Glimepiride-Teva - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 75.40 mg / 150.80 mg / 149.50 mg, corn starch 2.33 mg / 4.66 mg / 4.66 mg, sodium carboxymethyl starch 5.00 mg / 10.00 mg / 10.00 mg, povidone 3.00 mg / 6.00 mg / 7.00 mg, polysorbate 80 0.67 mg / 1.34 mg / 1.34 mg, talc 1.0 mg / 2.0 mg / 2.00 mg, magnesium stearate 0.60 mg / 1.20 mg / 1.20 mg, iron dye oxide yellow (E 172) - / - / 0.30 mg.

Description:

Tablets 1 mg: White, oblong, with bevelled edges of the tablet

Tablets 2 mg: White, oblong, with bevelled edges of a tablet with a fault line on one party

Tablets 3 mg: Light yellow with a brownish tint with a marble surface, oblong, with bevelled edges of a tablet with a fault line on one side.

Pharmacotherapeutic group:Hypoglycemic agent for oral use of the sulfonylurea group of the third generation

ATX: & nbsp

A.10.B.B.12 Glimepiride

Pharmacodynamics:

Glimepiride is a hypoglycemic preparation for oral use - a derivative of sulfonylureas of a new (third) generation.

Glimepiride acts mainly by stimulating the secretion and release of insulin from the beta cells of the pancreas (pancreatic action).As with other sulfonylureas, this effect is based on an increase in the response of beta cells of the pancreas to physiological stimulation with glucose, while the amount of secreted insulin is significantly less than that of traditional sulfonylurea derivatives. The least stimulating effect of glimepiride on the secretion of insulin provides a lower risk of hypoglycemia. In addition to this, glimepiride has an extra-pancreatic action - the ability to improve the sensitivity of peripheral tissues (muscle, fat) to the action of their own insulin, reduce the absorption of insulin by the liver; inhibits the production of glucose in the liver. Glimepiride selectively inhibits cyclooxygenase and reduces conversion of arachidonic acid into thromboxane A2, which promotes platelet aggregation, thus providing an antithrombotic effect.

Glimepiride promotes the normalization of lipid content, reduces the level of small 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, the activity of catalase, glutathione peroxidase and superoxide dismutase, which contributes to the reduction of the oxidative stress in the patient's body, which is constantly present in type 2 diabetes mellitus.

Pharmacokinetics:

With repeated administration of glimepiride in a daily dose of 4 mg, the maximum concentration in serum (C_max) is reached after about 2.5 hours and is 309 ng / ml; there is a linear relationship between dose and C_max, as well as between the dose and AUC (area under the curve "concentration - time"). When administered glimepiride, its bioavailability is 100%. Eating does not have a significant effect on absorption, except for a slight slowing of the absorption rate. For glimepiride characterized by a very low volume of distribution (about 8.8 liters) approximately equal to the albumin distribution volume, a high degree of binding to plasma proteins (99%) and low clearance (about 48 ml / min).

After a single intake of glimepiride dose, 58% are excreted by the kidneys and 35% through the intestine. An unchanged substance in the urine was not detected.The half-life at plasma concentrations of the drug in the serum, corresponding to a multiple dosing regimen, is 5-8 hours. After taking high doses, the elimination half-life increases slightly.

In urine and feces, two inactive metabolites are identified, most likely formed as a result of metabolism in the liver, one of them is a hydroxy derivative, and the other is a carboxy derivative. After ingestion of glimepiride, the terminal half-life of these metabolites is 3-5 hours and 5-6 hours, respectively.

Glimepiride is excreted in breast milk and penetrates the placental barrier. The drug does not penetrate the hemato-encephalic barrier poorly.

In patients with impaired renal function (with low creatinine clearance), there was a tendency to increase the clearance of glimepiride and to reduce its average serum concentrations, which is likely due to a faster elimination of the drug due to its lower binding to the protein. Thus, in this category of patients there is no additional risk of cumulation of the drug.

Indications:

The drug is indicated for the treatment of type 2 diabetes with ineffectiveness of a previously prescribed diet and exercise.

With the ineffectiveness of monotherapy with Glimepiride-Teva, its use in combination therapy with metformin or with insulin is possible.

