Flashcards in Statins (drugs to treat hyperlipidemia) Deck (66)
What is the most associated species with hyperlipidemia?
LDL (not triglycerides)
What are lipoprotein particles composed of?
1) lipid membranes
2) hydrophobic core
How do LDL differ from HDL?
LDL is 60% cholesterol while HDL is 20% cholesterol
What enzyme makes cholesterol?
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
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
How might HDL prevent atherosclerosis?
HDL promote the REVERSE cholesterol transport (from periphery back to liver where it can be secreted as bile)
What is target LDL?
What is target HDL?
What is target triglyceride?
What 4 drug classes inhibit LDL?
2) bile acid-resins
3) chol. absorption inhibs
4) PCSK9 inhibitors
What is the NUMBER ONE causative role of atherosclerosis?
high levels of LDL
What 2 drug classes inhibit triglycerides?
What is the treatment for moderate hypercholesterolemia with LOW cv risk?
What is the LDL level that indicates statins?
What are the 6 statins?
What are the 3 bile acid binding resins?
What is the primary clinical effect of statins?
(moderate reduction in triglycerides and increase in HDL)
What is the MOA of statin?
as an analog of the HMG CoA substrate, they inhibit HMG CoA reductase
What is the role of HMG CoA reductase?
to make cholesterol
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
What turns SREBP on?
decreased cholesterol levles
What 2 ways do statins decrease cholesterol?
1) reduced cholesterol formation
2) increase LDL receptor expression to sop up serum LDL
True or false: statins are effective at reducing CHD risk irrespective of initial baseline LDL
TRUE (can prevent primary and secondary CHD)
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)
What is the main side effect of statins/
Rhabdomyolysis (also causes myalgia)
Which statin is the best choice for minimizing drug interactions?
Where are statins absorbed?
intestine (metabolized by CYP3A4)
How are statins taken up into the liver?