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Active ingredients
Metformin
Release form
Pills
Composition
1 tablet contains: Metformin hydrochloride 850 mg Auxiliary substances: hypromellose - 30 mg, povidone - 45 mg, magnesium stearate - 5 mg
Pharmacological effect
A hypoglycemic drug from the biguanide group. Provides a decrease in both basal and postprandial glucose concentration in the blood. It does not stimulate insulin secretion and therefore does not lead to hypoglycemia. The action of metformin is probably based on the following mechanisms: - Reduced glucose production in the liver due to inhibition of gluconeogenesis and glycogenolysis; - Increased muscle sensitivity to insulin and, consequently, improved glucose absorption at the periphery and its utilization; - Inhibition of glucose absorption in the intestine. Metformin through its action on glycogen synthase stimulates the intracellular synthesis of glycogen. Increases the transport capacity of all membrane glucose transport proteins known to date. Regardless of the effect on blood glucose, it has a beneficial effect on lipid metabolism, leads to a decrease in total cholesterol, low density cholesterol and triglycerides.
Pharmacokinetics
Absorption After ingestion, Cmax in the blood plasma is reached in about 2.5 hours and at the maximum dosage does not exceed 4 μg / ml. When eating, absorption decreases and slightly slows down. Absolute bioavailability in healthy patients is approximately 50-60%. Distribution Practically not bound to plasma proteins. The average Vd is 63-276 liters. It accumulates in the salivary glands, muscles, liver and kidneys. It penetrates red blood cells. Excretion is excreted by the kidneys in unchanged form. Renal clearance is> 400 ml / min. T1 / 2 is about 6.5 hours. The pharmacokinetics in special clinical situations. With a decrease in kidney function, the clearance of metformin decreases in proportion to creatinine clearance. Thus, T1 / 2 is lengthened and the concentration of metformin in the plasma increases.
Indications
- diabetes mellitus type 2, especially in patients with overweight with the ineffectiveness of diet and exercise. It can be used as monotherapy or in combination with other oral hypoglycemic drugs and insulin.
Contraindications
- 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 (eg, dehydration, severe infectious disease); - intravascular injection of iodine-containing contrast agent - acute or chronic diseases that can cause tissue hypoxia (for example, cardiac or respiratory failure, recent myocardial infarction, shock); - liver failure; - lactic acidosis (including anamnesis); - pregnancy; - lactation period (breastfeeding); - acute alcohol intoxication, chronic alcoholism; - observance of a low-calorie diet (less than 1000 kcal / day); - children under 10 years old.- hypersensitivity to metformin or other components of the drug .
Precautionary measures
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 lactic acidosis.
Use 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 the event of pregnancy. When planning or approaching pregnancy in a patient with type 2 diabetes, the drug should be canceled, insulin therapy should be normalized or blood glucose levels as normal as possible to reduce the risk of fetal defects due to the pathological effects of hyperglycemia. Methformin penetrates the milk of laboratory animals. Similar data for a person are not available, so a decision should be made to discontinue breastfeeding or to discontinue the drug Siofor, taking into account the need to use the drug in the mother.
Dosage and administration
The drug should be taken orally during or after a meal. The dose and regimen of the drug, as well as the duration of treatment are set by the attending physician depending on the level of glucose in the blood. AdultsMonotherapy The recommended initial dose is 500 mg (1 tablet of the drug Siofor 500 or 1/2 tab. drug Siofor 1000) 1-2 times / day or 850 mg (1 tab.drug Siofor 850) 1 time / day. After 10-15 days after starting the drug, a further gradual increase in dose is possible depending on the level of glucose in the blood to the average daily dose: 3-4 tab. drug Siofor 500, 2-3 tab. preparation Siofor 850 or 2 tab. The drug Siofor 1000. A gradual increase in dose reduces the number of undesirable effects on the gastrointestinal tract. The maximum dose is 3000 mg / day in 3 doses (6 pills of the drug Siofor 500 or 3 pills of the drug Siofor 1000). For patients who are prescribed high doses (2000 -3000 mg / day) possible replacement 2 tab. drug Siofor 500 on 1 tab. When transferring a patient for treatment with Siofor with another antidiabetic drug, stop taking the latter and begin to take Siofor in the above doses. Combined use with insulin You can combine Siofor and insulin to improve glycemic control. The standard initial dose is 500 mg (1 tablet of the drug Siofor 500 or 1/2 tablet of the drug Siofor 1000) 1-2 times / day or 850 mg (1 tablet of the drug Siophor 850) 1 time / day, with a gradual increase in the dose with intervals of approximately one week to an average daily dose of 3-4 tab. drug Siofor 500, 2 tab. drug Siofor 1000 or 2-3 tab. drug Siofor 850; The dose of insulin is determined on the basis of the glucose concentration in the blood. The maximum dose is 3000 mg / day in 3 doses. Due to possible impairment of renal function in elderly patients, the dose of the preparation Siofor is selected taking into account the plasma creatinine concentration. Regular assessment of the functional state of the kidneys is necessary. Children aged 10 to 18 yearsMonotherapy and combined use with insulin. The standard initial dose is 500 mg (1 tablet of the drug Siofor 500 or 1/2 tablet of the drug Siofor 1000) 1 time / day or 850 mg ( 1 tablet of drug Siofor 850) 1 time / day. After 10-15 days after the start of the drug, a further gradual increase in the dose is possible depending on the level of glucose in the blood. A gradual increase in dose reduces the number of undesirable effects on the gastrointestinal tract. The maximum dose for children is 2000 mg / day (4 pills of drug Siofor 500 or 2 pills of drug Siofor 1000) in 2-3 doses. The dose of insulin is determined based on the level of glucose in the blood .
