Gliklazid-Zdorovye 0,08 No. 10х3

General characteristics. Structure:

International and chemical names: gliclazide; 1-(3-azabitsiklo [3,3,0] octyl-3)-3-(paratonilfsulfonit) urea;
main physical and chemical properties: tablets from almost white till cream color of a ploskotsilindrichesky form with a facet; 
structure: 1 tablet contains gliclazide 80 mg; 
excipients: lactoses monohydrate, cellulose microcrystallic, povidone, to silicon dioxide colloid, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Hypoglycemic means derivative of sulphonylurea of the second generation. Has the expressed hypoglycemic, haemo vascular and antioxidant properties.
Hypoglycemic properties. The mechanism of hypoglycemic action is caused both by increase in secretion of insulin, and strengthening of its effective action. Gliclazide stimulates secretion of  cells insulin of a pancreas that is followed by mobilization and strengthening of emission of endogenous insulin; exponentiates insulinosekretorny effect of glucose. Increases sensitivity of fabrics to insulin due to increase in number of insulinchuvstvitelny receptors on target cells. Improves utilization of glucose due to stimulation of a muscular glikogensintetaza. Has direct effect on intracellular transport of calcium ions that improves the bi-phase answer of  cells of a pancreas to meal: at patients with a diabetes mellitus of the 2nd type gliclazide recovers early peak of an insulinosekretion (immediate first peak of release of insulin) and increases the second phase of an insulinosekretion (the delayed phase).
The hypoglycemic effect develops gradually; at administration of drug the period between meal and the beginning of secretion of insulin is reduced. Normalizes a glycemic profile after several days of treatment.
Hematologic properties. Gliclazide partially inhibits adhesion and aggregation of thrombocytes, reduces quantity of markers of activation of thrombocytes, normalizes permeability of vessels, interferes with development of microthromboses, promotes the prevention of microcirculator disturbances, including a diabetic retinopathy, increases fibrinolitic activity (due to increase in release of a plasminogen activator).
Antioxidant properties. Gliclazide has antioxidant effect. Upatsiyentov with a diabetes mellitus of the 2nd type gliclazide reduces the level of peroxide lipids in plasma, increases activity of peroxide dismutase in erythrocytes, the content of thiols in plasma and the general antioxidant capacity. 
Haemo vascular and antioxidant properties of gliclazide provide decrease in risk of development of vascular complications in patients with a diabetes mellitus. Besides, at a diabetic nephropathy gliclazide promotes decrease in a proteinuria and normalization of arterial pressure. At patients with obesity at observance of the corresponding diet promotes decrease in body weight.

Pharmacokinetics. After intake it is quickly and fully absorbed from a digestive tract. Bioavailability – about 90%. The maximum concentration in blood is reached in 11 – 14 h. Linkng with proteins of plasma makes 94,2%. Hydroxylations, the glyukuronovaniya with formation of 8 inactive metabolites Biotransformirutsya in a liver by oxidation. The elimination half-life makes 20 h that allows to accept drug 2 times a day. It is removed in the form of metabolites mainly by kidneys. 

Indications to use:

Non-insulin-dependent diabetes mellitus (diabetes 2 types). 

Route of administration and doses:

Appoint the adult inside, it is desirable during food. 
The initial and supporting doses, time of reception and distribution of a daily dose are established individually on the basis of results of regular determination of level of glucose in blood and urine.
Initial dose. Sick up to 65 years appoint 80 mg of gliclazide (1 tablet) once a day at breakfast. At patients 65 years an initial dose are more senior makes 40 mg of gliclazide of 1 times a day. In need of strengthening of control of level of a glycemia the daily dose can be raised. Increase in a dose is recommended to spend not less than 14 days with an interval. 
Standard therapeutic dose – 160 mg of gliclazide (2 tablets) a day for two receptions.
Average daily dose – 80 – 240 mg of gliclazide (1 – 3 tablets) a day for two receptions.
The maximum daily dose – 320 mg (4 tablets) a day for two receptions.
At change of body weight or a way of life of the patient, and also at emergence of the factors promoting increase in risk of development hypo - or a hyperglycemia, it is necessary to carry out dose adjustment.

