Pancreatic Hormones, Antidiabetic Agents, & Glucagon

Question 1

Rapid-acting insulins

Answer 1

Lispro
Aspart
Glulisine

Question 2

MOA of metformin

Answer 2

Decreased endogenous glucose production (inhibits hepatic and renal gluconeogenesis)
Increases insulin sensitivity (stimulates glucose uptake and glycolysis in peripheral tissues)
Slows glucose absorption from GI tract
Reduces plasma glucagon levels

Question 3

Adverse side effects of metformin

Answer 3

GI disturbances (diarrhea, flatulence)
Lactic acidosis

Question 4

Increase insulin secretion from pancreatic beta cells by closing ATP-sensitive K+ channels

Answer 4

Glipizide, glyburide, glimepiride
Repaglinide, nateglinide (fast-acting; useful for administration just before a meal to control postprandial glucose levels)
Chlorpropamide, tolbutamide (older; lower potency, greater toxicity; rarely used)

Question 5

Adverse side effects of insulin secretagogues (e.g., glipizide)

Answer 5

Hypoglycemia (glyburide is the worst)

Weight gain

Question 6

Inhibits intestinal alpha-glucosidases

Answer 6

Acarbose, miglitol

Question 7

Side effects of acarbose

Answer 7

GI disturbances

Question 8

MOA of rosiglitazone, pioglitazone

Answer 8

Increase target tissue sensitivity to insulin by activating the PPAR-gamma receptor. PPAR-gamma regulates the transcription of genes encoding proteins involved in carbohydrate and lipid metabolism.
Expands adipose tissue and decreases serum FAs.

Question 9

Adverse effects of rosiglitazone/pioglitazone

Answer 9

Fluid retention, edema –> may worsen heart disease and increase risk of MI (pioglitazone possibly has less cardiovascular effects)
Weight gain
Anemia
Risk of osteopenia/Bone fractures in women
Increased risk of bladder cancer

Question 10

Analog of GLP-1 that activates GLP-1 receptors

Answer 10

Exenatide

Question 11

What does activation of GLP-1 do?

Answer 11

Augments glucose-stimulated insulin release from pancreatic B cells
Slows gastric emptying, which produces a feeling of satiety
Inhibits glucagon secretion

Question 12

Inhibitor of DPP-4, which degrades GLP-1 and other incretins

Answer 12

Sitagliptin

Question 13

Adverse side effects of exenatide

Answer 13

GI disturbances (nausea), headache
Has also caused serious and sometimes fatal acute pancreatitis

Question 14

Adverse side effects of sitagliptin

Answer 14

Rhinitis, URIs, rare allergic reactions

Question 15

Activates amylin receptors, which suppresses glucagon release, slows gastric emptying, and works in the CNS to reduce appetite

Answer 15

Pramlintide

Question 16

Adverse side effects of pramlintide

Answer 16

Hypoglycemia, Gi disturbances

Question 17

What is glucagon used for?

Answer 17

Severe hypoglycemia, beta-blocker overdose