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Therapeutics 2 - Exam 5 > anti-hyperlipidemia > Flashcards

anti-hyperlipidemia Flashcards

hockerman

1
Q

what is the role of cholesterol?

A

essential component of cell membranes
precursor to sterols and steroids

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2
Q

what is the role of TGs?

A

storage form of fuel to support generation of high energy compounds
component of structural lipids

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3
Q

what is a lipoprotein?

A

spherical macromolecular aggregate
trasports cholesterol and TG in the blood

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4
Q

what is the composition of lipoprotein surface?

A

phospholipid, free cholesterol, and protein (apoprotein)

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5
Q

what is the composition of a lipoprotein core?

A

TG
cholesterol ester

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6
Q

what is the function of apoproteins?

A

regulate transport and metabolism

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7
Q

what is the purpose of the lipoprotein lipase system?

A

release free fatty acids from lipoproteins

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8
Q

what are the major classes of lipoproteins?

A

chylomicrons
VLDL
IDL
LDL
HDL

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9
Q

what is a chylomicron?

A

lipoprotein involved in the transport of dietary lipids from the gut to liver and adipose tissue

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10
Q

what is a VLDL?

A

very low density lipoprotein
secreted by liver into blood as a source of TGs

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11
Q

what is a IDL?

A

an intermediate density lipoprotein that is basically just TG-depleted VLDL

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12
Q

what is a LDL?

A

low density lipoprotein
main cholesterol form in the blood

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13
Q

what is a HDL?

A

high density lipoprotein
secreted by liver
acquires cholesterol from peripheral tissues and atheromas
reverse cholesterol transport

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14
Q

what is the largest lipoprotein?

A

chylomicrons

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15
Q

what lipoprotein has the highest TG content?

A

chylomicrons

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16
Q

what lipoprotein is the smallest?

A

HDLs

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17
Q

what lipoprotein has the highest protein content?

A

HDL

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18
Q

what is ApoA-I?

A

structural apolipoprotein in HDL and ligand of the ABCA1 receptor
mediates reverse cholesterol transport

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19
Q

where is ApoA-I production location?

A

liver and intestine

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20
Q

what is ApoB-100?

A

structural apolipoprotein in VLDL, IDL, and LDL
LDL receptor ligand

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21
Q

where is ApoB-100 production located?

A

liver

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22
Q

what is ApoB-48?

A

structural apolipoprotein in chylomicrons

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23
Q

where is ApoB-48 production located?

A

intestine

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24
Q

what is ApoE?

A

apoplipoprotein that is a ligand for LDL remnant receptor
mediates reverse cholesterol transport with HDL

