Gliklazid-Borimed

General characteristics. Structure:

Active ingredient: 80 mg of gliclazide in 1 tablet.

Excipients: sodium lauryl sulfate, starch corn partially prezhelatinizirovanny, croscarmellose sodium, magnesium stearate, lactoses monohydrate.

Pharmacological properties:

Pharmacodynamics. Peroral hypoglycemic means derivative of generation sulphonylurea II. Stimulates insulin secretion with a pancreas, increases insulinosekretorny effect of glucose and sensitivity of peripheral fabrics to insulin. Stimulates activity of desmoenzymes – a muscular glikogensintetaza. Reduces a period from the meal moment prior to insulin secretion. Recovers early peak of secretion of insulin (unlike other derivatives of sulphonylurea which make impact mainly during the second stage of secretion).

Reduces a postprandialny hyperglycemia. It is effective at a metabolic, latent diabetes mellitus, at patients with exogenous and constitutional obesity. Normalizes a glycemic profile after several days of treatment. Prevents development of microvasculites, including defeats of a mesh cover of an eye. Suppresses aggregation of thrombocytes, considerably increases an index of relative disaggregation, increases heparin and fibrinolitic activity, increases tolerance to heparin. Shows antioxidant properties, improves conjunctiva vascularization.

At a diabetic nephropathy reduces a proteinuria. At a diabetic nephropathy against the background of prolonged use decrease in a proteinuria is noted. Does not lead to increase in body weight since makes preferential impact on early peak of an insulinosekretion and does not cause a giperinsulinemiya; promotes decrease in body weight at corpulent patients at observance of a low-calorie diet.

Has anti-atherogenous properties, lowers concentration in blood of the general cholesterol.

Pharmacokinetics. Absorption – high. After oral administration of 80 mg of Tmax – 4 h, Cmax. 2,2 - 8,0 mkg/ml, after reception of 40 mg these indicators make 2 - 3 h and 2 - 3 mkg/ml respectively. Communication with proteins of plasma – 85 - 97%, distribution volume – 0,35 l/kg. Css in blood is reached in 2 days of T½ – 8 - 12 h.

It is metabolized in a liver, at the same time 8 metabolites are formed. Quantity of the main metabolite which is found in blood – 2 - 3% of all amount of the accepted drug, he has no hypoglycemic properties, however has influence on microcirculation. It is removed by kidneys – 70% in the form of metabolites, less than 1% in not changed look; intestines - 12% in the form of metabolites.

Indications to use:

Diabetes mellitus of type 2 (non-insulin-dependent) in combination with a dietotherapy and a moderate exercise stress at inefficiency of the last.

Route of administration and doses:

Inside, during food. An initial daily dose – 80 mg, an average daily dose – 160 - 320 mg (in 2 receptions - in the morning and in the evening). The size of a dose depends on age, weight of a course of diabetes, concentration of glucose of blood on an empty stomach and in 2 h after food.

In combination with insulin 60 - 180 mg are during the day recommended.

Or at a chronic renal failure of weak and average expressiveness (KK of 15 - 80 ml/min.) of correction of the mode of dosing it is not required from patients of advanced age.

At the patients belonging to risk group of development of a hypoglycemia (insufficient or unbalanced food; the heavy or badly compensated endocrine frustration, including pituitary and adrenal insufficiency, a hypothyroidism, a hypopituitarism; cancellation of glucocorticosteroids after their long reception and/or reception in high doses; the expressed vascular defeats, including the heavy coronary heart disease (CHD), heavy atherosclerosis of carotid arteries, widespread atherosclerosis) it is recommended to use the prolonged gliclazide form.

Features of use:

During administration of drug regular definition of glucose of blood on an empty stomach and glikozilirovanny Hb is necessary.

Infectious diseases with a feverish syndrome can demand cancellation of peroral hypoglycemic HP and purpose of insulin.

It is necessary to warn patients about the increased risk of emergence of a hypoglycemia in cases of reception of ethanol and etanolsoderzhashchy medicines (including development of disulfiramopodobny reactions is possible: abdominal pain, nausea, vomiting, headache), NPVP, at starvation.

Dose adjustment at a physical and emotional overstrain, change of a diet is necessary.

As a rule, symptoms of a hypoglycemia pass after meal, carbohydrate-rich (for example, sugar), reception of sweeteners does not promote elimination of hypoglycemic symptoms. The hypoglycemia can recur, despite effective initial stopping. If hypoglycemic symptoms have the expressed character or are long, even in case of temporary improvement of a state after meal, carbohydrate-rich, rendering emergency medical service is necessary, up to hospitalization.

The patients who are not receiving the balanced food with the general weakened state, the patients suffering from pituitary and adrenal insufficiency are especially sensitive to action of hypoglycemic HP of the elderly person. Clinical manifestations of a hypoglycemia can mask at reception of beta adrenoblockers, a clonidine, Reserpinum, guanetidin. Development of secondary medicinal resistance is possible.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Hypoglycemia (at disturbance of the mode of dosing and an inadequate diet): a headache, increased fatigue, feeling of hunger, the increased sweating, sharp weakness, heartbeat, arrhythmia, increase in the ABP, drowsiness, sleeplessness, agitation, aggression, uneasiness, irritability, decrease in concentration of attention, impossibility to concentrate and the slowed-down reaction, a depression, a vision disorder, aphasia, a tremor, paresis, touch frustration, dizziness, feeling of helplessness, self-checking loss, a delirium, spasms, shallow breathing, bradycardia, a loss of consciousness, a coma.

