Глибомет®

General characteristics. Structure:

Active agents: Glibenclamidum of 2,5 mg
Metforminum hydrochloride of 400 mg
excipients: MKTs; starch corn; silicon dioxide high-disperse; gelatin; glycerin; talc; magnesium stearate; cellulose acetate-phthalate; diethyl phthalate

Description. Round, white, convex tablets, coated, with risky for division on one party.

Pharmacological properties:

Pharmacological properties. The peroral combined hypoglycemic means derivative of sulphonylurea II of generation and guanyl guanidine. Has pancreatic and extra pancreatic effects. Glibenclamidum concerns to group of derivatives of sulfanylurea 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 effect of insulin on glucose absorption by muscles and a liver, brakes линолиз in fatty tissue. Works in the second stage of secretion of insulin. Metforminum concerns to group of guanyl guanidines. The gluconeogenesis in a liver oppresses, reduces absorption of glucose from the digestive tract (DT) and increases its utilization in fabrics; reduces the content of triglycerides, LPNP and cholesterol in blood serum. Increases linkng of insulin with receptors (at absence in insulin blood the therapeutic effect is not shown). Does not cause hypoglycemic reactions.

The hypoglycemic effect of drug develops in 2 h and lasts 12 h.

Pharmacokinetics. Glibenclamidum quickly and rather fully (84%) is absorbed in a GIT. Time of achievement of the maximum concentration of 7-8 h. Communication with proteins makes 97%. Almost it is completely metabolized in a liver to inactive metabolites. For 50% it is brought by kidneys, to 50% - with bile. An elimination half-life - from 3 to 10-16 h.

Metforminum after absorption in a GIT (absorption - 48-52%) is absorbed from digestive tract rather fully, in Calais 20-20% of a dose are found. Absolute bioavailability makes from 50 to 60%. Metforminum is quickly distributed in fabric. Practically does not contact proteins. Is exposed to metabolism in very weak degree and it is removed by kidneys (preferential in a neizmeneny look), partially intestines. The elimination half-life makes 9-12 h.

Indications to use:

• A diabetes mellitus of type 2 at inefficiency of a dietotherapy, physical exercises
 and the previous therapy by Metforminum or Glibenclamidum.
• Substitution of the previous therapy by two drugs (Metforminum and Glibenclamidum) at patients with the stable and well controlled level of a glycemia.

Route of administration and doses:

The dose and the mode of administration of drug, and also duration of treatment are established by the attending physician first of all according to a condition of carbohydrate metabolism of the patient, depending on blood glucose level.

Usually initial dose makes 1-3 tablets a day during food with gradual selection of a dose before achievement of permanent compensation of a disease.

The optimum mode administration of drug 2 times a day (in the morning and in the evening) is considered though also other individual schemes are possible.

It is not recommended to take more than 5 pill of the drug Glibomet® a day.

Features of use:

Treatment by drug (appointment and dose adjustment) is carried out only by the doctor! At administration of drug it is necessary to observe strictly recommendations of the doctor about observance of a diet and self-checking behind blood glucose level. If during treatment by the drug Glibomet® the patient had a vomiting and abdominal pains accompanied with muscular spasms or a febricula, then it is necessary to stop administration of drug and to see immediately a doctor as the specified symptoms can be signs of development of a lactacidemia.

During treatment it is not recommended to accept alcohol.

During treatment by the drug Glibomet® because of possible development of a hypoglycemia ability to driving of motor transport and control of mechanisms can be broken.

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 some cases - cholestatic jaundice, increase in activity of "hepatic" enzymes, hepatitis.

From system of a hemopoiesis:

seldom - a leukopenia, thrombocytopenia, an erythrocytopenia; very seldom agranulocytosis, hemolitic or megaloblastny anemia, pancytopenia.

From TsNS:

headache, dizziness, weakness, it is rare - paresis, sensitivity disturbances.

Allergic and immunopathological reactions:

seldom - a small tortoiseshell, an erythema, a skin itch, fervescence, joint pains, emergence of protein in urine.

Dermatological reactions:

seldom - the raised photosensitivity.

From a metabolism:

increase in concentration of a lactate of blood is possible.

At emergence of symptoms of a lactacidemia (vomiting, abdominal pains, the general weakness, muscular spasms) it is necessary to stop administration of drug and to see immediately a doctor.

Others:

"antabusny effect" at alcohol intake.

Interaction with other medicines:

Hypoglycemic effect of drug can amplify at a concomitant use of a dikumarol and its derivatives, beta adrenoblockers, Cimetidinum, Oxytetracyclinum, Allopyrinolum, inhibitors of a monoaminooxidase (MAO), streptocides, phenylbutazone and its derivatives, chloramphenicol, a probenetsid and salicylates, Miconazolum in peroral forms, Sulfinpyrazonum and alcohol in large numbers. Adrenaline, glucocorticosteroids, oral contraceptives, drugs of hormones of a thyroid gland, thiazide diuretics and barbiturates reduce hypoglycemic effect of drug. Strengthening of effect of anticoagulative means is possible.

The concomitant use with Cimetidinum can strengthen risk of development of a lactacidemia.

b-adrenoblockers mask hypoglycemia symptoms.

Contraindications:

• hypersensitivity to Metforminum, Glibenclamidum or other derivatives of sulphonylurea, and also to other components of drug;
• diabetes mellitus of 1 type (insulin-dependent);
• hypoglycemia;
• diabetic ketoacidosis, diabetic prekoma, coma;
• pregnancy, breastfeeding period;
• a lactacidemia (including in the anamnesis);
• the serious illness which is followed by depression of function of a liver and / or kidneys;
• hypoxemic states (heart or respiratory failure, recent myocardial infarction, shock);
• the infectious diseases, big surgical interventions, injuries, extensive burns and other states demanding performing insulin therapy;
• acute states which can lead to change of function of kidneys:
dehydration, heavy infection, shock, intravascular introduction of iodinated contrast means;
• alcoholism, acute drunkenness;
• porphyria;
• 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 is more senior 60 laid down. performing hard physical activity that is connected with the increased risk of development in them of lactic acidosis.

With care of Glibomet® it is necessary to apply at:
• feverish syndrome;
• diseases of a thyroid gland (with dysfunction);
• hypofunctions of a front share of a hypophysis or bark of adrenal glands.

Overdose:

The overdose or existence of risk factors can provoke development of a lactacidemia as Metforminum is a part of drug. The lactacidemia is the state demanding emergency medical service; treatment of a lactacidemia 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 in oral cavities, 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 moderately severe glucose or solution of sugar are 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:

To store in the dry place at a temperature not above 30 °C. To store medicine in the place, unavailable to children.

Period of validity 3 years. Expiration date of a period of validity of drug is given on a folding cardboard pack and on the blister.

After a period of validity drug cannot be used!

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 400 mg + 2,5 mg.

On 20 tablets in the blister (from aluminum PVC / PVDH/foil).

On 2 blisters together with the application instruction place in a cardboard pack.