Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Med Chem 7 > Antilipidemics (3) > Flashcards

Antilipidemics (3) Flashcards

(60 cards)

Start Studying
1
Q

What are aryloxyisobutyric acids?

A

fibric acids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

fibrates overall effect

A
  • decrease plasma cholesterol decrease total lipid levels
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

fibrates MOA

A
  • originally unknown - activate PPAR
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Where does fibrates act?

A

before mevalonate formation accelerates turnover of removal of cholesterol from liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

T/F clofibrate is still used today

A

False

  • discontinued due to adverse effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

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

A

true!

  • myopathy
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Fenofibrate overall effects

A

Decreases LDL and VLDL

Increase HDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the carrier molecule for VLDL?

A

apolipoprotein B

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

How do fibrates increase hydrolysis of TGs?

A

induction of LPL

reduction of apoC-III expression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

(SAR) what is required in fibrates?

A

Requires acid (COOH) or ester (prodrug)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

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

A

Add Cl on aromatic ring

di-Cl on cyclopropyl ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

fibrates metabolism

A

excreted as glucuronides in urine

bound to plasma proteins because of acid groups

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

How does this get metabolized?

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

How does this get metabolized?

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Fibrates uses

A
  1. hypertriglycemia
  2. familial combine hyperlipidemia
  3. dysbeta lipoproteinemia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Fibrates cause the urinary loss of _____

A

betadine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

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

A

osmoregulation

methyl

lipid partitioning

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

statins + fibrates

A

increase myopathy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

insulin + clofibrate

A

increase insulin effect that results in hypoglycemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

fenofibric acid + simvastatin in diabetic patients

A

may increase cardiovascular risk in females

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
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
false! There has been renewed interest!
26
ACCORD study
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
Because of ACCORD study, the FDA is requiring what?
more clinical trials to evaluate cardiovascular effects of fenofibrate in patients who already take statins
28
cholesterol absorption inhibitors overal effect
inhibit LDL formation
29
Where do plant based sterols and stanols come from?
diet or supplement
30
Plant based sterols interfere with what? Why?
uptake of dietary and biliary cholesterol from intestinal tract Not fully understood
31
T/F plant sterols are virtually unabsorbable
false! stanols
32
T/F stanols are more ideal as hypocholesterolemic agents than sterols
true! because unabsorbable
33
Sterol or stanol?
stanol
34
Sterol or stanol?
sterol
35
the ____ of plant stanols has allowed their incorporation into various foods such as ____ without changing taste and texture
esterfication margarine
36
Plant stanol esters at a level of _____ have been shown to reduce LDL cholesterol by \_\_\_\_% without side effects
2-3g/d 10-15%
37
Plant ____ esters appear to be helpful dietary adjunct to a prudent diet to lower cholesterol
stanol
38
(SAR) The addition of ____ or ____ group on side chain of cholesterol result in poor intestinal absorption
methyl or ethyl
39
(SAR) the longer the side chain of sterol, the ___ it is abosrbed. why?
less absorbed because of increased hydrophobicity
40
(SAR) ____ of plant sterols to corresponding stanol renders them virtually unabsorbable
hydrogenation
41
Synthetic cholesterol absorption inhibitors overall effect
- reduce contribution of dietary and biliary cholesterol - reduce flux of cholesteryl esters into VLDL particles
42
With synthetic cholesterol absorption inhibitors there is a ____ repspone by the liver. Why?
compensatory to compensate for loss of cholesterol returning to liver from intestine \*\*partially offsets impact of cholesterol absorption inhibitors on plasma LDL
43
The effect of inhibiting cholesterol abosrption can be maximized by adding a \_\_\_\_
statin
44
What is an example of a synthetic cholesterol absorption inhibitor?
ezetimibe
45
How does ezetimibe work?
- inhibits absorption of cholesterol from SI - decrease amount of cholesterol in liver cells - combined with statins
46
(SAR) What is required in cholesterol absorption inhibitor?
azetidinone ring
47
(SAR) \_\_\_C chain length is important in cholesterol absorption inhbitor
3C chain
48
(SAR) sterochemistry of A or B is important?
A B not important: Mono \>\>di substitution
49
What metabolism occurs at A?
benzylic oxidation
50
What metabolism occurs at B?
demethylation
51
What metabolism occurs at C?
demethylation
52
What metabolism occurs at D?
ring opening
53
What metabolism occurs at E?
pendant phenyl oxidation
54
What does the group at A do?
block oxidation
55
What does the group at B do?
steroselective oxidation
56
What does the group at C do?
aklylated
57
What does the group at D do?
oxidation/demethylation blocked
58
Vytorin is a combo of what drugs?
simvastatin and ezetimibe
59
Why is vytorin not really used?
little difference between vytorin and simvastatin - little effect on buildup of plaque in arteries
60
vytorin overall effect
decrease LDL

Med Chem 7 (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions