Metfogamma^® (Tablets) Instructions for Use

ATC Code

A10BA02 (Metformin)

Active Substance

Metformin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Oral hypoglycemic drug

Pharmacotherapeutic Group

Oral hypoglycemic agent of the biguanide group

Pharmacological Action

An oral hypoglycemic drug from the biguanide group. It inhibits gluconeogenesis in the liver, reduces glucose absorption from the intestine, enhances peripheral glucose utilization, and increases tissue sensitivity to insulin. It does not affect insulin secretion by pancreatic beta-cells.

It reduces the level of triglycerides and LDL.

It stabilizes or reduces body weight.

It has a fibrinolytic effect due to the suppression of tissue-type plasminogen activator inhibitor.

Pharmacokinetics

Absorption

After oral administration, Metformin is absorbed from the gastrointestinal tract. The bioavailability after a standard dose is 50-60%. C_max after oral administration is reached after 2 hours.

Distribution

It practically does not bind to plasma proteins. It accumulates in the salivary glands, muscles, liver, and kidneys.

Elimination

It is excreted unchanged in the urine. T_1/2 is 1.5-4.5 hours.

Pharmacokinetics in special clinical cases

Accumulation of the drug is possible in cases of impaired renal function.

Indications

• Type 2 diabetes mellitus (non-insulin-dependent) without a tendency to ketoacidosis (especially in patients suffering from obesity) when diet therapy is ineffective.

ICD codes

Dosage Regimen

Tablets

The dose is set individually, taking into account the blood glucose level.

The initial dose is usually 850 mg (1 tablet)/day. A further gradual increase in the dose is possible depending on the therapy effect. The maintenance dose is 850-1700 mg (1-2 tablets)/day. The maximum daily dose is 2550 mg (3 tablets).

A daily dose exceeding 850 mg is recommended to be taken in 2 doses (in the morning and in the evening).

In elderly patients, the recommended dose should not exceed 850 mg/day.

The tablets should be taken with meals, swallowed whole with a small amount of liquid (a glass of water).

The drug is intended for long-term use.

Due to the increased risk of lactic acidosis, the dose of the drug should be reduced in cases of severe metabolic disorders.

Adverse Reactions

From the digestive system nausea, vomiting, abdominal pain, diarrhea, loss of appetite, metallic taste in the mouth (usually does not require discontinuation of treatment, and the symptoms disappear on their own without changing the drug dose; the frequency and severity of side effects can be reduced with a gradual increase in the metformin dose); rarely – pathological deviations in liver function tests, hepatitis (disappear after drug withdrawal).

Allergic reactions skin rash.

From the endocrine system hypoglycemia (when used in inadequate doses).

From the metabolism rarely – lactic acidosis (requires discontinuation of treatment), with long-term use – vitamin B₁₂ deficiency (absorption disorder).

From the hematopoietic system in some cases – megaloblastic anemia.

Contraindications

• Diabetic ketoacidosis, diabetic precoma, coma;
• Severe renal impairment;
• Cardiac and respiratory failure, acute phase of myocardial infarction, acute cerebrovascular accident, dehydration, chronic alcoholism and other conditions that may contribute to the development of lactic acidosis;
• Lactic acidosis and history of it;
• Major surgical operations and injuries (in these cases, insulin therapy is indicated);
• Liver dysfunction;
• Acute alcohol poisoning;
• Use for at least 2 days before and 2 days after radioisotope or X-ray examinations with the administration of iodine-containing contrast medium;
• Adherence to a hypocaloric diet (less than 1000 cal/day);
• Pregnancy;
• Lactation period (breastfeeding);
• Hypersensitivity to the drug components.

The drug is not recommended for use in patients over 60 years of age performing heavy physical work, due to the increased risk of developing lactic acidosis.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Special Precautions

During the use of the drug, indicators of renal function should be monitored. The lactate content in plasma should be determined at least 2 times a year, as well as when myalgia appears.

It is possible to use the drug Metfogamma^® 850 in combination with sulfonylurea derivatives or insulin, in which case especially careful monitoring of blood glucose levels is necessary.

Effect on the ability to drive vehicles and mechanisms

When used as monotherapy, the drug does not affect the ability to drive vehicles and work with mechanisms.

When metformin is combined with other hypoglycemic drugs (sulfonylurea derivatives, insulin), the development of hypoglycemic conditions is possible, in which the ability to drive vehicles and engage in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions is impaired.

Overdose

Symptoms the development of lactic acidosis with a fatal outcome is possible. The cause of lactic acidosis can also be the accumulation of the drug due to impaired renal function. Early symptoms of lactic acidosis are nausea, vomiting, diarrhea, decreased body temperature, abdominal pain, muscle pain; subsequently, rapid breathing, dizziness, impaired consciousness, and the development of coma are possible.

Treatment if signs of lactic acidosis appear, treatment with Metfogamma 850 must be stopped immediately, the patient must be urgently hospitalized and, after determining the lactate concentration, the diagnosis must be confirmed. Hemodialysis is most effective for removing lactate and metformin from the body. If necessary, symptomatic therapy is carried out.

Hypoglycemia may develop during combination therapy with sulfonylurea drugs.

Drug Interactions

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

With simultaneous use with corticosteroids, oral contraceptives, epinephrine (adrenaline), sympathomimetics, glucagon, thyroid hormones, thiazide and “loop” diuretics, phenothiazine derivatives, and nicotinic acid, the hypoglycemic effect of metformin may be reduced.

Cimetidine slows down the excretion of metformin, thereby increasing the risk of lactic acidosis.

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

With simultaneous intake with ethanol, the development of lactic acidosis is possible.

With simultaneous use, nifedipine increases the absorption of metformin, C_max, and slows down excretion.

Cationic drugs (amlodipine, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, vancomycin), which are secreted in the tubules, compete for tubular transport systems and, during long-term therapy, can increase the C_max of metformin by 60%.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 4 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.