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 750 mg is taken orally. Tablets are swallowed whole, without chewing, with plenty of fluid, once a day during dinner. Dose of drug Glucofage® Long in form of sustained-action tablets is chosen by a physician individually for each patient, based on the results of blood glucose concentration measurement.
- Monotherapy and combined therapy in combination with other hypoglycemic agents
-Recommended initial dose for patients who do not take metformin is 750 mg of Glucofage® Long once a day during dinner.
-Every 10-15 days it is recommended to adjust the dose on the basis of the results of plasma glucose concentration measurement. Slowly increasing the dose helps to reduce gastrointestinal side effects.
-Recommended dose of Glucofage® Long is 2 tablets of 750 mg once a day. If during taking the recommended dose it is not possible to achieve the adequate glycemic control, the maximum dose can be increased up to 3 tablets of 750 mg of Glucofage® Long once a day.
-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 tablets with normal release of the active ingredient at a dose greater than 2000 mg should not be recommended for switching to Glucofage® Long.
-If switching from another hypoglycemic drug is planned, it is necessary to stop taking the other drug and start Glucophage® Long at the dose indicated above. - Combination with insulin
To achieve better blood glucose control, metformin and insulin may be used as combination therapy. Usual starting dose of preparation Glucofage® Long is one tablet of 750 mg once a day during dinner, while insulin dose is chosen on the basis of blood glucose concentration measurement results. - Daily Dose
Maximal recommended dose of Glucofage® Long is 3 tablets, 750 mg per day (2250 mg).
If adequate glycemic control is not achieved by maximum recommended dose of glucophage® Long, sustained release tablets, switching to metformin with normal release of active ingredient (for example, Glucophage®, film-coated tablets) with maximum daily dose of 3000 mg is possible. - Patients with renal impairment
Metformin can be used in patients with moderate renal insufficiency (creatinine clearance 45-59 ml/min) only in case of absence of conditions that can increase the risk of lactoacidosis. The initial dose is 750 mg once daily. The maximum dose is 1000 mg per day. Renal function should be carefully monitored every 3-6 months.
If cretinin clearance is lower than 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 renal function assessment, which should be performed regularly (See “Special Precautions”). - Treatment duration
Glucofage® Long should be taken daily, without interruption. In case of discontinuation of treatment, the patient should inform the physician.
Skipping a dose - In case of missing the next dose, the patient should take the next dose at the usual time. Do not take a double dose of the drug Glucofage® Long
