Gluconorms

General characteristics. Structure:

Active agents: Metforminum a hydrochloride - 400 mg; Glibenclamidum - 2,5 mg;

Excipients: microcrystallic cellulose, starch corn, silicon dioxide colloid, gelatin, глицерол, magnesium the stearate, talc purified croscarmellose sodium, carboxymethyl sodium starch, целлацефат, diethyl phthalate.

Pharmacological properties:

Pharmacodynamics. Глюконорм® represents the fixed combination of two peroral hypoglycemic means of various pharmacological groups: Metforminum and Glibenclamidum.

Metforminum concerns to group of guanyl guanidines and reduces glucose level in blood serum due to increase in sensitivity of peripheral fabrics to effect of insulin and strengthening of capture of glucose. Reduces absorption of carbohydrates in digestive tract and brakes a gluconeogenesis in a liver. Drug also has favorable effect on a blood lipid profile, reducing the level of the general cholesterol, LPNP and triglycerides. Does not cause hypoglycemic reactions.
д treats group of derivatives of sulphonylurea II of generation. Stimulates secretion of insulin by reduction of the threshold of irritation with glucose of beta cells of a pancreas, increases sensitivity to insulin and extent of its linkng with target cells, increases insulin release, strengthens influence of insulin on glucose absorption by muscles and a liver, brakes a lipolysis in fatty tissue. Works in the second stage of secretion of insulin.

Pharmacokinetics. Glibenclamidum. At intake absorption makes 48-84% of the digestive tract (DT). Time of achievement of the maximum concentration (TCmax) – 1-2 hours, distribution volume – 9-10 l. Communication with proteins of plasma makes 95%. Almost another is completely metabolized in a liver with formation of two inactive metabolites, one of which is brought by kidneys, and – intestines. An elimination half-life (T1/2) – from 3 to 10-16 hours.

Metforminum after intake is absorbed from digestive tract rather fully, in Calais 20-30% of a dose are found. Absolute bioavailability makes from 50 to 60%. At a concomitant use of food absorption of Metforminum decreases and late. It is quickly distributed in fabric, practically does not contact proteins of plasma. Is exposed to metabolism in very weak degree and it is removed by kidneys. T1/2 makes about 9-12 hours.

Indications to use:

Diabetes mellitus 2 types at adults:
- at inefficiency of a dietotherapy, physical exercises and the previous therapy by Metforminum or Glibenclamidum;
- for substitution of the previous therapy by two drugs (Metforminum and Glibenclamidum) at patients with the stable and well controlled level of glucose of blood.

Route of administration and doses:

Drug is used inside, during food. The dose of drug is defined by the doctor individually for each patient depending on blood glucose level.

Usually initial dose makes 1 tablet Глюконорма® 400 of mg / 2,5 mg a day. Each 1-2 weeks after an initiation of treatment korregirut a dose of drug depending on blood glucose level. At substitution of the previous combination therapy Metforminum and glibeklamidy appoint 1 - 2 tablets Glyukonorma® depending on the previous dose of each component. The maximum daily dose makes 5 tablets Glyukonorma®.

Features of use:

Big surgical interventions and injuries, extensive burns, infectious diseases with a feverish syndrome can demand drug withdrawal and purpose of an insulin therapy.

It is regularly necessary to control the content of glucose in blood on an empty stomach and after meal.

It is necessary to warn patients about the increased risk of emergence of a hypoglycemia in cases of reception of ethanol, NPVP, at starvation.

Dose adjustment at a physical and emotional overstrain, change of a diet is necessary. During treatment it is not recommended to accept alcohol.

In 48 hours prior to surgical intervention or intravenous administration of iodinated X-ray contrast means reception of Glyukonorma® should be stopped. Treatment of Glyukonormom® is recommended to be resumed in 48 hours.

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:

From carbohydrate metabolism: the hypoglycemia is possible.

From a GIT and a liver: seldom - nausea, vomiting, abdominal pains, appetite loss, "metal" smack in a mouth; in some cases - cholestatic jaundice, increase in activity of "hepatic" enzymes, hepatitis.

From system of a hemopoiesis: seldom - a leukopenia, thrombocytopenia, an erythrocytopenia; very seldom - an agranulocytosis, hemolitic or megaloblastny anemia, a pancytopenia.

From the central nervous system: a headache, dizziness, weakness, increased fatigue, it is rare - paresis, sensitivity disturbances.

Allergic and immunopathological reactions: seldom - a small tortoiseshell, an erythema, a skin itch, fervescence, an arthralgia, a proteinuria.

Dermatological reactions: seldom - a photosensitization.

From a metabolism: lactoacidosis.

Others: the acute reaction of intolerance of alcohol after its use which is expressed complications from bodies of blood circulation and breath (disulfiramopodobny reaction: vomiting, feeling of heat in the person and an upper part of a trunk, tachycardia, dizziness, a headache).

