Oral Hypoglycemics

Question 1

What are the 3 possible modes of actions for oral hypoglycemics?

Answer 1

Question 2

5 oral hypoglycemic agents

Answer 2

Question 3

Sulfonyl

Overview

The name is derived from what 2 structural features?

Answer 3

Question 4

Why are sulfonylureas weak acids?

Answer 4

Question 5

Features of sulfonlyl

Like other weak acids they are?

How many generations of them?

Answer 5

• Weak acids protein bound
• 1,2,3
  
  • 1 and 2 are similar 3 is very different

Question 6

Sulf MOA

Answer 6

Question 7

4 first gen Sulfonylureas

Answer 7

Question 8

Tolbutamide (gen?)

What metabolite is formed?

What does this mean for its activity?

Answer 8

Question 9

Tolazamide (Gen?)

Metabolism?

Answer 9

Question 10

Metablized Tolazamide vs. Tolbutamide

Which one has the longer DOA and why?

Answer 10

Question 11

Chlopropamide (gen?)

What block metabolism of the carboxylic acid?

What does this do?

Answer 11

Question 12

What does the n-propyl chain of chlorpropamide do?

So what does this mean for the drug?

Answer 12

Question 13

Acetohexamide (gen)

What group is rapidly reduced?

Answer 13

Question 14

Acetohexamide metabolite and DOA

Answer 14

Question 15

What first generation sulf provides the core for second gen?

Answer 15

Acetohexamide

Question 16

2nd gen

What features do they all share?

Answer 16

Question 17

Are second generations more potent than first?

These 2nd gen agents undergo similar biotranformations but its important to note that the metabolites?

Answer 17

Question 18

Second gen sulfs 2

Answer 18

Glipizide and Glyburide

Question 19

Glipizide

Structural featurs and DOA

3 things we need to know

Answer 19

Question 20

Glyburide Structural features and DOA

Answer 20

Question 21

SAR of 1st and second gen

What must be on the urea nitrogen?

Answer 21

Question 22

SAR 1st and 2nd

Where must substitution be present?

Answer 22

Question 23

SAR 1st and 2nd

For second gen what appears to be important?

Answer 23

Question 24

3rd Gen

Structural features similar to?

What is the chief example

What 2 good things does this drug have?

Answer 24

Question 25

3rd gen Where is binding? How does it exert its hypoglycemic effects? What is Glimepiride less likely to produce? Notes on Glimepiride

Answer 25

Question 26

Glimiperide DOA Structural features

Answer 26

Question 27

Glimepiride Metabolism? Enzymes? What metabolite has activity and what one doesnt?

Answer 27

Question 28

Problems with sulfs 4

Answer 28

Question 29

Meglitinides Given example? Difference compared to other hypoglycemics? Potency? What is it free of?

Answer 29

Question 30

Meglitinides MOA? Sites of binding?

Answer 30

Question 31

Repaglinide Metabolism how is it metabolized?

Answer 31

Question 32

Nateglinide? MOA? Like repaglinide free of?

Answer 32

Question 33

Biguanides Goats rue Galegine

Answer 33

Question 34

What by itself was know to lower sugar? Example shown?

Answer 34

Question 35

Metformin MOA? What is it dependent on? has no effect on what three things?

Answer 35

Question 36

3 important components of Metformins Action 1. Inhibits 2. Increases 3. Increase 4. Overall metformin increases?

Answer 36

Question 37

Metformin doesnt induce? Protein binding and metabolism? Elimination where? Drug is active in pts that dont have? DOA?

Answer 37

Question 38

A glucosidase Is MOA To be absorbed from the GI tract what has to happen with carbs?

Answer 38

Question 39

Actual A-Glucosidase I MOA

Answer 39

Question 40

A-glucosidase Inhibitors MOA What to Type II pts have that make this type of drug useful?

Answer 40

Question 41

A-GI notes What do they not cause? What is the main SE? Think about where its working

Answer 41

Question 42

3 A-GIs

Answer 42

Question 43

Acarbose Why is it poorly absorbed?

Answer 43

Question 44

Acarbose What unit is important for activity? What type of drug?

Answer 44

Question 45

Miglitol and Voglibose What is a key part of its structure? What about it compared to Acarbose?

Answer 45

Question 46

Thiazolidine Glitazones What functionality do they have?

Answer 46

Question 47

NO

Answer 47

Question 48

Metabolic path of troglitazone What enzymes metabolize it? What metabolite may have toxicity? what is the toxicity?

Answer 48

Question 49

Glitazone MOA What does it do? What does it target? What are they called?

Answer 49

Question 50

What do glitazones bind to?

Answer 50

Question 51

Glitazone MOA What is the main action of this drug? What does it increase? What are these drugs dependent on?

Answer 51

Question 52

Pioglitazone and Rosiglitazone both undergo?

Answer 52

Question 53

Pioglitazone Metabolic pathway

Answer 53

Question 54

Rosiglitazone pathway

Answer 54

Question 55

Big picture

Answer 55