Wk2 Diabetes Drugs

Question 1

Main MOA is inhibiting gluconeogenesis but not fully known:

Answer 1

Metformin

Question 2

Reduces hepatic uptake of gluconeogenic substrates:

What side effect does this cause?

Answer 2

Metformin

lactate –> lactic acidosis

Question 3

Systemic effect of Metformin:

Answer 3

increases insulin sensitivity (tyrosine kinase)

reduces lipolysis

reduces glucose absorption from SI

Question 4

Binds SUR1 subunit of K+/ATP channel:

**How does this increase insulin secretion?

Answer 4

Glimepride

**closes channel –> DEPOLARIZES cell –> increases Ca++ –> induces fusing of insulin vesicles

Question 5

Slide 6….

Answer 5

**this is a big one!!!

Question 6

GLP-1 analog:

Answer 6

Exenatide

Question 7

How does GLP-1 analog work?

Answer 7

Activates Adenyl Cyclase –> increased cAMP –> increased Ca++ –> increased insulin secretion

Question 8

DPP-IV inhibitor:

Answer 8

Sitagliptin

Question 9

How does Sitagliptin work?

Answer 9

inhibits DDP-IV –> prevents degradation of GLP-1 and GIP

Question 10

K+ channel blockers:

Answer 10

–glinides

repaglinide, nataglinide

Question 11

Two drugs that block K+ channel:

Answer 11

Glimepiride

–glinides

**need some beta cell activity to work

Question 12

a-glucosidase inhibitors:

Answer 12

Acarbose

Miglitol

Question 13

amylin analog:

Answer 13

Pramlinitide

Question 14

How does Pramlintide work?

Answer 14

amylin analog

• inhibits glucagon synthesis
• inhibits gluconeogenesis in liver
• delays gatric emptying
• increases satiety

Question 15

PPARgamma receptor agonist:

Answer 15

TZDs

–litazones

Question 16

How do rosiglitazone and pioglitizone work?

Answer 16

activate PPARgamma (a transcription factor) –> upregulates GLUT transporter synthesis

**needs insulin present to work

Question 17

Bladder cancer

Answer 17

TZDs

Question 18

Two classes of insulin sensitizers:

Answer 18

metformin (biguanides)

TZDs

Question 19

Four classes of insulin secretagogues:

Answer 19

1. sulfonylureas – GLIMEPRIDE
2. meglinitides – “–GLINIDES”
3. GLP analogs – EXENATIDE
4. DDP-IV inhibitors – SITAGLIPTIN