Sophamet - instructions for use, doses, side effects, contraindications

Composition:1 tablet contains: active substance: metformin hydrochloride - 500.0 mg and 850.0 mg; Auxiliary substances (500 mg / 850 mg): Povidone K25 (30.0 mg / 46.0 mg), microcrystalline cellulose (38.0 mg / 7.0 mg), sorbitol (1.0 mg / 2.0 mg), magnesium stearate (6.0 mg / 15 , 0 mg). Sheath: opadrai II white (25.0 mg / 25.0 mg): hypromellose 2910 (10.0 mg / 10.0 mg), titanium dioxide (6.0 mg / 6.0 mg), lactose monohydrate (5.5 mg / 5.5 mg), Macrogol 3000 (2.0 mg / 2.0 mg), triacetin (1.5 mg / 1.5 mg).

Description:Tablets 500 mg: round biconvex tablets, covered with a white film membrane, on a broken white color.
Tablets 850 mg: oblong biconvex tablets, covered with a white film membrane, with a risk on both sides, on a broken white color.

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.

Pharmacokinetics:After oral administration metformin is absorbed from the gastrointestinal tract. Bioavailability is 50-60%. The maximum concentration in the blood plasma (Stach) is reached 2.5 hours after ingestion. Eating a meal reduces Stach by 40% and slows her achievement by 35 min. Virtually does not bind to plasma proteins. Exposed to a very weak degree of metabolism and excreted by the kidneys. The clearance of metformin in healthy subjects is 400 ml / min (4 times greater than the creatinine clearance), which indicates the presence of active tubular secretion. The half-life is 6.5 hours.
If the kidneys are damaged, cumulation of the drug is possible.

Indications:- Type 2 diabetes mellitus (especially in patients with obesity) without a tendency to ketoacidosis if diet therapy is ineffective;
- in combination with insulin - in type 2 diabetes mellitus, especially with a pronounced degree of obesity, accompanied by secondary insulin resistance.

Contraindications:- hypersensitivity to the drug;
- diabetic ketoacidosis, diabetic precoma, coma;
- impaired renal function (creatinine clearance less than 60 ml / min);
- acute diseases that occur at a risk of kidney dysfunction: dehydration (with diarrhea, vomiting), fever, severe infectious diseases, hypoxia conditions (shock, sepsis, kidney infections, bronchopulmonary diseases);
- clinically pronounced manifestations of acute and chronic diseases that can lead to the development of tissue hypoxia (cardiac or respiratory failure, acute myocardial infarction, etc.);
- Serious surgical operations and traumas (against which background insulin therapy is shown);
- impaired liver function;
- chronic alcoholism, acute alcohol poisoning;
- pregnancy, the period of breastfeeding;
- lactic acidosis (including in the anamnesis);
- use for at least 2 days before and within 2 days after carrying out radioisotope or X-ray studies with the introduction of iodine-containing contrast agent;
- compliance with the hypocaloric diet (less than 1000 kcal / day);
It is not recommended to use 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.

Pregnancy and lactation:When planning pregnancy, as well as in case of pregnancy on the background of taking metformin, it should be canceled and insulin therapy prescribed. Since there is no data on the penetration into human milk, this medication is contraindicated in breastfeeding. If metformin is needed during breastfeeding, breast-feeding should be discontinued.

Dosing and Administration:The dose of the drug is determined by the doctor individually depending on the concentration of glucose in the blood.
Film-coated tablets 500 mg: The initial dose is 500-1000 mg / day (1-2 tablets). After 10-15 days, a further gradual increase in dose, depending on the concentration of blood glucose, is possible. The maintenance dose of the drug is usually 1500-2000 mg / day (3-4 tablets). The maximum dose is 3000 mg / day (6 tablets).
Film-coated tablets 850 mg: The initial dose is 850 mg / day. After 10-15 days, a further gradual increase in dose, depending on the concentration of blood glucose, is possible. The maintenance dose of the drug is usually 1700 mg / day. The maximum dose is 2550 mg / day.
In elderly patients, the recommended daily dose should not exceed 1 g (2 tablets).
Tablets Sophamet should be taken whole during or immediately after meals, with a small amount of liquid (a glass of water). To reduce side effects from the gastrointestinal tract, the daily dose should be divided into 2-3 doses.
Due to the increased risk of lactic acidosis, the dose of the drug should be reduced in case of severe metabolic disorders.

