Universal reference book for medicines

Active substance: metformin

Type: Oral hypoglycemic drug

Manufacturer: ZENTIVA (Slovak Republic)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Oral hypoglycemic agent from the biguanide group (dimethyl biguanide).
The mechanism of action of metformin is related to its ability to suppress gluconeogenesis, as well as the formation of free fatty acids and the oxidation of fats. Increases the sensitivity of peripheral receptors to insulin and the utilization of glucose by cells.Metformin does not affect the amount of insulin in the blood, but changes its pharmacodynamics by reducing the ratio of bound insulin to free and increasing the ratio of insulin to proinsulin.
Metformin stimulates the synthesis of glycogen, affecting glycogen synthetase.
Increases the transport capacity of all types of glucose transporters. Delays the absorption of glucose in the intestine.
Reduces the level of triglycerides, LDL, VLDL.
Metformin improves the fibrinolytic properties of the blood by suppressing the inhibitor of the tissue type plasminogen activator.
On the background of taking metformin, the patient's body weight either remains stable or moderately decreases.

After ingestion, metformin is slowly and incompletely absorbed from the digestive tract.
C max in plasma is achieved after about 2.5 hours. With a single dose of 500 mg, absolute bioavailability is 50-60%. With simultaneous intake of food, absorption of metformin is reduced and delayed.
Metformin is quickly distributed into the tissues of the body.
Virtually does not bind to plasma proteins. It accumulates in salivary glands, liver and kidneys.
It is excreted by the kidneys unchanged.
T 1/2 from the plasma is 2-6 hours.
With violations of kidney function, cumulation of metformin is possible.

Diabetes mellitus type 2 (non-insulin-dependent) with ineffective diet and exercise, in obese patients: in adults - as monotherapy or in combination with other oral hypoglycemic agents or with insulin;
in children aged 10 years and older - as a monotherapy or in combination with insulin.
Is taken orally, during or after a meal.

The dose and frequency of administration depends on the dosage form used.

In monotherapy, the initial single dose for adults is 500 mg, depending on the dosage form used, the frequency of administration is 1-3 times / day.
Possible application of 850 mg 1-2 times / day. If necessary, the dose is gradually increased with an interval of 1 week. up to 2-3 g / day.
With monotherapy for children aged 10 years and older, the initial dose is 500 mg or 850 1 time / day or 500 mg 2 times / day.
If necessary, with an interval of at least 1 week, the dose may be increased to a maximum of 2 g / day in 2-3 doses.
After 10-15 days the dose should be adjusted based on the results of the determination of glucose in the blood.

With combined therapy with insulin, the initial dose of metformin is 500-850 mg 2-3 times / day.
The dose of insulin is selected based on the results of the determination of glucose in the blood.
On the part of the digestive system: nausea, vomiting, diarrhea, flatulence, a feeling of discomfort in the abdomen are possible (usually at the beginning of treatment);in isolated cases - a violation of liver function indicators, hepatitis (disappear after discontinuation of treatment).

From the side of metabolism: very rarely - lactate-acidosis (requires discontinuation of treatment).

From the hemopoietic system: very rarely - a violation of absorption of vitamin B 12 .

The profile of adverse reactions in children aged 10 years and older is the same as in adults.

Acute or chronic metabolic acidosis, diabetic ketoacidosis, diabetic precoma and coma;
renal failure, impaired renal function (CK <60 mL / min); dehydration, severe infection, hypoglycemic shock, which can lead to impaired renal function; clinically pronounced symptoms of acute and chronic diseases that can lead to the development of tissue hypoxia (including heart failure, acute myocardial infarction, respiratory failure); use of contrasting iodine-containing substances for intravascular administration (including for intravenous urography, intravenous cholangiography, angiography, CT); acute alcohol intoxication, chronic alcoholism;increased sensitivity to metformin.
Adequate and strictly controlled studies of the safety of metformin during pregnancy have not been conducted.
Application in pregnancy is possible in cases of extreme necessity, when the expected benefit of therapy for the mother exceeds the possible risk to the fetus. Metformin penetrates the placental barrier.
Metformin is released in small amounts with breast milk, while the concentration of metformin in breast milk may be 1/3 of the concentration in the mother's plasma.Side effects in newborns with breastfeeding against metformin were not observed.
However, due to the limited amount of data, use during breastfeeding is not recommended. The decision to stop breastfeeding should be taken in consideration of the benefits of breastfeeding and the potential risk of side effects in the child.
Pre-clinical studies have shown that metformin does not have teratogenic effects in doses that are 2-3 times higher than the therapeutic doses used in humans.Metformin does not have a mutagenic potential, does not affect fertility.

Contraindicated in severe impairment of kidney function.

Contraindicated in severe violations of liver function.

It is not recommended to use metformin in patients older than 60 years, which is associated with an increased risk of developing lactic acidosis.

Application is not recommended for acute infections, exacerbation of chronic infectious and inflammatory diseases, traumas, acute surgical diseases, the danger of dehydration.

Do not apply before surgery and within 2 days after their conduct.

Precautions should be taken with metformin in elderly patients and persons performing heavy physical work, which is associated with an increased risk of lactic acidosis.
In patients of senile age, asymptomatic renal dysfunction is often observed. Particular caution is required if the renal impairment is triggered by the use of antihypertensive drugs or diuretics, as well as NSAIDs.
If during the treatment the patient has muscle cramps, digestive disorders (abdominal pains) and severe asthenia, it should be borne in mind that these symptoms may indicate the onset of lactic acidosis.

During the treatment it is necessary to monitor the kidney function;
the plasma lactate content should be determined at least twice a year, as well as with the appearance of myalgia.
When metformin is used in the form of monotherapy in accordance with the dosage regimen, hypoglycemia usually does not occur.
However, when combined with insulin or with sulfonylureas, there is a risk of developing hypoglycemia. In such cases, a particularly careful control of the concentration of glucose in the blood is necessary.
During the treatment, patients should avoid drinking alcohol because of the risk of developing lactic acidosis.

Pre-clinical studies have shown that metformin does not have a carcinogenic potential.

When used simultaneously with derivatives of sulfonylurea, acarbose, insulin, salicylates, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate, cyclophosphamide, hypoglycemic action of metformin may be enhanced.

When used simultaneously with GCS, hormonal contraceptives for oral administration, danazolum, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, thiazide diuretics, nicotinic acid derivatives, a decrease in the hypoglycemic effect of metformin is possible.

In patients receiving metformin, the use of iodine-containing contrast agents for the purpose of conducting diagnostic tests (including intravenous urography, intravenous cholangiography, angiography, CT) increases the risk of acute renal dysfunction and lactic acidosis.
These combinations are contraindicated.
Beta 2 -adrenomimetiki in the form of injections increase the concentration of glucose in the blood due to stimulation?
2- adrenoreceptors. In this case, it is necessary to monitor the concentration of glucose in the blood. If necessary, it is recommended to prescribe insulin.
Simultaneous administration of cimetidine may increase the risk of developing lactic acidosis.

Simultaneous reception of "loop" diuretics can lead to the development of lactate-acidosis due to possible functional renal failure.

The simultaneous intake of ethanol increases the risk of developing lactic acidosis.

Nifedipine increases the absorption and C max of metformin.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim and vancomycin) secreted in the renal tubules compete with metformin over the tubular transport systems and can lead to an increase in its C max .

Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!