Diabefarm^® MR (Tablets) Instructions for Use

ATC Code

A10BB09 (Gliclazide)

Active Substance

Gliclazide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Oral hypoglycemic drug

Pharmacotherapeutic Group

Drugs for the treatment of diabetes mellitus; hypoglycemic drugs, except insulins; sulfonylurea derivatives

Pharmacological Action

An oral hypoglycemic agent, a second-generation sulfonylurea derivative. It stimulates insulin secretion by pancreatic beta-cells. It increases the sensitivity of peripheral tissues to insulin. It apparently stimulates 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 blood concentration of total cholesterol and LDL cholesterol, 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, a significant reduction in proteinuria is noted with long-term use of gliclazide.

Pharmacokinetics

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

When used in a 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 affects 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: reduction of the risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke).

ICD codes

Dosage Regimen

Take Diabefarm^® MR tablets orally. Swallow the tablet whole with a glass of water; do not crush, chew, or break the tablet.

The initial daily dose is 30 mg once daily. Take the tablet with breakfast.

For most patients, the maintenance dose is between 60 mg and 120 mg once daily. The maximum recommended daily dose is 120 mg.

Individualize the dosage based on glycemic control, as measured by fasting blood glucose and HbA1c levels. Titrate the dose in increments of 30 mg every 2-4 weeks until adequate control is achieved.

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

If a dose is missed, take it as soon as remembered on the same day. Do not double the dose the next day to make up for a missed dose.

Regularly monitor blood glucose and HbA1c to assess therapeutic response and adjust the dosage regimen accordingly.

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 failure; pregnancy, breastfeeding period; children and adolescents under 18 years of age; hypersensitivity to sulfonylurea derivatives and sulfonamides. Simultaneous 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 failure.

Use in Renal Impairment

Contraindicated for use in severe renal failure.

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, if 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.

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

Drug Interactions

The hypoglycemic effect of gliclazide is potentiated when used concomitantly with pyrazolone derivatives, salicylates, phenylbutazone, antibacterial sulfonamide drugs, theophylline, caffeine, MAO inhibitors.

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

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

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

When used concomitantly with corticosteroids (including topical dosage forms), diuretics, barbiturates, estrogens, progestins, combined estrogen-progestin drugs, diphenin, 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.