficient exercise, and, if necessary, weight loss are just as important for achieving optimal blood glucose control as regular Glimepiride supplementation.

Clinical symptoms of hyperglycemia (insufficient reduction of blood glucose levels) are: increased frequency of urination, severe thirst, dry mouth and dry skin. In the first weeks of treatment, the risk of hypoglycemia may increase, which requires particularly careful monitoring of the patient. During treatment with Glimepiride, hypoglycemia may develop with irregular meals or skipping meals.

Its possible symptoms are: headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disorders, restlessness, aggressiveness, impaired concentration, attention and reaction, depression, confusion, speech and visual disorders, aphasia, tremor, paresis, sensory disturbances, dizziness, delirium, cerebral convulsions, confusion or loss of consciousness, including coma, shallow breathing, bradycardia. In addition, as a result of the adrenergic feedback mechanism, sweating, anxiety, tachycardia, increased blood pressure, angina pectoris and cardiac arrhythmias can occur. Factors contributing to the development of hypoglycemia include::

The doctor should be informed about the above factors and episodes of hypoglycemia, as they require particularly strict monitoring of the patient. In the presence of such factors that increase the risk of hypoglycemia, the dose of Glimepiride or the entire treatment regimen should be adjusted. This should also be done in the event of an intercurrent disease or a change in the patient’s lifestyle.

Symptoms of hypoglycemia may be smoothed out or completely absent in elderly patients, in patients suffering from autonomic neuropathy or receiving simultaneous treatment with beta-blockers, clonidine, reserpine, guanethidine or other sympatholytic agents. Hypoglycemia can almost always be quickly stopped 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). Sweeteners are ineffective in treating hypoglycemia.

From the experience of using other sulfonylureas, it is known that, despite the initial success of stopping hypoglycemia, its recurrence is possible. In this regard, continuous and careful monitoring of the patient is necessary. Severe hypoglycemia requires immediate treatment under the supervision of a doctor, and in certain circumstances, hospitalization of the patient. If a patient suffering from diabetes is treated by different doctors (for example, during a hospital stay after an accident, during a weekend illness), they must inform them about their illness and previous treatment. During treatment with Glimepiride, regular monitoring of liver function and the peripheral blood picture (especially the number of white blood cells and platelets) is required.

In stressful situations (for example, trauma, surgery, infectious diseases accompanied by fever)   it may be necessary to temporarily transfer the patient to insulin therapy.

There is no experience of using Glimepiride in patients with severe hepatic and renal impairment or patients undergoing hemodialysis. Patients with severe renal and hepatic impairment should be switched to insulin therapy.

During treatment with Glimepiride, regular monitoring of blood glucose concentration, as well as the concentration of glycosylated hemoglobin, is necessary.

At the beginning of treatment, when switching from one medication to another, or when taking Glimepiride on an irregular basis, there may be:  decreased concentration of attention and speed of psychomotor reactions of the patient due to hypo – or hyperglycemia. This may negatively affect your ability to drive vehicles or manage various machines and mechanisms.

Storage conditions

At a temperature not exceeding 30°C. Keep out of reach of children.

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