Siofor tablets 500mg, No. 60

Diabetes mellitus type 2, especially in overweight patients with ineffective diet and exercise.

It can be used as monotherapy or in combination with other oral hypoglycemic drugs and insulin.

The drug should be taken orally during or after meals.

The dose and regimen of taking the drug, as well as the duration of treatment, are set by the attending physician, depending on the level of glucose in the blood.

Adults

Monotherapy

The recommended initial dose is 500 mg (1 tab.SioforЃ 500 or 1/2 tab.SioforЃ 1000) 1-2 times / day or 850 mg (1 tab.SioforЃ 850) 1 time / day. 10-15 days after the start of taking the drug, a further gradual increase in the dose is possible, depending on the level of glucose in the blood, up to an average daily dose: 3-4 tab. drug SioforЃ 500, 2-3 tab. drug SioforЃ 850 or 2 tab. the drug SioforЃ 1000.

A gradual increase in the dose reduces the number of adverse effects from the gastrointestinal tract. The maximum dose is 3000 mg / day in 3 divided doses (6 tablets of SioforЃ 500 or 3 tablets of SioforЃ 1000). For patients who are prescribed high doses (2000-3000 mg / day), it is possible to replace 2 tablets. the drug SioforЃ 500 per 1 tab. the drug SioforЃ 1000.

When transferring a patient to treatment with SioforЃ from therapy with another antidiabetic drug, stop taking the latter and start taking SioforЃ in the doses indicated above.

Combined use with insulin SioforЃ and insulin can be combined to improve glycemic control.

The standard initial dose is 500 mg (1 tab.SioforЃ 500 or 1/2 tab.SioforЃ 1000) 1-2 times / day or 850 mg (1 tab.SioforЃ 850) 1 time / day, with a gradual increasing the dose at intervals of approximately one week to an average daily dose of 3-4 tab. drug SioforЃ 500, 2 tab. the drug Siofor 1000 or 2-3 tab. SioforЃ 850; the insulin dose is determined based on the blood glucose concentration. The maximum dose is 3000 mg / day in 3 divided doses.

Due to the possible impairment of renal function in elderly patients, the dose of SioforЃ is selected taking into account the concentration of creatinine in the blood plasma.

Regular assessment of the functional state of the kidneys is required.

Children aged 10 to 18

Monotherapy and combined use with insulin

The standard initial dose is 500 mg (1 tab.SioforЃ 500 or 1/2 tab.SioforЃ 1000) 1 time / day or 850 mg (1 tab.SioforЃ 850) 1 time / day. 10-15 days after the start of taking the drug, a further gradual increase in the dose is possible, depending on the level of glucose in the blood. A gradual increase in the dose reduces the number of adverse effects from the gastrointestinal tract. The maximum dose for children is 2000 mg / day (4 tablets of SioforЃ 500 or 2 tablets of SioforЃ 1000) in 2-3 doses. Insulin dosage is determined based on blood glucose levels.

White coated tablets, round, biconvex.

1 tab.

metformin hydrochloride 500 mg

Excipients: hypromellose - 17.6 mg, povidone - 26.5 mg, magnesium stearate - 2.9 mg.

• Diabetic ketoacidosis, diabetic precoma;

• renal failure or impaired renal function (CC <60 ml / min);

• acute conditions that can have a negative effect on kidney function (for example, dehydration, severe infectious disease);

• intravascular administration of an iodine-containing contrast agent;

• acute or chronic diseases that can cause tissue hypoxia (for example, heart or respiratory failure, recent myocardial infarction, shock);

• liver failure; lactic acidosis (including history);

• pregnancy;

• lactation period (breastfeeding);

• acute alcohol intoxication, chronic alcoholism;

• adherence to a low-calorie diet (less than 1000 kcal / day);

• children under 10 years of age.

• hypersensitivity to metformin or other components of the drug.

