Glucostabil (Tablets) Instructions for Use

Marketing Authorization Holder

Gedeon Richter-Rus, JSC (Russia)

ATC Code

A10BB09 (Gliclazide)

Active Substance

Gliclazide (Rec.INN WHO registered)

Dosage Form

Glucostabil

Tablets 80 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, flat-cylindrical in shape, with a bevel and a score on one side.

Excipients: colloidal silicon dioxide, lactose monohydrate, povidone, glycerol dibehenate, magnesium stearate.

15 pcs. – blister packs (2) – cardboard cartons.
15 pcs. – blister packs (4) – cardboard cartons.

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 pancreatic beta-cells. 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 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, long-term use of gliclazide results in a significant reduction in proteinuria.

Pharmacokinetics

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

C_max in blood is achieved within 2 to 6 hours; C_ss is achieved after 2 days.

Plasma protein binding is about 95%. V_d is about 19 L. It is metabolized mainly in the liver to form 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 primarily 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

Start with an initial daily dose of 80 mg, typically administered as a single 80 mg tablet.

Take tablets twice daily, before the morning and evening meals.

Adjust the dose based on individual glycemic response, clinical condition, and tolerability.

The average daily maintenance dose ranges from 160 mg to 320 mg.

Do not exceed a maximum daily dose of 320 mg.

For doses requiring 160 mg or more per day, divide the total dose into two equal administrations.

Individualize the regimen according to fasting blood glucose and postprandial glucose levels.

Monitor blood glucose regularly to determine the minimum effective dose for metabolic control.

In elderly patients or those with renal or hepatic impairment, initiate therapy at the lowest dose and titrate cautiously.

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 fasting 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 recurrent 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.

Concurrent 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 tremor characteristic of hypoglycemia, while sweating may increase.

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

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

With concurrent use with corticosteroids (including topical formulations), diuretics, barbiturates, estrogens, progestins, combined estrogen-progestin drugs, diphenylhydantoin, 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.