Galvus
Galvus: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Galvus
ATX code: A10BH02
Active ingredient: vildagliptin (vildagliptin)
Producer: Novartis Pharma Stein (Switzerland), Novartis Farmaceutica (Spain)
Description and photo updated: 28.08.
Prices in pharmacies: from 672 rubles.
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Galvus is a dipeptidyl peptidase-4 inhibitor, an oral hypoglycemic drug.
Release form and composition
Dosage form - tablets: from light yellow to white, round, with beveled edges, with a smooth surface and NVR overprinting on one side, FB - on the other (7 pcs. Or 14 pcs. In a blister, in a cardboard box 2, 4, 8 or 12 blisters and instructions for the use of Galvus).
1 tablet contains:
- active substance: vildagliptin - 50 mg;
- auxiliary components: sodium carboxymethyl starch, anhydrous lactose, microcrystalline cellulose, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Vildagliptin - the active substance of Galvus, is a representative of the class of stimulants of the islet apparatus of the pancreas. The substance selectively inhibits the enzyme DPP-4 (dipeptidyl peptidase-4). Complete (> 90%) and rapid inhibition leads to an increase in basal and food-stimulated secretion of GLP-1 (glucagon-like peptide type 1) and GIP (glucose-dependent insulinotropic polypeptide) into the systemic circulation from the intestine throughout the day.
With an increase in the concentration of GLP-1 and GIP, the sensitivity of β-cells of the pancreas to glucose increases, which improves glucose-dependent insulin secretion.
In the case of using 50-100 mg of vildagliptin per day in patients with type 2 diabetes mellitus, there is an improvement in the function of β-cells of the pancreas. The effectiveness of therapy is determined by the degree of their initial damage. In individuals with normal plasma glucose concentration (without diabetes), vildagliptin does not stimulate insulin secretion and does not reduce glucose concentration. With an increase in the concentration of endogenous GLP-1, the sensitivity of β-cells to glucose increases, which causes an improvement in glucose-dependent regulation of glucagon secretion. A decrease in the increased concentration of glucagon during meals, in turn, leads to a decrease in insulin resistance.
With an increase in the insulin / glucagon ratio against the background of hyperglycemia, which is due to an increase in the concentration of GIP and GLP-1, a decrease in the production of glucose by the liver during / after a meal is noted. As a result, there is a decrease in the plasma concentration of glucose in the blood.
Taking vildagliptin helps to reduce the concentration of lipids in the blood plasma after a meal, while this effect is not associated with its effect on GLP-1 or GIP and improving the function of the islet cells of the pancreas.
It has been established that an increase in the concentration of GLP-1 can cause a slowdown in gastric emptying, but during therapy with vildagliptin, this effect is not observed.
According to the results of the studies, when using vildagliptin as monotherapy or in combination with metformin, sulfonylurea derivatives, thiazolidinedione or insulin in patients with type 2 diabetes, there is a significant prolonged decrease in the concentration of HbA1c (glycated hemoglobin) and fasting blood glucose.
When combined treatment with metformin as an initial therapy in patients with type 2 diabetes for 24 weeks, a dose-dependent decrease in the concentration of HbA1c was observed compared with monotherapy with these drugs. In both treatment groups, the incidence of hypoglycemia was minimal.
When 50 mg vildagliptin is used once a day for 6 months in patients with type 2 diabetes in the presence of moderate or severe renal function impairment (with a glomerular filtration rate ≥ 30 and <50 ml / min / 1.73 m 2 or <30 ml / min / 1.73 m 2, respectively), there was a clinically significant decrease in HbA1c concentration compared to placebo.
The incidence of hypoglycemia in the vildagliptin group is comparable to that in the placebo group.
Pharmacokinetics
Vildagliptin, when taken orally on an empty stomach, is rapidly absorbed, C max (maximum concentration of the substance) in blood plasma is reached in 1.75 hours. In the case of simultaneous intake with food, the rate of absorption of vildagliptin decreases slightly: there is a decrease in C max by 19%, while the time to reach it increases by 2.5 hours. However, food intake does not affect the degree of absorption and AUC (area under the concentration-time curve).
Vildagliptin is rapidly absorbed, and its absolute bioavailability is 85%. The C max and AUC values in the therapeutic dose range increase approximately in proportion to the dose.
The substance is characterized by a low degree of binding to blood plasma proteins (at the level of 9.3%). Vildagliptin is evenly distributed between erythrocytes and blood plasma. The distribution of the substance occurs, presumably, extravascular, V ss (volume of distribution in an equilibrium state) after intravenous administration is 71 liters.
