Treatment
Table 1. Properties Of Currently Available Glucose-Lowering
Agents that may Guide Treatment Choice in Individual
Patients With T2DM
Cellular
Mechanism
Primary
Physiological
Action(s)
Class
Compound(s)
Biguanides
• Metformin
Activates
AMP-kinase
• ↓ Hepatic
glucose
production
Sulfonylureas
• 2nd generation
• Glyburide/
glibenclamide
• Glipizide
• Glimepiride
• Repaglinide
• Nateglinide
Closes KATP
channels on β-cell
plasma membranes
• ↑ Insulin
secretion
Closes KATP
channels on β-cell
plasma membranes
• ↑ Insulin
secretion
Thiazolidinediones
• Pioglitazone
• Rosiglitazoneb
Activates
the nuclear
transcription
factor PPAR-γ
• ↑ Insulin
sensitivity
α-Glucosidase
inhibitorsa
• Acarbose
• Miglitol
Inhibits intestinal
α-glucosidase
• Slows intestinal
carbohydrate
digestion/
absorption
DPP-4 inhibitors
• Sitagliptin
• Vildagliptina
• Saxagliptin
• Linagliptin
Inhibits DPP-4
activity, increasing
postprandial
active incretin
(GLP-1, GIP)
concentrations
Bile acid
sequestrantsa
• Colesevelam
Binds bile acids
in intestinal tract,
increasing hepatic
bile acid production;
? activation of
farnesoid X receptor
(FXR) in liver
• ↑ Insulin
secretion
(glucosedependent)
• ↓ Glucagon
secretion (glucosedependent)
• Unknown
• ? ↓ Hepatic
glucose
production
• ? ↑ Incretin
levels
Meglitinides
(glinides)
8
