Gliclazide Canon sustained release pills 30mg, 60pcs

Composition

Long-release tablets.

1 tablet contains:

Active ingredient:  

gliclazide 30 mg;

Auxiliary substances:

hypromellose (hydroxypropyl methylcellulose) 50 mg,

silicon dioxide colloid 3.5 mg

mannitol 10 mg,

magnesium stearate 1.8 mg,

vegetable oil hydrogenated 3.6 mg,

microcrystalline cellulose of 81.1 mg.

Pharmacological action of the

hypoglycemic agent for oral use of sulfonylureas II generation

ICD-10:

IV. E10-E14. E11 non-Insulin-dependent diabetes mellitus

ATKH:

A. 10. B. B. 09 Gliclazide

Pharmacodynamics :

Gliclazide is a sulfonylurea derivative, a hypoglycemic drug for oral use, which differs from similar drugs in the presence of an N-containing heterocyclic ring with an endocyclic bond.

Gliclazide reduces the concentration of blood glucose, stimulating the secretion of insulin by 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 its effect on carbohydrate metabolism, gliclazide has hemovascular effects.

Effect on insulin secretion

In type 2 diabetes mellitus, gliclazide restores the early peak of insulin secretion in response to glucose intake and enhances the second phase of insulin secretion. A significant increase in insulin secretion is observed in response to stimulation due to food intake or glucose use.

Hemovascular effects

Gliclazide reduces the risk of small vessel thrombosis by influencing the mechanisms that may cause the development of complications in diabetes mellitus: partial inhibition of platelet aggregation and adhesion and a decrease in the concentration of platelet activation factors (beta-thromboglobulin, thromboxane B2), as well as restoration of fibrinolytic activity of the vascular endothelium and increased activity of the tissue plasminogen activator. Intensive glycemic control based on the use of gliclazide with prolonged release (target glycosylated hemoglobin (HbAlc))

Pharmacokinetics:

Suction

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

Distribution

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

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

Metabolism

Gliclazide is primarily metabolized in the liver. Active metabolites are absent in plasma.

Deduction

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

Special populations

No clinically significant changes in pharmacokinetic parameters are observed in the elderly.

Indications

Type 2 diabetes mellitus with insufficient effectiveness of diet therapy, physical exertion and weight loss.

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

Contraindications

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

– type 1 diabetes mellitus;

– diabetic ketoacidosis, diabetic precoma, diabetic coma;

– severe renal or hepatic insufficiency;

– taking miconazole;

– pregnancy and lactation;

– age up to 18 years.

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

With caution:

Advanced age, irregular and/or unbalanced diet, severe diseases of the cardiovascular system (including coronary heart disease, atherosclerosis), hypothyroidism, adrenal or pituitary insufficiency, hypopituitarism, renal and/or hepatic insufficiency, long-term therapy with glucocorticosteroids (corticosteroids), alcoholism, glucose-6-phosphate dehydrogenase deficiency.

Side effects

Hypoglycemia in the case of irregular food intake, and especially if the meal is missed, can be accompanied by the following symptoms: headache, severe hunger, nausea, vomiting, increased fatigue, sleep disturbance, irritability, agitation, decreased concentration, delayed reaction, depression, confusion, visual and speech disorders, aphasia, tremor, paresis, impaired perception, dizziness, weakness, convulsions, bradycardia, delirium, respiratory disorders, drowsiness, loss of consciousness with the possible development of coma, up to a fatal outcome.

There may also be adrenergic reactions: increased sweating, “sticky” skin, anxiety, tachycardia, increased blood pressure, palpitation, arrhythmia and angina pectoris.

Other side effects

From the gastrointestinal tract:  nausea, vomiting, diarrhea, abdominal pain, constipation (the severity of these symptoms decreases when taken with food).

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

From the circulatory and lymphatic system:  anemia, thrombocytopenia, leukopenia, granulocytopenia. As a rule, these phenomena are reversible in the case of discontinuation of therapy.

Liver and biliary tract disorders:  increased activity of “liver” enzymes (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), alkaline phosphatase), hepatitis (isolated cases). If cholestatic jaundice occurs, therapy should be discontinued.

From the side of the visual organ:  transient visual disturbances may occur due to changes in blood glucose concentrations, especially at the beginning of therapy.

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

Also, against the background of taking other sulfonylurea derivatives, there was an increase in the activity of “liver” enzymes, impaired liver function (for example, with the development of cholestasis and jaundice) and hepatitis. These symptoms decreased over time after discontinuation of sulfonylureas, but in some cases led to life-threatening liver failure.

