28.11.2020

Metformin

Metformin is a popular drug designed to reduce the content of glucose in the blood. The main purpose of the drug Metformin is the treatment of diabetes of the second type. The drug does not increase insulin production from the beta cells of the pancreas and gently control blood sugar, leading to its excessive reduction.

What is diabetes and how dangerous it is?

Diabetes mellitus is divided into two types. Type one diabetes is called insulin dependent. With this type of disease impaired synthesis in the pancreas of a special enzyme – the insulin involved in the breakdown of glucose. Type II diabetes is called insulin-independent. In this type of diabetes the pancreas is not violated, however, a decrease in insulin sensitivity in peripheral tissues and increases the production of glucose in the liver.

Most people are ill with diabetes of the second type in old age, recently, however, diabetes significantly “younger”. The reason for this was a sedentary lifestyle, stress, addiction to fast food and wrong eating habits. Meanwhile, diabetes is a dangerous disease that in the absence of significant external manifestations is many times increases the risk of early heart attack and stroke, abnormalities of the blood vessels. So scientists have long sought drugs that would help to reduce the blood sugar levels and thus would not harm the body.

The description of the drug

From the chemical point of view, Metformin belongs to biguanides, guanidine derivatives. The nature of the guanidine and / is contained in some plants, for example, Galega officinalis, which was used to treat diabetes since the middle ages. However, net guanidine and / is quite toxic to the liver.

Metformin was synthesized on the basis of guanidine in the 20-ies of the last century. It was already known about its hypoglycemic properties, however, because of the fashion on insulin medication for some time forgotten. Only since 1950-ies, when it became clear that treatment with insulin in case of diabetes of the second type has many shortcomings, the drug has been used as antidiabetic remedies and in a short time gained recognition due to its efficiency, safety and relatively small number of side effects and contraindications.

To date, Metformin is the most commonly prescribed antidiabeticeski drug in the world. It is included in the list of essential medicines of the who. It is well established that regular use of Metformin can reduce the risk of death from pathologies of the cardiovascular system caused by diabetes. Studies have shown that people suffering from excess weight and type II diabetes, treatment with Metformin is 30% percent more efficient than treatment with insulin and other antidiabetic drugs, and 40% more effective than treatment only through diet. The drug compared with other anti-diabetic remedies has less side effects, monotherapy is virtually threat of hypoglycemia, it very rarely causes a dangerous complication, lactic acidosis (poisoning of blood lactic acid).

Metformin belongs to a class of drugs intended for the treatment of type II diabetes. After taking Metformin reduces the concentration of blood glucose, glycosylated hemoglobin and increases the body’s tolerance to glucose. The drug is not carcinogenic, does not affect fertility.

The mechanism of therapeutic action of Metformin versatile. First, it reduces the production of glucose in the liver. In diabetes the second type, the production of glucose in the liver increased several times compared to the norm. Metformin reduces by one third this figure. This action is due to the activation by Metformin of certain liver enzymes that play an important role in the metabolism of glucose and fats.

However, the mechanism of Metformin reduce blood glucose not limited to the suppression of the formation of glucose in the liver. Metformin also has the following effects:

  • improves metabolic processes
  • reduces absorption of glucose from the intestine ,
  • improves glucose disposal in peripheral tissues,
  • increases tissue sensitivity to insulin,
  • it has a fibrinolytic action.

In the absence of blood insulin, the drug does not show its hypoglycemic activity. Unlike many other antidiabetic medications, Metformin does not lead to dangerous complications – lactic acidosis. In addition, it does not affect the production of insulin cells of the pancreas. Also, the drug is able to lower LDL “bad” cholesterol – low-density lipoprotein and triglycerides (not reducing the number of “good” cholesterol – high density lipoprotein), decrease the intensity of fat oxidation and production of free fatty acids. Importantly, Metformin eliminates the property of insulin to stimulate the formation of adipose tissue, whereby the drug has the ability to reduce or stabilize the body weight. The last property of Metformin is the reason that this drug is often used by those who want to lose weight.

It should also be noted the positive impact of the drug on the cardiovascular system. Metformin strengthens the smooth muscle of blood vessels, prevents the development of diabetic angiopathy.

Pharmacokinetics

Tablets Metformin presented in the form of hydrochloride. It is a colorless crystalline powder, soluble in water.

Metformin – a drug relative slow action. Usually positive effect from taking it begins to emerge 1-2 days later. In this period there is the equilibrium concentration of the drug in the blood, reaching 1 µg/ml. the maximum concentration of drug in the blood can be observed already after 2.5 h after administration. The drug weakly binds to the blood protein. The half-life is 9-12 h. write mainly kidneys unchanged.

In people with impaired kidney function may experience drug accumulation in the body.

Testimony

The main indication for use of the drug Metformin is a diabetes of the second type. The disease does not have to be complicated by ketoacidosis. It is preferable to prescribe the drug for patients who are not helps a low-carb diet, and patients who are overweight. In some cases, the drug can be used in combination with insulin. Also, the drug may sometimes be prescribed in gestational diabetes (diabetes caused by pregnancy).

Can be used the drug and in that case, if a person has violated tolerance to insulin, blood glucose does not exceed the critical. This condition is called prediabetes. However, most experts are inclined to believe that in this situation, a more useful exercise and diet and antidiabetic drugs with prediabetes do not have great efficiency.