The main route of elimination of vildagliptin is biotransformation, which is exposed to 69% of the dose. The main metabolite is LAY151 (57% of the dose). It does not exhibit pharmacological activity and is a product of the hydrolysis of the cyano component. About 4% of the dose undergoes amide hydrolysis.
During preclinical studies, a positive effect of DPP-4 on the hydrolysis of vildagliptin was established. Cytochrome P 450 isozymes do not take part in the metabolism of a substance. Vildagliptin is not a substrate of P 450 isoenzymes (CYP); cytochrome P 450 isoenzymes neither inhibit nor induce.
After taking vildagliptin inside, about 85% of the dose is excreted by the kidneys, through the intestines - about 15%. The renal excretion of unchanged substance is 23%. The average T 1/2 (half-life) for intravenous administration is 2 hours, renal clearance and total plasma clearance of vildagliptin are 13 and 41 l / h, respectively. T 1/2 after oral administration, regardless of the dose, is about 3 hours.
Pharmacokinetic features in patients with impaired liver function:
- mild and moderate severity (6-9 points on the Child-Pugh scale): after a single use of vildagliptin, there is a decrease in its bioavailability by 20% and 8%, respectively;
- severe degree (10-12 points on the Child-Pugh scale): the bioavailability of vildagliptin increases by 22%.
Changes (increase or decrease) in the maximum bioavailability of a substance in excess of 30% are considered clinically significant. There was no correlation between the bioavailability of vildagliptin and the severity of liver dysfunction.
Pharmacokinetic features in patients with mild, moderate or severe renal impairment (in comparison with healthy volunteers):
- AUC of vildagliptin: increases by 1.4; 1.7 and 2 times, respectively;
- AUC of the LAY151 metabolite: increases by 1.6; 3.2 and 7.3 times, respectively;
- AUC of the BQS867 metabolite: increases by 1.4; 2.7 and 7.3 times, respectively.
Limited information in end-stage CKD (chronic kidney disease) suggests that the indicators of this group are similar to those in patients with severe renal impairment. The concentration of the metabolite LAY151 in end-stage CKD increases 2–3 times compared with the concentration in patients with severe renal impairment.
With hemodialysis, the excretion of vildagliptin is limited (4 hours after a single dose is 3% with a procedure duration of more than 3-4 hours).
In elderly patients (over 65–70 years old), the maximum increase in the bioavailability of vildagliptin by 32%, C max - by 18% does not affect DPP-4 inhibition and is not clinically significant.
Pharmacokinetic features in patients under 18 years of age have not been established.
Indications for use
The use of Galvus is indicated for the treatment of type 2 diabetes mellitus while adhering to diet therapy and exercising:
- initial drug therapy in patients with insufficient effect from diet therapy and exercise - in combination with metformin;
- monotherapy indicated for patients with a contraindication to taking metformin or if it is ineffective - in the absence of a clinical effect from diet therapy and exercise;
- two-component combination therapy with metformin, thiazolidinedione, a sulfonylurea derivative or insulin - in the absence of a clinical effect from diet therapy, exercise and monotherapy with one of these drugs;
- triple combination therapy in combination with metformin and sulfonylurea derivatives - in the absence of adequate glycemic control after preliminary treatment with metformin and sulfonylurea derivatives against the background of diet therapy and exercise;
- triple combination therapy in combination with metformin and insulin - in the absence of adequate glycemic control after preliminary treatment with insulin and metformin against the background of diet therapy and exercise.
Contraindications
- type 1 diabetes mellitus;
- age up to 18 years;
- syndrome of glucose-galactose malabsorption, galactose intolerance, lactase deficiency;
- chronic heart failure IV functional class according to the NYHA functional classification (New York Heart Association);
- metabolic acidosis (diabetic ketoacidosis) in chronic or acute form (including in combination with or without coma);
- lactic acidosis (including history);
- liver dysfunction, including increased activity of liver enzymes [alanine aminotransferase (ALT) and aspartate aminotransferase (AST)] 3 or more times higher than the upper limit of normal;
- the period of pregnancy and breastfeeding;
- hypersensitivity to Galvus components.
It is recommended to use Galvus tablets with caution in case of a history of acute pancreatitis, end-stage chronic kidney disease (in patients undergoing hemodialysis or on hemodialysis), chronic heart failure class III according to the NYHA functional classification.
Galvus, instructions for use: method and dosage
Galvus tablets are taken orally, regardless of the meal.
The dose should be selected taking into account the individual efficacy and tolerability of the drug.
