Glucovance pills 2.5 mg + 500 mg 30 pcs
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Active ingredients
Glibenclamide + Metformin
Release form
Pills
Composition
1 tablet contains: Glibenclamide 2.5 mg Metformin hydrochloride 500 mg Supplemental substances: croscarmellose sodium - 14 mg, povidone K30 - 20 mg, microcrystalline cellulose - 56.5 mg, magnesium stearate - 7 mg.
Pharmacological effect
Combined hypoglycemic drug for oral administration. Glucovance is a fixed combination of two oral hypoglycemic agents of different pharmacological groups: metformin and glibenclamide. Metformin belongs to the group of biguanides and reduces the content of both basal and postprandial plasma glucose. Metformin does not stimulate insulin secretion and therefore does not cause hypoglycemia. It has 3 mechanisms of action: - reduces the production of glucose by the liver due to inhibition of gluconeogenesis and glycogenolysis; - increases the sensitivity of peripheral receptors to insulin, the consumption and utilization of glucose by the cells in muscles; - delays glucose absorption from the gastrointestinal tract. total cholesterol, LDL and TG. Glibenclamide belongs to the group of II generation sulfonylurea derivatives. Glucose content when taking glibenclamide is reduced as a result of insulin secretion stimulation by pancreatic β-cells. Metformin and glibenclamide have different mechanisms of action, but mutually complement each other's hypoglycemic activity. The combination of two hypoglycemic agents has a synergistic effect in reducing glucose levels.
Pharmacokinetics
Glibenclamide Absorption and Distribution When ingested, absorption from the gastrointestinal tract is more than 95%. Glibenclamide, which is part of Glucovance, is micronized. Cmax in plasma is reached in about 4 hours. Vd - about 10 liters. Plasma protein binding is 99%. Metabolism and excretion Almost completely metabolized in the liver to form two inactive metabolites, which are excreted by the kidneys (40%) and with bile (60%). T1 / 2 - from 4 to 11 am. Methtformin Absorption and distribution Metetformin after oral administration is absorbed from the gastrointestinal tract quite fully. Cmax in plasma is reached within 2.5 h.Absolute bioavailability ranges from 50 to 60%. Methformin is rapidly distributed in tissues, practically does not bind to plasma proteins. Metabolism and elimination of T1 / 2 averages 6.5 hours. It is metabolized to a very low degree and excreted by the kidneys. Approximately 20-30% of metformin is excreted through the gastrointestinal tract unchanged. The combination of metformin and glibenclamide in a single dosage form has the same bioavailability as when taking pills containing metformin or glibenclamide in isolation. The bioavailability of metformin in combination with glibenclamide is not affected by food intake, as well as the bioavailability of glibenclamide. However, the absorption rate of glibenclamide increases with food intake. Pharmacokinetics in special clinical situations In renal dysfunction, renal clearance decreases, as does CC, while T1 / 2 increases, which leads to an increase in plasma metformin concentration.
Indications
Diabetes mellitus type 2 in adults: - with the ineffectiveness of diet therapy, exercise and previous monotherapy with metformin or a sulfonylurea derivative; - to replace the previous therapy with two drugs (metformin and a sulfonylurea derivative) in patients with stable and well-controlled glycemia.
Contraindications
- type 1 diabetes; - diabetic ketoacidosis; - diabetic precoma, diabetic coma; - renal failure or impaired renal function (CK <60 ml / min); - acute conditions that can lead to changes in renal function: dehydration, severe infection, shock, intravascular injection of iodine-containing contrast agents; - acute or chronic diseases that are accompanied by tissue hypoxia: cardiac or respiratory failure, recent myocardial infarction, shock; - liver failure; - porphyria; - birch menstruality; - lactation period (breastfeeding); - concomitant use of miconazole; - extensive surgical procedures; - chronic alcoholism, acute alcohol intoxication; - lactic acidosis (including a history); - observance of a low-calorie diet (less than 1000 cal / day ); - hypersensitivity to the components of the drug; - hypersensitivity to other sulfonylurea derivatives. It is not recommended to use the drug in patients over the age of 60 years who perform heavy physical work, which is associated with an increased risk of developing them lactacidosis. Glucovance contains lactose,therefore, its use is not recommended for patients with rare hereditary diseases associated with galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.
Precautionary measures
It should be used with caution in febrile syndrome, adrenal insufficiency, hypofunction of the anterior pituitary gland, diseases of the thyroid gland with uncompensated violation of its function.