From the alimentary system: dyspepsia (nausea, vomiting, diarrhea, abdominal pain, a lock) - expressiveness decreases at inclusion in food time; seldom - abnormal liver functions (hepatitis, cholestatic jaundice – demands drug withdrawals, increase in activity of "hepatic" transaminases, ShchF).

From bodies of a hemopoiesis: oppression of a marrowy hemopoiesis (anemia, thrombocytopenia, leukopenia, granulocytopenia).

Allergic reactions: skin itch, small tortoiseshell, skin rash, including makulopapulezny and violent), erythema, allergic vasculitis.

Others: vision disorder.

Interaction with other medicines:

(Warfarin) strengthens effect of anticoagulants, anticoagulant dose adjustment can be required.

Miconazolum (at system introduction and when using gel on a mucous membrane of an oral cavity) strengthens hypoglycemic effect of drug (possibly development of a hypoglycemia up to coma).

Phenylbutazone (system introduction) strengthens hypoglycemic effect of drug (forces out from communication with proteins of plasma and/or slows down removal from an organism), control of glucose of blood and dose adjustment of gliclazide is necessary, both during phenylbutazone reception, and after its cancellation.

Ethanol and etanolsoderzhashchy HP strengthens a hypoglycemia, inhibiting compensatory reactions, can promote development of a hypoglycemic coma.

At a concomitant use with other hypoglycemic HP (insulin, acarbose, guanyl guanidines), beta adrenoblockers, flukonazoly, APF inhibitors (captopril, enalapril), blockers of H2-histamine receptors (Cimetidinum), fluoxetine, MAO inhibitors, anabolic steroids, fibrata, chloramphenicol, tetracyclines, streptocides, theophylline, and NPVP - strengthening of hypoglycemic effect and risk of a hypoglycemia.

Danazol - diabetogenic effect. Control of glucose of blood and dose adjustment of gliclazide is necessary, both during reception of a danazol, and after its cancellation.

Chlorpromazinum in high doses (more than 100 mg/days) increases the content of glucose in blood, reducing insulin secretion. Control of glucose of blood and dose adjustment of gliclazide is necessary, both during reception of Chlorpromazinum, and after its cancellation.

GKS (system, intra joint, external, rectal use) a glucagon, thiazide diuretics, rifampicin, hormones of a thyroid gland, lithium salt, high doses of niacin, oral contraceptives and estrogen weaken effect of gliclazide. Control of glucose of blood and dose adjustment of gliclazide is necessary, both during reception of data of HP, and after their cancellation.

Ritodrinum, salbutamol, тербуталин (intravenous administration) - increase the content of glucose of blood. Control of glucose of blood and if necessary - transfer of the patient into therapy is recommended by insulin.

Contraindications:

Hypersensitivity, diabetes mellitus of type 1 (including juvenile MODY type), diabetic ketoacidosis, a diabetic giperosmolyarny prekoma and a coma, a heavy liver and/or renal failure, the accompanying therapy by Miconazolum, extensive injuries and burns, hypo - and a hyperthyroidism, pregnancy, the lactation period, age up to 18 years.

In connection with the contents in a tablet of lactose it is contraindicated at an inborn lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption.

Precautionary measures. Advanced age, irregular and/or unbalanced food, a serious illness of cardiovascular system (including an ischemic heart disease, atherosclerosis), a hypothyroidism, adrenal or pituitary insufficiency, a hypopituitarism, a renal and/or liver failure, long therapy by glucocorticosteroids, alcoholism, insufficiency glyukozo-6-fosfatdegidrogenazy, the accompanying therapy by phenylbutazone and danazoly.

Overdose:

Symptoms: hypoglycemia (feeling of hunger, alarm, tremor, tachycardia, perspiration, expansion of pupils), consciousness disturbance, hypoglycemic coma.

Treatment: if the patient in consciousness, inside to accept sugar; at disorder of consciousness - intravenous administration of 50 ml of 20 - 30% of solution of a dextrose, then intravenously kapelno 10% dextrose solution before achievement of concentration of glucose in blood of 5,55 mol/l, 1 - 2 mg of a glucagon intramusculary, control of concentration of glucose of blood every 15 min., and also definition of pH, urea, creatinine and electrolytes in blood.

After recovery of consciousness it is necessary to give to the patient the food rich with digestible carbohydrates (in order to avoid repeated development of a hypoglycemia). At wet brain - Mannitolum and dexamethasone. Dialysis is inefficient.

Storage conditions:

In the place protected from light and moisture at a temperature not over 25 ºС. To store in the place, unavailable to children. Period of validity 2 years. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, in packaging No. 10 x 3, No. 10 x 6.