Siofor tab 850 p / v 850mg film 60 pcs

Description

Composition
Active substance:
1 tablet contains: metformin hydrochloride – 850.0 mg ;.
Excipients:
Hypromellose – 30.0 mg Povidone – 45.0 mg Magnesium stearate – 5.0 mg.
Coating: Hypromellose – 10.0 mg macrogol 6000 – 2.0 mg of titanium dioxide, E 171 – 8.0 mg.
Description:
Oblong tablets, white coated with a two-way risk.
Product form:
Coated tablets, 850 mg.
15 tablets in blisters (blister) [PVC film / aluminum foil].
2, 4 or 8 blisters together with instructions for use placed in a cardboard box.
Contraindications
Hypersensitivity to metformin or excipients of the formulation; diabetic ketoacidosis, diabetic precoma, coma; renal dysfunction (creatinine clearance
With care for children between the ages of 10 to 12 years; breastfeeding; persons over 60 years, performing heavy physical work (increased risk of developing lactic acidosis).
Dosage
850 mg
Indications
Type 2 diabetes, especially in patients with overweight, to control the concentration of glucose in the blood plasma. y adults as monotherapy or in combination therapy with other oral hypoglycemic agents and / or insulin. y children older than 10 years as monotherapy or in combination with insulin.
Treatment of diabetes type 2 to be accompanied by an increase correction diet and physical activity (in the absence of contraindications).
Interaction with other drugs
The simultaneous use is contraindicated
Iodine-containing X-ray contrast agents
Intravascular administration of iodinated contrast media in patients with diabetic renal failure may be complicated, whereby metformin accumulates and increases the risk of lactic acidosis. Use of the preparation should be discontinued Siofor® 850 for 48 hours before and not to resume earlier than 48 hours after radiological studies using iodinated contrast media under normal serum creatinine concentration.
Simultaneous use is not recommended
Alcohol and drugs etanolsoderzhaschie
The risk of lactic acidosis increases with acute alcohol intoxication, or the simultaneous use of ethanol-containing preparations, especially against the background of fasting or eating disorders, and liver failure. During the metformin avoid intake of alcohol and drugs containing ethanol.
Simultaneous use requires caution
The simultaneous use of metformin with danazol may lead to the development of hyperglycemia effect. If necessary, treatment with danazol and after the termination of its use required a dose adjustment of metformin under the control of plasma glucose concentration.
Chlorpromazine: when used in high doses (100 mg daily) increases the concentration of plasma glucose, decreasing insulin release. When neuroleptic treatment and after discontinuation of the past required a dose adjustment of metformin under the control of concentrations in plasma glucose.
While the use of oral contraceptives, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, nicotinic acid may increase plasma concentrations of glucose. Nifedipine increases absorption, the maximum concentration in the blood plasma metformin, prolongs its elimination.
Cationic drugs (amiloride, morphine, procainamide, quinidine, hiniin, ranitidine, triamterene, vancomycin) is secreted in the tubules, competing for renal tubular transport systems and long-term therapy may increase the maximum concentration of metformin in plasma. Metformin reduces the maximum concentration and half-life of furosemide; may weaken the effect of indirect anticoagulants.
Glucocorticoids (systemic and topical application), beta2-agonists (by injection) have hyperglycaemic activity. It should be more carefully monitored in the plasma glucose concentration, particularly early in treatment. If necessary, the dose of metformin should be adjusted for the period of simultaneous application, and after withdrawal of these drugs.
While the use of diuretics, particularly “loop”, may increase the risk of lactic acidosis, because of the potential ability of diuretics to reduce kidney function.
ACE inhibitors and other antihypertensive drugs can reduce plasma glucose concentration. If necessary, the dose of metformin can be adjusted.
Substrates organic cation transporter 2 (OST2)
With simultaneous use of ranolazine 500 mg and 1000 mg 2 times daily and metformin 1000 mg 2 times a day, metformin plasma concentration in patients with type 2 diabetes increases by 1.4 and 1.8 times respectively.
With simultaneous application of cimetidine 400 mg twice a day in 7 healthy volunteers metformin AUC and Cmax increased by 50% to 81%, respectively.
With simultaneous use of metformin with sulfonylureas, insulin, acarbose, salicylates may increase hypoglycemic action.
Overdose
When metformin in doses up to 85 g of hypoglycemia was not observed.
When a large overdose may develop lactic acidosis, symptoms are severe weakness, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, lowering blood pressure, reflex bradyarrhythmia. May experience muscle cramps, confusion and loss of consciousness. If you suspect that the development of lactic acidosis recommended the immediate withdrawal of the drug and emergency hospitalization.
The most effective method to remove lactate and metformin from the body – hemodialysis.
pharmachologic effect
Pharmacological group:
Hypoglycemic agent for oral use biguanide group.
Pharmacodynamics:
Metformin belongs to the biguanide group. It has hypoglycemic action. It reduces both basal and postprandial blood glucose levels. It does not stimulate insulin secretion and therefore does not lead to hypoglycemia.
