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

Excipients: hypromellose (hydroxypropylmethylcellulose) 50 mg, silicon dioxide colloid 3,5 mg, mannitol 10 mg, magnesium stearate 1.8 mg, vegetable oil hydrogenated 3.6 mg, microcrystalline cellulose 81.1 mg.

Dosage of 60 mg

1 tablet contains:

Active substance: gliclazide 60 mg;

Excipients: hypromellose (hydroxypropylmethyl cellulose) 100 mg Colloidal silicon dioxide 7 mg, 80 mg mannitol, 3.6 mg of magnesium stearate, hydrogenated vegetable oil 7.2 mg Microcrystalline cellulose 102.2 mg.

Description:

Tablets are round, biconvex (dosage of 30 mg); tablets are round, biconvex with a risk (dosage of 60 mg), white or almost white. Allowed a slight marbling.

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

ATX: & nbsp

A.10.B.B.09 Gliclazide

Pharmacodynamics:

Gliklazid is a derivative of sulfonylurea, a hypoglycemic preparation for ingestion, which differs from similar drugs in the presence N-containing heterocyclic ring with an endocyclic bond.

Gliklazid reduces the concentration of blood glucose, stimulating the secretion of insulin beta cells of the islets of Langerhans. An increase in the concentration of postirandial insulin and C-peptide persists after 2 years of therapy. In addition to the effect on carbohydrate metabolism glycazide has hemovascular effects.

Influence on secretion of insulin

In type 2 diabetes mellitus glycazide restores the early peak of insulin secretion in response to the intake of glucose and enhances the second phase of insulin secretion. A significant increase in insulin secretion is observed in response to stimulation caused by food intake or the introduction of glucose.

Hemovascular effects

Gliklazid reduces the risk of thrombosis of small vessels, affecting the mechanisms that can cause complications in diabetes mellitus: partial inhibition of platelet aggregation and adhesion and a decrease in the concentration of platelet activating factors (beta-thromboglobulin, thromboxane B₂), as well as to restore the fibrinolytic activity of the vascular endothelium and increase the activity of the tissue activator of plasminogen. Intensive glycemic control based on the use of glyclazide with prolonged release (target of glycosylated hemoglobin (HbAlc) <6.5%) significantly reduces the risk of micro- and macrovascular complications of diabetes mellitus 2 type, in comparison with standard glycemic control (study ADVANCE).

Pharmacokinetics:

Suction

After oral administration glycazide completely absorbed. Eating does not affect the degree of absorption. The concentration of gliclazide in the plasma increases gradually, reaching a maximum and reaching the plateau after 6-12 hours. Individual variability is relatively low. The relationship between the dose taken and the concentration curve of the drug in the plasma is a linear time dependence.

Distribution

About 95% of the drug binds to plasma proteins. Gliclazide is metabolized primarily in the liver and is excreted mainly by the kidneys. The volume of distribution is about 30 liters.

Taking the drug at a dose of 30 mg once a day ensures maintenance of an effective concentration of gliclazide in the blood plasma for more than 24 hours.

Metabolism

Gliklazid is metabolized primarily in the liver. There are no active metabolites in the plasma.

Excretion

Excretion is carried out mainly by the kidneys in the form of metabolites, less than 1% is excreted unchanged. The half-life of gliclazide averages 16 hours (12 to 20).

Special Populations

In elderly people, clinically significant changes in pharmacokinetic parameters are not observed.

Indications:

Diabetes mellitus type 2 with insufficient effectiveness of diet therapy, exercise and weight loss.

Prevention of complications of diabetes: risk reduction microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke) in patients with type 2 diabetes by intensive glycemic control.

Contraindications:

- Hypersensitivity to gliclazide or any of the excipients of the drug, other derivatives of sulfonylureas, sulfonamides;

- type 1 diabetes mellitus;

- Diabetic ketoacidosis, diabetic precoma, diabetic coma;

- severe renal or hepatic insufficiency;

- miconazole;

- pregnancy and the period of breastfeeding;

- age to 18 years.

It is not recommended to use the drug simultaneously in combination with phenylbutazone or dibazol.

Carefully:

Elderly age, irregular and / or unbalanced nutrition, severe cardiovascular diseases (incl.ischemic heart disease, atherosclerosis), hypothyroidism, adrenal or pituitary insufficiency, hypopituitarism, renal and / or hepatic insufficiency, long-term glucocorticosteroid therapy (GCS), alcoholism, insufficiency of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:

Experience with glycazide during pregnancy is absent.

