Composition, structure and packing
Tablets, coated in white, film, round, biconvex, transverse section of - homogeneous white mass. 1 tab. metformin hydrochloride 500 mg. Excipients: povidone, magnesium stearate. The composition of the shell membrane: gipromelloza.
Tablets, coated in white, film, round, biconvex, transverse section of - homogeneous white mass. biconvex. 1 tab. metformin hydrochloride 850 mg. Excipients: povidone, magnesium stearate. The composition of the shell membrane: gipromelloza.
Tablets, coated in white, film, oval, biconvex, with risks on both sides and engraved "1000" on one side, and on cross section - a homogeneous white mass. 1 tab. metformin hydrochloride 1000 mg. Excipients: povidone, magnesium stearate. The composition of the shell membrane: opadray net (gipromelloza, macrogol 400, macrogol 8000).
Clinico-pharmacological group: oral hypoglycemic drug.
Pharmacological action
Oral hypoglycemic drug from the biguanide group. Glyukofazh reduces hyperglycemia, does not cause hypoglycemia. Does not stimulate insulin secretion and does not have hypoglycemic action in healthy individuals. Increases the sensitivity of peripheral receptors to insulin and stimulates glucose uptake by muscle cells. Hinders gluconeogenesis in the liver. Delays absorption of carbohydrates in the intestines. Has a beneficial effect on lipid metabolism: reduces total cholesterol, triglycerides and LDL.
Pharmacokinetics
Absorption
After taking the drug inside metformin adequately absorbed from the gastrointestinal tract. At the same time food intake and decreased absorption of metformin delayed. The absolute bioavailability of 50-60%. In the plasma Cmax is approximately 2 ug / ml or 15 uM and reached through 2.5 hours
Distribution
Metformin rapidly distributed in body tissues. Practically not bound to plasma proteins.
Metabolism
In a very small extent exposed to metabolic and displayed by the kidneys.
Withdrawal
Clearance of metformin in healthy subjects is 440 ml / min (4 times greater than CC), indicating that active tubular secretion. T1 / 2 approximately 6.5ch.
Pharmacokinetics in special clinical situations
In patients with renal insufficiency T1 / 2 increases, there is a risk of metformin accumulation in the body.
Statement
Type 2 diabetes in adults;
in combination with insulin in diabetes mellitus type 2, especially in obese with secondary insulin resistance;
Type 2 diabetes in children older than 10 years (monotherapy, in combination with insulin).
Dosage regimen
Monotherapy and combination therapy with other oral hypoglycemic means the adult starting dose is 500 mg 2-3 times / day after or during meals.
Perhaps a further gradual increase in the dose depending on the level of glucose in the blood. Maintenance daily dose of 1500-2000 mg / day. To reduce the side effects on the gastrointestinal dose should be divided into 2-3 reception. The maximum daily dose is 3000 mg / day, divided into 3. The slow increase in dose may improve gastrointestinal tolerability.
Patients taking metformin at doses of 2000-3000 mg / day, may be transferred to the reception Glyukofazha 1000 mg. The maximum recommended dose is 3000 mg / day, divided into 3. In the case of planning for the transition to therapy with other hypoglycemic Glyukofazhem funds should stop taking the other way and start accepting Glyukofazha in a dose above. Combination with insulin to achieve better control of blood glucose levels with metformin and insulin may be used as combination therapy. The initial dose of the drug Glyukofazh a dose of 500 mg and 850 mg of 1 tab. 2-3 times / day; Glyukofazh drug at a dose of 1000 mg of 1 tab. 1 times / day. Insulin is selected on the basis of measurement of blood glucose.
In children older than 10 years of age Glyukofazh can be used as a monotherapy and in combination with insulin. The initial dose is 500 mg 2-3 times / day after or during meals. After 10-15 days, the dose should be adjusted based on the results of measurement of blood glucose. The maximum daily dose is 2000 mg, divided into 2-3 reception. Elderly patients due to a possible reduction in kidney function dose of metformin should be selected for regular monitoring indicators of renal function (creatinine level control serum no less than 2-4 times per year). Do not use the drug in patients aged over 60 years of performing heavy physical work.
