Galvus 50mg tbl N28

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Manufacturer: Новартис
Рецептурный препарат
галвус 50мг тбл n28
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Brief information

Производитель

Новартис

Действующее вещество

Вилдаглиптин

The appearance of the product may differ from the photos on the site.

General description
Источник: РЛС

Composition

Pills 1 table.
active substance:  
vildagliptin 50 mg
excipients: MCC-95.68 mg; anhydrous lactose-47.82 mg; sodium carboxymethyl starch-4 mg; magnesium stearate-2.5 mg  

Description of the dosage form

Tablets: white to light yellow, round, smooth, with beveled edges, on one side marked NVR, on the other-FB.

Pharmacokinetics

Absorption. Vildagliptin is rapidly absorbed when ingested with an absolute bioavailability of 85%. In the therapeutic dose range, the increase in C max of vildagliptin in plasma and AUC is almost directly proportional to the increase in the dose of the drug.

After ingestion on an empty stomach, t max vildagliptin in blood plasma is 1 h 45 min. when taken with food, the absorption rate of the drug decreases slightly: there is a decrease from max by 19% and an increase in T max to 2 h 30 min. However, food intake does not affect the degree of absorption and AUC.

Distribution. The binding of vildagliptin to plasma proteins is low (9.3%). The drug is distributed equivalently between plasma and red blood cells. The distribution of vildagliptin is presumably extravascular, the V ss after I / V administration is 71 l.

Metabolism. Biotransformation is the main route of excretion of vildagliptin. In the human body, 69% of the drug dose is converted. The main metabolite — LAY151 (57% of the dose) - is pharmacologically inactive and is a product of hydrolysis of the cyanocomponent. About 4% of the drug dose is subjected to amide hydrolysis.

In experimental studies, there is a positive effect of DPP-4 on the hydrolysis of the drug. Vildagliptin is not metabolized with the participation of cytochrome P450 isoenzymes. Vildagliptin is not a substrate of CYP450 isoenzymes and does not inhibit or induce cytochrome P450 isoenzymes.

Breeding. After ingestion, about 85% of the dose is excreted by the kidneys and 15% - through the intestines, renal excretion of unchanged vildagliptin is 23%. T 1/2 after oral administration is about 3 hours regardless of the dose. Gender, body mass index, and ethnicity do not affect the pharmacokinetics of vildagliptin.

Special patient groups

Violation of liver function. In patients with mild to moderate hepatic impairment (6-10 points according to the child-Pugh classification), after a single application of the drug, there is a decrease in the bioavailability of vildagliptin by 20 and 8%, respectively. In patients with severe hepatic impairment (child-Pugh score 12), the bioavailability of vildagliptin is increased by 22%. An increase or decrease in the maximum bioavailability of vildagliptin not exceeding 30% is not clinically significant. There was no correlation between the severity of liver function disorders and the drug's bioavailability.

Impaired kidney function. In patients with mild, moderate, or severe renal impairment, the AUC of vildagliptin increased 1.4, 1.7, and 2 times, respectively, in comparison with healthy volunteers. The AUC of the LAY151 metabolite increased 1.6; 3.2; and 7.3 times, and the bqs867 metabolite increased 1.4; 2.7; and 7.3 times in patients with mild, moderate, and severe renal impairment, respectively. Limited data in patients with end-stage CPN indicate that the indicators of this group are similar to those in patients with severe renal impairment. The concentration of the metabolite LAY151 in patients with end-stage CPN increased 2-3 times compared with patients with severe renal impairment. When using the drug in patients with impaired renal function may require dose adjustment. Excretion of vildagliptin during hemodialysis is limited (4 hours after a single dose is 3% with the duration of the procedure more than 3-4 hours).

Patients ≥65 years old. The maximum increase in the bioavailability of the drug by 32% (an increase from max by 18%) in patients older than 70 years is not clinically significant and does not affect the inhibition of DPP-4.

