Formetin Long sustained release pills 1000mg, 60pcs

Composition

Per tablet:

Active ingredient: metformin hydrochloride – 500.00 mg,750.00 mg,80.00 mg,1000.0 mg.

Excipients: hypromellose (hydroxypropyl methylcellulose 200000 SDR) – 248,00 mg of 330.00 mg of 374.00 mg of 294.00 mg; of hyprolose (hydroxypropyl cellulose) to 40.0 mg 60,00 mg of 68.00 mg of 70.00 mg; magnesium stearate – 4.00 mg 6.00 mg of 6.80 mg of 7.00 mg; silicon dioxide colloidal (Aerosil) – 4,00 mg 6.00 mg of 6.80 mg of 7.00 mg; lactose monohydrate – 4.00 mg of 48.00 mg,54,40 mg of 22.00 mg.

Shell: VIVACOAT® RA-1 R-000 [hypromellose (hydroxypropyl methylcellulose 6 SDR) – of 9.36 mg of 14.04 mg,15,99 mg,16,38 mg; titanium dioxide – 7,20 mg of 10.80 mg 12,30 mg of 12.60 mg; Polydextrose – 3,60 mg of 5.40 mg of 6.15 mg of 6.30 mg; talc – 2,40 mg of 3.60 mg of 4.10 mg,4.20 mg; polyethylene glycol 3350 (macrogol-3350) – 1,44 mg of 2.16 mg of 2.46 mg of 2.52 mg] – 24,00 mg of 36.00 mg 41,00 mg of 42.00 mg.

Pharmacological properties

Pharmacotherapeutic group:

Hypoglycemic agent for oral use of the biguanide

ATX group:  

A. 10. B. A. 02 Metformin

Pharmacodynamics :

Metformin is a hypoglycemic biguanide that reduces both basal and postprandial plasma glucose concentrations. It does not stimulate insulin secretion and therefore does not cause hypoglycemia. Increases the sensitivity of peripheral insulin receptors and the utilization of glucose by cells. Reduces liver glucose production by inhibiting gluconeogenesis and glycogenolysis. Delays the absorption of glucose in the intestines. Metformin stimulates glycogen synthesis by acting on glycogen synthase. Increases the transport capacity of all types of membrane glucose transporters. While taking metformin, the patient’s body weight either remains stable or decreases moderately.

Metformin has a beneficial effect on lipid metabolism: it reduces the content of total cholesterol, low-density lipoproteins and triglycerides.

Pharmacokinetics:

Suction

After oral use of the drug in the form of long-acting tablets, the absorption of metformin is slowed down compared to tablets with a normal release of metformin.

The time to reach the maximum concentration of Cmax at an average value is 5-7 hours (in the range from 4 to 12 hours). At the same time, the TMAX for a normal-release tablet is 2.5 hours.

At steady state, identical to the steady state of metformin with normal release, the maximum concentration (Cmax) and area under the concentration – time curve (AUC) increase out of proportion to the dose taken. After a single oral dose of 2000 mg of metformin in the form of long-acting tablets, the AUC is similar to that observed after taking 1000 mg of metformin in the form of tablets with a normal release twice a day. Intra-individual variability in Cmax and AUC after taking metformin in the form of long-acting tablets is similar to that observed after taking metformin in the form of tablets with a normal release.

The absorption of metformin from long-acting tablets does not change depending on food intake. No accumulation is observed with repeated use of up to 2000 mg of metformin in the form of long-acting tablets.

Distribution

The association with plasma proteins is insignificant. Cmax in blood is lower than Cmax in plasma and is reached after approximately the same time. The average volume of distribution (Vd) varies in the range of 63-276 liters.

Metabolism

No metabolites were detected in humans.

Deduction

Metformin is excreted unchanged by the kidneys.

Renal clearance of metformin is > 400 ml / min, which indicates that metformin is eliminated by glomerular filtration and tubular secretion. After oral use, the elimination half-life is about 6.5 hours. With impaired renal function, metformin clearance decreases in proportion to creatinine clearance, and the elimination half-life increases, which can lead to an increase in the concentration of metformin in plasma.

Indications

Type 2 diabetes mellitus in adults, especially in obese patients, when diet therapy and exercise are ineffective:

– as monotherapy;

– in combination with other oral hypoglycemic agents or with insulin.

Contraindications

– Hypersensitivity to Metformin or to any accessory ingredient;

– diabetic ketoacidosis, diabetic precoma, coma;

renal failure or impaired renal function (creatinine clearance less than 45 ml/min);

acute condition of proceeding with the risk of developing kidney problems: dehydration (chronic or severe diarrhea, repeated vomiting), severe infection (e. g., respiratory tract infections, urinary tract infections), shock;

– symptomatic manifestations of acute or chronic diseases which can lead to the development of tissue hypoxia (including cardiac or respiratory failure, acute myocardial infarction);

– extensive surgery and trauma, when shown holding insulin (see section “Special instructions”);

– liver failure, liver dysfunction;

chronic alcoholism, acute alcohol poisoning;

– pregnancy;

– lactic acidosis (including history);

– application in less than 48 hours before and within 48 hours after the radioisotope or radiological examinations with use of iodinated contrast agents (e. g., internal urography, angiography) (see section “Interaction with other medicines”);

– adherence to a reduced-calorie diet (less than 1000 cal/day);

– lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

– children up to age 18 years due to a lack of data on the application.