Side effect
Frequency of side effects was estimated as follows: very common (≥ 1 / 10), often (≥ 1 / 100, <1 / 10), infrequently (≥ 1 / 1000, <1 / 100), rare (≥ 1 / 10000, < 1 / 1000), very rarely (<1 / 10000). Side effects presented in order of decreasing importance.
From the side of the central nervous system: often - breach of taste.
On the part of the digestive system: very often - nausea, vomiting, abdominal pain, loss of appetite. Most symptoms occur in the initial period of treatment and in most cases spontaneously resolve.
Allergic reactions: seldom - erythema, pruritus, rash.
On the part of metabolism: very often - laktatsidoz (requires discontinuation of the drug), with prolonged use - vitamin deficiencies of vitamin B12 (malabsorption). These effects are rapidly reversible with the abolition of metformin and usually clinically insignificant (<0.01%). Reduced vitamin B12 should be taken into account in patients with megaloblastic anemia.
From the hepato-biliary system: isolated cases - violation indicators of liver function, hepatitis. After the abolition of metformin adverse effects completely disappear. Published data, potsmarketingovye data and the data controlled clinical studies in limited populations of children aged 10 to 16 years show that the adverse effects on nature and gravity similar to those in adult patients.
Contraindications
diabetic ketoacidosis;
diabetic precoma;
diabetic coma;
renal dysfunction (CC <60 ml / min);
acute diseases in which there is the risk of renal dysfunction: dehydration (vomiting, diarrhea), fever, severe infections, the state of hypoxia (shock, sepsis, renal disease, broncho-pulmonary disease);
symptomatic manifestations of acute and chronic diseases that can lead to tissue hypoxia (respiratory failure, heart failure, acute myocardial infarction);
major surgical operations and injuries, and (when shown an insulin);
liver problems;
chronic alcoholism and acute ethanol poisoning;
laktatsidoz (including history);
period of not less than 2 days before and within 2 days after the radioisotope, or radiological investigations with the introduction of iodine contrast agents;
compliance with the hypocaloric diet (<1000 kcal / day);
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components. Do not use the drug in patients aged over 60 years of performing heavy physical work.
Pregnancy and lactation
The drug is contraindicated during pregnancy and during breastfeeding. When planning a pregnancy or Glyukofazh should be abolished and appoint insulin. The patient should notify the need to notify the doctor in case of pregnancy. For the mother and child should be placed under observation.
It is not known whether metformin is allocated with breast milk. If necessary, use during lactation should stop breastfeeding.
Application for violations of liver function
Contraindicated in liver problems.
Application for violations of renal function
Contraindicated in renal events.
Cautions
Patients should notify the need to stop taking the drug and consult a doctor if vomiting, abdominal pain, muscle pain, general weakness and severe malaise. These symptoms may be a sign of incipient laktatsidoza. Glyukofazh should be abolished for 48 h before and during the period of 48 hours after the radiographic examination (including urography, in / in angiography) using X-ray facilities.
As shown in the urine metformin, before drug treatment and regularly thereafter to be determined levels of serum creatinine. Particular caution should be exercised in violation of renal function, for example, in the initial period of therapy of antihypertensive therapy, diuretics, NSAIDs.
It should inform the patient about the need for treatment to the doctor with symptoms of bronchopulmonary infection or infectious disease urinary organs. Against the background of the drug Glyukofazh should refrain from taking alcohol.
Use in Pediatrics
In children older than 10 years of age Glyukofazh can be used as a monotherapy and in combination with insulin.
Effects on ability to drive vehicles and management mechanisms
As monotherapy, the drug does not cause hypoglycemia Glyukofazh and therefore does not affect your ability to drive and operate machinery. However, patients should be treated with caution to the risk of hypoglycemia when using metformin in combination with other hypoglycemic agents (including derivatives sulfanilmocheviny, insulin, repaglinidom).
Overdose
Symptoms: Using Glyukofazha a dose of 85 g of hypoglycemia was not observed, but noted the development laktatsidoza. Early symptoms laktatsidoza are nausea, vomiting, diarrhea, fever, abdominal pain, muscle pain, in the future possibly rapid breathing, dizziness, impaired consciousness, the development of coma.
Treatment: immediate cancellation Glyukofazha, urgent hospitalization, the definition of the concentration of lactate in blood, if necessary, carry symptomatically. For the excretion of lactate and metformin is most effective hemodialysis.
