Description
Metformin Long Pharmacodynamics
Metformin is a hypoglycemic agent of the biguanide group, which reduces both basal and postprandial blood 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
Diabetes mellitus type 2 in adults, especially in patients with obesity, with ineffectiveness of diet therapy and physical activity:
– As monotherapy;
– in combination with other oral hypoglycemic agents, or with insulin.
Contraindications
– Hypersensitivity to metformin or to any excipient of the drug;
– Diabetic ketoacidosis, diabetic precoma, coma;
renal insufficiency or impaired renal function (CKR less than 45 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 expressed manifestations of acute or chronic diseases that can 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;
hepatic insufficiency, liver dysfunction; chronic alcoholism, acute alcohol poisoning; pregnancy;
Lactoacidosis (including in anamnesis);
use for less than 48 hours before and within 48 hours after radioisotopic or radiological studies with iodine-containing contrast media (e.g., intravenous urography, angiography);
Following a low-calorie diet (less than 1,000 kcal/day);
children under 18 years of age due to lack of data on its use.
Dosage and administration
- Tablets should be taken orally, swallowed whole, without chewing, with plenty of fluid, once a day during or after dinner.
- Dosage of the drug is chosen by a doctor individually depending on blood glucose concentration.
- Monotherapy and combined therapy in combination with other hypoglycemic agents
– In patients who do not take metformin, the recommended initial dose of the drug is 500 mg or 750 mg per day during or after dinner. Every 10 to 15 days, it is recommended that the dose be adjusted based on the results of plasma glucose concentration measurements. Slowly increasing the dose promotes better tolerability from the gastrointestinal tract.
– In case of switching from another hypoglycemic drug, Metformin Long dose selection is performed as described above, starting with 500 mg or 750 mg, with possible subsequent transition to 1000 mg of metformin.
– The drug Metformin Long 1000 mg should be taken once a day during or after dinner.
– Metformin Long 1000 mg is prescribed as maintenance therapy for patients taking metformin in the form of regular-release tablets at a dose of 1,000 mg and 2,000 mg. To switch to Metformin Long, the daily dose should 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 should not be recommended to switch to Metformin Long. - Combination with Insulin
To achieve better glycemic control, Metformin Long and insulin may be used as combination therapy. Usual starting dose of Metformin Long is 1 tablet of 500 mg or 750 mg once a day with supper, while the dose of insulin is chosen on the basis of blood glucose measurements. Further, it is possible to switch to metformin with prolonged release of 1000 mg. - Daily Dose
The maximum recommended daily dose of Metformin Long is 2000 mg. If at taking the maximum recommended dose once a day it is not possible to achieve an adequate glycemic level, the maximum dose may be divided into 2 doses: 1 tablet of 1000 mg at breakfast and 1 tablet of 1000 mg at supper. Patients with impaired renal function
Metformin Long can be used in patients with renal insufficiency of intermediate degree of severity (CKD 45-59 ml/min) only in case of absence of conditions that can increase risk of lactoacidosis. - The initial dose is 500 mg or 750 mg once daily. The maximum dose is 1000 mg per day divided into 2 doses. Renal function should be monitored closely (every 3-6 months). If the CK is lower than 45 ml/min, the drug should be stopped immediately.
- Elderly patients and patients with reduced renal function
For elderly patients, the dose is adjusted on the basis of renal function evaluation, which should be done regularly at least twice a year. - Duration of treatment course
The drug Metformin Long should be taken daily, without interruption. In case of discontinuation of treatment the patient should inform the physician. - Skipping a dose
If the next dose is missed, the next dose should be taken at the usual time. Do not take a double dose of the drug.
