Gliclada^® (Tablets) Instructions for Use

ATC Code

A10BB09 (Gliclazide)

Active Substance

Gliclazide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Oral hypoglycemic drug

Pharmacotherapeutic Group

Hypoglycemic agent for oral administration of the second-generation sulfonylurea group

Pharmacological Action

An oral hypoglycemic agent, a second-generation sulfonylurea derivative. It stimulates insulin secretion by the beta-cells of the pancreas. It increases the sensitivity of peripheral tissues to insulin. It appears to stimulate the activity of intracellular enzymes (in particular, muscle glycogen synthase). It reduces the time interval from food intake to the onset of insulin secretion. It restores the early peak of insulin secretion and reduces the postprandial peak of hyperglycemia.

Gliclazide reduces platelet adhesion and aggregation, slows the development of parietal thrombosis, and increases vascular fibrinolytic activity. It normalizes vascular permeability. It has anti-atherogenic properties: it lowers the concentration of total cholesterol and LDL cholesterol in the blood, increases the concentration of HDL cholesterol, and also reduces the number of free radicals. It prevents the development of microthrombosis and atherosclerosis. It improves microcirculation. It reduces vascular sensitivity to adrenaline.

In diabetic nephropathy, long-term use of gliclazide results in a significant reduction in proteinuria.

Pharmacokinetics

After oral administration, it is completely absorbed from the gastrointestinal tract.

When using the prolonged/modified-release dosage form, C_max in the blood is reached within 6 hours; C_ss is maintained for 6-12 hours.

Plasma protein binding is about 95%. V_d is about 19 L. It is metabolized mainly in the liver with the formation of 8 metabolites. The main metabolite does not have a hypoglycemic effect but does affect microcirculation.

T_1/2 ranges from 12 to 20 hours. It is excreted mainly by the kidneys: 70% as metabolites, less than 1% is excreted unchanged in the urine.

Indications

Type 2 diabetes mellitus with insufficient effectiveness of diet therapy, physical exercise, and body weight reduction.

Prevention of complications of type 2 diabetes mellitus: reducing the risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke).

ICD codes

Dosage Regimen

Take the recommended daily dose once daily, preferably with breakfast. Swallow the tablet whole; do not crush or chew.

The initial dose is typically 30 mg once daily. Titrate the dose based on glycemic control and tolerability.

Increase the dose in increments of 30 mg no more frequently than every two weeks. The usual maintenance dose ranges from 60 mg to 120 mg daily.

The maximum daily dose is 120 mg. Do not exceed this dose.

For patients switching from another sulfonylurea, initiate Gliclada at 30 mg daily. Discontinue the previous agent to avoid overdose.

In elderly patients or those with renal or hepatic impairment, initiate therapy at the lowest possible dose of 30 mg. Monitor blood glucose closely during dose titration.

Regularly monitor fasting blood glucose and postprandial glucose levels. Assess glycated hemoglobin (HbA1c) periodically to evaluate long-term glycemic control.

If a dose is missed, take it with the next meal. If it is almost time for the next dose, skip the missed dose. Do not double the dose to make up for a forgotten one.

Adjust the dosage regimen during concomitant illness or major surgery; temporary insulin therapy may be required.

Adverse Reactions

From the digestive system rarely – anorexia, nausea, vomiting, diarrhea, epigastric pain.

From the hematopoietic system in some cases – thrombocytopenia, agranulocytosis or leukopenia, anemia (usually reversible).

From the endocrine system in case of overdose – hypoglycemia.

Allergic reactions skin rash, itching.

Contraindications

Type 1 diabetes mellitus (insulin-dependent), ketoacidosis, diabetic precoma and coma, severe renal and/or hepatic insufficiency; pregnancy, breastfeeding period; children and adolescents under 18 years of age; hypersensitivity to sulfonylurea derivatives and sulfonamides. Concurrent use of gliclazide and imidazole derivatives (including miconazole).

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindicated for use in severe hepatic insufficiency.

Use in Renal Impairment

Contraindicated for use in severe renal insufficiency.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Gliclazide is used to treat non-insulin-dependent diabetes mellitus in combination with a low-calorie, low-carbohydrate diet.

During treatment, blood glucose levels should be regularly monitored on an empty stomach and after meals, as well as daily fluctuations in glucose levels.

In case of surgical interventions or decompensation of diabetes mellitus, the possibility of using insulin preparations should be considered.

If hypoglycemia develops and the patient is conscious, glucose (or a sugar solution) should be administered orally. In case of loss of consciousness, glucose should be administered intravenously or glucagon subcutaneously, intramuscularly, or intravenously. After regaining consciousness, the patient should be given food rich in carbohydrates to prevent the recurrence of hypoglycemia.

With the simultaneous use of gliclazide and verapamil, regular monitoring of blood glucose levels is necessary; with acarbose, careful monitoring and adjustment of the dosage regimen of hypoglycemic agents is required.

Concomitant use of gliclazide with cimetidine, phenylbutazone, danazol is not recommended.

Drug Interactions

The hypoglycemic effect of gliclazide is potentiated by concurrent use with pyrazolone derivatives, salicylates, phenylbutazone, antibacterial sulfonamide drugs, theophylline, caffeine, MAO inhibitors.

Concurrent use with non-selective beta-blockers increases the likelihood of hypoglycemia and may also mask the tachycardia and hand tremors characteristic of hypoglycemia, while sweating may increase.

When gliclazide and acarbose are used together, an additive hypoglycemic effect is observed.

Cimetidine increases the plasma concentration of gliclazide, which can cause severe hypoglycemia (CNS depression, impaired consciousness).

When used concurrently with corticosteroids (including topical formulations), diuretics, barbiturates, estrogens, progestins, combined estrogen-progestin drugs, diphenyl, rifampicin, the hypoglycemic effect of gliclazide is reduced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.