L18: Hyperlipidsss Flashcards
Fibrates MOA
PPAR-alpha ligand: upregulates LDL and fatty acid oxidation genes
Best drug for increasing HDL
Niacin
How is ezetimibe therapy given?
only in combination with statins: synergistic
Niacin side effects
Nausea
Abdominal discomfort
Flush due to vasodilation
Impaired glucose tolerance
Severe hepatoxicity (rare)
Fibrates adverse effects
Gallstones
May increase LDL in combined hyperlipidemias
Inhibit statins (gemfibrozil)
Side effect: Myopathy and/or muscle pain (w/ increased serum creatine kinase)
Statins
MOA for HMG-CoA Reductase Inhibitors
Active forms are structural analogs of HMG-CoA reductase intermediate in mevalonate synthesis
Reduce plasma LDL by inhibiting the reductase to increase high-affinity LDL receptors
Drugs that don’t work for Homozygous familial hypercholesterolemia
Resins
b/c no functional LDL receptors to upregulate when bile acids are lost
In cases of rhabdomyolysis (statins)
Use osmotic diuresis to flush out?
Side effect: Rarely - rhabdomyolysis/myoglobinuria —> renal shutdown
Statins
Gemfibrozil (fibric acid derivative) drug interaction
Inhibits metabolism of statins
Most effective drug to lower LDL
Statins
Resins side effects
Constipation
Bloating
Floaty poops?
Ezetimibe MOA
Blocks intestinal absorption (zebra with diarrhea lol)
No decrease in CV endpoints (mortality)
PCSK9 MOA
Cause increased LDL degradation by inhibiting PCSK9 binding to LDLR on liver
-I guess PCSK9 binding on liver has an inhibitory effect on the LDLR? and more available LDLR means more LDL degradation
