Mechanisms/Drug Class Flashcards by Melissa V | Brainscape

Q

What is the mechanism of action of α-glucosidase inhibitors?

A

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

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Q

acarbose

A

α-glucosidase inhibitor

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Q

miglitol

A

α-glucosidase inhibitor

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Q

voglibose

A

α-glucosidase

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Q

What is the mechanism of action of exogenous insulin?

A

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

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Q

regular insulin

A

prandial bolus exogenous insulin

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Q

insulin lispro

A

prandial bolus exogenous insulin

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Q

insulin aspart

A

prandial bolus exogenous insulin

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Q

insulin glulisine

A

prandial bolus exogenous insulin

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Q

NPH insulin

A

basal “long-acting” exogenous insulin

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Q

insulin glargine

A

basal “long-acting” exogenous insulin

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Q

insulin detemir

A

basal “long-acting” exogenous insulin

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Q

What is the mechanism of action of secretagogues?

A

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

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Q

acetohexamide

A

first-generation sulfonylurea

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Q

chlorproamide

A

first-generation sulfonylurea

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Q

tolazamide

A

first-generation sulfonylurea

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Q

tolbutamide

A

first-generation sulfonylurea

Q

glimepriride

A

second-generation sulfonylurea

Q

glipizide

A

second-generation sulfonylurea

Q

glibenclamide (glyburide)

A

second-generation sulfonylurea

Q

gliclazide

A

second-generation sulfonylurea

Q

gliquidone

A

second-generation sulfonylurea

Q

nateglinide

A

meglitinide

Q

regaglinide

A

meglitinide

Q

What is the mechanism of action of insulin sensitizers: biguanides?

A

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

Q

metformin

A

insulin sensitizer: biguandes

Q

What is the mechanism of action of amylin analogue?

A

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

Q

pramlintide

A

amylin analogue

Q

What is the mechanism of action of incretins?

A

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

Q

exenatide

A

GLP-1 analogue (incretin)

Q

liraglutide

A

GLP-1 analogue (incretin)

Q

sitagliptin

A

DPP-4 inhibitor (incretin)

Q

saxagliptin

A

GLP-1 analogue (incretin)

Q

What is the mechanism of action of insulin sensitizers: thiazolidinediones (TZDs)?

A

They bind and stimulate the nuclear receptor peroxisome proliferator-activated receptor-γ (PPARγ), thereby increasing insulin sensitivity in adipose tissue, liver, and muscle

Q

pioglitazone

A

insulin sensitizer: thiazolidinedione

Q

rosiglitazone

A

insulin sensitizer: thiazolidinedione

Q

What is the mechanism of action of diazoxide?

A

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

Q

What is the mechanism of action of somatostatin analogues?

A

Inhibits GHRH release

Q

octreotide

A

somatostatin analogue

Q

What is the mechanism of action of exogenous glucagon?

A

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