Drug Interactions
Deprecated when used with a combination drug Glyukofazh with danazol may develop hyperglycemic effect. If necessary, treatment of danazol after the termination of his admission required dosage adjustment Glyukofazha under the control of blood glucose levels.
With simultaneous use of the drug with alcohol and Glyukofazh etanolsoderzhaschimi drugs increases the risk of laktatsidoza during acute alcohol intoxication, especially during fasting or low calorie diet compliance, as well as in liver failure. Combinations which require special care Chlorpromazine in high doses (100 mg / day) reduces the release of insulin and increases the level of glucose in the blood.
When applied simultaneously with neuroleptics and after the termination of their admission require dosage adjustment Glyukofazha under the control of blood glucose levels. GCS (for systemic and topical) reduce glucose tolerance and increased blood glucose levels, in some cases causing ketosis.
If necessary, use of such a combination, and after stopping GCS requires dosage adjustment Glyukofazha under the control of blood glucose.
With simultaneous use of the "loop" diuretics and a risk of Glyukofazha laktatsidoza because of the possible occurrence of functional renal insufficiency. You should not assign Glyukofazh if CC <60 ml / min. Radiological study using iodine radiopaque agents may cause the development laktatsidoza in patients with diabetes against the background of functional renal failure.
Application Glyukofazha should be abolished for 48 h before and did not reopen after 2 days after the X-ray studies using X-ray facilities. Appointment in the form of injections beta2-sympathomimetic reduce hypoglycemic effect Glyukofazha due β2-adrenoceptor stimulation. In this case, should monitor blood glucose and insulin, if necessary, appoint. ACE inhibitors and other antihypertensive drugs may reduce the level of glucose in the blood.
If necessary, adjust the dose of metformin. With simultaneous application Glyukofazha with derivatives sulfonylureas, insulin, acarbose, and salicylates may be increased hypoglycemic action.
Terms and Conditions of storage
The drug should be stored out of reach of children at or above 25 ° C. Shelf life for tablets 500 mg and 850 mg - 5 years. Shelf life for tablets 1000 mg - 3 years.
Tablets, coated in white, film, round, biconvex, transverse section of - homogeneous white mass. 1 tab. metformin hydrochloride 500 mg. Excipients: povidone, magnesium stearate. The composition of the shell membrane: gipromelloza.
Tablets, coated in white, film, round, biconvex, transverse section of - homogeneous white mass. biconvex. 1 tab. metformin hydrochloride 850 mg. Excipients: povidone, magnesium stearate. The composition of the shell membrane: gipromelloza.
Tablets, coated in white, film, oval, biconvex, with risks on both sides and engraved "1000" on one side, and on cross section - a homogeneous white mass. 1 tab. metformin hydrochloride 1000 mg. Excipients: povidone, magnesium stearate. The composition of the shell membrane: opadray net (gipromelloza, macrogol 400, macrogol 8000).
Clinico-pharmacological group: oral hypoglycemic drug.
Pharmacological action
Oral hypoglycemic drug from the biguanide group. Glyukofazh reduces hyperglycemia, does not cause hypoglycemia. Does not stimulate insulin secretion and does not have hypoglycemic action in healthy individuals. Increases the sensitivity of peripheral receptors to insulin and stimulates glucose uptake by muscle cells. Hinders gluconeogenesis in the liver. Delays absorption of carbohydrates in the intestines. Has a beneficial effect on lipid metabolism: reduces total cholesterol, triglycerides and LDL.
Pharmacokinetics
Absorption
After taking the drug inside metformin adequately absorbed from the gastrointestinal tract. At the same time food intake and decreased absorption of metformin delayed. The absolute bioavailability of 50-60%. In the plasma Cmax is approximately 2 ug / ml or 15 uM and reached through 2.5 hours
Distribution
Metformin rapidly distributed in body tissues. Practically not bound to plasma proteins.
Metabolism
In a very small extent exposed to metabolic and displayed by the kidneys.
Withdrawal
Clearance of metformin in healthy subjects is 440 ml / min (4 times greater than CC), indicating that active tubular secretion. T1 / 2 approximately 6.5ch.
