Antihyperlipidemics Flashcards
(91 cards)
1
Q
What are the lowest density lipoproteins?
A
Chylomicrons
2
Q
What are the apolipoproteins on chylomicrons?
A
B48
C
E
A
3
Q
What are the apolipoproteins on VLDL?
A
C
B-100 E
4
Q
What are the apolipoproteins on LDL?
A
B100
5
Q
What are the apolipoproteins on HDL?
A
AI AII C E D
6
Q
What type of lipoprotein has the highest ratio of TG;cholesterol?
A
Chylomicrons
7
Q
Where are chylomicrons synthesized?
A
Intestines
8
Q
Where aer VLDLs synthesized?
A
liver
9
Q
Where are HDL particles synthesized?
A
intestines, liver
10
Q
Cholesterol enters enterocytes through what protein?
A
Niemann-Pick C1-like protein (NPC1L1)
11
Q
Once inside the enterocytes cholesterol is reesterified by what enzyme?
A
acetyl-CoA: cholesterol acyltransferase (ACAT)
12
Q
What are the apolipoproteins that chylomicrons receive from HDL?
A
E
C-II
13
Q
What is the MOA of ezetimibe?
A
Inhibits NPC1L1
14
Q
What percent of bile is lost through the feces normally?
A
5%
15
Q
What is the function of apolipoprotein CII?
A
Binds to lipoprotein lipase, causing breakdown of the chylomicron
16
Q
Where does HDL get its apolipoprotein CII from?
A
From the reminants of LDL
17
Q
What is the function of apolipoprotein E on HDL?
A
Binds to receptor on liver for breakdown
18
Q
What is lipoprotein lipase, and where is it found?
A
Enzyme that breaks down chylomicron TGs,
found on cell surface of tissues
19
Q
What is the consequence of a decrease in apo CII expression?
A
Hypertriglyceridemia
20
Q
What are the receptors on the liver that apo E binds to?
A
remnant receptors
21
Q
What are the two fates of IDL?
A
Conversion to LDL
Broken down by liver
22
Q
What is the apolipoprotein that forms the structural component and is the messenger tag for LDL degradtion by the live ?
A
B100
23
Q
What happens to the apolipoproteins on IDLs as they are converted to LDL?
A
apo E and CII are transferred to HDL
24
Q
What is the receptor on LDL that serves as the receptor for degradation in the liver?
A
B100
25
What is the function of apolipoprotein AI on HDLs?
Facilitates the exchange of cholesterol from macrophages/other cells
26
What are the tissues in the body that can synthesize cholesterol de novo?
Liver
Gonads
Adrenal cortex
27
What are the substrates for cholesterol synthesis de novo?
Acetyl-coa and acetoacetyl coa
28
What is the enzyme that converted HMG CoA to mevalonate, a precursor to cholesterol?
HMG CoA reductase
29
What is the enzyamtic target of statins?
HMG CoA reducatase
30
What is the function of LCAT?
Convertes cholesterol into cholesterol esters in HDL particles for storage in HDLs
31
What is the receptor on the liver that binds to Apo A1 on HDL particles for uptake?
SRBI
32
What lipoprotein has the apolipoprotein AI on it? What is its function?
HDL, chylomicrons
Activates LCAT
Ligand for SRB1 receptor
33
What lipoprotein has the apolipoprotein A-II on it? What is its function?
HDL, chylomicrons
Structural protein for HDL
34
What lipoprotein has the apolipoprotein B-48 on it? What is its function?
Chylomicrons
Structural protein
35
What lipoprotein has the apolipoprotein B100 on it? What is its function?
VLDL, IDL, LDL
Structural protein that binds to LDL receptor
36
What lipoprotein has the apolipoprotein C-II on it? What is its function?
Chylomicrons, VLDL, HDL
Cofactor for lipoprotein lipase
37
What lipoprotein has the apolipoprotein E on it? What is its function?
Chylomicrons, VLDL, IDL, HDL
Ligand for binding to LDL receptor and remnant
38
What are the major goals of treating dyslipidemias?
Prevent acute pancreatitis
Prevent CVD
39
How does endothelial dysfunction lead to the development of CVD?
altered NO biosynthesis
40
How does injury of dysfunction endothelium lead to the development of CVD?
Expression of adhesion molecules, encouraging monocyte attachment
41
How does LDL transport into vessel walls lead to CVD?
production of ROS
42
What are the components of fatty streaks on vessels?
Foam cells
| T cells
43
What is the protective effect of HDL?
Uptake of lipids from arterial walls
44
What is the inflammatory fibroproliferative response seen in atherosclerosis?
cytokine activation of immune cells leading to deposition of CT
45
Why are plaque ruptures bad?
