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Glucophage

Glucophage
Glucophage is used in type 2 diabetes mellitus, especially in obese patients, with ineffective diet therapy and physical activity. Also used for prevention of type 2 diabetes mellitus in patients with prediabetes with additional risk factors for type 2 diabetes mellitus, in whom lifestyle changes did not allow achieving adequate glycemic control.

Brand: Metformin

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: November 2023
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Glucophage 1000 mg
360 pills - 1000 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$167.95 $0.47 $188.81 Add to cart
240 pills - 1000 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$124.95 $0.52 $112.89 Add to cart
180 pills - 1000 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$103.01 $0.57 $75.37 Add to cart
120 pills - 1000 mg $77.45 $0.65 $41.47 Add to cart
90 pills - 1000 mg $64.79 $0.72 $24.40 Add to cart
60 pills - 1000 mg $47.09 $0.78 $12.37 Add to cart
30 pills - 1000 mg $29.73 $0.99 No Add to cart
Glucophage 850 mg
360 pills - 850 mg $87.91 $0.24 $175.97 Add to cart
240 pills - 850 mg $61.93 $0.26 $113.99 Add to cart
180 pills - 850 mg $52.65 $0.29 $79.29 Add to cart
120 pills - 850 mg $45.95 $0.38 $42.01 Add to cart
90 pills - 850 mg $39.99 $0.44 $25.98 Add to cart
60 pills - 850 mg $35.32 $0.59 $8.66 Add to cart
30 pills - 850 mg $21.99 $0.73 No Add to cart
Glucophage 500 mg
360 pills - 500 mg $69.99 $0.19 $129.81 Add to cart
240 pills - 500 mg $47.95 $0.20 $85.25 Add to cart
180 pills - 500 mg $41.12 $0.23 $58.78 Add to cart
120 pills - 500 mg $36.26 $0.30 $30.34 Add to cart
90 pills - 500 mg $33.23 $0.37 $16.72 Add to cart
60 pills - 500 mg $25.32 $0.42 $7.98 Add to cart
30 pills - 500 mg $16.65 $0.56 No Add to cart

Product description

Pharmacodynamics of Glucophage 

Buy Glucophage in Canada

Metformin reduces hyperglycemia without leading to the development of hypoglycemia. Unlike sulfonylurea derivatives, it does not stimulate insulin secretion and does not have a hypoglycemic effect in healthy individuals. Increases the sensitivity of peripheral receptors to insulin and glucose utilization by cells. Reduces the production of glucose by the liver by inhibiting gluconeogenesis and glycogenolysis. Delays the absorption of glucose in the intestine. Metformin stimulates glycogen synthesis by acting on glycogen synthetase.

Increases the transport capacity of all types of membrane glucose transporters. In addition, it has a beneficial effect on lipid metabolism: it reduces the content of total cholesterol, LDL and triglycerides. While taking metformin, the patient's body weight either remains stable or moderately decreases. Clinical studies have also shown the efficacy of Glucophage® for the prevention of diabetes mellitus in patients with prediabetes with additional risk factors for the development of overt type 2 diabetes mellitus, in whom lifestyle changes did not allow achieving adequate glycemic control.

Pharmacokinetics

Absorption and distribution. After oral administration, metformin is absorbed from the gastrointestinal tract. The absolute bioavailability is 50-60%. Cmax (approximately 2 μg / L or 15 μmol) in plasma is reached after 2.5 hours. With simultaneous intake of food, the absorption of metformin decreases and is delayed.

Metformin is rapidly distributed in tissues, practically does not bind to plasma proteins.

Metabolism and excretion. It is metabolized to a very weak extent and excreted by the kidneys. The clearance of metformin in healthy subjects is 400 ml / min (4 times more than Cl creatinine), which indicates the presence of active tubular secretion. T1/2 is approximately 6.5 hours. With renal failure, T1/2 increases, there is a risk of drug accumulation.

Indications of Glucophage®

Glucophage for the treatment of diabetes

type 2 diabetes mellitus, especially in obese patients, with ineffective diet therapy and physical activity:

- in adults as monotherapy or in combination with other oral hypoglycemic agents or insulin;

- in children from 10 years of age as monotherapy or in combination with insulin;

prevention of type 2 diabetes mellitus in patients with prediabetes with additional risk factors for type 2 diabetes mellitus, in whom lifestyle changes did not allow achieving adequate glycemic control.

