Tefor

Tefor is a hypoglycemic drug for oral use.

Metformin is an orally administered hypoglycemic agent that belongs to the biguanide subgroup, which has antihyperglycemic activity. [ 1 ]

Metformin hydrochloride helps stimulate insulin secretion processes and does not lead to the development of hypoglycemia. The active element has a positive effect on lipid metabolism – reducing LDL cholesterol, total cholesterol and triglycerides. [ 2 ]

Indications Tefor

It is used for the treatment of type 2 diabetes mellitus (non-insulin-dependent form) in the case of lack of effect from diet therapy (especially in obese individuals).

In combination with insulin, it is prescribed in cases of type 1 diabetes mellitus, especially in severe obesity accompanied by secondary insulin resistance.

Release form

The medicinal element is released in the form of tablets - 10 pieces per blister pack; there are 3 such packs inside the package.

Pharmacodynamics

The hypoglycemic effect in the case of metformin use is realized in 3 ways:

• inhibition of intrahepatic glucose binding processes – through slowing down gluconeogenesis with glycogenolysis;
• increased cellular sensitivity to insulin with increased peripheral penetration and utilization of glucose by muscles;
• stimulation of intracellular collagen binding and increased glucose transport into the cell membrane region.

Pharmacokinetics

Absorption.

Metformin is absorbed in the small intestine and duodenum. The substance reaches plasma Cmax and maximum antidiabetic effect after 2-4 hours from the moment of administration. The bioavailability level is 50-60%.

Distribution processes.

Small amounts of metformin hydrochloride are synthesized with protein. Some of the substance is also converted into red blood cells.

Withdrawal.

The half-life of metformin is 9-12 hours. It is excreted unchanged in the urine.

Dosing and administration

The dosage size of the medicine is selected individually, taking into account blood sugar levels.

The initial dosage is 0.5-1 g per day. After 10-15 days, the portion can be gradually increased (taking into account glycemic indicators). The size of the standard maintenance portion is 1.5-2 g per day. The maximum permissible daily dosage is 3 g.

To relieve negative symptoms associated with the gastrointestinal tract, the daily dose should be divided into 2-3 doses. Tablets are taken with or after food; there is no need to chew them.

The duration of the course is selected taking into account the severity of the pathology.

• Application for children

Tefor is not indicated in pediatrics.

Use Tefor during pregnancy

There is no epidemiological information regarding the use of Tefor during pregnancy, which is why it is not prescribed during this period. In pregnant women, blood sugar levels are regulated using insulin - to reduce the likelihood of congenital malformations associated with uncontrolled glycemia.

There are no clinical data on whether metformin hydrochloride is excreted in breast milk, which is why it is not prescribed during lactation.

Contraindications

Main contraindications:

• severe intolerance to the active component or other elements of the drug;
• comatose state, diabetic ketoacidosis and diabetic coma;
• renal failure or weakened renal function (creatinine clearance level is <60 ml per minute);
• acute stages of conditions that can affect kidney function: dehydration, severe infection, intravascular administration of iodine contrast agents and circulatory shock;
• alcoholism;
• active or chronic forms of conditions that can provoke hypoxia: respiratory or cardiac failure, circulatory shock, or a recent myocardial infarction;
• leukemia;
• liver failure;
• active form of alcohol poisoning;
• hypovitaminosis type B1;
• serious injuries or surgeries (which require insulin therapy);
• lactic acidosis (also present in the anamnesis);
• use for a period of at least 2 days before or after X-rays or radioisotope procedures using an iodine contrast element;
• low-calorie diet regimen (less than 1000 calories per day).

It is prohibited to prescribe to people over 60 years of age who are engaged in heavy physical labor - due to the high probability of developing lactate-type acidosis.

