Pharm: Insulin, sulfonylureas, meglitinides, GLP-1 agonists, DPP-4 inhibitors

Question 1

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

Answer 1

glulisine, aspart, and lispro

“Girls and Lads” sign on the tall tower - like the tall peak in insulin

Question 2

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

Answer 2

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

Question 3

The two intermediate-acting insulin analgos are __________. (These form dimers.)

Answer 3

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 4

Insulin induces __________ receptor translocation.

Answer 4

GLUT4 (think of the four door)

Question 5

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

Answer 5

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

Question 6

The most potent stimulator of insulin release is _________.

Answer 6

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

Question 7

The two long-acting insulins are ______________.

Answer 7

detemir and glargine

“Don’t Go” sign under the flat part of the roof

Question 8

Hypoglycemia presents with signs similar to ____________.

Answer 8

autonomic hyperactivity (tachycardia, palpitations, sweating and nausea)

Question 9

“Glucagon… for when you glucose _____________.” AKA When do you have high levels of glucagon?

Answer 9

is gone (fasting state)

Question 10

How does sulfonylurea work?

Answer 10

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

(Think of the sulfonylurea swan in the beta cell pond behind the CLOSED K+ banana garden.)

Question 11

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

Answer 11

• amide
  ex: tolbutamide and chlorpropamide

(Think of how the sulfonylurea swan is in A MaID outfit)

Question 12

The second-generation sulfonylurea drugs are _______, _______, and _______.

Answer 12

glyburide, glipizide, and glimepiride (think of the TWO little swans RIDing on mama swan’s back and the one ZIPing along side her)

Question 13

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

Answer 13

glipizide- therefore less hypoglycemia (glipi-sig-sagging around)

Question 14

What drug class works the same way as the sulfonylureas?

Answer 14

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

Question 15

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

Answer 15

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

Question 16

The main side effect of sulfonylureas and meglitinides are _________.

Answer 16

hypoglycemia particularly in the long-acting forms (think of all the fallen overripe candies)

Question 17

Why do meglitinides and sulfonylureas cause weight gain?

Answer 17

Because insulin- induced to release- causes anabolism/growth (think of the fat witch under the tree eating the overripe candy)

Question 18

Do not _________ while taking first-generation sulfonylureas.

Answer 18

drink alcohol- because it can lead to a disulfiram-like reaction (think of the “Do Not Drink” sign by the swan lake)

Question 19

The GLP-1 analogs are ______ and _______.

Answer 19

exenatide and liraglutide (the witch with her ExenaTIDE detergent)

Question 20

GLP is released from ___________.

Answer 20

intestinal L cells

Question 21

In the muscles, insulin stimulates _________.

Answer 21

glycogen and protein synthesis (think of the glycogen-glazed ham)

Question 22

What does GLP-1 do?

Answer 22

1. Induces satiety
2. Stimulates insulin release
3. Reducing glucagon release
4. Delaying gastric emptying

(The galling packets of glucagon; stopped up stomach)

Question 23

What does DPP-4 stand for?

Answer 23

dipeptidyl peptidase 4

Question 24

The DPP-4 inhibitos end in ________.

Answer 24

-gliptin: sitaliptin, saxagliptin, and linagliptin (think of the DriPPing cloths cLIPped in clothes pins)

Question 25

What does glucagon do?

Answer 25

Stimulates gluconeogensis and glycogenolysis (processes that increase blood sugar)

Question 26

What side effects can the DPP-4 inhibitors have?

Answer 26

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

Question 27

True or flase: the GLP-1 agonists and DPP4- inhibitors can cause hypoglycemia.

Answer 27

False. Their glucose-release effects stops when glucose normalizes.

Question 28

________ open in response to closing of potassium channels.

Answer 28

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

Question 29

Insulin does what in liver cells?

Answer 29

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

Question 30

In adipocytes, insulin ____________.

Answer 30

Stimulates the conversion of carbohydrates into fat

Question 31

Insulin binds to a ___________ type of receptor.

Answer 31

tyrosine kinase (just like the tyrosine tire swing)

Question 32

Remember that insulin administration causes a drop in __________ in addition to glucose.

Answer 32

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

Question 33

Increased intracellular ATP leads to ________ of potassium channels.

Answer 33

closure (think of the closed gate of the K+ banana graden)

Question 34

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

Answer 34

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

Question 35

Glucose increases ___________ (molcule) in beta cells.

Answer 35

ATP (from glycolysis)