HLYUKOVANS

Active material: Glibenclamide, Metformin
When ATH: A10BD02
CCF: Oral hypoglycemic agents
ICD-10 codes (testimony): E11
When CSF: 15.02.08
Manufacturer: NYCOMED AUSTRIA GmbH (Austria)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated light orange, kapsulovidnye, lenticular, Engraved “2.5” on one side.

Excipients: povidone K30, magnesium stearate, sodium croscarmellose, microcrystalline cellulose, Opadry (Opadri) OY-L-24 808, Purified water.

15 PC. – blisters (2) – cardboard boxes.
20 PC. – blisters (3) – cardboard boxes.

Pills, coated yellow color, kapsulovidnye, lenticular, Engraved “5” on one side.

Excipients: povidone K30, magnesium stearate, sodium croscarmellose, microcrystalline cellulose, Opadry (Opadri) 31F22700, Purified water.

15 PC. – blisters (2) – cardboard boxes.
20 PC. – blisters (3) – cardboard boxes.

Pharmacological action

Combined hypoglycemic drug for oral use.

Hlyukovans^® a fixed combination of two oral hypoglycemic agents of various pharmacological groups.

Metformin belongs to the group of biguanides and lowers blood glucose in the serum by increasing the sensitivity of peripheral tissues to insulin and increased glucose uptake. Metformin reduces the absorption of carbohydrates from the gastrointestinal tract and inhibits hepatic gluconeogenesis. Also it has a favorable effect on the lipid composition of blood, reducing total cholesterol, LDL and TG.

Glibenclamide belongs to the sulfonylureas II generation. The glucose level when receiving glibenclamide reduced by stimulating insulin secretion β-cells of the pancreas.

Pharmacokinetics

Glibenclamide

Absorption and distribution

After ingestion of absorption from the gastrointestinal tract 48-84%. The time to reach C_max plasma - 1-2 no, V_d – 9-10 l. Plasma protein binding is 95%.

Metabolism and excretion

Almost completely metabolized in the liver with the formation of two inactive metabolites, one of which is excreted by the kidneys, and the other - the bile. T_1/2 It is between 3 to 10-16 no.

Metformin

Absorption and distribution

Once inside absorbed from the gastrointestinal tract adequately. The absolute bioavailability is between 50 to 60%. Simultaneous food intake and reduced absorption of metformin delayed. Metformin is rapidly distributed to the tissues, practically does not bind to plasma proteins.

Metabolism and excretion

It is metabolized to a lesser degree, and excreted in the urine; 20-30% the dose – with feces.

T_1/2 approximately 9-12 no.

Testimony

Diabetes mellitus type 2 adult:

- As a second line when poor diet, exercise and previous therapy with metformin or glibenclamide;

- To replace the previous therapy with two drugs (metformin and glibenclamide) in patients with stable and well-controlled blood glucose levels.

Dosage regimen

The dose determined by the physician individually for each patient, depending on the level of glucose.

Typically, the initial dose Glyukovansa^® is 1 tab. 500 mg / 2.5 mg per day. When replacing the previous combination therapy with metformin and glibenclamide appointed 1-2 tab. Glyukovansa^® 500 mg / 2.5 mg depending on the previous dose level. Every 1-2 weeks after initiation of treatment dose adjusted depending on the level of glycemic.

The tablets should be taken with food.

The maximum daily dose is 4 tab. Glyukovansa^® 500 mg / 2.5 mg or 2 tab. Glyukovansa^® 500 mg / 5 mg.

Side effect

Due to metformin

From the digestive system: early treatment can occur nausea, vomiting, stomach ache, loss of appetite (in most cases, they are their own and do not require special treatment; for the prevention of these symptoms it is recommended to take the drug in 2 or 3 admission; slow increase in the dose of the drug also improves the tolerability); perhaps – “metal” taste in the mouth.

Other: эritema, megaloblastnaya anemia, Lactic acidosis.

Conditional glibenclamide

From the digestive system: nausea, vomiting, epigastric pain, increase in liver enzymes.

From the hematopoietic system: leukopenia, thrombocytopenia; rarely - agranulocytosis, gemoliticheskaya anemia, pancytopenia.

Allergic reactions: – hives, rash, itching.

Other: gipoglikemiâ, “precipitates a effect” by alcohol.