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25
where is ApoE production located?
liver and other tissues?
26
What is ApoCII?
apolipoprotein that binds to lipoprotein lipase to enhance TG hydrolysis
27
what is the location of ApoCII?
chylomicrons and VLDL
28
what is hepatic lipase?
enzyme produced in the liver that degrades the TG in IDL to form LDL
29
what is lipoprotein lipase (LPL)?
enzyme found in capillaries of fat, cardiac muscle, and skeletal muscle breaks down TGs into free FA and glycerol
30
what is lecithin-cholesterol acyltransferase (LCAT)?
enzyme on LDL and HDL esterfies free cholesterol to form cholesterol esters for HDL transport
31
what is cholesterol ester transfer protein (CETP)?
protein in HDL allows HDL to transfer cholesterol esters to other lipoproteins in exchange for TGs
32
what is the major source of cholesterol?
liver synthesis
33
what ratio is associated with an increased risk of CVD?
greater than 4.5 of total cholesterol to HDL
34
what are the diseases associated with hyperlipoproteinemia?
atherosclerosis premature coronary artery disease stroke (neurologic disease)
35
what are the diseases associated with hyperTGemia?
pancreatitis xanthomas (raised, waxy skin lesions) increased risk of CHD
36
what is atherosclerosis?
excess accumulation of cholesterol in the form of LDL in vascular smooth muscle which causes accumulated plaques
37
what are the goals of therapy for hyperlipidemia?
reduce reabsorption of excreted bile acids decrease secretion of VLDL from liver decrease synthesis of cholesterol increase liver LDL receptor number increase hydrolysis of lipoprotein TG
38
what is % reduction in incidence of CHD compared to reduction in cholesterol levels?
for every 10% reduce in cholesterol levels, theres a 10-30% reduction in CHD risk
39
what are the drug classes that target high cholesterol?
bile acid binding resins inhibitors of cholesterol absorption inhibitors of cholesterol synthesis PCSK9 inhibitors MTTP inhibitors
40
what are drugs that target high TGs?
fibrates niacin omega 3 FA
41
what is MOA of BARs?
inhibit reabsorption of bile acids from intestine done by binding bile acids to form insoluble complex excreted in feces up regulate LDL receptors in liver
42
what is the structure of BARs?
large molecular weight polymers (resins) that exchange chloride ion for bile acids
43
what drugs are BARs?
cholestyramine (questran) colestipol (colestid)
43
what is the % reduction in LDL for BARs?
20% but may increase HDL and TG
43
what is the indication of BARs?
primary hypercholesterolemia
43
what are counseling points of BARs?
take before meals high fiber diet and water helps resolve side effects
44
what are the SE of BARs?
constipation bloating
45
what drugs absorptions are influenced by BARs?
acetaminophen zetia thiazides warfarin digoxin fibrates OCs corticosteroids TZDs
46
what is zetia?
cholesterol and phytosterol absorption inhibitor that inhibits NPC1L1
47
what is NPC1L1
neimann-pickC1-like1 transporter expressed on apical surface of enterocytes in the small intestine moves free FA from the lumen of the gut or bile into enterocytes of hepatocytes
48
what is the indication of zetia?
reduction of LDL levels used in combination with statins
49
what is % reduction in LDL levels of taking zetia?
17% enhances statin action up to 20%
50
what are the SE of zetia?
generally well-tolerated with a low incidence of liver/skeletal muscle damage
51
what drugs are HMG-CoA reductase inhibitors?
fluvastatin (lescol) rosuvastatin (crestor) atorvastatin (lipitor) lovastatin (mevacor) simvastatin (zocor) pravastatin (pravachol) pitavastatin (livalo)
52
what statins are prodrugs?
lovastatin simvastatin
53
what is the MOA of statins?
competitively inhibits HMG-CoA reductase up-regulates LDL receptors enables more LDL to be delivered to liver thus reducing cholesterol
54
what about statins structure is relavant?
they are structurally similar to HMG-CoA
55
what is HMG-CoA reductase?
rate-limiting enzyme in cholesterol biosynthesis
56
what is SREBP?
sterol regulatory element binding protein transcription factor that up-regulates the expression of gene encoding the LDL receptor
57
what is SCAP?
SREBP cleavage activating protein binds cholesterol and acts as a sterol sensor
58
what is the indication of statins?
hypercholesterolemia (elevated LDL with slightly elevated TGs) used immediately after an MI regardless of lipid levels
59
what is the % in LDL, TG, and HDL due to statins?
20-60% reduction in LDL 10-33% reduction in TG 5-10% increase in HDL
60
when should short half-life statins be administered?
in the evening to inhibit nocturnal cholesterol synthesis
61
what statins have short half-lives?
IR fluvastatin IR lovastatin simvastatin
62
what statins are metabolized by CYP3A4?
lovastatin simvastatin atorvastatin
63
what drugs interact with statin and CYP3A4?
macrolide antibiotics cyclosporine ketoconazole grape fruit juice
64
how competing CYP3A4 drugs interact with statins?
cause statins to accumulate
65
what statins are metabolized by CYP2C9?
fluvastatin rosuvastatin
66