Features of use:

With care use drug at a feverish syndrome, alcoholism, pituitary and adrenal insufficiency, diseases of a thyroid gland (hypo - or a hyperthyroidism), at patients of advanced age and at patients with abnormal liver functions.
Drug should be accepted against the background of a low-calorie diet with the small content of carbohydrates. For prevention of a hypoglycemia it is necessary to date accurately administration of drug for meal, to avoid starvation and to refuse completely alcohol intake. Simultaneous use of  adrenoblockers can disguise hypoglycemia symptoms. In case of surgical interventions or a decompensation of a diabetes mellitus it is necessary to consider a possibility of use of drugs of insulin.
At emergence of clinical signs of a hypoglycemia (sweating strengthening, pallor, tachycardia, an indisposition) drug dose adjustment is necessary.
At long monotherapy (more than 5 years) development of secondary resistance is possible.
Control of laboratory indicators. During selection of a dose (especially in combination with an insulin therapy) definition of a sugar profile and dynamics of a glycemia (several times a week), further – regular control of level of glucose in blood and urine, and also concentration of glikozilirovanny hemoglobin is necessary (at least 1 time in 3 months) that will allow to reveal primary or secondary resistance to drug in time. Besides, it is necessary to control function of a liver and a picture of peripheral blood (especially quantity of thrombocytes and leukocytes).
The states demanding transfer of the patient from gliclazide on an insulin therapy: extensive burns, a severe multiple injury, extensive surgical interventions, disturbances of absorption of food and medicines in digestive tract (intestinal impassability, intestines paresis), heavy abnormal liver functions and kidneys, including stay on a hemodialysis. Need of temporary transfer on insulin can arise in stressful situations (injuries, surgical interventions, infectious diseases which are followed by fever).
Risk of development of a hypoglycemia in an initiation of treatment gliclazide. In the first weeks of treatment the risk of development of a hypoglycemia (can increase especially at irregular meal or the admission of meal). Its development can be promoted by the following factors:
unwillingness or (especially at advanced age) insufficient ability of the patient to cooperation with the doctor;
irregular food, admission of meal, malnutrition;
imbalance between exercise stresses and the use of carbohydrates;
changes in a diet;
alcohol intake, especially at a hyponutrient or the admission of meal;
renal failures;
heavy abnormal liver functions;
drug overdose;
the noncompensated associated diseases of endocrine system influencing carbohydrate metabolism or counterregulation of a hypoglycemia (including dysfunction of a thyroid gland, pituitary or adrenocortical insufficiency);
concomitant use of some other drugs (see the section "Interaction with Other Medicines").
Symptoms of a hypoglycemia can be poorly expressed or even to be absent at its gradual development in patients of advanced age, and also in patients with vegetative dysfunction or at the same time receiving treatment by  adrenoceptors blockers, a clonidine, Reserpinum, guanetidiny or other sympatholytics.

