Galvus - instructions for use, reviews, analogs and formulations (tablets 50 mg, with metformin 50 + 500, 50 + 850, 50 + 1000 Mets) of a drug for the treatment of type 2 diabetes in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Galvus. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Galvus in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Galvusa in the presence of existing structural analogues. Use for the treatment of type 2 diabetes in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Galvus - oral hypoglycemic drug.Vildagliptin (active ingredient of Galvus) is a representative of the class of stimulants of the islet apparatus of the pancreas, selectively inhibits the enzyme dipeptidyl peptidase-4 (DPP-4). Rapid and complete inhibition of DPP-4 activity (more than 90%) causes an increase in both basal and food-stimulated secretion of glucagon-like peptide type 1 (GLP-1) and a glucose-dependent insulinotropic polypeptide (GIP) from the intestine to the systemic blood stream throughout the day.

Increasing concentrations of GLP-1 and HIP, vildagliptin causes an increase in the sensitivity of beta cells of the pancreas to glucose, which leads to an improvement in glucose-dependent secretion of insulin.

When using vildagliptin in a dose of 50-100 mg per day in patients with type 2 diabetes mellitus, there is an improvement in the function of β-cells of the pancreas. The degree of improvement in beta-cell function depends on the degree of their initial damage; so in individuals who do not have diabetes mellitus (with a normal level of glucose in the blood plasma), vildagliptin does not stimulate insulin secretion and does not reduce the level of glucose.

Increasing the concentration of endogenous GLP-1, vildagliptin increases the sensitivity of α-cells to glucose, which leads to an improvement in glucose-dependent regulation of glucagon secretion.Reducing the level of excess glucagon during meals, in turn, causes a decrease in insulin resistance.

An increase in the ratio of insulin / glucagon to a background of hyperglycemia, caused by an increase in the concentrations of GLP-1 and HIP, causes a decrease in glucose production in the liver both in the prandial period and after eating, which leads to a decrease in the concentration of glucose in the blood plasma.

In addition, against the background of the use of vildagliptin, there is a decrease in the level of lipids in the blood plasma, but this effect is not associated with its effect on GLP-1 or GIP and the improvement of beta-cell function of the pancreas.

It is known that an increase in the level of GLP-1 can lead to a slowdown in gastric emptying, but against the background of the use of vildagliptin, this effect is not observed.

Galvus Met is a combined oral hypoglycemic drug. The composition Galvus Met contains two hypoglycemic agents with different mechanisms of action: vildagliptin, belonging to the class of inhibitors of dipeptidyl peptidase-4, and Metformin (in the form of hydrochloride), a representative of the biguanide class. The combination of these components allows more effective control of the concentration of glucose in the blood in patients with diabetes mellitus2 types for 24 hours.

Composition

Vildagliptin + auxiliary substances (Galvus).

Vildagliptin + Metformin hydrochloride + excipients (Galvus Met).

Pharmacokinetics

Vildagliptin

When administered on an empty stomach, vildagliptin is rapidly absorbed. With simultaneous intake with food, the absorption rate of vildagliptin decreases slightly, but food intake does not affect the degree of absorption and AUC. The drug is distributed evenly between the plasma and erythrocytes. Biotransformation is the main way of removing vildagliptin. In the human body, a 69% dose of the drug is converted. After ingestion, about 85% of the dose is excreted by the kidneys and 15% by the intestine, while renal excretion of unchanged vildagliptin is 23%.

Sex, body mass index and ethnicity do not affect the pharmacokinetics of vildagliptin.

Pharmacokinetic features of vildagliptin in children and adolescents under the age of 18 years have not been established.

Metformin

Against the background of food intake, the degree and rate of metformin absorption are somewhat reduced. The preparation practically does not bind to plasma proteins, while sulfonylureas compounds bind to them more than 90%.Metformin penetrates into erythrocytes (probably the amplification of this process with time). With a single intravenous injection of healthy volunteers, metformin is excreted by the kidneys unchanged. At the same time, it is not metabolized in the liver (the person does not have any metabolites) and is not excreted with bile. When ingested, approximately 90% of the absorbed dose is excreted through the kidneys within the first 24 hours.

The sex of patients does not affect the pharmacokinetics of metformin.

Pharmacokinetic features of metformin in children and adolescents under the age of 18 years have not been established.

Vildagliptin + Metformin

The effect of food on the pharmacokinetics of vildagliptin and metformin in the composition Galvus Met did not differ from that for both drugs alone.

Indications

Diabetes mellitus type 2:

• as a monotherapy in combination with diet and exercise;
• in patients who previously received combination therapy with vildagliptin and metformin in the form of monopreparations (for Galvus Met);
• in combination with metformin as an initial drug therapy with insufficient effectiveness of diet and exercise;
• as part of a two-component combination therapy with metformin, sulfonylurea derivatives, thiazolidinedione or with insulin in the case of ineffectiveness of diet therapy, exercise and monotherapy of these drugs;
• as part of triple combination therapy: in combination with derivatives of sulfonylurea and metformin in patients previously treated with sulfonylureas and metformin derivatives against diet and exercise and who did not achieve adequate glycemic control;
• in the triple combination therapy: in combination with insulin and metformin in patients who previously received insulin and metformin against diet and exercise and who did not achieve adequate glycemic control.

Forms of release

Tablets 50 mg (Galvus).

The tablets covered with a cover 50 + 500 mg, 50 + 850 mg, 50 + 1000 mg (Galvus Met).

Instructions for use and dosing regimen

Galvus

Galvus is taken internally regardless of food intake.

Dosage regimen should be selected individually, depending on the effectiveness and tolerability.

The recommended dose of the drug during monotherapy or as part of a two-component combination therapy with metformin,thiazolidinedione or insulin (in combination with metformin or without metformin) is 50 mg or 100 mg per day. In patients with a more severe course of type 2 diabetes mellitus receiving insulin treatment, Galvus is recommended to be used at a dose of 100 mg per day.

The recommended dose of Galvus in combination therapy (vildagliptin + sulfonylurea derivatives + metformin) is 100 mg per day.

A dose of 50 mg per day should be given in one morning. A dose of 100 mg per day should be given 50 mg twice a day in the morning and evening.

When used as part of a two-component combination therapy with sulfonylurea derivatives, the recommended dose of Galvus is 50 mg once a day in the morning. When administered in combination with sulfonylurea derivatives, the efficacy of therapy with a drug at a dose of 100 mg per day was similar to that of a dose of 50 mg per day. If the clinical effect is insufficient, against the background of application of the maximum recommended daily dose of 100 mg for the better control of glycemia, it is possible to prescribe other hypoglycemic drugs: metformin, sulfonylureas, thiazolidinedione or insulin.

Patients with mild impairment of renal and hepatic function do not require correction of the dosing regimen of the drug. In patients with moderate or severe renal dysfunction (including the terminal stage of chronic renal failure on hemodialysis), the drug should be administered at a dose of 50 mg 1 time per day.

In elderly patients (more than 65 years), Galus dosage adjustment is not required.

Since the experience of using the drug in children and adolescents under the age of 18 does not, it is not recommended to use the drug in this category of patients.

Galvus Met

The drug is used inside. Dosage regimen Galvus Met must be selected individually, depending on the effectiveness and tolerability. When using Galvus Met, do not exceed the recommended maximum daily dose of vildagliptin (100 mg).

The recommended initial dose of the Galvus Met drug should be selected, taking into account the treatment regimens already used in the patient with vildagliptin and / or metformin. To reduce the severity of side effects from the digestive system, characteristic of metformin, Galvus Met is taken with meals.

The initial dose of Galvus Met with the ineffectiveness of monotherapy with vildagliptin: treatment with Galvus Med can be started with a single tablet of 50 mg / 500 mg twice a day, and after an evaluation of the therapeutic effect, the dose can be gradually increased.

The initial dose of Galvus Met with metformin monotherapy is ineffective: depending on the dose of metformin already taken, treatment with Galvus Met can be started with a single pill of 50 mg / 500 mg, 50 mg / 850 mg or 50 mg / 1000 mg twice a day.

The initial dose of Galvus Met in patients who previously received combination therapy with vildagliptin and metformin as separate tablets: depending on the doses of vildagliptin or metformin already taken, treatment with Galvus Meth should be started with the tablet as close as possible to the existing treatment of 50 mg / 500 mg , 50 mg / 850 mg or 50 mg / 1000 mg, and titrated by effect.

The initial dose of Galvus Met as an initial therapy in patients with type 2 diabetes with insufficient effectiveness of diet and exercise: as a starting therapy Galvus Met should be administered at an initial dose of 50 mg / 500 mg once a day and after evaluating the therapeutic effect gradually titrate the dose to 50 mg / 100 mg 2 times a day.

Combination therapy with Galvus Met together with sulfonylureas or insulin: the dose of Galvus Meth is calculated from the dose of vildagliptin 50 mg twice a day (100 mg per day) and metformin in a dose equal to that previously taken as a mono drug.

The use of Galvus Met is contraindicated in patients with renal insufficiency or with impaired renal function.

Metformin is excreted by the kidneys. Since patients with a history of over 65 years of age often have a decreased kidney function, this category of Galvus Met patients is prescribed at the lowest dose that provides normalization of glucose concentration, only after the determination of QC to confirm normal kidney function. When using the drug in patients older than 65 years, it is necessary to regularly monitor the kidney function.

Since the safety and efficacy of Galvus Meth in children and adolescents under the age of 18 have not been studied, the use of the drug is contraindicated in this category of patients.

Side effect

• headache;
• dizziness;
• tremor;
• chills;
• nausea, vomiting;
• gastroesophageal reflux;
• abdominal pain;
• diarrhea, constipation;
• flatulence;
• hypoglycemia;
• hyperhidrosis;
• fatigue;
• skin rash;
• hives;
• itching;
• arthralgia;
• peripheral edema;
• Hepatitis (reversible upon discontinuation of therapy);
• pancreatitis;
• localized skin peeling;
• blisters;
• decrease in absorption of vitamin B12;
• lactic acidosis;
• metallic taste in the mouth.

Contraindications

• renal failure or renal dysfunction: the level of blood serum creatinine above 1.5 mg% (more than 135 micromol / L) for men and more than 1.4 mg% (110 pmol / l) for women;
• acute conditions occurring at risk for renal dysfunction: dehydration (diarrhea, vomiting), fever, severe infectious disease, condition, hypoxia (shock, sepsis, kidney infections, bronchopulmonary diseases);
• acute and chronic heart failure, acute myocardial infarction, acute cardiovascular failure (shock);
• respiratory insufficiency;
• impaired liver function;
• Acute or chronic metabolic acidosis (including diabetic ketoacidosis in combination with or without coma). Diabetic ketoacidosis should be corrected by insulin therapy;
• laktatsidoz (including in the anamnesis);
• the drug is not prescribed for 2 days before surgery, radioisotope,X-ray studies with the introduction of contrast agents and within 2 days after their conduct;
• pregnancy;
• lactation period;
• type 1 diabetes mellitus;
• chronic alcoholism, acute alcohol poisoning;
• adherence to a hypocaloric diet (less than 1000 kcal per day);
• children under 18 years of age (efficacy and safety of use not established);
• increased sensitivity to vildagliptin or metformin or any other components of the drug.

Since patients with liver dysfunction in some cases had lactic acidosis, possibly one of the side effects of metformin, Galvus Met should not be used in patients with liver disease or liver biochemical indices.

With caution, it is recommended to use drugs containing metformin in patients over 60 years of age, as well as when performing heavy physical work in connection with the increased risk of lactic acidosis.

Application in pregnancy and lactation

Since there is no sufficient data on the use of Galvus or Galvus Met in pregnant women, the use of the drug in pregnancy is contraindicated.

If there is a violation of glucose metabolism in pregnant women, there is an increased risk of developing congenital anomalies, as well as the incidence of neonatal morbidity and mortality. To normalize blood glucose concentration during pregnancy, monotherapy with insulin is recommended.

In experimental studies with the appointment of vildagliptin in doses 200 times higher than recommended, the drug did not cause impairment of fertility and early development of the embryo and did not have a teratogenic effect on the fetus. When appointing vildagliptin in combination with metformin at a ratio of 1:10, there was also no teratogenic effect on the fetus.

Since it is not known whether vildagliptin or metformin is excreted in human milk, the use of Galvus during breastfeeding is contraindicated.

Use in children

Contraindicated in children and adolescents under the age of 18 years (efficacy and safety of use not established).

Application in elderly patients

Caution is advised to use drugs containing metformin in patients older than 60 years.

special instructions

In patients receiving insulin, Galvus or Galvus Met can not replace insulin.

Since the increase in aminotransferase activity (usually without clinical manifestations) with vildagliptin was noted somewhat more often than in the control group, it is recommended to determine the biochemical parameters of liver function before prescribing Galvus or Galvus Met, and also regularly during drug treatment. If the patient has an increased activity of aminotransferases, this result should be confirmed by a second study, and then regularly performed biochemical indices of liver function until they are normalized. If the excess of AST or ALT activity is 3 or more times higher than that of UGN is confirmed by repeated examination, it is recommended to cancel the drug.

