Lipid Lowering Flashcards
PCSK9 Inhibitors
Alirocumab and Evolocumab
PCSK9 Inhibitors MOA
Monoclonal Antibodies stop PCSK9 proteins; proteins cant bind to LDL anymore = more free LDL to be cleared from blood
PCSK9 Inhibitors ADRs
Injection site reactions Headache Arthralgia Myalgia Limb pain Fatigue
PCSK9 inhibitors target
targets LDL; familial hypercholesteremia
don’t use with statin
Fibric Acid Derivatives drugs
Gemfibrozil and Fenofibrate
Fibric Acid Derivatives MOA
Agonist at PPAR Alpha Receptor
Decreases VLDL synthesis in liver
Increased Lipolysis (breaks down TG)
Fibric Acid Derivatives ADRs
Myopathy (with statins) Increased LFTs Nausea GI upset Skin Rash
Fibric Acid Derivatives Contraindications
NO gemfibrizil and simvastatin because of additive myopathy effect
Fibric Acid Derivative Target
Used in patients with TG>500, very effective
Omega 3s
Fish Oil (OTC) Vascepa, Lovaza
Omega 3s MOA
Inhibition of TG secretion from the liver Promotes metabolism of TG
Omega 3s ADRs
Fishy taste, burping, Antiplatelet effects at high doses
Stop before surgery
HMG CoA Reductase Inhibitors
Rosuvastatin Atorvastatin Simvastatin Lovastatin Pravastatin Fluvastatin
HMG CoA Reductase Inhibitors MOA
Competitive inhibition of HMG CoA reductase to stop synthesis of cholesterol
Liver will up regulate LDL receptor to result
increased LDL uptake by liver (more cholesterol clearance)
Intensity of statins
High Intensity: atorvastatin (40-80mg) and rosuvastatin (20-40mg)
Moderate intensity: Atorvastatin (10-20mg), Rosuvastatin (5-10 mg), Simvastatin (20-40mg), Pravastatin (40-80mg), Lovastatin (40mg)
low intensity: fluvastatin (20-40mg)
HMG CoA Inhibitor ADRs
Teratogenic
Hepatic dysfunction (AST/ALT monitor)
Headache
Statins and Muscle Complications
Myalgia: pain (no variation in CPK)
Myopathy: weakness (slight CPK elevation)
Rhabdomyolysis: breakdown (high CPK)
Bile Acid Sequestrants
Cholestyramine
Colestipol
Colesevelam
Bile Acid Seq MOA
Bind to Bile acid in GI tract to increase excretion = less bile acid = use up more cholesterol to make bile acid = decrease LDL
Bile Acid Seq ADRs
Poorly tolerated (only for statin intolerant) GI effects: bloating, gas, constipation, abdominal pain, increased TG?
Bile Acid Seq Interactions
binds to many medications and makes meds ineffective
Give med 1 hour before or 4 hours after
Bile Acids and Pregnancy
Safe to use in pregnancy
Niacin
Vitamin B3
Niacin target
TGs; used in hypertriglyceridema, can possibly increase HDL and lower LDL
Niacin MOA
Decrease VLDL synthesis (targets endogenous cholesterol)
HDL is a byproduct of VLDL synthesis
Niacin ADRs
FLUSHING Pruritis Increased Uric Acid (gout) and or glucose Nausea Abdominal Discomfort Pregnancy Category X
Niacin interactions
For those who are potentially statin intolerant
Don’t combine with statins
Cholesterol Absorption Inhibitor
Ezetimibe
Ezetimibe target
LDL
Ezetimibe MOA
Stops absorption of cholesterol in the intestines
Less cholesterol= less chylomicrons=less serum LDL
Ezetimibe ADRs
Diarrhea
Arthralgia
Fatigue
Increased LFTs (with statins)
Ezetimibe contraindications
do not combine with bile acid sequestrants
Ezetimibe combinations
Use with statins
considered 2nd in line treatment (after statins)
