vildagliptin
Drug group: blood sugar
Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vidagliptin subsequently acts by inhibiting the inactivation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) by DPP-4. This inhibitory activity ultimately results in a two-fold action where GLP-1 and GIP are present to potentiate the secretion of insulin by beta cells and suppress glucagon secretion by alpha cells in the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions
Mechanism of effect
Type-2 diabetes is a disease in which the pancreas does not make enough insulin to control the level of glucose (sugar) in the blood or when the body is unable to use insulin effectively. The active substance in Galvus, vildagliptin, is a dipeptidyl-peptidase-4 (DPP-4) inhibitor. It works by blocking the breakdown of ‘incretin’ hormones in the body. These hormones are released after a meal and stimulate the pancreas to produce insulin. By increasing levels of incretin hormones in the blood, vildagliptin stimulates the pancreas to produce more insulin when blood glucose levels are high. Vildagliptin does not work when the blood glucose is low. Vildagliptin also reduces the amount of glucose made by the liver, by increasing insulin levels and decreasing the levels of the hormone glucagon. Together, these processes reduce blood glucose levels and help to control type-2 diabetes
Pharmacodynamic
Absorption
Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%.
Half-life
The elimination half-life is approximately 90 minutes
Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%.
Half-life
The elimination half-life is approximately 90 minutes
Drug indications
Vildagliptin is indicated in the treatment of type-2 diabetes mellitus in adults:
as monotherapy:
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
as monotherapy:
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
Dosage
one tablet in the morning and another in the evening (100 mg per day), when used alone, with metformin, with a thiazolidinedione, with metformin plus a sulphonylurea, or with insulin (with or without metformin);
one tablet in the morning (50 mg per day) when taken with a sulphonylurea. A lower dose of the sulphonylurea may also be considered to reduce the risk of hypoglycaemia (low blood glucose levels).
The daily dose should not exceed two tablets (100 mg). In patients with moderate or severe kidney problems, the recommended dose is 50 mg once daily
one tablet in the morning (50 mg per day) when taken with a sulphonylurea. A lower dose of the sulphonylurea may also be considered to reduce the risk of hypoglycaemia (low blood glucose levels).
The daily dose should not exceed two tablets (100 mg). In patients with moderate or severe kidney problems, the recommended dose is 50 mg once daily
Alerts
Points of recommendation
The most common side effect with Galvus (seen in between 1 and 10 patients in 100) is dizziness. For the full list of all side effects reported with Galvus, including side effects occurring when Galvus is taken with other antidiabetes medicines, see the package leaflet
Galvus must not be used in people who are hypersensitive (allergic) to vildagliptin or any of the other ingredients
Because vildagliptin has been associated with liver problems, patients should have tests to check their liver function before treatment with Galvus and at regular intervals during treatment
Galvus must not be used in people who are hypersensitive (allergic) to vildagliptin or any of the other ingredients
Because vildagliptin has been associated with liver problems, patients should have tests to check their liver function before treatment with Galvus and at regular intervals during treatment
Drug forms
Galvus
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