Pharmacology of Insulin

Question 1

Insulin levels rise

Answer 1

After meals

But is always secreted (base line levels)

Question 2

Four cell types in the pancreas and their product

Answer 2

Alpha - Glucagon (found on the periphary

Beta - Insulin

Delta - somatostatin

PP - Pancreatic polypeptide

Question 3

Insulin acts on which organs ?

Gets there through?

Answer 3

Liver, muscle & fat

Portal system

Question 4

Describe insulin action on beta cell intracellulary

Answer 4

Glucose activate GLUT2

ATP levels rise & close K channel

K intracellular levels rise and cause depolarization and opening of Ca channels

Preformed insulin granules that are complexed to Zn released

Question 5

Proinsulin post translation modification

Answer 5

C peptide

Alpha & beta chains

Question 6

What type of receptor does insulin bind

Answer 6

Tyrosine kinase activity

• Alpha and beta subunit
• Activation = Beta units auto-phosphorylate

Question 7

What types of receptors on liver, fat & muscle

Answer 7

Fat, liver & muscle

Question 8

Effect of insulin

Answer 8

Insulin promotes the storage of glucose as glycogen, amino acids as proteins, and fatty acids as triglycerides. Furthermore, insulin inhibits the breakdown of glycogen, proteins, and fats. Thus, insulin promotes the build-up and storage of cellular nutrients, and inhibits their breakdown.

Question 9

The insulin tyrosike kinases phosprolates…

Answer 9

Insulin Receptor Substrates

Question 10

Long term effects of insulin

Answer 10

Altered gene expression

Question 11

How is insulin injected

Answer 11

SubQ

Question 12

4 big categories of insulin preparations

Answer 12

Rapid acting
Short acting - regular insulin
Intermediateacting
Long actin

Question 13

Rapid Acting

• Name
• Modification
• Mechanism
• Taken how soon before a meal

Answer 13

Lispro

Modificatin
Reverse aa 28(pro)-19(lys)

Mechanism

• Less insulin aggregation around Zn so works fast by not having to aggregate first
• Minimizes postprandial hyperglycemia
• 0-15 min

Question 14

Long acting isulin (one)

• Name
• Modification
• Mechanism
• Taken how soon before a meal

Answer 14

Glargine

Modification

• Alpha chain: Convert asn to gly
• Beta chain: Add 2 arginines

Mechanism
- Precipitates at certain pH in subQ environment so diffuses into blood stream slowly so will not see insulin peak

Question 15

Long acting isulin (two)

• Name
• Modification
• Mechanism
• Taken how soon before a meal

Answer 15

Detemir

Modification
- Add fatty acid

Mechanism
- Less soluble because of fatty acids

Question 16

Usual dosing mechanism

Answer 16

Basal bolus
Short & long/intermediate insulins

Insulin pump can do the same thing

Question 17

Why is aggressive control of glucose important

Answer 17

Reduces percent of people with progressive retinopathy

Question 18

Main SE of insulin

Answer 18

Hypoglcemia

Question 19

How do you tell synthetic insulin from natural insulin

Answer 19

Natural insulin produced by the body is accompanied by C peptide release