Drug should be accepted only in the appointed doses and in a certain time of day. 
Time of reception and distribution of a daily dose of drug is defined by the doctor with features of a day regimen of the patient. Meal not later than in 1 h after administration of drug is obligatory.
For achievement of optimum control of level of a glycemia at purpose of gliclazide it is necessary to keep in addition to the corresponding diet, to carry out physical exercises and, in case of need, to reduce body weight. It is necessary to refuse long stay in the sun and to limit the use of greasy food.
Mistakes in administration of drug. Errors in gliclazide reception (the admission of reception of a dose because of forgetfulness) cannot be corrected by the subsequent reception of higher dose at all. The doctor and the patient have to discuss previously measures which should be accepted in case of mistakes in administration of drug (the admission of reception of a dose, the admission of meal) or in situations when administration of drug at the scheduled time is impossible. 
The patient has to inform immediately the doctor in case of accidental reception of too high or excess dose of drug.
Use in a combination with insulin. Gliclazide in a combination with insulin is appointed in case it is not possible to reach normalization of concentration of glucose in blood reception of the maximum dose of gliclazide in monotherapy. At the same time against the background of the last gliclazide dose appointed to the patient, treatment with insulin begins with its minimum dose, with possible subsequent gradual increase in a dose of insulin under control of concentration of glucose in blood. The combined treatment demands obligatory medical control. At a gliclazide combination with insulin the dose of the last can be lowered by 25 – 50%. The recommended gliclazide doses in combination with insulin – 80 – 160 mg (1 – 2 tablets) a day.
At transfer of the patient into gliclazide from other drugs сульфонилмочевині (except for Chlorproramidum) and insulin in a daily dose less than 20 PIECES are not required the period of gradual transition. 
Use during pregnancy and feeding by a breast. Drug is contraindicated during pregnancy and feeding by a breast. Patients during pregnancy and planning pregnancy have to be transferred to insulin. Nursing mothers have to be transferred to insulin or refuse completely feeding by a breast.
Influence on an opportunity to manage vehicles and mechanisms. In an initiation of treatment or at irregular reception of gliclazide it can be noted caused hypo - or a hyperglycemia decrease in concentration of attention and speed of psychomotor reactions of the patient. In such situations it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From a metabolism: a hypoglycemia (see the sections "Overdose" and "Features of Use"); very seldom – increase in sensitivity to alcohol, increase in body weight, a dislipidemiya, adjournment of fatty tissue; after long use – hypofunction of a thyroid gland.
From the alimentary system: seldom (especially at non-compliance with the recommendation to accept gliclazide with food) – gastrointestinal frustration in the form of nausea, dyspepsia, a diarrhea, a lock; very seldom – heavy feeling or discomfort in epigastriums, an abdominal pain, heartburn, loss or increase in appetite, change of flavoring feelings, an abnormal liver function, cholestatic jaundice, a porphyria, hepatitis. At cholestatic jaundices it is necessary to stop treatment by drug.
From mucous membranes and skin: very seldom – skin rash, a skin itch, a small tortoiseshell, violent rash.
From system of blood: very seldom – hemolitic or aplastic anemia, an agranulocytosis, a leukopenia, a pancytopenia, thrombocytopenia, an eosinophilia. 
From laboratory indicators: very seldom – increase in level of enzymes of a liver (ALT, nuclear heating plant), an alkaline phosphatase.
Others: hyponatremia, hypoosmolarity or syndrome of inadequate secretion of antidiuretic hormone (depression, dizziness, lethargy, face edemas, anklebones and hands, spasms, stupor, coma), passing disorder of accommodation.
The cross allergy with other derivatives of sulphonylurea, streptocides and tiazidopodobny drugs is possible. 
At drug withdrawal the undesirable phenomena disappear.

Interaction with other medicines:

Strengthening of hypoglycemic effect of gliclazide can be observed at simultaneous use with insulin or other hypoglycemic drugs, inhibitors of an angiotensin-converting enzyme,  adrenoblockers, Allopyrinolum, anabolic steroids and male sex hormones, chloramphenicol, Cimetidinum, coumarin derivatives, tsiklo-, tro-and isophosphamide, fenfluraminy, feniramidoly, fibrata, fluoxetine, guanetidiny, monoamine oxidase inhibitors, Miconazolum, flukonazoly, pentoksifilliny, theophylline, phenylbutazone, oksifenbutazony, azapropanony, probenitsidy, salicylates (in high doses), Sulfinpyrazonum, streptocides of long action, tetracyclines, tritokvaliny.
Weakening of hypoglycemic effect of gliclazide is possible at simultaneous use with acetazoleamide, barbiturates, glucocorticosteroids, diazoxide, saluretics, thiazide diuretics, Epinephrinum (adrenaline) and other sympathomimetics, a glucagon, purgatives (at prolonged use), niacin (in high doses) and its derivatives, estrogen and progestogens, oral contraceptives, fenotiaziny, Phenytoinum, rifampicin, hormones of a thyroid gland, lithium salts, Chlorpromazinum.
Both strengthening, and weakening of hypoglycemic effect of gliclazide can be observed at simultaneous use with blockers of histamine H2 receptors, a clonidine and Reserpinum, one-time or chronic alcohol intake.
Against the background of reception of gliclazide strengthening or weakening of action of derivatives of coumarin can be observed.
Let's combine with guanyl guanidines. It is incompatible with Miconazolum.

