Gliclazid-AKOS - instructions for use, dose, side effects, contraindications

Gliclazide is an oral hypoglycemic drug, derivative of sulfonylurea of the second generation. It stimulates the secretion of insulin with β-cells of the pancreas, enhances the insulin secretory effect of glucose, increases the sensitivity of peripheral tissues to insulin. Stimulates the activity of intracellular enzymes - muscle glycogen synthetase. Reduces the interval from the time of food intake to the beginning of secretion of insulin. It restores the early peak of insulin secretion (unlike other sulfonylureas, which mainly affect the second stage of secretion). Decreases the postprandial increase in glucose. In addition to the effect on carbohydrate metabolism, it improves microcirculation: it reduces adhesion and aggregation of platelets, normalizes vascular permeability, prevents the development of microthrombrosis and atherosclerosis, restores the process of physiological parietal fibrinolysis.Reduces the sensitivity of receptors of blood vessels to epinephrine. Slows the development of diabetic retinopathy at the non-proliferative stage. With diabetic nephropathy against a background of long-term use causes a significant decrease in the expression of proteinuria. Does not lead to an increase in body weight, since it has a predominant effect on the early peak of insulin secretion and does not cause hyperinsulinemia; contributes to weight loss in obese patients with a proper diet. It has anti-atherogenic properties, lowers the concentration in the blood of total cholesterol.

Pharmacokinetics:

After ingestion, it is rapidly absorbed in the gastrointestinal tract. Absorption is high. After oral administration of 80 mg, the maximum concentration in the blood (2.2-8 μg / ml) is reached after about 4 hours, after taking 40 mg the maximum concentration in the blood (2-3 μg / ml) - after 2-3 hours. plasma proteins - 85-97%, the volume of distribution - 0.35 l / kg. The equilibrium concentration in the blood is reached after 2 days. Metabolised in the liver, with the formation of 8 metabolites. The amount of the main metabolite found in the blood is 2-3% of the total amount of the drug taken, it has no hypoglycemic effect, but improves microcirculation.It is excreted by the kidneys - 70% in the form of metabolites, less than 1% unchanged; through the intestine - 12% in the form of metabolites.

The half-life is 8-20 hours.

Indications:

Diabetes mellitus type 2 in adults in combination with diet and moderate exercise in case of ineffectiveness of the latter.

Contraindications:

hypersensitivity to the drug;
diabetes mellitus type 1;
Diabetic ketoacidosis, diabetic precoma, diabetic coma;
hyperosmolar coma;
severe hepatic and / or renal insufficiency;
large surgical interventions, extensive burns, injuries and other conditions requiring insulin therapy;
intestinal obstruction, paresis of the stomach;
conditions, accompanied by a violation of food intake, development of hypoglycemia (infectious diseases);
leukopenia;
pregnancy, the period of breastfeeding.

Carefully:

With caution (the need for more careful observation and selection of a dose) is prescribed for febrile syndrome, alcoholism and thyroid diseases (with a violation of its function).

Dosing and Administration:

The dose of the drug is determined individually, depending on the patient's age, clinical manifestations of the disease and the level of fasting glycemia and 2 hours after eating. The initial daily dose is 80 mg, the average daily dose is 160 mg, the maximum daily dose is 320 mg. The drug Gliklazid-AKOS is taken orally 2 times a day (morning and evening) 30-60 minutes before meals.

Side effects:

Hypoglycaemia (with violation of the dosing regimen and inadequate diet): headache, fatigue, hunger, sweating, severe weakness, aggression, anxiety, irritability, inattention, inability to concentrate and delayed reaction, depression, visual impairment, aphasia, tremor, feelings of helplessness, sensory disorders, dizziness, loss of self-control, delirium, convulsions, hypersomnia, loss of consciousness, shallow breathing, bradycardia, palpitations.