Pharmacokinetics in special clinical situations
In patients with renal insufficiency T1 / 2 increases, there is a risk of metformin accumulation in the body.
Statement
Type 2 diabetes in adults;
in combination with insulin in diabetes mellitus type 2, especially in obese with secondary insulin resistance;
Type 2 diabetes in children older than 10 years (monotherapy, in combination with insulin).
Dosage regimen
Monotherapy and combination therapy with other oral hypoglycemic means the adult starting dose is 500 mg 2-3 times / day after or during meals.
Perhaps a further gradual increase in the dose depending on the level of glucose in the blood. Maintenance daily dose of 1500-2000 mg / day. To reduce the side effects on the gastrointestinal dose should be divided into 2-3 reception. The maximum daily dose is 3000 mg / day, divided into 3. The slow increase in dose may improve gastrointestinal tolerability.
Patients taking metformin at doses of 2000-3000 mg / day, may be transferred to the reception Glyukofazha 1000 mg. The maximum recommended dose is 3000 mg / day, divided into 3. In the case of planning for the transition to therapy with other hypoglycemic Glyukofazhem funds should stop taking the other way and start accepting Glyukofazha in a dose above. Combination with insulin to achieve better control of blood glucose levels with metformin and insulin may be used as combination therapy. The initial dose of the drug Glyukofazh a dose of 500 mg and 850 mg of 1 tab. 2-3 times / day; Glyukofazh drug at a dose of 1000 mg of 1 tab. 1 times / day. Insulin is selected on the basis of measurement of blood glucose.
In children older than 10 years of age Glyukofazh can be used as a monotherapy and in combination with insulin. The initial dose is 500 mg 2-3 times / day after or during meals. After 10-15 days, the dose should be adjusted based on the results of measurement of blood glucose. The maximum daily dose is 2000 mg, divided into 2-3 reception. Elderly patients due to a possible reduction in kidney function dose of metformin should be selected for regular monitoring indicators of renal function (creatinine level control serum no less than 2-4 times per year). Do not use the drug in patients aged over 60 years of performing heavy physical work.
Side effect
Frequency of side effects was estimated as follows: very common (≥ 1 / 10), often (≥ 1 / 100, <1 / 10), infrequently (≥ 1 / 1000, <1 / 100), rare (≥ 1 / 10000, < 1 / 1000), very rarely (<1 / 10000). Side effects presented in order of decreasing importance.
From the side of the central nervous system: often - breach of taste.
On the part of the digestive system: very often - nausea, vomiting, abdominal pain, loss of appetite. Most symptoms occur in the initial period of treatment and in most cases spontaneously resolve.
Allergic reactions: seldom - erythema, pruritus, rash.
On the part of metabolism: very often - laktatsidoz (requires discontinuation of the drug), with prolonged use - vitamin deficiencies of vitamin B12 (malabsorption). These effects are rapidly reversible with the abolition of metformin and usually clinically insignificant (<0.01%). Reduced vitamin B12 should be taken into account in patients with megaloblastic anemia.
From the hepato-biliary system: isolated cases - violation indicators of liver function, hepatitis. After the abolition of metformin adverse effects completely disappear. Published data, potsmarketingovye data and the data controlled clinical studies in limited populations of children aged 10 to 16 years show that the adverse effects on nature and gravity similar to those in adult patients.
Contraindications
diabetic ketoacidosis;
diabetic precoma;
diabetic coma;
renal dysfunction (CC <60 ml / min);
acute diseases in which there is the risk of renal dysfunction: dehydration (vomiting, diarrhea), fever, severe infections, the state of hypoxia (shock, sepsis, renal disease, broncho-pulmonary disease);
symptomatic manifestations of acute and chronic diseases that can lead to tissue hypoxia (respiratory failure, heart failure, acute myocardial infarction);
major surgical operations and injuries, and (when shown an insulin);
liver problems;
chronic alcoholism and acute ethanol poisoning;
laktatsidoz (including history);
period of not less than 2 days before and within 2 days after the radioisotope, or radiological investigations with the introduction of iodine contrast agents;
compliance with the hypocaloric diet (<1000 kcal / day);
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components. Do not use the drug in patients aged over 60 years of performing heavy physical work.
