Glyukofazh

Active material: Metformin
When ATH: A10BA02
CCF: Oral hypoglycemic agents
ICD-10 codes (testimony): E11
When CSF: 15.02.02
Manufacturer: MERCK SANTE s.a.s. (France)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated white, film; round, lenticular; the cross-section – homogeneous white mass.

Excipients: povidone, magnesium stearate.

The composition of the coating film: gipromelloza.

10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
15 PC. – blisters (2) – packs cardboard.
20 PC. – blisters (3) – packs cardboard.
20 PC. – blisters (5) – packs cardboard.

Pills, coated white, film; round, lenticular; the cross-section – homogeneous white mass. lenticular.

Excipients: povidone, magnesium stearate.

The composition of the coating film: gipromelloza

15 PC. – blisters (2) – packs cardboard.
20 PC. – blisters (3) – packs cardboard.
20 PC. – blisters (5) – packs cardboard.

Pills, coated white, film; Oval, lenticular, scored on both sides and engraved “1000” on one side; the cross-section – homogeneous white mass.

Excipients: povidone, magnesium stearate.

The composition of the coating film: Opadry clean (gipromelloza, macrogol 400, macrogol 8000).

10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
10 PC. – blisters (12) – packs cardboard.
15 PC. – blisters (2) – packs cardboard.
15 PC. – blisters (3) – packs cardboard.
15 PC. – blisters (4) – packs cardboard.

Pharmacological action

Oral hypoglycemic agents from the group of biguanides.

Glyukofazh^® snijayet gipyerglikyemiyu, without causing hypoglycemia. It does not stimulate insulin secretion and has no hypoglycemic effect in healthy persons.

It increases the sensitivity of peripheral insulin receptors and stimulates glucose uptake by muscle cells. Inhibits hepatic gluconeogenesis. Delays the absorption of carbohydrates in the intestine. Has a beneficial effect on lipid metabolism: reduces total cholesterol, triglycerides and LDL.

Pharmacokinetics

Absorption

After oral administration, metformin adequately absorbed from the gastrointestinal tract. Simultaneous food intake and reduced absorption of metformin delayed. The absolute bioavailability of 50-60%. C_max in plasma is approximately 2 ug / ml or 15 mol and is achieved through 2.5 no.

Distribution

Metformin is rapidly distributed in the body tissues. Almost does not bind to plasma proteins.

Metabolism

In a very small extent it is metabolized and excreted by the kidneys.

Deduction

The clearance of metformin in healthy individuals is 400 ml / min (in 4 times, than CK), indicating that active tubular secretion.

T_1/2 approximately 6.5ch.

Pharmacokinetics in special clinical situations

In patients with renal insufficiency T_1/2 increases, there is a risk of metformin accumulation in the body.

Testimony

- Diabetes mellitus type 2 adult;

- In combination with insulin in diabetes type 2, especially in patients with severe obesity with insulin resistance secondary;

- Diabetes mellitus type 2 in children older 10 years (monotherapy, in combination with insulin).

Dosage regimen

Monotherapy and combination therapy with other oral hypoglycemic agents

In adults, the initial dose is 500 mg 2-3 times / day during or after a meal. Perhaps further gradual increase in the dose depending on the glucose levels in the blood.

Supporting the daily dose is 1500-2000 mg / day. To reduce the side effects from the gastrointestinal tract the dose should be divided into 2-3 admission. The maximum daily dose is 3000 mg / day, razdelennaya of 3 admission.

The slow increase in the dose may improve gastrointestinal tolerability.

Patients, taking metformin doses 2000-3000 mg / day, can be transferred to the reception Glyukofazh^® 1000 mg. The maximum recommended dose is 3000 mg / day, razdelennaya of 3 admission.

In the case of planning for the transition to therapy Glyukofazh^® with other hypoglycemic agents to stop taking other means and start taking Glucophage^® dose, above.

Combination with insulin

To achieve a better glycemic control with metformin and insulin may be administered as a combination therapy.

The initial dose of the drug Glucophage^® dose 500 mg 850 mg of 1 tab. 2-3 times / day; drug Glucophage^® dose 1000 mg of 1 tab. 1 time / day. The insulin dose is selected based on the results of measurement of blood glucose.

In children over the age of 10 Glyukofazh^® It can be used as monotherapy, and in combination with insulin. The initial dose is 500 mg 2-3 times / day during or after a meal. Through 10-15 day dose should be adjusted on the basis of blood glucose measurements. The maximum daily dose is 2000 mg, razdelennaya of 2-3 admission.

In elderly patients due to a possible decrease in renal function the dose of metformin should be selected for regular monitoring of indicators of kidney function (control the level of serum creatinine at least 2-4 once a year). It is not recommended to use the drug in patients aged 60 years, performing heavy physical work.

Side effect

The frequency of side effects was estimated as follows:: Often (≥1/10), often (≥1/100, <1/10), infrequently (≥1/1000, <1/100), rarely (≥1/10000, <1/1000), rarely (<1/10000). Side effects presented in order of decreasing importance.

CNS: often – taste disturbance.

From the digestive system: Often – nausea, vomiting, stomach ache, anorexia. Most often the symptoms occur in the initial period of treatment and in most cases subside spontaneously.

Allergic reactions: rarely – эritema, itching, rash.