On the part of the digestive system: dyspepsia (nausea, diarrhea, a feeling of heaviness in the epigastrium); anorexia - the severity decreases with admission during meals; violations of the liver (cholestatic jaundice, increased activity of "liver" transaminases).

From the hematopoiesis: anemia, thrombocytopenia, and leukopenia.

Allergic reactions: itching, urticaria, maculopapular rash.

Overdose:

With an overdose, hypoglycemia is possible, up to the development of hypoglycemic coma.

Treatment: if the patient is conscious - inside accept easily assimilated carbohydrates (sugar), with a loss of consciousness - intravenously enter a 40% solution of dextrose (glucose), 1-2 mg glucagon intramuscularly. After the restoration of consciousness, the patient should be given food rich in easily assimilated carbohydrates (in order to avoid the re-development of hypoglycemia). With edema of the brain - mannitol and dexamethasone.

Interaction:

The hypoglycemic effect of gliclazide is enhanced by inhibitors of the angiotensin-converting enzyme (captopril, enalapril), H2-histamine receptor blockers (cimetidine), antifungal drugs (miconazole, fluconazole), non-steroidal anti-inflammatory drugs (phenylbutazone, indomethacin, diclofenac), fibrates (clofibrate, bezafibrate), antituberculous drugs (ethionamide), salicylates, indirect anticoagulants of the coumarin series, anabolic steroids, beta adrenoblockers, cyclophosphamide, chloramphenicol, monoamine oxidase inhibitors, prolonged-action sulfanilamides, fenfluramine, fluoxetine, pentoxifylline, guanethidine, theophylline, drugs that block tubular secretion, reserpine, bromocriptine, disopyramide, pyridoxine, allopurinol, ethanol and ethanol-containing drugs, as well as other hypoglycemic drugs (acarbose, biguanides, insulin).

Weaken the hypoglycemic effect of gliclazide barbiturates, glucocorticosteroids, sympathomimetics (epinephrine, clonidine, ritodrin, salbutamol, terbutaline), phenytoin, blockers of "slow" calcium channels, inhibitors of carbonic anhydrase (acetazolamide), thiazide diuretics, chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, glucagon, rifampicin, thyroid hormones, lithium salts, in high doses - a nicotinic acid, chlorpromazine, estrogens and oral contraceptives containing them.

When interacting with ethanol, it is possible to develop a disulfiram-like reaction: Gliclazide increases the risk of ventricular extrasystole on the background of cardiac glycosides.

Beta-blockers, clonidine, reserpine, guanethidine may mask the clinical manifestations of hypoglycemia.

Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

Special instructions:

Treatment with Gliclazide-AKOS is performed in combination with a low-calorie diet with a low carbohydrate content. It is necessary to regularly monitor the glucose in the blood on an empty stomach and after eating.

In the case of large surgical interventions and injuries, extensive burns, infectious diseases with febrile syndrome, it is necessary to consider the possibility of using insulin preparations.

It is necessary to warn patients about the increased risk of hypoglycemia in the case of taking ethanol, nonsteroidal anti-inflammatory drugs and fasting. In case of taking ethanol, it is also possible to develop a disulfiram-like syndrome (abdominal pain, nausea, vomiting, headache).

It is necessary to adjust the dose of the drug in case of physical or emotional overstrain, change in diet.

Particularly sensitive to the effects of hypoglycemic drugs are the elderly; Patients,not receiving a balanced diet; weakened patients; patients suffering from pituitary-adrenal insufficiency.

Effect on the ability to drive transp. cf. and fur:At the beginning of treatment, during the selection of a dose, patients prone to developing hypoglycemia are not recommended to engage in activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 80 mg.

Packaging:

For 10 or 20 tablets in a contour mesh package.

2, 4, 6 or 10 contour cell packs of 10 tablets or 1.2, 3 contour packs of 20 tablets with instructions for use in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002377 / 01

Date of registration:24.11.2008

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp29.04.2017

Illustrated instructions

Instructions

Gliclazide-AKOS (Gliclazide-AKOS)