Hyperlipidemia Flashcards
First line tx for hyperlipidemia?
Lifestyle modification
What disease has an LDL receptor deficiency (due to gene mutation) leading to increased levels of LDLs?
Familiar hypercholesterolemia
Why do you chest cholesterol levels after pt has undergone weight loss and not during their weight loss?
B/c cholesterol levels are low during weight loss and stabilize for one month after
Lovastatin, Simivastatin, Atorvastatin are what dug class?
HMG-CoA Reductase inhibitors
-statins
MOA for Lovastatin, Simivastatin, Atorvastatin?
Inhibit HMG-CoA reductase to increase high affinity LDL receptors (more LDL into cells to reduce serum LDL levels)
DOC for lowering LDLs?
Statins (most effective when LDL is elevated)
Also lower TGs and increase HDL and stabilize plaques
What size dose of Atorvastatin do you give in high risk in atherosclerosis CVD pts?
High dose (stabilize plaques)
What two statin drugs are pro drugs?
Lovastatin and simvastatin
What drug class interacts w/ P450s-CYP3A4?
Statins
At what time of day should statins be taken?
Before bed (peak cholesterol synthesis at night)
What can Atorvastatin be taken at anytime of day?
Longer half life
What drug class increases serum levels of aminotransferase (LFTs)?
Stains (metabolized in liver)
May cause liver damage in pts w/ established liver disease or alcoholics
Myopathy, increased serum creatine kinase (due to exercise) and rhabdomyolysis are adverse effects of what drug class?
Statins
What two populations are statins contraindicated?
Pregnant, Active liver disease
Do P450 inhibitors increase or decrease plasma concentration of statins?
Increase
EX: grapefruit, ,macrolides, ketoconazole, ritonavir
Do P450 activators increase or decrease plasm concentration so statins?
Decrease
EX: Barbiturates, Rifampin, griseofulvin, phenytoin
Cholestyramine is what class of meds?
Bile acid binding resins
MOA for Cholestyramine?
Bind bile acids and prevent their intestinal reabsorption (increased LDL receptors –> increased LDL absorption –> decreased LDL levels
Does cholestyramine have any effect on homozygous familial hypercholesterolemia?
No
What makes Cholestyramine a safe drug?
It is not absorbed by the body.
Safe in pregnancy
When should cholestyramine be taken?
With meals b/c needs bile production to be effective
Most common side effects of Cholestyramine?
Bloating and constipation
Cholestyramine may impair the absorption of what drugs?
Acids or fat soluble drugs like: Digitalis, thiazides, statins, tetracylines, thyroxine, aspirin
What is the MOA for Niacin?
Lowers plasma VLDL and LDL by inhibiting VLDL secretion
Also inhibits hepatic cholesterolgenesis
Niacin is a combo of what?
nicotinic acid and Vit. B3
Will Niacin increase or decrease levels of HDL?
Increase (most effective agent to do so)
- Used in pts who can’t exercise
Cutaneous vasodilation, feeliing like “on fire” is a side effect of what drug?
Niacin
TX w/ prostaglandin aspirin beforehand
Why should Niacin be avoided in DM pts?
Impairs glucose tolerance
Gemfibrozil is what drug class?
Fibric acid derivative
MOA for Gemfibrozil?
Up regulates lipoprotein lipase activity (increases catabolism of VLDL) and turns on genes to involved in fatty acid oxidation via nuclear receptor
What does Gemofibrozil lower?
VLDLs, TGs, Cholesterol
DOC for hypertriglyceridemia?
Gemfibrozil (fibrates)
What meds will increase LFTs and incidence of cholelithiasis/gallstones?
Gemfibrozil (fibrates)
What class of drugs lowers LDLs the most?
Statins (HMG-CoA reductase inhibitors)
What drug blocks intestinal absorption of cholesterol?
Ezetimibe
What drug has no effect on CV endpoints?
Ezetimibe
Ezetimibe is often combinesdwith what drug for synergistic effects?
Statins
Ezetimibe can only be used in combo therapy
Alirocumab and Evolocumab are what drug class?
PCSK9 Inhibitors
MOA for Alirocumab and Evolocumab
Antibodies that inhibit PCSK9 from binding to LDL Receptor
PCSK9 binds to LDLR on hepatocyte surface –> LDLR degradation
How are Alirocumab and Evolocumab administered?
Monthly subQ injections