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 derivatives of sulfonylureas or to sulfonamide preparations (risk of developing hypersensitivity reactions);
severe violations of liver function;
severe violations of kidney function (including patients on hemodialysis);
lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
children's age till 18 years;
insufficiency of glucose-6-phosphate dehydrogenase;
pregnancy and the period of breastfeeding.

Carefully:Conditions requiring the transfer of the patient to insulin therapy (extensive burns, severe multiple injuries, extensive surgical interventions); adrenal insufficiency; Thyroid gland diseases(hypothyroidism, thyrotoxicosis); disturbances in the absorption of food and drugs in the gastrointestinal tract, including intestinal obstruction, intestinal paresis; infectious fever; alcoholism; in the first days of treatment (increased risk of hypoglycemia); at an increased risk of hypoglycemia (see section "Special instructions"); with intercurrent illnesses during treatment or when changing the patient's lifestyle (changing diet and eating time, increasing or decreasing physical activity).

Pregnancy and lactation:

Glimepiride is contraindicated for use in pregnant women. In the case of a planned pregnancy or at the onset of pregnancy, a woman should be transferred to insulin therapy.

As glimepiride, apparently, penetrates into breast milk, it should not be prescribed to women during lactation. In this case, you need to switch to insulin therapy or stop breastfeeding.

Dosing and Administration:

The drug is administered orally. The initial and maintenance doses of Glimepiride-Teva are set individually based on the results of regular monitoring of blood glucose concentrations.

Initial dose and dose selection

At the beginning of treatment, 1 mg Glimepiride-Teva is prescribed once a day. When the optimal therapeutic effect is achieved, it is recommended to take this dose as a supporting dose. In the absence of glycemic control, the daily dose should be incrementally increased by regular monitoring of blood glucose concentrations (at intervals of 1-2 weeks) to 2 mg, 3 mg or 4 mg per day. Doses over 4 per day are effective only in exceptional cases. Maximum recommended daily dose of 6 mg.

Use in combination with metformin

In the absence of glycemic control in patients taking metformin, concomitant therapy with Glimepiride-Teva may be initiated. If the dose of metformin remains at the same level, treatment with Glimepiride-Teva begins with a minimal 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 conducted under close medical supervision.

Use in combination with insulin

In cases where glycemic control can not be achieved by taking the maximum dose of Glimepiride-Teva, in monotherapy or in combination with a maximum dose of metformin,a combination of Glimepiride-Teva and insulin is possible.

In this case, the latter assigned to the patient a dose of glimepiride, Teva remains unchanged. In this case, treatment with insulin begins with a minimal dose, with the possible subsequent gradual increase in its dose under the control of the concentration of glucose in the blood. Combined treatment requires compulsory medical supervision.

The time and frequency of daily intake is determined by the doctor, taking into account the lifestyle of the patient. It is usually sufficient assignment daily dose in one step directly before or during breakfast or dense first main meal. Tablets glimepiride take-Teva whole, not chewed, with a sufficient amount of liquid (about 0.5 cups). It is very important not to skip meals after taking Glimepiride-Teva. Duration of treatment As a rule, treatment with Glimepirid-Teva is long.

Transfer of a patient from another oral hypoglycemic preparation to glimepiride

When transferring the patient with other oral hypoglycemic drug on glimepiride-Teva initial daily dose of the latter should be 1 mg (even if the patient is transferred to glimepiride-Teva with a maximum dose of another oral hypoglycemic drug).Any increase in the dose of Glimepiride-Teva should be carried out in stages in accordance with the above recommendations. 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 (eg, chlorpropamide), there may be a need for a temporary (within a few days) cessation of treatment to avoid an additive effect that increases the risk of developing hypoglycemia.

Transfer of a patient with insulin to Glimepiride-Teva

In exceptional cases, with insulin therapy in patients with type 2 diabetes mellitus, with disease compensation and with the secretory function of beta cells of the pancreas, replacement of insulin with Glimepirid-Teva is possible. The translation should be carried out under the close supervision of a physician. In this case, the patient's transfer to Glimepiride-Teva begins with a minimum dose of 1 mg.

