Glibomet, pills, 40pcs

Composition

Active ingredients:

metformin hydrochloride-400 mg,

glibenclamide-2.5 mg.

Excipients: 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:

acetyl phthalylcellulose – 2.0 mg,

diethyl phthalate-0.5 mg,

talc-2.5 mg

Pharmacological action

Glibomet® is an oral combined hypoglycemic agent, a second-generation sulfonylurea and bituanide derivative. It has pancreatic and extra-pancreatic effects.

Glibenclamide belongs to the group of second-generation sulfonylurea derivatives. It stimulates insulin secretion by lowering the threshold of glucose stimulation of pancreatic beta cells, increases sensitivity to insulin and the degree of its binding to target cells, increases insulin release, enhances the effect of insulin on glucose uptake by muscles and liver, and inhibits lipolysis in adipose tissue. It acts in the second stage of insulin secretion.

Metformin belongs to the biguanide group. It stimulates the peripheral sensitivity of tissues to the action of insulin (increases the binding of insulin to receptors, enhances the effects. insulin at the post-receptor level), reduces the absorption of glucose in the intestine, suppresses gluconeogenesis and has a beneficial effect on lipid metabolism, helps reduce excess body weight in patients with diabetes mellitus, and also has a fibrinolytic effect by suppressing the tissue-type plasminogen activator inhibitor. The hypoglycemic effect of the drug develops in 2 hours and lasts for 12 hours.

A synergistic combination of two active components of the drug – the stimulating effect of a sulfonylurea derivative on the production of endogenous insulin (pancreatic effect) and the direct effect of biguanide on muscle and adipose tissue (a significant increase in glucose uptake – extra-pancreatic effect) and liver tissue (a decrease in gluconeogenesis), allows for a certain dose ratio to reduce the content of each component. This helps to avoid over-stimulation of pancreatic beta cells, and therefore reduces the risk of impaired pancreatic function, as well as increases the safety of hypoglycemic drugs and reduces the frequency of side effects.

Pharmacokinetics

Glibenclamide is rapidly and fairly fully absorbed (84%) in the gastrointestinal tract (GIT), the time to reach the maximum concentration is 1-2 hours. Binding to plasma proteins is 97%. It is almost completely metabolized in the liver to form inactive metabolites. It is excreted by the kidneys-50% and with bile-50%. The half-life is from 5 to 10 hours. Metformin is fairly fully absorbed in the gastrointestinal tract, quickly distributed in tissues, and practically does not bind to plasma proteins. It is not metabolized in the body, it is excreted unchanged mainly by the kidneys and, partially, by the intestines. The elimination half-life is approximately 7 hours.

Indications

Type 2 diabetes mellitus (if diet therapy and previous therapy with sulfonylureas or biguanides, as well as other oral hypoglycemic agents, are ineffective).

Use during pregnancy and lactation

The use of Glibomet® during pregnancy and lactation is contraindicated.

Contraindications

• hypersensitivity to metformin, glibenclamide or other sulfonylurea derivatives, as well as to other components of the drug; 
• type 1 diabetes mellitus; 
• gestational diabetes;
• diabetic ketoacidosis, diabetic precoma, diabetic coma;
• lactic acidosis (including in the anamnesis);
• conditions accompanied by impaired absorption of food and the development of hypoglycemia;
• impaired liver function;
• acute conditions that can lead to changes in kidney function: dehydration, severe infection, shock, intravascular use of iodine-containing contrast agents; 
• renal failure or impaired renal function (creatinine levels above 135 mmol/l for men and above 110 mmol/l for women);
• infectious diseases, gangrene, major surgery, trauma, acute massive hemorrhage, extensive burns and other conditions requiring insulin therapy;
• hypoxic condition (cardiac or respiratory failure, recent myocardial infarction, shock, severe respiratory disease);
• the period of 48 hours before and 48 hours after the radioisotope or radiological examinations with the use of iodinated contrast agents; 
• a period of 48 hours before and 48 hours after surgery; 
• dystrophic diseases (myotonic dystrophy, lipodystrophy);
• leukopenia;
• porphyria;
• chronic alcoholism, acute alcohol intoxication;
• strict hypocaloric diet (less than 1000 kcal / day);
• glucose-6-phosphodehydrogenase deficiency; 
• pregnancy, breast-feeding period;
• age up to 18 years.

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

With caution

• : febrile syndrome;
• thyroid disorders (with impaired function);
• hypofunction of the anterior pituitary and/or adrenal cortex;
• heavy physical work (risk of lactic acidosis).

Side effects

From the digestive system:  Rarely:  nausea, vomiting, loss of appetite, abdominal pain, diarrhea, metallic taste sensation; in some cases: increased activity of liver enzymes.

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

From the central nervous system:  Infrequently:  headache.

From the side of the skin:  Rarely:  urticaria, erythema, pruritus, photosensitivity.

From the side of metabolism:  Rarely:  hypoglycemia. Very rare:  lactic acidosis.

