Formetin, tablets 500 mg 60 pcs

Name: Formetin, tablets 500 mg 60 pcs
SKU: 220278
Availability: InStock

€3.24

EAN: 4601669004062 SKU: 220278 Categories: Diabetes, Hypoglycemic drugs, Medicine

Description

Formethine has hypoglycemic effect.

Pharmacodynamics

Metformin inhibits gluconeogenesis in the liver, reduces glucose absorption from the intestine, increases peripheral glucose utilization and increases tissue sensitivity to insulin.

With this it has no effect on insulin secretion 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 tissue-type plasminogen activator inhibitor.

Pharmacokinetics

After oral administration, metformin is slowly absorbed from the gastrointestinal tract. Bioavailability after a standard dose is 50-60%. Maximum plasma concentration is reached 2.5 hours after oral administration. It practically does not bind with plasma proteins.

It is accumulated in salivary glands, muscles, liver and kidneys. It is excreted unchanged by kidneys. Period of half-life is 1.5-4.5 hours. Cumulation of the drug is possible in patients with impaired renal function.

Indications

Type 2 diabetes

Type 2 diabetes mellitus when diet therapy is ineffective (especially in obese patients).

Active ingredient

Metformin

How to take, the dosage

Ingestion. Tablets are swallowed whole, without chewing, with a small amount of liquid, 1 time/day with dinner.

The dose of Merifatin MB is adjusted by the physician individually for each patient based on the results of blood glucose concentration determination.

Adult patients with normal renal function (CK ≥ 90 ml/min)

Monotherapy and combination therapy in combination with other hypoglycemic agents

Merifatin MB in dose of 1000 mg should be taken once daily (once/day) at supper time.

– Merifatin MB in a dose of 1000 mg is indicated as maintenance therapy for patients taking normally-released metformin in a dose of 1000 mg or 2000 mg. To switch to Merifatin CF at a dose of 1000 mg, the daily dose of metformin must be equivalent to the daily dose of normal-release metformin.

– Patients taking metformin in the form of normal-release tablets at a dose greater than 2000 mg are not recommended to switch to Merifatin CF at a dose of 1000 mg.

– For patients not taking metformin, the recommended starting dose of Merifatin MB is 500 mg or 750 mg once daily, with dinner. It is recommended that the dose be adjusted every 10 to 15 days based on the results of blood glucose concentrations. Slowly increasing the dose helps reduce gastrointestinal (GI) side effects.

– If switching from another hypoglycemic drug, select the dose as described above, starting with Merifatin MB at 500 mg or 750 mg, with a possible subsequent switch to Merifatin MB at 1000 mg.

Combination with insulin

In order to achieve better control of blood glucose concentrations, metformin and insulin may be used as a combination therapy. The usual starting dose of Merifatin MB is 1 tablet 500 mg once daily or 750 mg once daily with dinner, while the dose of insulin is adjusted based on blood glucose measurements. A switch to Merifatin MB at a dose of 1000 mg is then possible.

The daily dose

The maximum recommended dose of Merifatin MB is 4 tablets 500 mg daily (2000 mg) or 3 tablets 750 mg daily (2250 mg) or 2 tablets 1000 mg daily (2000 mg).

If adequate glycemic control is not achieved by taking the maximum recommended dose once daily during dinner, then the maximum dose may be divided into two doses: 2 500 mg tablets at breakfast and 2 500 mg tablets at dinner, or one 1000 mg tablet at breakfast and one 1000 mg tablet at dinner.

If adequate glycemic control is not achieved with the maximum recommended dose of Merifatin MB sustained release tablets, conversion to normal-release metformin with a maximum daily dose of 3000 mg is possible.

Use in Special Clinical Patient Groups

Dose skipping

If the next dose is missed, the next dose should be taken at the usual time. Do not take a double dose of Merifatin MB.

Patients with renal impairment

Metformin may be used in patients with renal impairment with a CK of 30 to 59 mL/min only if there are no conditions/risk factors that may increase the risk of lactoacidosis.

Patients in the elderly

Because of the possible decrease in renal function, the dose of metformin is adjusted based on renal function assessment, which should be performed regularly.

Children and adolescents under 18 years of age

The use of the drug is contraindicated in children and adolescents under 18 years of age (due to a lack of clinical data on efficacy and safety).

The duration of treatment

Merifatin MB should be taken daily, without interruption. If treatment is discontinued, the patient should inform the physician.

Renal function should be monitored closely: CK should be determined every 3-6 months in patients with a CK of 45-59 mL/min and every 3 months with a CK of 30-44 mL/min.

If creatinine clearance is below 30 mL/min, metformin should be stopped immediately.

Interaction

Contraindicated combinations

Iodine-containing radiopaque agents: Against the background of functional renal insufficiency in patients with diabetes mellitus, radiological examination with iodine-containing radiopaque agents may cause development of lactocidosis. Metformin administration should be discontinued depending on renal function 48 hours prior to or at the time of radiology with iodine-based radiopaque agents and should be restarted not earlier than 48 hours after, on condition that renal function was found to be normal during the examination.