Patients less than 18 years old. Pharmacokinetic features of vildagliptin in children and adolescents under 18 years of age have not been established.

Pharmacodynamics

Vildagliptin-a representative of the class of stimulators of the pancreatic islet apparatus, selectively inhibits the enzyme dipeptidylpeptidase-4 (DPP-4). Rapid and complete inhibition of DPP-4 activity (>90%) causes an increase in both basal and food-stimulated secretion of glucagon-like type 1 peptide (GPP-1) and glucose-dependent insulinotropic polypeptide (GIP) from the intestine into the systemic bloodstream throughout the day.

By increasing the concentration of GPP-1 and GIP, vildagliptin causes an increase in the sensitivity of pancreatic β-cells to glucose, which leads to an improvement in glucose-dependent insulin secretion.

When using vildagliptin at a dose of 50-100 mg/day in patients with type 2 diabetes mellitus (DM), there is an improvement in the function of pancreatic beta cells. The degree of improvement in the function of β-cells depends on the degree of their initial damage; so in people who do not suffer from DM (with normal plasma glucose concentration), vildagliptin does not stimulate insulin secretion and does not reduce glucose levels.

By increasing the concentration of endogenous GPP-1, vildagliptin increases the sensitivity of α-cells to glucose, which leads to improved glucose-dependent regulation of glucagon secretion. Reducing the increased concentration of glucagon during meals in turn causes a decrease in insulin resistance.

The increase in the ratio of insulin/glucagon with hyperglycemia due to increased levels of GLP-1 and GIP, causes a decrease in hepatic glucose production in the prandial period and after meals, reducing glucose concentration in the blood plasma.

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

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

When vildagliptin was used in 5795 patients with type 2 diabetes for 12 to 52 weeks as monotherapy or in combination with Metformin, sulfonylurea derivatives, thiazolidinedione or insulin, there was a significant long-term decrease in the concentration of glycated hemoglobin (HbA 1c ) and fasting blood glucose.

When using a combination of vildagliptin and Metformin as the initial therapy of patients with type 2 diabetes for 24 weeks, there was a dose-dependent decrease in HbA 1c and body weight in comparison with monotherapy with these drugs. Cases of hypoglycemia were minimal in both treatment groups.

In a clinical study in the application of vildagliptin at a dose of 50 mg 1 time a day for 6 months in patients with diabetes mellitus type 2 with impaired renal function moderate (glomerular filtration rate — GFR — ≥30, but <50 ml/min/1.73 m2) or severe (EGFR <30 ml/min/1.73 m2) to the degree noted a clinically significant reduction in HbA1c compared with the group receiving placebo.

In a clinical study, when using vildagliptin at a dose of 50 mg 2 times a day together with / without Metformin in combination with insulin (average dose of 41 UNITS/day) in patients with type 2 diabetes, there was a decrease in The HBA 1c index at the end point (-0.77%), with an initial indicator of an average of 8.8%. The difference with placebo (-0.72%) was statistically significant. The frequency of hypoglycemia in the study group was comparable to the frequency of hypoglycemia in the placebo group.

In a clinical study, when vildagliptin was administered at a dose of 50 mg 2 times a day simultaneously with Metformin (≥1500 mg / day) in combination with glimepiride (≥4 mg/day) in patients with type 2 diabetes, the HbA 1c index significantly decreased by 0.76% (the baseline average of 8.8%).

Indications of the drug

Type 2 diabetes:

as a monotherapy in combination with diet therapy and exercise;

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 insulin in case of inefficiency of diet therapy, exercise and monotherapy with these drugs;

as part of a triple combination therapy: in combination with sulfonylurea derivatives and Metformin, in patients previously treated with sulfonylurea derivatives and Metformin on the background of diet therapy and exercise and did not achieve adequate glycemic control;

as part of the triple combination therapy: in combination with insulin and Metformin, in patients who previously received insulin and Metformin, on the background of diet therapy and exercise and did not achieve adequate control of glycemia.

