Hyperlipidemia Pharm Flashcards
Statin MOA and effect
- Lovastatin, Fluvastatin, Simvastatin, Pravastatin,
- Atrovastatin, Rosuvastatin
Inhibit HMG-CoA Reductase, the rate limiting step in cholesterol synthesis
*leads to increased LDL receptor expression on hepatocytes, leading to a decrease in circulating LDL
Lovastatin, Fluvastatin, Simvastatin, Pravastatin decrease LDL-C in the _____-_____ range.
low-medium range
Atrovastatin, Rosuvastatin decrease LDL-C in the _____-_____ range.
medium-high range
Absolute contraindications for statins (2)
Liver disease, pregnancy
- relative contraindications are use with fibrates or niacin
- metabolized by CYP450 enzymes
Most common statin side effects (2)
myalgias (with normal CK), new onset DM
Which statin is not metabolized by the CYP450 system?
Pravastatin
Ezetimibe MOA and indication
Blocks cholesterol uptake by blocking the NPC1L1 transport protein in enterocytes and liver canaliculi
Indications:
- adjunct to statin therapy in high risk pts
- alternative if statins not tolerated
- homozygous sitosterolemia (rare dz where body stores plant sterols)
Evolocumab MOA
*same as alirocumab
anti-PCSK9 ab
*PSCK9 normally binds and tags LDL receptors for lysosomal destruction, blocking PSCK9 increases LDL receptor recycling and therefore increases LDL uptake by the liver
Bile acid sequesterant MOA
*Cholestyramine, Colesevelam
Binds bile acids, preventing reabsorption
- increases hepatic bile acid synthesis from cholesterol, leading to increased LDL receptor activity and LDL removal from the blood
- decreased coronary deaths in clinical trials
NIacin (vitamin B3) MOA
inibits hepatocyte diacylglycerol aceyltransferase-2, a key enzyme for TG synthesis
- lowers TG, LDL, increases HDL
- no longer recommended, no decrease in CVD mortality
Niacin adverse effects
Flushing, GI distress, hepatotoxicity, hyperglycemia, hyperuricemia
Fibrate drug effects and indication
Gemfibrozil, fenofibrate
(unknown MOA)
Fibrates primarily decrease serum TG levels
- ASCVD benefits not proven
- Primay indication is prevention of acute pancreatitis in those with very high TGs
Gemfizobril possible adverse effect when combined with statin
Risk of myopathy +/- rhabdomyolysis
- Fenofibrate does not have this risk!!!
- fibrates also increase risk of cholesterol gallstones (moreso with older ones)
Omega-3-acid Ethyl Esters (fish oil) effects
*Eicosapentaenoic acid (EPA) and Docosahexaenoic acid (DHA)
(unknown MOA)
Decreased hepatic production of VLDL
*decreased cardiovascular events!!!
Metabolic syndrome criteria (5)
*need 3/5 for diagnosis
- Elevated waist circumference
- Elevates TG
- Elevated fasting glucose
- HTN
- Reduced HDL