The action of metformin based on the following mechanisms: -reduction of glucose production in the liver due to inhibition of gluconeogenesis and glycogenolysis; increasing the sensitivity of muscles to insulin and consequently improve glucose uptake in the periphery and glucose utilization at the periphery; -ugnetenie glucose absorption in the intestine.
Metformin by acting on glikiencintetazu stimulates intracellular glycogen synthesis. Increases the transport capacity of all hitherto known glucose membrane transport proteins.
It has, independently of its effects on plasma concentrations of glucose, a beneficial effect on lipid metabolism, reduces the concentration of total cholesterol, LDL cholesterol and triglycerides.
Against the background of metformin in patients with diabetes or body weight remained stable or moderately reduced.
Pharmacokinetics:
Suction
After taking the drug inside, metformin is absorbed almost completely from the gastrointestinal tract, maximum concentration (Cmax) in plasma is reached after 2.5 hours and at the maximum dose does not exceed 4 micrograms / ml. Food intake reduces the extent of absorption (Cmax decreased by 40%, area under the curve “concentration-time» (AUC) 25%) and slightly slows down the absorption of metformin from the gastrointestinal tract (time reaching Cmax decreased by 35 minutes). When used in the recommended doses equilibrium plasma concentration is attained within 24-48 hours and usually less than 1 ug / ml. The absolute bioavailability in healthy volunteers, approximately 50 – 60%.
Distribution
Practically does not bind to plasma proteins. Penetrate into erythrocytes. Cmax in the blood lower Cmax in plasma and reached approximately the same time. Probably, erythrocytes are secondary compartment distribution. The mean volume of distribution (Vd) is 63-276 l.
Metabolism and excretion
Excreted by the kidneys unchanged. Metabolites in the human body is not found. Renal clearance of> 400 ml / min. When half-life (T1 / 2) is about 6.5 hours. By reducing renal clearance is reduced proportionally metformin creatinine clearance, respectively, the half-life of metformin is prolonged and the concentration in the blood plasma increases.
Children
A single application of metformin in children at a dose of 500 mg, pharmacokinetic parameters were similar to those in adults.
Pregnancy and breast-feeding
Uncontrolled diabetes during pregnancy may increase the risk of congenital abnormalities and perinatal mortality.
Limited data suggests that the use of metformin in pregnant women increases the risk of birth defects in children.
Data obtained in animal studies, did not reveal any adverse effects on pregnancy, embryonic development of the fetus during childbirth or postnatal development.
When planning a pregnancy with diabetes, as well as in case of attack, the use of insulin is recommended to maintain the concentration of plasma glucose at the level closest to the normal values ​​in order to reduce the risk of fetal malformations.
Patients with diabetes should be warned about the need to put in a doctor’s reputation in the event of pregnancy.
Metformin passes into breast milk. In newborns / infants are breastfed, mothers who received metformin, metformin no negative effects were noted. However, given the limited data, the use of metformin is not recommended for women during breastfeeding. The decision to terminate breast-feeding should be made taking into account the benefit of breast-feeding and the potential risk of adverse reactions in children.
Conditions of supply of pharmacies
On prescription.
side effects
Possible side effects when using the drug are listed below in accordance with the classification the World Health Organization in descending frequency of occurrence: very often (> 1/10), often (> 1/100, 1/1000, 1/10000,
Disorders of the nervous system:
Common: taste disturbance.
Violations by the gastrointestinal system:
Very common: nausea, vomiting, diarrhea, abdominal pain, loss of appetite.
These adverse effects often occur at the beginning of therapy and in most cases take place spontaneously. To prevent symptoms of the dose is recommended to distribute to 2-3 doses during or after meals. The gradual increase in the dose improves the tolerability of the gastrointestinal tract.
Violations by the skin and subcutaneous tissue disorders:
Very rare: Skin reactions such as redness, itching, rash.
Violations by the Metabolism and nutrition:
Very rare: Lactic acidosis (requires discontinuation of treatment). Symptoms of lactic acidosis – see section “Overdose”..
With prolonged use of a decrease in vitamin B12 absorption and a decrease in its plasma concentrations. This should be considered if the patient megaloblastic anemia.
Disorders of the liver and biliary tract:
Very rarely reversible liver function abnormalities lead to increases in liver transaminases, or hepatitis extending after discontinuation of metformin.
Children:
According to data obtained in the course of post-registration application and the results of controlled clinical trials with metformin for 1 year in children aged 10-16 years, the frequency of occurrence and severity of adverse events were comparable to those of adults.
special instructions
Lactic acidosis – a serious pathological condition is extremely rare, due to the accumulation of lactate in the blood, the cause of which could be accumulation of metformin (the symptoms of lactic acidosis – see section “Overdose”.). Lactic acidosis diagnostic laboratory parameters are decreased blood pH less than 7.25, the content of lactate in blood plasma over 5 mg / dL, elevated anionic gap and the ratio of lactate / pyruvate. Described cases of lactic acidosis in patients receiving metformin were observed primarily in diabetic patients with significant renal failure. Prevention of lactic acidosis involves identifying all related risk factors, such as decompensated diabetes, ketosis, prolonged fasting, excessive alcohol intake, hepatic insufficiency and any condition associated with hypoxia. If you suspect that the development of lactic acidosis recommended the immediate withdrawal of the drug and emergency hospitalization.