Contraindications

hypersensitivity to vildagliptin and any other components of the drug;

hereditary galactose intolerance, lactase deficiency glucose-galactose malabsorption.

It is not recommended to use vildagliptin in patients with chronic heart failure of functional class IV according to the NYHA classification due to the lack of clinical data on the use of vildagliptin in this group of patients.

The efficacy and safety of the drug in children under 18 years of age has not been established.

With caution: severe disturbances of liver function, including increased activity of hepatic enzymes (ALT or AST >2.5 times the ULN — 2.5 x ULN); end-stage chronic renal failure patients on hemodialysis (since application experience is limited); chronic heart failure III functional class classification NYHA (because data are limited and do not allow to draw a definitive conclusion).

Use during pregnancy and lactation

In experimental studies, when used in doses 200 times higher than recommended, the drug did not cause a violation of fertility and early development of the embryo and did not have a teratogenic effect on the fetus. Sufficient data on the use of the drug Galvus in pregnant women is not available, and therefore the drug should not be used during pregnancy.

Since it is not known whether vildagliptin is excreted in human breast milk, the drug Galvus should not be used during breastfeeding.

Dosage and administration

Inside, regardless of food intake.

The dosage regimen of the drug 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 it) - 50 or 100 mg once a day. In patients with more severe type 2 diabetes receiving insulin treatment, Galvus is recommended to be used at a dose of 100 mg/day.

The recommended dose of Galvus in the triple combination therapy (vildagliptin + sulfonylurea derivatives + Metformin) is 100 mg/day.

The dose of 50 mg / day should be taken 1 time in the morning, the dose of 100 mg/day should be divided into 2 doses of 50 mg in the morning and evening. If you skip the reception, the next dose of the drug should be taken as early as possible, and should not exceed the daily dose.

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 effectiveness of therapy with the drug at a dose of 100 mg/day was similar to that at a dose of 50 mg / day.

If there is insufficient clinical effect against the background of the maximum recommended daily dose of 100 mg for better control of glycemia, additional administration of other hypoglycemic drugs — Metformin, sulfonylurea derivatives, thiazolidinedione or insulin is possible.

Special patient groups

Impaired liver or kidney function. In patients with mild renal and hepatic impairment, correction of the dosage regimen is not required. In patients with moderate to severe renal impairment (including end-stage CPN on hemodialysis), the drug should be used at a dose of 50 mg 1 time per day.

Patients ≥65 years old. Elderly patients do not need to adjust the dosage regimen of the drug Galvus.

Use in patients less than 18 years of age. Since there is no experience of using the drug Galvus in children and adolescents under 18 years of age, it is not recommended to use the drug in this category of patients.

Side effect

When using the drug Galvus as monotherapy or in combination with other drugs, most of the adverse reactions were mild, had a temporary nature and did not require discontinuation of therapy. No correlation was found between the frequency of adverse events (NYA) and age, gender, ethnicity, duration of use, or dosage regimen.

The incidence of angioedema during treatment with Galvus was ≥1/10000, Angioedema was most often observed when the drug was used in combination with ACE inhibitors. In most cases, angioedema was of moderate severity and resolved independently during the continuation of therapy with vildagliptin.

Against the background of therapy with Galvus, liver function disorders (including hepatitis) of an asymptomatic course were rarely observed. In most cases, these violations and deviations of liver function indicators from the norm were resolved independently without complications after discontinuation of therapy with the drug. When using the drug Galvus at a dose of 50 mg 1 or 2 times a day, the frequency of increase in the activity of liver enzymes (ALT or AST ≥3×VGN) was 0.2 or 0.3%, respectively (compared with 0.2% in the control group). The increase in liver enzyme activity in most cases was asymptomatic, did not progress and was not accompanied by cholestasis or jaundice.

