Composition

Each tablet contains 50 mg vildagliptin.

Vildagliptin Biomed

Vildagliptin belongs to a group of medicines called oral antidiabetics, is used to treat patients with type 2 diabetes when it can not be controlled by diet and exercise alone. 

Vildagliptin works by making the pancreas produce more insulin and less glucagon. This helps to control the blood sugar level.

Mechanism of Action

Vildagliptin, is a potent and selective Dipeptidyl peptidase 4 inhibitor that rapidly and completely inhibit its activity, resulting in increased fasting and postprandial endogenous levels of the incretion hormones GLP-1 and GIP which enhances the sensitivity of beta cells to glucose, resulting in improved glucose-dependent insulin secretion. Treatment with vildagliptin significantly improve markers of beta cell function. Vildagliptin also enhances the sensitivity of alpha cells to glucose, which results in a decrease in fasting and postprandial hepatic glucose production, leading to reduced glycaemia.  

Absorption

Following oral administration in the fasting state, vildagliptin is rapidly absorbed, with peak plasma concentrations observed at 1.7 hours. Food slightly delays the time to peak plasma concentration to 2.5 hours, but does not alter the overall exposure (AUC). Administration of vildagliptin with food resulted in a decreased Cmax (19%). However, the magnitude of change is not clinically significant, so that Vildagliptin can be given with or without food. The absolute bioavailability is 85%.

Distribution

The plasma protein binding of vildagliptin is low (9.3%) and vildagliptin distributes equally between plasma and red blood cells.

Biotransformation

Metabolism is the major elimination pathway for vildagliptin, accounting for 69% of the dose. The major metabolite (LAY 151). DPP-4 contributes partially to the hydrolysis of vildagliptin. Vildagliptin is not metabolized by CYP 450 enzymes.

Elimination

Following oral administration of vildagliptin, approximately 85% of the dose was excreted into the urine and 15% of the dose is recovered in the faeces. Renal excretion of the unchanged vildagliptin accounted for 23% of the oral dose. The elimination half-life is approximately 3 hours.

Indications

Vildagliptin is indicated in the treatment of type 2 diabetes mellitus as dual oral therapy in combination with:

- Metformin, in patients with insufficient glycaemic control despite maximal tolerated dose of monotherapy with metformin,

- Sulphonylurea, in patients with insufficient glycaemic control despite maximal tolerated dose of a sulphonylurea and for whom metformin is inappropriate due to contraindications or intolerance,

- Thiazolidinedione, in patients with insufficient glycaemic control and for whom the use of a thiazolidinedione is appropriate.

Contraindications

Hypersensitivity to vildagliptin or to any of the other ingredients

Special populations

Renal impairment: In subjects with mild, moderate, or severe renal impairment, systemic exposure to vildagliptin was increased (Cmax 8-66%; AUC 32-134%) and total body clearance was reduced compared to subjects with normal renal function.

Pediatric: The use of Vildagliptin in children and adolescents is not recommended.

Special warnings and precautions

- Vildagliptin is not a substitute for insulin in insulin-requiring patients. Vildagliptin should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

- There is limited experience in patients with moderate to severe renal impairment or in patients with end-stage renal disease on haemodialysis. The use of Vildagliptin is not recommended in these patients.

- Vildagliptin should not be used in patients with hepatic impairment, including patients with pre-treatment (ALT) or (AST) > 3x the upper limit of normal. Patients who develop jaundice or other signs suggestive of liver dysfunction should discontinue Vildagliptin.

- Rare cases of hepatic dysfunction have been reported. Liver function tests should be performed prior to the initiation of treatment and during treatment at three-month intervals during the first year and periodically thereafter.

- Vildagliptin should be used cautiously in patients with congestive heart failure.

- Monitoring skin disorders, such as ulceration is recommended.

Drug Interactions

Cytochrome P450: Vildagliptin has a low potential for interactions with co-administered medicinal products. Vildagliptin is not likely to interact with active substances that are substrates, inhibitors or inducers of cytochrome P450 enzymes.

Combination with pioglitazone, metformin, glyburide, Digoxin, and warfarin: Results from studies conducted with these drugs have shown no clinically relevant pharmacokinetic interactions.

Combination with amlodipine, ramipril, valsartan or simvastatin: no clinically relevant pharmacokinetic interactions were observed after co-administration these drugs with vildagliptin.

Other interactions: As with other oral antidiabetic medicinal products the hypoglycaemic effect of vildagliptin may be reduced by: Thiazides, corticosteroids, thyroid products and sympathomimetics.

Pregnancy and lactation

Vildagliptin should not be used during pregnancy or lactation.

Effects on ability to drive and use machines

Patients who experience dizziness should avoid driving vehicles or using machines.

Side Effects

The majority of adverse reactions were mild and transient, not requiring treatment discontinuations.
Common: Tremor, headache, dizziness, fatigue, nausea, hypoglycemia, asthenia, peripheral edema, and weight increase.
Rare: Angioedema, (ALT) or (AST) elevations, Hepatic dysfunction (hepatitis). If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor.

Missed dosage

If you forget to take a dose of this medicine, take it as soon as you remember. Then take your next dose at the usual time. If it is almost time for your next dose, skip the dose you missed. Do not take a double dose to make up for a forgotten tablet.

Overdose

Information regarding overdose with vildagliptin is limited. At 400 mg, there were muscle pain, fever, oedema and a transient increase in lipase levels. At 600 mg, there were oedema of the feet and hands, and increases in: Creatine phosphokinase, (AST), C-reactive protein (CRP) and myoglobin levels. In the event of an overdose, supportive management is recommended. Vildagliptin cannot be removed by haemodialysis but the major hydrolysis metabolite (LAY 151) can be removed by haemodialysis.

Dosage and method of administration

(Vildagliptin is used in combination with either metformin or thiazolidinedione or sulphonylurea)  

Vildagliptin can be administered with or without a meal in the morning or in the morning and evening. Swallow the tablets whole with some water.

- When used in dual combination with metformin or a thiazolidinedione, the recommended daily dose of vildagliptin is 100 mg, administered as one dose of 50 mg in the morning and one dose of 50 mg in the evening.

- When used in dual combination with a sulphonylurea, the recommended dose of vildagliptin is 50 mg once daily administered in the morning.

- Do not stop taking Vildagliptin unless your doctor tells you to. Take Vildagliptin every day for as long as your doctor tells you.

- The safety and efficacy of vildagliptin as triple oral therapy in combination with metformin and a thiazolidinedione or with metformin and a sulphonylurea has not been established.

Presentation

Vildagliptin Biomed: box contains 30 tablets