Lipid Drugs Flashcards
Why do people with familial hypercholesterolemia have such high LDL
They dont have (many) LDL receptors
What is the MOA of statins
Inhibiting HMG-CoA to increase LDL receptors = lower LDL
What is the most effective drug for lowering LDL
Statins
What are some of the other beneficial effects of statins?
Decrease CRP (anti-inflammation!)
Increase production of NO= vasodilation
Stabilize plaques
Decrease lipoprotein oxidation
Decreased platelet aggregation
Which two statins are considered Pro drugs and need to be hydrolyzed to be active
Lovastatin
Simvastatin
What time of day do statins need to be taken
Evening (due to the diurnal pattern of cholesterol synthesis)
What are the adverse effects of statin
Increased liver enzymes ***
Myopathy/muscle pain***
Increased CK with exercise***
Rhabdomyolysis***
Who can NOT have statins
Pregnant women*** cat X
Active liver disease*******
Use caution in alcoholics or hx of liver dz
What drugs/things inhibit p450 and will INCREASE the plasma concentrations (MORE TOXICITY) of statins?
Grapefruit juice***
Prob all you need to know but here are more:
Macrolides
Cyclosporine
Ketoconazole
Verapamil
Ritonavir
What drug will inhibit the metabolism of statins and cause increased toxicity?
Gemfibrozil (a fibrate!)
What happens if you wash your simvastatin down with a glass of grapefruit juice
Liver damage and rhabdomolysos
Name 3 resins
Cholestyramine (Questran)
Colestipol (Colestid)
Colesevelam (WelChol)
Why do patients hate taking bile acid-binding resins?
It has a sandy/gritty texture
What is the MOA of bile acid-binding resins
Binds bile acids and prevents their reabsorption
= liver makes more LDL receptors to increase uptake of LDL to make more bile
Who will not have any benefit from taking bile-acid resins?
Homozygous familial hypercholesterolemia -they don’t have functional LDL receptors
Will bile acid binding resins help lower triglycerides?
NO
When are bile acid binding resins effective?
When LDL is elevated
No effect on Triglycerides
Are Bile Acid Bindinf resins safe in preganncy?
Yes
What is the most common side effect of bile acid binding resins?
Constipation and bloating!
Bacteria get to feast on the lipids your bile should have been breaking down
What effect will bile acid resins have on patients taking warfarin
Hypoprothrombinemia due to vitamin K malabsorption (increased bleeding)
Although it just fucks with your absorption of everything so warfarin effects could also be decreased
What drugs will not be absorbed well if you take bile acid resins
Digitalis
Thiazides
Statins
Tetracycline
Thyroxine
Aspirin
What si the MOA of niacin (Nicotinic acid/B3)
Inhibits VLDL secretion (VLDL is the source of LDL)
What drug is the most effective at increasing HDL
Niacin
What are the main side effects of niacin
FLUSHING
Impairs glucose tolerance
How could you prevent the flushing from niacin?
Take aspirin before - flushing is dependent on prostaglandins
Name 3 fibrates
Gemfibrozil (Lopid)
Fenofibrate (TriCor)
Fenofibrate acid (Fibricor)
What lipid panel value will be lowered with fibrates
Triglycerides **
NOT LDL!!!! Might even RAISE LDL!
What is the MOA of fibrates
Increase LPL activity = VLDL broken down = Lower Triglycerides
What is the main side effect of fibrates
Gallstones!!**
30 yo woman with 2kids had high Triglycerides at her last checkup. She got a drug form the doctor and now complains that she has R-sided back pain especially after a fatty meal. What drug did she get
A fibrate (gave her gallstones)
What is the MOA of ezetimibe (Zetia)
Blocks intestinal absorption of cholesterol
What do you need to give Ezetemibe (Zetia) with for it to really do anything?
A statin
Synergistic!
What are the 2 PCSK9 inhibitors
Alirocumab (Praluent)
Evolocumab (Repatha)
Whaat is the MOA of PCSK9 inhibitors
Increases # of LDL receptors on the liver so LDL in blood drops
How are PCSK9 inhibitors given?
Monthly subcutaneous injections
What’s the big deal if you have high cholsterol
High= cardiovascular problems
SUPER high= pancreatitis
Best drug to lower LDL
Statins
Best drug to decrease triglycerides
Fibrates