The following criteria were used to estimate the frequency of NYA: very often (≥1/10); often (≥1/100, <1/10); infrequently (≥1/1000, <1/100); rarely (≥1/10000, <1/1000); very rarely (

Use of the drug Galvus as monotherapy

When using the drug Galvus at a dose of 50 mg 1 or 2 times a day, the frequency of discontinuation of therapy due to the development of adverse reactions (0.2 or 0.1%, respectively) was not higher than that in the placebo group (0.6%) or the comparison drug (0.5%).

Against the background of monotherapy with Galvus at a dose of 50 mg 1 or 2 times a day, the incidence of hypoglycemia without increasing the severity of the condition was 0.5% (2 patients out of 409) or 0.3% (4 out of 1082), which is comparable to the comparison drug and placebo (0.2%). When using the drug Galvus in the form of monotherapy, there was no increase in body weight of patients.

From the Central nervous system: often-dizziness; infrequently-headache.

From the digestive system: infrequently-constipation.

General disorders and disorders at the site of administration: infrequently-peripheral edema.

Long-term clinical studies lasting up to 2 years did not reveal any additional deviations in the safety profile or unforeseen risks when using vildagliptin as monotherapy.

Use of the drug Galvus in a dose of 50 mg 1 or 2 times a day in combination with Metformin

When using the drug Galvus at a dose of 50 mg 1 time per day in combination with Metformin, the frequency of discontinuation of therapy due to the development of adverse reactions was 0.4% (in the groups vildagliptin (50 mg 2 times a day) + Metformin and placebo + Metformin, there were no cases of discontinuation of therapy due to the development of adverse reactions).

When using the drug Galvus at a dose of 50 mg 1 or 2 times a day in combination with Metformin, hypoglycemia was observed in 0.9 and 0.5% of cases, respectively (in the placebo + Metformin group-0.4%). No severe hypoglycemia was observed in the Galvus group. Combination therapy vildagliptin + Metformin did not affect the body weight of patients.

From the nervous system: often-tremor, dizziness, headache.

Long-term clinical studies lasting up to 2 years have not revealed any additional safety profile deviations or unforeseen risks when using vildagliptin in combination with Metformin.

When using the drug Galvus at a dose of 50 mg 1 time a day in combination with sulfonylurea derivatives

When using the drug Galvus at a dose of 50 mg once a day in combination with glimepiride, the frequency of discontinuation of therapy due to the development of adverse reactions was 0.6% (compared with 0% in the glimepiride + placebo group).

The incidence of hypoglycemia in patients treated with Galvus at a dose of 50 mg once a day with glimepiride was 1.2% (compared with 0.6% in the placebo + glimepiride group). No severe hypoglycemia was observed in the Galvus group.

When using the drug Galvus in the recommended dose (50 mg 1 time per day) in combination with glimepiride, there was no increase in body weight of patients.

From the nervous system: often-tremor, dizziness, headache.

General disorders and disorders at the site of administration: often-asthenia.

When using the drug Galvus at a dose of 50 mg 1 or 2 times a day in combination with thiazolidinedione derivatives

When using the drug Galvus at a dose of 50 mg once a day in combination with pioglitazone, the frequency of discontinuation of therapy due to the development of adverse reactions was 0.7% (in the groups vildagliptin (50 mg 2 times a day) + pioglitazone and placebo + pioglitazone, cases of discontinuation of therapy due to the development of adverse reactions were not noted).

In applying the drug Galvus dose 50 mg 1 times / day in combination with pioglitazone at a dose of 45 mg were observed hypoglycemia; group vildagliptin (dose 50 mg 2 times a day) + pioglitazone (at a dose of 45 mg) was observed hypoglycemia in 0.6% of cases, and in patients receiving placebo + pioglitazone at a dose of 45 mg, 1.9% of cases. No severe hypoglycemia was observed in the Galvus group. The average increase in body weight compared to placebo in patients receiving Galvus at a dose of 50 mg 1 or 2 times a day with pioglitazone was + 0.1 or + 1.3 kg, respectively. When adding the drug Galvus at a dose of 50 mg 1 or 2 times a day to pioglitazone at a dose of 45 mg/day, the frequency of peripheral edema was 8.2 and 7%, respectively (compared with 2.5% on the background of pioglitazone monotherapy). However, when the initial combination therapy with vildagliptin at a dose of 50 mg 1 or 2 times a day with pioglitazone at a dose of 45 mg / day, the development of peripheral edema was observed in 3.5 or 6.1% of patients, respectively (compared with 9.3% against the background of pioglitazone monotherapy at a dose of 30 mg/day).

General disorders and disorders at the site of administration: often-peripheral edema.

Laboratory and instrumental data: often — the increase in body weight.

When using the drug Galvus at a dose of 50 mg 2 times a day in combination with insulin

When using the drug in combination with insulin (in combination with Metformin or without Metformin), the frequency of cancellation of therapy due to the development of side effects was equal to 0.3% in the group of vildagliptin therapy, in the placebo group there were no cases of cancellation of therapy.

When using the drug in combination with insulin (in combination with Metformin or without Metformin), there was no increase in the risk of hypoglycemia compared to the placebo + insulin combination (14% in the vildagliptin group and 16.4% in the placebo group). 2 patients in the vildagliptin group and 6 patients in the placebo group developed severe hypoglycemia.

At the time of completion of the study, the drug had no effect on the average body weight (body weight increased by + 0.6 kg compared to the baseline in the vildagliptin group, and in the placebo group, no changes were noted).

When using vildagliptin 50 mg 2 times a day in combination with insulin (with or without Metformin)

From the nervous system: often-headache.

From the gastrointestinal tract: often-nausea, GERD; infrequently-diarrhea, flatulence.

General disorders and disorders at the site of administration: often-chills.

Laboratory and instrumental data: often-hypoglycemia.

When using Galvus in combination with sulfonylureas and Metformin

There were no cases of drug withdrawal associated with NSAIDS in the combination therapy group with vildagliptin, Metformin, and glimepiride. In the group of combined therapy with placebo, Metformin and glimepiride, the frequency of NYA was 0.6%.

Hypoglycemia was observed frequently in both groups (5.1% in the combination therapy group with vildagliptin, Metformin and glimepiride, and 1.9% in the combination therapy group with placebo, Metformin and glimepiride). One episode of severe hypoglycemia was observed in the vildagliptin group.

At the end of the study, there was no significant effect on body weight (+0.6 kg in the vildagliptin group and -0.1 kg in the placebo group).

When using vildagliptin 50 mg 2 times a day in combination with Metformin and sulfonylureas

From the nervous system: often-dizziness, tremor.

General disorders and disorders at the site of administration: often-fatigue.

From the side of metabolism and nutrition: often-hypoglycemia.

From the skin and subcutaneous tissues: often-hyperhidrosis.

Post-marketing research

During post-marketing studies, the following adverse reactions were identified (since \ t reports were received voluntarily from a population of undetermined size, it is not possible to reliably determine the frequency of these NYA, and therefore they are classified as an unknown frequency): hepatitis (reversible upon discontinuation of therapy), urticaria, pancreatitis, local skin peeling or blistering.

If any of the side effects listed in the description are aggravated or the patient has noticed any other side effects not listed in the description, you should inform your doctor.

Interaction

The drug Galvus has a low potential for drug interaction.

Since the drug is not a substrate of cytochrome P450 enzymes, and does not inhibit or induce these enzymes, the interaction of the drug Galvus with drugs that are substrates, inhibitors or inducers of cytochrome P450 is unlikely. When used simultaneously, vildagliptin also does not affect the rate of metabolism of drugs that are substrates of the enzymes CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4/5.

Clinically significant interaction of the drug Galvus with drugs most commonly used in the treatment of type 2 diabetes (glibenclamide, pioglitazone, Metformin) or having a narrow therapeutic range (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin) has not been established.

