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

Excipients: calcium hydrogen phosphate dihydrate 24.4 mg, croscarmellose sodium 3 mg, corn starch 14 mg, mannitol 45 mg, magnesium stearate 0.6 mg, povidone-KZO 2 mg.

Dosage 2 mg

1 tablet contains:

active substance: glimepiride 2 mg;

Excipients: calcium hydrophosphate dihydrate 30 mg, croscarmellose sodium 3.7 mg, corn starch 16 mg, mannitol 55 mg, magnesium stearate 0.8 mg, povidone-KZO 2.5 mg.

Dosage 3 mg

1 tablet contains:

active substance: glimepiride 3 mg;

Excipients: calcium hydrophosphate dihydrate 40.5 mg, croscarmellose sodium 5 mg, corn starch 22.1 mg, mannitol 75 mg, magnesium stearate 1 mg, povidone-KZO 3.4 mg.

Dosage 4 mg

1 tablet contains:

active substance: glimepiride 4 mg;

Excipients: calcium hydrophosphate dihydrate 53.3 mg, croscarmellose sodium 6.7 mg, corn starch 30 mg, mannitol 100 mg, magnesium stearate 1.5 mg, povidone-KZO 4.5 mg.

Description:

Tablets are round, flat-cylindrical, with a facet (dosages of 1 mg and 3 mg); round, planocylindrical, with a facet and a risk (dosages of 2 mg and 4 mg), white or almost white.

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

ATX: & nbsp

A.10.B.B.12 Glimepiride

Pharmacodynamics:

Glimepiride stimulates the secretion and release of insulin from the beta cells of the pancreas (pancreatic action). This effect is based on an increase in the response of the pancreatic beta cells to physiological stimulation with glucose, while the amount of insulin secreted is significantly less than that of other sulfonylureas, thus providing a lower risk of hypoglycemia. Besides, 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 the conversion of arachidonic acid to thromboxane A2, which promotes platelet aggregation, thus providing an antiaggregant effect.

Glimepiride promotes the normalization of lipid content, reduces the concentration of malonic aldehyde in the blood, which leads to a significant decrease in lipid peroxidation, this contributes to the anti-atherogenic effect of the drug. Glimepiride contributes to the reduction of the degree of 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 the blood (Сmах) is achieved after 2.5 hours and is 309 ng / ml. There is a linear relationship between dose and Сmах a also between the dose and the area under the concentration-time curve (AUC). 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. The volume of distribution is 8.8 liters. Communication with proteins - 99%, clearance - 48 ml / min.

Metabolised in the liver. It is excreted mainly in the form of metabolites by the kidneys (60% of the administered dose) and the intestine (40%). Glimepiride is excreted in breast milk and penetrates the placental barrier. Poorly penetrates the blood-brain barrier. The half-life (T1 / 2) is 5-8 hours.

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

Indications:

Diabetes mellitus type 2 with ineffectiveness of diet and exercise (in monotherapy or as part of combination therapy with metformin or insulin).

Contraindications:

diabetes mellitus type 1;
hypersensitivity to glimepiride or other components of the drug, other derivatives of sulfonylureas or sulfonamides;
diabetic ketoacidosis, diabetic precoma and coma, hyperosmolar coma;
severe hepatic and renal failure (including patients on hemodialysis);

leukopenia;
pregnancy, lactation;
children's age till 18 years.

Carefully:

in the first weeks of treatment (increased risk of hypoglycemia);
if there are risk factors for the development of hypoglycemia;
in the presence of conditions requiring a transfer to insulin therapy (extensive burns, severe multiple injuries, extensive surgical interventions);
with violations of absorption of food and drugs in the gastrointestinal tract (GI tract) (including intestinal obstruction, intestinal paresis);
with insufficiency of glucose-6-phosphate dehydrogenase.

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

Dosing and Administration:

At the beginning of treatment, the Glimepiride Canon preparation is administered orally at a dose of 1 mg 1 time per day (immediately before or during a hearty breakfast), if necessary gradually increasing the dose by 1 mg for 1-2 weeks to 2 mg, 3 mg, 4 mg, 6 mg, 8 mg. The maximum recommended daily dose is 6 mg. Doses over 6 mg are effective only in exceptional cases.

It is very important not to skip meals after taking glimepiride.

