The pharmaceutical market is replenished with drugs that effectively reduce the level of glucose in the blood.Such drugs are especially necessary for patients with diabetes mellitus, but have many side effects. The year 1957 supplemented the list with three drugs at once — phenformin, buformin, metformin.
Of these, only the last drug has taken root and is actively used in clinical practice.Metformin is prescribed to diabetics, for the treatment of polycystic ovary syndrome, in combination with diet and exercise – to reduce body weight.What is Metformin? Leading positions in the treatment of type 2 diabetes took Metformin.He belongs to the biguanides.
These are substances that reduce the level of glucose in the blood.The effectiveness of the means is proved by time, practice of application, as evidenced by patient reviews.This is the only medical product that is used to treat diabetes in children.Metformin has several names, it is given as Glucophage .
Composition and release form
Metformin is available in pill form.They are round, biconvex, covered with an enteric coating of white color.Packed medicine in blisters of 10 or 15 pieces.Carton packs will contain 30 tablets.Each tablet can be 500 mg, 850 mg or 1000 mg of the active ingredient Metformin hydrochloride.
Pharmacodynamics and pharmacokinetics Metformin inhibits the synthesis of ATP (adenosine triphosphate) in mitochondria (specialized cell organelles).This process has a direct impact on a number of biochemical reactions associated with carbohydrate metabolism.
Once in the body, dimethylbiguanide causes a decrease in sugar concentration due to several mechanisms: it inhibits gluconeogenesis (the formation of glucose from non-carbohydrate compounds) in the liver;increases the sensitivity of tissues to insulin;improves glucose utilization by cells;slows the absorption of glucose in the small intestine.
Under the action of the drug after a meal, there is no drastic change in the level of glucose.Drug: does not cause hypoglycemia (pathology associated with a decrease in the level of glucose);no effect on insulin synthesis;reduces the level of triglycerides, low density lipoproteins in the blood plasma;It has a fibrinolytic (thrombo-absorbing) effect due to the inhibition of a tissue plasminogen activator inhibitor (a protein that promotes the synthesis of a fibrinolytic enzyme).
Drug absorption occurs from the gastrointestinal tract.The standard dose of the drug has 50-60% bioavailability.Metformin does not react with blood proteins.The substance accumulates in the salivary glands, muscle tissues, kidneys, and liver.
Excreted by the kidneys unchanged.Monotherapy with metformin compared with other drugs to normalize sugar levels reduces: the risk of myocardial infarction;death rates in patients with type 2 diabetes.
Indications for use
This medication is on the list of essential medications approved by WHO (World Health Organization).
Metformin is prescribed for such conditions as: Diabetes mellitus type 2 (insulin dependence).Statistics on the use of the drug fixes a decrease in the mortality of patients by 30% compared with other drugs prescribed for diabetes.Positive dynamics is observed in all patients, especially in patients with overweight.Pre-diabetes (increased risk of diabetes).Polycystic ovary syndrome.The drug began to be used for the treatment of PCOS at the turn of the 80-90s of the twentieth century.The connection of this pathology with the hypersecretion of insulin, a violation of the metabolic response of tissues to insulin during a normal reaction to this ovarian hormone was revealed.When dimethylbiguanide is included in the complex of medicines, 80% of women diagnosed with polycystic disease have a positive dynamic.Obesity treatment.Metabolic syndrome.
How to take
Tablets are swallowed whole, washed down with plenty of water.The initial minimum dose is 500 mg 1 time per day, the maximum – 2 , 5 -3 g.
It is recommended to take Metformin tablets after dinner or immediately before bedtime.The dosage of the drug is best increased gradually.A large initial dose of dimethylbiguanide causes gastric dysfunction and disrupts digestion.Metallic taste, nausea – signs of overdose in the initial stages of the use of the drug.
In case of monotherapy with a drug, it is better to adhere to the proven scheme: In the first week, the medicine in the amount of 500 mg is taken 1 time.Next, increase the daily dose to 850-1000 mg and divide it into 2 doses.
If the metabolic processes are not satisfactory with a maximum dose of 2000 mg, sulfonylureas should be added to metformin or insulin should be used.Increasing the dosage depends on the glucose values.The regimen is selected by the doctor individually.In elderly patients, the maximum daily dose is 1000 mg.
As the drug is taken it is necessary to control the functionality of the kidneys.2 times a year it is important to determine the level of lactate (lactic acid) in the plasma.This is a must if muscle pain occurs.
An important indicator is the level of creatinine (metabolite in the protein metabolism).It characterizes the state of the muscular system and kidneys.Analysis to determine the concentration of this substance should be carried out 1 time in half a year.
The drug should be stopped 2 days before and 2 days after the radiopaque study.If you have a bronchopulmonary infection, infectious diseases of the urogenital system, you should immediately contact your doctor.The drug affects the ability to drive machinery and vehicles.
