Description

Simple

A once-daily medication used to lower blood sugar in people with diabetes.

Clinical

A once-daily dipeptidyl peptidase 4 (DPP-4) inhibitor used in the management of type 2 diabetes mellitus.

Overview

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.

Pharmacology

Indication

Used to reduce hyperglycemia in type 2 diabetes mellitus.

Pharmacodynamic

Vildagliptin belongs to a class of orally active antidiabetic drugs (DPP-IV inhibitors) that appear to have multiple functional benefits beyond simple blood-glucose control. One of these is a potential protective effect on pancreatic beta cells, which deteriorate in diabetes. Vildagliptin appears to... Read more

Mechanism of action

Vildagliptin inhibits dipeptidyl peptidase-4 (DPP-4). This in turn inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to potentiate the secretion of insulin in the beta cells. Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP and the degra... Read more

Absorption

Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%.

Protein binding

9.3%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

The elimination half-life is approximately 90 minutes.

Route of elimination

Information currently not available.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Vildagliptin is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinoline
The therapeutic efficacy of Vildagliptin can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Vildagliptin.
Acarbose
The risk or severity of hypoglycemia can be increased when Acarbose is combined with Vildagliptin.
Acebutolol
The therapeutic efficacy of Vildagliptin can be increased when used in combination with Acebutolol.
Acetazolamide
The therapeutic efficacy of Vildagliptin can be increased when used in combination with Acetazolamide.
Acetohexamide
Vildagliptin may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazole
The therapeutic efficacy of Vildagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acid
The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Vildagliptin.
Agmatine
The risk or severity of hypoglycemia can be increased when Agmatine is combined with Vildagliptin.
AICA ribonucleotide
The risk or severity of hypoglycemia can be increased when AICA ribonucleotide is combined with Vildagliptin.
Alaproclate
The risk or severity of hypoglycemia can be increased when Alaproclate is combined with Vildagliptin.
Albiglutide
The risk or severity of hypoglycemia can be increased when Vildagliptin is combined with Albiglutide.
Alclometasone
The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Vildagliptin.
Aldosterone
The risk or severity of hyperglycemia can be increased when Aldosterone is combined with Vildagliptin.
Allicin
The risk or severity of hypoglycemia can be increased when Vildagliptin is combined with Allicin.
Alogliptin
The risk or severity of angioedema can be increased when Vildagliptin is combined with Alogliptin.
Aloxiprin
Aloxiprin may increase the hypoglycemic activities of Vildagliptin.
Alprenolol
The therapeutic efficacy of Vildagliptin can be increased when used in combination with Alprenolol.
Alteplase
The risk or severity of angioedema can be increased when Alteplase is combined with Vildagliptin.
1 References
  1. 1 . Balas B, Baig MR, Watson C, Dunning BE, Ligueros-Saylan M, Wang Y, He YL, Darland C, Holst JJ, Deacon CF, Cusi K, Mari A, Foley JE, DeFronzo RA: The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab. 2007 Apr;92(4):1249-55. Epub 2007 Jan 23.PubMed: 17244786