Metformin
Metformin – one of the “oldest” drugs in the treatment of type 2 diabetes metformin sale mellitus (type 2 diabetes), first synthesized in 1922 and started to be used in clinical practice since the late 50’s. last century. Metformin to date – the only representative of the biguid group, used to treat type 2 diabetes.
Pharmacokinetics
After ingestion, metformin is absorbed from the digestive tract. Bioavailability after taking a standard dose is 50-60%. C max in blood plasma is achieved 2.5 hours after ingestion. Virtually does not bind to plasma proteins. It accumulates in the salivary glands, metformin sale muscles, liver and kidneys. It is allocated in an unchanged form by kidneys. T 1/2 is 1.5-4.5 h.
With violations of kidney function, cumulation of the drug is possible.
Indications for use of the drug
– Type 2 diabetes mellitus without a tendency to ketoacidosis (especially in obese patients) with ineffectiveness of diet therapy.
Dosing regimen
The dose of the drug is set by the doctor individually depending on the level of glucose in the blood.
Tablets 0.5 g: the initial dose is 0.5-1 g / day. After 10-15 days, a further gradual increase in the dose, depending on the level of glucose in the blood, is possible. The maintenance dose of the drug is usually 1.5-2 g / day. The maximum dose is 3 g / day.
Tablets 0.85 g: the initial dose is 0.85 g / day. After 10-15 days, a further gradual increase in the dose, depending on the level of glucose in the blood, is possible. The maintenance dose of the drug is usually 1.7 g / day. The maximum dose is 2.55 g / day. In elderly patients, the recommended daily dose should not exceed 0.85 – 1 g.
Metformin-Richter tablets should be taken wholly during or immediately after meals, with a small amount of liquid (a glass of water). To reduce side effects from the gastrointestinal tract, the daily dose should be divided into 2-3 doses.
Due to the increased risk of developing lactic acidosis, the dose of the drug should be reduced in case of severe metabolic disturbances.
Features of the appointment
Based on the results of numerous studies and long-term worldwide clinical experience, metformin has become an obvious dominant in the treatment of type 2 diabetes. A recently published study proved for the first time the feasibility of an early start of metformin therapy in type 2 diabetes. In the group of 1799 patients with type 2 diabetes, clinical success was metformin sale assessed with a different start-up period from the time of diagnosis: 40% of patients who had metformin with the first-line drug started taking it within the next 3 months; 25% – after 3 months or more; 27% started taking metformin with 
Researchers regarded as a secondary failure of therapy an increase in HbA1c> 7.5% or the need to prescribe other antidiabetic agents in the form of an addition to or replacement of metformin. In general, during the observation period, 42% of secondary failures (17% / year) were recorded. At the same time, the lowest failure rate was observed among patients who started metformin treatment within 3 months after diagnosis of diabetes (12.2% / year), and patients who started drug therapy at a level of HbA1c <7% (12.3% / year) year). In cases when the start of therapy was postponed for 4-11 months, the onset of failure of therapy was 56% more likely (OR 1.56, 95% CI 1.12-2.18), and in cases of refusal of therapy for three or more years, the probability of failure was the highest (OR 2.20, 95% CI 1.68-2.87).
To date, according to the recommendations of the American Diabetes Association and the European Association for the Study of Diabetes (ADA / EASD), metformin metformin sale is positioned as the first choice for treatment of type 2 diabetes, a pathogenetic agent that safely and effectively combines with most of the present antidiabetic drugs, a drug that should appear in the life of a patient with type 2 diabetes as early as possible and can accompany it for as long as possible.
Side effects Metformin
On the part of the digestive system: nausea, vomiting, “metallic” taste in the mouth, lack of appetite, diarrhea, flatulence, abdominal pain.
From the side of metabolism: rarely – lactate-acidosis (requires discontinuation of treatment); with prolonged treatment – hypovitaminosis B12 (impaired absorption).
On the part of the hematopoiesis system: in some cases – megaloblastic anemia.
On the part of the endocrine system: hypoglycemia (when used in inadequate doses).
Allergic reactions: skin rash.
Contraindications to the use of the drug
– diabetic ketoacidosis, diabetic precoma, coma;
– severe renal dysfunction;
– cardiac and respiratory insufficiency, acute phase of myocardial infarction, acute disturbance of cerebral circulation, dehydration, chronic alcoholism and other metformin sale conditions that may contribute to the development of lactic acidosis;
– pregnancy and the period of breastfeeding;
– Serious surgical interventions and injuries, when insulin therapy is indicated;
– impaired liver function;
– Acute alcohol poisoning;
– Lactate acidosis (including in the anamnesis);
– adherence to a hypocaloric diet (less than 1000 kcal / day);
– Hypersensitivity to the drug.
Contraindicated use of the drug for at least 2 days before and within 2 days after carrying out radioisotope and radiographic studies with the introduction of iodide-containing contrast medium.
It is not recommended to use the drug for people over 60 who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis.
Application of the drug during pregnancy and lactation
The drug is contraindicated in pregnancy and during breastfeeding.
Application for violations of liver function
Contraindicated in patients with impaired liver function
Application for violations of kidney function
Contraindicated in severe impairment of kidney function.
With violations of kidney function, cumulation of the drug is possible. During the treatment it is necessary to monitor the kidney function.
Special instructions
During the treatment it is necessary to monitor the kidney function. The content of lactate in the blood plasma should be determined at least 2 times a year, as well as metformin sale with the appearance of myalgia.
Influence on the ability to drive vehicles and work with mechanisms.
With monotherapy, Metformin-Richter does not affect the ability to drive vehicles.
When metformin is combined with other hypoglycemic agents (derivatives of sulfonylureas, insulin, etc.) hypoglycemic conditions may develop, in which the ability to drive vehicles and engage in other potentially dangerous activities that require increased attention and rapid psychomotor reactions deteriorates.
Overdose
With an overdose of Metformin, lactate-acidosis may develop with a fatal outcome. The cause of lactate acidosis may also be cumulation of the drug due to impaired renal function. The earliest symptoms of lactic acidosis are nausea, vomiting, diarrhea, lower metformin sale body temperature, abdominal pain, muscle pain, and then there may be more breathing, dizziness, impaired consciousness and coma development.
Treatment: in case of signs of lactic acidosis, treatment with Metformin-Richter should be stopped immediately, the patient should immediately hospitalize and, after determining the concentration of lactate in the blood, confirm the diagnosis. The most effective measure for excretion from the body of lactate and metformin is hemodialysis. Conduct also symptomatic treatment. With combined therapy with Metformin-Richter with sulfonylureas, hypoglycemia can develop.
Drug Interactions
With simultaneous use with sulfonylurea derivatives, acarbose, insulin, NVPs, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate derivatives, cyclophosphamide, beta-adrenoblockers, hypoglycemic effect of metformin may be enhanced.
When used simultaneously with glucocorticosteroids, oral contraceptives, epinephrine, sympathomimetics, glucagon, thyroid hormones, thiazide and loop diuretics, phenothiazine derivatives, nicotinic acid derivatives, a decrease in the hypoglycemic metformin sale effect of metformin is possible.
Cimetidine slows the excretion of metformin, which increases the risk of lactate acidosis.
Metformin can weaken the effect of anticoagulants (coumarin derivatives).
With the simultaneous intake of alcohol, lactate acidosis may develop.
Conditions of leave from pharmacies
The drug is released by prescription.
Terms and conditions of storage
Storage conditions
List B. Store at a temperature of no higher than 25 ° C in a place inaccessible to children.