Interaction

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

Contraindicated combinations

Miconazole (systemic use or application of gel on the oral mucosa):  increases the hypoglycemic effect of gliclazide (hypoglycemia may develop up to coma).

Not recommended combinations

of Phenylbutazone (systemic use) increases the hypoglycemic effect of sulfonylurea derivatives (displaces them from binding to plasma proteins and / or slows down 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 and after taking phenylbutazone. Ethanol:  increases hypoglycemia by inhibiting compensatory reactions, may contribute to the development of hypoglycemic coma. It is necessary to stop taking medications that contain ethanol, and drinking alcohol.

Combinations that require precautions

Taking gliclazide in combination with certain medications, for example, other hypoglycemic agents – insulin, acarbose, biguanides; beta-blockers, dipeptidyl peptidase-4 inhibitors, glucagon-like peptide – 1 receptor agonists, fluconazole; angiotensin-converting enzyme inhibitors-captopril, enalapril; H2-histamine blockers anti-inflammatory drugs; monoamine oxidase inhibitors; sulfonamides, clarithromycin and nonsteroidal anti-inflammatory drugs, accompanied by an increased hypoglycemic effect and a risk of hypoglycemia.

2) Drugs that weaken the effect of gliclazide:

Not recommended combinations

Danazol:  it has a diabetogenic effect. If taking this drug is necessary, the patient is recommended to carefully monitor the concentration of blood glucose. If co-use of drugs is necessary, it is recommended to select the dose of gliclazide both during the use of danazol and after its withdrawal.

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 co-use of drugs is necessary, it is recommended to select the dose of gliclazide both during the use of chlorpromazine and after its withdrawal.

CORTICOSTEROIDS (systemic and local use: intra-articular, external and rectal use): increase the concentration of glucose in the blood with the possible development of ketoacidosis (reduced tolerance to carbohydrates). It is recommended to carefully monitor the blood glucose concentration, especially at the beginning of treatment. If co-use of drugs is necessary, it may be necessary to adjust the dose of the hypoglycemic agent both during the use of corticosteroids and after their withdrawal.

Ritodrin, salbutamol, terbutaline (intravenous):

Beta-2-adrenomimetics help to increase the concentration of blood glucose.

Special attention should be paid to the importance of self-monitoring blood glucose concentrations. If necessary, it is recommended to transfer the patient to insulin therapy.

Combinations that should be taken into account

Anticoagulants (e. g. warfarin): sulfonylurea derivatives may enhance the effect of anticoagulants when taken together. You may need to adjust the dose of the anticoagulant.

How to take, course of use and dosage

The drug is intended for adults only.

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 tablet whole, without chewing or chopping.

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

Initial dose

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

When replacing Gliclazide Canon with another hypoglycemic agent, no transition period of time is required.

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

Dose selection

An increase in the dose is possible no earlier than after 1 month of therapy with the drug at the previously prescribed dose. Dose selection should be carried out in accordance with the indicator of blood glucose concentration after the start of treatment. Each subsequent dose change may be made after at least a two-week period.

Maintenance therapy

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

Elderly patients

Recommended doses of the drug for the elderly are identical to those for adults under 65 years of age.

Kidney failure

The recommended doses of the drug for mild to moderate renal insufficiency are identical to those for people with normal renal function. Careful medical monitoring of patients is recommended.

Patients at risk of hypoglycemia

In patients at risk of developing hypoglycemia (insufficient or unbalanced nutrition; severe or poorly compensated endocrine disorders – pituitary and adrenal insufficiency, hypothyroidism; withdrawal of CORTICOSTEROIDS after prolonged use and/or high doses; severe diseases of the cardiovascular system (severe coronary heart disease, severe carotid artery atherosclerosis, advanced atherosclerosis), it is recommended to use a 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 until the target HbAlc level is reached. You should be aware of the risk of hypoglycemia. In addition, other hypoglycemic medications can be added to therapy, such as metformin, an alpha-glucosidase inhibitor, a thiazolidinedione derivative, or insulin.

Overdose

Overdose of sulfonylurea derivatives, including gliclazide, can lead to the development of hypoglycemia, up to hypoglycemic coma. Moderate symptoms of hypoglycemia without impaired consciousness or neurological symptoms are corrected by taking carbohydrates, selecting the dose, and / or changing the diet. Careful monitoring of the patient’s condition should continue until it is certain that the patient’s health is not in danger.

