Endo: Diabetes Medications

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 satietyStimulates insulin releaseReducing glucagon releaseDelaying 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.

Question 36

The first line treatment for type 2 diabetes is _____________.

Answer 36

metformin

Question 37

What is the mechanism of metformin?

Answer 37

It decreases hepatic gluconeogenesis by inhibiting the mitochondrial enzyme glycerophosphate dehydrogenase (think of the girl –whom the METaphOR-wielding boy is trying to woo –who is biting a mitochondria-shaped candy). Also, it activates AMPK, an enzyme that also works to inhibit gluconeogenesis. (Think of the AMPKandy bag.) Lastly, it increases peripheral insulin sensitivity (like the open Valentine’s mailbox on the bench by the metformin metaphor boy).

Question 38

What side effects can metformin cause?

Answer 38

Lactic acidosis from impaired gluconeogenesis (think of the spilled, spoiled milk). This needs to be thought of in patients with renal failure, because metformin is just excreted unmodified by the kidneys (think of the cracked, kidney-shaped tray that the lactic acid is on). Also, GI upset can be caused (like the green-faced girl about to barf at the metformin boy).

Question 39

What are the thiazolidinedione drugs?

Answer 39

Rosiglitazone and pioglitazone (think of the girl reading “ROSes are red” on the GLITter-covered card)

Question 40

What is the mechanism of thiazolidinediones?

Answer 40

They act on peroxisome proliferator-activated receptor gamma (PPAR-gamma), an intracellular nuclear receptor that increases glucose uptake and decreases glucose production (like the “life of the PPARy” shirt that the thiazolidinedione boy is wearing). One of the proteins expressed is adiponectin (like his turtleneck). Another protein is GLUT4 (like the GLUT4 mailbox).

Question 41

Explain the unique relationship between the thiazolidinediones and weight gain.

Answer 41

Thiazolidinediones lead to increased fatty-acid storage in adipocytes differentiation of adipocytes, leading to decreased triglyceride levels and weight gain. (Think of the boy eating doughnuts to represent fat storage.)

Question 42

True or false: thiazolidinediones take days to weeks to become effective.

Answer 42

True. Because it works by increasing gene expression, it takes time.

Question 43

Which non-insulin-raising diabetic meds increases weight gain?

Answer 43

The thiazolidinediones –”they put extra GLIT in your ZONE”

Question 44

What big side effect do you need to worry about with the thiazolidinediones (not related to weight gain)?

Answer 44

Peripheral edema due to increased fluid retention (like the thiazolidinedione boy’s baggy pants) – do not give to patients with CHF (like the baggy heart being crushed by the boy’s chair)

Question 45

The non-insulin-raising drug that acts on the peroxisome proliferator-activator receptor gamma can cause which side effect that is especially common in older women?

Answer 45

Osteoporosis (think of the boy’s chair, which has a femur-shaped leg that is breaking)

Question 46

What cells normally secrete amylin?

Answer 46

The pancreatic islet cells that also secrete insulin! Amylin is secreted with insulin and acts to decrease glucagon and delay gastric emptying (just like the full, stomach-shaped water cooler and torn glucagon packets next to the furious AMY and LyNn who were asked out by the same boy). The analogue is pramlintide.

Question 47

Pramlintide can be used to treat the _______________ in both types of diabetes.

Answer 47

postprandial glucose spike

Question 48

The two main side effects with pramlintide are _____________.

Answer 48

hypoglycemia (the falling candy jar that AMY is kicking) and nausea (Brayden getting sick at the embarassment)

Question 49

These two drugs work by inhibiting intestinal-brush-border alpha glucosidase: _________________.

Answer 49

acarbose (A-Carb candies) and miglitol (wIgGLer candies)

Question 50

The alpha glucosidase work to ____________.

Answer 50

delay glucose absorption (just like the frustrated boy is delayed in eating his Wiggler gummy worms)

Question 51

What are the main side effects of alpha glucosidase inhibitors?

Answer 51

Diarrhea and flatulence –both related to the massive load of undigested disaccharides that hits the colon

Question 52

What are the SGLT-2 inhibitors?

Answer 52

The -flozins: canagliflozin and dapagliflozin (just like the teacher FLOssing the salty/sweet kettle corn – sodium and glucose – out of his teeth)

Question 53

True or false: the SGLT-2 inhibitors work by decreasing glucose absorption in the small intestine.

Answer 53

False. They prevent glucose re-uptake in the proximal convoluted tubule.

Question 54

What are two (totally logical) side effects of SGLT-2 use?

Answer 54

Vaginal candidiasis, because of the increased glucose in the ureter (think of the CANadian boy throwing a snowball – white like candida – at the substitute’s crotch)And osmotic diuresis causing hypotension (the falling boy and the cracked kidney tray symbolizing contraindication in renal failure)