Side effects Tefor

Side effects include:

• digestive dysfunction: vomiting, bloating, metallic taste, taste change, nausea, abdominal pain, diarrhea and loss of appetite are mainly observed. Often, such signs develop at the initial stage of therapy and disappear on their own as it continues. Weight loss is occasionally observed. To relieve negative symptoms, the drug should be taken with food or immediately after it, 2-3 times a day. A gradual increase in dosage also helps to improve the tolerability of the drug. If signs of dyspepsia are constantly present, therapy should be discontinued;
• disorders of the nervous system: taste disturbances are often observed. Anxiety, fatigue, headaches and weakness occasionally appear;
• epidermal lesions: itching, urticaria, redness and rashes occur sporadically;
• problems with metabolic processes: lactic acidosis develops occasionally. It is possible that absorption of folic acid and cyanocobalamin may be weakened, as well as their serum values may decrease, with subsequent development of megaloblastic anemia (with prolonged use of the drug);
• Disorders associated with the hepatobiliary system: individual cases with changes in functional values during liver tests or the development of hepatitis are noted. Liver function is restored after discontinuation of metformin.

Overdose

Hypoglycemia is not observed when administering doses up to 85 g, but with such doses, the occurrence of lactate acidosis may be noted. Risk factors together with large doses of Tefor increase the likelihood of the above-mentioned disorder.

Early signs of the disorder include vomiting, abdominal pain, diarrhea, nausea, fever, and muscle pain; dizziness, respiratory distress, and loss of consciousness may occur, as well as the development of a comatose state.

If symptoms of lactate acidosis develop, therapy should be discontinued and the patient should be hospitalized immediately, after which the diagnosis can be confirmed by determining the lactate level. Infusion procedures are performed, as well as (in severe cases) hemodialysis. In addition, symptomatic actions are taken.

Interactions with other drugs

The drug should not be used with alcoholic beverages, since acute alcohol poisoning increases the likelihood of developing lactic acidosis, especially in cases of reduced weight, starvation, or liver failure.

It is prohibited to use together with iodine contrast elements, since their intravenous administration in radiology can provoke renal failure, which may lead to accumulation of metformin hydrochloride and development of lactate acidosis. It is necessary to cancel the drug before the procedure and not to use it for at least 48 hours after the end of the study.

Topical and general GCS, thiazides with other diuretics, gestagens, estrogens and other substances with hormonal effect, β-agonists, phenothiazines and agents blocking the action of channels, Ca demonstrate a hyperglycemic effect. Therefore, when combined with these drugs, it is necessary to constantly monitor blood sugar values, especially at the beginning of treatment. If necessary, antidiabetic therapy can be selected for the period of use of these drugs and after their completion.

The drug demonstrates synergistic activity when used with insulin, sulfonylurea derivatives and acarbose.

The bioavailability of the drug increases when administered with famotidine, amiloride, morphine, and also with cimetidine, digoxin, triamterene and quinidine. In addition, the list includes substances that block the action of Ca channels, trimethoprim with procainamide and ranitidine.

When combined with furosemide, serum values of Tefor increase, and the half-life and indicators of furosemide decrease.

Use with probenecid, rifampicin, clofibrate, salicylates, propranolol and sulfonamides requires a reduction in the dosage of the drug.

Medicines that can provoke hyperglycemia (diuretics, thyroid hormones, glucocorticosteroids, methionine, sympathomimetics and isoniazid) can weaken the effect of Tefor.

Reserpine with clonidine and guanethidine, as well as agents that block the activity of ß-adrenergic receptors (taenolol with propranolol), when taken for a long time, can provoke severe hypoglycemia.

The use of metformin increases the rate of excretion of coumarin derivatives, which is why blood coagulation function should be monitored in individuals using this combination.

ACE inhibitors can provoke hypoglycemia, which is why when using drugs with them in combination, it may be necessary to adjust antidiabetic treatment.

Salicylates with MAOIs, sulfonamides and other drugs with hypoglycemic effect alter the effect of metformin hydrochloride.

Symptoms of hypoglycemia (such as tremor) may be masked by β-adrenergic blockers.

Cationic substances (including morphine, trimethoprim and ranitidine with amiloride, vancomycin and procainamide with digoxin, as well as quinidine and cimetidine) and drugs excreted via tubular secretion can reduce the excretion rate of metformin hydrochloride (with varying degrees of intensity).

Storage conditions

Tefor must be stored in a place protected from small children, sunlight and moisture. Temperature level – maximum 30°C.

Shelf life

Tefor is approved for use within a 36-month period from the date of manufacture of the medicinal product.

Analogues

The analogs of the drug are Glucophage, Panfor with Bagomet, Metfogama and Insufor.