Pharmacology: Lipid Metabolism Flashcards

1
Q

two layers of lipoproteins

A
  1. hydrophobic core (cholesterol and TAGs)

2. hydrophilic coat (phospholipids, cholesterol)

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2
Q

four classes of lipoproteins

A
  • HDL (apoA-I and apoA-II)
  • LDL (apoB-100)
  • VLDL (apoB-100)
  • chylomicrons (apoB-48)
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3
Q

role of apoB-containing lipoproteins

A

deliver TAGs to muscle for ATP and adipocytes for storage

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4
Q

three stages in the lifecycle of apoB-containing lipoproteins

A
  1. assembly
  2. intravascular metabolism
  3. receptor mediated clearance
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5
Q

where are apoB-100 lipoproteins synthesised?

A

liver

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6
Q

where are apoB-48 lipoproteins synthesised?

A

intestine (NPC1L1)

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7
Q

how are chylomicrons and VLDLs activated?

A

apoC-II from HDL

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8
Q

what does apoC-II facilitate?

A

binding of chylomicrons and VLDL to LPL

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9
Q

what does LPL do?

A

hydrolyses TAGs

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10
Q

receptor mediated clearance

A

remnants return to the liver

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11
Q

why is LDL bad cholesterol

A

LDL ix oxidised to OXLDL in the artery which causes migration of monocytes which turn into macrophages and take up OXLDL and form foam cells to make a fatty streak, which stimulates proliferation of smooth muscle and deposition of collagen and formation of a plaque

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12
Q

why is HDL good cholesterol?

A

it transfers excess cholesterol from plasma membrane to the liver which removes cholesterol from the body

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13
Q

two classes of drugs that lower lipids

A
  1. statins

2. fibrates

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14
Q

examples of statins

A

simvastatin

atrovastatin

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15
Q

what are statins first lines for?

A

reducing LDLs

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16
Q

mechanism of action of statins

A

inhibits HMG-CoA which decreases LDL expression and clearance

17
Q

what are statins useless in

A

familial hypercholesterolaemia where LPL receptors are absent

18
Q

adverse of statins

A

myositis

rhabdoymyolosis

19
Q

examples of fibrates

A

bezafibrate

gemifibrozil

20
Q

what are fibrates first line for?

A

reducing TAGs

21
Q

mechanism of action of fibrates

A

agonists of the nuclear receptor PPAR-alpha which enhances transcription of LPL genes

22
Q

adverse of fibrates

A

myositis, rhabdomyolysis, GI symptoms, pruritus and rash

23
Q

two types of drugs that inhibit cholesterol absorption

A
  • bile acid binding resins

- ezetimibe

24
Q

examples of bile acid binding resins

A

colestyramine
colestipol
colsevelam

25
Q

mechanism of action of bile acid binding resins

A

excretion of bile salts increased so there is decreased absorption of TAGs

26
Q

adverse of bile acid binding resins

A

GI tract irritation

27
Q

mechanism of action of ezetimibe

A

inhibits NPC1L1, reducing absorption of cholesterol

28
Q

adverse of ezetimibe

A

diarrhoea
abdominal pain
headaches