Description
Latin name
SIOFOR ®
Release form
film-coated tablets.
packaging 60 pcs
Pharmacological action
Pharmacodynamics
Hypoglycemic drug from the biguanide group. Provides a decrease in both basal and postprandial blood glucose concentrations. It does not stimulate insulin secretion and therefore does not lead to hypoglycemia. The action of metformin is probably based on the following mechanisms:
decreased glucose production in the liver due to inhibition of gluconeogenesis and glycogenolysis
increased muscle sensitivity to insulin and, therefore, improved peripheral glucose uptake and utilization
inhibition of intestinal glucose absorption.
Metformin through its action on glycogen synthetase stimulates intracellular glycogen synthesis. It increases the transport capacity of all the glucose membrane transport proteins known to date.
Regardless of the effect on blood glucose, it has a beneficial effect on lipid metabolism, leading to a decrease in total cholesterol, low density cholesterol and triglycerides.
Pharmacokinetics
Absorption
After ingestion, Cmax in plasma is reached after about 2.5 hours and does not exceed 4 μg / ml at maximum dosage. When eating, absorption decreases and slightly slows down. The absolute bioavailability in healthy patients is approximately 50-60%.
Distribution of
Virtually non-binding to plasma proteins. The average Vd is 63-276 liters. It accumulates in the salivary glands, muscles, liver and kidneys. Penetrates red blood cells.
Excretion
Excreted by the kidneys unchanged. Renal clearance is> 400 ml / min. T1 / 2 is about 6.5 hours.
Pharmacokinetics in special clinical cases
With decreased renal function, metformin clearance decreases in proportion to creatinine clearance. Thus, T1 / 2 lengthens and the concentration of metformin in plasma increases.
Indications
Type 2 diabetes mellitus, especially in patients with overweight with the ineffectiveness of diet therapy and physical activity.
May be used as monotherapy or in combination with other oral hypoglycemic drugs and insulin.
Contraindications
Hypersensitivity to metformin or other components of the
preparation diabetic ketoacidosis, diabetic precoma
renal failure or impaired renal function (CC < 60 ml / min) acute conditions that could adversely affect kidney function (e.g. dehydration, severe infectious disease) intravascular injection of iodine-containing contrast agent acute or chronic diseases that can cause tissue hypoxia (e.g., heart or respiratory failure, recently myocardial infarction, shock) liver failure lactic acidosis (including history) pregnancy and lactation (breastfeeding) acute alcohol sycation, chronic alcoholism adherence to a low-calorie diet (less than 1000 kcal / day) children’s age up to 10 years. Caution: the drug should be used in children aged 10 to 12 years old in patients older than 60 years who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis in them. Use during pregnancy and lactation The drug is contraindicated in pregnancy and lactation (breastfeeding). The patient should be warned about the need to inform the doctor in case of pregnancy. When planning or having a pregnancy in a patient with type 2 diabetes, the drug should be discontinued, with the help of insulin therapy, normalize or bring the blood glucose level as normal as possible to reduce the risk of defects in the fetus 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 whether to stop breastfeeding or to discontinue Siofor ® taking into account the need for the mother to use the drug. Composition 1 tablet contains: Active substances: metformin hydrochloride 1000 mg. Excipients: hypromellose – 35.2 mg, povidone – 53 mg, magnesium stearate – 5.8 mg. Shell composition: hypromellose – 11.5 mg, macrogol 6000 – 2.3 mg, titanium dioxide (E171) – 9.2 mg. Dosage and administration of The drug should be taken orally during or after meals. The dose and regimen of the drug, as well as the duration of treatment, are determined by the attending physician depending on the level of glucose in the blood. Adults Monotherapy Recommended starting dose is 500 mg (1 tablet of Siofor ® 500 or 1/2 tablet of Siofor 1000) 1-2 times / day or 850 mg (1 tablet of Siofor ® 850) 1 time /day. 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 to the average daily dose: 3-4 tab. Siofor ® 500 preparation, 2-3 tab. preparation Siofor ® 850 or 2 tab. Siofor ® 1000. A gradual increase in dose reduces the number of undesirable effects from the gastrointestinal tract. The maximum dose is 3,000 mg / day in 3 divided doses (6 tablets of Siofor ® 500 or 3 tablets of Siofor ® 1000). For patients who are prescribed high doses (2000-3000 mg / day), replacement of 2 tablets is possible. Siofor ® 500 preparation for 1 tab. Siofor ® 1000. When transferring a patient to treatment with Siofor ® with another antidiabetic drug, stop taking the latter and start taking Siofor ® in the above doses. Combined insulin use Siofor ® and insulin can be combined to improve glycemic control. The standard starting dose is 500 mg (1 tablet of Siofor ® 500 or 1/2 tablet of Siofor 1000) 1-2 times / day or 850 mg (1 tablet of Siofor ® 850) 1 time / day, with gradual dose increase with an interval of