Data on the use of other derivatives of sulfonylurea during pregnancy are limited.

In studies on laboratory animals teratogenic effects of glycazide were not revealed.

Oral hypoglycemic drugs during pregnancy are not applied.

The drug of choice for the treatment of diabetes in pregnant women is insulin. It is recommended to replace gliclazide with insulin therapy, as in the case of a planned pregnancy, and if the pregnancy occurred against the background of taking the drug.

Breastfeeding period

Taking into account the lack of data on the intake of glycazide in breast milk and the risk of developing neonatal hypoglycemia, it is contraindicated during therapy with the drug.

Dosing and Administration:

The drug is intended only for adults.

The recommended dose of the drug should be taken orally, 1 time / day, preferably during breakfast.

The daily dose is 30-120 mg (1-4 tablets) in 1 dose. It is recommended to swallow the whole tablet without chewing or grinding.

If you skip one or more doses of the drug, you can not take a higher dose to the next dose, the missed dose should be taken the next day. As with other hypoglycemic drugs, the dose of the drug in each case must be selected individually, depending on the concentration of blood glucose and glycosylated hemoglobin (HbAlc).

Initial dose

The initial recommended dose in adults who had not previously received treatment (including elderly people ≥65 years) is 30 mg / day (1 tablet), then the dose is selected individually until the desired result is achieved.

When replacing the drug with Gliclazide, the canon of another hypoglycemic agent does not require any transitional period of time.

You must first stop taking this drug and only then take the drug Gliklazid Canon.

Dose selection

Increase in the dose is possible not earlier than after 1 month of therapy with the drug in the previously prescribed dose. The dose should be selected in accordance with the blood glucose concentration index after the start of treatment. Each subsequent dose change can be undertaken after at least a two-week period.

Supportive therapy

The maintenance daily dose is from 30 to 90-120 mg (from 1 to 3-4 tablets), and should not exceed 120 mg. Gliclazide The canon can be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.

Elderly patients

Recommended dosage for elderly people is identical to that for adults up to 65 years of age.

Renal insufficiency

The recommended doses of the drug for renal failure of mild to moderate severity are identical to those for persons with normal renal function. It is recommended that careful medical supervision of patients is carried out.

Patients at risk of developing hypoglycemia

In patients who are at risk for developing hypoglycemia (inadequate or unbalanced nutrition, severe or poorly compensated endocrine disorders - pituitary and adrenal insufficiency,hypothyroidism; abolition of SCS after their long reception and / or intake in high doses; severe diseases of the cardiovascular system (severe ischemic heart disease, severe carotid artery atherosclerosis, widespread atherosclerosis) it is recommended to apply the minimum dose (30 mg) of the drug.

Prevention of complications of diabetes mellitus

To achieve intensive glycemic control, you can gradually increase the dose of Gliclazide Canon 120 mg / day in addition to diet and exercise before reaching the target level HbAlc. It should be remembered about the risk of developing hypoglycemia. In addition, other hypoglycemic drugs may be added to therapy, for example, metformin, an alpha-glucosidase inhibitor, a thiazolidinedione derivative or insulin.

Side effects:

Hypoglycemia in case of irregular intake of food and especially if the meal is missed may be accompanied by the following symptoms: headache, severe hunger, nausea, vomiting, fatigue, sleep disturbance, irritability, agitation, decreased concentration of attention, delayed reaction, depression, confusion consciousness,impaired vision and speech, aphasia, tremor, paresis, impaired perception, dizziness, weakness, convulsions, bradycardia, delirium, impaired breathing, drowsiness, loss of consciousness with the possible development of coma, or death.

Also can be marked adrenergic reactions: sweating, "sticky" skin, anxiety, tachycardia, hypertension, palpitations, arrhythmia, and angina pectoris.

Other side effects

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, constipation (the severity of these symptoms decreases with admission during meals).

From the skin and subcutaneous tissue: rash, pruritus, urticaria, erythema, maculopapular rash, bullous reactions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis).

From the side of the circulatory and lymphatic system: but notmia, thrombocytopenia, leukopenia, granulocytopenia. As a rule, these phenomena are reversible in the event of discontinuation of therapy.

From the liver and biliary tract: increased activity of "hepatic" enzymes (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), alkaline phosphatase), hepatitis (isolated cases). When cholestatic jaundice occurs, therapy should be discontinued.

From the side of the organ of vision: there may be transient visual impairment caused by changes in blood glucose concentration, especially at the beginning of therapy.

Common side effects of sulfonylurea derivatives: erythropenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia.

