Antihyperlipidemics Flashcards

1
Q

what is the lowest density lipoprotein?

A

chylomicron

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2
Q

what are the roles of the apolipoproteins?

A
  1. cofactors
  2. ligands for receptors
  3. structural stability
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3
Q

what is the role of NPC1L1?

A

cholesterol uptake

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4
Q

which drug inhibits the NPC1L1 enzyme?

A

ezetimibe

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5
Q

what is the role of acetyl CoA cholesterol acyltransferase?

A

converts cholesterol to cholesterol ester

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6
Q

what is the role of diglyceride acyltransferase?

A

converts monoglycerides to TGs

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7
Q

where are chylomicrons associated with the B28 apoprotein?

A

intestine

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8
Q

where do chylomicrons associate with apoC2 and apo3?

A

lymphatic system

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9
Q

where are the chylomicrons broken down to TGs by lipoprotein lipase?

A

capillaries (via apoC2)

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10
Q

what is the importance of apoE?

A

allows chylomicron remnants to be taken back up by liver

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11
Q

what is the importance of apoB100 for VLDL particles?

A

ligand for LDL receptors (important for clearance of cholesterol from circulatory system)

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12
Q

what is reverse cholesterol transport?

A
  1. HDL accepts excess cholesterol from peripheral tissues
  2. HDL is transported to liver where it binds SRB1 via apoA1 and cholesterol esters are selectively delivered to hepatocytes
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13
Q

apoA1 is associated with which lipoproteins? what is its function?

A
  1. HDL, chylomicrons

2. structural for HDL, activates LCAT, SRB1 ligand

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14
Q

apoA2 is associated with which lipoproteins? what is its function?

A
  1. HDL, chylomicrons

2. structural for HDL

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15
Q

apoB48 is associated with which lipoproteins? what is its function?

A
  1. chylomicrons, remnants

2. structural

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16
Q

apoB100 is associated with which lipoproteins? what is its function?

A
  1. VLDL, LDL, IDL

2. structural for above, ligand for LDL

17
Q

apoC2 is associated with which lipoproteins? what is its function?

A
  1. chylomicrons, VLDL, HDL

2. COFACTOR FOR LIPOPROTEIN LIPASE

18
Q

apoE is associated with which lipoproteins? what is its function?

A
  1. chylomicron, VLDL, IDL, HDL

2. ligand for LDL and remnant receptors

19
Q

what is the cause of primary chylomicronemia? how does it manifest?

A
  1. decrease in lipoprotein lipase activity

2. increased chylomicrons, VLDL

20
Q

what is the cause of familial hypertriglyceridemia? how does it manifest?

A
  1. impaired removal of VLDL and/or chylomicrons

2. increased VLDL (moderate), VLDL AND chylomicrons (severe)

21
Q

what is the cause of familial combined hyperlipoproteinemia? how does it manifest?

A
  1. increased VLDL production by liver

2. increased VLDL, LDL

22
Q

what is the cause of familial dysbetalipoproteinemia? how does it manifest?

A
  1. decreased clearance of VLDL, IDL, and chylomicrons due to dysfunction or absence of apoE
  2. increased IDL chylomicrons
23
Q

what is the cause of primary familial hypercholesterolemia? how does it manifest?

A
  1. LDLr impairments, high fat diet, inactivity

2. increased LDL

24
Q

what is the cause of familial ligand defective apoB? how does it manifest?

A
  1. mutation in apoB100 - impaired endocytosis of LDL

2. increased LDL

25
Q

what do the fibrates do? what is the MOA?

A
  1. activate PPAR receptor
  2. increase plasma HDL, lower TGs
  3. increase oxidation of fatty acids
26
Q

what are the fibrate drugs?

A
  1. gemfibrozil

2. fenofibrate

27
Q

the fibrates are good for what condition?

A

hypertriglyceridemia

28
Q

what are the bile acid binding resins?

A
  1. cholestyramine
  2. colesevelam
  3. colestipol
29
Q

what do the bile acid binding resins do? what is the MOA?

A
  1. soak up bile acids in intestine
  2. liver makes more bile acids and uptakes cholesterol to do so
  3. increases LDL receptors - decreases plasma LDL
30
Q

what does niacin do? what is the MOA?

A
  1. decreases VLDL and LDL
  2. increases HDL, decreases plasma free fatty acids which decreases VLDL synthesis by liver
  3. may also decrease plasma plasminogen (anti-thrombosis)
31
Q

what are the side effects of niacin?

A
  1. cutaneous flushing and itching

2. hyperuricemia (gout susceptible)

32
Q

what is the main cholesterol uptake inhibitor drug? what is the MOA?

A
  1. ezetimibe

2. inhibits nieman pick C1 like protein

33
Q

how do the statins work? what is the MOA?

A
  1. inhibits cholesterol synthesis
  2. competitive inhibitor of HMG CoA reductase
  3. increases concentration of LDLr in blood, hepatocytes, and extrahepatic sites
34
Q

what are the most potent statins?

A

atorvastatin and rosuvastatin

35
Q

what are the adverse effects of the statins?

A
  1. liver failure
  2. myopathy
  3. contraindicated during pregnancy