Description
Glucophage Long Pharmacodynamics
Metformin is a biguanide with hypoglycemic action, which reduces both basal and postprandial plasma glucose content. It does not stimulate insulin secretion and therefore does not cause hypoglycemia. Increases the sensitivity of peripheral receptors to insulin and glucose utilization by cells. Reduces glucose production by the liver by inhibiting gluconeogenesis and glycogenolysis. Delays the absorption of glucose in the intestine.
Metformin stimulates glycogen synthesis by acting on glycogen synthase. Increases the transport capacity of all types of membrane glucose transporters.
During metformin administration, the patient’s body weight either remains stable or decreases moderately.
Metformin has a favorable effect on lipid metabolism: it reduces total cholesterol, low-density lipoproteins and triglycerides.
Indications
Type 2 diabetes mellitus in adults, especially in obese patients, when diet therapy and physical activity are ineffective:
– As monotherapy;
– In combination with other oral hypoglycemic agents or with insulin.
Contraindications
-High sensitivity to metformin or any excipient.
-Diabetic ketoacidosis, diabetic precoma, coma.
-Renal insufficiency or impaired renal function (creatinine clearance less than 45 ml/min).
-Acute conditions with risk of renal dysfunction: dehydration (with chronic or severe diarrhea, repeated bouts of vomiting), severe infectious diseases (e.g., respiratory tract infections, urinary tract infections), shock.
-Clinically expressed manifestations of acute or chronic diseases that may lead to the development of tissue hypoxia (including acute heart failure, chronic heart failure with unstable hemodynamic parameters, respiratory failure, acute myocardial infarction).
-Extensive surgical operations and injuries when insulin therapy is indicated (see section “Special indications”).
-Hepatic insufficiency, liver dysfunction.
-Chronic alcoholism, acute alcohol poisoning.
-Pregnancy.
-Lactoacidosis (including in anamnesis).
Administration for less than 48 hours before and for 48 hours after radioisotopic or radiological studies with iodine-containing contrast media (e.g., intravenous urography, angiography) (see section “Interaction with other medicinal products”);
-Hypocaloric diet (less than 1000 kcal/day).
-Children under 18 years of age due to the lack of data on its use.
Dosage and administration
- Glucofage® Long in the form of sustained-release tablets, 500 mg, is taken orally. Tablets are swallowed whole, without chewing, with a small amount of liquid, once a day during dinner.
- Dose of drug Glucofage® Long in form of sustained-release tablets is chosen by a doctor individually for each patient, based on the results of blood glucose concentration measurement.
- Monotherapy and combined therapy in combination with other hypoglycemic agents
– For patients who do not receive metformin, the recommended initial dose of Glucofage Long is 500 mg
once a day during dinner.
– Depending on plasma glucose concentrations, a slow increase of the dose (by 500
mg), until a maximum daily dose (2000 mg) is reached. Slow dose increases help to reduce gastrointestinal side effects.
– For patients already receiving treatment with metformin, the initial dose of Glucofage Long should be equivalent to the daily dose of tablets with normal release.
– Patients taking metformin in the form of normal-release tablets of the active ingredient at a dose
in excess of 2000 mg, switching to Glucofage Long is not recommended.
– If switching from another hypoglycemic drug is planned, it is necessary to stop taking the other drug and start taking Glucofage Long at the dose specified above. - Combination with insulin To achieve better blood glucose control, metformin and insulin can
can be used as a combination therapy. Usual starting dose of Glucofage Long is one tablet of 500 mg once a day during dinner, while the dose of insulin is adjusted on the basis of blood glucose
blood glucose concentrations. - Daily Dose
Maximum recommended dose of Glucofage Long is 4 tablets 500 mg per day (2000 mg). If the maximum recommended dose once daily at supper time fails to achieve
adequate glycemic control, then the maximum dose can be divided into two doses: 2 tablets 500 mg at breakfast and 2 tablets 500 mg at dinner. If adequate glycemic control is not achieved at the intake of 2000 mg - Glucofage” Long, tablets with prolonged release, it is possible to switch to metformin with
normal release of active ingredient (for example, Glucofage®, film-coated tablets) with maximum daily dose of 3000 mg. 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 lactoacidosis. The initial dose is 500 mg once daily. The maximum dose is 1000 mg per day. Nocicular function should be carefully monitored
every 3 to 6 months. If creatinine clearance is below 45 ml/min, the drug should be stopped immediately. - Elderly patients Because of a possible decrease in renal function, the dose of metformin is adjusted based on the assessment of rhinoceros function, which should be performed regularly, at least 2 times a year. Duration of treatment course
Glucofage® Long should be taken daily, without interruption. In case of discontinuation of treatment the patient should inform the physician. Dose skipping In case of missing the next dose, the patient should take the next dose at the usual time. Ns
should take a double dose of Glucofage Long.
