(3) Blood & Inflammation: Dyslipidemia (2.1-2.3) Flashcards
How is dietary cholesterol sent to the liver?
(1) Converted to cholesterol esters
(2) Packaged in chylomicrons
Which apoliproteins do chylomicrons have?
A-E
(A, B, C, E)
What enzyme releases FFAs from chylomicrons and VLDLs?
LPL
(Lipoprotein Lipase)
What is the receptor and ligand for receptor-mediated endocytosis of chylomicrons?
Receptor: LDL receptor
Ligand: ApoE
What is the product of HMG-CoA reductase?
Mevalonate
What apolipoprotein is found on “bad cholesterol”?
ApoB100
What is the receptor and ligand for receptor-mediated endocytosis of LDL?
Receptor: LDL receptor
Ligand: ApoB100
(Also scavenger receptor)
What enzyme converts free cholesterol to cholesterol esters for transport by HDL?
LCAT
(Lecithin cholesterol acyltransferase)
What are two mechanisms HDLs transfer cholesterol to the liver?
(1) Deliver to LDLs via CETP
(2) Receptor-mediated endocytosis via SR-1
MOA: Statins
Inhibits HMG-CoA reductase
(↓ Intracellular Cholesterol ⇒ Upregulation of LDL receptors ⇒ ↑ Rate of peripheral cholesterol removal)
What part of the lipid fraction do statins reduce?
(1) ↓↓↓ LDL
(2) ↓ TGs
(3) ↑ HDL
What is the first-line treatment for hypercholesterolemia?
Lifestyle modification + statins
What is the most effective lipid-lowering drug to prevent future cardiovascular events?
Statins
Adverse Effects (3) : Statins
(1) Myopathy
(2) ↑ LFTs
(3) Teratogen
What is the only statin drug not metabolized by the CYP-450 system?
Pravastatin
(Primadonna-statin = Too good for CYP-450 system)
MOA: Bile acid resins
Inhibits bile acid reabsorption
(∴ ⇒ Stimulate HMG-CoA reductase & Upregulate LDL receptors)
What are two examples of bile acid resins?
(1) Cholestyramine
(2) Cholestipol
What effect do bile acid resins have on lipid fraction?
(1) ↓↓↓ LDL
(2) ↑ TGs
Why might bile acid resins cause colicky pain?
↑ Risk of gallstones
What type of vitamin deficiency can result from using bile acid resins?
Fat-soluble vitamin deficiency
(A, D, E, K)
What is the treatment protocol for administering bile acid resins with statins?
Administer > 4 hrs apart
MOA: Ezetimibe
Inhibits intestinal absorption of cholesterol
Adverse Effects (2) : Ezetimibe
(1) ↑ LFTs
(2) Diarrhea
MOA: Evolocamab
Inhibits PCSK9
(∴ Inhibits degradation of LDL receptors)
What are the possible fates of FFAs released by LPL?
(1) Used by muscle
(2) Coverted back to TG in adipose tissue
What are two examples of fibrate drugs?
(1) Gemfibrozil
(2) Fenofibrate
MOA: Fibrate drugs
Activate PPAR-α
(⇒ ↑ LPL ⇒ ↓ TG levels)
What effect do fibrates on the lipid fraction?
(1) ↓↓↓ TGs
(2) ↓ LDL
(3) ↑ HDL
* (↑ HDL by increasing ApoA1 and ApoA2)*
Adverse Effects (2) : Fibrates
(1) Myopathy
(2) Gallstones
Contraindication: Fibrates
Gallbladder disease
(↑ Risk of gallstones)
What is the most effective drug for increasing HDL levels?
Niacin
What effect does Niacin have on the lipid fraction?
(1) ↓ TGs
(2) ↓ LDL
(3) ↑↑↑ HDL
Adverse Effect: Niacin
Cutaneous flushing
What drug should be given prior to taking Niacin?
NSAID
Contraindications (3) : Niacin
(1) Liver disease
(2) Diabetics
(3) Gout
Fish oil is rich in what type of fatty acid?
ω-3 fatty acids
How does fish oil lower serum triglycerides?
(1) ↓ VLDL
(2) ↓ ApoB