Contraindications

- Diabetes mellitus type 1;

- Diabetic ketoacidosis;

- Diabetic precoma, diabeticheskaya coma;

- Renal failure or renal dysfunction (serum creatinine above 135 mmol / l – for men and above 110 mmol / l – for women);

- Acute conditions, which may result in changes in renal function: degidratatsiya, severe infection, shock, intravascular administration of iodine-containing contrast agents;

- Acute or chronic disease, accompanied by tissue hypoxia: cardiac or respiratory failure, recent myocardial infarction, shock;

- Liver failure;

- Porphyria;

- Pregnancy;

- Lactation (breast-feeding);

- Concomitant use of miconazole;

- State, requiring insulin (incl. infectious diseases, major surgery, injury, extensive burns );

- Abnormal liver function;

- Alcoholism, acute alcohol intoxication;

- Lactic acidosis (incl. history);

- Application for at least 48 hours prior to and during 48 hours after the radioisotope or radiological examinations with administration of iodine-containing contrast agent;

- Compliance with a reduced-calorie diet (less 1000 cal / day);

- Hypersensitivity to metformin, glyburide, or other derivatives of sulfonylurea, as well as auxiliary substances.

It is not recommended to use the drug in people over 60 years, performing heavy physical work, which it is associated with an increased risk of developing lactic acidosis.

FROM caution It should be applied in a feverish syndrome, Thyroid diseases (with impaired), hypofunction of the anterior pituitary or the adrenal cortex, alcoholism.

Pregnancy and lactation

During treatment Glyukovansom^® the patient should inform the doctor about the planned pregnancy and the occurrence of pregnancy. When planning a pregnancy, and in the case of pregnancy while taking Glyukovansa^® the drug should be withdrawn and treatment with insulin.

Hlyukovans^® contraindicated during breastfeeding, since there are no data on its ability to penetrate into breast milk.

Cautions

During treatment Glyukovansom^® should regularly monitor blood glucose fasting and after eating.

Patients should be warned about, if during treatment Glyukovansom^® appear vomiting and abdominal pain, followed by muscle cramps or general malaise, then the drug should be discontinued and seek medical advice immediately, as these symptoms may be signs of lactic acidosis.

The patient must inform the doctor about the appearance of bronchopulmonary infection or urinary tract infection.

For 48 h before surgery or on / in the iodine-containing contrast media reception Glyukovansa^® discontinue. Treatment Glyukovansom^® recommended resumes 48 no.

During treatment is not recommended to drink alcohol.

Effects on ability to drive vehicles and management mechanisms

During treatment Glyukovansom^® should not engage in activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: overdose or risk factors can trigger the development of lactic acidosis, tk. of the drug include metformin. Lactic acidosis is a condition, medical emergency; treatment of lactic acidosis must be carried out in the clinic. The most effective method of treatment is hemodialysis.

Overdosing can also cause hypoglycemia due to presence of a drug glibenclamide. Symptoms of hypoglycemia: hunger, increased sweating, weakness, heartbeat, pale skin, paresthesia oral, tremor, general anxiety, headache, abnormal sleepiness, sleep disorders, a sense of fear, dystaxia, Temporary neurological disorders. With the progression of hypoglycemia may lose self-control and awareness.

Treatment: hypoglycemia mild or moderate glucose or sugar solution taken orally.

In the case of severe hypoglycemia (loss of consciousness) introducing / in 40% Dextrose (Glucose) or glucagon / in, / m, n / a. After regaining consciousness of the patient is necessary to give food, rich in carbohydrates, in order to avoid a recurrence of hypoglycemia.

Patients with liver disease may increase the clearance of glibenclamide. Glibenclamide is not displayed during dialysis, Since the activity of proteins associated with blood.

Drug Interactions

Preparations, reinforcing action Glyukovansa^® (increasing the risk of hypoglycemia)

In an application with Glyukovansom^® miconazole may provoke hypoglycemia (until the development of coma).

Флуконазол увеличивает T_1/2 sulfonylureas and increase the risk of hypoglycemic reactions.

Drinking alcohol increases the risk of hypoglycemic reactions (until the development of coma). During treatment Glyukovansom^® Avoid drinking alcohol and drugs, containing ethanol (alcohol).

The use of ACE inhibitors (captopril, Enalapril) It increases the risk of hypoglycemic reactions in patients with diabetes mellitus for the treatment of sulfonylureas by improving glucose tolerance and decrease the need for insulin.

Beta-blockers increase the frequency and severity of hypoglycemia. Beta-blockers mask the symptoms of hypoglycemia, palpitations and tachycardia.

Preparations, reduces the effect of Glyukovansa^®

Danazol has a hyperglycemic effect. If necessary, danazol treatment and discontinuation of the last requires dose adjustment Glyukovansa^® under the control of blood glucose levels.

Chlorpromazine high doses (100 mg / day) It causes an increase in blood glucose.

Corticosteroids increase glycemia and can lead to the development of ketoacidosis.

Beta₂-adrenostimulyatorov due to stimulation of β₂-adrenergic receptors increase blood glucose levels.

Diuretic (especially “loop”) provoke the development of ketoacidosis due to the development of functional renal failure.

In / in the introduction of iodine-containing contrast agents can cause renal failure, which in turn lead to drug accumulation in the body and the development of lactic acidosis.

Beta-blockers mask the symptoms of hypoglycemia, like palpitations, and tachycardia.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 3 year.