Dosing and Administration of Glucophage

Glucophage packaging

Inside.

Adults

Monotherapy and combination therapy in combination with other oral hypoglycemic agents for type 2 diabetes mellitus. The usual starting dose is 500 or 850 mg 2–3 times daily after or during meals.

It is recommended to adjust the dose every 10-15 days based on the results of measuring the concentration of glucose in blood plasma. A slow increase in the dose helps to reduce side effects from the gastrointestinal tract.

The maintenance dose of the drug is usually 1500–2000 mg / day. To reduce side effects from the gastrointestinal tract, the daily dose should be divided into 2-3 doses. The maximum dose is 3000 mg / day, divided into 3 doses.

Patients receiving metformin in doses of 2000-3000 mg / day may be transferred to the drug Glucophage® 1000 mg. The maximum recommended dose is 3000 mg / day, divided into 3 doses.

In case a planning receiving another hypoglycemic agent: it is necessary to stop taking any other means, and to startreception Glyukofazh preparation at a dose above®.

Combination with insulin. To achieve better blood glucose control, metformin and insulin can be used in combination therapy in patients with type 2 diabetes. The usual initial dose of Glucophage® is 500 or 850 mg 2-3 times a day, while the dose of insulin is selected based on the blood glucose concentration.

Monotherapy for prediabetes. The usual dose is 1000-1700 mg / day after or during a meal, divided into 2 doses.

It is recommended to regularly conduct glycemic control to assess the need for further use of the drug.

Renal failure Metformin can be used in patients with moderate renal failure (Cl creatinine 45–59 ml / min) only in the absence of conditions that may increase the risk of lactic acidosis.

Patients with Cl creatinine 45–59 ml / min. The initial dose is 500 or 850 mg once a day. The maximum dose is 1000 mg / day, divided into 2 doses.

Renal function should be closely monitored (every 3–6 months).

If Cl creatinine is below 45 ml / min, the drug should be stopped immediately.

Elderly age. Due to a possible decrease in renal function, the dose of metformin must be selected under regular monitoring of renal function indicators (determine the concentration of creatinine in the blood serum at least 2-4 times a year).

Children and adolescents

In children from 10 years of age, Glucophage® can be used both in monotherapy and in combination with insulin. The usual starting dose is 500 or 850 mg once daily after or during a meal. After 10-15 days, the dose must be adjusted based on the blood glucose concentration. The maximum daily dose is 2000 mg, divided into 2-3 doses.

Duration of treatment

Glucophage® should be taken daily, without interruption. In case of discontinuation of treatment, the patient must inform the doctor about it.


Overdose

With the use of metformin at a dose of up to 85 g (42.5 times the maximum daily dose), the development of hypoglycemia was not observed. However, in this case, the development of lactic acidosis was observed. Significant overdose or associated risk factors can lead to the development of lactic acidosis (see "Special instructions").

Treatment: if signs of lactic acidosis appear, treatment with the drug must be stopped immediately, the patient must be urgently hospitalized and, having determined the concentration of lactate, the diagnosis must be clarified. The most effective measure to remove lactate and metformin from the body is hemodialysis. Symptomatic treatment is also carried out.

Special instructions

Lactic

Lactic acidosisacidosis is a rare but serious (high mortality rate in the absence of emergency treatment) complication that can occur due to the accumulation of metformin. Cases of lactic acidosis while taking metformin occurred mainly in patients with diabetes mellitus with severe renal failure.

Other associated risk factors should be considered, such as decompensated diabetes mellitus, ketosis, prolonged fasting, alcoholism, liver failure, and any condition associated with severe hypoxia. This can help reduce the incidence of lactic acidosis.

The risk of developing lactic acidosis should be taken into account when nonspecific signs appear, such as muscle cramps, accompanied by dyspeptic disorders, abdominal pain and severe asthenia. Lactic acidosis is characterized by acidotic dyspnea, abdominal pain, and hypothermia followed by coma. Diagnostic laboratory parameters are a decrease in blood pH less than 7.25, plasma lactate content over 5 mmol / L, an increased anion gap and a lactate / pyruvate ratio. If you suspect metabolic acidosis, you should stop taking the drug and consult a doctor immediately.