Contraindications:

The increased individual sensitivity to gliclazide, to other derivatives of sulphonylurea, to sulfanamide drugs, to auxiliary components of drug. An insulin-dependent diabetes mellitus (І type), including at youthful age, diabetic ketoacidosis, a diabetic prekoma and a coma, a heavy liver and/or renal failure (clearance of creatinine less than 30 ml/min., including the patients who are on a hemodialysis), treatment by Miconazolum, the pregnancy period, the feeding period a breast, children's age (efficiency and safety of use of drug are not established). 

Overdose:

At overdose by gliclazide the hypoglycemia develops. Symptoms: sweating strengthening, feeling of alarm, tachycardia, increase in arterial pressure, a heart consciousness, pains in heart, arrhythmia, a headache, sharp increase in appetite, nausea, vomiting, apathy, drowsiness, concern, aggression, disturbance of concentration of attention, a depression, confusion of consciousness, a tremor, paresis, disturbance of sensitivity, a spasm of the central genesis. The clinical picture of a hypoglycemia can sometimes remind a stroke. Development of a coma is possible. 
Treatment: The easy and moderate hypoglycemia can be quickly stopped by immediate reception of carbohydrates (glucose or sugar, for example, in the form of pieces of sugar, sweet fruit juice or tea). In this regard the patient has to have always at himself not less than 20 g of glucose (4 pieces of sugar). Sweeteners at treatment of a hypoglycemia are inefficient. In hard cases of a hypoglycemia owing to overdose of the patient it is necessary to hospitalize. It is necessary to cause vomiting, to appoint liquid reception (water or lemonade with the activated coal/adsorbent and sulfate sodium/laxative). To immediately begin administration of glucose, in need of a type of intravenous jet administration of 50 ml of 40% of solution with the subsequent infusions more diluted (10%) solution with careful monitoring of level of glucose in blood for maintenance of an easy hyperglycemia of 100 mg/dl, then 1 – 2 mg of a glucagon intramusculary (for mobilization of hepatic glucose), diazoxide of 300 mg intravenously within 30 min. or 200 mg inside each 4 h during the monitoring of level of sodium and control of arterial pressure. Carry out monitoring of a glycemia, definition to blood рН, an urea nitrogen, creatinine, elekrolit each 1 – 3 h. Further carry out a symptomatic treatment. At wet brain enter a mannitol intravenously and dexamethasone, at a hypopotassemia – potassium drugs. At treatment of the hypoglycemia which developed owing to accidental reception of gliclazide by chest or small children to avoid a hyperglycemia, it is necessary to control a dextrose dose (50 ml of 40% of solution) and to continuously monitorirovat concentration of glucose in blood. It is necessary to consider that provocation of an acute/excessive hyperglycemia introduction of hypertonic salt solution of glucose stimulates additional emission of insulin that aggravates a hypoglycemia.

Storage conditions:

To store in the dry, protected from light place at температуреот 8 °C to 25 °C. To store in the place, unavailable to children.
Period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

Tablets of 80 mg No. 10, No. 10x3, No. 30 in the blister in a box.