Because metformin excreted by the kidneys, when using the drug Siofor® 850 should be monitored regularly serum creatinine concentration: – at least once a year for patients with normal renal function; – at least 2-4 times a year in patients with serum creatinine concentration close to the upper limit of normal and in elderly patients.
Particular caution should be exercised in cases where there is a risk of renal dysfunction, for example, at the beginning of therapy, antihypertensive drugs, diuretics or non-steroidal anti-inflammatory drugs (NSAIDs).
Treatment with Siofor® 850 to temporarily replace therapy other hypoglycemic agents (e.g., insulin) for 48 hours before and 48 hours after radiological studies with intravenous administration of iodinated contrast radiopaque substances.
Use of the drug Siofor® 850 should be stopped for 48 hours before elective surgery under general anesthesia, with a spinal or epidural anesthesia. Therapy should continue after the resumption of oral food or no earlier than 48 hours after surgery subject to confirmation of normal renal function.
The drug Siofor® 850 does not replace diet and daily exercise – these therapies should be combined according to your doctor’s recommendations. During treatment Siofor® 850 all patients should adhere to dietary carbohydrate intake evenly throughout the day. Patients who are overweight should observe low-calorie diet.
Standard for patients with diabetes mellitus laboratory tests should be carried out regularly.
Before using the product Siofor® 850 children from 10 to 18 years should confirm the diagnosis of type 2 diabetes.
During controlled clinical studies lasting 1 year, the effect of metformin on growth and development, and sexual maturation of children is not observed, the data on these indicators at a long-term use are not available. In this regard, we recommend careful monitoring of the relevant parameters in children receiving metformin, particularly in prepubertal (10-12 years).
Monotherapy Siofor® 850 does not lead to hypoglycemia, but caution is recommended when used together with insulin formulation or sulfonylureas.
Metformin did not affect the fertility of male or female rats when used in doses (600 mg / kg / day) three times exceeding the maximum recommended daily dose for humans.
The effect on the ability to operate vehicles, machinery
Use of the drug Siofor® 850 does not cause hypoglycemia, so does not affect the ability to drive vehicles and maintenance mechanisms.
With the simultaneous application of the drug Siofor® 850 with other hypoglycemic drugs (sulfonylureas, insulin, repaglinide), may develop hypoglycemic states, so care must be taken when driving and other potentially hazardous activities that require concentration and psychomotor speed reactions.
Storage conditions
At a temperature of not higher than 25 C.
Drug store out of reach of children !.
Dosing and Administration
Inside.
The dose and dosing regimen of the drug, as well as the duration of treatment established by the attending physician depending on the concentration of glucose in the blood plasma.
Adults
Monotherapy or in combination therapy with other hypoglycemic agents for oral use
The recommended starting dose is 850 mg (1 tablet formulation Siofor® 850) 2-3 times a day, during or after meals.
10-15 days after initiation of drug may further gradual increase in the dose as a function of concentration in plasma glucose to an average daily dose of 2-3 tablets drug Siofor® 850. The gradual increase in the dose improves the tolerability of the gastrointestinal tract.
The maximum dose is 3000 mg per day in 3 divided doses.
In the case of transferring a patient on drug treatment therapy Siofor® 850 with other hypoglycemic drugs, discontinue use of the latter and 850 start taking Siofor® drug in the above dosage.
Concomitant use with insulin
Preparation Siofor® 850 and insulin can be combined to improve glycemic control. The standard starting dose of 850 mg (1 tablet formulation Siofor® 850) 2-3 times a day, gradually increasing doses at intervals of about one week to an average daily dose of 2-3 tablets; dose of insulin is determined based on the concentration of glucose in blood plasma.
The maximum dose is 3000 mg per day in 3 divided doses.
elderly patients
Because of the possible renal dysfunction in older patients the dose Siofor® 850 are selected considering the creatinine concentration in blood plasma. Requires regular assessment of renal function.
Children from 10 to 18 years
Monotherapy and combined use with insulin
The standard starting dose of 850 mg (1 tablet formulation Siofor® 850) 1 times a day, during or after meals.
10-15 days after initiation of drug may further gradual increase in the dose as a function of concentration in blood plasma glucose. The gradual increase in the dose improves the tolerability of the gastrointestinal tract.
The maximum dose for children is 2000 mg per day in 2 – 3 divided doses.
When applied simultaneously with insulin insulin is determined based on the concentration of glucose in blood plasma.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist