Metformin tablets p/o 850mg №10×3

Name:
Metformin. Forms of release Tablets. INN Metformin. FTGHypoglycemic agent for oral use of the biguanide group.
Description:
Coated tablets with a biconvex surface, green; tablets with a dosage of 500 mg and 1000 mg – with a risk, a dosage of 850 mg – without a risk. Composition Each tablet contains: active ingredient – metformin hydrochloride – 500 mg or 850 mg, or 1000 mg; excipients – starch 1500 (corn starch partially pregelatinized), povidone, sodium croscarmellose, magnesium stearate, microcrystalline cellulose, opadry II (contains: polyvinyl alcohol, macrogol 3350, talc, titanium dioxide E 171, indigo carmine E 132, yellow quinoline E 104) . Pharmacotherapeutic group Medicines for the treatment of diabetes mellitus. Drugs for lowering blood glucose levels, except for insulin. ATX code: A10BA02. Pharmacological properties Pharmacodynamics Metformin reduces hyperglycemia, does not lead to the development of hypoglycemia. Unlike sulfonylurea, it does not stimulate insulin secretion and does not cause a hypoglycemic effect in healthy individuals. Reduces in the blood plasma both the initial glucose level and the glucose level after a meal. The hypoglycemic effect of metformin can be realized through three mechanisms: – reduction of glucose production in the liver due to inhibition of gluconeogenesis and glycogenolysis; – improving the capture and utilization of peripheral glucose in the muscles by increasing insulin sensitivity; – delayed absorption of glucose in the intestine. Metformin stimulates intracellular glycogen synthesis by influencing glycogen synthetase. Increases the transport capacity of all types of membrane glucose transporters (GLUT). Regardless of its effect on glycemia, metformin causes a positive effect on lipid metabolism: it reduces the content of total cholesterol, LDL and triglycerides. Increases the sensitivity of peripheral receptors to insulin and the utilization of glucose by cells. Inhibits gluconeogenesis in the liver. Delays the absorption of carbohydrates in the intestines. Pharmacokinetics After oral administration, it is rapidly absorbed from the gastrointestinal tract. Absolute bioavailability on an empty stomach is 50 – 60%. The maximum concentration (Cmax) is reached after about 2.5 hours, intake with food reduces Cmax by 40% and slows down its achievement by 35 minutes. Plasma concentration does not exceed 1 μg / ml. The volume of distribution (Vd) is 296 – 1012 liters. Communication with plasma proteins is insignificant, it can accumulate in erythrocytes. The half-life (T½) is about 6.5 hours (initial T½ from 1.7 to 3 hours, terminal – from 9 to 17 hours). The renal clearance makes more than 400 ml/min. It is excreted by the kidneys, mainly unchanged (glomerular filtration and tubular secretion) and through the intestines (up to 30%). In renal insufficiency, clearance decreases in proportion to creatinine clearance. T½ lengthens, there is a risk of cumulation of the drug and the concentration of metformin in plasma increases. Indications for use Diabetes mellitus type II (insulin-independent) with the ineffectiveness of diet therapy, especially in obese patients: – as monotherapy or combination therapy in conjunction with other oral hypoglycemic agents or in combination with insulin for the treatment of adults. – as monotherapy or combination therapy with insulin for the treatment of children over 10 years of age. Dosage and administration Monotherapy or combination therapy in conjunction with other oral hypoglycemic agents. Adults. The usual initial dose is 500 mg or 850 mg of metformin 2 to 3 times a day during or after meals. After 10 to 15 days of treatment, the dose must be adjusted according to the results of measurements of glucose levels in the blood serum. Gradual increase in dose helps to reduce side effects from the digestive tract. The maximum recommended dose is 3000 mg per day, divided into 3 doses. In the treatment of high doses, the drug Metformin, coated tablets 1000 mg, is used. In the case of switching to treatment with the drug Metformin, coated tablets, it is necessary to stop taking another antidiabetic agent. Combination therapy in combination with insulin. To achieve better control of blood glucose levels, metformin and insulin can be used as a combination therapy. The usual starting dose is 500 mg or 850 mg metformin 2 to 3 times a day, while the insulin dose is titrated according to blood glucose measurements. Monotherapy or combination therapy in combination with insulin. Children. Metformin is prescribed