Provide a substrate for thrombosis
46
What are mixed hyperlipidemias?
High cholesterol and TG levels
47
What is the cause of, and manifestation of: primary chylomicronemia?
Decrease in LPL activity
Increased chylomicron VLDL
48
What is the cause of, and manifestation of: familial hypertriglyceridemia?
Impaired removeal of VLDL and/or chylomicrons
Increased VLDL/chylomicrons
49
What is the cause of, and manifestation of: Familiaal combined hyperlipoproteinemia
Increased VLDL production
Increased VLDL
50
What is the cause of, and manifestation of: familial dysbetalipoproteinemia?
Decreased clearance of VLDL, IDL and chylomicrons
Increased above
51
What is the cause of, and manifestation of: familial hyper-cholesterolemia?
LDLR impairments
Increased LDL
52
What is the cause of, and manifestation of: familial ligand-defective apoB?
Mutation in apoB, resulting in impaired endocytosis of LDL
Increased LDL
53
Major or minor risk factor for atherosclerosis: low HDL
Major
54
Major or minor risk factor for atherosclerosis: elevated LDL
Major
55
Major or minor risk factor for atherosclerosis: high triglycerides
Minor
56
Major or minor risk factor for atherosclerosis: VLDL and IDL remnatns
minor
57
What is the general MOA of fibric acid derivatives?
PPAR activators
58
What happens to plasma triglyceridea when using fibric acid derivatives? HDL?
Decreased triglycerides
| Increased HDL
59
What are the two fibric acid derivatives?
Gemfibrozil and fenofibrate
60
What is the MOA of gemfibrozil?
PPAR activators
61
What is the MOA of fenofibrate?
PPAR activator
62
What is PPAR alpha and how do fibratesuse this to treat hyperlipidemia?
transcription factor that increases the expression of lipoprotein lipase, Apo AI, AII, and decreases inhibitor apoprotein C-III
63
What is the effect of the upregulation of apoA-I and apoA-II proteins by fibrate activation of PPARs?
Increase HDL
64
What is the effect of the downregulation of apoC-III proteins by fibrate activation of PPARs?
Increase FA uptake
65
What is the effect of the upregulation of LPL proteins by fibrate activation of PPARs?
Increase FA uptake and breakdown
66
What is the major adverse effec of combining fibrates with statins?
Myopathy
67
What is the MOA of chloestyramine?
Bind to bile acids in the intestines, causing increased synthesis of bile acids
68
What is the MOA of colesevelam?
Bind to bile acids in the intestines, causing increased synthesis of bile acids
69
What is the MOA of colestipol?
Bind to bile acids in the intestines, causing increased synthesis of bile acids
70
What happens to the liver when bile acid-binding resins are used?
Increased LDL receptor to increase the uptake of LDL by the liver for bile acid synthesis
71
What is the major adverse efect of bile-acid binding resins?
Tend to increase plasma triglycerides
72
What is the drug of choice for pregnant women for treating hypercholesterolemias? Why?
Cholesterol binding resins since they are not absorbed
73
What is the MOA of niacin for treating dyslipidemias?
Binds to GPCR on adipocytes, decreasing hormone sensitive lipase activity
74
What is the function of hormone sensitie lipase?
Incrase lipolysis during fasting states when activation by epi, or other hormones
75
What are the adverse symptoms of Niacin?
Hyperuricemia
| Hepatotoxicity
76
How does niacin increase HDL levels?
Increaseing levels of apo AI
77
What is the MOA of ezetimibe?
Blocks intestinal absorption of cholesterol by inhibiting NPC1 protein
78
What is the effect on the liver of ezetimibe use?
Increases LDL receptors
79
What are the adverse effects of ezetimibe?
Few, if any
80
What is the MOA of all of the statins?
Competitive inhibitor of HMG-CoA reductase
81
What is the least potent statin?
Fluvastatin
82
What are the two most potent statins?
Rosuvastatin
| Atorvastatin
83
What is the effect of statins on the liver? Why?
Increases LDL receptor
Attempt to obtain more cholesterol from the plasma
84
What are the pleotropic effects of statins?
Whole bunch of good things
85
What are the adverse effects of statins?
Myopathy
Rhabdo
Hepatotoxicity
86
What are the labs that are commonly elevated with statin use? When are these concerning?
LFTs
| Concerning if bili rises as well
87
True or false: statins are contraindicated in pregnancy
True
88
What is niacin used in the treatment of?
All triglycerideemias and hypercholesterolemias
89
What are resins used to treat?
Familiar hypercholesterolemias
90
What is the drug of choice for treating familial dysbetalipoproteinemia?
Fibrates
91
What is the drug of choice for treating primary chylomicronemia?
Fibrates
