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33 Cards in this Set

  • Front
  • Back
What is intestinal cholesterol absorption mediated by (protein)
Niemann-Pick C-1 like protein 1 (NPC 1L1)
What does the majority of fat enter circulation as
chylomicrons (90%)
What makes up the majority of plasma cholesterol
LDL - 66%
What does LDL do
deliver cholesterol to the vessel walls and to the tissues
Why is LDL bad
LDL --> oxidized --> macrophages --> foam cells --> atherosclerotic plaques
T/F - antioxidant vitamins prevent formation of atherosclerotic plaques
-false
How does HDL work
binds to macrophages, endothelia and sucks in cholesterol
-delivers cholesterol to the liver
What does HDL exchange cholesterol ester for
triglycerides (from chylomicrons and VLDL)
-requires cholesterol ester transfer protein
What does hepatic lipase do
-takes apart HDL triglycerides
T/F - most of the cholesterol in your body is synthesized in your liver
-true
What is the rate limiting step of cholesterol synthesis
-HMG-CoA reductase
What do statins target
HMG-CoA reductase
Statins:
what
effectiveness
-CI of HMG-CoA reductase in liver
-most effective and best tolerated drugs for hypercholesterolemia
How does the body react to statins
-liver makes more LDL receptor to get more cholesterol from blood = less LDL is available to deliver cholesterol/TAG to tissues
simvastatin and resuvastatin may do what
-increase HDL levels
lovastatin and simvastatin are administered as what
-inactive lactones which enter liver by diffusion and then are activated
How are the majority of statins chemically formed
-beta-hydroxy acids
Statins:
bioavailability
-5-30% due to first pass effects
Which two statins have half lives of 20 hours
-atorvastatin and rosuvastatin
Three major side effects of statins
elevated AST levels leading to liver failur rarely, myopathy, drug interactions (fibrates, cyclosporine, digoxin, warfarin, macrolide abx, azole af)
pravastatin and fluvastatin have what directions
-take at bed time away from meals and cholesterol sequestering agents
atorvastatin and rosuvastatin are taken when
once per day - have a long half life
rosuvastatin interactis with what
gemfibrozil - increases plasma concentration
Which statin SHOULD be taken with meals
-lovastatin
How do bile acid sequestrants work
-anion exchange resins that bind bile acids and cause excretion of bile
-bile is not reabsorbed so there is net loss of cholesterol
Cholestyramine and colestipol
-what are they
-interactions
-bile acid sequestrants
-absorption of fat soluble vitamins, lots of drugs, statins
Colesevelam
-what is it
-why its better
-bile acid sequestrant
-doesn't interfere with many drugs like others
Niacin:
-how it works
-in large doses inhibits TAG synthesis and increases ApoB degradation = less VLDL = less C transported out to cells
-also increases ABCA-1 and reduces clearance of HDL-ApoA1 so there is more HDL removing cholesterol from plaque forming cells at a faster rate
Niacin:
uses
-w/sequesterants and statins
-increases HDL and reduces LDL
clofibrate:
-what is it
-uses
-fibric acid derivative
-triglyceridemias (in mild cases will raise HDL, in moderate cases will raise LDL)
What is the drug of choice for hypertriglyceridemia and chylomicronemia syndrome
-fibric acid derivatives
Ezetimibe:
-how it works
-what it does
-inhibits NPC1L1 in jejunum = reduces absorption up to 70%
-lowers total and LDL cholesterol
Ezetimibe:
-usually prescribed
-interaction
-in combo with statins
-bile sequestrants block absorption of the drug