Diaformin OD - instructions for use, doses, side effects, contraindications

Excipients: cellulose microcrystalline - 240 mg; carmellose; sodium - 150 mg; purified water * - q. s .; hypromellose - 100 mg; magnesium stearate - 5 mg.

* -sprayaetsya in the production process.

Description:Biconvex tablets are oval in shape, from white to almost white, with engraving "500" on one side and smooth on the other side.

Pharmacotherapeutic group:hypoglycemic agent for oral administration of the biguanide group

ATX: & nbsp

A.10.B.A.02 Metformin

Pharmacodynamics:

Metformin inhibits gluconeogenesis in the liver, reduces the absorption of glucose from the intestine, enhances peripheral utilization of glucose, and also increases the sensitivity of tissues to insulin. In this case, it has no effect on the secretion of insulin by beta cells of the pancreas, does not cause hypoglycemic reactions. Reduces the level of triglycerides and low density lipoproteins in the blood. Stabilizes or reduces body weight. Has a fibrinolytic effect due to inhibition of the inhibitor of tissue-type plasminogen activator.

Pharmacokinetics:

Suction

After oral administration of sustained-release tablets, metformin absorption is slowed compared to a tablet with the usual release of metformin. Time to reach the maximum concentration (TC_m_Oh) is 7 hours. Fluctuations in the maximum concentration of metformin (C_m_Oh) and the area under the concentration-time curve (AUC) in individual patients in the case of taking metformin in the form of long-acting tablets are comparable with those of the tablets with a conventional release profile.

Distribution

The connection with plasma proteins is negligible. Metformin partially associated with erythrocytes. FROM_m_Oh in the blood below C_m_Oh in plasma, and is reached approximately in the same time. At usual therapeutic doses, metformin is not metered in plasma, except in cases of impaired renal function. The average volume of distribution varies in the range of 63-276 liters.

Metabolism

Metformin is metabolized in an unbound form. Metabolites were not found.

Excretion

Metformin is excreted unchanged by the kidneys. The renal clearance of metformin is> 400 ml / min, indicating that metformin is excreted due to glomerular filtration and tubular secretion. After oral administration, the elimination half-life is about 6.5 hours.

With impaired renal function the clearance of metformin decreases in proportion to the clearance of creatinine, the half-life increases, which can lead to an increase in the concentration of metformin in the plasma.

Indications:Treatment of type 2 diabetes in adults (especially in obese patients), with ineffective diet and exercise as a monotherapy or in combination with other oral hypoglycemic agents or with insulin.

Contraindications:

- Hypersensitivity to metformin or to any auxiliary substance;

- diabetic ketoacidosis, diabetic precoma, coma;

- renal failure or impaired renal function (creatinine clearance less than 60 ml / min);

- acute conditions that occur with a risk of developing renal dysfunction;

- Dehydration (with diarrhea, vomiting), severe infectious diseases, shock;

- the state of hypoxia (shock, sepsis, kidney infections, broncho-pulmonary diseases);

- clinically pronounced manifestations of acute and chronic diseases that can lead to the development of tissue hypoxia (including cardiac or respiratory failure, acute myocardial infarction);

- extensive surgery and trauma, when insulin therapy is indicated (see section "Special instructions");

- liver failure, a violation of liver function;

- chronic alcoholism, acute alcohol poisoning;

- pregnancy, the period of breastfeeding;

- lactic acidosis (including in the anamnesis);

- use for at least 48 hours before and within 48 hours after the radioisotope or X-ray studies with the introduction of iodine-containing contrast medium (see section "Interaction with other drugs");

- compliance with the hypocaloric diet (less than 1000 kcal / day);

- Children under 18 years.

Carefully:

Use the drug in people over 60 years of age, performing heavy physical work, which is associated with an increased risk of developing lactic acidosis.

Pregnancy and lactation:

When planning pregnancy, as well as in case of pregnancy on the background of taking metformin, the drug should be canceled and insulin therapy prescribed.

The patient should inform the doctor about the onset of pregnancy on the background of admission preparation of metformin.

Since there is no data on the penetration of metformin into breast milk, this drug is contraindicated in breastfeeding. If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Diaformin® OD is administered orally. Tablets are swallowed without chewing, during dinner (1 time per day) or during breakfast and dinner (2 times a day). Tablets should be taken only during meals.

The dose of the drug is determined based on the glucose content in the blood plasma.

Monotherapy and combination therapy in combination with other hypoglycemic agents

Usual initial dose: 1 tablet 1 time per day during dinner.