Side effects:

Rarely:

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

From the side of the organs of sight: during treatment (especially at the beginning), a transient decrease in vision due to a change in the concentration of glucose in the blood can be observed.

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

On the part of the hematopoiesis system: thrombocytopenia (from moderate to severe), leukopenia, hemolytic or aplastic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia.

Sometimes:

On the part of the digestive system: nausea, vomiting, a 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 (itching, skin rash). Such reactions are, as a rule, moderately expressed, but can progress, accompanied by a drop in blood pressure, dyspnea, until the development of anaphylactic shock. When symptoms of urticaria appear, consult a doctor immediately. A cross-allergy with other derivatives of sulfonylurea, sulfonamides, or similar substances is possible, and development of allergic vasculitis is also possible.

In exceptional cases:

Other side effects: possibly the development of photosensitization, hyponatremia.

Since some side effects, such as severe hypoglycemia, severe changes in the blood picture, severe allergic reactions, liver failure, can under certain circumstances pose a life threat, if the unwanted or severe reactions develop, the patient should immediately be notified of the treating doctor and do not continue taking the drug without his recommendation.

Overdose:

Symptoms: hypoglycemia (nausea, vomiting and pain in the epigastric region, anxiety, tremor, visual disturbances, impaired coordination, drowsiness, coma and convulsions).

Treatment: if the patient is conscious - induction of vomiting, copious drinking, Activated carbon and laxative. In case of severe overdose, intravenous bolus administration of dextrose solution (50 ml of 40% solution), then - infusion of 10% solution. It is necessary to constantly monitor the patient, maintain vital functions and control the concentration of glucose in the blood (it is possible to repeat episodes of hypoglycemia). Further treatment is symptomatic.

Interaction:

Glimepiride is metabolized fromthe power of cytochrome P450 2C9 (CYP2C9).

When used simultaneously with inducers of the isoenzyme CYP2C9, for example rifampicin, a decrease in the hypoglycemic action of glimepiride and an increased risk of hypoglycemia in the event of their cancellation without correction of the dose of glimepiride. When used simultaneously with inhibitors of the isoenzyme CYP2C9, for example, fluconazole, the hypoglycemic effect of glimepiride may be increased and the risk of hypoglycemia and side effects of glimepiride may increase, and its hypoglycemic action may be reduced when they are withdrawn without correction of the glimepiride dose. The increase in hypoglycemic action 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, derivatives of coumarin, cyclo-, tri- and isophosphamide, fenfluramine, disopyramide, fibrates, fluoxetine,(guanethidine), monoamine oxidase inhibitors (MAO), miconazole, fluconazole, pentoxifylline (with parenteral administration at high doses), phenylbutazone, azapropion, oxyphenbutazone, probenicid, quinolones, salicylates and aminosalicylic acid, sulfinpyrazone, certain long-acting sulfonamides, tetracyclines, tritqualin .

The weakening of hypoglycemic action and the associated increase in the concentration of glucose in the blood can be observed with the 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. The blockers of H2-histamine receptors, clonidine and reserpine how can potentiate or weaken the hypoglycaemic action of glimepiride. Under the influence of sympatholytic agents such as beta-blockers, clonidine, guanethidine and reserpine, possibly weakening or lack of clinical signs of hypoglycemia.

Against the background of taking glimepiride, there may be an increase or decrease in the action of coumarin derivatives.

With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.

A single or chronic use of alcohol can both enhance and weaken the hypoglycemic effect of glimepiride.

Special instructions:

Glimepiride-Teva should be taken at recommended doses and at the appointed time. Errors in the use of the drug, for example, admission, can never be eliminated by the subsequent administration of a higher dose. The doctor and the patient must preliminarily discuss the measures to be taken in case of such mistakes (for example, skipping a drug or eating a meal) or in situations where it is not possible to take the next dose of the drug at the set time. The patient should immediately inform the doctor if too high a dose is taken.

If the patient develops a hypoglycemic reaction with 1 mg of Glimepiride-Teva per day, this indicates that in this patient the normalization of blood glucose level can be achieved with the help of a single diet.

