Glybomet, 2.5mg+400 mg 40 pcs

Glibomet® is an oral combined hypoglycemic agent, a sulfonylurea derivative of the II generation and bituanide. It has pancreatic and extrapancreatic effects.

Glibenclamide belongs to the group of sulfonylurea derivatives of the II generation. It stimulates insulin secretion by decrease of glucose irritation threshold of pancreatic beta cells, increases insulin sensitivity and extent of its binding to target cells, increases insulin release, increases insulin influence on glucose absorption by muscle and liver, inhibits lipolysis in adipose tissue. Acts in the second stage of insulin secretion.

Metformin belongs to the group of biguanides. It stimulates peripheral tissue sensitivity to insulin action (increases insulin binding to receptors, increases effects of insulin on postreceptor level), decreases glucose absorption in intestine, inhibits gluconeogenesis and favors lipid exchange, promotes reduction of excess body weight in diabetic patients, and has fibrinolytic effect due to inhibition of tissue plasminogen activator inhibitor.
Hypoglycemic effect of the drug develops in 2 hours and lasts 12 hours.

. Synergetic combination of two active components of the preparation – stimulating effect of sulfonylurea derivative on endogenous insulin production (pancreatic action) and direct effect of biguanide on muscle and fat tissue (significant increase in glucose assimilation – extrapancreatic action) and liver tissue (decrease of gluconeogenesis) – enables to reduce content of each component at certain dose ratio. This helps to avoid excessive stimulation of the beta cells of the pancreas and, therefore, reduce the risk of impairment of its function, and also provides increased safety of hypoglycemic drugs and reduced frequency of side effects.

Pharmacokinetics

. Glibenclamide is rapidly and fairly completely (84%) absorbed in the gastrointestinal tract (GIT), time to reach maximum concentration of 1-2 hours. Blood plasma protein binding is 97%. Almost completely metabolized in the liver with the formation of inactive metabolites. It is excreted by the kidneys – 50% and in the bile – 50%. Period of half-life is from 5 to 10 hours.
Metformin is completely absorbed in the gastrointestinal tract, rapidly distributed in tissues, practically does not bind with blood plasma proteins. It is not metabolized in the body and is excreted unchanged mainly by the kidneys and partially by the intestine. The elimination half-life is about 7 hours.

Indications

Type 2 diabetes

Type 2 diabetes mellitus (if diet therapy and prior therapy with sulfonylurea derivatives or biguanides or other oral hypoglycemic agents are ineffective).

Active ingredient

Glibenclamide, Metformin

Composition

Active ingredients:

metformin hydrochloride – 400 mg,

glibenclamide – 2.5 mg.

Auxiliary substances: core:

microcrystalline cellulose – 65.0 mg,

corn starch – 57.5 mg,

colloidal silicon dioxide – 20.0 mg,

gelatin – 40.0 mg,

glycerin (glycerol) -17.5 mg,

talc – 15.0 mg,

magnesium stearate – 7.5 mg.

Shell:

acetylphthalyl cellulose – 2.0 mg,

diethyl phthalate – 0.5 mg,

talc – 2.5 mg.

How to take, the dosage

Internal administration.
The dose and regimen of the drug, as well as the duration of treatment are established by the attending physician, primarily in accordance with the state of carbohydrate metabolism of the patient, depending on the concentration of glucose in the blood plasma.

As a rule, the initial dose is 1-3 tablets daily with the main meal, with gradual selection of the dose until steady normalization of plasma glucose concentration is achieved. Maximal daily dose is 6 tablets of Glybomet®.

Interaction

The hypoglycemic effect of Glybomet® is increased by concomitant administration of coumarin derivatives (warfarin, syncoumar), beta-adrenoblockers, cimitidine, oxytetracycline, allopurinol, monoamine oxidase inhibitors (MAOIs), Sulfonamides, phenylbutazone and its derivatives, chloramphenicol, probenecid and salicylates, cyclophosamide, sulfonamide, perhexiline, pheniramidol, myconazole in oral forms, sulfinpyrazone and alcohol.

Adrenaline, glucocorticosteroids, oral contraceptives, thyroid hormone drugs, thiazide diuretics and barbiturates decrease the hypoglycemic effect of Glybomet®.

Simultaneous use may increase the effect of anticoagulant drugs.
Simultaneous use with cimitidine may increase the risk of lactoacidosis. The use of beta-adrenoblockers may mask the symptoms of hypoglycemia (except for sweating).

The use of iodine-containing radiopaque agents (for. intravascular administration) may lead to the development of renal dysfunction and cumulation of metformin, which increases the risk of lactoacidosis.

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Special Instructions

During treatment, patients should strictly follow the doctor’s recommendations regarding the dosage and route of administration of the drug, as well as the accompanying diet, exercise regime and self-monitoring of blood plasma glucose concentrations.

Lactoacidosis is a rare and life-threatening pathological condition characterized by the accumulation of lactic acid in the blood, which may be caused by metformin accumulation. Described cases of lactoacidosis in patients treated with metformin were observed mainly in patients with diabetes mellitus with severe cardiac and renal insufficiency. Prevention of lactoacidosis involves identifying all associated risk factors, such as decompensated diabetes mellitus, ketosis, prolonged fasting, excessive alcohol consumption, liver failure, and any condition associated with hypoxia.

