Tephor

Tephor is a hypoglycemic medicine for oral administration.

Metformin is an oral hypoglycemic substance that belongs to the subgroup of biguanides with antihyperglycemic activity. [1]

Metformin hydrochloride helps to stimulate the processes of insulin secretion 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 Tephor

It is used for therapy in type 2 diabetes mellitus (insulin-independent form) in the absence of effect from diet therapy (especially in obese people).

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

Release form

The release of the drug element is realized in the form of tablets - 10 pieces each inside the cell pack; inside the package - 3 such packs.

Pharmacodynamics

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

• inhibition of the processes of intrahepatic glucose binding - through slowing down gluconeogenesis with glycogenolysis;
• an increase in cellular sensitivity to insulin with an increase in peripheral penetration and use of glucose by the muscles;
• stimulation of intracellular binding of collagen and increased movement of glucose into the area of the cell membrane.

Pharmacokinetics

Absorption.

Metformin is absorbed inside the small intestine and duodenum 12. The substance reaches the plasma Cmax and the maximum antidiabetic effect after 2-4 hours from the moment of application. 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.

Excretion.

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

Dosing and administration

The size of the portion of the medication is selected individually, taking into account the blood sugar values.

The initial dosage is 0.5-1 g per day. After 10-15 days, the portion may gradually increase (taking into account the glycemic indicators). The standard maintenance serving size is 1.5-2 g per day. The maximum allowable daily dosage is 3 g.

To weaken the negative symptoms associated with the work of the gastrointestinal tract, the daily portion should be divided into 2-3 uses. The tablets are used with or after food; you do not need to chew them.

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

• Application for children

Tephor is not prescribed in pediatrics.

Use Tephor during pregnancy

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

There is no clinical information regarding whether metformin hydrochloride is excreted in mother's milk, which is why it is not prescribed for lactation.

Contraindications

The main contraindications:

• severe intolerance to the active component or other elements of the drug;
• coma, diabetic ketoacidosis and diabetic coma;
• failure of the kidneys or weakened renal function (CC 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: insufficiency of respiratory or cardiac function, circulatory form of shock, or a recent myocardial infarction;
• leukemia;
• insufficiency of liver function;
• active form of alcohol poisoning;
• hypovitaminosis type B1;
• serious injury or surgery (which requires insulin therapy);
• lactate type of acidosis (also available in history);
• use for a period of at least 2 days before or after performing an X-ray or radioisotope procedures using an iodine contrast element;
• low-calorie diet regimen (less than 1000 calories per day).

It is forbidden to prescribe to people over the age of 60 who are engaged in hard physical labor - due to the high likelihood of lactate-type acidosis in them.

Side effects Tephor

Among the side effects:

• Digestive dysfunction: Mainly vomiting, bloating, metal taste, taste changes, nausea, abdominal pain, diarrhea and loss of appetite. Often, such signs develop at the initial stage of therapy and disappear on their own with its continuation. Weight loss is occasionally noted. To alleviate negative symptoms, you should take the medicine with food or immediately after it, 2-3 times a day. A gradual increase in dosage also helps to improve drug tolerance. With the constant presence of signs of dyspepsia, therapy should be discontinued;
• disorders of the activity of the National Assembly: often there is a taste disturbance. Occasionally, anxiety, fatigue, headaches and weakness appear;
• epidermal lesions: itching, urticaria, redness and rashes occur singly;
• problems with metabolic processes: a lactate form of acidosis develops singly. It is possible to weaken the absorption of folic acid and cyanocobalamin, as well as a decrease in their serum values with the further appearance of a megaloblastic form of anemia (with prolonged use of the drug);
• disorders associated with the hepatobiliary system: there are individual cases with a change in functional values during liver tests or the development of hepatitis. Hepatic function is restored after discontinuation of metformin use.

Overdose

Hypoglycemia is not observed with the introduction of portions up to 85 g, but at such dosages, the appearance of a lactate form of acidosis may occur. Risk factors, together with large doses of Tefora, increase the likelihood of the above violation.

Early signs of the disorder include vomiting, abdominal pain, diarrhea, nausea, fever, and muscle pain; further, the appearance of dizziness, respiratory and consciousness disorders, as well as the development of a coma is possible.

With the development of symptoms of the lactate form of acidosis, therapy should be canceled, and the patient should be immediately hospitalized, after which, having identified the level of lactate, the diagnosis should be confirmed. Infusion procedures are performed, as well as (in case of a severe degree of violation) hemodialysis. In addition, symptomatic actions are carried out.

Interactions with other drugs

You can not use the drug with alcoholic beverages, since in acute alcohol poisoning, the likelihood of developing lactate acidosis increases, especially with reduced weight, starvation or liver failure.

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

Topical and general corticosteroids, thiazides with other diuretics, gestagens, estrogens and other substances with hormonal influence, β-agonists, phenothiazines and channel blocking agents, Ca show 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 using these medications and after the end of their intake.

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

The bioavailability index of the drug increases when administered with famotidine, amiloride, morphine, and in addition 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 Tefora values increase, and the half-life and furosemide values also decrease.

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

Medicines that can provoke hyperglycemia (diuretic drugs, thyroid hormones, GCS, methionine, sympathomimetics and isoniazid) can weaken the effect of Tefora.

Reserpine with clonidine and guanethidine, and besides this, drugs that block the activity of ß-adrenergic receptors (taenolol with propranolol), with prolonged use, can provoke severe hypoglycemia.

The use of metformin increases the rate of excretion of coumarin derivatives, which is why it is necessary to monitor the blood-clotting function in persons using such a combination.

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

Salicylates with MAOIs, sulfonamides and other drugs that have a hypoglycemic effect change the effect of metformin hydrochloride.

Symptoms of hypoglycemia (such as tremors) can be masked by β-adrenergic blockers.

Cationic substances (among them morphine, trimethoprim and ranitidine with amiloride, vancomycin and procainamide with digoxin, as well as kinidine and cimetidine) and drugs excreted through the secretion of the tubules can reduce the rate of excretion of metformin hydrochloride (with varying degrees of intensity).

Storage conditions

Tephor must be kept out of the reach of small children, sunlight and moisture. Temperature level - maximum 30 ° C.

Shelf life

Tephor is allowed to be used within a 36-month term from the date of manufacture of the medicinal product.

Analogs

The analogs of the drug are the substances Glukofazh, Panfor s Bagomet, Metfogama and Insufor.