Against the background of hormonal imbalance, pregnant women may develop gestational diabetes.Long-term clinical experience of using metformin during pregnancy proves its efficacy and safety in the treatment of diabetes.The active substance passes through the placenta, but does not cause pathologies of fetal development.Doctors in some cases consider this drug as an alternative to insulin for the treatment of type 2 diabetes in pregnant women.For children The drug is prescribed to children from 10 years of age with diagnosed insulin-dependent diabetes, which is accompanied by obesity, in other cases according to the instructions, it is contraindicated up to 18 years.Diabetes cure Metformin is prescribed as mototherapy, in combination with other hypoglycemic drugs or insulin.
The drug is indicated for children in the absence of a therapeutic effect of a hypoglycemic diet.The dosage and duration of treatment is determined by the attending physician.The standard treatment regimen involves the use of 500-850 mg of the drug 1 time.If necessary, within two weeks, the dosage is gradually increased.The maximum permissible amount of active ingredient is 2000 mg.
With complex treatment, the amount of insulin is selected in accordance with the level of glucose.Metformin for weight loss About the bottom of the names of the drug on the pharmaceutical market – Glucophage, or “glucose eater.”
T Which effect is achieved by the simultaneous launch of multiple biochemical mechanisms which contribute to weight loss: accelerated oxidation of fatty acids;digestion of sugar, which gets from the gastrointestinal tract (GIT), decreases;suppressed glucose synthesis in the liver;increases the sensitivity of insulin receptors;muscle tissue more actively consumes glucose;by reducing insulin levels, nutrients are not converted into fat and are not deposited in the stock;absorption of fat in the gastrointestinal tract and blood plasma decreases, the formation and deposition of fatty tissue in the liver decreases.
To prevent the occurrence of hyperglycemia, the drug is not prescribed simultaneously with danazol.Caution required combination with chlorpromazine and neuroleptics.In these cases, the dosage of dimethylbiguanide depends on the level of sugar.The increased hypoglycemic effect of the drug is observed when it is used simultaneously with: sulfonylurea;insulin;acarbose;inhibitors of monoamine oxidase (MAO) (an enzyme that is contained in the nerve endings and contributes to an increase in the concentration of serotonin, dopamine, norepinephrine and other monoamines in the synapse due to their destruction);oxytetracycline;ACE inhibitors (angiotensin-converting enzyme) (drugs that help with hypertension);beta blockers;clofibrate derivatives;cyclophosphamide.Increases the risk of lactic acidosis in patients receiving cimetidine.
Metformin reduces the effects of anticoagulants.A decrease in the hypoglycemic effect of the drug is observed in combination with: glucocorticosteroids;oral contraceptives;glucagon;epinephrine;diuretics;thyroid hormones;derivatives of nicotinic acid.
The use of Metformin is not recommended against the backdrop of alcohol.Great risk of lactic acidosis – a sharp increase in the concentration of lactic acid.This condition is extremely dangerous.According to statistics, mortality from lactic acidosis is from 50 to 90%.The risk group includes diabetics over 50 years of age, in whom the condition is aggravated by chronic diseases of the kidneys, liver, heart and blood vessels.
Symptoms of lactic acidosis in this case occur simultaneously with diabetic coma.
The most dangerous condition that can occur with metformin therapy is lactic acidosis.With proper treatment, the risk of its occurrence is negligible.Side effects on the use of the drug are observed on the part of the digestive system: intestinal upset;nausea, vomiting;stomach ache;decreased appetite;metallic taste.All symptoms occur in the initial stages of therapy and disappear on their own as the drug is consumed.In case of hypersensitivity to the active substance of the pharmaceutical agent, allergic reactions may occur.
These are skin rashes and redness.With prolonged treatment, the absorption of vitamin B12 is impaired, the risk of hypoglycemia increases.Anorexia and anemia are described as side effects.The girl put her hands to the stomach
With non-compliance with the treatment regimen, improper dosage of the drug develops lactic acidosis.The accumulation of the drug contributes to renal dysfunction.
Symptoms of overdose: diarrhea;vomiting;nausea;abdominal and muscle pain;decrease in body temperature;dizziness;rapid breathing;convulsions;disturbance of consciousness;development of coma.When the symptoms described, the drug should be stopped immediately, the patient should be hospitalized, the concentration of lactate should be determined, the diagnosis should be clarified.Hemodialysis is the most effective measure for lactic acidosis.Symptomatic treatment to restore vital functions is carried out after the withdrawal of the drug from the body.
The drug metformin has numerous contraindications.They are associated with acute, chronic diseases of the patient, his lifestyle, special conditions.These are: kidney dysfunction;diabetic ketoacidosis (a condition associated with dehydration due to insulin deficiency);diabetic coma or a condition preceding it;renal infections;dehydration with diarrhea, vomiting;fever;bronchopulmonary diseases;acute myocardial infarction;heart and respiratory failure;insulin therapy for complex surgical operations and injuries;abnormal liver function;compliance with low-calorie diet (less than 1000 kcal);pregnancy and lactation;hypersensitivity to the drug.
Terms of sale and storage
Sugar tablets Metformin is stored in a dry place inaccessible to children at a temperature not higher than + 25 ° C. Do not take medicine after the expiration date. The drug can be purchased at pharmacies with a prescription.