Diabetes Drugs

Question 1

Biguanide example

Answer 1

Metformin

Question 2

Sulfonylurea example

Answer 2

Glimiperide

Question 3

Incretin example

Answer 3

Exanitide

Question 4

Depeptidyl peptidase IV inhibitor example

Answer 4

Sitagliptin

Question 5

Megalitinide/Glinide examples (2)

Answer 5

Repaglinide

Nataglinide

Question 6

Alpha glucosidase inhibitor examples (2)

Answer 6

Acarbose

Miglitol

Question 7

Amylin analog example

Answer 7

Pramlinitide

Question 8

Tiazolidendione example

Answer 8

Rosaglitazone

Piaglitazone

Question 9

Metformin class and MOA

Answer 9

Biguanide

Decreases hepatic glucose production by inhibiting gluconeogenesis via a few mechanisms

1. inhibits enzyme activities to reduce hepatic uptake of substrates such as lactate)
2. Increases insulin sensitivity
3. Reduces lipolysis in adipocytes and glucose intestinal absorption via suppression of ETC
4. Increase insulin receptor TK activity and stimulation of GLUT4 transporter

Question 10

SE of Metformin

Answer 10

Diarrhea
Lactic acidosis (circulating lactate not used as substrate for gluconeogenesis), worse with renal failure
Rarely hypoglycemia

Question 11

MOA of insulin secretagogues

Answer 11

Promote beta cell insulin secretion.
Closure of K+ channel changes membrane potential and leads to Ca channel opening.
Promotes hormone vesicles to fuse and secrete hormone

Question 12

MOA of Glimepiride

Answer 12

Insulin secretagogue

Binds to the SUR1 subunit of the ATP-sensitive K channel and closes it
- leads to an activation of Ca channels, increasing intracellular Ca and releases insulin filled vesicles

Question 13

SE of glimepiride?

Answer 13

Hypoglycemia

Weight gain

Question 14

MOA of Exanitide (GLP-1 analog)

Answer 14

Stimulates insulin and inhibits glucagon secretion
Delays gastric emptying
Induces satiety

Question 15

SE of exanitide?

Answer 15

GI disturbances
Nausea
Vomiting
Pancreatitis

Question 16

What enzyme degrades exanitide?

Answer 16

dipeptidyl peptidase IV

Question 17

MOA of stigaliptin (Januvia)

Answer 17

Inhibits dipeptidyl peptidase IV
This enzyme normally degrades incretins
More GLP-1 = more insulin secretion and more glucagon suppression

Question 18

MOA of Repaglinide and Nataglinide?

Answer 18

K+ channel blocker (binds to SUR1)
Promotes Ca channel opening and increases intracellular Ca
More intracellular Ca = more vesicle secretion of insulin

Question 19

SE of Repaglinide and Nataglinide

Answer 19

Hypoglycemia

Weight gain

Question 20

MOA of Acarbose and Miglitol

Answer 20

Glucosidase inhibitor – Interfere with hydrolysis of disaccharides and complex carbohydrates to monosaccharides
Slows digestion

Question 21

SE if Acarbose and Miglitol?

Answer 21

Mainly GI

Question 22

What is the benefit of Acarbose and Miglitol?

Answer 22

Can be used with other oral hypoglycemics to lower post prandial glucose levels

Question 23

Pramlinitide MOA?

Answer 23

Delay gastric emptying and inhibits glucagon secretion by binding to amylin receptors

Question 24

What is the effect of inhibiting an amylin receptor?

Answer 24

Inhibits glucagon synthesis
Inhibits glucose synthesis in the liver
Delays gastric emptying
Increases satiety

Question 25

Rosiglitazone and Pioglitazone MOA?

Answer 25

PPAR gamma receptor agonist (a steroid transcription factor) | Increases glucose uptake and utilization by increasing synthesis and transport of GLUT to muscles, adipose and liver

Question 26

This drug decreases hepatic glucose production by inhibition of gluconeogensis

Answer 26

Metformin (Biguanides)

Question 27

This drug class increases uptake of skeletal muscle insulin and increases cell responsiveness to insulin

Answer 27

PPAR agonists -- Rosiglitazone and Piaglitazone

Question 28

These drugs close K+ channels on pancreatic beta cells - promoting an increase in intracellular calcium and release of insulin

Answer 28

Glimepiride (Sulfonureas) | Repaglinide, Nateglinide (Meglitinide/glinide)

Question 29

These drug classes activate adenyl cyclase

Answer 29

GLP analogs | Dipeptidase IV inhibitors (Increase GLP)