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Flashcards in L24 Deck (32):
1

Receptor for HDL on liver for steroidogenic tissues

SR-B1
Scavenger receptor

2

What drug class is the most effective at reducing LDL

Statins

3

Statin mechanism of lowering cholesterol

X HMG co-reductase
- No cholesterol synthesis
More LDL-R expression b/c less LDL in circulation - sensitizes the system

4

Statin mechanism for CV benefits

Anti-inflam
Anti-thrombogenic

5

How are most statins metabolized? Exceptions?

First pass extraction in liver via CYP enzymes
Except
- Prava
- Rosuva only slightly metab by liver

6

Statin adverse SEs

1. Hepatitis that presents as flu-like sickness
2. Rhabdomyolysis - can progress to kidney failure
3. New onset diabetes
4. Teratogenic - don't give to pregnant women
5. Peripheral neuropathy
6. cP450 drug ints

7

What 2 enzyme levels are you going to monitor for pts on statins

Serum liver transaminases
Creatinine

8

Should you give statins to diabetic pts?

Yes
Higher risk of experiencing a cardiac event or death if diabetic
But benefits >> risk

9

When should pts take their statins?

Before bed
Cholesterol levels highest at night

10

What are the 3 1st gen statins?

Simvastatin
Pravastatin
Lovastatin

11

What are the 2, 2nd gen statins?

Atorvastatin
Rosuvastatin
More potent forms

12

What is the mechanism of bile acid binding resins?

Bile acids contain cholesterol
- Usually recycled to preserve cholesterol stores
Instead, bind them and excrete them
Force the liver to use cholesterol to make more
Less cholesterol in circulation, reflex increase LDL-R expression

13

Which pts should you NOT give bile acid binders to?

High TGs
Bide acid binders also increase VLDL for unknown reasons --> increases TGs

14

Bind acid binder SEs

GI

15

Name the 2 bile acid binding resins

Cholestyramine
Colesevelam

16

Which cholesterol absorption inhibitor do you need to know

Ezetimibe

17

Ezetimibe mechanism

Blocks cholesterol and plant sterol GI absorption via X NPC1L1
Acts on dietary AND biliary cholesterol
Decreases serum:
- Cholesterol
- LDL
No change to TGs

18

How is ezetimibe excreted

Feces - with whatever it bound!

19

Evidence shows ezetimibe acts best when added to which statin specifically

Simvastatin

20

3 PCSK9 inhibitors you need to know

Alirocumab
Evolocumab

21

PCSK9 inhibitor mechanism

PCSK9 = internalization of LDL-R
Give w/ statins b/c when you ↑LDL-R, you also ↑PCSK9 levels

22

What is a gain of function PCSK9 mutation associated with?

FHyperlipidemia

23

What disease is secondarily benefited by ↓LDL

Metabolic syndrome

24

Fibrates mechanism

Ligand for peroxisome proliferator-activated receptor (PPAR)
= nuclear receptors
↓TG + ↑HDL

25

2 fibrates you need to know

Gemfibrozil
Fenofibrate

26

Use of fibrates

BEST method to ↓TGs
↓CV events

27

Which drug interaction should you keep in mind with fibrates?

Warfarin
Adjust dosing since fibrates bind plasma proteins warfarin would otherwise bind

28

Fibrates SEs

GI
↑risk gallstones b/c ↑biliary cholesterol

29

Which drug will give the largest ↑HDL

Nicotinic acid (this is the active form)
Also some ↓LDL & TGs

30

Nicotinic acid mechansim

Activates Niacr1 on adipose tissue
X lipolysis --> no FFAs toliver for TG or VLDL synthesis

31

Is there a benefit to combining niacin w/ statins?

No - niacin goal is not for LDL reduction
Use alone to ↓TGs

32

Niacin SEs

Skin flushing
- Prostaglandin vasodilation of skin
- ↓if use time release forms
Makes diabetes worse