Lactacidosis is a very rare but severe metabolic complication arising from the accumulation of metformin in the body. Lactacidosis in patients with metformin was mainly observed in patients with diabetes mellitus with renal insufficiency of high severity. The risk of developing lactic acidosis increases in patients with diabetes mellitus, which is difficult to treat,with ketoacidosis, prolonged starvation, long-term alcohol abuse, liver failure and diseases that cause hypoxia.

With the development of lactic acidosis, shortness of breath, abdominal pain and hypothermia, followed by a coma. The following laboratory indicators are of diagnostic value: a decrease in blood pH, a serum lactate concentration above 5 nmol / L, and an increased anion interval and an increased lactate / pyruvate ratio. When suspected of metabolic acidosis, the drug should be discontinued and the patient immediately hospitalized.

Since metformin is largely excreted by the kidneys, the risk of its accumulation and development of lactic acidosis is higher the more the renal function is more affected. When using Galvus Met, the renal function should be assessed regularly, especially in the following conditions that contribute to its disruption: the initial phase of treatment with antihypertensive drugs, hypoglycemic agents, or NSAIDs. As a rule, the kidney function should be evaluated before starting treatment with Galvus Met, and then at least once a year for patients with normal renal function and at least 2-4 times a year for patients with serum creatinine higher than UGN.In patients with a high risk of impaired renal function, it should be monitored more than 2-4 times a year. If there are signs of impaired renal function, Galvus Met should be discarded.

When carrying out X-ray studies that require intravascular injection of iodine-containing radiopaque agents, Galvus Met should be temporarily discontinued (48 hours before, and also within 48 hours after the study), because intravascular injection of iodine-containing radiopaque agents can lead to a sharp deterioration in kidney function and increase the risk development of lactic acidosis. Renewal of Galvus Met is possible only after a repeated assessment of renal function.

In acute cardiovascular insufficiency (shock), acute heart failure, acute myocardial infarction and other conditions for which hypoxia is characteristic, lactacidosis and prerenal acute renal failure may develop. If the above conditions occur, the drug should be immediately discontinued.

For the duration of surgical interventions (except for small surgeries not related to the restriction of food and liquid intake) Galvus Met should be canceled.You can resume taking the drug after the patient starts eating on his own and shows that the kidney function is not broken.

It is established that ethanol (alcohol) enhances the effect of metformin on the metabolism of lactate. Patients should be warned about the inadmissibility of alcohol abuse when using Galvus Met.

It was found that metformin in approximately 7% of cases causes an asymptomatic decrease in serum vitamin B12 concentration. Such a decrease in very rare cases leads to the development of anemia. Apparently, after the withdrawal of metformin and / or replacement therapy with vitamin B12, the serum concentration of vitamin B12 is quickly normalized. Patients receiving Galvus Met are recommended to perform a general blood test at least once a year and, if any violations are found, determine their cause and take appropriate measures. Apparently, in some patients (for example, in patients with insufficient intake or impaired absorption of vitamin B12 or calcium), there is a predisposition to lower serum vitamin B12 concentrations.In such cases, it may be recommended to determine the serum concentration of vitamin B12 at least once every 2-3 years.

If a patient with type 2 diabetes who previously responded to therapy showed signs of worsening (laboratory changes or clinical manifestations), and the symptoms are not clearly expressed, tests should be performed immediately to detect ketoacidosis and / or lactic acidosis. If acidosis is confirmed in one form or another, Galvus Met should be immediately abolished and appropriate measures taken.

Typically, patients receiving only Galvus Met, hypoglycemia is not noted, but it can occur against a low calorie diet (when the intense physical load is not compensated by the calorie content of food), or against the background of alcohol consumption. Hypoglycemia is most likely in elderly, debilitated or depleted patients, as well as against hypopituitarism, adrenal insufficiency or alcohol intoxication. In elderly patients and in patients receiving beta-adrenoblockers, the diagnosis of hypoglycemia may be difficult.

With stress (fever, trauma, infection,surgical intervention) that has arisen in a patient receiving hypoglycemic drugs using a stable scheme, possibly a sharp decrease in the effectiveness of the latter for some time. In this case, it may be necessary to cancel Galvus Met and prescribe insulin. You can resume treatment with Galvus Met after the end of the acute period.

Impact on the ability to drive vehicles and manage mechanisms

Effect of the drug Galvus or Galvus Met on the ability to drive vehicles and work with mechanisms has not been studied. With the development of dizziness against the background of the drug should be refrained from driving and working with mechanisms.

Drug Interactions

Vildagliptin + Metformin

With simultaneous application of vildagliptin (100 mg 1 time per day) and metformin (1000 mg once a day) there was no clinically significant pharmacokinetic interaction between them. Neither during clinical trials nor during extensive clinical use of the Galvus Meth preparation in patients receiving other concomitant medications and substances, there was no unforeseen interaction.