Metabolism: rarely – Lactic acidosis (It requires the preparation); prolonged use – vitamin deficiencies of vitamin B₁₂ (malabsorption). These effects are quickly reversible when canceling metformin and usually clinically insignificant (<0.01%). Reduced levels of vitamin B₁₂ be taken into account in patients with megaloblastic anemia.

From the hepatobiliary system: isolated cases – violation of liver function tests, hepatitis. After the cancellation of metformin adverse effects disappear completely.

Published data, post-marketing data, and a data-controlled clinical trials limited pediatric population aged 10 to 16 years show, side effects of the nature and severity similar to those in adults.

Contraindications

- Diabetic ketoacidosis;

- Diabetic precoma;

- Diabeticheskaya coma;

- Renal dysfunction (CC<60 ml / min);

- Acute diseases, where there is a risk of renal dysfunction: degidratatsiya, (vomiting, diarrhea), fever, serious infectious disease, state hypoxia (shock, sepsis, kidney infection, bronchopulmonary diseases);

- Symptomatic manifestations of acute and chronic diseases, which can lead to tissue hypoxia (respiratory insufficiency, heart failure, acute myocardial infarction);

- Major surgery or injury, and (when it is shown holding insulin);

- Abnormal liver function;

- Chronic alcoholism, acute ethanol poisoning;

- Lactic acidosis (incl. history);

- A period of at least 2 days prior to and during 2 days after the radioisotope or radiological examinations with administration of iodine-containing contrast agents;

- Compliance with a reduced-calorie diet (<1000 kcal / day);

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

It is not recommended to use the drug in patients aged 60 years, performing heavy physical work.

Pregnancy and lactation

The drug is contraindicated in pregnancy and during breastfeeding.

When planning a pregnancy, or Glucophage^® should be withdrawn and insulin. The patient should be warned of the need to notify the doctor in the event of pregnancy. For mother and child should establish monitoring.

Unknown, whether it is allocated metformin in breast milk. If necessary, use during lactation should stop breastfeeding.

Cautions

Patients should be warned about the need to stop taking the drug and consult a doctor if symptoms persist, stomachache, muscle aches, general weakness and severe malaise. These symptoms may be a sign of incipient lactic acidosis.

Glyukofazh^® should be abolished for 48 hours before and during the period 48 hours after the X-ray inspection (incl. urography, I / Angiography) with the use of contrast media.

As metformin is excreted in the urine, before the start of treatment and regularly thereafter follows to determine the levels of serum creatinine.

Particular caution should be exercised in violation of the kidney, eg, in the initial treatment period antihypertensives, Diuretics, NSAIDs.

It should inform the patient about the need to resort to the doctor with symptoms of bronchopulmonary infection or infectious disease urinary organs.

Against the background of the drug Glucophage^® should refrain from drinking alcohol.

Use in Pediatrics

In children over the age of 10 Glyukofazh^® It can be used as monotherapy, and in combination with insulin.

Effects on ability to drive vehicles and management mechanisms

Monotherapy preparatom Glyukofazh^® It does not cause hypoglycaemia and therefore has no effect on ability to drive and use machines. However, patients should be treated with caution in the risk of hypoglycaemia when metformin in combination with other hypoglycemic agents (incl. sulfonylurea derivatives, insulinom, repaglinidom).

Overdose

Symptoms: the application of Glucophage^® dose 85 g was observed hypoglycemia, but noted the development of lactic acidosis. Early symptoms of lactic acidosis include nausea, vomiting, diarrhea, fever, stomach ache, muscle aches, further possible shortness of breath, dizziness, disturbance of consciousness, the development of coma.

Treatment: the immediate withdrawal of Glucophage^®, urgent hospitalization, determining the concentration of lactate in the blood; if necessary, symptomatic therapy. For the excretion of lactate and metformin is more effective hemodialysis.

Drug Interactions

Not recommended combinations

With the simultaneous use of the drug Glucophage^® with danazol may develop hyperglycemic effect. If necessary, treatment with danazol and after termination of his admission Dosage adjustment Glyukofazh^® under the control of blood glucose levels.

With the simultaneous use of the drug Glucophage^® alcohol and ethanol-containing drugs increases the risk of lactic acidosis in acute alcohol intoxication, especially when starvation or low calorie diet compliance, and liver failure.

Combinations, require special care

Chlorpromazine high doses (100 mg / day) reduces the release of insulin and increases blood glucose levels. While the use of neuroleptics and after the termination of their admission Dosage adjustment Glyukofazh^® under the control of blood glucose levels.

GCS (for systemic and topical administration) reduced glucose tolerance and increased blood glucose levels, in some cases, causing ketosis. If necessary, use a combination and after discontinuation of corticosteroids require dose adjustment Glyukofazh^® under the control of blood glucose levels.

In an application “loop” diuretics and Glûkofaža^® there is a risk of lactic acidosis due to the possible occurrence of functional renal failure. It should appoint Glyukofazh^®, If QC<60 ml / min.

Appointment as an injection of beta₂-sympathomimetic reduce hypoglycemic effect of Glucophage^® due to stimulation of β₂-adrenoreceptorov. In this case it is necessary to monitor blood glucose and insulin when needed designate.

ACE inhibitors and other antihypertensive drugs can reduce the blood glucose level. If necessary, adjust the dose of metformin.

With simultaneous use of Glucophage^® with sulfonylureas, insulinom, acarbose and salicylates may increase hypoglycemic action.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life for tablets 500 mg 850 mg – 5 years. Shelf life for tablets 1000 mg – 3 year.