Use during pregnancy and lactation
The use of the drug is contraindicated in pregnancy. The patient should be warned that during the period of treatment with the drug Glucovance, it is necessary to inform the doctor about the planned pregnancy and the onset of pregnancy. When planning pregnancy, as well as in the event of pregnancy during the period of use of the drug Glucovance, the drug should be canceled and insulin treatment should be prescribed. Glucovance is contraindicated during breastfeeding, since there are no data on the ability of the active substances of the drug to penetrate into breast milk.
Dosage and administration
The dose of the drug is determined by the doctor individually for each patient, depending on the level of glycemia. The initial dose of the drug Glucovance is 1 tab. 2.5 mg / 500 mg or 5 mg / 500 mg 1 time / day. To avoid hypoglycemia, the initial dose should not exceed the daily dose of glibenclamide (or an equivalent dose of another previously taken sulfonylurea drug) or metformin, if they were used as first-line therapy. It is recommended to increase the dose by no more than 5 mg glibenclamide / 500 mg metformin per day every 2 or more weeks to achieve adequate control of blood glucose. Substitution of the previous combination therapy with metformin and glibenclamide: the initial dose should not exceed the daily dose of glibenclamide (or equivalent dose another drug sulfonylurea) and metformin, taken earlier. Every 2 or more weeks after the start of treatment, the dose of the drug is adjusted depending on the level of glycemia. The maximum daily dose is 4 tab. drug Glucovance 5 mg / 500 mg or 6 tab. Glucovance 2.5 mg / 500 mg. The dosing regimen is set individually. For 2.5 mg / 500 mg and 5 mg / 500 mg dosages: - 1 time / day, in the morning during breakfast - with the appointment of 1 tab. per day; - 2 times / day, in the morning and in the evening - with the appointment of 2 or 4 tab. per day. For dosing 2.5 mg / 500 mg: - 3 times / day, in the morning, in the afternoon and in the evening - with the appointment of 3, 5 or 6 tab.per day. For dosage 5 mg / 500 mg: - 3 times / day, in the morning, in the afternoon and in the evening - with the appointment of 3 tab. per day. Tablets should be taken with meals. Each drug intake should be accompanied by the ingestion of a sufficiently high carbohydrate content to prevent the onset of hypoglycemia. For elderly patients, the dose is established taking into account the state of kidney function. The initial dose should not exceed 1 tab. drug Glucovance 2.5 mg / 500 mg. It is necessary to conduct a regular assessment of kidney function. The drug Glucovance is not recommended for use in children.
Side effects
Metabolism: hypoglycemia; rarely, episodes of hepatic porphyria and cutaneous porphyria; very rarely - lactic acidosis. With prolonged use of metformin - a decrease in the absorption of vitamin B12, accompanied by a decrease in its concentration in serum. If megaloblastic anemia is detected, the possibility of such an etiology must be considered. Disulfiram-like reaction when drinking alcohol. On the part of the digestive system: very often - nausea, vomiting, diarrhea, abdominal pain and lack of appetite. These symptoms are more common at the beginning of treatment and in most cases disappear on their own. To prevent the development of these symptoms, it is recommended to take the drug in 2 or 3 doses; a slow increase in the dose of the drug also improves its tolerability. Very rarely - a violation of liver function or hepatitis, requiring discontinuation of treatment. From the blood-forming organs: rarely - leukopenia and thrombocytopenia; very rarely - agranulocytosis, hemolytic anemia, bone marrow aplasia and pancytopenia. These adverse events disappear after drug withdrawal. From the sensory organs: often - a violation of taste (metallic taste in the mouth). At the beginning of treatment, a temporary visual impairment may occur due to a decrease in the glucose content in the blood. From the skin: rarely - itching, maculo-papular rash; very rarely - erythema multiforme, exfoliative dermatitis, photosensitization. Allergic reactions: rarely - urticaria; very rarely - skin or visceral allergic vasculitis, anaphylactic shock. Cross-hypersensitivity reactions to sulfonamides and their derivatives are possible. Laboratory parameters: infrequently - an increase in serum urea and creatinine concentrations from moderate to moderate; very rarely - hyponatremia.