Recommended dosage:
- monotherapy or combination with thiazolidinedione, metformin or insulin: 50 mg 1-2 times a day, but not more than 100 mg;
- double combination therapy with sulfonylurea preparations: 50 mg once a day, in the morning. In patients of this category, the therapeutic effect of taking Galvus in a daily dose of 100 mg is identical to that of a dose of 50 mg per day;
- triple combination therapy with simultaneous intake of sulfonylurea derivatives and metformin: 100 mg per day.
If the daily dose is 50 mg, it is taken once, in the morning, if 100 mg - 50 mg each morning and evening. If you accidentally miss a dose, you should take it as soon as possible during the day. Do not allow Galvus to be taken in a dose exceeding the individual daily dose.
In the absence of sufficient glycemic control against the background of monotherapy at a maximum daily dose of 100 mg, treatment should be supplemented with the appointment of sulfonylurea derivatives, metformin, thiazolidinedione or insulin.
With mild to moderate renal dysfunction [creatinine clearance (CC) above 50 ml / min], the dose of Galvus is not changed.
With moderate (CC 30-50 ml / min) and severe (CC less than 30 ml / min) renal dysfunction, including end-stage chronic kidney disease (patients on hemodialysis or undergoing hemodialysis), the daily dose of Galvus is taken once, and it is not should exceed 50 mg.
Elderly patients (over 65 years of age) do not require Galvus dosage adjustment.
Side effects
The development of undesirable effects with monotherapy or in combination with other drugs in most cases is mild, temporary and does not require the abolition of Galvus.
The appearance of angioedema is most often observed in combination with angiotensin-converting enzyme inhibitors. Usually it is of moderate severity, it goes away on its own against the background of ongoing therapy.
Rarely, the use of Galvus causes hepatitis and other asymptomatic liver dysfunctions. In most cases, these conditions do not require drug treatment, and after the abolition of Galvus, liver function is restored.
An increase in the activity of hepatic enzymes at a dose of vildagliptin 50 mg 1-2 times a day in most cases is asymptomatic, does not progress and does not cause cholestasis or jaundice.
With monotherapy at a dose of 50 mg 1-2 times a day, the following adverse events may develop:
- from the nervous system: often - dizziness; infrequently - headache;
- parasitic and infectious pathologies: very rarely - nasopharyngitis, upper respiratory tract infections;
- from the side of the vessels: infrequently - peripheral edema;
- from the gastrointestinal tract: infrequently - constipation.
When you combine Galvus at a dose of 50 mg 1-2 times a day with metformin, the following side effects may occur:
- from the nervous system: often - headache, tremor, dizziness;
- from the gastrointestinal tract: often - nausea.
The combination therapy with metformin does not affect the patient's body weight.
When using Galvus in a daily dose of 50 mg in combination with sulfonylurea derivatives, the patient may experience the following pathologies:
- parasitic and infectious pathologies: very rarely - nasopharyngitis;
- from the gastrointestinal tract: infrequently - constipation;
- from the nervous system: often - headache, tremor, dizziness, asthenia.
The patient's weight does not increase when combined with glimepiride.
The use of Galvus at a dose of 50 mg 1-2 times a day in combination with thiazolidinedione derivatives can cause the following undesirable effects:
- from the side of the vessels: often - peripheral edema;
- on the part of metabolism and nutrition: often - an increase in body weight.
Taking Galvus at a dose of 50 mg 2 times a day in combination with insulin can cause:
- from the nervous system: often - headache; with an unknown frequency - asthenia;
- from the gastrointestinal tract: often - gastroesophageal reflux, nausea; infrequently - flatulence, diarrhea;
- from the side of metabolism and nutrition: often - hypoglycemia;
- general disorders: often - chills.
The patient's weight does not increase in this combination.
The use of Galvus 50 mg 2 times a day in combination with metformin and sulfonylurea preparations can lead to the development of the following side effects:
- from the side of metabolism and nutrition: often - hypoglycemia;
- from the nervous system: often - tremor, dizziness, asthenia;
- dermatological reactions: often - hyperhidrosis.
Triple combination therapy has no effect on the patient's body weight.
In addition, in post-registration studies, the following undesirable phenomena were recorded: urticaria, increased activity of liver enzymes, hepatitis, pancreatitis, skin lesions of bullous or exfoliative etiology, myalgia, arthralgia.
Overdose
When using up to 200 mg of vildagliptin per day, therapy is well tolerated.