Surgical operations

The use of metformin should be discontinued 48 hours before elective surgery and can be continued no earlier than 48 hours after, provided that the renal function was found to be normal during the examination.

Renal function

Since metformin is excreted by the kidneys, it is necessary to determine creatinine clearance before starting treatment and regularly thereafter: at least once a year in patients with normal renal function and 2-4 times a year in elderly patients, as well as in patients with Cl creatinine on NGN.

In the case of Cl creatinine less than 45 ml / min, the use of the drug is contraindicated.

Special care should be taken in case of possible impaired renal function in elderly patients, while using antihypertensive drugs, diuretics or NSAIDs.

Heart failure

Patients with heart failure have a higher risk of developing hypoxia and renal failure. Patients with CHF should regularly monitor cardiac and renal function while taking metformin. Reception of metformin in heart failure with unstable hemodynamic parameters is contraindicated.

Children and adolescents

The diagnosis of type 2 diabetes must be confirmed before starting metformin treatment.

In clinical studies lasting 1 year, it was shown that metformin does not affect growth and puberty. However, in the absence of long-term data, careful monitoring of the subsequent effect of metformin on these parameters in children is recommended, especially during puberty. The most careful monitoring is necessary for children aged 10-12 years.

Other Precautions

Patients are advised to continue on a regular carbohydrate diet throughout the day. Overweight patients are advised to continue to follow a hypocaloric diet (but not less than 1000 kcal / day).

It is recommended that routine laboratory tests be performed regularly to control diabetes. Metformin alone does not cause hypoglycemia, but caution is advised when using it in combination with insulin or other hypoglycemic agents (for example, sulfonylurea derivatives, repaglinide).

The use of Glucophage® is recommended for the prevention of type 2 diabetes mellitus in persons with prediabetes and additional risk factors for the development of overt type 2 diabetes mellitus, such as age less than 60 years; BMI ≥35 kg / m2; a history of gestational diabetes mellitus; family history of diabetes mellitus in first-degree relatives; increased concentration of triglycerides; reduced concentration of HDL-C, arterial hypertension.

Influence on the ability to drive vehicles and mechanisms. Monotherapy with Glucophage® does not cause hypoglycemia and therefore does not affect the ability to drive vehicles and mechanisms. However, patients should be warned about the risk of hypoglycemia when using metformin in combination with other hypoglycemic drugs (including sulfonylurea derivatives, insulin, repaglinide).

Contraindications

  • Hypersensitivity to metformin or any of the excipients;
  • diabetic ketoacidosis, precoma and coma;
  • renal failure or impaired renal function (Cl creatinine <45 ml / min);
  • acute conditions occurring with the risk of developing impaired renal function: dehydration (with diarrhea, vomiting), severe infectious diseases, shock;
  • clinically pronounced manifestations of acute or chronic diseases that can lead to the development of tissue hypoxia (including acute heart failure, chronic heart failure with unstable hemodynamic parameters, respiratory failure, acute myocardial infarction);
  • extensive surgical operations and trauma, when insulin therapy is indicated (see "Special instructions");
  • liver failure, impaired liver function;
  • chronic alcoholism, acute alcohol poisoning;
  • lactic acidosis (including history);
  • application for less than 48 hours before and within 48 hours after carrying out radioisotope or X-ray studies with the introduction of an iodine-containing contrast agent (see "Interaction");
  • adherence to a hypocaloric diet (less than 1000 calories / day);
  • pregnancy.

With caution: patients over 60 years of age, performing heavy physical work, which is associated with an increased risk of developing lactic acidosis; patients with renal insufficiency (Cl creatinine 45-59 ml / min); period of breastfeeding.

Use in pregnancy and lactation

Decompensated diabetes mellitus during pregnancy is associated with an increased risk of congenital malformations and perinatal mortality. Limited evidence suggests that taking metformin in pregnant women does not increase the risk of developing birth defects in children.