When switching from the drug metformin with the usual release of the active ingredient, the initial dose of Diaformin® OD should be equal to the daily dose of metformin with the usual release of the active ingredient.

Titration of the dose. Depending on the level of glucose in the blood plasma, every 10-15 days, the dose is slowly increased by 500 mg to the maximum daily dose.

The maximum daily dose: 4 tablets 1 time per day during dinner.

If glucose control is not achieved at the maximum daily dose, taken once a day, then you can consider the possibility of dividing this dose into several doses per day according to the following scheme: 2 tablets at breakfast and 2 tablets at dinner.

Combination with insulin

When using the preparation of D-iformin® OD together with insulin, the usual initial dose of the drug is 1 tablet once a day, and the insulin dose is selected based on the results of measuring the concentration of glucose in the blood plasma.

Duration of treatment

Diaformin® OD should be taken daily, without interruption.In the event of discontinuation of treatment, the patient should inform the physician about this.

Dose skip

If the next dose is missed, the next dose should be taken at the usual time. You can not double the dose of the drug.

Elderly patients and patients with reduced renal function

Elderly patients and patients with reduced renal function dose adjusted to the basis of renal function assessment, which must be done regularly at least 2 times a year.

Children

Diaformin® OA should not be used in children and adolescents because of lack of application data.

Side effects:

The frequency of side effects of the drug is assessed as follows:

Very Frequent: ≥ 1/10

Frequent: ≥ 1/100, < 1/10

Infrequent: ≥ 1/1000, < 1/100

Rare: ≥ 1/10 000, < 1/1000

Very rare: <1/10 000

Single: can not be evaluated with the available data.

Side-effect is presented in order of decreasing importance:

Nervous system:

Often: a taste disorder (metallic taste in the mouth).

Gastrointestinal disorders:

Very often: nausea, vomiting, diarrhea, abdominal pain and lack of appetite.

Most often they occur during the initial period of treatment and in most cases spontaneously pass. To prevent symptoms, it is recommended to take metformin during or after a meal, dividing the daily dose into 2 divided doses per day.Slow increase in dose may improve gastrointestinal tolerance. If the symptoms persist for a long time, stop taking the medication and seek medical advice.

Skin and subcutaneous tissue:

Very rarely: skin reactions, such as erythema, pruritus, urticaria.

Metabolic disorders:

Very rarely: lactic acidosis (See "Special instructions").

Hepatobiliary disorders:

There are isolated reports of impaired liver function or hepatitis; After the withdrawal of metformin, undesirable phenomena completely disappear.

If dyspeptic symptoms do not disappear, metformin treatment should be discontinued.

Other:

In patients treated with metformin for a long time, there may be a decrease in vitamin absorption AT₁₂, accompanied by a decrease in its concentration in the blood serum. When detecting megaloblastic anemia, it is necessary to consider the possibility of such etiology.

Overdose:

When metformin was used at a dose of 85 g (42.5 times the maximum daily dose), no development of hypoglycemia was observed. However, lactoacidosis was observed in this case.The early symptoms of lactic acidosis are nausea, vomiting, diarrhea, lower body temperature, abdominal pain, muscle pain, there may be more rapid breathing, dizziness, impaired consciousness and coma development.

Treatment: in the case of the appearance of signs of lactic acidosis, the drug should be discontinued immediately, the patient should be hospitalized immediately and, after determining the concentration of lactate, clarify the diagnosis. The most effective measure for excretion from the body of lactate and metformin is hemodialysis. Conduct also symptomatic treatment.

Interaction:

Contraindicated combinations

Iodine-containing radiopaque agents: on the background of functional renal failure in patients with diabetes mellitus, a radiological study using iodine-containing radiocontrast agents can cause lactic acidosis.

Unrecommended combinations

Alcohol intake increases the risk of lactic acidosis during acute alcohol intoxication, especially in case of malnutrition, compliance with a low-calorie diet of liver failure.

When taking the drug, avoid drinking alcohol and medications containing ethanol.

Combinations requiring special care

Danazol: It is not recommended simultaneous reception of danazolum in order to avoid hyperglycemic action of the latter. If necessary, treatment with danazol and after stopping the latter requires a dose adjustment of metformin under the control of glucose.

Chlorpromazine: when taken in high doses (100 mg per day) increases glycemia, reducing the release of insulin

When treating with neuroleptics and after stopping the intake of the latter, correction of the dose of the drug under the control of glycemia is required.

