Expiration date: 05/2025

The composition and form of issue: 

The modified-release tablets. 1 tablet contains active substance: 

gliclazide in terms of 100% substance, 30 mg

excipients: hypromellose — 44 mg MKC — 123 mg of colloidal silicon dioxide 1 mg magnesium stearate 2 mg 

in packing contour cell 10 PCs. in cardboard pack of 3 or 6 packs.

Description pharmaceutical form:

Tablet valium shape with facet, white or white with kremovatam white color allowed the existence of "marbling".

Pharmacokinetics:

Plasma concentration increases smoothly, coming to a plateau after 6-12 hours after ingestion. Absorption and bioavailability are high, eating does not affect the extent of absorption. Connection with plasma proteins — 85-97%. T1/2 — 16 h. the elderly clinically significant changes in pharmacokinetic parameters were observed.

Metabolized in the liver to form 8 metabolites. The amount of the main metabolite found in blood 2-3% of the total number of drugs. It has hypoglycemic properties, but has the influence on the microcirculation. Excreted by the kidneys — 70% as metabolites, <1% unchanged to the intestine of 12% in the form of metabolites.

Description pharmacological action:

The oral hypoglycemic agent, derived sulfonylureas II generation. Stimulates the secretion of insulin by the pancreas, increases insulinsecreting action of glucose and the sensitivity of peripheral tissues to insulin. Stimulates the activity of intracellular enzymes and muscle glikogensintetazy. Reduces the period of time from the moment the meal before insulin secretion. Restores the early peak of insulin secretion (in contrast to the other derivatives of sulfonylurea, such as glibenclamide, which impact mainly during the second stage of secretion).

In addition to the impact on carbohydrate metabolism, influences the microcirculation. Reduces postprandial hyperglycemia, reduces adhesion and aggregation of platelets, delays the development of mural thrombosis, normalizes the permeability of blood vessels and prevents the development of mikrotromboza and atherosclerosis, restores the physiological process of the parietal fibrinolysis, prevents increased response to epinephrine of the blood vessels in the microvascular complications.

Slows the progression of diabetic retinopathy at the nonproliferative stage.

In diabetic nephropathy on the background of the prolonged use noted a significant decrease in proteinuria.

Does not increase body weight, because it has a preferential effect on the early peak of insulinsecretion, and does not cause hyperinsulinemia promotes weight loss in obese patients in compliance with appropriate diet. It has anti-atherogenic properties, lowers blood concentration of total cholesterol.

Indications:

• diabetes mellitus type 2 in adults (with inefficiency diet and physical activity).
  

Contraindications:

• hypersensitivity
  
• diabetes mellitus type 1
  
• diabetic ketoacidosis
  
• diabetic precoma and coma
  
• severe hepatic and/or renal failure
  
• concomitant treatment with miconazole
  
• pregnancy, lactation
  
• the age of 18.
  

With caution: advanced age, irregular and/or unbalanced diet, heavy diseases of the cardiovascular system (including ischemic heart disease, atherosclerosis), hypothyroidism, adrenal or pituitary failure, hypopituitarism, renal and/or hepatic insufficiency, long-term therapy of corticosteroids, alcoholism, deficiency of glucose-6-phosphate dehydrogenase, concomitant therapy with phenylbutazone, danazol and.

Side effects:

Hypoglycemia (in violation of the dosing and inadequate diet): headache, fatigue, hunger, sweating, sudden weakness, palpitations, arrhythmia, increased blood pressure, drowsiness, insomnia, agitation, aggressiveness, anxiety, irritability, poor concentration, inability to concentrate, and slow reaction, depression, blurred vision, aphasia, tremor, paresis, sensory disturbances, dizziness, helplessness, loss of self-control, delirium, convulsions, shallow breathing, bradycardia, loss of consciousness, coma.

From the digestive system: dyspepsia (nausea, vomiting, diarrhea, abdominal pain, constipation) — severity is reduced when taken during meals rarely — infringements of function of a liver (a hepatitis, cholestatic jaundice requires discontinuation of the drug, increase in liver transaminases, alkaline phosphatase).

On the part of the blood: oppression kostnomozgovy blood (anemia, thrombocytopenia, leukopenia, granulocytopenia).

Allergic reactions: skin itching, urticaria, skin rash (including maculopapular and bullous) erythema.

Other: blurred vision.

Common side effects of sulfonylureas: erythropenia, agranulocytosis, haemolytic anaemia, pancytopenia, allergic vasculitis ginepraia liver failure.

Drug interactions:

Enhances the action of anticoagulants (warfarin), you may need to adjust dose of anticoagulant.

Miconazole (with systemic administration and the use of the gel on the mucous membrane of the oral cavity) enhances the hypoglycemic effect of the drug (may develop hypoglycemia up to coma).