When planning a pregnancy, as well as in case of pregnancy while taking metformin for prediabetes and type 2 diabetes mellitus, the drug should be canceled, and insulin therapy should be prescribed in case of type 2 diabetes. Plasma glucose should be kept close to normal to reduce the risk of fetal malformations.

Metformin passes into breast milk. Side effects were not observed in newborns with breastfeeding while taking metformin. However, due to the limited amount of data, the use of the drug during breastfeeding is not recommended. The decision to stop breastfeeding should be made in light of the benefits of breastfeeding and the potential risk of side effects in the baby.

Interaction

Contraindicated combinationscontrastcontrast

Iodine-containing X-rayagents: against the background of functional renal failure in patients with diabetes mellitus, X-ray examination using iodine-containing X-rayagents can cause the development of lactic acidosis. Treatment with Glucophage® should be discontinued 48 hours before or at the time of X-ray studies using iodinated contrast media, and not to resume within 48 hours after, with the proviso that the survey renal function was considered normal.

Combinations not recommended

Alcohol: acute alcohol intoxication increases the risk of lactic acidosis, especially in the case of malnutrition, adherence to a low-calorie diet, and liver failure. While taking the drug, you should avoid the use of alcohol and drugs containing ethanol.

Combinations requiring caution

Danazol: simultaneous administration of Danazol is not recommended in order to avoid the hyperglycemic effect of the latter. If it is necessary to treat with danazol and after stopping the intake of the latter, a dose adjustment of Glucophageis required® under the control of blood glucose concentration.

Chlorpromazine: When taken in high doses (100 mg / day), it increases the concentration of glucose in the blood, decreasing the release of insulin. When treating with antipsychotics and after discontinuing the latter, a dose adjustment of the drug is required under the control of blood glucose concentration.

GCS of systemic and local action reduce glucose tolerance, increase the concentration of glucose in the blood, sometimes causing ketosis. When treating corticosteroids and after stopping the intake of the latter, a dose adjustment of Glucophageis required® under the control of blood glucose concentration.

Diuretics: Concomitant use of loop diuretics can lead to the development of lactic acidosis due to possible functional renal failure. You should not prescribe Glucophage®if the Cl creatinine is below 60 ml / min.

Prescribed in the form of injection β2-adrenergic agonists: increase the concentration of glucose in the blood due to stimulation of β2-adrenergic receptors. In this case, it is necessary to control the concentration of glucose in the blood. Insulin administration is recommended if necessary.

With the simultaneous use of the above drugs, more frequent monitoring of blood glucose may be required, especially at the beginning of treatment. If necessary, the dose of metformin can be adjusted during treatment and after its termination.

Antihypertensive drugs, with the exception of ACE inhibitors, can reduce the concentration of glucose in the blood. The dose of metformin should be adjusted if necessary.

With the simultaneous use of the drug Glukofazh® with sulfonylurea derivatives, insulin, acarbose, salicylates, hypoglycemia may develop.

Nifedipine increases the absorption and Cmax of metformin.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim and vancomycin), secreted in the renal tubules, compete with metformin for tubular transport systems and can lead to an increase in its Cmax.


Side effects

The frequency of side effects of the drug is assessed as follows: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rare (<1/10000).

Side effects are presented in decreasing order of importance.

From the side of metabolism and nutrition: very rarely - lactic acidosis (see "Special instructions"). With long-term use of metformin, there may be a decrease in the absorption of vitamin B12.

When detecting megaloblastic anemia, it is necessary to consider the possibility of such an etiology.

From the nervous system: often - taste disturbance.

From the gastrointestinal tract: very often - nausea, vomiting, diarrhea, abdominal pain, lack of appetite. Most often they occur during the initial period of treatment and in most cases disappear spontaneously. To prevent symptoms, it is recommended to take metformin 2 or 3 times daily with or after meals. Slowly increasing the dose may improve gastrointestinal tolerance.

On the part of the skin and subcutaneous tissue: very rarely - skin reactions such as erythema, itching, rash.

Violations of the liver and biliary tract: very rarely - abnormal liver function indicators or hepatitis; after the abolition of metformin, these undesirable effects completely disappear.

Published data, post-marketing data, as well as controlled clinical trials in a limited pediatric population in the 10-16 age group show that side effects are similar in nature and severity to those in adult patients.