The admission of the drug can not be eliminated by the subsequent administration of its higher dose leading to hypoglycemia. Tablets are taken whole, not liquid, squeezed with enough water (about 0.5 cup).

Treatment is long, under the control of the glucose in the blood.

Application in combination with metformin

In the case of insufficient stabilization of the concentration of glucose in the blood in patients, host metformin, concomitant therapy with glimepiride may be initiated.

If the dose of metformin remains at the same level, treatment with glimepiride begins with a minimum dose of 1 mg, and then its dose gradually increases depending on the desired concentration of glucose in the blood, up to the maximum daily dose. Combination therapy should be conducted under close medical supervision.

Application in combines with insulin

In cases where it is not possible to achieve normalization of blood glucose concentration by taking the maximum dose of glimepiride in monotherapy or in combination with the maximum dose of metformin, a combination of glimepiride and 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 minimal dose, with a possible subsequent gradual increase in the dose of insulin under the control of the concentration of glucose in the blood.

Combined treatment requires compulsory medical supervision.

Transfer of painient from another oral hypoglycemic preparation to glimepiride

There is no exact correlation between doses of glimepiride and other oral hypoglycemic drugs. When transferring from such drugs to glimepiride the initial daily dose of the latter should be 1 mg (even if the patient is transferred to glimepiride with a maximum dose of another oral hypoglycemic drug). Any increase in the dose of glimepiride should be carried out in stages, taking into account the response to glimepiride in accordance with the above recommendations. It is necessary to take into account the dose used and the duration of the effect of the previous hypoglycemic agent. In some cases, especially when taking hypoglycemic drugs with a long half-life, 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 from insulin to glimepiride

In exceptional cases, when carrying out insulin therapy in patients with type 2 diabetes mellitus, with disease compensation and with the secretory function of beta cells of the pancreas, translation into glimepiride. The translation should be carried out under the close supervision of a physician. In this case, the transfer of the patient to glimepiride begin with a minimum dose of glimepiride in 1 mg.

Side effects:

From the side of metabolism: hypoglycemic reactions may develop. These reactions, mainly occur shortly after taking the drug, can have severe form and course and they can not always be easily stopped. The onset of these symptoms depends on individual factors, such as eating habits and dosing.

From the side of the organ of vision: During treatment (especially at the beginning), transient visual impairments due to changes in glucose concentration in the blood can be observed.

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; 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.

Allergic reactions: possibly the appearance of urticaria, skin rash, itching. Such reactions are, as a rule, moderately expressed, but can progress, accompanied by a decrease in blood pressure, shortness of breath, until the development of anaphylactic shock. When urticaria appears, consult a doctor immediately. Possible cross-allergy to other derivatives of sulfonylureas, sulfonamides and other sulfonamides also may develop allergic vasculitis.

Other: in exceptional cases, the development of headache, asthenia, hyponatremia, photosensitization, late cutaneous porphyria is possible.

Overdose:

When ingesting a large dose of glimepiride, development of hypoglycemia with a duration of 12-72 hours is possible, which can be repeated after the initial restoration of the glucose concentration in the blood.

Treatment: if the patient is conscious - immediate reception of carbohydrates (glucose or a piece of sugar, sweet fruit juice or tea).In most cases, monitoring in a hospital is recommended. When receiving a large amount of the drug showed gastric lavage followed by the introduction of activated carbon (adsorbent) and sodium sulfate (laxative), the introduction of dextrose intravenously struino: 50 ml of 40% solution, then infusion of 10% solution. It is necessary to constantly monitor and maintain vital functions, the concentration of glucose in the blood (at least 5.5 mmol / l) for at least 24-48 hours (possible repeated episodes of hypoglycemia). After the restoration of consciousness, it is necessary to give the patient food rich in easily digestible carbohydrates (in order to avoid the re-development of hypoglycemia). In the future, treatment should be symptomatic.

In the treatment of hypoglycemia, which has developed as a result of the unintentional administration of glimepiride by a thoracic or small child, the dose of dextrose should be carefully controlled in order to avoid dangerous hyperglycemia.

Interaction:

The simultaneous use of glimepiride with certain drugs can cause both an increase and a decrease in the hypoglycemic effect of the drug.Therefore, other medications can be taken only after consultation with the doctor.

