Cholesterol Flashcards
How is Cholesterol made? What increase cholesterol production?
- Made by liver all the time but increases when we eat saturated fat
- Liver uses the Enzyme HMG CO-A to make more cholesterol
Name the 3 different types of cholesterol
VLDL
LDL
HDL
This kind of cholesterol delivers triglycerides to adipose and is linked to CAD/pancreatitis
VLDL
This cholesterol is a bad guy!
-when demand for cholesterol increases, cells increase # of _____ receptors and cell takes in more
LDL!
This cholesterol is good, is associated with the removal of cholesterol, and reduces risk of CAD
HDL
happy
2 strategies to drug therapy for lipid disorders
- decrease LDL
2. decrease triglycerides
The goal of treating lipid disorder is to prevent _____ and ______
Prevent atherosclerosis and CAD
What is the Framingham risk prediction score? What is it based on?
predicts risk of CAD based on Age, gender, total CHO, smoker, HDL, BP
Modifiable changes to prevent CAD/decrease cholesterol?
Diet (low saturated fat) ; exercise; weight control; smoking cessation
Diabetics are at _____ risk for developing CAD
equivalent
Long term concerns for managing high cholesterol?
- Metabolic Syndrome
- Life-long treatment
prototype for HMG-CoA Reductase Inhibitors aka “Statins”
atorvastatin (Lipitor)
Which drug is 1st line therapy for Lipid disorders?
atorvastatin (Lipitor)
HMG-CoA Reductase Inhibitors aka “Statins”
How does atorvastatin (Lipitor) decrease mortality?
better plaque stability, decrease inflammation, slower progression of CAD, improve endothelial BV fxn (dilate better), decrease Afib, Decrease clots
which drug is MOST effective at lowering LDL and Total Cholesterol?
atorvastatin (Lipitor)
Which drug do we give to diabetics even when their LDL is normal b/c it is so effective at prevnting CV events?
atorvastatin (Lipitor)
How does atorvastatin (Lipitor) fxn?
- Inhibit cholesterol synthesis in the liver
- Stimulate hepatocytes to produce more LDL receptors
- LDL receptors remove the LDL from the blood
What time of day should atorvastatin (Lipitor) be given?
night time!
That is when we make most of our cholesterol
Common side effects of atorvastatin (Lipitor)?
-headache, rash, memory loss, GI disturbance
Rare but serious side effects of atorvastatin (Lipitor)?
- Hepatotoxicity (elevated LFT)
- Myopthathy/Rhabdomyolysis (elevated CK)
- Increase cataract occurence
Who is not taking atorvastatin (Lipitor)
- pregnant
2. liver disease
Drug drug interactions with atorvastatin (Lipitor)?
- CYP34A: grapefruit, azoles, erythromycin, amiodarone
- increase SE with other lipid lowering drugs
Prototype for Bile-Acid Sequestrants
colesevelam (Welchol)
how does colesevelam (Welchol) function?
- Biologically inert
- BIND to bile acids to form complexes that are excreted
- Since bile acids are made from cholesterol
- Liver makes more bile acids using LDL
- Increases LDL receptors to uptake more LDL
2 lipid lowering drugs that only work in GI tract?
colesevelam (Welchol)
Ezetimibe (Zetia)–> small intestine
Side effects of colesevelam (Welchol)
Bile-Acid Sequestrant
GI only !
-constipation, bloating, indigestion
How to administer colesevelam (Welchol)?
Bile-Acid Sequestrant
Administer with food + H20
Prototype for Cholesterol Absorption Inhibitor?
Ezetimibe (Zetia)
How does Ezetimibe (Zetia) fxn?
Cholesterol Absorption Inhibitor
- Blocks cholesterol absorption in the small intestine
- Also blocks cholesterol secreted in bile
*Works only in GI tract
3 lipid lowering drugs causing hepatotoxicity?
- atorvastatin (Lipitor) HMG-CoA Reductase Inhibitors aka “Statins”
- gemfibrozil (Lopid) Fibric Acid Derivatives (Fibrates)
- Ezetimibe (Zetia) Cholesterol Absorption Inhibitor
combining Ezetimibe (Zetia) with ______ will increase hepatotoxicity
statin!
Does Ezetimibe (Zetia) have side effects?
they are = to the placebo in trials
+ statin = hepatotoxicity
what is vytorin?
- ezetimibe (Zetia) ( Cholesterol Absorption Inhibitor)+ simvistatin (HMG-CoA Reductase Inhibitors)
- —>blocks from food + synthesis
prototype for Fibric Acid Derivatives (Fibrates)
gemfibrozil (Lopid)
how does gemfibrozil (Lopid) fxn?
accelerate the clearance of VLDLs
drug that is most effective for lowering Triglyceride levels and has little to no effect on LDL?
gemfibrozil (Lopid)
(Fibric Acid Derivatives (Fibrates))
side effects of gemfibrozil (Lopid) ?
Fibric Acid Derivatives (Fibrates)
- Rash and GI upset
- Increased risk of gallstones
- Myopathy
- Hepatotoxicity
2 drug drug interaction with gemfibrozil (Lopid) ?
Fibric Acid Derivatives (Fibrates)
Warfarin: Increase risk of bleeding
Statins: increased risk of rhabdo
prototype for Monoclonal Antibodies “mabs” -PCSK9 inhibitors ?
evolocumab (Repatha)
how does evolocumab (Repatha)fxn?
Monoclonal Antibodies “mabs” -PCSK9 inhibitors
- -binds to PCSK9 which blocks PCSK9 binding to LDL receptors.
- This increases LDL receptors, allowing LDL to bind to the receptors and be removed from the blood
This drug is used to treat familial hypercholesterolemia or Atherosclerotic heart problems who maxed out on statins.
Monoclonal Antibodies “mabs” -PCSK9 inhibitors
Prototype: evolocumab (Repatha)
What is the route for evolocumab (Repatha)
Monoclonal Antibodies “mabs” -PCSK9 inhibitors
Administered SQ , $450/month
Side effects of evolocumab (Repatha)
Monoclonal Antibodies “mabs” -PCSK9 inhibitors
injection site reactions, vasculitis, rash, urticaria. Antibody production can occur.
only lipid lowering drug that is subq?
Monoclonal Antibodies “mabs” -PCSK9 inhibitors
Prototype: evolocumab (Repatha)
3 other agents for lowering cholesterol
-Fish Oil
-Plant Sterols and Sterol Esters
Benecol and Promise brands
-Cholestin
=made from rice fermented with red yeast
this cholesterol lowering agent is made from rice fermented with red yeast
Cholestin
List the 5 categories of lipid lowering drugs?
- HMG-CoA Reductase Inhibitors aka “Statins”
- Bile-Acid Sequestrants
- Cholesterol Absorption Inhibitor
- Fibric Acid Derivatives (Fibrates)
- Monoclonal Antibodies “mabs” -PCSK9 inhibitors