Side effects:On the part of the digestive system: nausea, vomiting, "metallic" taste in the mouth, lack of appetite, diarrhea, flatulence, abdominal pain.
These symptoms occur especially often at the beginning of treatment and, as a rule, pass by themselves. These symptoms can be reduced by the appointment of antacids, m-hloblinblokatorov or antispasmodics. In rare cases - increased activity of "hepatic" transaminases or hepatitis, disappearing after drug withdrawal.
From the side of metabolism: in rare cases - lactic acidosis (requires discontinuation of treatment); with prolonged treatment - hypovitaminosis B12 (a violation of its absorption).
From the hematopoiesis: in some cases - megaloblastic anemia.
From the endocrine system: hypoglycemia.
Allergic reactions: skin rash, itching.

Overdose:With an overdose, it is possible to develop lactic acidosis with a fatal outcome. The cause of the development of lactic acidosis may also be cumulation of the drug due to impaired renal function. 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 case of signs of lactic acidosis, the drug should be stopped immediately, the patient should be hospitalized immediately and, having determined the concentration of lactate, confirm the diagnosis.The most effective measure for excretion from the body of lactate and metformin is hemodialysis. Conduct also symptomatic treatment.
With combined therapy with sulfonylureas, hypoglycemia may develop.

Interaction:Not recommended combinations: It is not recommended simultaneous reception of danazolum in order to avoid hyperglycemic action of the latter. If it is necessary to treat danazol and after stopping the intake of the latter, correction of the dose of metformin under the control of the level of glycemia is required.
Combinations that require special care: Chlorpromazine - when taken in high doses (100 mg per day) increases the concentration of glucose in the blood, reducing the release
insulin. When treating with neuroleptics and after stopping the intake of the latter, correction of the dose of metformin is required under the control of blood glucose concentration.
When used simultaneously with derivatives of sulfonylurea, salicylates, acarbose, insulin, non-steroidal anti-inflammatory drugs, monoamine oxidase inhibitors, oxytetracycline, angiotensin converting enzyme inhibitors, fibrolic acid derivatives, cyclophosphamide, P-blockers, hypoglycemic action of metformin is possible.When used simultaneously with glucocorticosteroids, oral contraceptives, epinephrine, sympathomimetics, glucagon, preparations of iodine-containing thyroid hormones, thiazide and loop diuretics, phenothiazine derivatives, nicotinic acid derivatives, a decrease in the hypoglycemic effect of metformin is possible.
Nifedipine increases absorption, Cmax, slows the excretion of metformin.
Cimetidine slows the excretion of metformin, which increases the risk of developing lactic acidosis.
Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene and vancomycin), secreted by the renal tubules, compete for tubular transport systems and, with prolonged therapy, can increase Cmax by 60%.
Metformin can weaken the effect of indirect anticoagulants (coumarin derivatives).
The risk of developing lactic acidosis increases with acute alcohol intoxication, especially in case of fasting, compliance with a low-calorie diet or liver failure. During treatment should refrain from taking alcohol and medications containing ethanol.
Possible cumulation of metformin and the development of lactic acidosis with intravascular injection iodine containing contrast agents.

Special instructions:During the treatment it is necessary to monitor the kidney function. At least 2 times a year, as well as the appearance of myalgia should determine the content of lactate in the plasma. In addition, once in 6 months, monitoring the level of serum creatinine (especially in elderly patients) is necessary.
Possible use of the drug metformin in combination with sulfonylurea derivatives. In this case, a particularly careful monitoring of blood glucose levels is necessary.
48 hours before and within 48 hours after the radiocontrast study (urography, intravenous angiography) should stop taking metformin.
When a patient has a broncho-pulmonary infection or an infectious disease of the genito-urinary organs, the doctor should be informed immediately about it. During treatment, one should refrain from taking alcohol and medications containing ethanol.

Effect on the ability to drive transp. cf. and fur:The use of the drug in monotherapy does not affect the ability to drive vehicles and work with mechanisms.
When metformin is combined with other hypoglycemic agents (derivatives of sulfonylureas, insulin, etc.), hypoglycemic conditions may develop, in which the ability to drive vehicles and engage in other potentially dangerous activities that require increased attention and rapid psychomotor reactions deteriorates.

Form release / dosage:Tablets, film-coated 500 mg and 850 mg.

Packaging:10 tablets in a blister of PVC / aluminum foil.
5 blisters (500 mg tablets) or 3 blisters (850 mg tablets) together with instructions for use in a cardboard pack.

Storage conditions:List B.
In a dry and dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004840/10

Date of registration:27.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria

Manufacturer: & nbsp

SOPHARMA, AD Bulgaria

Information update date: & nbsp2016-09-26

Illustrated instructions

Instructions

Sofamet (Sophamet)