Antidiabetics (3)

Question 1

What do incretins do?

Answer 1

GI hormones increase in amount of insulin released after eating, but before blood glucose levels are elevated

Question 2

Incretins inhibit glucagon release from what cells?

Answer 2

a cells of islets of Langerhan

Question 3

What does glucagon do?

Answer 3

incease blood glucose levels

Question 4

What are the 2 main incretins?

Answer 4

GLP-1

GIP

Question 5

What inactivates GLP-1 and GIP?

Answer 5

DPP-4

Question 6

Where is GLP-1 secreted from?

Answer 6

L cells in jejunum and ileum

Question 7

long term effects of GLP-1 in animals

Answer 7

increas B cell mass

maintain B cell function

Question 8

GIP and GLP-1 in T2D

Answer 8

defective

Question 9

MOA GLP-1

Answer 9

• promote release of insulin
• lower glucagon levels
• promote satiety (slow gastric emptying)

Question 10

GLP-1 drugs

Answer 10

Byetta (exenatide)

Bydureon

Victoza (liraglutide)

Question 11

Bydureon

Answer 11

encapsulated form of Byetta

slow release

Question 12

What drug is also used in nondiabetics for obesity?

Answer 12

liraglutide (Victoza)

Question 13

What is GIP also known as?

Answer 13

glucose dependent insulinotropic peptide

Question 14

GIP drugs

Answer 14

still in research

not on market yet

Question 15

GIP MOA

Answer 15

thought to induce insulin secretion

Question 16

DPP4 acts as a ____ protein involved in important pysiological processes

Answer 16

multifunctional

Question 17

DP4 is also known as

Answer 17

CD26

adenosine-deaminase binding protein (ADAbp)

Question 18

DPP4 cleaves off _____ which is a specific ____

Answer 18

dipeptide HisAla

antagonist

Question 19

Gliptans are what type of drug?

Answer 19

DPP4 inhibitor

Question 20

DPP-4 has a strong influence on ____ and ____

Answer 20

insulin sensitivity

glucose homeostasis

Question 21

What is poised to be next major drug class for treatment of T2D?

Answer 21

DPP4 inhibitors

Question 22

Active site of DPP4 inhibitor

Answer 22

within large cavity at interface of b-propeller and hydrolase domain

**wide structural variety

Question 23

What other two DPP share identical active stie with DPP4?

Answer 23

8 and 9

Question 24

DDP4 inhibitors must possess a potency and PK profile that produces _____% inhibition for ____ hours

Answer 24

>90%

24 hours

Question 25

DPP4 inhibitors must develop what?

Answer 25

selectivity against DPP8 and 9

Question 26

What drugs are gliptans?

Answer 26

sitagliptin

vidaglipitin

saxagliptin

alogliptin

linagliptin

Question 27

T/F januvia can cause your blood glucose to go too low

Answer 27

false. does not work when blood glucose is low

Question 28

Is byetta or januvia indicated as an earlier treatment?

Answer 28

januvia

Question 29

side effects of GLP-1 and DPP4 inhibitors

Answer 29

increased risk of pancreatitis

Question 30

a-glucosidase inhibitor MOA

Answer 30

delay of digestion of carbs

decrease postprandial blood glocuose and insulin

**delay absorption

Question 31

Metabolism of a-glucosidase inhibitors

Answer 31

O methylated

O sulfated

O glucuronate

Question 32

(SAR) a-glucosidase inhibitors have inhibition of what?

Answer 32

kinetics of a-glucosidase complex

Question 33

(SAR) cleavage of a-glucosidase inhibitors occurs how?

Answer 33

energy oxonium ion

Question 34

(SAR) a-glucosidase inhibitors require what groups that appear glucose like?

Answer 34

NH2 and OH groups

Question 35

(SAR) a-glucosidase inhibitors possess what?

Answer 35

protonate amines that occupy position of oxonium