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