Sketchy Pharm: Insulin, Sulfonylureas, Meglitinides, GLP-1 agonists, DPP-4 Inhibitors

Question 1

Beta cells produce insulin in response to beta-____ stimulation (among many other things).

Answer 1

2 (think of LangerHansel with the beta-2-tuba)

Question 2

The most potent stimulator of insulin release is ________.

Answer 2

glucose (like LangerHansel’s candy that is super large)

Question 3

Glucose increases _________ in beta cells.

Answer 3

ATP (from glycolysis)

Question 4

Increased intracellular ATP leads to ________ of potassium channels.

Answer 4

closing

Question 5

____________ open in response to closing of potassium channels.

Answer 5

Voltage-sensitive calcium channels (think of the calci-yum ice-cream flowers bending over the fence when Gretel grabs the candy)

Question 6

Insulin binds to a __________.

Answer 6

tyrosine kinase (just like the tyrosine tire swing)

Question 7

Insulin induces ___________ translocation.

Answer 7

GLUT4 (think of the four door)

Question 8

Insulin does what in liver cells?

Answer 8

Increases glycogen storage (think of the liver-shaped jar being filled with glycogen candies)

Question 9

In the muscles, insulin stimulates __________.

Answer 9

glycogen and protein synthesis (think of the glycogen glaze)

Question 10

In adipocytes, insulin ___________.

Answer 10

stimulates the conversion of carbohydrates into fat

Question 11

Remember that insulin administration causes a drop in __________.

Answer 11

potassium (just like the banana bitten off by the old hags)

Question 12

List the rapid-acting, short-duration insulin analogs (great for postprandial needs).

Answer 12

Glulisine, aspart, and lispro

“Girls And Lads” sign on the tall tower –like the tall peak in insulin

Question 13

Why are the glulisine, aspart, and lispro agents fast-acting?

Answer 13

They don’t polymerize like insulin because of amino-acid modifications.

Question 14

The two intermediate-acting insulin analogs are ___________. (These form dimers.)

Answer 14

regular insulin and NPH (neutral protamine hagedorn) insulin

(Think of the “Rest Now” sign above the more gradual peak on the witch’s house.)

Question 15

The only insulin drug that can be given IV is ________. Subcutaneous insulin is harder to control.

Answer 15

regular insulin (like the IVy under the “Rest” sign)

Question 16

The two long-acting insulins are _______________.

Answer 16

detemir and glargine (“Don’t Go”)

Question 17

Hypoglycemia presents with signs similar to ___________.

Answer 17

autonomic hyperactivity (tachycardia, palpitations, sweating, and nausea)

Question 18

“Glucagon… for when your glucose __________.

Answer 18

is gone.”

Question 19

How does sulfonylurea work?

Answer 19

It binds and closes the potassium channels in beta cells, stimulating the depolarization that causes release of insulin.

(Think of the sulfonylurea swan in the beta cell pond.)

Question 20

The first-generation sulfonylurea drugs end in the ______ suffix.

Answer 20

-amide (tolbutamide and chlorpropamide), just like how the sulfonylurea swan is in A MaID outfit

Question 21

The second-generation sulfonylurea drugs are __________.

Answer 21

glyburide, glipizide, and glimepiride (think of the TWO little swans RIDing on the big swan’s back)

Question 22

__________ has the shortest half-life of the second-generation sulfonylurea drugs.

Answer 22

Glipizide (glipi-zig-zagging around)

Question 23

What drug class works the same way as the sulfonylureas?

Answer 23

The meglitinides (like the goose GLIDing above the swan): rapaglinide and nateglinide

Question 24

The meglitinides do not contain __________ and are thus ideal for patients with allergies.

Answer 24

sulfa (because the father goose – GLIDing above –does not lay stinky sulfur eggs)

Question 25

The main side effect of sulfonylurea and meglitinide is ___________.

Answer 25

hypoglycemia particularly in the long-acting forms

Question 26

Why do meglitinides and sulfonylureas cause weight gain?

Answer 26

Because insulin –induced to release –causes growth

Question 27

Do not __________ while taking first-generation sulfonylureas.

Answer 27

drink alcohol (because it can lead to a disulfiram-like reaction)

Question 28

The GLP-1 analogs are ____________.

Answer 28

exenatide and liraglutide (the witch with her ExenaTide detergent)

Question 29

GLP is released from __________.

Answer 29

intestinal L cells

Question 30

What does GLP-1 do?

Answer 30

Induces satiety
Stimulates insulin release
Reducing glucagon release
Delaying gastric emptying

(The falling packets of glucagon; the stopped up stomach;

Question 31

DPP-4 is _____________.

Answer 31

dipeptidyl peptidase 4

Question 32

The DPP-4 inhibitors end in ___________.

Answer 32

-gliptin: sitagliptin, saxagliptin, and linagliptin

Question 33

What does glucagon do?

Answer 33

Stimulates gluconeogenesis and glycogenolysis (processes that increase blood sugar)

Question 34

What side effects can the DPP-4 inhibitors have?

Answer 34

Nasopharyngitis, URIs (the clip on the witch’s nose), and acute pancreatitis (witch squeezing the pancreas sponge)

Question 35

True or false: the DPP-4 inhibitors can cause hypoglycemia.

Answer 35

False. Their glucose-releasing effects stop when glucose normalizes.