for children over 10 years of age. The usual starting dose is 500 mg or 850 mg Metformin once daily with or after meals. After 10 to 15 days of treatment, the dose must be adjusted according to the results of measurements of glucose levels in the blood serum. Gradual increase in dose helps to reduce side effects from the digestive tract. The maximum recommended dose is 2000 mg per day, divided into 2 to 3 doses. In elderly patients, deterioration of renal function is possible, therefore the dose of metformin should be selected on the basis of an assessment of renal function, which must be carried out regularly. Side effects Side effects according to the frequency of occurrence are classified into the following categories: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1 /10000 and <1/1000), very rarely (<1/10000). From the side of the nervous system. Often: taste disturbance. From the digestive tract. Very common: nausea, vomiting, diarrhea, abdominal pain, lack of appetite, metallic taste in the mouth, flatulence. Most often, these side effects occur at the beginning of treatment and, as a rule, spontaneously disappear. To prevent the occurrence of side effects from the gastrointestinal tract, it is recommended to slowly increase the dosage and use the drug 2-3 times a day during or after meals. From the side of the blood system. Very rare: megaloblastic anemia. From the skin and subcutaneous tissue. Very rare: skin rash, erythema, pruritus, urticaria. Metabolism. Very rare: lactic acidosis. With prolonged use of the drug, the absorption of vitamin B12 may decrease, which is accompanied by a decrease in its level in the blood serum. It is observed when prescribing metformin to patients with megaloblastic anemia. From the hepatobiliary system. Very rare: abnormal liver function tests or hepatitis, which completely disappear after discontinuation of metformin. Allergic reactions: very rarely: erythema, itching, skin rash. In cases of side effects, the dose should be reduced or temporarily discontinued. Contraindications - hypersensitivity to metformin and other biguanides; - diabetic ketoacidosis, diabetic precoma and coma; - chronic renal failure (with a serum creatinine level of more than 1.5 mg / dl in men and 1.4 mg / dl in women or creatinine clearance less than 60 ml / min); - violations of liver function (lack of liver function above II degree according to Child-Pugh); - conditions that can contribute to the development of lactic acidosis, incl. chronic heart failure, acute myocardial infarction, respiratory failure, acute cerebrovascular accident, dehydration, drinking with alcohol; - lactic acidosis (including history); - hypocaloric diet (less than 1000 kcal/day); - pregnancy and lactation; - children's age up to 10 years; - the drug is not prescribed 2 days before surgery, radioisotope, x-ray studies with the introduction of contrast drugs and within 2 days after they are carried out; - acute conditions that occur with a risk of developing renal dysfunction: dehydration of the body; fever, severe infectious diseases; clinical expression of manifestations of acute and chronic diseases that can lead to the development of tissue hypoxia (heart or respiratory failure, acute myocardial infarction, shock, sepsis, kidney infections, bronchopulmonary diseases); - acute alcohol intoxication, alcoholism; - major surgery and trauma (when insulin therapy is indicated); - It is not recommended to use the drug in people over 60 years of age who perform heavy physical activity. Precautions Lactic acidosis is a rare but severe metabolic complication that can occur as a result of metformin accumulation. Cases of lactic acidosis have been reported in patients with diabetes mellitus and severe renal failure. Risk factors for lactic acidosis: poorly controlled diabetes mellitus, ketosis, prolonged fasting, excessive alcohol consumption, liver failure, or any condition associated with hypoxia. Lactic acidosis is characterized by muscle cramps, acidotic dyspnea, abdominal pain and hypothermia, and coma may develop in the future. Laboratory signs of the development of lactic acidosis are an increase in the level of serum lactate more than 5 mmol / l, a decrease in blood pH against the background of electrolyte disturbances and an increase in the lactate / pyruvate ratio. If lactic acidosis is suspected, it is necessary to stop the use of the drug and immediately hospitalize the patient. Renal failure. Since metformin is excreted by the kidneys, serum creatinine levels should be checked before and during treatment with