Glucocorticosteroids (GCS): systemic and local effects reduce glucose tolerance, increase glycemia, sometimes causing ketosis. In the treatment of GCS and after stopping the intake of the latter, correction of the dose of metformin under the control of glycemia is required.

Diuretics: simultaneous administration of "loop" diuretics can lead to the development of lactic acidosis due to possible functional renal failure. Do not assign metformin, if the creatinine clearance is less than 60 ml / min.

Assigned in the form of injections beta₂-adrenomimetics: increase glycemia due to beta stimulation₂adrenoreceptors. In this case, it is necessary to control glycemia. If necessary, the appointment of insulin is recommended.

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

Angiotensin converting enzyme inhibitors and other antihypertensive drugs can reduce the glucose in the blood. If necessary, the dose of metformin should be adjusted.

With the simultaneous use of metformin with derivatives of sulfonylurea, insulin, acarboseth, salicylates possibly increased hypoglycemia.

"Loop" diuretics and non-steroidal anti-inflammatory drugs (NSAIDs) increase the risk of decreased kidney function. In this case, care must be taken when applying metformin.

Nifedipine: increases absorption and C_m_Oh metformin.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim and vancomycin), secreted in the renal tubules, compete for tubular transport systems.

Special instructions:

Lactic acidosis is rare, but serious (high mortality in the absence The complication that can arise from cumulation metformin. Cases of lactic acidosis in patients who received metformin, arose in mainly in patients with diabetes mellitus with severe renal failure.

Other associated risk factors, such as poorly controlled diabetes, ketosis, prolonged starvation, alcoholism, liver failure and any condition associated with severe hypoxia, should be considered. This can help reduce the incidence of lactoacidosis.

The risk of developing lactic acidosis when nonspecific signs appear, such as muscle pains, convulsions accompanied by dyspeptic disorders, abdominal pain, general weakness and severe malaise should be considered. In this case, the patient should stop taking the drug and immediately consult a doctor.

Lactic acidosis is characterized by acidotic dyspnea, abdominal pain and hypothermia followed by coma. Diagnostic laboratory indicators are a decrease in blood pH (less than 7.25), a lactate content in the blood plasma above 5 mmol / l, an increased anion gap and a lactate / pyruvate ratio. If you suspect a metabolic acidosis, stop taking the medication and consult a doctor immediately.

The use of metformin should be discontinued 48 hours before planned surgery and can be continued no earlier than 48 hours after, provided that during the examination the kidney function was recognized normal. Appointment of the drug Diaformin® OD should be discontinued 48 hours before and not resumed 48 hours after the X-ray examination using iodine-containing radiopaque agents, provided that during the examination the kidney function was normal.

Because the metformin is excreted by the kidneys, before the beginning of treatment and regularly in then, it is necessary to determine the content and / or clearance of creatinine (CC) in serum: 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 QC at the lower limit of the norm.

Therapy with Diaformin® OD is recommended to begin after assessment of kidney function.

With a decrease in QC kidney function should be monitored at least 2-4 times a year.

It should be very careful with possible kidney dysfunction in elderly patients, with the simultaneous use of antihypertensive drugs, diuretics or non-steroidal anti-inflammatory drugs (NSAIDs).

The patient should inform the doctor of a bronchopulmonary infection or infectious diseases of the urino-genital organs.

Regular laboratory tests should be performed regularly to monitor diabetes mellitus

It is necessary to warn the patient that inactive components of the drug Diaformin® OD can be released unchanged through the intestines, which does not affect the therapeutic activity of the drug.

Effect on the ability to drive transp. cf. and fur:

Monotherapy with Diaformin® OD does not cause hypoglycemia, so it does not affect the ability to drive vehicles and work with mechanisms.

When using Diaphorm-OD with other hypoglycemic agents (sulfonylureas, insulin, etc.), hypoglycemic conditions may develop,at which the ability to manage motor vehicles and engage in other potentially hazardous activities that require increased attention and rapid psychomotor reactions deteriorates.

Form release / dosage:

Long-acting tablets, 500 mg.

Packaging:

10 tablets in a contour mesh package (blister) from PVC / PVDC / Al; 3, 6, 9 blisters in a cardboard box together with instructions for use.

Storage conditions:

Store in a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000636

Date of registration:28.09.2011 / 15.02.2016

Expiration Date:28.09.2016

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp03.11.2016

Illustrated instructions

Instructions

Diaformin® OD (Diaformin® OD)