Antilipemics Flashcards
What are the “statin” drug’s mech of action?
Inhibit HMG-CoA Reductase- the rate limiting enzyme of cholesterol synthesis
What effects do the statin drugs have?
- Reduce LDL
- Reduce TG
- Increase HDL
List the statin drugs (that are on the condensed drug list)
I LOVe and ATORe SIM PRAV: Lovastatin, Atorvastatin, Simvastatin, Pravastatin
These statins have the lowest bioavailability (about 5%)
Lovastatin, Simvastatin
This statin has the highest renal excretion
Pravastatin
This statin has the highest fecal and lowest renal excretion
Atorvastatin
Of the ones on our drug list, which is the most potent statin?
Atorvastatin
This statin is CYP3A4 metabolized
Lovastatin, Simvastatin
Sleep disturbance, memory loss, myalgia, and TERATOGEN are side effects of?
Statins
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
BILE ACID SEQUESTRANTS
List the bile acid sequestrants
CC: Colestipol, Cholestyramine
Bile acid sequestrant effect on LDL?
Lowers LDL
Bile acid sequestrant effect on TG?
Does NOT decrease TG.. Shit, they may even go up!
Where are the bile acid sequestrants absorbed?
They are NOT ABSORBED they just bind to bile acids and prevent the bile acids from enterohepatic cycling
What do the bile acid sequestrants go good with to lower LDL and reduce CHD death and non-fatal MI?
Statins.. A good combo is a statin drug with a bile acid sequestrant
This drug is a cholesterol absorption inhibitor
Ezetimibe
Ezetimibe’s effects on LDL, HDL, TG?
Lowers LDL and TG; increases HDL
Where is Ezetimibe excreted mostly?
Bile; it does enterohepatic circulation
Ezetimibe and bile acid sequestrants are both enterohepatically circulated. What is the significance of this?
Dont take the two together!
List the nicotinic acids
Niacor, Niaspan
Nicotinic Acids have 4 mechs of action. List them
- Inhibits mobilization of FFA from adipocytes
- Reduces hepatic TG synthesis and ApoB synthesis
- Enhances ATP cassette mediated transfer of cholesterol from macrophage to HDL
- Promotes conversion of VLDL to LDL via enhanced LPL
Unique effect of nicotinic acids?
Reduce Lp(a) which is shown to increase risk of atherosclerotic diseases
Difference between the two nicotinic acids (Niacor and Niaspan)?
Nicacor is IR, Niaspan is ER. Think Niaspan has a longer SPAN of release
Purpose of prescribing Niaspan over Niacor?
The ER Niaspan is better tolerated and produces less flushing (a side effect of these drugs)
Fish oil is a?
Omega-3 polyunsaturated fatty acid
Mechs of action of fish oil? (2)
- Reduce TG synthesis by reducing SREBP-1c
2. Increase FA oxidation via PPARa activation
Effects of fish oil?
Reduce TG; no effect on HDL/LDL
List the fibric acid derivatives
Gemfibrozil, Fenofibrate
Clinical use of the fibric acid derivatives?
Hypertriglyceridemia.. they decrease TG’s up to 50%
How do the fibrates increase LPL activity thus increasing the clearance of TG-rich LP’s?
The fibrates supress the transcription of ApoCIII (remember that apoCIII is an inhibitor of LPL while apoCII is required for LPL activity)
Which of the fibrates (Gemfibrozil or Fenofibrate) is safe for pts with renal dz?
Gemfibrozil because it is extensively hepatically metabolized.. Fenofibrate is not good for ppl with renal dz!!!
Can you use the fibrates with statins?
Hell no!