• The drug should be used with caution in children aged 10 to 12 years; in patients over 60 years of age who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis in them.

pharmachologic effect

A hypoglycemic drug from the biguanide group. Provides a decrease in both basal and postprandial blood glucose concentration. Does not stimulate insulin secretion and therefore does not lead to hypoglycemia. The action of metformin is probably based on the following mechanisms: a decrease in the production of glucose in the liver due to inhibition of gluconeogenesis and glycogenolysis; increasing the sensitivity of muscles to insulin and, therefore, improving the absorption of glucose in the periphery and its utilization; inhibition of glucose absorption in the intestine. Metformin, through its action on glycogen synthetase, stimulates intracellular glycogen synthesis. Increases the transport capacity of all hitherto known membrane transport proteins of glucose. Regardless of the effect on blood glucose levels, it has a beneficial effect on lipid metabolism,leads to a decrease in total cholesterol, low-density cholesterol and triglycerides.

Pharmacokinetics

Suction

After oral administration, Cmax in blood plasma is reached after about 2.5 hours and does not exceed 4 ?g / ml at the maximum dosage. With food intake, absorption decreases and slows down slightly. The absolute bioavailability in healthy patients is approximately 50-60%.

Distribution

Practically does not bind to plasma proteins. Average Vd is 63-276 liters. Accumulates in salivary glands, muscles, liver and kidneys. Penetrates into erythrocytes.

Withdrawal

It is excreted by the kidneys unchanged. Renal clearance is> 400 ml / min. T1 / 2 is about 6.5 hours.

Pharmacokinetics in special clinical situations

With a decrease in renal function, the clearance of metformin decreases in proportion to the clearance of creatinine. Thus, T1 / 2 is lengthened and the concentration of metformin in plasma increases.

Side effect

From the nervous system: often - taste disturbance. From the digestive system: nausea, vomiting, 'metallic' taste in the mouth, lack of appetite, diarrhea, abdominal pain. These adverse events often occur at the beginning of therapy and in most cases go away spontaneously. To prevent the onset of symptoms, the dose of the drug is recommended to be divided into 2-3 doses during or after meals. A gradual increase in the dose reduces the likelihood of adverse effects from the gastrointestinal tract. Allergic reactions: very rarely - skin reactions (eg, flushing, itching, urticaria). From the side of metabolism: very rarely: - lactic acidosis (requires discontinuation of treatment). With prolonged use, there is a decrease in the absorption of vitamin B12 and a decrease in its concentration in the blood plasma.This should be taken into account if the patient has megaloblastic anemia. On the part of the liver and biliary tract: individual reports - reversible liver dysfunction, expressed in an increase in the activity of hepatic transaminases, or hepatitis, which disappears after stopping metformin.

Application during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding). The patient should be warned about the need to notify the doctor in case of pregnancy. When planning or the onset of pregnancy in a patient with type 2 diabetes mellitus, the drug should be canceled, with the help of insulin therapy, the blood glucose level should be normalized or as close to normal as possible in order to reduce the risk of developing fetal defects due to the pathological effects of hyperglycemia. Metformin passes into the milk of laboratory animals. There are no similar data for humans, so a decision should be made to stop breastfeeding or to discontinue SioforЃ taking into account the need to use the drug in the mother.

Application for violations of liver function

The drug is contraindicated in liver failure.

Application for impaired renal function

The drug is contraindicated in renal failure or impaired renal function (CC <60 ml / min);

Application in children

The use of the drug is contraindicated in children under the age of 10 years. The drug should be used with caution in children aged 10 to 12 years.

Use in elderly patients

The drug should be used with caution in patients over 60 years of age who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis in them.