At achievement of indemnification of a diabetes of type 2 sensitivity to an insulin raises. In this regard, the treatment process may reduce the need for Glimepiride-Teva. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or to abolish Glimepiride-Teva. Correction of the dose should also be carried out with a change in the patient's body weight, with a change in his lifestyle or with the appearance of other factors that increase the risk of developing hypo- or hyperglycemia.

Adequate diet, regular and sufficient physical exercise and, if necessary, weight loss are just as important for achieving optimal control of blood glucose levels, as is the regular intake of Glimepiride-Teva.

Clinical symptoms hyperglycemia (insufficient reduction in blood glucose) are: increased frequency of urination, severe thirst, dry mouth and dry skin.

In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly careful monitoring of the patient. Against the backdrop of treatment with glimepiride-Teva with irregular intake of food or skipping meals can develop hypoglycemia. Its possible symptoms are: headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbances, anxiety, aggressiveness, observation of the patient. In the presence of such factors, increasing the risk of violation of 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, superficial breathing, bradycardia. In addition, as a result of the adrenergic feedback mechanism, sweating, anxiety, tachycardia, increased blood pressure, angina and heart rhythm disturbances may occur.

Factors contributing to the development of hypoglycemia include:

reluctance or (especially in old age) the patient's inadequate ability to cooperate with a doctor;
inadequate, irregular meals, skipping meals, starvation, changes in the habitual diet;
an imbalance between exercise and carbohydrate intake;
alcohol consumption, especially when combined with a skipping meal;
impaired renal function;
severe liver dysfunction;
an overdose of Glimepiride-Teva;
Some uncompensated diseases of the endocrine system affecting the carbohydrate metabolism (for example, thyroid dysfunction, pituitary insufficiency or adrenocortical insufficiency);
simultaneous use of drugs that enhance the action of Glimepiride-Teva (see section "Interaction with other drugs").

The doctor should be informed of the above factors and episodes of hypoglycemia, because they require very strict monitoring of the patient. If there are such factors that increase the risk of hypoglycaemia, you should adjust the dose of Glimepiride-Teva or the entire treatment regimen. This must also be done in the case of an intercurrent disease or a change in the patient's lifestyle.

Symptoms of hypoglycemia can be smoothened 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 the immediate intake 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 have at least 20 grams of glucose (4 pieces of sugar). Sugary substitutes are ineffective in the treatment of hypoglycemia.

From experience with other sulfonylureas, it is known that, despite the initial success of stopping hypoglycemia, it is possible to relapse. In this regard, continuous and careful monitoring of the patient is necessary. Severe hypoglycemia requires immediate treatment under the supervision of a doctor, and under certain circumstances and hospitalization of the patient. If a patient suffering from diabetes mellitus is treated by different doctors (for example, during a hospital stay after an accident, during a weekend illness), he must necessarily inform them about his illness and about the previous treatment.

During treatment with Glimepiride-Teva, regular monitoring of liver function and peripheral blood pattern (especially the number of leukocytes and platelets) is required.

In stressful situations (for example, with trauma, surgical intervention, infectious diseases accompanied by fever), there may be a need for a temporary transfer of the patient to insulin therapy. There is no experience of using Glimepirid-Teva in patients with severe impairment of liver and kidney function or patients on hemodialysis. Patients with severe impairment of kidney and liver function are indicated by a transfer to insulin therapy.

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

Effect on the ability to drive transp. cf. and fur:At the beginning of treatment, when switching from one drug to another, or with an irregular intake of Glimepiride-Teva, there may be a decrease in the concentration and speed of the psychomotor reactions of the patient due to hypo- or hyperglycemia. This can adversely affect the ability to drive vehicles or to manage various machines and mechanisms.

Form release / dosage:

Tablets 1 mg, 2 mg, 3 mg.

Packaging:For 10 tablets in a blister of PVC / PVDC / aluminum foil.For 3 or 6 blisters with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005208/08

Date of registration:03.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:Pliva of Hrvatska dooPliva of Hrvatska doo Croatia

Manufacturer: & nbsp

PLIVA HRVATSKA, d.o.o. Croatia

Representation: & nbspPliva of Hvartska dooPliva of Hvartska doo

Information update date: & nbsp30.04.2017

Illustrated instructions

Instructions

Glimepiride-Teva (Glimepiride-Teva)