Metformin - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Metformin inhibits glknoneogenesis in the liver, reduces absorption of glucose from the intestine, enhances peripheral utilization of glucose, and also increases the sensitivity of tissues to insulin.In this case, it has no effect on the secretion of insulin by beta cells of the pancreas, does not cause hypoglycemic reactions. Reduces the level of triglycerides and low density lipoproteins in the blood. Stabilizes or reduces body weight. Has a fibrinolytic effect due to inhibition of the inhibitor of tissue-type plasminogen activator.

Pharmacokinetics:

After oral administration metformin is absorbed from the gastrointestinal tract. Bioavailability after taking a standard dose is 50-60%. The maximum concentration in the blood plasma is achieved after 2.5 hours after ingestion. Virtually does not bind to plasma proteins. It accumulates in the salivary glands, muscles, liver and kidneys. It is allocated in an invariable kind by kidneys. The half-life is 9-12 hours.

With violations of kidney function, cumulation of the drug is possible.

Indications:

Type 2 diabetes mellitus without a tendency to ketoacidosis (especially in obese patients) with dietary inefficiency.

- in combination with insulin - in type 2 diabetes mellitus, especially with a pronounced degree of obesity, accompanied by secondary insulin resistance.

Contraindications:

- Diabetic ketoacidosis, diabetic precoma, coma;

- impaired renal function;

- acute diseases that occur at a risk of kidney dysfunction: dehydration (with diarrhea, vomiting), fever, severe infectious diseases, hypoxia conditions (shock, sepsis, kidney infections, bronchopulmonary diseases);

- clinically pronounced manifestations of acute and chronic diseases that lead to the development of tissue hypoxia (cardiac or respiratory failure, acute myocardial infarction, etc.);

- Serious surgical operations and traumas (when insulin therapy is shown);

- impaired liver function;

- chronic alcoholism, acute alcohol poisoning;

- pregnancy, the period of breastfeeding;

- hypersensitivity to the drug;

- lactic acidosis (including in the anamnesis);

- use for at least 2 days before and within 2 days after carrying out radioisotope or X-ray studies with the introduction of iodine-containing contrast medium;

- adherence to a hypocaloric diet (less than 1000 calories / day);

It is not recommended to use the drug in people over 60 years of age who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis.

Pregnancy and lactation:When planning pregnancy, as well as in case of pregnancy on the background of Metformin, it must be canceled and insulin therapy prescribed. Since there is no data on the penetration into breast milk, this drug is contraindicated in breastfeeding. If Metformin is needed during breastfeeding, breastfeeding should be discontinued.

Dosing and Administration:

The dose of the drug is set by the doctor individually depending on the level of glucose in the blood.

The initial dose is 500-1000 mg / day. (1-2 tablets). After 10-15 days, a further gradual increase in the dose, depending on the level of blood glucose, is possible.

The maintenance dose of the drug is usually 1500-2000 mg / day (3-4 tablets). The maximum dose is 3000 mg / day. (6 tablets).

In elderly patients, the recommended daily dose should not exceed 1 g (2 tablets).

Pills Metformin should be taken entirely 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 lactic acidosis, the dose of the drug should be reduced in case of severe metabolic disorders.

Side effects:

On the part of the digestive system: nausea, vomiting, "metallic" taste in the mouth, lack of appetite, diarrhea, flatulence, abdominal pain.

These symptoms occur especially often at the beginning of treatment and, as a rule, pass by themselves. These symptoms can reduce the use of anthocides, atropine derivatives or antispasmodics.

From the side of metabolism: in rare cases - lactic acidosis (requires discontinuation of treatment); with prolonged treatment - hypovitaminosis B12 (impaired absorption).

From the hematopoiesis: in some cases - megaloblastic anemia.

From the endocrine system: hypoglycemia.

Allergic reactions: skin rash.

Overdose:

With an overdose of Metformin, lactoacidosis can develop with a fatal outcome. The cause of the development of lactic acidosis may also be cumulation of the drug due to impaired renal function. The earliest symptoms of lactic acidosis are nausea, vomiting, diarrhea, lower body temperature, abdominal pain, muscle pains.In the future, there may be a rapid increase in respiration, dizziness, impaired consciousness and coma development.

Treatment: In case. the appearance of signs of lactic acidosis, treatment with Metformin should be stopped immediately, the patient immediately hospitalized and, after determining the concentration of lactate, confirm the diagnosis. The most effective measure for excretion from the body of lactate and metformin is hemodialysis. Conduct also symptomatic treatment.

When combined therapy with the drug Metformin with drugs of sulfonylureas may develop hypoglycemia.

Interaction:

Not recommended combinations: simultaneous danazol is not recommended to avoid hyperglycemia. If it is necessary to treat danazol and after stopping the intake of the latter, correction of the dose of metformin under the control of the level of glycemia is required.

Combinations that require special care: chlorpromazine - when taken in high doses (100 mg per day) increases glycemia, reducing the release of insulin. When treating with antipsychotics and after stopping the intake of the latter, correction of the dose of metformin is required under the control of the level of glycemia.

When used simultaneously with sulfonylurea derivatives, acarbose, insulin, non-steroidal anti-inflammatory agents, monoamine oxidase inhibitors, oxytetracycline, angiotensin converting enzyme inhibitors, clofibrate derivatives, cyclophosphamide, P-blockers, 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 effect of metformin is possible. Cimetidine slows the excretion of metformin, resulting in increased risk of lactic acidosis.

Metformin can weaken the effect of anticoagulants (coumarin derivatives).

Alcohol intake increases the risk of developing lactic acidosis during acute alcohol intoxication, especially in cases of fasting or low-calorie diet, as well as in liver failure.

Special instructions:

During the treatment it is necessary to monitor the kidney function. At least 2 times a year, as well as the appearance of myalgia should determine the content of lactate in the plasma.

In addition, once in 6 months, monitoring the level of serum creatinine (especially in patients, the elderly) should not be prescribed Metformin, if the level of creatinine in the blood is higher than 135 μmol / l in men and 110 μmol / l in women. Possible use of the drug Metformin in combination with sulfonylurea derivatives. In this case, a particularly careful control of the glucose level in the blood is necessary.

48 hours before and within 48 hours after radiopaque (urography, intravenous angiography), Metformin should be discontinued. If a patient develops bronchopulmonary infection or an infectious disease of the urogenital organs, the doctor should be informed immediately.

During treatment should refrain from taking alcohol and medications containing ethanol.

Effect on the ability to drive transp. cf. and fur:

The use of the drug in monotherapy does not affect the ability to drive vehicles and work with mechanisms.

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.

Form release / dosage:Intestinal-coated tablets 500 mg.

Packaging:For 10 tablets in a blister from AL / PVC. For 3 blisters together with instructions for use in a pack of cardboard.

Storage conditions:Store in a dry, protected from light place at a temperature of 15 to 25 ° C. Keep out of the reach of children!

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007322/08

Date of registration:12.09.2008 / 24.02.2016

Expiration Date:Unlimited

The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia

Manufacturer: & nbsp

Hemomont d.o.o. Montenegro

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp11.05.2018

Illustrated instructions

Instructions

Metformin (Metformin)