Diabefarm, tablets 80 mg 60 pcs

Pharmacotherapeutic group: oral hypoglycemic agent of generation II sulfonylurea group

ATC code: A10BV09

Pharmacological action

Pharmacodynamics

Glicliquid stimulates insulin secretion by pancreatic p-cells, increases insulin-secretory action of glucose, increases peripheral tissue sensitivity to insulin. Stimulates the activity of intracellular enzymes – muscle glycogen synthetase. Reduces the period of time from the moment of food intake to the beginning of insulin secretion. Restores the early peak of insulin secretion (unlike other sulfonylurea derivatives, which have an effect mainly during the second stage of secretion).

Limits postprandial increase of blood glucose level.
Besides influence on carbohydrate metabolism it improves microcirculation: decreases adhesion and aggregation of thrombocytes, normalizes vascular permeability, prevents development of microthrombosis and atherosclerosis, restores process of physiological fasting fibrinolysis. It reduces the sensitivity of vascular receptors to adrenaline.

It slows down the development of diabetic retinopathy at the iaproliferative stage. In diabetic nephropathy against the background of long-term use there is a significant reduction in the severity of proteinuria. It does not lead to weight gain, as it mainly influences the early peak of insulin secretion and does not cause hyperinsulinemia; it promotes weight loss in obese patients by keeping a proper diet. Has anti-atherogenic properties, lowers the blood concentration of total cholesterol.

Pharmacokinetics

After oral administration is quickly absorbed in the gastrointestinal tract. Absorption is high. After oral administration of 80 mg, maximum concentration in blood (2.2-8 mcg/ml) is reached after about 4 hours, after administration of 40 mg, maximum concentration in blood (2-3 mcg/ml) is reached after 2 -3 hours. Plasma protein binding is 85-97%, the volume of distribution is 0.35 l/kg. Equilibrium concentration in blood is reached after 2 days. It is metabolized in liver, 8 metabolites are formed.

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% as metabolites, less than 1% unchanged; through the intestines – 12% as metabolites.
Half-life is 8 – 20 hours.

Indications

Diabetes mellitus type 2 in adults combined with diet therapy and moderate physical activity if the latter is ineffective.

Active ingredient

Gliclazide

Composition

1 tablet contains

Active ingredient:

gliclazide 80 mg

Excipients: lactose monohydrate (milk sugar), povidone, magnesium stearate.

How to take, the dosage

The drug dose is adjusted individually, depending on the patient’s age, clinical manifestations of the disease and blood glucose levels on an empty stomach and 2 hours after meals. The initial daily dose is 80 mg, the average daily dose is 160 mg, the maximum daily dose is 320 mg. Diabefarm is taken orally 2 times a day (morning and evening) 30-60 minutes before a meal.

Interaction

Angiotensin-converting enzyme inhibitors (captopril, enalapril), H2-histamine receptor blockers (cimetidine), antifungal drugs (miconazole, fluconazole) enhance the hypoglycemic effect of Diabefarm, nonsteroidal anti-inflammatory drugs (phenylbutazone, indomethacin, diclofenac), fibrates (clofibrate, besafibrate), anti-tuberculosis drugs (etionamide), salicylates, coumarin-type anticoagulants, anabolic steroids, beta-adrenoblockers, cyclophosphamide, chloramphenicol, monoamine oxidase inhibitors, long-acting sulfonamides, phenfluramine, fluoxetine, pentoxifylline, guanethidine, theophylline, drugs that block tubular secretion, reserpine, bromocriptine, disopyramide, pyridoxine, allopurinol, ethanol and ethanol-containing drugs, and other hypoglycemic drugs (acarbose, biguanides, insulin).

The hypoglycemic effect of Diabefarm is weakened by barbiturates, glucocorticosteroids, sympathomimetics (epinephrine, clonidine, ritodrine, salbutamol, terbutaline), phenytoin, “slow” calcium channel blockers, carboenhydrase inhibitors (acetazolamide), thiazide diuretics, Chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, glucagon, rifampicin, thyroid hormones, lithium salts, in high doses – nicotinic acid, chlorpromazine, estrogens and oral contraceptives containing them.

In interaction with ethanol a disulfiram-like reaction is possible.

Diabefarm increases the risk of ventricular extrasystole during cardiac glycosides.

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

Drugs that depress medullary hematopoiesis increase the risk of myelosuppression.

Special Instructions

Treatment with Diabefarm is carried out in combination with a low-calorie low-carbohydrate diet. It is necessary to regularly monitor blood glucose content on an empty stomach and after meals.
In case of surgical interventions or decompensation of diabetes, it is necessary to consider the possibility of using insulin drugs.

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

The drug dose should be corrected in case of physical or emotional stress, change of diet.

The hypoglycemic drugs are especially sensitive to the action of elderly patients, patients without a balanced diet, weakened patients, patients suffering from hypophysial-adrenal insufficiency.

At the beginning of treatment and during dose adjustment, patients prone to the development of hypoglycemia are not recommended to engage in activities requiring increased attention and rapid psychomotor reactions.

Contraindications

Hypersensitivity to the drug; type 1 diabetes mellitus; diabetic ketoacidosis, diabetic precoma, diabetic coma; hyperosmolar coma; severe hepatic and/or renal failure; major surgical interventions, extensive burns, injuries and other conditions requiring insulin therapy; intestinal obstruction, paresis of the stomach; conditions accompanied by disorders of food absorption, the development of hypoglycemia (infectious diseases); leukopenia; pregnancy, breast-feeding, children under 18 years of age.

With caution (need for closer monitoring and dose selection) is administered in febrile syndrome, alcoholism and thyroid disease (with impaired thyroid function).

Side effects

Hypoglycemia (in case of violation of the dosing regimen and inadequate diet): headache, fatigue, hunger, sweating, sudden weakness, aggressiveness, anxiety, irritability, decreased concentration and delayed reaction, depression, visual disturbances, aphasia, tremor, sensory disorders, dizziness, loss of self-control, delirium, seizures, hypersomnia, loss of consciousness, shallow breathing, bradycardia.

Allergic reactions: itching, urticaria, maculopapular rash.

Blood organs: anemia, thrombocytopenia, leukopenia.

Digestive system: dyspepsia (nausea, diarrhea, feeling of heaviness in the epigastrium); anorexia – the severity is reduced when taken with food; liver disorders (cholestatic jaundice, increased activity of “liver” transaminases).

Overdose

Symptoms: hypoglycemia is possible, up to hypoglycemic coma.

Treatment: if the patient is conscious – intravenous administration of digestible carbohydrates (sugar), in case of loss of consciousness – intravenous injection of 40% dextrose solution (glucose), 1-2 mg glucagon intramuscularly. After recovery of consciousness the patient should be given food rich in easily digestible carbohydrates (to avoid recurrence of hypoglycemia). Mannitol and dexamethasone for cerebral edema.

Pregnancy use

The drug is contraindicated in pregnancy and during lactation.

If you become pregnant, the drug should be immediately discontinued.

Similarities

Diabeton MB, Glidiab, Diabefarm MB, Gliclazid MB, Diabetalong, Gliclazid Canon, Gliclazid, Golda MB