- Antidiabetic agents
- Pharmaceutical Form : Tablets
- Composition : vildagliptin 50 mg /Tab
- Active Substance : vildagliptin
Mechanism of action :
The administration of vildagliptin results in a rapid and complete inhibition of DPP-4 activity, resulting in increased fasting and postprandial endogenous levels of the incretin hormones GLP-1 (glucagon-like peptide 1) and GIP (glucose-dependent insulinotropic polypeptide).
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. Administration of vildagliptin with food resulted in a decreased Cmax (19%). The absolute bioavailability is 85%.
Metabolism is the major elimination pathway for vildagliptin in humans, accounting for 69% of the dose.
Distribution: The plasma protein binding of vildagliptin is low (9.3%) and vildagliptin distributes equally between plasma and red blood cells.
Elimination: approximately 85% of the dose was excreted into the urine and 15% of the dose is recovered in the faeces.
Vildagliptin is indicated in the treatment of type 2 diabetes mellitus in adults:
– in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance.
As dual oral therapy in combination with:
– metformin, in patients with insufficient glycaemic control despite maximal tolerated dose of monotherapy with metformin.
– a 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.
– a thiazolidinedione, in patients with insufficient glycaemic control and for whom the use of a thiazolidinedione is appropriate.
As triple oral therapy in combination with:
– a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
-Vildagliptin is also indicated for use in combination with insulin (with or without metformin) when diet and exercise plus a stable dose of insulin do not provide adequate glycaemic control.
Hypersensitivity to the active substance or to any of the excipients.
General: 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.
Renal impairment: Vildagliptin should be used with caution in these patients.
Hepatic impairment: Vildagliptin should not be used in patients with hepatic impairment
Liver enzyme monitoring: Rare cases of hepatic dysfunction (including hepatitis) have been reported.
Liver function tests should be performed prior to the initiation of treatment with Vildagliptin in order to know the patient’s baseline value.
Liver function should be monitored during treatment with Vildagliptin at three-month intervals during the first year and periodically thereafter.
Patients who develop jaundice or other signs suggestive of liver dysfunction should discontinue Vildagliptin.
Cardiac failure: A clinical trial of vildagliptin showed that treatment with vildagliptin was not associated with a change in left-ventricular function or worsening of pre-existing congestive heart failure (CHF) versus placebo.
Skin disorders: Skin lesions, including blistering and ulceration have been reported in extremities of monkeys in non-clinical toxicology studies. In keeping with routine care of the diabetic patient, monitoring for skin disorders, such as blistering or ulceration, is recommended.
Pancreatitis: In post-marketing experience there have been reported adverse reactions of acute pancreatitis.
Patients should be informed of the characteristic symptom of acute pancreatitis: persistent, severe abdominal pain.
Resolution of pancreatitis has been observed after discontinuation of vildagliptin.
If pancreatitis is suspected, vildagliptin and other potentially suspect medicinal products should be discontinued.
Hypoglycemia: Sulphonylureas are known to cause hypoglycemia. Patients receiving vildagliptin in combination with a sulphonylurea may be at risk for hypoglycemia. Therefore, a lower dose of sulphonylurea may be considered to reduce the risk of hypoglycemia.
As monotherapy: Hypoglycaemia, Dizziness, Headache, Vascular disorder, Oedema peripheral, Constipation, and Arthralgia.
In combination with Metformin: Hypoglycaemia, Tremor, Headache, Dizziness, Fatigue, Nausea.
In combination with a sulphonylurea: Nasopharyngitis, Hypoglycaemia, Tremor, Headache, Dizziness, Asthenia, Constipation.
In combination with thiazolidinedione: Weight increase, Hypoglycaemia, Headache, Asthenia, Oedema peripheral.
In combination with metformin and a sulphonylurea: Hypoglycaemia, Dizziness, tremor, Hyperhidrosis, Asthenia.
In combination with insulin (with or without metformin): Decreased blood glucose, Headache, chills, Nausea, gastro-oesophageal reflux disease, Diarrhoea, flatulence.
Vildagliptin has a low potential for interactions with co-administered medicinal products.
Combination with pioglitazone, metformin and glyburide:
Results from studies conducted with these oral antidiabetics have shown no clinically relevant pharmacokinetic interactions.
Clinical studies performed with healthy subjects have shown no clinically relevant pharmacokinetic interactions.
Combination with amlodipine, ramipril, valsartan or simvastatin:
Drug-drug interaction studies in healthy subjects were conducted with amlodipine, ramipril, valsartan and simvastatin. In these studies, no clinically relevant pharmacokinetic interactions were observed after co-administration with vildagliptin.
Combination with ACE-inhibitors:
There may be an increased risk of angioedema in patients concomitantly taking ACE-inhibitors.
As with other oral antidiabetic medicinal products the hypoglycaemic effect of vildagliptin may be reduced by certain active substances, including thiazides, corticosteroids, thyroid products and sympathomimetics.
Pregnancy: Due to lack of data, vildagliptin should not be used during pregnancy.
Breast-feeding: It is unknown whether vildagliptin is excreted in human milk.
Vildagliptin should not be used during breast-feeding.
Dosage and administrations:
Adults: When used as monotherapy, in combination with metformin, in combination with thiazolidinedione, in combination with metformin and a sulphonylurea, or in combination with insulin (with or without metformin) the recommended daily dose of vildagliptin is 100mg, 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 50mg once daily administered in the morning. In this patient population, vildagliptin 100mg daily was no more effective than vildagliptin 50mg once daily.
When used in combination with a sulphonylurea, a lower dose of the sulphonylurea may be considered to reduce the risk of hypoglycaemia.
Doses higher than 100mg are not recommended.
If a dose of vildagliptin is missed, it should be taken as soon as the patient remembers. A double dose should not be taken on the same day.
The safety and efficacy of vildagliptin as triple oral therapy in combination with metformin and a thiazolidinedione have not been established.
Elderly (≥ 65 years):
No dose adjustments are necessary in elderly patients.
Renal impairment: No dose adjustment is required in patients with mild renal impairment (creatinine clearance ≥ 50 ml/min).
In patients with moderate or severe renal impairment, the recommended dose of vildagliptin is 50 mg once daily.
Hepatic impairment: vildagliptin should not be used in patients with hepatic impairment.
Pediatric population: vildagliptin not recommended for use in children and adolescents (< 18 years).
Vildagliptin can be administered with or without a meal.
Do not store above 30˚c, protect from moisture.
Store in original package.
Packaging: Pack contains 30 tablets