Antihyperlipidemics Flashcards Preview

Year 2 Pharmacology > Antihyperlipidemics > Flashcards

Flashcards in Antihyperlipidemics Deck (35):
1

what is the lowest density lipoprotein?

chylomicron

2

what are the roles of the apolipoproteins?

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

3

what is the role of NPC1L1?

cholesterol uptake

4

which drug inhibits the NPC1L1 enzyme?

ezetimibe

5

what is the role of acetyl CoA cholesterol acyltransferase?

converts cholesterol to cholesterol ester

6

what is the role of diglyceride acyltransferase?

converts monoglycerides to TGs

7

where are chylomicrons associated with the B28 apoprotein?

intestine

8

where do chylomicrons associate with apoC2 and apo3?

lymphatic system

9

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

capillaries (via apoC2)

10

what is the importance of apoE?

allows chylomicron remnants to be taken back up by liver

11

what is the importance of apoB100 for VLDL particles?

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

12

what is reverse cholesterol transport?

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

13

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

1. HDL, chylomicrons
2. structural for HDL, activates LCAT, SRB1 ligand

14

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

1. HDL, chylomicrons
2. structural for HDL

15

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

1. chylomicrons, remnants
2. structural

16

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

1. VLDL, LDL, IDL
2. structural for above, ligand for LDL

17

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

1. chylomicrons, VLDL, HDL
2. COFACTOR FOR LIPOPROTEIN LIPASE

18

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

1. chylomicron, VLDL, IDL, HDL
2. ligand for LDL and remnant receptors

19

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

1. decrease in lipoprotein lipase activity
2. increased chylomicrons, VLDL

20

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

1. impaired removal of VLDL and/or chylomicrons
2. increased VLDL (moderate), VLDL AND chylomicrons (severe)

21

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

1. increased VLDL production by liver
2. increased VLDL, LDL

22

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

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

23

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

1. LDLr impairments, high fat diet, inactivity
2. increased LDL

24

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

1. mutation in apoB100 - impaired endocytosis of LDL
2. increased LDL

25

what do the fibrates do? what is the MOA?

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

26

what are the fibrate drugs?

1. gemfibrozil
2. fenofibrate

27

the fibrates are good for what condition?

hypertriglyceridemia

28

what are the bile acid binding resins?

1. cholestyramine
2. colesevelam
3. colestipol

29

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

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

what does niacin do? what is the MOA?

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

what are the side effects of niacin?

1. cutaneous flushing and itching
2. hyperuricemia (gout susceptible)

32

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

1. ezetimibe
2. inhibits nieman pick C1 like protein

33

how do the statins work? what is the MOA?

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

34

what are the most potent statins?

atorvastatin and rosuvastatin

35

what are the adverse effects of the statins?

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

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