Overdose
Symptoms: hypoglycemia may develop due to the presence of a sulfonylurea derivative. Prolonged overdose or the presence of associated risk factors can trigger the development of lactic acidosis, because The drug includes metformin. Treatment: Mild and moderate symptoms of hypoglycemia without loss of consciousness and neurological manifestations can be corrected by immediate consumption of sugar. You must perform dose adjustment and / or change the diet. The occurrence of severe hypoglycemic reactions in patients with diabetes mellitus, accompanied by coma, paroxysm or other neurological disorders, requires the provision of emergency medical care. It is necessary to / in the introduction of a solution of dextrose immediately after establishing a diagnosis or the occurrence of a suspicion of hypoglycemia, before the patient is hospitalized. After the recovery of consciousness, it is necessary to give the patient food rich in easily digestible carbohydrates (in order to avoid the recurrence of hypoglycemia). Lactic acidosis is a condition requiring emergency medical care; treatment of lactic acidosis should be carried out in the clinic. Hemodialysis is the most effective treatment method that allows lactate and metformin to be removed. Plasma glibenclamide may increase in blood plasma in patients with liver disease. Since glibenclamide is actively associated with blood proteins, the drug is not eliminated during dialysis.
Interaction with other drugs
Contraindicated combinationsGlibenclamide associated with the use of Glucovance miconazole can simultaneously induce hypoglycemia (up to the development of coma). If associated with the use of metformin, depending on the renal function, the drug should be stopped 48 hours before or after i / o administration of iodine-containing contrast agents. using sulfonylurea derivatives: A disulfiram-like reaction (alcohol intolerance) is very rare with one modern ethanol and glibenclamide intake. Taking alcohol can increase the hypoglycemic effect (by inhibiting compensatory reactions or delaying its metabolic inactivation), which can contribute to the development of hypoglycemic coma.During the period of treatment with Glucovance, alcohol and drugs containing ethanol should be avoided. Phenylbutazone increases the hypoglycemic effect of sulfonylurea derivatives (replacing sulfonylurea derivatives at protein-binding sites and / or reducing their elimination). It is preferable to use other anti-inflammatory drugs, which are characterized by a less pronounced interaction, or warn the patient about the need for independent control of the level of glycemia. If necessary, the dose should be adjusted when the anti-inflammatory agent is used together and after it is discontinued. Associated with the use of glibenclamide, Bosentan in combination with glibenclamide increases the risk of a hepatotoxic effect. It is recommended to avoid taking these drugs at the same time. It is also possible to reduce the hypoglycemic effect of glibenclamide. Associated with the use of metformin The risk of developing lactic acidosis increases with acute alcohol intoxication, especially in the case of fasting, or poor nutrition, or liver failure. During the period of treatment with Glucovance, alcohol and drugs containing ethanol should be avoided. Combinations that require caution Associated with the use of all hypoglycemic agents Chlorpromazine in high doses (100 mg / day) causes an increase in glycemia (reducing the release of insulin). With the simultaneous use of the patient should be warned about the need for self-monitoring of blood glucose; if necessary, the dose of the hypoglycemic drug should be adjusted during the simultaneous use of an antipsychotic and after discontinuing its use. The corticosteroids and tetracosactids cause an increase in blood glucose, sometimes accompanied by ketosis (GCS cause a decrease in glucose tolerance). With the simultaneous use of the patient should be warned about the need for self-monitoring of blood glucose; if necessary, the dose of the hypoglycemic agent should be adjusted during the simultaneous use of the corticosteroids and after discontinuation of their use. Danazol has a hyperglycemic effect.If necessary, treatment with danazol and discontinuation of the latter requires a dose adjustment of the drug Glucovance under the control of the glycemic level. Beta2-adrenomimetics due to stimulation of β2-adrenoreceptors increase the concentration of glucose in the blood. With the simultaneous use of the patient should be warned and to establish the control of glucose in the blood, it is possible to transfer to insulin therapy. Diuretics can increase blood glucose. With the simultaneous use of the patient should be warned about the need for self-monitoring of blood glucose; may require dose adjustment of the drug Glucovance during simultaneous use with diuretics and after discontinuation of their use. The use of ACE inhibitors (captopril, enalapril) helps to reduce blood glucose. If necessary, the dose of Glucovance should be adjusted during simultaneous use with ACE inhibitors and after cessation of their use. Associated with the use of metformin Lactacidosis, which occurs when taking metformin against the background of functional renal failure caused by the administration of diuretics, especially loopbacks. , reserpine, guanethidine, and sympathomimetics mask some of the symptoms of hypoglycemia: heartbeat and tachycardia; most non-selective beta-blockers increase the incidence and severity of hypoglycemia. The patient should be warned about the need for self-monitoring of blood glucose, especially at the beginning of treatment. When used simultaneously with fluconazole, an increase in T1 / 2 of glibenclamide occurs with the possible occurrence of manifestations of hypoglycemia. The patient should be warned about the need for self-monitoring of blood glucose; It may be necessary to adjust the dose of the drug Glucovance during simultaneous treatment with fluconazole and after discontinuation of its use. , anticoagulants (coumarin derivatives), MAO inhibitors, chloramphenicol, pent oxyphylline, lipid-lowering drugs from the group of fibrates, disopyramide.