The increase in hypoglycemic action and, associated with this, the possible development of hypoglycemia can be observed with the simultaneous use of glimepiride with insulin, metformin or other oral hypoglycemic agents, angiotensin converting enzyme (ACE) inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide , trophosphamide and ifosfamide, fenfluramine, fibrates, fluoxetine, sympatholytics (guanethidine), monoa inhibitors (MAO), miconazole, pentoxifylline (with parenteral administration at high doses), phenylbutazone, azaprope, oxyphenbutazone, probenecid, antimicrobial agents - quinolone derivatives, salicylates (including aminosalicylic acid), sulfinpyrazone, some prolonged-release sulfanilamides, tetracyclines, tritqualin , fluconazole.

The weakening of hypoglycemic action, and associated with it,an increase in the concentration of glucose in the blood can be observed with the simultaneous use of glimepiride with acetazolamide, barbiturates, glucocorticosteroids, diazoxide, saluretic, thiazide diuretics, epinephrine and other sympathomimetic agents, glucagon, laxatives! (with prolonged use), nicotinic acid (in high doses) and nicotinic acid derivatives, estrogens and progestogens, phenothiazine derivatives, including chlorpromazine, phenytoin, rifampicin, thyroid hormones, lithium salts.

The blockers of H2-histamine receptors, clonidine and reserpine are able both to potentiate and weaken the hypoglycemic action of glimepiride.

Under the action of beta-adrenoblockers, clonidine, guanetidine and reserpine, weakening or lack of clinical signs of hypoglycemia is possible. Against the background of taking glimepiride, there may be an increase or decrease in the action of coumarin derivatives.

When used simultaneously with drugs that depress 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 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 that should be taken in case of such errors (for example, skipping a drug or eating a meal) or in situations when it is not possible to take the next dose of the drug at the set time. The patient should immediately inform the doctor if the dose is too high.

The development of hypoglycemia in a patient after taking 1 mg of glimepiride per day means the possibility of controlling glycemia solely with the help of a diet. When you reach the compensation of type 2 diabetes, the sensitivity to insulin increases. In this regard, the treatment process may reduce the need for glimepiride. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or cancel glimepiride. Correction of the dose should also be carried out with a change in the patient's body weight, lifestyle or other factors contributing to an increased risk of hypo- or hyperglycaemia.

In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly careful monitoring of the patient. Factors that contribute to the risk of developing hypoglycemia include:

unwillingness or inability of the patient to cooperate with a doctor (more often observed in elderly patients);
malnutrition, irregular eating or skipping meals;
an imbalance between exercise and carbohydrate intake;
changing diet;
alcohol consumption, especially when combined with meals;
severe renal dysfunction;
an overdose of glimepiride;
some decompensated endocrine disorders that disrupt carbohydrate metabolism or adrenergic counterregulation in response to hypoglycemia (eg, dysfunction of the thyroid gland and anterior pituitary gland, insufficiency of the adrenal cortex);
concomitant use of certain medicines.section "Interaction with other drugs";
reception glimepirida in the absence of indications for its reception.

Symptoms of hypoglycemia can be smoothened or completely absent in the elderly, in patients with autonomic neuropathy or receiving simultaneous treatment with beta-blockers, clonidine, reserpine, guanethidine. 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 not effective in the treatment of hypoglycemia.

Treatment with derivatives of sulfonylurea, which includes glimepiride, can lead to the development of hemolytic anemia, therefore, patients with glucose-6-phosphate dehydrogenase deficiency should be especially careful in the appointment of glimepiride and it is better to use hypoglycemic agents that are not derivatives of sulfonylurea.

During treatment with glimepiride, 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, surgery, infectious diseases accompanied by fever), it may be necessary to temporarily transfer the patient to insulin therapy.

There is no experience with glimepiride 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 glimepiride, 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:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 1 mg, 2 mg, 3 mg, 4 mg.

Packaging:

For 10, 20 or 30 tablets per contour cell pack of film polyvinylchloride and aluminum foil printed lacquered.

According to 1, 3, 6 contour cell packs of 10 tablets or 3, 5 contour packs of cells of 20 tablets or 1,2, 3, 4 contour cell packs of 30 tablets together with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001446

Date of registration:20.01.2012 /17.01.2013

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp26.01.2016

Illustrated instructions

Instructions

Glimepiride Canon (Glimepiride)