It is possible to develop severe hypoglycemic conditions, accompanied by coma, convulsions or other neurological disorders. If such symptoms occur, it is necessary to provide emergency medical care and immediate hospitalization. If hypoglycemic coma is suspected or diagnosed, the patient is given 50 ml of 40% dextrose (glucose) solution intravenously. Then intravenously drip 5% dextrose solution to maintain the required blood glucose concentration of about 1 g/l. Careful monitoring of blood glucose concentrations and monitoring of the patient should be carried out for at least 48 consecutive hours. Later, depending on the patient’s condition, the question of the need for further monitoring of the patient’s vital functions should be decided.

Dialysis is ineffective due to the pronounced binding of gliclazide to plasma proteins.

Special instructions

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

The drug Gliclazide Canon can only be prescribed to those patients who eat regularly and include breakfast. It is very important to maintain an adequate intake of carbohydrates with food, as the risk of hypoglycemia increases with irregular or insufficient nutrition, as well as with the consumption of food that is poor in carbohydrates. Hypoglycemia is more likely to occur with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol, or when taking several hypoglycemic medications at the same time.

As a rule, the symptoms of hypoglycemia disappear after eating a meal rich in carbohydrates (for example, sugar). It should be borne in mind that taking sweeteners does not help eliminate hypoglycemic symptoms.

Experience with other sulfonylurea derivatives suggests that hypoglycemia may recur despite effective initial management of the condition.

If the hypoglycemic symptoms are pronounced or are prolonged, even in the case of temporary improvement in the condition after eating a meal rich in carbohydrates, it is necessary to provide emergency medical care, up to hospitalization.

To avoid the development of hypoglycemia, careful individual selection of medications and dosage regimens is necessary, 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 doctor’s instructions and monitor their condition:

– insufficient and irregular nutrition, skipping meals, fasting and changing the diet;

– an imbalance between physical activity and the amount of carbohydrates taken;

– kidney failure:

– severe liver failure;

– overdose of the drug Gliclazide Canon;

– some endocrine disorders (diseases of the thyroid gland, pituitary and adrenal insufficiency);

– simultaneous use of certain medications.

Sulfonylurea derivatives may cause hemolytic anemia in patients with glucose-6-phosphate dehydrogenase deficiency. Since gliclazide is a sulfonylurea derivative, caution should be exercised when prescribing it to patients with glucose-6-phosphate dehydrogenase deficiency. The possibility of prescribing a hypoglycemic drug of a different group should be evaluated.

Hepatic / renal insufficiency

In patients with severe hepatic and/or renal insufficiency, the pharmacokinetic and/or pharmacodynamic properties of gliclazide may change. Hypoglycemia developing in these patients may be quite prolonged, in such cases, it is necessary to immediately conduct appropriate therapy.

Patient Information

The patient and their family members should be informed about the risk of hypoglycemia, its symptoms, and conditions that contribute to its development. The patient should be informed about the potential risks and benefits of the proposed treatment. The patient should be made aware of the importance of diet, the need for regular exercise, and regular monitoring of blood glucose levels.

Insufficient glycemic control

Glycemic control in patients receiving hypoglycemic therapy may be weakened in the following cases: fever, injuries, infectious diseases, or major surgical interventions. In these conditions, it may be necessary to stop therapy with Gliclazide Canon and prescribe insulin therapy. In many patients, the effectiveness of oral hypoglycemic agents, including:gliclazide, tends to decrease after a prolonged period of treatment. This effect may be due to both the progression of the disease and a decrease in the therapeutic response to the drug. This phenomenon is known as secondary drug resistance, which must be distinguished from the primary one, in which the drug does not give the expected clinical effect even at the first appointment. Before a patient is diagnosed with secondary drug resistance, it is necessary to assess the adequacy of dose selection and compliance with the prescribed diet.

Monitoring of laboratory parameters

Regular measurement of fasting blood glucose and glycosylated hemoglobin is recommended to assess glycemic control.

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

Influence on the ability to drive vehicles and mechanisms:

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

Form of production

Tablets are round, biconvex (dosage 30 mg); tablets are round, biconvex with a risk (dosage 60 mg), white or almost white in color. Minor marbling is allowed.

Active ingredient

Gliclazide

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

For adults as directed by your doctor

Indications

Type 2 Diabetes