Interaction with other medicines:

Inhibitors of an angiotensin-converting enzyme (captopril, enalapril), H2 blockers - histamine receptors (Cimetidinum), antifungal medicines (Miconazolum, флуконазол), non-steroidal anti-inflammatory drugs (NPVP) (phenylbutazone, азапропазон, оксифенбутазон), fibrata (Clofibratum, безафибрат), antitubercular (Etioniamidum), salicylates, anticoagulants of a coumarinic row, anabolic steroids, beta adrenoblockers, monoaminooxidase inhibitors, streptocides of long action, cyclophosphamide, chloramphenicol, фенфлурамин, fluoxetine, гуанетидин, пентоксифиллин, tetracycline, theophylline, blockers of canalicular secretion, Reserpinum, Bromocriptinum, Disopyramidum, a pyridoxine, others hypoglycemic drug (acarbose, guanyl guanidines, insulin, etc.), Allopyrinolum strengthen hypoglycemic effect of drug.

Barbiturates, glucocorticosteroids, adrenostimulyator (Epinephrinum, clonidine), antiepileptic drugs (Phenytoinum), blockers of "slow" calcium channels, inhibitors of a karboangidraza (acetazoleamide), thiazide diuretics, Chlortalidonum, furosemide, Triamterenum, asparaginase, Baclofenum, даназол, diazoxide, an isoniazid, morphine, Ritodrinum, salbutamol, тербуталин, a glucagon, rifampicin, iodinated hormones of a thyroid gland, lithium salt, in high doses - niacin, Chlorpromazinum, oral contraceptives and estrogen weaken effect.

The medicines acidifying urine (ammonium chloride, Calcii chloridum, ascorbic acid in high doses) strengthen action due to reduction of extent of dissociation and increase in a reabsorption of Glibenclamidum.

Ethanol strengthens probability of development of lactoacidosis.

Metforminum reduces the maximum concentration in blood (Cmax) and T1/2 of furosemide by 31 and 42,3% respectively.

Furosemide increases Cmax of Metforminum by 22%.

Nifedipine increases absorption, Cmax, slows down Metforminum removal.

Cationic medicines (amiloride, digoxin, morphine, procaineamide, quinidine, quinine, ranitidine, Triamterenum and Vancomycinum) cosecreting in tubules compete for tubular transport systems and at long therapy can increase Cmax of Metforminum by 60%.

Contraindications:

- hypersensitivity to Metforminum, Glibenclamidum or other derivatives of sulphonylurea, and also to excipients;
- diabetes mellitus of 1 type;
- diabetic ketoacidosis, diabetic prekoma, diabetic coma;
- hypoglycemia;
- heavy renal failures;
- acute states which can lead to change of function of kidneys: dehydration, heavy infection, shock;
- the acute or chronic diseases which are followed by a hypoxia of fabrics: heart or respiratory failure, recent myocardial infarction, shock;
- liver failure;
- porphyria;
- pregnancy, breastfeeding period;
- concomitant use of Miconazolum;
- the infectious diseases, big surgical interventions, injuries, extensive burns and other states demanding performing insulin therapy;
- alcoholism, acute drunkenness;
- lactoacidosis (including in the anamnesis);
- use within not less than 48 hours to and within 48 hours after carrying out radio isotope or X-ray inspections with administration of iodinated contrast medium;
- observance of a hypocaloric diet (less than 1000 кал / days).

It is not recommended to use drug at persons 60 years performing hard physical activity that is connected with the increased risk of development of lactoacidosis at them are more senior.

With care
Feverish syndrome, adrenal insufficiency, hypofunction of a front share of a hypophysis, disease of a thyroid gland with disturbance of its function.

Use during pregnancy and breastfeeding
During pregnancy use of Glyukonorma® is contraindicated. When planning pregnancy, and also in case of approach of pregnancy during reception of Glyukonorma®, drug has to be an insulin therapy is cancelled and is appointed.
Глюконорм® it is contraindicated when breastfeeding as Metforminum gets into breast milk. In this case it is necessary to pass to an insulin therapy or to stop feeding by a breast.

Overdose:

The overdose or existence of risk factors can provoke development of lactoacidosis as Metforminum is a part of drug. At emergence of symptoms of lactoacidosis (vomiting, abdominal pains, the general weakness, muscular spasms) it is necessary to stop administration of drug. Lactoacidosis is the state demanding emergency medical service; treatment of lactoacidosis has to be carried out in a hospital. The most effective method of treatment is the hemodialysis.

The overdose can also lead to development of a hypoglycemia because of presence at composition of drug of Glibenclamidum. Hypoglycemia symptoms: feeling of hunger, the increased perspiration, weakness, heartbeat, pallor of integuments, paresthesia of a mucous membrane of an oral cavity, a tremor, the general concern, a headache, pathological drowsiness, frustration of a dream, sensation of fear, a lack of coordination of movements, temporary neurologic frustration. When progressing a hypoglycemia loss by the patient of self-checking and consciousness is possible.

At a hypoglycemia easy or the moderately severe dextrose (glucose) or solution of sugar is accepted inside. In case of a heavy hypoglycemia (loss of consciousness) solution of a dextrose (glucose) or a glucagon intravenously, intramusculary, subcutaneously enter intravenously 40%. After consciousness recovery the patient needs to give food, carbohydrate-rich, in order to avoid repeated development of a hypoglycemia.

Storage conditions:

In the dry, protected from light place at a temperature below 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 2,5 mg + 400 mg.
On 10, 20 or 30 tablets in the Al/PVC blister.
On 1, 2, 3, 4 blisters together with the application instruction in a cardboard pack.