With caution:

Apply the drug:

– in people over 60 years of age who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis;

– in patients with renal insufficiency (creatinine clearance 45-59 ml / min)

– during breastfeeding.

Side effects

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

Very frequent: ≥ 1/10.

Frequent: ≥ 1/100, < 1/10.

Infrequent: ≥ 1/1000, < 1/100.

Rare: ≥ 1/10 000,

Very rare: <1/10,000.

Metabolic and nutritional disorders:

Very rare: lactic acidosis (see “Special instructions”).

With prolonged use of metformin, there may be a decrease in the absorption of vitamin B12. If megaloblastic anemia is detected, it is necessary to consider the possibility of such an etiology.

Nervous system disorders:

Common: taste disorder (metallic taste in the mouth).

Disorders of the gastrointestinal tract:

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

Most often, they occur during the initial period of treatment and in most cases pass spontaneously. To prevent symptoms, it is recommended to take metformin with a meal. Slowly increasing the dose may improve gastrointestinal tolerance.

Liver and biliary tract disorders:

Very rare: impaired liver function and hepatitis; after discontinuation of metformin, these adverse events completely disappear.

Skin and subcutaneous tissue disorders:

Very rare: skin reactions such as erythema (redness of the skin), pruritus, urticaria.

If any of the side effects listed in the instructions get worse, or any other side effects that are not listed in the instructions are noticed, you should inform your doctor.

Interaction

Contraindicated combinations

of iodine-containing radiopaque agents: against the background of functional renal failure in patients with diabetes mellitus, radiological examination with the use of iodine-containing radiopaque agents may cause the development of lactic acidosis. Taking Formetin® Long-term therapy should be discontinued, depending on renal function,48 hours before or during the X-ray examination using iodine-containing radiopaque agents, and resumed no earlier than 48 hours after, provided that renal function was found to be normal during the examination.

Not recommended combinations

Alcohol: acute alcohol intoxication increases the risk of developing lactic acidosis, especially in the case of:

– insufficient nutrition, compliance with a low-calorie diet;

– liver failure.

While taking the drug, you should avoid taking alcohol and drugs containing ethanol.

Combinations that require caution

Medications with indirect hyperglycemic effects (for example, glucocorticosteroids (corticosteroids) and tetracosactide (systemic and local action), beta-2-adrenomimetics, danazol, chlorpromazine when taken in large doses (100 mg per day) and diuretics: more frequent monitoring of blood glucose concentration may be required, especially at the beginning of treatment. If necessary, the dose of the drug Formetin® Long can be adjusted during treatment and after its termination, based on the level of glycemia.

Diuretics: concomitant use of loop diuretics may lead to lactic acidosis due to possible functional renal failure. Do not prescribe Formetin® Long if the creatinine clearance is less than 45 ml/min.

With simultaneous use of the drug Formetin® Long 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.

Colesevelam, when used concomitantly with metformin in the form of long-acting tablets, increases the concentration of metformin in blood plasma (an increase in AUC without a significant increase in Cmax).

How to take, course of use and dosage

Formetin®preparation Long, film-coated long-release tablets,500 mg,750 mg,850 mg,1000 mg taken orally. Tablets are swallowed whole, without chewing, with a small amount of liquid, once a day during dinner.

The dose of the drug is selected by the doctor individually for each patient based on the results of measuring the concentration of glucose in the blood.

Monotherapy and combination therapy in combination with other hypoglycemic agents

– for patients who do not take metformin, the recommended initial dose of Formetin® Long, a film-coated long-release tablet, is 500 mg,750 mg, or 850 mg once daily with dinner. Every 10-15 days, it is recommended to adjust the dose, depending on the concentration of glucose in the blood plasma. A slow increase in the dose helps to reduce gastrointestinal side effects;

– for patients already receiving metformin treatment, the initial dose of Formetin®is recommended. Long should be equivalent to the daily dose of normal-release tablets;

– patients taking metformin in the form of tablets with a normal release of the active ingredient in a dose exceeding 2000 mg are not recommended to switch to Formetin® Long;

– in the case of planning a transition from another hypoglycemic agent, the dose selection is carried out as described above, starting with the appointment of Formetin® Long in a dose of 500 mg,750 mg or 850 mg, with a possible subsequent transition to the drug Formetin® Long 1000 mg.

Combination with insulin

To achieve better blood glucose control, metformin and insulin can be used as a combination therapy. Usual starting dose of Formetin® Long is one tablet of 500 mg,750 mg or 850 mg once a day with dinner, while the dose of insulin is selected based on the results of measuring the concentration of glucose in the blood. Then you can switch to Formetin® Long 1000 mg.

