Mechanisms of Action of Antidiabetic Drugs

Question 1

Meglitinides

Answer 1

Bind to the ATP-dependent K+(KATP) channel on pancreatic beta cells, leading to increased insulin secretion.
Hypoglycaemia.
e.g. repaglinide, nateglinide

Question 2

DPP4 inhibitors

Answer 2

Inhibit the enzyme DPP4, resulting in increased availability of GLP-1 levels in the body.
e.g. sitagliptin, alogliptin

Question 3

Metformin

Answer 3

Inhibits the mitochondrial respiratory chain in the liver, leading to the activation of AMPK.

Question 4

Thiazolidinediones

Answer 4

Activate Peroxisome proliferator-activated receptors (PPARs) , leading to increased insulin sensitivity.
Bad for CVD, HF, bladder ca, fracture risk
e.g. pioglitazone, rosiglatzone

Question 5

SGLT-2 inhibitors

Answer 5

Reversibly inhibit sodium-glucose co-transporter 2 (SGLT-2) in the renal proximal convoluted tubule to reduce glucose reabsorption and increase urinary glucose excretion.
Glycosuria –> UTI
e.g canagliflozin, dapagliflozin and empagliflozin

Question 6

Sulphonylureas

Answer 6

Bind to the ATP-dependent K+(KATP) channel on pancreatic beta cells, leading to increased insulin secretion.
Hypoglycaemia.
Can’t use in pregnancy/breastfeeding.
e.g. gliclazide

Question 7

GLP-1 mimetic

Answer 7

Increase insulin secretion and inhibit glucagon secretion.
Weight loss.
e.g. exenatide, semaglutide