Vildagliptin

Vildagliptin has a low potential for drug interaction.Since vildagliptin is not a substratum of cytochrome P450 isoenzymes, nor does it inhibit or induce these isoenzymes, its interaction with drugs that are substrates, inhibitors or P450 inducers is unlikely. With simultaneous application of vildagliptin does not affect the metabolic rate of drugs that are substrates of enzymes: CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 / 5.

Clinical significant interaction between vildagliptin and drugs most commonly used in the treatment of type 2 diabetes mellitus (glibenclamide, pioglitazone, metformin) or having a narrow therapeutic range (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin) has not been established.

Metformin

Furosemide increases Cmax and AUC metformin, but does not affect its renal clearance. Metformin reduces Cmax and AUC of Furosemide and does not affect its renal clearance.

Nifedipine increases suction, Cmax and AUC of metformin; in addition, it increases the excretion of it with urine. Metformin practically does not affect the pharmacokinetic parameters of nifedipine.

Glibenclamide does not affect the pharmacokinetic / pharmacodynamic parameters of metformin.Metformin generally lowers Cmax and AUC of glibenclamide, but the magnitude of the effect varies greatly. For this reason, the clinical significance of this interaction remains unclear.

Organic cations, for example, amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, Vancomycin and others, excreted by the kidneys through tubular secretion, can theoretically interact with metformin, as they compete for common kidney tubule transport systems. Cimetidine increases both the concentration of metformin in plasma / blood, and its AUC by 60% and 40%, respectively. Metformin does not affect the pharmacokinetic parameters of cimetidine.

Care should be taken when using Galvus Met along with drugs that affect kidney function or the distribution of metformin in the body.

Some drugs may cause hyperglycemia and contribute to inefficiencies hypoglycemic agents for such preparations include thiazides and other diuretics, glucocorticosteroids (GCS), phenothiazines, hormones, thyroid medications, estrogen, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blockers, and isoniazid.In the appointment of such concomitant medications, or, on the contrary, in the event of their withdrawal, it is recommended to carefully monitor the effectiveness of metformin (its hypoglycemic effect) and, if necessary, adjust the dose of the drug.

It is not recommended simultaneous reception of danazol in order to avoid hyperglycemic action of the latter. If necessary, treatment with danazol and after stopping the latter requires a dose adjustment of metformin under the control of glucose levels.

Chlorpromazine, when taken in high doses (100 mg per day) increases glycemia, reducing the release of insulin. When treating with neuroleptics and after stopping the intake of the latter, correction of the dose of the drug under the control of glucose level is required.

Radiological study using iodine-containing radiocontrast agents can cause the development of lactic acidosis in patients with diabetes mellitus on the background of functional renal failure.

Prescribed as injections, beta2-sympathomimetics increase glycemia due to stimulation of beta2-adrenergic receptors. In this case, it is necessary to control glycemia.If necessary, the appointment of insulin is recommended.

With the simultaneous use of metformin with derivatives of sulfonylurea, insulin, acarbose, salicylates, hypoglycemic action may be increased.

Since the use of metformin in patients with acute alcohol intoxication increases the risk of developing lactic acidosis (especially during fasting, exhaustion or liver failure), patients with Galvus Meth should be refrained from drinking alcohol and drugs containing ethanol (alcohol).

Analogues of the drug Galvus

Structural analogs for the active substance:

• Galvus Met.

Analogues on the pharmacological group (hypoglycemic agents):

• Avandamet;
• Avandia;
• Arfazetine;
• Bagomet;
• Bethanase;
• Bukarban;
• Victoria;
• Glemaz;
• Glybenez;
• Glibenclamide;
• Glybometh;
• Glidiab;
• Glyclad;
• Gliclazide;
• Glimepiride;
• Gliminfor;
• Glitisol;
• Gliiformin;
• Glukobay;
• Glucobene;
• Gluconorm;
• Glucophage;
• Glucophage Long;
• Diabetolong;
• Diabeton;
• Diaglitazone;
• Diaformin;
• Langerin;
• Maninil;
• Meglymide;
• Metadiene;
• Metglybe;
• Metogamma;
• Metformin;
• Nova Met;
• Pioglit;
• Reclild;
• Roglit;
• Siofor;
• Sofamet;
• Subette;
• Tragenta;
• Formethine;
• Formina Pliva;
• Chloropropamide;
• Euglucon;
• Januvia;
• Yanumet.

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