Also on the background of taking other sulfonylureas, there was an increase in the activity of "liver" enzymes, a violation of liver function (for example, with the development of cholestasis and jaundice) and hepatitis. These manifestations decreased with time after the withdrawal of sulfonylureas, but in some cases led to life-threatening liver failure.

Overdose:

Overdose of sulfonylurea derivatives, including glycazide, can lead to the development of hypoglycemia, down to hypoglycemic coma. Moderate symptoms of hypoglycemia without disturbance of consciousness or neurologic symptoms are corrected by taking carbohydrates, choosing a dose and / or changing the diet. Careful observation of the patient's condition should continue until there is no certainty that the patient's health is not threatened.

Possible development of severe hypoglycemic conditions, accompanied by coma, seizures or other neurological disorders. If such symptoms appear, emergency medical care and immediate hospitalization are necessary. If suspected or diagnosis of hypoglycemic coma, the patient intravenously struino inject 50 ml 40% solution of dextrose (glucose). Then, 5% dextrose solution is dripped intravenously to maintain the necessary blood glucose concentration of about 1 g / l. Careful monitoring of blood glucose concentrations and patient monitoring should be done for at least 48 consecutive hours. Later, depending on the patient's condition, it is necessary to decide the need for further monitoring of the patient's vital functions.

Dialysis is ineffective due to the expressed binding of glycazide to plasma proteins.

Interaction:

1) Drugs that enhance the effect of glycazide (increased risk of hypoglycemia):

Contraindications

Miconazole (systemic administration or use of the gel on the oral mucosa): enhances the hypoglycemic effect of glycazide (hypoglycemia may develop up to the state of coma).

Unrecommended combinations

Phenylbutazone (systemic administration) enhances the hypoglycemic effect of derivatives of sulfonylureas (displaces them from the bond with plasma proteins and / or slows their elimination from the body). It is preferable to use another anti-inflammatory drug. If taking phenylbutazone is necessary, the patient should be warned about the need to monitor blood glucose concentrations. If necessary, the dose of gliclazide should be adjusted during the administration of phenylbutazone and after its termination. Ethanol: increases hypoglycemia, inhibiting compensatory reactions, can contribute to the development of hypoglycemic coma. It is necessary to refuse to take medications, which include ethanol, and the use of alcohol.

Combinations, requiring precautions

Admission gliclazide in combination with certain medicines, for example, other hypoglycemic agents - insulin, acarbose, biguanides; beta-adrenoblockers, inhibitors of dipeptidyl peptidase-4, glucagon-like peptide-1 receptor agonists, fluconazole; inhibitors of the angiotensin-converting enzyme - captopril, enalapril; blockers H₂-gistaminovyh receptors; monoamine oxidase inhibitors; sulfonamides, clarithromycin and non-steroidal anti-inflammatory drugs, is accompanied by increased hypoglycemic effect and risk of hypoglycemia.

2) drugs that reduce the effect of gliclazide:

Unrecommended combinations

Danazol: has a diabetic effect. If the drug is needed, the patient should carefully monitor the blood glucose concentration. If it is necessary to jointly take medications, it is recommended that the dose of gliclazide be selected both during and after danazol administration.

Combinations, requiring precautions

Chlorpromazine: in high doses (more than 100 mg per day) increases the concentration of glucose in the blood, reducing the secretion of insulin. It is recommended to carefully monitor the concentration of blood glucose. If it is necessary to take joint medications, it is recommended that the dose of gliclazide be selected both during the intake of chlorpromazine and after its withdrawal.

GCS (systemic and topical application: intraarticular, external and rectal administration): increase the concentration of glucose in the blood with possible development of ketoacidosis (decrease in tolerance to carbohydrates). It is recommended that blood glucose concentration be carefully monitored, especially at the beginning of treatment. If it is necessary to take medications together, it may be necessary to correct the dose of the hypoglycemic agent both during the administration of the GCS and after their withdrawal.

Ritodrine, salbutamol, terbutaline (intravenous administration):

Beta-2-adrenomimetics contribute to increased blood glucose concentrations.

It is necessary to pay special attention to the importance of self-monitoring of blood glucose concentration. If necessary, it is recommended to transfer the patient to insulin therapy.

Combinations that need to be taken into account

Anticoagulants (for example, warfarin): derivatives of sulfonylureas can enhance the effect of anticoagulants when taken together. You may need to adjust the dose of anticoagulant.

