Glydiab MR (Tablets) Instructions for Use

Marketing Authorization Holder

Akrikhin Chemical and Pharmaceutical Plant, JSC (Russia)

ATC Code

A10BB09 (Gliclazide)

Active Substance

Gliclazide (Rec.INN registered by WHO)

Dosage Form

Glydiab MR

Modified-release tablets 30 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Modified-release tablets white or white with a creamy tint, flat-cylindrical, with a bevel; the presence of “marbling” is allowed.

Excipients: hypromellose – 0.044 g, microcrystalline cellulose – 0.123 g, colloidal silicon dioxide – 0.001 g, magnesium stearate – 0.002 g.

10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.
15 pcs. – blister packs (4) – cardboard packs.

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

The initial dose for most patients is 30 mg once daily.

Adjust the dose based on glycemic control and fasting blood glucose levels. Titrate the dose in increments of 30 mg every 2-4 weeks.

The maintenance dose typically ranges from 30 mg to 90 mg daily.

Do not exceed the maximum daily dose of 120 mg.

For elderly patients or those with renal/hepatic impairment, initiate therapy at the lowest possible dose and monitor closely.

In case of a missed dose, take it as soon as remembered on the same day. Do not take a double dose the following day.

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. 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 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 simultaneous use of gliclazide with 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 by simultaneous use with pyrazolone derivatives, salicylates, phenylbutazone, antibacterial sulfonamide drugs, theophylline, caffeine, MAO inhibitors.

Simultaneous 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.

With simultaneous use of gliclazide and acarbose, an additive hypoglycemic effect is observed.

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

With simultaneous use with corticosteroids (including topical dosage forms), 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.