In the sixties of the twentieth century, biochemists defined the basic concept of the mechanism of the development of type 2 diabetes - obesity is accompanied by insulin resistance, which in turn causes hyperinsulinemia, and as a result leads to an absolute deficiency of insulin and hyperglycemia.
Insulin resistance of muscle, adipose tissue and hepatic cells is genetically determined, the main component of the origin of type 2 diabetes mellitus, closely associated with such pathological conditions as dyspidemia, obesity, hypertension.
In clinical practice, for more than half a century, a biguanide class preparation( Glucophage( metformin hydrochloride)) has been used for the treatment of type 2 diabetes.
Form release, pharmacological action
The preparation is produced in the form of round, biconvex tablets of white color, coated with a film membrane. Each Glucophage tablet contains an active ingredient - metformin hydrochloride( 500, 850, 1000 mg) and ancillary elements - magnesium stearate,
Long-acting Glucophage Long contains 750 mg of metformin hydrochloride and additional components - magnesium stearate, hypromellose and povidone.
Metformin is an active substance that has a pronounced hypoglycemic property that develops only in conditions of hypoglycemia, that is, in people with normal blood glucose levels. The substance has no hypoglycemic effect.
The mechanism of action of Glucophage and Glucophage Long is based on the ability to inhibit glycogenolysis and gluconeogenesis, reduce glucose absorption in the gastrointestinal tract and increase insulin sensitivity. The drug contributes to an effective reduction in the production of glucose in the liver, actively reduces its concentration in the blood plasma and stimulates the utilization of glucose in the muscles.
Metformin, in addition to pronounced antihyperglycemic action, has the effect of improving lipid metabolism, reducing the level of cholesterol, triglycerides and lipoproteins. Also, it is able to reduce and stabilize the weight, therefore, specialists sometimes appoint Glucophage for weight loss.
The drug is adsorbed in the gastrointestinal tract, the peak concentration in the plasma is reached after 2-2,5 hours after administration. The time of maximum plasma concentration of metformin in Glucophage Long is 7 hours. This property of the drug is used to reduce possible side effects.
When ingested, the absolute bioavailability reaches 50-60%.The substance in the body is practically not metabolized and is mainly excreted by the kidneys, only a small percentage - by the intestine. There are reviews of Glucophage, confirming its ability to reduce appetite.
Indications and contra-indications for use
The instruction for Glucophage recommends the prescription of a drug for patients suffering from type 2 diabetes mellitus, accompanied by a pronounced obesity. Glucophage and Glucophage Long can be used both in monotherapy and in combination with insulin or other hypoglycemic substances. The instruction to Glucophage informs that the drug can be prescribed to adults and children from 10 years of age.
Numerous reviews of Glucophage show its good tolerability, however, like any drug substance, this drug has a list of certain contraindications. Glucophage can not be administered to people who are hypersensitive to the components of the drug, for the treatment of diabetic ketoacidosis or diabetic coma.
The Glucophage Instruction prohibits the use of the drug in cases of impaired renal function, and in the case of severe conditions that may be accompanied by similar disorders, including shock, complex forms of infectious diseases, dehydration.
The drug can not be used in the following cases:
- for violations of the liver;
- for respiratory or heart failure, diseases that are accompanied by hypoxia, myocardial infarction;
- on a background of a hypocaloric diet;
- for chronic alcoholism or acute alcohol poisoning.
It is forbidden to take the drug before surgery, during lactation and pregnancy. It is not recommended to appoint Glucophage to people over 60 years of age and adolescents during puberty.
Glucophage Instruction how to apply correctly
The drug is intended for oral use, the coated tablet should be swallowed without chewing, and washed down with a sufficient amount of liquid. The drug is taken after or during meals.
When combined or monotherapy, for adults, the initial dose of glucosulphate is 500-850 mg, taken two to three times a day. Supportive dose of the drug varies from 1500 to 2000 mg per day, take the substance needed two to three times a day. The maximum daily dose of glucosulphate should not exceed 3000 mg.
For children and adolescents, Glucophage is prescribed in an initial dose of 500 mg, which should be taken two to three times a day. Ten days after the start of therapy, the dose of the drug is adjusted and can be increased to 2000 mg per day, but no more. Adequate dosage of the drug to elderly people is calculated strictly individually.
Glucophage Long adults are usually prescribed to take one tablet, once a day, in the evening. Ten days after the start of the therapeutic course, the dosage is adjusted depending on the level of glucose in the blood plasma. The drug of prolonged action to children under eighteen years is not appointed.
Take glucose for weight loss in a person who does not have diabetes, in a minimum dose, 2-3 times a day, 500 mg each. The course of treatment should be no more than three months, and it can be repeated only after a break of at least three months. Using Glukofazh for weight loss, it is strictly forbidden to take alcohol, starve, conduct debilitating sports training, take diuretics, vitamins and medicinal substances that contain iodine. Taking glucosulphate for weight loss, it must be remembered that the drug is intended for the treatment of diabetes, so it should be taken only under the supervision and on the appointment of a doctor.
Although the drug is well tolerated when treated correctly, and many reviews of Glucophage have confirmed this, there have been a number of reported side effects:
- appearance of metallic taste in the mouth;
- lack of appetite, general weakness, nausea, diarrhea, myalgia, vomiting;
- allergic reactions in the form of itching or skin rashes.
In case of manifestation of such clinical symptoms, it is necessary to stop taking the drug for a while and adjust the dosage. Specific treatment is not required, usually the symptoms go away on their own. On the part of the hematopoietic system, megaloblastic anemia can occur. Very rarely there are reviews of Glucophage, indicating the development of various violations of the functions of the liver and metabolism.
This drug should be extremely carefully prescribed in conjunction with other drugs, especially those that in any way affect the synthesis of insulin.
Analogues of Glucophage - Siofor, Glimifor, Metformin, Bagomet.