Statins (drugs to treat hyperlipidemia) Flashcards Preview

Pharmacology > Statins (drugs to treat hyperlipidemia) > Flashcards

Flashcards in Statins (drugs to treat hyperlipidemia) Deck (66)
Loading flashcards...
1

What is the most associated species with hyperlipidemia?

LDL (not triglycerides)

2

What are lipoprotein particles composed of?

1) lipid membranes
2) hydrophobic core
3) apolipoproteins

3

How do LDL differ from HDL?

LDL is 60% cholesterol while HDL is 20% cholesterol

4

What enzyme makes cholesterol?

HMG-CoA reductase

5

In normal cholesterol states, where does LDL go?

binds to LDL receptor and is degraded in the lysosome into cholesterol which goes to membranes, steroid hormones, bile acids, lipoproteins

6

When does LDL become a problem?

When there is too much of it and it isn't taken up into the cell - stays in blood
- endothelial injury allows entry of LDL
- macrophages take up LDL becoming FOAM cells
- necrosing FOAM cells release cholesterol into matrix making fatty streak

7

How might HDL prevent atherosclerosis?

HDL promote the REVERSE cholesterol transport (from periphery back to liver where it can be secreted as bile)

8

What is target LDL?

9

What is target HDL?

>50mg/dL

10

What is target triglyceride?

11

What 4 drug classes inhibit LDL?

1) statins
2) bile acid-resins
3) chol. absorption inhibs
4) PCSK9 inhibitors

12

What is the NUMBER ONE causative role of atherosclerosis?

high levels of LDL

13

What 2 drug classes inhibit triglycerides?

1) niacin
2) fibrates

14

What is the treatment for moderate hypercholesterolemia with LOW cv risk?

lifestyle change

15

What is the LDL level that indicates statins?

>190mg/dL

16

What are the 6 statins?

atorvastatin
fluvastatin
lovastatin
simvastatin
pravastatin
rosuvastatin

17

What are the 3 bile acid binding resins?

cholestryamin
colestipol
colesevelam

18

What is the primary clinical effect of statins?

REDUCE LDL
(moderate reduction in triglycerides and increase in HDL)

19

What is the MOA of statin?

as an analog of the HMG CoA substrate, they inhibit HMG CoA reductase

20

What is the role of HMG CoA reductase?

to make cholesterol

21

What is the SREBP transcription factor?

a protein that is activated in the face of reduced cholesterol synthesis and works to INCREASE expression of LDL receptor which increases clearance of serum LDL

22

What turns SREBP on?

decreased cholesterol levles

23

What 2 ways do statins decrease cholesterol?

1) reduced cholesterol formation
2) increase LDL receptor expression to sop up serum LDL

24

True or false: statins are effective at reducing CHD risk irrespective of initial baseline LDL

TRUE (can prevent primary and secondary CHD)

25

If you double the dose of statins, do you double the effects?

NO (only increases like 5-6% but significantly increasing it can cause adverse effects)

26

What is the main side effect of statins/

Rhabdomyolysis (also causes myalgia)

27

Which statin is the best choice for minimizing drug interactions?

Pravastatin

28

Where are statins absorbed?

intestine (metabolized by CYP3A4)

29

How are statins taken up into the liver?

OATP2

30

How are statins excreted?

bile and feces