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Active ingredients
Glibenclamide
Release form
Pills
Composition
1 tablet contains: Glibenclamide 2.5 mg Metformin hydrochloride 400 mg Supplementary substances: microcrystalline cellulose - 65 mg, corn starch - 57.5 mg, colloidal silicon dioxide - 20 mg, gelatin - 40 mg, glycerol - 17.5 mg, talc - 15 mg, magnesium stearate - 7.5 mg. Coat composition: acetylphthalyl cellulose - 2 mg, diethyl phthalate - 0.5 mg, talc - 2.5 mg.
Pharmacological effect
Combined oral hypoglycemic drug, contains a second-generation sulfonylurea derivative and biguanide. It has pancreatic and extra-pancreatic effects. Glibenclamide is a sulfonylurea derivative of the second generation. It stimulates insulin secretion by lowering the glucose stimulation threshold of β-cells of the pancreas, increases insulin sensitivity and its binding to target cells, increases insulin release, enhances the effect of insulin on glucose absorption by muscles and liver, inhibits lipolysis in adipose tissue. It acts in stage II of insulin secretion. Metformin refers to the group of biguanides. Stimulates the peripheral sensitivity of tissues to the action of insulin (increases insulin binding to receptors, enhances the effects of 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 to reduce overweight in patients with diabetes, also has a fibrinolytic effect due to the suppression of a tissue type plasminogen activator inhibitor. The hypoglycemic effect of the drug develops through 2 hours and lasts 12 hours. A synergistic combination of two active ingredients of the drug - the stimulating effect of the 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 absorption - extrapancreatic effect) and liver tissue (decrease gluconeogenesis), allows at a certain dose ratio to reduce the content of each component. This helps to avoid excessive stimulation of β-cells of the pancreas, and, consequently, reduce the risk of dysfunction, and also provides increased safety of hypoglycemic drugs and reduced frequency of side effects.
Pharmacokinetics
Glibenclamide Absorption and distribution is rapidly and completely (84%) absorbed from the gastrointestinal tract, the time to reach Cmax is 1-2 hours. Plasma protein binding is 97%. Metabolism and elimination Almost completely metabolized in the liver to inactive metabolites. Excreted by the kidneys (50%) and with bile (50%). T1 / 2 is from 5 to 10 hours. Metformin Absorption and distribution Absolutely fully absorbed in the gastrointestinal tract, quickly distributed in the tissue, practically does not bind to plasma proteins. Metabolism and elimination Does not metabolize in the body, is excreted unchanged mainly by the kidneys and, in part, intestines. T1 / 2 is approximately 7 hours.
Indications
- diabetes mellitus type 2 with the ineffectiveness of diet and prior therapy with sulfonylurea or biguanide derivatives, as well as other oral hypoglycemic agents.
Contraindications
- type 1 diabetes mellitus; - gestational diabetes mellitus; - diabetic ketoacidosis, diabetic precoma, diabetic coma; - lactic acidosis (including in history); - conditions involving impaired food absorption and the development of hypoglycemia; - impaired liver function; - Acute conditions that can lead to changes in kidney function (dehydration, severe infection, shock, intravascular injection 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, large surgical interventions, injuries, acute massive blood loss, extensive burns and other conditions requiring insulin therapy; - hypoxic conditions (heart or respiratory failure, recent myocardial infarction, shock, serious diseases respiratory tract); - 48 hours before the start and 48 hours after radioisotope or x-ray studies with the introduction of iodine-containing contrast agent; - period for 48 hours before the start and 48 hours after the test surgical interventions; - dystrophic diseases (myotonic dystrophy, lipodystrophy); - leukopenia; - porphyria; - chronic alcoholism, acute alcohol intoxication; - adherence to a strict low-calorie diet (less than 1000 kcal / day); - glucose-6-phosphate dehydrogenase deficiency; - pregnancy; - lactation period (breastfeeding); - children and adolescents under 18 years of age; - hypersensitivity to metformin, glibenclamide or other sulfonylurea derivatives,as well as to other components of the drug. It is not recommended to use the drug in patients over 60 years old who perform hard physical work, which is associated with an increased risk of developing lactic acidosis in them.
Precautionary measures
With caution should use the drug for febrile syndrome; thyroid diseases (with impaired function); hypofunction of the anterior lobe of the pituitary and / or the adrenal cortex.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation (breastfeeding).
Dosage and administration
The drug is taken orally during the meal. The dosage mode and duration of treatment are set by the attending physician depending on the state of carbohydrate metabolism and on the concentration of glucose in the blood. The initial dose is usually 1-3 tab./day with a further gradual selection of the effective dose until reaching stable normalization of glucose concentration in the blood. The maximum daily dose of the drug Glibomet is 6 tab.