If you experience symptoms of lactic acidosis (vomiting, abdominal pain, general weakness, muscle cramps), you should immediately stop taking the drug and immediately consult a doctor.

Other services:  disulfiram-like reaction when taking alcohol at the same time (most common signs: redness of the skin of the face and upper body, headache, nausea and vomiting, palpitation, increased blood pressure).

Interaction

The hypoglycemic effect of Glibomet® is enhanced by concomitant use of coumarin derivatives (warfarin, sinkumar), beta-blockers, cimitidine, oxytetracycline, allopurinol, monoamine oxidase (MAO) inhibitors, sulfonamides, phenylbutazone and its derivatives, chloramphenicol, probenecid and salicylates, cyclophosamide, sulfonamide, perhexylin, phenyramidol, miconazole in oral forms, sulfinpyrazone and alcohol.

Epinephrine, glucocorticosteroids, oral contraceptives, thyroid hormone preparations, thiazide diuretics and barbiturates reduce the hypoglycemic effect of Glibomet®.

With simultaneous use, it is possible to increase the effect of anticoagulants. Concomitant use with cimitidine may increase the risk of lactic acidosis. The use of beta-blockers may mask the symptoms of hypoglycemia (with the exception of sweating).

The use of iodine-containing radiopaque preparations (for. intravascular use) can lead to the development of impaired renal function and accumulation of metformin, which increases the risk of lactic acidosis.

How to take, course of use and dosage

Inside. The dose and mode of use of the drug, as well as the duration of treatment, are set 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 per day with the main meal, with a gradual selection of the dose until a stable normalization of the concentration of glucose in the blood plasma is achieved. The maximum daily dose is 6 tablets of Glibomet®.

Overdose

Overdose can trigger the development of lactic acidosis, since the drug contains metformin. Symptoms of lactic acidosis include severe weakness, muscle pain, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, low blood pressure, reflex bradyarrhythmia, confusion and loss of consciousness. If lactic acidosis is suspected, immediate discontinuation of the drug and emergency hospitalization are recommended.

The most effective method for removing lactate and metformin from the body is hemodialysis. Overdose can also lead to the development of hypoglycemia due to the presence of glibenclamide in the drug. Symptoms of hypoglycemia: hunger, increased sweating and palpitation, weakness, pallor of the skin, paresthesia in the oral cavity, tremor, general anxiety, headache, abnormal drowsiness, sleep disorders, fear, impaired coordination of movements, temporary neurological disorders.With the progression of hypoglycemia b, the patient may lose self-control and consciousness.

With mild hypoglycemia, you should take a piece of sugar, food or drinks with a high carbohydrate content (jam, honey, a glass of sweet tea).

In case of loss of consciousness,40-80 ml of 40% dextrose (glucose) solution should be administered intravenously, then 5-10% dextrose solution should be infused. Then you can additionally administer 1 mg of glucagon intravenously (intramuscularly or subcutaneously). If the patient does not regain consciousness, these actions are recommended to be repeated. In the absence of an effect, intensive care is indicated.

Special instructions

During treatment, patients should strictly follow the doctor’s recommendations regarding the dosage and method of use of the drug, as well as concomitant nutrition, exercise regimen and self-monitoring of blood glucose concentration.

Lactic acidosis is a rare and life-threatening pathological condition characterized by the accumulation of lactic acid in the blood, which can be caused by the accumulation of metformin. The described cases of lactic acidosis in patients treated with metformin were observed mainly in patients with diabetes mellitus with severe cardiac and renal insufficiency. Prevention of lactic acidosis 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®, the concentration of serum creatinine should be monitored regularly: – at least once a year in patients with normal renal function; – at least 2-4 times a year in patients with serum creatinine concentrations close to the upper limit of normal, as well as in elderly patients. Caution should be exercised in cases where there is a risk of impaired renal function, for example, when prescribing antihypertensive or diuretic drugs, at the beginning of therapy with nonsteroidal anti-inflammatory drugs (NSAIDs).

Treatment with Glibomet® should be discontinued 48 hours before the X-ray examination with intravenous use of iodine-containing contrast agents and replaced with other hypoglycemic agents (for example, insulin).

The use of Glibomet® should be discontinued 48 hours before elective surgery under anesthesia with spinal or epidural anesthesia. Therapy should be continued after the resumption of oral nutrition, or not earlier than 48 hours after surgery, provided that normal renal function is confirmed.

Alcohol can cause hypoglycemia, as well as a disulfiram-like reaction (nausea, vomiting, abdominal pain, a feeling of heat on the face and upper body, tachycardia, dizziness, headache), so you should refrain from taking alcohol during treatment with Glibomet®.

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

When taking Glibomet® hypoglycaemia may develop and, as a result, a decrease in the ability to concentrate and react; therefore, during treatment with Glibomet®, caution should be exercised when driving vehicles, mechanisms and engaging in potentially dangerous activities.

Form of production

Coated tablets.

Storage conditions

Keep out of reach of children at a temperature not exceeding 30°C.

Shelf

life is 3 years.

Active ingredient

Glibenclamide, Metformin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Type 2 Diabetes