Mechanisms/Drug Class Flashcards
What is the mechanism of action of α-glucosidase inhibitors?
They are carbohydrate analogues that bind avidly to intestinal brush border α-glucosidase enzyme; slowing breakdown and absorption of dietary carbohydrates, such as starch, dextrin, and dissaccharides
acarbose
α-glucosidase inhibitor
miglitol
α-glucosidase inhibitor
voglibose
α-glucosidase
What is the mechanism of action of exogenous insulin?
Insulin is the classic anabolic hormone, insulin promotes carbohydrate metabolism and facilitates glucose, amino acid, and triglyceride uptake and storage in the liver, cardiac, and skeletal muscle, and adipose tissue
regular insulin
prandial bolus exogenous insulin
insulin lispro
prandial bolus exogenous insulin
insulin aspart
prandial bolus exogenous insulin
insulin glulisine
prandial bolus exogenous insulin
NPH insulin
basal “long-acting” exogenous insulin
insulin glargine
basal “long-acting” exogenous insulin
insulin detemir
basal “long-acting” exogenous insulin
What is the mechanism of action of secretagogues?
Sulfonylureas and meglitinides inhibit the β-cell K+/ATP channel at the SUR1 subunit, thereby stimulating insulin release from pancreatic β-cells and increasing circulating insulin to levels sufficient to overcome insulin resistance
acetohexamide
first-generation sulfonylurea
chlorproamide
first-generation sulfonylurea
tolazamide
first-generation sulfonylurea
tolbutamide
first-generation sulfonylurea
glimepriride
second-generation sulfonylurea
glipizide
second-generation sulfonylurea
glibenclamide (glyburide)
second-generation sulfonylurea
gliclazide
second-generation sulfonylurea
gliquidone
second-generation sulfonylurea
nateglinide
meglitinide
regaglinide
meglitinide
What is the mechanism of action of insulin sensitizers: biguanides?
Activates AMP-dependent protein kinase (AMPK) to block synthesis of fatty acids and to inhibit hepatic gluconeogenesis and glucogenolysis; increases insulin receptor activity and metabolic responsiveness in liver and skeletal muscle
metformin
insulin sensitizer: biguandes
What is the mechanism of action of amylin analogue?
It is co-released with insulin from the β-cell; acts on receptors in the CNS to slow gastric emptying, reduce postprandial glucagon and glucose released, and promote satiety
pramlintide
amylin analogue
What is the mechanism of action of incretins?
They act on glucagon-like peptide-1 (GLP-1) receptor (GLP-1 analogues) or prolong GLP-1 activity (DPP-4 inhibitors) to enhance glucose-dependent insulin secretion, inhibit glucagon secretion, delay gastric emptying, and decrease appetite
exenatide
GLP-1 analogue (incretin)
liraglutide
GLP-1 analogue (incretin)
sitagliptin
DPP-4 inhibitor (incretin)
saxagliptin
GLP-1 analogue (incretin)
What is the mechanism of action of insulin sensitizers: thiazolidinediones (TZDs)?
They bind and stimulate the nuclear receptor peroxisome proliferator-activated receptor-γ (PPARγ), thereby increasing insulin sensitivity in adipose tissue, liver, and muscle
pioglitazone
insulin sensitizer: thiazolidinedione
rosiglitazone
insulin sensitizer: thiazolidinedione
What is the mechanism of action of diazoxide?
Binds to SUR1 subunit of K+/ATP channels in pancreatic β-cells and stabilizes the ATP-bound (open) state of the channel so that β-cells remain hyperpolarized, this decreases insulin secretion by the cells
What is the mechanism of action of somatostatin analogues?
Inhibits GHRH release
octreotide
somatostatin analogue
What is the mechanism of action of exogenous glucagon?
Glucagon is a polypeptide hormone produced by the α-cells in the islets of Langerhans in the pancreas, that stimulates gluconeogenesis and glucogenolysis in the liver, resulting in an increase in blood sugar