Daily dose

The maximum recommended dose of the drug Formetshg Long, film-coated long-release tablets,500 mg and 1000 mg, respectively, is 4 tablets of 500 mg (2000 mg) or 2 tablets of 1000 mg (2000 mg) per day. If when taking the maximum recommended dose of Formetin® Long 500 mg or 1000 mg once daily can not achieve adequate glycemic control, the maximum dose can be divided into two doses: 2 tablets of 500 mg-during breakfast and 2 tablets of 500 mg – during dinner, or one tablet of 1000 mg – during breakfast and one tablet of 1000 mg during dinner.

Recommended dose of Formetin® Long, film-coated long-acting tablets,750 mg and 850 mg are, respectively,2 tablets of 750 mg (1500 mg) or 2 tablets of 850 mg (1700 mg) once a day. If when taking the recommended dose of Formetin® If adequate glycemic control is not achieved for long periods of 750 mg or 850 mg, it is possible to increase the dose to the maximum – respectively,3 tablets of no 750 mg (2250 mg) or 3 tablets of 850 mg (2550 mg) of Formetin® Long once a day. To reduce side effects from the gastrointestinal tract, take a daily dose of Formetin® Long 750 mg or 850 mg can be divided into 2 doses.

If adequate glycemic control is not achieved when taking the maximum recommended dose of Formetin® Long, it is possible to switch to metformin with the usual release of the active ingredient (for example, Formetin ® tablets 0.5 g,0.85 g,1.0 g) with a maximum daily dose of 3000 mg.

Use of the drug in patients with renal insufficiency

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

The initial dose is 500 mg or 750 mg once a day. The maximum dose is 1000 mg per day. Renal function should be carefully monitored every 3-6 months. If the creatinine clearance is below 45 ml / min, the drug should be discontinued.

Use of the drug in elderly patients

In elderly patients, the metformin dose is adjusted based on an assessment of renal function, which should be performed regularly, but at least 2 times a year (See “Special Instructions”).

Duration of treatment

Formetin® Long should be taken daily, without interruption. If treatment is discontinued, the patient should inform the doctor.

Skipping a dose

If the next dose is missed, the patient should take the next dose at the usual time. Do not take a double dose of Formetin® Long.

Overdose

Hypoglycemia was not observed when metformin was administered at a dose of 85 g (42.5 times the maximum daily dose). However, in this case, the development of lactic acidosis was observed. Significant overdose or associated risk factors may lead to lactic acidosis (see “Special instructions”).

Treatment: in case of signs of lactic acidosis, treatment with 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 removing lactate and metformin from the body is hemodialysis. Symptomatic treatment is also performed.

Special instructions

Lactic acidosis

Lactic acidosis is a rare but serious complication (high mortality in the absence of urgent treatment) that can occur due to the accumulation of metformin. Cases of lactic acidosis during metformin use occurred mainly in patients with diabetes mellitus with severe renal insufficiency.

Other associated risk factors should also 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 considered if there are non-specific signs, such as muscle cramps accompanied by dyspeptic disorders, abdominal pain and severe asthenia.

Lactic acidosis is characterized by severe malaise with general weakness, acidotic dyspnea, vomiting, abdominal pain, muscle cramps, and hypothermia followed by coma. Diagnostic laboratory parameters are a decrease in blood pH (less than 7.25), a concentration of lactate in blood plasma over 5 mmol / l, an increased anion gap and the ratio of lactate/pyruvate. If lactic acidosis is suspected, stop taking the drug and immediately consult a doctor.

Surgical operations

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

Kidney function

Since metformin is excreted by the kidneys, before starting treatment and regularly thereafter, it is necessary to determine creatinine clearance: 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 creatinine clearance at the lower limit of normal.

Special care should be taken in case of possible renal impairment in elderly patients, when concomitant use of antihypertensive drugs, diuretics or nonsteroidal anti-inflammatory drugs.

Heart failure

Patients with heart failure have a higher risk of developing hypoxia and kidney failure. Patients with chronic heart failure should have their heart function and kidney function monitored regularly while taking metformin. Metformin is contraindicated in patients with acute heart failure and chronic heart failure with unstable hemodynamic parameters.

Other safety measures:

– Patients are advised to continue to follow a diet with a uniform intake of carbohydrates throughout the day. Overweight patients are recommended to continue to follow a hypocaloric diet (but not less than 1000 kcal / day). Patients should be regularly do physical exercises;

– patients should inform the doctor about any ongoing treatment and any infectious diseases such as colds, respiratory infections or urinary tract infections;

– it is recommended to regularly conduct standard laboratory tests for the control of diabetes;

Metformin monotherapy does not cause hypoglycaemia, but are advised to exercise caution in its use in combination with insulin or other oral hypoglycemic agents (e. g. sulfonylureas or Repaglinide, etc. ). Symptoms of hypoglycemia are weakness, headache, dizziness, sweating, palpitations, blurred vision, or impaired concentration of attention;

– it is necessary to warn the patient that the inactive components of the drug Formatin® Longs can be excreted unchanged through the intestines, which does not affect the therapeutic activity of the drug;

– each tablet contains 4.00 mg,48.00 mg,54.40 mg,22.00 mg of lactose. The drug is contraindicated in patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Influence on the ability to drive vehicles and mechanisms:<

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