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Med Chem 7 > Antilipidemics (3) > Flashcards

Antilipidemics (3) Flashcards

1
Q

What are aryloxyisobutyric acids?

A

fibric acids

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2
Q

fibrates overall effect

A
  • decrease plasma cholesterol decrease total lipid levels
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3
Q

fibrates MOA

A
  • originally unknown - activate PPAR
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4
Q

Where does fibrates act?

A

before mevalonate formation accelerates turnover of removal of cholesterol from liver

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5
Q

T/F clofibrate is still used today

A

False

  • discontinued due to adverse effects
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6
Q

T/F FDA withdrew approval of fenofibrate with statins used together

A

true!

  • myopathy
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7
Q

Fenofibrate overall effects

A

Decreases LDL and VLDL

Increase HDL

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8
Q

What is the carrier molecule for VLDL?

A

apolipoprotein B

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9
Q

Fibrates regulate the transcription of the major ____ apolipoproteins (___ & ____). As a result, partially mediates the ____ effects of HDL levels

A

HDL

ApoA-I

apoA-II

Inductive

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10
Q

What are the 3 ways fibrates can initiate the hypotriglyceridemic actions?

A
  1. incrase hydrolysis of plasma TG
  2. stimulate cellular FA uptake and conversion to acyl-CoA derivatives
  3. decrease synthesis of FA and TG & decreased production of VLDL
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11
Q

How do fibrates increase hydrolysis of TGs?

A

induction of LPL

reduction of apoC-III expression

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12
Q

How do fibrates stimulate FA uptake and conversion to acyl-CoA derivatives

A

due to increased expression of genes for FA transport protein and acyl-CoA synthetase

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13
Q

(SAR) what is required in fibrates?

A

Requires acid (COOH) or ester (prodrug)

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14
Q

(SAR) what are 2 ways to increase t1/2 in fibrates?

A

Add Cl on aromatic ring

di-Cl on cyclopropyl ring

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15
Q

fibrates metabolism

A

excreted as glucuronides in urine

bound to plasma proteins because of acid groups

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16
Q

How does this get metabolized?

A
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17
Q

How does this get metabolized?

A
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18
Q

Fibrates uses

A
  1. hypertriglycemia
  2. familial combine hyperlipidemia
  3. dysbeta lipoproteinemia
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19
Q

Clofibrate had increased mortality from non-coronary heart diseases

A
  • malignancy
  • gall bladder disease
  • pancreatitis

**also seen with other compounds of this class

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20
Q

Fibrates cause the urinary loss of _____

A

betadine

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21
Q

Betadine is an essential metabolite that is involved in _____, in ____ group metabolism and affects _____ in body

A

osmoregulation

methyl

lipid partitioning

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22
Q

statins + fibrates

A

increase myopathy

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23
Q

insulin + clofibrate

A

increase insulin effect that results in hypoglycemia

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24
Q

fenofibric acid + simvastatin in diabetic patients

A

may increase cardiovascular risk in females

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25
Q

T/F because most of the cardiac risk remains despite successful statin therapy, there has not been a renewed interest in fibrate therapy for persisting hyperlipidemia

A

false! There has been renewed interest!

26
Q

ACCORD study

A

fenofibrate + simvastatin DID NOT reduce rate of fatal cardiovascular events

**do not support routine combo of these two!

Major risk for those with T2D

27
Q

Because of ACCORD study, the FDA is requiring what?

A

more clinical trials to evaluate cardiovascular effects of fenofibrate in patients who already take statins

28
Q

cholesterol absorption inhibitors overal effect

A

inhibit LDL formation

29
Q

Where do plant based sterols and stanols come from?

A

diet or supplement

30
Q

Plant based sterols interfere with what?

Why?

A

uptake of dietary and biliary cholesterol from intestinal tract

Not fully understood

31
Q

T/F plant sterols are virtually unabsorbable

A

false! stanols

32
Q

T/F stanols are more ideal as hypocholesterolemic agents than sterols

A

true! because unabsorbable

33
Q

Sterol or stanol?

34
Q

Sterol or stanol?

35
Q

the ____ of plant stanols has allowed their incorporation into various foods such as ____ without changing taste and texture

A

esterfication

margarine

36
Q

Plant stanol esters at a level of _____ have been shown to reduce LDL cholesterol by ____% without side effects

A

2-3g/d

10-15%

37
Q

Plant ____ esters appear to be helpful dietary adjunct to a prudent diet to lower cholesterol

38
Q

(SAR) The addition of ____ or ____ group on side chain of cholesterol result in poor intestinal absorption

A

methyl or ethyl

39
Q

(SAR) the longer the side chain of sterol, the ___ it is abosrbed. why?

A

less absorbed

because of increased hydrophobicity

40
Q

(SAR) ____ of plant sterols to corresponding stanol renders them virtually unabsorbable

A

hydrogenation

41
Q

Synthetic cholesterol absorption inhibitors overall effect

A
  • reduce contribution of dietary and biliary cholesterol
  • reduce flux of cholesteryl esters into VLDL particles
42
Q

With synthetic cholesterol absorption inhibitors there is a ____ repspone by the liver. Why?

A

compensatory

to compensate for loss of cholesterol returning to liver from intestine

**partially offsets impact of cholesterol absorption inhibitors on plasma LDL

43
Q

The effect of inhibiting cholesterol abosrption can be maximized by adding a ____

44
Q

What is an example of a synthetic cholesterol absorption inhibitor?

45
Q

How does ezetimibe work?

A
  • inhibits absorption of cholesterol from SI
  • decrease amount of cholesterol in liver cells
  • combined with statins
46
Q

(SAR) What is required in cholesterol absorption inhibitor?

A

azetidinone ring

47
Q

(SAR) ___C chain length is important in cholesterol absorption inhbitor

48
Q

(SAR) sterochemistry of A or B is important?

A

A

B not important: Mono >>di substitution

49
Q

What metabolism occurs at A?

A

benzylic oxidation

50
Q

What metabolism occurs at B?

A

demethylation

51
Q

What metabolism occurs at C?

A

demethylation

52
Q

What metabolism occurs at D?

A

ring opening

53
Q

What metabolism occurs at E?

A

pendant phenyl oxidation

54
Q

What does the group at A do?

A

block oxidation

55
Q

What does the group at B do?

A

steroselective oxidation

56
Q

What does the group at C do?

57
Q

What does the group at D do?

A

oxidation/demethylation blocked

58
Q

Vytorin is a combo of what drugs?

A

simvastatin and ezetimibe

59
Q

Why is vytorin not really used?

A

little difference between vytorin and simvastatin

  • little effect on buildup of plaque in arteries
60
Q

vytorin overall effect

A

decrease LDL

Med Chem 7 (9 decks)

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