special instructions

Lactic acidosis is a serious pathological condition that is extremely rare, associated with the accumulation of lactic acid in the blood, which can be caused by the accumulation of metformin. The described cases of the development of lactic acidosis in patients receiving metformin were observed mainly in patients with diabetes mellitus with severe renal failure. Prevention of lactic acidosis involves identifying all associated risk factors, such as decompensated diabetes, ketosis, prolonged fasting, excessive alcohol consumption, liver failure, and any condition associated with hypoxia. If you suspect the development of lactic acidosis, immediate withdrawal of the drug and emergency hospitalization are recommended. Since metformin is excreted by the kidneys, the concentration of creatinine in the blood plasma should be determined before starting treatment, and then regularly.Particular care should be taken in cases where there is a risk of impaired renal function, for example, at the beginning of therapy with antihypertensive drugs, diuretics or NSAIDs. Treatment with SioforЃ must be temporarily replaced with therapy with other hypoglycemic drugs (for example, insulin) 48 hours before and 48 hours after the X-ray examination with intravenous administration of iodine-containing contrast agents. The use of SioforЃ should be discontinued 48 hours before the planned surgery under general anesthesia, with spinal or epidural anesthesia. Continue therapy should be after resumption of oral nutrition or no earlier than 48 hours after surgery, provided that normal renal function is confirmed.SioforЃ is not a substitute for diet and daily exercise - these therapies must be combined according to your doctor's recommendations. During treatment with SioforЃ, all patients should adhere to a diet with an even intake of carbohydrates throughout the day. Overweight patients should follow a low-calorie diet. Laboratory tests, standard for patients with diabetes mellitus, should be carried out regularly. Before using SioforЃ in children aged 10 to 18 years, the diagnosis of type 2 diabetes mellitus should be confirmed. In the course of one-year controlled clinical trials, the effect of metformin on the growth and development, as well as on puberty, was not observed in children; there are no data on these indicators with longer use.In this regard, it is recommended to carefully monitor the relevant parameters in children receiving metformin, especially in the prepubertal period (10-12 years). Monotherapy with SioforЃ does not lead to hypoglycemia, however, it is recommended to be careful while using the drug with insulin or sulfonylurea derivatives.

Influence on the ability to drive vehicles and use mechanisms

The use of SioforЃ does not cause hypoglycemia, therefore it does not affect the ability to drive vehicles and maintain mechanisms. With the simultaneous use of SioforЃ with other hypoglycemic drugs (sulfonylurea derivatives, insulin, repaglinide), hypoglycemic conditions may develop, therefore, care must be taken when driving vehicles and other potentially hazardous activities that require concentration of attention and speed of psychomotor reactions.

Overdose

When using metformin in doses up to 85 g, hypoglycemia was not observed. Symptoms: with a significant overdose, lactic acidosis may develop, the symptoms of which are severe weakness, respiratory disturbances, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, decreased blood pressure, reflex bradyarrhythmia. Muscle pain, confusion, and loss of consciousness may occur. Treatment: immediate withdrawal of the drug and emergency hospitalization are recommended. The most effective method for removing lactate and metformin from the body is hemodialysis.

Drug interactions

Contraindicated combinations Intravascular administration of iodine-containing contrast agents in patients with diabetes mellitus may be complicated by renal failure, as a result of which metformin accumulates and increases the risk of lactic acidosis. The use of SioforЃ should be discontinued 48 hours before and should not be resumed earlier than 2 days after X-ray examination using iodine-containing contrast agents, provided that the concentration of serum creatinine is normal. Combinations not recommended The risk of developing lactic acidosis increases with acute alcohol intoxication or simultaneous use with ethanol-containing drugs, especially against the background of dieting or malnutrition, as well as liver failure. Combinations,requiring caution The simultaneous use of metformin with danazol can lead to the development of a hyperglycemic effect. If it is necessary to treat with danazol and after the termination of its use, a dose adjustment of metformin is required under the control of the blood glucose concentration. With simultaneous use with oral contraceptives, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, nicotinic acid, an increase in the concentration of glucose in the blood is possible. Nifedipine increases the absorption, Cmax in the blood plasma of metformin, prolongs its excretion. Cationic drugs (amiloride, morphine, procainamide, quinidine, ranitidine, triamterene, vancomycin) secreted in the tubules compete for tubular transport systems and, with prolonged therapy, can increase the Cmax of metformin in blood plasma.Cimetidine slows down the elimination of the drug, as a result of which the risk of developing lactic acidosis increases. Metformin reduces Cmax and T1 / 2 of furosemide. Metformin can weaken the effect of indirect anticoagulants. Glucocorticoids (for systemic and local use), beta-adrenomimetics and diuretics have hyperglycemic activity. The concentration of glucose in the blood should be more closely monitored, especially at the beginning of treatment. If necessary, the dose of metformin should be adjusted for the period of simultaneous use and after the withdrawal of these drugs. ACE inhibitors and other antihypertensive drugs can lower blood glucose. The dose of metformin can be adjusted if necessary. With the simultaneous use of the drug SioforЃ with sulfonylurea derivatives, insulin, acarbose,salicylates may increase the hypoglycemic effect.