Phenylbutazone (systemic) enhances the hypoglycemic effect of the drug (displaces from its Association with plasma proteins and/or slow excretion from the body). It is necessary to control blood glucose and correction doses of gliclazide, as in people phenylbutazone and after its cancellation.

Ethanol and etanolsodergaszczye drugs increase hypoglycemia by inhibiting compensatory reactions, may contribute to the development of hypoglycemic coma. At simultaneous reception with other hypoglycemic drugs (insulin, acarbose, biguanides), &beta-blockers, fluconazole, ACE inhibitors (captopril, enalapril), and blockers of H2-histamine receptors (cimetidine), MAO inhibitors, sulfonamides and NSAIDs — increased hypoglycemic effect and risk of hypoglycemia.

The danazol — diabetogenic effect. It is necessary to control blood glucose and correction doses of gliclazide, as while taking the danazol, and after its cancellation.

Chlorpromazine in high doses (more 100 mg/day) increases the content of glucose in the blood, reducing insulin secretion. It is necessary to control blood glucose and correction doses of gliclazide, as while taking chlorpromazine, and after its cancellation.

Corticosteroids (systemic, intra-articular, outer, rectal) increase of glucose of blood with the possible development of ketoacidosis (reduced tolerance to carbohydrates). It is necessary to control blood glucose and correction doses of gliclazide, as while taking corticosteroids and after their withdrawal.

Ritodrin, salbutamol, terbutaline (in/in the introduction) is the increase of glucose of blood. It is recommended to monitor blood glucose and, if necessary, transfer the patient to insulin therapy.

Method of application and dose:

Inside.

Take 1 time per day during Breakfast. If the drug was skipped, then the next day the dose should not be increased. The initial recommended dose is 30 mg (including of persons older than 65 years). Each subsequent dose change can be undertaken after a minimum two week period. Daily dose should not exceed 120 mg. If the patient previously received therapy with sulfonylureas with a longer T1/2, should be carefully monitored (1-2 weeks) to avoid hypoglycemia caused by the superposition of their effects.

In elderly patients or in chronic renal failure mild and moderate severity (creatinine Cl — 15-80 ml/min) the drug is prescribed in the same doses.

In patients at risk of hypoglycemia (inadequate or unbalanced diet severe or poorly compensated endocrine disorders, including pituitary and adrenal insufficiency, hypothyroidism, hypopituitarism cancel GKS after a long reception and/or reception of high doses of expressed vascular disorders, including severe coronary artery disease, severe atherosclerosis of the carotid arteries, a common atherosclerosis), it is recommended to use a minimum dose of 30 mg.

Overdose:

Symptoms: hypoglycaemia, impaired consciousness, hypoglycaemic coma.

Treatment: if the patient is conscious, inside take sugar in disorders of consciousness in/with the introduction of a 40% solution of dextrose, and then in/drip in 5% dextrose to achieve a concentration of glucose in the blood of 5.55 mol/l, 1-2 mg glukagona/m, control of the concentration of blood glucose every 15 min and determination of pH, urea, creatinine and electrolytes in blood. After recovering consciousness should give the patient foods rich in easily digestible carbohydrates (to avoid a recurrence of hypoglycemia). Cerebral edema — mannitol and dexamethasone. Dialysis is ineffective.

Precautions:

While taking the drug need regular determination of fasting blood glucose and glycosylated hemoglobin.

Major surgery and trauma, extensive burns, infectious diseases febrile syndrome may require the cancellation of oral hypoglycemic drugs and insulin purpose.

It should warn patients about the increased risk of hypoglycemia in cases of reception of ethanol and etanolsodergaszczye drugs (including perhaps the development disulfiramopodobna reactions: abdominal pain, nausea, vomiting, headache), NSAIDs, when fasting.

A correction dose with physical and emotional stress, change in diet.

Generally, symptoms of hypoglycemia are after a meal rich in carbohydrates (such as sugar), intake of sugar substitutes is not conducive to the elimination of hypoglycemic symptoms. Hypoglycemia can recur despite effective initial relief. If hypoglycemic symptoms are severe or are prolonged, even in the case of a temporary improvement the condition after a meal rich in carbohydrates, necessary medical care until hospitalization.

Particularly sensitive to hypoglycemic drugs the elderly, patients who are not receiving a balanced diet with a weakened General condition, patients suffering from pituitary-adrenal insufficiency. The clinical manifestations gipoglikemii may be masked in the admission &beta-adrenoblokatorov, clonidine, rezerpina, guanetidina. Perhaps the development of secondary drug resistance (necessary to distinguish from primary at which BOS already during the first appointment does not give the expected clinical effect).

Effects on ability to drive or to perform work requiring high speed physical and mental reactions

During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.