In the case of Galvus application at a dose of 400 mg per day, the following symptoms may occur: muscle pain, rarely - fever, light / transient paresthesias, edema and transient increase in lipase activity (2 times higher than the upper limit of the norm).
With therapy in a daily dose of 600 mg, the appearance of edema of the extremities in combination with paresthesias and an increase in the activity of CPK (creatine phosphokinase), myoglobin and C-reactive protein, the activity of AST is possible.
All changes in laboratory parameters and symptoms of overdose are reversible and disappear after stopping therapy.
Elimination of vildagliptin from the body using dialysis is unlikely. The metabolite LAY151 can be removed from the body by hemodialysis.
special instructions
The patient should be informed about the need to consult a doctor if the listed side effects are aggravated or other undesirable effects appear during the use of tablets.
The drug does not cause impairment of fertility.
In insulin-dependent patients, Galvus should be used only in combination with insulin.
In case of chronic heart failure of class I according to the NYHA functional classification, the drug can be taken without restrictions in normal physical activity.
In chronic heart failure of the II class, moderate restriction of physical activity is required, since the usual load causes the patient to have a palpitations, weakness, shortness of breath, fatigue. At rest, these symptoms are absent.
If symptoms of acute pancreatitis appear, vildagliptin should be discontinued.
Before the start of use and then regularly every 3 months during the first year of therapy, it is recommended to conduct biochemical studies of liver function indicators, since the action of Galvus in rare cases can cause an increase in the activity of aminotransferases. If, upon re-examination, the activity indicators of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) exceed the upper limit of the norm by 3 times or more, the drug should be discontinued.
With the development of signs of liver dysfunction (including jaundice) while taking Galvus, an immediate discontinuation of the drug is required; it cannot be resumed after restoration of liver function indicators.
To reduce the risk of hypoglycemia in combination with sulfonylurea preparations, it is recommended to use them in the minimum effective dose.
Influence on the ability to drive vehicles and complex mechanisms
Patients in whom the reception of Galvus causes the development of dizziness should not drive vehicles or mechanisms.
Application during pregnancy and lactation
Galvus is not prescribed during pregnancy / lactation.
Pediatric use
For patients under 18 years of age, Galvus is contraindicated.
With impaired renal function
For patients with end-stage CKD who are on hemodialysis or undergoing hemodialysis, Galvus is prescribed with caution (experience with the drug is limited).
For violations of liver function
Patients with impaired hepatic function, including patients with increased activity of hepatic enzymes (ALT or AST 3 or more times higher than the upper limit of the norm), should not take Galvus.
Drug interactions
With the simultaneous use of Galvus with glibenclamide, metformin, pioglitazone, amlodipine, ramipril, digoxin, valsartan, simvastatin, warfarin, no clinically significant interaction has been established.
The hypoglycemic effect of vildagliptin may decrease when combined with thiazides, glucocorticosteroids, sympathomimetics, and thyroid hormone preparations.
The likelihood of developing angioedema increases with concomitant therapy with angiotensin-converting enzyme inhibitors. It should be noted that taking vildagliptin should be continued when angioedema appears, since it passes gradually, on its own and does not require discontinuation of therapy.
Interaction of Galvus with drugs that are substrates, inductors or inhibitors of cytochrome P 450 (CYP) is unlikely.
Galvus does not affect the metabolic rate of drugs that are substrates for the enzymes CYP1A2, CYP3A4, CYP3A5, CYP2C8, CYP2C9, CYP2D6, CYP2C19, CYP2E1.
Analogs
Galvus analogs are: Vildagliptin, Galvus Met.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C in a dark place.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Galvus
Reviews about Galvus are mostly positive. Subject to all the doctor's recommendations regarding diet therapy and exercise, taking the drug is effective in type 2 diabetes mellitus. A convenient dosing regimen is considered an important advantage.
Price for Galvus in pharmacies
The approximate price for Galvus (28 tablets) is 724–864 rubles.
Galvus: prices in online pharmacies
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Drug name Price Pharmacy |
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Galvus 50 mg tablets 28 pcs. RUB 672 Buy |
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Galvus Met 50 mg + 500 mg film-coated tablets 30 pcs. 998 RUB Buy |
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Galvus Met 50 mg + 1000 mg film-coated tablets 30 pcs. RUB 1100 Buy |
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Galvus Met 50 mg + 850 mg film-coated tablets 30 pcs. 1349 RUB Buy |
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Galvus met tab. p / o film. 50mg + 1000mg No. 30 1449 RUB Buy |
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Galvus met tab. p / o film. 50mg + 500mg No. 30 1471 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