When taking Glibomet® preparation serum creatinine concentration should be controlled regularly:
– at least once a year in patients with normal renal function;
– at least 2-4 times a year in patients with serum creatinine concentration close to upper limit of normal and elderly patients. Caution should be observed in cases when there is a risk of renal function impairment, for example, when prescribing hypotensive or diuretics, in the beginning of therapy with non-steroidal anti-inflammatory drugs (NSAIDs).

The treatment with Glibomet® must be stopped 48 hours before the X-ray examination with intravenous administration of iodine-containing contrast agents and replaced with other hypoglycemic agents (e.g., insulin).

The use of Glybomet® must be discontinued 48 hours prior to elective surgery under spinal or epidural anesthesia. The therapy should be continued after resumption of oral nutrition or not earlier than 48 hours after surgical intervention on condition of confirmation of normal renal function.

Alcohol can provoke hypoglycemia as well as disulfiram-like reactions (nausea, vomiting, abdominal pain, fever of the face and upper trunk, tachycardia, dizziness, headache), therefore, alcohol should be avoided during treatment with Glibomet®.

Impact of the drug on the ability to drive vehicles and other mechanisms

Hypoglycemia may occur when taking Glybomet® and as a consequence the ability to concentrate and react may decrease; That is why during the treatment with Glibomet® care should be exercised while driving vehicles and operating machinery as well as during potentially dangerous activities.

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Contraindications

• high sensitivity to metformin, glibenclamide or other sulfonylurea derivatives, or other drug components;
• gestational diabetes;
• diabetic ketoacidosis, diabetic precoma, diabetic coma;
• lactoacidosis (incl.ч. history);
• states accompanied by impaired food absorption and development of hypoglycemia;
• disorders of liver function;
• acute conditions that may lead to changes in renal function: dehydration, severe infection, shock, intravascular administration of iodine-containing contrast agents;
• renal failure or impaired renal function (creatinine level above 135 mmol/L for men and above 110 mmol/L for women);
• hypoxic conditions (cardiac or respiratory failure, recent myocardial infarction, shock, severe respiratory disease);
• period 48 hours before and 48 hours after radioisotopic or radiological studies with iodine contrast agent;
• period within 48 hours before and 48 hours after surgical intervention;
• dystrophic diseases (myotonic dystrophy, lipodystrophy);
• leukopenia;
• porphyria;
• chronic alcoholism, acute alcohol intoxication;
• suffering a strict hypocaloric diet (less than 1000 kcal/day.
• deficiency of glucose-6-phosphodehydrogenase;
• pregnancy, breastfeeding;
• age before 18 years.

The drug is not recommended for persons older than 60 years of age who perform heavy physical work, because of the increased risk of lactoacidosis in them.

With caution

• fever syndrome;
• thyroid disease (with impaired function);
• hypofunction of the anterior pituitary and/or adrenal cortex;
• heavy physical work (risk of lactoacidosis).

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Side effects

Digestive system disorders:
Rarely: nausea, vomiting, loss of appetite, abdominal pain, diarrhea, sensation of metallic taste; in isolated cases: increased activity of liver enzymes.

With the hematopoietic system:
Rarely: leukopenia, thrombocytopenia, erythrocytopenia; very rarely, agranulocytosis, hemolytic or megaloblastic anemia, pancytopenia.

An effect of the central nervous system:
Infrequent: headache.

Skin disorders:
Rare: urticaria, erythema, itching, photosensitization.

Metabolism disorders:
Rarely: hypoglycemia.
Very rarely: lactoacidosis.

In case of symptoms of lactoacidosis (vomiting, abdominal pain, general weakness, muscle cramps) the drug should be stopped immediately and the patient should immediately consult a doctor.

Others: disulfiram-like reaction in concomitant use of alcohol (the most common signs: redness of the skin of the face and upper half of the trunk, headache, nausea and vomiting, palpitations, increased blood pressure).

Overdose

An overdose may provoke lactocidosis because the drug contains metformin. Symptoms of lactocidosis are marked weakness, muscle pain, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, decreased blood pressure, reflex bradyarrhythmia, confusion and loss of consciousness. If lactoacidosis is suspected, immediate withdrawal of the drug and emergency hospitalization is recommended.

The most effective method of removing lactate and metformin from the body is hemodialysis. Overdose can also lead to hypoglycemia due to the presence of glibenclamide in the drug. Symptoms of hypoglycemia: feeling of hunger, increased sweating and palpitation, weakness, pale skin, paresthesia in the mouth, tremor, general restlessness, headache, pathological sleepiness, sleep disorders, feelings of fear, movement coordination disorders, temporary neurological disorders. With progression of hypoglycemia in the patient may lose self-control and consciousness.

In mild hypoglycemia, a piece of sugar, food or drinks with high carbohydrate content (jam, honey, a glass of sweet tea) should be taken orally.

In case of loss of consciousness, 40-80 ml of 40% dextrose (glucose) solution should be administered intravenously, followed by an infusion of 5-10% dextrose solution. Then an additional 1 mg of glucagon may be administered intravenously (intramuscularly or subcutaneously). If the patient does not regain consciousness, it is recommended to repeat these actions. If there is no effect, intensive therapy is indicated.

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Pregnancy use

The use of the drug Glybomet® is contraindicated in pregnancy and during breast-feeding.

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Similarities

Glucovance, Gluconorm, Gluconorm Plus, Metglyb Force