Special instructions:

When taking sulfonylurea derivatives, including glycazide, hypoglycemia may develop, and in some cases - in severe and prolonged form, requiring hospitalization and intravenous administration of a dextrose solution for several days.

The drug Gliclazide canon can be prescribed only to those patients, whose meals are regular and include breakfast. It is very important to maintain sufficient intake of carbohydrates with food, because The risk of developing hypoglycemia increases with irregular or inadequate nutrition, as well as when consuming food poor in carbohydrates. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol or taking several hypoglycemic drugs at the same time.

Typically, the symptoms of hypoglycemia go away after eating a meal rich in carbohydrates (such as sugar). It should be borne in mind that the use of sugar substitutes does not help to eliminate hypoglycemic symptoms.

The experience of using other sulfonylurea derivatives suggests that hypoglycemia can recur despite effective initial arrest of this condition.

In the event that hypoglycemic symptoms have a pronounced character or are prolonged, even in the case of temporary improvement after a meal rich in carbohydrates, it is necessary to provide emergency medical care, up to hospitalization.

In order to avoid the development of hypoglycemia, careful individual selection of drugs and dosing regimens is required, as well as providing the patient with complete information about the proposed treatment.

An increased risk of hypoglycemia may occur in the following cases:

- refusal or inability of the patient (especially the elderly) to follow the prescriptions of the doctor and monitor their condition:

- insufficient and irregular meals, skipping meals, fasting and changing diets;

- an imbalance between exercise and the amount of carbohydrates taken;

- kidney failure:

- severe hepatic impairment;

- an overdose of the drug Gliklazid Kanon;

- Some endocrine disorders (thyroid gland diseases, pituitary and adrenal insufficiency);

- simultaneous reception of certain medicines.

Derivatives of sulfonylureas can cause hemolytic anemia in patients with glucose-6phosphate dehydrogenase. Because the glycazide is a derivative of sulfonylureas, caution should be exercised when it is administered to patients with glucose-6phosphate dehydrogenase.One should evaluate the possibility of prescribing a hypoglycemic drug of another group.

Hepatic / Renal Failure

In patients with hepatic and / or renal insufficiency, severe changes in the pharmacokinetic and / or pharmacodynamic properties of gliclazide. Hypoglycemia developing in these patients can be quite long, in such cases immediate therapy is necessary.

Information for patients

It is necessary to inform the patient and his family about the risk of developing hypoglycemia, its symptoms and conditions that contribute to its development. The patient should be informed of the potential risks and benefits of the proposed treatment. The patient needs to clarify the importance of dieting, the need for regular exercise and regular monitoring of blood glucose concentrations.

Insufficient glycemic control

Glycemic control in patients receiving therapy with hypoglycemic agents may be weakened in the following cases: fever, trauma, infectious diseases or large surgical interventions.With these conditions, it may be necessary to discontinue therapy with Gliclazide Canon and prescribe insulin therapy. In many patients, the effectiveness of oral hypoglycemic agents, incl. glyclazide, tends to decline after a long treatment period. This effect can be due to both the progression of the disease and the decrease in the therapeutic response to the drug. This phenomenon is known as secondary drug resistance, which must be distinguished from the primary, in which the drug already at the first appointment does not give the expected clinical effect. Before diagnosing the patient for secondary drug resistance, it is necessary to assess the adequacy of dose selection and adherence to the prescribed diet.

Control of laboratory indicators

For evaluation of glycemic control, regular determination of fasting blood glucose and glycosylated hemoglobin is recommended.

In addition, it is advisable to regularly conduct self-monitoring of concentration blood glucose.

Effect on the ability to drive transp. cf. and fur:

Patients should be aware of the symptoms of hypoglycemia and take care when driving vehicles or performing work that requires a high rate of psychomotor reactions, especially at the beginning of therapy.

Form release / dosage:

Tablets with prolonged release, 30 mg and 60 mg.

Packaging:

Dosage of 30 mg: on 10 or 30 tablets in a contour cellular package from a film of polyvinylchloride and a foil of aluminum printed varnished. According to 3, 6 contour cell packs of 10 tablets or 1.2 contour packs of 30 tablets with instructions for use are placed in a pack of cardboard.

Dosage of 60 mg: on 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered. According to 3, 6 contour cell packs of 10 tablets or 2, 4 contour cell packs of 15 tablets with instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C, in the manufacturer's packaging.

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-003964

Date of registration:15.11.2016

Expiration Date:15.11.2021

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: & nbsp29.04.2017

Illustrated instructions

Instructions

Gliclazide Canon (Gliclazide Canon)