Pregnancy and lactation
The drug is contraindicated during pregnancy and during breastfeeding. When planning a pregnancy or Glyukofazh should be abolished and appoint insulin. The patient should notify the need to notify the doctor in case of pregnancy. For the mother and child should be placed under observation.
It is not known whether metformin is allocated with breast milk. If necessary, use during lactation should stop breastfeeding.
Application for violations of liver function
Contraindicated in liver problems.
Application for violations of renal function
Contraindicated in renal events.
Cautions
Patients should notify the need to stop taking the drug and consult a doctor if vomiting, abdominal pain, muscle pain, general weakness and severe malaise. These symptoms may be a sign of incipient laktatsidoza. Glyukofazh should be abolished for 48 h before and during the period of 48 hours after the radiographic examination (including urography, in / in angiography) using X-ray facilities.
As shown in the urine metformin, before drug treatment and regularly thereafter to be determined levels of serum creatinine. Particular caution should be exercised in violation of renal function, for example, in the initial period of therapy of antihypertensive therapy, diuretics, NSAIDs.
It should inform the patient about the need for treatment to the doctor with symptoms of bronchopulmonary infection or infectious disease urinary organs. Against the background of the drug Glyukofazh should refrain from taking alcohol.
Use in Pediatrics
In children older than 10 years of age Glyukofazh can be used as a monotherapy and in combination with insulin.
Effects on ability to drive vehicles and management mechanisms
As monotherapy, the drug does not cause hypoglycemia Glyukofazh and therefore does not affect your ability to drive and operate machinery. However, patients should be treated with caution to the risk of hypoglycemia when using metformin in combination with other hypoglycemic agents (including derivatives sulfanilmocheviny, insulin, repaglinidom).
Overdose
Symptoms: Using Glyukofazha a dose of 85 g of hypoglycemia was not observed, but noted the development laktatsidoza. Early symptoms laktatsidoza are nausea, vomiting, diarrhea, fever, abdominal pain, muscle pain, in the future possibly rapid breathing, dizziness, impaired consciousness, the development of coma.
Treatment: immediate cancellation Glyukofazha, urgent hospitalization, the definition of the concentration of lactate in blood, if necessary, carry symptomatically. For the excretion of lactate and metformin is most effective hemodialysis.
Drug Interactions
Deprecated when used with a combination drug Glyukofazh with danazol may develop hyperglycemic effect. If necessary, treatment of danazol after the termination of his admission required dosage adjustment Glyukofazha under the control of blood glucose levels.
With simultaneous use of the drug with alcohol and Glyukofazh etanolsoderzhaschimi drugs increases the risk of laktatsidoza during acute alcohol intoxication, especially during fasting or low calorie diet compliance, as well as in liver failure. Combinations which require special care Chlorpromazine in high doses (100 mg / day) reduces the release of insulin and increases the level of glucose in the blood.
When applied simultaneously with neuroleptics and after the termination of their admission require dosage adjustment Glyukofazha under the control of blood glucose levels. GCS (for systemic and topical) reduce glucose tolerance and increased blood glucose levels, in some cases causing ketosis.
If necessary, use of such a combination, and after stopping GCS requires dosage adjustment Glyukofazha under the control of blood glucose.
With simultaneous use of the "loop" diuretics and a risk of Glyukofazha laktatsidoza because of the possible occurrence of functional renal insufficiency. You should not assign Glyukofazh if CC <60 ml / min. Radiological study using iodine radiopaque agents may cause the development laktatsidoza in patients with diabetes against the background of functional renal failure.
Application Glyukofazha should be abolished for 48 h before and did not reopen after 2 days after the X-ray studies using X-ray facilities. Appointment in the form of injections beta2-sympathomimetic reduce hypoglycemic effect Glyukofazha due β2-adrenoceptor stimulation. In this case, should monitor blood glucose and insulin, if necessary, appoint. ACE inhibitors and other antihypertensive drugs may reduce the level of glucose in the blood.
If necessary, adjust the dose of metformin. With simultaneous application Glyukofazha with derivatives sulfonylureas, insulin, acarbose, and salicylates may be increased hypoglycemic action.
Terms and Conditions of storage
The drug should be stored out of reach of children at or above 25 ° C. Shelf life for tablets 500 mg and 850 mg - 5 years. Shelf life for tablets 1000 mg - 3 years.
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