approximately one week to an average daily dose of 3-4 tab. Siofor ® 500 preparation, 2 tab. Siofor ® 1000 or 2-3 tab. Siofor ® 850 preparation, the dose of insulin is determined based on the concentration of glucose in the blood. The maximum dose is 3,000 mg / day in 3 divided doses. Due to a possible impaired renal function in elderly patients, the dose of Siofor ® is selected taking into account the concentration of creatinine in the blood plasma. A regular assessment of the functional state of the kidneys is necessary. Children 10 to 18 years old Monotherapy and combined use with insulin The standard starting dose is 500 mg (1 tablet of Siofor ® 500 or 1/2 tablet of Siofor ® 1000) 1 time / day or 850 mg ( 1 tablet of Siofor ® 850) 1 time / day. 10-15 days after the start of the drug, a further gradual increase in dose is possible depending on the level of glucose in the blood. A gradual increase in dose reduces the number of undesirable effects from the gastrointestinal tract. The maximum dose for children is 2000 mg / day (4 tablets. Siofor ® 500 or 2 tablets. Siofor ® 1000) in 2-3 doses. The dose of insulin is determined based on the level of glucose in the blood. Side effects of Possible side effects when using the drug are given depending on the frequency of occurrence: often ( 1/100, <1/10) infrequently ( 1/1000, <1/100) rarely ( 1 / 10,000, <1/1000) is very rare (<1/10 000), including individual messages. From the nervous system: often – a violation of taste. 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 pass spontaneously. To prevent the onset of symptoms, the dose of the drug is recommended to be distributed in 2-3 doses during or after meals. A gradual increase in dose reduces the likelihood of unwanted effects from the gastrointestinal tract. Allergic reactions: very rarely – skin reactions (eg, hyperemia, 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 blood plasma. This should be considered if the patient has megaloblastic anemia. On the part of the liver and biliary tract: separate messages are reversible dysfunctions of the liver, expressed in increased activity of hepatic transaminases, or hepatitis, passing after stopping the use of metformin. Drug Interaction Contraindications combinations Intravascular administration of iodine-containing contrast drugs in patients with diabetes mellitus may complicate renal failure, resulting in metformin cumulative development and increased cumulative risk. The use of the drug Siofor ® should be discontinued 48 hours prior to administration and should not be resumed earlier than 2 days after radiological examination using iodine-containing contrast agents under normal serum creatinine concentration. Not recommended combinations The risk of developing lactic acidosis increases with acute alcohol intoxication or concomitant use with ethanol-containing drugs, especially against diet or malnutrition, and liver failure. Combinations with caution Concomitant use of metformin with danazol may lead to the development of a hyperglycemic effect. If necessary, treatment with danazol and after discontinuation of its use requires a dose adjustment of metformin under the control of blood glucose. When used concurrently with oral contraceptives, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, nicotinic acid, blood glucose may increase. Nifedipine increases absorption, Cmax in the plasma of metformin, prolongs its excretion. Cationic drugs (amiloride, morphine, procainamide, quinidine, ranitidine, triamterene, vancomycin), secreted in tubules, compete for tubular transport systems and may increase Cmax of metformin in blood plasma with prolonged therapy. Cimetidine slows the elimination of the drug, which increases the risk of lactic acidosis. Metformin reduces Cmax and T1 / 2 furosemide. Metformin may weaken the effect of indirect anticoagulants. Glucocorticoids (for systemic and topical use), beta-adrenomimetics and diuretics have hyperglycemic activity. Blood glucose levels should be more closely monitored, especially at the beginning of treatment. If necessary, the dose of metformin should be adjusted for concomitant use and after discontinuation of these drugs. ACE inhibitors and other antihypertensive drugs can lower blood glucose. If necessary, the dose of metformin can be adjusted. With the simultaneous use of the drug Siofor ® with sulfonylureas, insulin, acarbose, salicylates, hypoglycemic effects may increase. Overdose No hypoglycemia was observed with metformin at doses up to 85 g. Symptoms: Lactic acidosis, with symptoms of severe weakness, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, decreased blood pressure, reflex bradyarrhythmia, is possible with a significant overdose. Muscle pain, confusion and loss of consciousness may be noted. Treatment: Immediate withdrawal and emergency hospitalization are recommended. The most effective method of removing lactate and metformin from the body is hemodialysis. Storage conditions Keep out of the reach of children at a temperature not exceeding 25 ° C. Expiration 3 years. Deystvuyuschee substances Metformin Terms of delivery from pharmacies Prescription dosage form dosage form tablets Berlin-Chemie / Menarini Germany
