Antilipemics

Question 1

What are the “statin” drug’s mech of action?

Answer 1

Inhibit HMG-CoA Reductase- the rate limiting enzyme of cholesterol synthesis

Question 2

What effects do the statin drugs have?

Answer 2

1. Reduce LDL
2. Reduce TG
3. Increase HDL

Question 3

List the statin drugs (that are on the condensed drug list)

Answer 3

I LOVe and ATORe SIM PRAV: Lovastatin, Atorvastatin, Simvastatin, Pravastatin

Question 4

These statins have the lowest bioavailability (about 5%)

Answer 4

Lovastatin, Simvastatin

Question 5

This statin has the highest renal excretion

Answer 5

Pravastatin

Question 6

This statin has the highest fecal and lowest renal excretion

Answer 6

Atorvastatin

Question 7

Of the ones on our drug list, which is the most potent statin?

Answer 7

Atorvastatin

Question 8

This statin is CYP3A4 metabolized

Answer 8

Lovastatin, Simvastatin

Question 9

Sleep disturbance, memory loss, myalgia, and TERATOGEN are side effects of?

Answer 9

Statins

Question 10

These antilipemic drugs interrupt enterohepatic recycling of cholesterol by binding to neg charged bile acids in the gut to prevent the uptake of bile acids

Answer 10

BILE ACID SEQUESTRANTS

Question 11

List the bile acid sequestrants

Answer 11

CC: Colestipol, Cholestyramine

Question 12

Bile acid sequestrant effect on LDL?

Answer 12

Lowers LDL

Question 13

Bile acid sequestrant effect on TG?

Answer 13

Does NOT decrease TG.. Shit, they may even go up!

Question 14

Where are the bile acid sequestrants absorbed?

Answer 14

They are NOT ABSORBED they just bind to bile acids and prevent the bile acids from enterohepatic cycling

Question 15

What do the bile acid sequestrants go good with to lower LDL and reduce CHD death and non-fatal MI?

Answer 15

Statins.. A good combo is a statin drug with a bile acid sequestrant

Question 16

This drug is a cholesterol absorption inhibitor

Answer 16

Ezetimibe

Question 17

Ezetimibe’s effects on LDL, HDL, TG?

Answer 17

Lowers LDL and TG; increases HDL

Question 18

Where is Ezetimibe excreted mostly?

Answer 18

Bile; it does enterohepatic circulation

Question 19

Ezetimibe and bile acid sequestrants are both enterohepatically circulated. What is the significance of this?

Answer 19

Dont take the two together!

Question 20

List the nicotinic acids

Answer 20

Niacor, Niaspan

Question 21

Nicotinic Acids have 4 mechs of action. List them

Answer 21

1. Inhibits mobilization of FFA from adipocytes
2. Reduces hepatic TG synthesis and ApoB synthesis
3. Enhances ATP cassette mediated transfer of cholesterol from macrophage to HDL
4. Promotes conversion of VLDL to LDL via enhanced LPL

Question 22

Unique effect of nicotinic acids?

Answer 22

Reduce Lp(a) which is shown to increase risk of atherosclerotic diseases

Question 23

Difference between the two nicotinic acids (Niacor and Niaspan)?

Answer 23

Nicacor is IR, Niaspan is ER. Think Niaspan has a longer SPAN of release

Question 24

Purpose of prescribing Niaspan over Niacor?

Answer 24

The ER Niaspan is better tolerated and produces less flushing (a side effect of these drugs)

Question 25

Fish oil is a?

Answer 25

Omega-3 polyunsaturated fatty acid

Question 26

Mechs of action of fish oil? (2)

Answer 26

1. Reduce TG synthesis by reducing SREBP-1c

2. Increase FA oxidation via PPARa activation

Question 27

Effects of fish oil?

Answer 27

Reduce TG; no effect on HDL/LDL

Question 28

List the fibric acid derivatives

Answer 28

Gemfibrozil, Fenofibrate

Question 29

Clinical use of the fibric acid derivatives?

Answer 29

Hypertriglyceridemia.. they decrease TG’s up to 50%

Question 30

How do the fibrates increase LPL activity thus increasing the clearance of TG-rich LP’s?

Answer 30

The fibrates supress the transcription of ApoCIII (remember that apoCIII is an inhibitor of LPL while apoCII is required for LPL activity)

Question 31

Which of the fibrates (Gemfibrozil or Fenofibrate) is safe for pts with renal dz?

Answer 31

Gemfibrozil because it is extensively hepatically metabolized.. Fenofibrate is not good for ppl with renal dz!!!

Question 32

Can you use the fibrates with statins?

Answer 32

Hell no!