what drugs are CYP2C9 inhibitors that interact with statins?
cimetidine metronidazole amiodarone
67
how does CYP2C9 inhibitors interact with statins?
increasing plasma levels of statins
68
what is the metabolism of pravastatin?
sulfation most excreted unchanged
69
what is the metabolism of pitavastatin?
enterohepatic recirculation most excreted unchanged in bile
70
what is the SE of statins?
skeletal muscle effects with renal dysfunction myoglobinuria hepatotoxicity increased incidence of T2DM
71
what should be monitored with statins
serum creatine phosphokinase (CPK) and serum transaminase activity
72
when is the incidence of rhabdomyolysis increased?
co-administration of statin and CYP inhibitors or gemfibrozil
73
what drugs are used adjacent to statins?
bempedoic acid PCSK9 inhibitors
74
what is bempedoic acid?
nexletol ACL inhibitor that reduces serum LDL and total cholesterol levels when added to statin therapy used in patients with heterozygous familial hypercholesterolemia (HeFH) or established ASCVD
75
what is ACL?
ATP-citrate lyase inhibitor enzyme upstream of HMG-CoA reductase in the cholesterol synthetic pathway
76
what is SE of bempedoic acid?
hyperuricemia gout --> due to OAT2 inhibition in renal tubules
77
what is the metabolism of bempedoic acid?
metabolized by glucuronidation and excreted via kidneys
78
what is half life of bempedoic acid?
21 hours (so take 1QD PO)
79
what is PCSK9?
proprotein convertase subtilisin kexin type 9 serin protease that promotes degradation of LDL receptors in the liver
80
what drugs are PCSK9 inhibitors?
alirocumab (praluent) evolocumab (repatha) inclisiran (leqvio)
81
how do praluent and repatha function?
human IgG antibodies against PCSK9 increase LDL-R number and reduce serum LDL-C levels
82
what is the indication of praluent and repatha?
adjunct to diet and maximally tolerated statin therapy in patients with established ASCVD, HeFH, and HoFH
83
what is inclisiran?
siRNA hybridizes PCSK9 mRNA directs degradation in hepatocytes lowers LDL cholesterol
84
what is the indication of inclisiran?
adjunct to statins in HeFH and ASCVD
85
what is SE of inclisiran?
injection site reaction arthralgia
86
what drugs are used to lower serum cholesterol in patients with HoFH?
juxtapid (lomitapide) mipomersen (kynamro) evinacumab (evkeeza)
87
what is juxtapid?
lomitapide MTTP inhibitor that inhibits the assembly of ApoB containing lipoproteins in the liver and intestine
88
what is the indication of juxtapid?
adjunct to other treatments in patients with HoFH
89
what is the SE of juxtapid?
risk of liver damage
90
what is the indication of mipomersen?
adjunct to other treatments for patients with HoFH
91
what is the SE of mipomersen?
risk of liver damage risk of hepatic steatosis
92
what is evinacumab?
evkeeza antibody that increases LPL and endothelial lipase (EL) activity through preventing ANGPTL3 mediated inhibition lowers LDL cholesterol
93
what is the indication of evinacumab?
treatment of HoFH
94
what are fibric acid derivatives?
molecules that bind to PPAR-a regulate gene transcription along with the retinoic acid receptor (RXR)
95
what drugs are fibric acid derivatives?
clofibrate gemfibrozil fenofibrate ciprofibrate bezafibrate
96
what is the % changes of LDL, TGs, and HDLs due to fibric acid derivatives?
6-20% reduction in serum LDL 35-53% reduction in serum TGs 15-30% elevation of HDL
97
what are the indications of fibric acid derivatives?
hypertriglyceridemia with predominant VLDL and second-line for mixed hyperlipidemia
98
what are the SE of fibric acid derivatives?
gallstones rhabdomyolysis use in caution with statins
99
what is the main drug-drug interaction of fibric acid derivatives?
potentiate warfarin effects
100
what is niacin?
vit B3 (nicotinic acid) can lower serum lipids at high doses (1-3g/day)
101
what are changes that occur in lipids due to niacin?
reduce serum TGs increase LPL activity --> increase clearance of VLDL decrease hepatic VLDL production may significantly reduce serum LDL and TGs increase HDL levels
102
what are the targets of niacin?
adipose tissue liver macrophages
103
what is the MOA of niacin in adipose tissue?
inhibits TG lipolysis by hormone-sensitive lipase via activation of GPR109A decreases FA transport to liver
104
what is the MOA of niacin in liver?
inhibits FA synthesis and esterification --> reducing TG export via VLDL reduces clearance of apoA-I but not CE --> increasing HDL levels and reverse transport
105
what is the MOA of niacin in macrophages?
increase expression of CD36 and ABCA1 decreases the CE content via HDL-mediated reverse transport
106
what is the indication of niacin?
mixed hyperlipidemias hyperTGemia by 25-30% with risk of pancreatitis raising HDL levels by 15-35% in combination with resin drugs or statins to treat hyperlipidemia
107
what is the SE of niacin?
marked vasodilation (cutaneous flushing) itching tingling of upper body headache hepatotoxicity
108
what mediates the initial SE of niacin?
prostaglandins treat with ibuprofen or aspirin

Therapeutics 2 - Exam 5 (14 decks)

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