In addition, the drug may be administered and in some other diseases, for example, when polycystic ovarian syndrome, nonalcoholic fatty liver disease, early puberty. These diseases have in common is that when they observed insensitivity of tissues to insulin. However, the efficacy of Metformin in these diseases does not yet have the same evidence as in diabetes. Sometimes the drug is used for weight loss, although the official medicine to this Metformin use treats with skepticism, especially if we are not talking about people with pathologically overweight.

Release form

The drug is available only in the form of tablets having a dosage of 500 and 1000 mg. there are Also tablets of prolonged action dosage of 850 mg, is coated with a special enteric-coated.

The main structural analogue of Metformin containing the same active substance, is a French remedy Glucophage. This drug is considered the original and other drugs with Metformin manufactured by different pharmaceutical companies worldwide – generics. The drug is released in pharmacies without a prescription.

Contraindications

The drug has a number of contraindications:

  • severe forms of heart, respiratory and kidney failure;
  • violation of the liver;
  • acute myocardial infarction;
  • acute violation of cerebral circulation;
  • diabetic ketoacidosis;
  • diabetic coma and precoma;
  • lactic acidosis (including in history);
  • diseases and conditions in which there is a risk of renal dysfunction;
  • dehydration;
  • severe infection (primarily respiratory and renal);
  • hypoxia;
  • shock;
  • sepsis;
  • severe surgical operation (in this case shown the use of insulin);
  • chronic alcoholism or alcohol intoxication (risk of lactic acidosis);
  • diagnostic studies with injections of iodine-containing substances (two days before the procedure and two days after);
  • hypocaloric diet (less than 1000 Kcal per day);
  • high level of creatinine in the blood (135 µmol/l in men and 115 µmol/l in women);
  • the syndrome of “diabetic foot”;
  • fever.

With caution should designate product for the elderly and people performing hard physical work (risk of lactic acidosis).

Not recommended the drug to patients younger than 18 years, pregnancy and lactation, hypersensitivity to the drug. In some cases it is possible to use the drug during pregnancy and in childhood (over 10 years) under strict medical supervision.

Special instructions

If treatment is ongoing, it is necessary to monitor renal function. At least twice a year to check the concentration of lactic acid in the blood. When pain in the muscles, you should immediately check the concentration of lactic acid.

Also 2-4 times a year you should check the functionality of the kidney (creatinine levels in the blood). This is especially true of older people.

In monotherapy, the drug has no effect on the Central nervous system, so the drug use from people driving vehicles and performing work that requires concentration.

Side effects

Main side effects while taking Metformin is associated with gastrointestinal tract. Often when the pill can be observed phenomena such as abdominal pain, nausea, vomiting, diarrhea, flatulence. To avoid this, you should take the tablets during or immediately after a meal. You may also receive a metallic taste in the mouth, lack of appetite, skin rash.

All of the above side effects do not pose a threat. They usually occur at the beginning of therapy and tested independently. In order to avoid unpleasant effects associated with the gastrointestinal tract, you can take antispasmodics or antacid.

Very rarely the medication may cause lactic acidosis, megaloblastic anemia, hypoglycemia, reduction in the production of thyroid hormones and testosterone in men. Hypoglycemia most often occurs in the case if, in conjunction with Metformin taken some antidiabetic drugs, such as sulfonylureas. With prolonged use of the drug may lead to vitamin B12 deficiency.

It is also possible hypoglycemic effects while taking NSAIDs, ACE inhibitors and MAO, beta-blockers, cyclophosphamide. When taking corticosteroids, epinephrine, sympathomimetics, diuretics, thyroid hormones, glucagon, estrogen, calcium antagonists, nicotinic acid, on the contrary, decreases the effect of the drug.

Medicines with iodine content can cause renal insufficiency and increase the risk of lactic acidosis. In cases of suspected lactic acidosis needs immediate hospitalization.

Usage instructions

As a rule, at the beginning of therapy the drug should be administered at 0.5-1 g once a day. This dosage should be followed for three days. From 4 to 14 days, you must take the pill Metformin 1 g three times a day. If the glucose level is decreased, the dose can be reduced. As a maintenance dose and should take the pills for Metformin 1500-2000 mg per day. In the case of tablets of prolonged action (850 mg), you should take the drug 1 tablet twice a day – morning and evening.

The maximum dose of 3 g (6 tablets of 500 mg) per day. The elderly may impair renal function, therefore the maximum daily dose they should not exceed 1000 mg (2 tablets of the drug at 500 mg). Also, they should not stop treatment with the drug, in such a case they should notify the doctor.

It is best to take the tablets immediately after eating, squeezed enough water. Taking the drug during a meal may reduce its absorption into the blood. The daily dose is divided into 2-3 reception.

The dosage of the drug when used together with insulin (dose of insulin less than 40 IU/day) is usually the same as without insulin. In the first days of Metformin do not reduce the dose of insulin. Subsequently, the insulin dose can be reduced. This process should be under the supervision of a physician.

Overdose

Metformin is a relatively safe drug and even his large dose (no drug interaction), as a rule, do not lead to a dangerous decrease of blood sugar. However, in overdose there is another, no less formidable danger – the increase in the concentration of lactic acid in the blood, called lactic acidosis. Symptoms of lactic acidosis are abdominal pain and muscles, modifying body temperature, impaired consciousness. This complication in the absence of medical care can lead to a lethal outcome as a result of development of coma. Therefore, in that case, if for some reason there was an overdose of the drug, the patient must be transported to the doctor. In case of overdose symptomatic therapy. Effective removal of the drug from the blood with hemodialysis.

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