Side effects
On the part of the nervous system: often - a violation of taste. On the part of 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 disappear 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 dose reduces the likelihood of undesirable effects from the gastrointestinal tract. Allergic reactions: very rarely - skin reactions (eg, hyperemia, itching, urticaria). On the metabolic side: 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 side of the liver and biliary tract: individual reports are reversible abnormalities in liver function, resulting in increased activity of hepatic transaminases, or hepatitis, after stopping metformin.
Interaction with other drugs
Contraindicated combinations Intravascular injection 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. Drug use Siofor should be discontinued 48 hours before and should not be resumed earlier than 2 days after x-ray examination with the use of iodine-containing contrast preparations under the condition of normal serum creatinine. Recommended combinations The risk of lactic acidosis increases with acute alcohol intoxication or simultaneous use with ethanol-containing drugs, especially against a diet or eating disorder, as well as liver failure. Combinations that require caution caution Simultaneous use of metformin with danazol may lead to the development of a hyperglycemic effect. If necessary, treatment with danazol and after discontinuation of its application requires dose adjustment of metformin under the control of glucose concentration in the blood. When used simultaneously with oral contraceptive drugs, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, nicotinic acid, the concentration of glucose in the blood may increase. Nipedipine increases the blood glucose concentration. absorption,Cmax in metformin blood plasma, prolongs its elimination. Cationic drugs (amiloride, morphine, procainamide, quinidine, ranitidine, triamterene, vancomycin) secreted in tubules compete for tubular transport systems and with prolonged therapy can increase Cmax of metformin in blood plasma. Cimetidine slows down the excretion of the drug, resulting in an increased risk of lactic acidosis. Metformin reduces Cmax and T1 / 2 of furosemide. Metformin can weaken the effect of indirect anticoagulants. Glucocorticoids (for systemic and local applications), beta-adrenomimetics and diuretics possess hyperglycemic activity. The concentration of glucose in the blood should be more carefully controlled, especially at the beginning of treatment. If necessary, the dose of metformin should be adjusted for the period of simultaneous use and after discontinuation of these drugs. ACE inhibitors and other antihypertensive drugs may reduce blood glucose. If necessary, the dose of metformin can be adjusted. With simultaneous use of the drug Siofor with sulfonylurea derivatives, insulin, acarbose, salicylates, hypoglycemic action may increase.
special instructions
Lactic acidosis is a serious pathological condition that is extremely rare and is associated with the accumulation of lactic acid in the blood, which can be caused by cumulation of metformin. The described cases of lactic acidosis in patients treated with metformin were observed mainly in patients with diabetes mellitus with severe renal insufficiency. Prevention of lactic acidosis involves the determination of all associated risk factors, such as decompensated diabetes, ketosis, prolonged fasting, excessive drinking, 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 eliminated by the kidneys, the concentration of creatinine in the blood plasma should be determined before the start of treatment, and then regularly. Particular caution should be exercised in cases where there is a risk of impaired renal function, for example, at the beginning of therapy with antihypertensive drugs,diuretics or NPVS. Treatment with Siofor should be temporarily replaced with other hypoglycemic drugs (eg, insulin) 48 hours before and 48 hours after an x-ray study with iv injection of iodine-containing contrast agents. Use of Siofor should be stopped 48 hours before the planned surgical operations 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 renal function is confirmed. Siofor does not replace diet and daily exercise - these types of therapy should be combined in accordance with the recommendations of the doctor. During treatment with the preparation Siofor, all patients should follow a dietary meal with an even carbohydrate intake throughout the day. Overweight patients should follow a low-calorie diet. Standard laboratory tests for diabetics should be performed regularly. Before using Siofor in children aged 10 to 18 years, a diagnosis of type 2 diabetes should be confirmed. During one-year controlled clinical studies of the effect of metformin growth and development, as well as puberty of children was not observed, data on these indicators with longer use are not available. In this regard, it is recommended that the relevant parameters be carefully monitored in children receiving metformin, especially in the prepubertal period (10-12 years). Monotherapy with the drug Siofor does not lead to hypoglycemia, but caution is recommended when using the drug with insulin or sulfonylurea derivatives at the same time. ability to drive vehicles and control mechanismsThe use of the drug Siophora does not cause hypoglycemia, and therefore does not affect the ability to drive vehicles and maintenance of mechanisms. If Siofor is used simultaneously with other hypoglycemic drugs (sulfonylurea derivatives, insulin, repaglinide), hypoglycemic states may develop, so care should be taken when driving and other potentially dangerous activities that require attention and quickness of psychomotor reactions.