Unrecommended combinations

Alcohol: acute alcohol intoxication increases the risk of lactoacidosis, especially if:

– inadequate diet, compliance with a low-calorie diet;

– hepatic insufficiency.

When using the drug, alcohol consumption and taking drugs containing ethanol should be avoided.

Combinations requiring caution.

Drugs with indirect hyperglycemic effects (e.g., GKS (systemic and topical) and tetracosactide, β2-adrenomimetics, danazol, chlorpromazine at high doses (100 mg daily) and diuretics: Blood glucose control may be required more frequently, especially at beginning of treatment. If necessary, the dose of Merifatin MB may be adjusted during treatment and after discontinuation based on glycemic levels.

Diuretics: concomitant use of “loop” diuretics may lead to the development of lactoacidosis due to possible functional renal failure.

The concomitant use of Merifatin MB with sulfonylurea derivatives, insulin, acarbose, salicylates may lead to hypoglycemia.

Nifedipine increases absorption and Cmax of metformin.

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

Colesevelam, when used concomitantly with metformin in the form of sustained-release tablets, increases plasma metformin concentrations (increases AUC without significantly increasing Cmax). Hypoglycemic action of metformin may be decreased by phenothiazides, glucagon, estrogens, oral contraceptives, phenytoin, sympathomimetics, nicotinic acid, isoniazid, “slow” calcium channel blockers, sodium levothyroxine.

Concomitant use with cimetidine decreases metformin excretion rate, which may lead to lactoacidosis.

In healthy volunteers, concomitant use of metformin and propranololol and use of metformin and ibuprofen showed no change in their pharmacokinetic parameters.

Metformin may decrease the effect of indirect anticoagulants.

Organic cation transporter substrates 1 and 2 (OCT1 and OCT2)

Metformin is a substrate of organic cations OCT1 and OCT2.

When used together with metformin:

OST1 inhibitors (such as verapamil) may decrease the hypoglycemic effects of metformin;
OST1 inducers (such as rifampicin) may increase gastrointestinal absorption of metformin and increase its hypoglycemic effects;
OCT2 inhibitors (such as cimetidine, dolutegravir, ranolazine, trimethoprim, vandetanib, izavuconazole) may reduce the renal excretion of metformin and lead to an increase in its plasma concentration;
OCT1 and OCT2 inhibitors (such as crizotinib, olaparib) may reduce the hypoglycemic effect of metformin.

Special Instructions

Lactoacidosis

Lactoacidosis is a rare but serious (high mortality if not treated urgently) complication that can occur due to metformin cumulation. Cases of lactoacidosis when taking metformin have occurred mainly in patients with diabetes mellitus with severe renal insufficiency.

The risk of lactoacidosis should be considered if nonspecific signs occur, such as muscle cramps accompanied by dyspeptic disorders, abdominal pain, and marked asthenia.

Lactoacidosis is characterized by severe malaise with general weakness, acidotic dyspnea and vomiting, abdominal pain, muscle cramps and hypothermia followed by coma. Diagnostic laboratory indicators are decreased blood pH (less than 7.35), plasma lactate concentrations greater than 5 mmol/L, and elevated anion gap and lactate/pyruvate ratio. If lactoacidosis is suspected, discontinue the drug and consult a physician immediately.

Intravascular administration of iodine-containing radiopaque agents may lead to renal failure and metformin cumulation, which increases the risk of lactoacidosis. Metformin should be discontinued, depending on renal function, 48 hours before or during radiological examination with iodine-containing radiopaque agents, and not resumed until 48 hours after, provided that renal function has been found normal during the examination.

Surgical surgeries

The use of metformin should be discontinued 48 hours before elective surgical procedures and may not be resumed until 48 hours after, provided that renal function has been found to be normal in the evaluation.

Renal function

Because metformin is excreted by the kidneys, serum CK and/or CK levels should be determined before initiating treatment and regularly thereafter: at least once a year in patients with normal renal function and 2-4 times a year in elderly patients and in patients with CK at the lower limit of normal.

Particular caution should be exercised if renal function may be impaired in elderly patients, concomitant use of hypotensive drugs, diuretics or non-steroidal anti-inflammatory drugs.

In case of dehydration (chronic or severe diarrhea, repeated bouts of vomiting).

Heart failure

Patients with heart failure have a higher risk of developing hypoxia and renal failure. Patients with chronic heart failure should have regular monitoring of cardiac renal function while taking metformin. Metformin administration is contraindicated in acute heart failure and chronic heart failure with unstable hemodynamic parameters.

Other precautions

Patients are advised to continue on a diet with an even carbohydrate intake throughout the day. Patients who are overweight are recommended to continue on a hypocaloric diet (but at least 1000 kcal/day). Patients should also do regular exercise.

– Patients should inform their doctor about any treatments they are taking and any infectious diseases, such as colds, respiratory infections, or urinary tract infections.

– Regular standard laboratory tests to control diabetes are recommended.

– Metformin does not cause hypoglycemia during monotherapy, but caution is recommended when it is used in combination with insulin or other oral hypoglycemic agents (e.g., sulfonylurea derivatives or repaglinide, etc.). Symptoms of hypoglycemia include weakness, headache, dizziness, increased sweating, palpitations, visual impairment, or impaired concentration.

– The patient should be cautioned that the excipients of Merifatin may be excreted unchanged through the intestine without affecting the pharmacological effects of the drug.

Influence on the ability to operate vehicles and mechanisms:

Merifatin monotherapy does not cause hypoglycemia and therefore does not affect the ability to operate vehicles and mechanisms. Nevertheless, hypoglycemia may develop when using metformin in combination with other hypoglycemic drugs (sulfonylurea derivatives, insulin, repaglinide, etc.). When symptoms of hypoglycemia occur, do not drive vehicles and mechanisms.

Contraindications

– Hypersensitivity to metformin or any excipient;

– diabetic ketoacidosis, diabetic precoma, coma;

– renal insufficiency or impaired renal function (CKG less than 30 ml/min);

– acute conditions with risk of renal impairment: dehydration (with chronic or severe diarrhea, repeated bouts of vomiting), severe infectious diseases (e.g., respiratory tract infections, urinary tract infections), shock;

– clinically manifest acute or chronic conditions that may lead to the development of tissue hypoxia (includingacute heart failure, chronic heart failure with unstable hemodynamic parameters, respiratory failure, acute myocardial infarction);

– major surgical operations and injuries when insulin therapy is indicated (see “Special Precautions. “

– hepatic insufficiency, impaired liver function;

– chronic alcoholism, acute alcohol intoxication;

– pregnancy;

– lactoacidosis (including

– use less than 48 hours before and 48 hours after radioisotopic or radiological studies with iodine contrast media (e.g., intravenous urography, angiography). “Interaction with other drugs”);

– compliance with a hypocaloric diet (< 1000 calories/day);

– age under 18 years (due to the lack of data on the effectiveness and safety of use in this age group).

With caution:

– In patients over 60 years of age who perform heavy physical work, due to the increased risk of lactoacidosis in them;

– In patients with renal insufficiency (CK 30-59 ml/min);

– During breastfeeding.

Side effects

Classification of the incidence of HP when using the drug according to the recommendations of the World Health Organization (WHO): very frequently (≥1/10); frequently (≥1/100, < 1/10); infrequently (≥1/1000, < 1/100); rarely (≥1/10000, < 1/1000); very rarely (< 1 /10000).

Metabolic disorders: very rare – lactoacidosis (see “Special Precautions”).

Long-term administration of metformin may result in decreased absorption of vitamin B12. If megaloblastic anemia is detected, the possibility of this etiology should be considered.

Nervous system disorders: often – taste disorders (metallic taste in the mouth).

Gastrointestinal disorders: very often – nausea, vomiting, diarrhea, abdominal pain and lack of appetite. They occur most frequently during the initial period of treatment and in most cases spontaneously go away. To prevent the symptoms, it is recommended that metformin be taken with or after meals. Slowly increasing the dose may improve tolerability on the gastrointestinal side.

Liver and biliary tract side effects: very rare – impaired liver function and hepatitis; these HP disappear completely after discontinuation of the drug.

Skin and subcutaneous tissue disorders: very rare – skin reactions such as erythema (skin redness), itching, urticaria.

If any of the HP listed in the instructions worsened or other HP not listed in the instructions appeared, you should tell your doctor.

Overdose

Hypoglycemic episodes were not observed when using metformin at a dose of up to 85 g (42.5 times the maximum daily dose). However, in this case, the development of lactoacidosis was observed. Significant overdose or associated risk factors may lead to the development of lactoacidosis.

The symptoms of lactoacidosis are: marked weakness, myalgia, abdominal pain, respiratory disorders, increased somnolence. In severe lactoacidosis, the development of arterial hypotension and resistant bradyarrhythmia has been noted.

Treatment: in case of signs of lactocidosis, the drug should be stopped immediately, the patient should be urgently hospitalized and, having determined the lactate concentration, the diagnosis should be clarified. The most effective measure for lactate and metformin elimination from the body is hemodialysis. Symptomatic treatment is also carried out.

Pregnancy use

Formethine is contraindicated in pregnancy and during lactation (breastfeeding).

Similarities

Siofor 500, Siofor 850, Metformin-Teva, Siofor 1000, Glucofage Long, Formetin, Metformin, Merifatin

Additional information

Weight	0.080 kg
Shelf life	2 years
Conditions of storage	Store in a place protected from light, at a temperature not exceeding 25°C.
Manufacturer	Pharmstandard-Leksredstva, Russia
Medication form	pills
Brand	Pharmstandard-Leksredstva