Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Med Chem 7 > Antilipidemics (2) > Flashcards

Antilipidemics (2) Flashcards

You may prefer our related Brainscape-certified flashcards:
Periodic Table flashcards Chemistry 101 flashcards AP® Chemistry flashcards Organic Chemistry 101 flashcards
1
Q

T/F cholesterol levels and statins are still controversial with suggestions that lower the better

A

true

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

Even at levels within normal range, statins may cause ______

A

endothelial dysfunction

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

Four groups targeted for statins

A
  1. people who already have heart disease
  2. LDL levels >190
  3. T2D between 40-75
  4. People 40-75 who have estimated 10 year risk of heart attack or stroke of 7.5 or higher
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What % of men are recommended to take statins?

A

44%

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

What % of women of women are recommended to take statins

A

15%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is another name for the HMG-CoA reductase pathway?

A

mevolonate pathway

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

Statins inhibit what?

A

HMG-CoA reductase

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

What animal model is indicated to be the best?

A

dog especially when pretreated with cholestyramine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What was the first statin created, but never made it to the market?

A

Mevastatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Lovastatin metabolism

A

by CYP3A4 no grapefruit juice

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

which statin is cleared by the kidneys?

A

pravastatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Fluvastatin metabolism

A

multiple CYP enzymes envolved in metabolism (2C9, 3A4, 2C)

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

T/f generally the more CYPs metabolized the less DDI

A

true

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

T/F fluvastatin has more DDI than other statins

A

false

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

what is the world’s best selling medication?

A

atorvastatin

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

Why was cerivastatin voluntarily withdrawn from the market?

A

fatal rhabdomyolysis

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

what is considered a super statin?

A

rosuvastatin

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

Which statin has a FDA advisory for east asian patients and why?

A

rosuvastatin risk of myopathy due to how the drug is processed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Pitavastatin metabolism

A

glucurondiation CYP450 (NOT 3A4)

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

Which statin has neutral effect on glucose regulation?

A

pitavastatin

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

Which statin appears to have improved tolerability in its metabolic profile?

A

pitavastatin

22
Q

All statin mimic what?

A

HMG-CoA (S) 3-hydroxy-3-methylgluteryl CoA

23
Q

statins are what kind of inhibitors with human enzyme

A

co-crystallized

24
Q

T/f due to statins flexibility, they bind not only to HMG-binding pocket but also part of the CoA binding surface

A

true

25
Q

T/F not all statins bind to the same binding pocket

A

false! All fill same pocket

26
Q

The 6 fluoro ring of statins stacks between what?

A

Arg590 and phenyl ring

27
Q

The 6 fluoro ring of statins has polar interaction between what?

A

N of Arg590 and fluorine

28
Q

the sulfonamide of rosuvastatin has polar interaction with____

A

Arg568

29
Q

the polar side chain of atorvastatin what interactions?

A

H bond with Ser565

30
Q

The _____ ring system is necessary to anchor statins to active site (SAR)

A

decalin **replacing with cyclohexane ring reduces activity 10,000 fold

31
Q

(SAR) t/f replacing ester with ether increases activity of statins

A

false!! decreases activity

32
Q

(SAR) t/f stereochemistry on ester side chain of statins is important

A

false! not important

33
Q

(SAR) ____ substitution (R2) increases activity

A

methyl

34
Q

(SAR) Introduction of ____ increases hydrophilicity and may enhance cellular _____

A

B-OH (above plane R1) specificity

35
Q

(SAR) W,X,Y can either be ____ or _____ and ___ or ____ membered ring

A

C or N

5 or 6

36
Q

(SAR) t/f p-fluorine cannot be coplanar with central aromatic ring

A

true!

decreases activity

37
Q

(SAR) substiution of ____ groups enhances lipophilicity and inhibitor activity

A

aryl

38
Q

T/F cats are more sensitive to statins

A

False

Dogs!

39
Q

Statins metabolism

A

extensive 1st pass

excreted in bile

*lactone must be hydrolyzed for activity

**species differences

40
Q

What are the 3 ways statins can be metabolized?

A
  1. 6 B-hydroxy
  2. 3 hydroxy
  3. 6 exomethylene
41
Q

How is atorvastatin metabolized?

Active or inactive?

A

o,p hydroxylation

active

42
Q

How is fluvastatin metabolized?

Active or less active?

A

hydroxylation

active

43
Q

How is cervastatin metabolised?

Active or less active?

A

demethylation

less active

44
Q

T/F you can use statins with bile acid sequestrants and niacin

A

True, but not multiple statins at the sasme time

45
Q

T/F statins are not used in pregnant or lactating women

A

true

46
Q

statins use

A

hypercholesteremia

familial hyperlipidemia

47
Q

ADE statins

A

most directly related to their biochemical MOA and are result of potent and reversible inhibition of an enzyme involved in homeostasis

48
Q

toxicity studies show targets of statins are

A

liver

kidney

muscle

nonglandular stomach

lymph

eyes, CNS, testes

49
Q

Type I vs Type II statin

A

Type I: declain ring

Type II: fluorophenyl group

50
Q

What is the enzyme?

A

HMG CoA reductase

51
Q

How did lovastatin differ from mevastatin?

A

Lovastatin: CH3

Mevastatin: H

52
Q

What are most statins CI?

A

pregnancy

breastfeeding

liver diseaee

Med Chem 7 (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions