Gliclazide stimulates insulin secretion of pancreatic p-cells, enhances glucose insulinosekretornoe effect, increases the sensitivity of peripheral tissues to insulin. It stimulates the activity of intracellular enzymes – muscle glycogen. It testosterone propionate half life reduces the time period from the beginning of the meal to insulin secretion. Restores the early peak of insulin secretion (as opposed to other sulfonylureas that affect primarily during the second stage of secretion). Reduces the postprandial increase in blood glucose levels. In addition to the effects on carbohydrate metabolism, improves microcirculation: it reduces the adhesion and aggregation of platelets, normalizes vascular permeability, prevents the development of atherosclerosis and mikrotrombozov, restores the physiological process of the parietal fibrinolysis. It reduces the sensitivity of vessels to adrenaline receptors. Slows the development of diabetic retinopathy on yaeproliferativnoy stage. In diabetic nephropathy in the background of long-term use was a significant reduction of proteinuria. Does not increase body weight, asIt has predominant effects on early peak of insulin secretion and hyperinsulinemia causes; It promotes weight loss in obese patients, subject to an appropriate diet. It has anti-atherogenic properties, lowers the concentration of total cholesterol in the blood. Pharmacokinetics After oral administration, rapidly absorbed from the gastrointestinal tract. Absorption – high. After oral administration of 80 mg of the maximum blood concentration (2,2-8 mg / ml) is achieved in about 4 hours after administration of 40 mg of the maximum concentration in blood (3.2 ug / ml) – achieved in 2 hours Connection -3. to plasma proteins – 85-97%, the volume of distribution – 0.35 l / kg. The equilibrium concentration in the blood is reached after 2 days. It is metabolized in the liver, forming eight metabolites. The amount of basic metabolites occurring in the blood is 3.2% of the total amount of the drug taken, it does not have a hypoglycemic action, but improves. Excreted by the kidneys – 70% in the form of metabolites, less than 1% in an unmodified form; through the intestine -. 12% as metabolites half-life of 8 – 20 hours.
Type 2 diabetes mellitus in adults in combination with diet and moderate physical activity with the ineffectiveness of the past.
Hypersensitivity to the drug; type 1 diabetes; diabetic ketoacidosis, diabetic precoma, diabetic coma; hyperosmolar coma; severe hepatic and / or renal failure;major surgery, extensive burns, trauma and other conditions requiring insulin therapy; testosterone propionate half life ileus, gastroparesis; State, accompanied by malabsorption of food, the development of hypoglycemia (infectious diseases); leukopenia; pregnancy, lactation, children under 18 years.
The caution (the need for more careful monitoring and dose titration) is prescribed for feverish syndrome, alcoholism and diseases of the thyroid gland (in violation of its functions).
Pregnancy and lactation
The drug is contraindicated in pregnancy and during breastfeeding.
In the event of pregnancy, the drug should be discontinued immediately.
Dosing and Administration
The dose is established individually, depending on the age of the patient, the clinical manifestations of the disease and the level of fasting blood glucose and 2 hours after eating. The initial daily dose – 80 mg, the average daily dose – 160 mg, the maximum daily dose – 320 mg. taken orally two times a day (morning and evening) for 30-60 minutes before meals.
Side effects: Hypoglycemia (in violation of the dosing and inadequate diet): headache, fatigue, hunger, sweating, severe weakness, aggressiveness, anxiety, irritability, attention, concentration decrease and slow reaction, depression, blurred vision, aphasia, tremor, sensory disorders, dizziness, self-loss, delirium, convulsions, hypersomnia, fainting, shallow breathing, bradycardia. Allergic reactions: itching, rash, maculo-papular rash. From the side of blood: anemia, thrombocytopenia, leukopenia. From the digestive system: dyspepsia (nausea, diarrhea, feeling of heaviness in the epigastric); anorexia – the severity is reduced when taking while eating; abnormal liver function (cholestatic jaundice, increased activity of “hepatic” transaminases).
Symptoms of hypoglycemia can, until the development of hypoglycemic coma.
Treatment: If the patient is conscious – to take into carbohydrate (sugar), with disorders of consciousness – enter intravenously 40% dextrose (glucose), 1-2 mg of glucagon intramuscularly. After regaining consciousness of the patient is necessary to give food rich in carbohydrate (to avoid a recurrence of hypoglycemia). When brain edema – mannitol and dexamethasone.
Interaction with other drugs
Strengthen hypoglycemic effect a angiotensin converting enzyme inhibitors (captopril, enalapril), blockers H2-histamine receptors (cimetidine), antifungals (miconazole, fluconazole), non-steroidal anti-inflammatory drugs (phenylbutazone, indomethacin, diclofenac), fibrates (clofibrate, bezafibrate), anti-TB drugs (ethionamide), salicylates, anticoagulants coumarin, anabolic steroids, beta-blockers, cyclophosphamide, chloramphenicol, monoamine oxidase inhibitors, sulfonamides prolonged action, fenfluramine, fluoxetine, pentoxifylline, guanethidine, theophylline, drugs that block tubular secretion, reserpine , bromocriptine, disopyramide, pyridoxine, allopurinol, ethanol etanolsoderzhaschie drugs, and other hypoglycemic agents (acarbose, biguanides, insulin).
Loosen hypoglycemic effect a barbiturates, steroids, sympathomimetics (epinephrine, clonidine, ritodrine, salbutamol, terbutaline), phenytoin, blockers “slow” calcium channel blockers, carbonic anhydrase inhibitors (acetazolamide), thiazide diuretics, chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, glucagon, rifampicin, thyroid hormones, lithium salt, in high doses – nicotinic . acid, chlorpromazine, estrogens and containing their oral contraceptives
. The interaction with ethanol can disulfiramopodobnyh reaction
. increases the risk of ventricular arrhythmias in patients receiving cardiac glycosides
Beta-blockers, clonidine, reserpine, guanethidine may mask clinical – manifestations of hypoglycemia.
Medicines suppress bone marrow blood, increases the risk of myelosuppression.
om Treatment is carried out in conjunction with a low calorie diet low in carbohydrates. Regularly monitor blood glucose fasting and after eating.
In the case of surgical interventions or decompensated diabetes, it is necessary to take into account the possibility of insulin preparations.
It is necessary to warn patients about the increased risk of hypoglycemia in the case of reception of ethanol, nonsteroidal anti-inflammatory drugs, fasting. . In the case of reception of ethanol may also develop disulfiramopodobnyh syndrome (abdominal pain, nausea, vomiting, headache)
needed correction doses in case of physical or emotional strain, diet change
is especially sensitive to testosterone propionate half life hypoglycemic drugs the elderly; Patients who do not receive a balanced diet; debilitated patients; patients with pituitary-adrenal insufficiency.
In the beginning of treatment, during dose adjustment to patients prone to hypoglycemia, is not recommended to engage in activities requiring increased attention and psychomotor speed reactions.