metformin, especially in patients with impaired renal function and in elderly patients. Caution should be exercised in cases where renal function may be impaired, for example, at the beginning of treatment with antihypertensive drugs, diuretics and at the beginning of NSAID therapy. Iodine-containing radiopaque agents. When conducting radiological studies using radiopaque agents, it is necessary to stop the use of Metformin 48 hours before the study and not resume earlier than 48 hours after the X-ray examination and assessment of renal function. Surgical interventions. It is necessary to stop the use of metformin 48 hours before the planned surgical intervention, and not resume earlier than 48 hours after the operation and evaluation of renal function. Children. According to the results of clinical studies, there was no effect of metformin on growth and puberty in children. However, there are no data on the effect of metformin on growth and puberty with long-term use of the drug, so the drug should be used with extreme caution in children during puberty, especially those aged 10 to 12 years. Patients need to follow a diet and monitor laboratory parameters. With the combined use of metformin with insulin or sulfonylurea derivatives, an increase in the hypoglycemic effect is possible. Influence on the ability to drive vehicles and control mechanisms When the drug is combined with other hypoglycemic drugs (sulfonylurea derivatives, insulin), hypoglycemic conditions may develop, in which the ability to drive vehicles and other potentially hazardous activities that require increased attention and speed of psychomotor reactions deteriorate. Use during pregnancy and lactation The drug is contraindicated for use during pregnancy and during breastfeeding. If pregnancy is planned or occurs, Metformin should be discontinued and insulin therapy prescribed. The patient should be warned about the need to notify the doctor in case of pregnancy. The mother and child should be monitored. It is not known whether metformin is excreted in breast milk. If necessary, the use of the drug during lactation should stop breastfeeding. OverdoseSymptoms: hypoglycemia with the use of metformin in doses up to 85 g / day is not observed, but lactic acidosis develops. Early symptoms are severe weakness, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, lowering blood pressure, reflex bradyarrhythmia, muscle pain, later on, rapid breathing, dizziness, disturbance and loss of consciousness and development of coma. Treatment: if signs of lactic acidosis appear, treatment with metformin should be stopped, the patient should be urgently hospitalized, the concentration of lactate should be determined. Hemodialysis is most effective for removing lactate and metformin from the body. If necessary, carry out symptomatic therapy (intravenous sodium bicarbonate, hypotonic sodium chloride solution). Interaction with other drugs Incompatible with ethanol, loop diuretics, iodine-containing radiopaque agents, as it increases the risk of lactic acidosis, especially in cases of starvation or a low-calorie diet. During the use of metformin, the use of alcoholic beverages and drugs containing alcohol should be avoided. When conducting an x-ray examination, the drug must be canceled 48 hours before and not renewed within 2 days after the study. Use with caution in combination with indirect anticoagulants and cimetidine. Sulfonylureas, insulin, acarbose, monoamine oxidase inhibitors, oxytetracycline, angiotensin-converting enzyme inhibitors, clofibrate, cyclophosphamide and salicylates enhance the action of metformin. With simultaneous use with glucocorticosteroids, injectable beta-agonists, combined oral contraceptives, danazol, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives (chlorpromazine), nicotinic acid, thiazide diuretics, the effect of metformin may decrease. Nifedipine increases absorption, Cmax, slows down excretion. Cationic substances (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, and vancomycin) compete for tubular transport systems and, with long-term therapy, can increase Cmax by 60%. Upakovka10 tablets in a blister pack of PVC film and aluminum foil. 3 blister packs, together with the leaflet, are placed in a pack of cardboard (No. 10x3). Storage conditions In a place protected from light and moisture, at a temperature not exceeding 25ºС. Keep out of the reach of children. Shelf life 2 years. Do not use the drug after the expiration date. Conditions for dispensing from pharmacies By prescription. Buy Metformin tablets p/o 850mg No. 10x3