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1. Cardiovascular > Lipid Drugs > Flashcards

Lipid Drugs Flashcards

1
Q

What are transported in blood within lipoproteins?

A

Non polar lipids

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2
Q

Give some examples of non polar lipids?

A

cholesterol esters and triglycerides

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3
Q

What do lipoproteins consist of?

A

hydrophobic core - containing esterified cholesterol and triglycerides
hydrophilic coat - comprising a monolayer of amphipathic cholesterol, phospholipids and one, or more, apoproteins (apo)

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4
Q

What do HDL particles contain?

A

apoA1 and apoA2

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5
Q

What do LDL particles contain?

A

apoB-100

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6
Q

What do Very-low density lipoprotein (VLDL) particles contain?

A

apoB-100

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7
Q

What do Chylomicrons contain?

A

apoB-48

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8
Q

What do apoB containing lipoproteins deliver and to where?

A

triglycerides

- to muscle for ATP biogenesis and adipocytes for storage

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9
Q

Where are Chylomicrons formed and what do they transport?

A

formed in intestinal cells

transport dietary triglycerides (exogenous pathway)

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10
Q

Where are VLDL particels formed and what do they transport?

A

formed in liver cells

transport triglycerides synthesised in that organ (endogenous pathway)

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11
Q

Name the 3 main steps of the ApoB-containing liposomes life cycle.

A
  1. Assembly
  2. Intravascular metabolism
  3. Receptor Mediated clearance
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12
Q

Describe the assembly step of VLDL particles.

A

VLDL particles containing triglycerides are assembled in liver hepatocytes from free fatty acids derived from

  1. adipose tissue (particularly during fasting)
  2. de novo synthesis
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13
Q

Describe the assembly step of Chylomicrons.

A

In the endoplasmic reticulum in the Enterocyte, triglycerides bind with apoB-48 and undergo lipidation, by the Microsomal triglyceride transfer protein. This then happens again and then the chylomicron leaves, following the addition of a second apoprotein apoA1 and enters lymphatics.

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14
Q

How are Chylomicrons and VLDLs activated?

A
  • transfer of apoCII from HDL proteins
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15
Q

What are Lipoprotein lipase (LPL)?

A

lipolytic enzyme associated with the endothelium of capillaries in adipose and muscle tissue

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16
Q

What is the intravascular metabolism of ApoB-containing lipoprotiens?

A
  • ApoCII facilitates binding of chylomicrons and VLDL particles to LPL
  • LPL hydrolyses core triglycerides to free fatty acids and glycerol which enter tissues
  • Particles depleted of triglycerides are now called chylomicron and VLDL remnants
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17
Q

What is the mechanisms of clearance for ApoB-containing lipoproteins?

A

LPL causes chylomicrons and VLDL particles to become relatively enriched in cholesterol due to triglyceride metabolism
Chylomicrons and VLDL dissociate from LPL
ApoCII is transferred to HDL particles in exchange for apoE which is a high affinity ligand for receptor mediated clearance. Particles are now remnants
Remnants return to the liver and are further metabolised by hepatic lipase
All apoB48-containing remnants and 50% of apo100 containing-remnants are cleared by receptor-mediated endocytosis into hepatocytes
Remaining apoB100-containing remnants loose further triglyceride through hepatic lipase, become smaller and enriched in cholesteryl ester and via intermediate density lipoproteins (IDL) become LDL particles lacking apoE and retaining solely apoB100

18
Q

What does the clearance of LDL particas depend on?

A

LDL receptor expressed by the liver and other tissues. Clearance by liver is most important

19
Q

What does cellular uptake of LDL particles occur by?

A

via receptor-mediated endocytosis

20
Q

What does cholesteryl ester release by hydrolysis?

A

cholesterol

21
Q

What does released cholesterol cause?

A
  • inhibition of HMG-CoA reductase which is the rate limiting enzyme in de novo cholesterol synthesis
  • down regulation of LDL receptor expression
  • storage of cholesterol as cholesterol ester
22
Q

What does an atheromatous plaque consist of?

A

lipid core - product from dead foam cells

firbous cap - smooth muscle cells and connective tissue

23
Q

What is the role of HDL cholesterol?

A

removing excess cholesterol from cells by transporting it in plasma to the liver (reverse cholesterol transport)

24
Q

Where is HDL formed and as what?

A

liver

initially as ApoA1 in association with a small amount of surface phospholipid and unesterified cholesterol (pre–HDL)

25
Q

What mediates transfer of cholesteryl esters from HDL to VLDL and LDL?

A

cholesterol ester transfer protein (CETP)

26
Q

When does primary dayslipidaemia occur?

A

combination of diet and genetic factors

27
Q

When does secondary dayslipidaemia occur?

A

consequence of diseases

e.g. type II diabetes, hypothyroidism, alcoholism, liver disease

28
Q

How is the Frederickson Classification of Primary Dyslipidaemia and Drug Treatment graded?

A 
I
IIa
IIb
III
IV
V
29
Q

Give 2 examples of Statins

A

Simvastatin

Atorvastatin

30
Q

What do statins reduce?

A

LDL

31
Q

What are statins competitive inhibitors of?

A

3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase

32
Q

What is HMG-CoA?

A

rate limiting step in cholesterol synthesis in hepatocytes

33
Q

What does a decrease in hepatocyte cholesterol synthesis cause?

A

compensatory increase in LDL receptor expression and enhanced clearance of LDL

34
Q

What do Fibrates decrease and increase?

A

Decreases - triglycerides and LDL

Increases - HDL

35
Q

How do Fibrates act?

A

they are agonists of a nuclear receptor (PPAR) to enhance the transcription of several genes, including that encoding LPL

36
Q

What can statins and fibrates cause?

A

myositis

37
Q

What do Bile acid binding resins cause?

A

the excretion of bile salts resulting in more cholesterol to be converted to bile salts

  • decreased triglyceride absorption
  • increased LDL receptor expression
38
Q

How do Bile acid binding resins act?

A

by interrupting enterohepatic recycling

- prevent the reabsorption of bile salts

39
Q

Examples of bile acid binding resins?

A

colestyramine, colestipol, colsevelam

40
Q

Name a drug that inhibits cholesterol absorption?

A

Ezetimibe

41
Q

How does Ezetimibe act?

A

Inhibits Niemann-Pick C1 like-1 (NPC1L1) transport protein in enterocytes of the duodenum, reducing the absorption of cholesterol

42
Q

When is Ezetimibe used?

A
  • in combination with statins when statins alone dont achieve a sufficient response

1. Cardiovascular (30 decks)

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