. 2010 May 5;690:29–51. doi: 10.1007/978-90-481-9060-7_3

Table 3.4.

Currently and potentially used oral hypoglycemic medications and proposed mechanisms for the management of T2DM

Major class of drugs	Site of actions and proposed mechanisms	Some specific drugs
β-cell secretagogues
Sulfonylureas	• Act on the pancreas • Enhance β-cell secretion by acting on the ATP-dependent potassium channel • Use with or without insulin but hypoglycemia	– Tolbutamide Glipizide Meglitinides Nateglinide – Exenatide, Liraglutide; – Sitagliptin, Vidagliptin;
GLP-1 analogues/DPP-IV inhibitors/Amylin analogue	• Act on the pancreas • Enhance β-cell secretion and/or cell mass • Do not cause weight gain but GI side effects	– Synthetic amylin
α-glucosidase inhibitors	• Act on the gastrointestinal tract • Lower blood glucose by delaying the digestion and absorption of carbohydrates • Do not cause weight gain and hypoglycemia but concomitant with gas, bloating and diarrhea	– Acarbose – Miglitol
Insulin sensitizers
Biguanides	• Act primarily on the liver • Decrease liver’s glucose production and slightly increase muscle glucose uptake • Do not cause weight gain and hypoglycemia while inducing nausea, diarrhea or loss of appetite	– Metformin – Metformin (extended release) – Metformin (liquid)
Thiazolidinediones (TZDs)	• Act on the peripheral tissues • Decrease insulin resistance at the muscle & liver levels • Improve cholesterol and triglyceride status while but cause weight gain	– Pioglitazone – Rosiglitazone – Troglitazone
RAS blockers	• Act on the pancreas and the peripheral tissues • Improve β-cell function, structure and/or insulin resistance	– ACEIs (Ramipril) – ARBs (Losartan, Valsartan)
Combination drugs	• Act on different tissue-organ levels • Potential advantages and disadvantages for each drug in the combination listed separately above	– Metformin + TZD, – Metformin + DPP-IV inhibitor, – TZD + Sulfonylurea

Major class of drugs

Site of actions and proposed mechanisms

Some specific drugs

β-cell secretagogues

Sulfonylureas

• Act on the pancreas

• Enhance β-cell secretion by

acting on the ATP-dependent

potassium channel

• Use with or without insulin

but hypoglycemia

– Tolbutamide

Glipizide

Meglitinides

Nateglinide

– Exenatide, Liraglutide;

– Sitagliptin, Vidagliptin;

GLP-1 analogues/DPP-IV inhibitors/Amylin analogue

• Act on the pancreas

• Enhance β-cell secretion

and/or cell mass

• Do not cause weight gain but

GI side effects

– Synthetic amylin

α-glucosidase inhibitors

• Act on the gastrointestinal

tract

• Lower blood glucose by

delaying the digestion and

absorption of carbohydrates

• Do not cause weight gain and

hypoglycemia but

concomitant

with gas, bloating and

diarrhea

– Acarbose

– Miglitol

Insulin sensitizers

Biguanides

• Act primarily on the liver

• Decrease liver’s glucose

production and slightly

increase muscle glucose

uptake

• Do not cause weight gain and

hypoglycemia while inducing

nausea, diarrhea or loss of

appetite

– Metformin

– Metformin (extended release)

– Metformin (liquid)

Thiazolidinediones

(TZDs)

• Act on the peripheral tissues

• Decrease insulin resistance at

the muscle & liver levels

• Improve cholesterol

and triglyceride status while

but cause weight gain

– Pioglitazone

– Rosiglitazone

– Troglitazone

RAS blockers

• Act on the pancreas and the

peripheral tissues

• Improve β-cell function,

structure and/or insulin

resistance

– ACEIs (Ramipril)

– ARBs

(Losartan, Valsartan)

Combination drugs

• Act on different tissue-organ

levels

• Potential advantages and

disadvantages for each drug

in the combination listed

separately above

– Metformin + TZD,

– Metformin + DPP-IV

inhibitor,

– TZD + Sulfonylurea

RAS, Renin-angiotensin system; ACEIs, Angiotensin-converting enzyme inhibitors; ARBs, Angiotensin receptor blockers; GLP-1, Glucagon-like peptide-1; DPP-IV, Dipeptidyl peptidase IV.