Side effects
On the part of the digestive system: rarely - nausea, vomiting, loss of appetite, abdominal pain, diarrhea, metallic taste in the mouth; in some cases - an increase in liver enzymes. From the hematopoietic system: rarely - leukopenia, thrombocytopenia, erythrocytopenia; very rarely - agranulocytosis, hemolytic or megaloblastic anemia, pancytopenia. On the CNS side: infrequently - headache. On the skin side: rarely - urticaria, erythema, pruritus, photosensitivity. On the side of metabolism: rarely - hypoglycemia; very rarely - lactic acidosis. When symptoms of lactic acidosis appear (vomiting, abdominal pain, general weakness, muscle cramps), it is necessary to immediately stop taking the drug and consult a doctor promptly. Other: disulfiram-like reaction while taking alcohol (the most common signs are reddening of the skin and upper torso, headache, nausea and vomiting, palpitations, increased blood pressure).
Overdose
Symptoms: lactic acidosis is possible (caused by the action of metformin), hypoglycemia (caused by the action of glibenclamide). Symptoms of lactic acidosis: severe weakness, muscle pain, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain,hypothermia, lowering blood pressure, reflex bradyarrhythmia, confusion and loss of consciousness. Symptoms of hypoglycemia: hunger, increased sweating, weakness, palpitations, pallor of the skin, paresthesia in the mouth, tremor, general anxiety, headache, pathological drowsiness, sleep disorders, feeling fear, incoordination, temporary neurological disorders. With the progression of hypoglycemia, loss of self-control and consciousness is possible. Treatment: if lactic acidosis is suspected, immediate withdrawal of the drug and emergency hospitalization are recommended. Hemodialysis is the most effective treatment method. In mild hypoglycemia, a piece of sugar, food or drinks with a high carbohydrate content (jam, honey, a cup of sweet tea) should be ingested. If unconscious, 40-80 ml of a 40% dextrose solution is necessary. (glucose), then hold an infusion of 5-10% dextrose solution. Then you can additionally enter 1 mg of glucagon in / in, in / m or s / c. If the patient does not regain consciousness, these actions are recommended to be repeated. In the absence of effect, intensive therapy is indicated.
Interaction with other drugs
Hypoglycemic effect of glibium miconazole (for oral administration), sulfinpirazon and ethanol. Adrenaline, GCS, oral contraceptives, thyroid hormone drugs, thiazide diuretics and barbiturates mind The hypoglycemic effect of the drug Glibomet. If used simultaneously with the drug Glibomet, the effect of anticoagulants may be enhanced. Simultaneous use with cimetidine may increase the risk of developing lactic acidosis. Applying beta-adrenergic blockers may mask the symptoms of hypoglycemia (except for excessive sweating). ) can lead to impaired renal function and cumulation of metformin, which increases the risk of lactic acidosis.
special instructions
During treatment, patients must strictly follow the doctor's recommendations regarding the dosage and method of use of the drug, as well as dieting, exercise and self-monitoring of blood glucose levels. Lactic acidosis is a rare and life-threatening pathological condition characterized by the accumulation of lactic acid in the blood which can be cumulation metformin. The described cases of lactic acidosis in patients treated with metformin were observed mainly in patients with diabetes mellitus with severe heart and renal failure. Prevention of lactic acidosis involves the determination of all associated risk factors, such as decompensated diabetes, ketosis, prolonged fasting, excessive alcohol consumption, liver failure, and any condition associated with hypoxia. When taking the drug Glibomet, you should regularly monitor the concentration of serum creatinine: - at least 1 time per year in patients with normal renal function - at least 2-4 times per year in patients with serum creatinine concentrations close to VGN, as well as in patients n residential vozrasta.Sleduet caution in cases where there is a risk of renal dysfunction, for example, the appointment of antihypertensive or diuretic, at the beginning of therapy, NSAIDs. Treatment with Glibomet should be stopped 48 hours before X-ray examination with i / v administration of iodine-containing contrast agents and replaced with other hypoglycemic drugs (eg, insulin) by therapy. Glibomet should be stopped 48 hours before a planned operation under general anesthesia, with spinal or epidural anesthesia. The therapy should be continued after the resumption of oral nutrition or not earlier than 48 hours after surgery, provided that normal kidney function is confirmed. Ethanol can provoke the development of hypoglycemia, as well as a disulfiram-like reaction (nausea, vomiting, abdominal pain, sensation of heat on the face and upper parts of the body, tachycardia, dizziness, headache), so you should refrain from drinking alcohol during treatment with Glibomet. Impact on the ability to drive motor vehicles and control mechanisms. When taking the drug Glibomet, hypoglycemia may develop, and, as a result, the ability to concentrate and the speed of psychomotor reactions may decrease,therefore, during the period of drug treatment, caution should be exercised when driving vehicles, machinery, and occupations of potentially hazardous activities.