special instructions
During the period of treatment with Glucovance, blood glucose level should be regularly monitored on an empty stomach and after a meal. Lactic acidosis Lactic acidosis is an extremely rare, but serious (high mortality in the absence of emergency treatment) complication that may occur due to cumulation of metformin. Cases of lactic acidosis in patients treated with metformin, occurred mainly in patients with diabetes mellitus with severe renal failure. Other associated risk factors should be considered, such as poorly controlled diabetes, ketosis, prolonged fasting, excessive alcohol consumption, liver failure, and any condition associated with severe hypoxia. The risk of lactic acidosis should be taken into account in the event of the appearance of non-specific signs, such as muscle cramps, accompanied by dyspeptic disorders, abdominal pain and severe indisposition. In severe cases, acidotic dyspnea, hypoxia, hypothermia and coma can be noted. Diagnostic laboratory indicators are: low blood pH, plasma lactate concentration above 5 mmol / l, increased anion interval and lactate / pyruvate ratio. accompanied by the risk of hypoglycemia in the patient. Gradual dose titration after starting treatment can prevent the onset of hypoglycemia. This treatment can only be prescribed to a patient adhering to a regular mealtime (including breakfast). It is important that the consumption of carbohydrates is regular, because the risk of hypoglycemia increases with late meals, inadequate or unbalanced carbohydrate intake. The development of hypoglycemia is most likely with a hypocaloric diet, after an intense or prolonged exercise, while drinking alcohol or taking a combination of hypoglycemic agents. Due to compensatory reactions caused by hypoglycemia, sweating, fear, tachycardia, hypertension, palpitations, stenocardia arrhythmia. The last symptoms may be absent if hypoglycemia develops slowly, in the case of autonomic neuropathy or while taking beta-blockers, clonidine,reserpine, guanethidine, or sympathomimetics. Other symptoms of hypoglycemia in diabetic patients may include headache, hunger, nausea, vomiting, severe fatigue, sleep disorders, agitation, aggression, impaired concentration and psychomotor reactions, depression, confusion, speech disorder, blurred vision, trembling, paralysis, paresthesia, dizziness, delirium, convulsions, drowsiness, unconsciousness, shallow breathing and bradycardia. Careful administration of the drug, dose selection and Proper patient instructions are important for reducing the risk of hypoglycemia. If a patient has bouts of hypoglycemia that are either severe or associated with ignorance of symptoms, consider the possibility of treatment with other hypoglycemic agents. Factors contributing to the development of hypoglycemia: simultaneous use of alcohol, especially during fasting; refusal or (especially for older patients) the inability of the patient to interact with the physician and follow the recommendations outlined in the instructions for use; - poor nutrition, irregular eating, fasting or changes in the diet; - imbalance between exercise and carbohydrate intake; - renal insufficiency; - severe hepatic insufficiency; - overdose of the drug Glucovance; - separate endocrine disorders: insufficiency of the thyroid gland, pituitary and adrenal glands; - simultaneous intake of individual medications. Pharmacokinetics and / or pharmacodynamics may vary in patients with hepatic insufficiency or severe renal insufficiency. Hypoglycemia in such patients may be prolonged, in which case appropriate treatment should be initiated. Blood glucose instability In case of surgery or another cause of diabetes mellitus decompensation, it is recommended to provide a temporary switch to insulin therapy. Symptoms of hyperglycemia are frequent urination, severe thirst, dry skin. After 48 h before a planned surgical intervention or i / v administration of an iodine-containing radiopaque agent, taking Glucovance should be stopped.Treatment is recommended to resume after 48 hours and only after the kidney function has been evaluated and is considered normal. in patients with normal renal function, and 2-4 times a year in elderly patients, as well as in patients with QC on VGN. in old age, or in the case of the beginning of antihypertensive therapy, taking diuretics or NSAIDs. take precautions when driving and working with mechanisms that require increased concentration and speed ps homotornyh reactions.