Overdose

The drug Galvus is well tolerated when administered at a dose of up to 200 mg/day.

Symptoms: when using the drug at a dose of 400 mg/day, muscle pain may be observed, rarely-light and transient paresthesia, fever, edema and transient increase in the concentration of lipase (above VGN 2 times). If the dose of Galvus is increased to 600 mg/day, it is possible to develop edema of the limbs with paresthesias and an increase in the concentration of ck, ALT, C-reactive protein and myoglobin. All symptoms of overdose and changes in laboratory parameters disappear after discontinuation of the drug.

Treatment: elimination of the drug from the body using dialysis is unlikely. However, the main hydrolytic metabolite of vildagliptin (LAY151) can be removed from the body by hemodialysis.

Special instruction

Heart failure

Since data on the use of vildagliptin in patients with functional class III CHF according to the NYHA classification (see table 1) are limited and do not allow to draw a final conclusion, it is recommended to use Galvus with caution in this category of patients.

It is not recommended to use vildagliptin in patients with functional class IV CHF according to the NYHA classification due to the lack of clinical data on its use in this group of patients.

Table 1

NYHA classification of functional status of patients with CHF (modified), 1964

\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t\t
Functional class Restriction of physical activity and clinical manifestations
I There are no restrictions on physical activity. Normal physical activity does not cause severe fatigue, weakness, shortness of breath or palpitations
II Moderate restriction of physical activity. At rest, there are no pathological symptoms. Normal physical activity causes weakness, fatigue, palpitations, shortness of breath, and other symptoms
III Severe restriction of physical activity. The patient feels comfortable only at rest, but the slightest physical activity leads to weakness, palpitations, shortness of breath and other symptoms
IV The inability to perform any load without causing discomfort. Symptoms of heart failure are present at rest and increase with any physical activity

Impaired liver function

Because in rare cases, when using vildagliptin was marked elevation of transaminases (usually without clinical manifestations), the appointment of a drug Galvus, and regularly during the first year of treatment (1 every 3 months) is recommended to determine the biochemical indicators of liver function. If the patient has an increased activity of aminotransferases, this result should be confirmed by repeated research, and then regularly determine the biochemical parameters of liver function until they are normalized. If the excess activity of AST or ALT to 3×VGN confirmed by repeated research, the drug is recommended to cancel.

If jaundice or other signs of liver dysfunction develop while using Galvus, therapy with The drug should be stopped immediately. After normalization of liver function indicators, treatment with the drug can not be resumed. If necessary, insulin therapy drug Galvus is used only in combination with insulin.

The drug should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

Influence on the ability to drive vehicles and / or work with mechanisms. The effect of the drug Galvus on the ability to drive vehicles or work with mechanisms has not been established. If dizziness develops during treatment with the drug, patients should not drive vehicles or work with mechanisms.

Form release

Tablets, 50 mg. in a blister, 7 or 14 PCs. 2, 4, 8, 12 BL. in a cardboard.

Conditions of supply of pharmacies

By prescription.

Manufacturer

1. Novartis Pharma Stein AG, Switzerland.

2. Novartis Pharmaceuticals S. A., Spain.

Registration certificate holder: Novartis Pharma AG. 35 Lichtstrasse, 4056 Basel, Switzerland.

Additional information about the drug can be obtained at: 125315, Moscow, Leningradsky Ave., 72, korp. 3.

Tel: (495) 967-12-70; Fax: (495) 967-12-68.

In the case of packaging in the Russian Federation, it is indicated: packing/packaging/producing quality control: CJSC ORTAT. Russia.

The appearance of the product may differ from the photos on the site.

Information about prescription drugs is for professionals only. The information provided should not be used by patients to make an independent decision on the use of the presented drugs and cannot serve as a substitute for a full-time consultation with a doctor.

A description of the active substances of the drug is provided. The scientific information provided is generalized and cannot be used to decide on the possibility of using a specific drug.

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