Metformin

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Available since: 2019-09-19

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Clinical Pharmacology

Oral hypoglycemic agent from the group of biguanides (dimethylbiguanide). The mechanism of action of metformin is associated with its ability to inhibit gluconeogenesis, as well as the formation of free fatty acids and fat oxidation. Increases the sensitivity of peripheral insulin receptors and glucose utilization 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 glycogen synthesis by acting on glycogen synthase. Increases the transport capacity of all types of membrane glucose transporters. Delays the absorption of glucose in the intestine.

Reduces triglycerides, LDL, VLDL. Metformin improves blood fibrinolytic properties by suppressing a tissue-type plasminogen activator inhibitor.

While taking metformin, the patient's body weight either remains stable or decreases moderately.

Pharmacokinetics

After oral administration, metformin is slowly and completely absorbed from the gastrointestinal tract. Cmax in plasma is reached in approximately 2.5 hours. With a single dose of 500 mg, the absolute bioavailability is 50-60%. With a simultaneous meal, the absorption of metformin is reduced and delayed.

Metformin is rapidly distributed in body tissues. Practically does not bind to plasma proteins. Accumulates in the salivary glands, liver and kidneys.

Excreted by the kidneys in unchanged form. T1 / 2 of plasma is 2-6 hours.

In case of impaired renal function, cumulation of metformin is possible.

Indications

Diabetes mellitus type 2 (insulin-independent) with the ineffectiveness of diet therapy and exercise, in patients with obesity: in adults - as monotherapy or in combination with other oral hypoglycemic agents or insulin; in children aged 10 years and older - as monotherapy or in combination with insulin.

Composition

pills with a prolonged release of white or almost white, oval, biconvex.

	1 tab.
metformin hydrochloride	750 mg

Excipients: hypromellose 2208 (hydroxypropyl methylcellulose 2208), hypromellose (hydroxypropyl methyl cellulose) 2910, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose.

Metformin is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Metformin Long Canon			pills
			pills
Metformin-Teva	Teva	Israel	pills
Metformin	Canonpharma	Russia	pills
Siofor	Berlin-Chemie/Menarini	Germany	pills
Formetin	Pharmstandard	Russia	pills
Metformin-richter	Gedeon Richter	Hungary	pills
Glucophage Long	Merck sante	France	pills
Gliformin	Akrikhin	Russia	pills
Glucophage	Merck sante	France	pills

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Dosage and Administration

Metformin should be administered during or after a meal.

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

With monotherapy, the initial single dose for adults is 500 mg, depending on the dosage form used, the multiplicity of intake is 1-3 times / day. Perhaps the use of 850 mg 1-2 times / day. If necessary, gradually increase the dose 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 can be increased to a maximum of 2 g / day in 2-3 doses.

After 10-15 days, the dose must be adjusted based on the results of determination of glucose in the blood.

In combination therapy with insulin, the initial dose of metformin is 500-850 mg 2-3 times / day. The insulin dose is selected based on the results of the determination of glucose in the blood.

Adverse reactions

On the part of the digestive system: possible (usually at the beginning of treatment) nausea, vomiting, diarrhea, flatulence, discomfort in the abdomen; in rare cases - violation of liver function indicators, hepatitis (disappear after stopping treatment).

Metabolism: very rarely - lactate acidosis (discontinuation of treatment is required).

On the part of the blood system: very rarely - a violation of the absorption of vitamin B12.

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

Contraindications

Acute or chronic metabolic acidosis, diabetic ketoacidosis, diabetic precoma and coma; renal failure, impaired renal function (CC less than 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); the use of contrast iodine-containing substances for intravascular administration (including during intravenous urography, intravenous cholangiography, angiography, CT); acute alcohol intoxication, chronic alcoholism; hypersensitivity to metformin.

Drug interactions

With simultaneous use with sulfonylurea derivatives, acarbose, insulin, salicylates, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate, cyclophosphamide, the hypoglycemic effect of metformin may be enhanced.

With simultaneous use with GCS, hormonal contraceptives for oral administration, danazol, epinephrine, glucagon, thyroid hormones, phenothiazine derivatives, thiazide diuretics, nicotinic acid derivatives may reduce the hypoglycemic action of metformin.

In patients receiving metformin, the use of iodine-containing contrast agents for the purpose of conducting diagnostic studies (including IV urography, IV cholangiography, angiography, CT) increases the risk of developing acute renal dysfunction and lactate acidosis. These combinations are contraindicated.

Beta2-adrenergici in the form of injections increase the concentration of glucose in the blood due to stimulation of β2-adrenergic receptors. In this case, the control of blood glucose concentration is necessary. If necessary, it is recommended to appoint insulin.

Simultaneous use of cimetidine may increase the risk of lactic acidosis.

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

Pro concomitant use with ethanol increases the risk of lactic acidosis.

Nifedipine increases the absorption and Cmax of metformin.

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

Pregnancy and Lactation

Adequate and strictly controlled studies of the safety of metformin in pregnancy have not been conducted. Use during 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 in small amounts is excreted in breast milk, while the concentration of metformin in breast milk can be 1/3 of the concentration in the mother's plasma. Side effects in newborns during breastfeeding while taking 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 made taking into account the benefits of breastfeeding and the potential risk of side effects in the child.

Special instructions

Not recommended for use in acute infections, exacerbations of chronic infectious and inflammatory diseases, injuries, acute surgical diseases, the risk of dehydration.

Do not apply before surgery and for 2 days after their implementation.

Caution should be used metformin in elderly patients and those performing heavy physical work, which is associated with an increased risk of developing lactic acidosis. Elderly patients often have asymptomatic renal dysfunction. Special care is required if the renal dysfunction is triggered by taking antihypertensive drugs or diuretics, as well as NSAIDs.

If during treatment the patient has muscle cramps, indigestion (abdominal pain) and severe asthenia, then it should be borne in mind that these symptoms may indicate the onset of lactic acidosis.

During treatment, it is necessary to monitor renal function; determination of plasma lactate should be carried out at least 2 times a year, as well as the appearance of myalgia.

When using metformin as monotherapy in accordance with the dosing regimen, hypoglycemia does not usually occur. However, when combined with insulin or sulfonylurea derivatives, there is a risk of hypoglycemia. In such cases, particularly careful monitoring of glucose concentration in the blood is necessary.

During treatment, patients should avoid alcohol because of the risk of lactic acidosis.

Preclinical studies have shown that metformin does not have carcinogenic potential.