Week 7: Antilipidemics Flashcards
HMG CoA Reductase Inhibitors - “statins” (Atorvastatin/Rosuvastatin) MOA
- in liver, block synthesis of cholesterol by inhibiting the HMG CoA reductase activity
- best at lowering LDL
HMG CoA Reductase Inhibitors - drug interactions
grapefruit juice
HMG CoA reductase inhibitors cautions/ contraindications
- Pregnancy Category X
- Avoid in active liver disease (bc this works in liver)
- Avoid grapefruit juice with simvastatin, lovastatin and atorvastatin (can increase toxicity)
HMG CoA reductase inhibitors ADRs
- myalgias/myopathies (draw creatinine kinase to see severity of myalgia/arthalgia)– > increased CPK
- rhabdo/metabolic acidosis: headache, fatigue, abdominal pain
Statin Monitoring
- check lipid levels 4 to 6 weeks after starting therapy and then every 3 to 4 months until control is established
- baseline LFTs and then 3 to 6 months later only is suspected issues or underlying hepatic disease
- draw CK to see severity of myalgia/arthalgia
Niacin (Vitamin B3) MOA
- uncertain but appears to reduce VLDL synthesis - best at increasing HDL
- NOT recommended for hyperlipidemia
Niacin cautions/ contraindications
- avoid w/ hx of gout
- avoid w/ hepatic dysfunction
- avoid in uncontrolled diabetes (causes hyperglycemia)
- avoid w/ active peptic ulcers
- NO pregnancy
Niacin ADRs
- pruritis, flushing, hepatotoxicity (rare), rash, diarrhea
Niacin Pt education
- take anti-inflammatory strength NSAID/aspirin 30 minutes prior to dose to decrease ADRs (it increases prostaglandin activity which leads to flushing of head/neck and pruritis)
- non pharm to tx hyperlipidemia
Fibrates (Gemfibrozil/Fenofibrate) MOA
**best at decreasing triglyceride levels** For high trig usually > 400 (then once its 300, switch to statins)
- increases lipolysis of triglycerides via lipoprotein lipase –> decreases triglycerides, increase in HDL
Fibrates ADRs
- dyspepsia, abdominal pain
- cholelithiasis/gall stones
- increase transaminase, diarrhea
- increase in myalgia/arthralgia if combined with statins (DON’T combine)
Fibrates cautions/ contraindications
- avoid in liver or renal disease
- avoid in pre-existing gallbladder disease
- avoid in pregnancy and lactation
Bile Acid Sequestrants (Cholestyramine (Questran), cholestipol, colesevelam) MOA
- indirectly blocks absorption of cholesterol by forming a nonabsorbable complex (resin) with bile acids in the intestine/gut (to poop out LDL cholesterol)
- (those with liver disease can use this med but caution with other meds in gut that has narrow TI like digoxin and warfarin)
Bile Acid sequestrants ADRs
flatulence, bloating, abdominal pain, constipation
Bile Acid sequestrants cautions/ contraindications
- avoid in pts w/ elevated triglycerides >300 (can increase levels)
- safe in pregnancy and lactation
- avoid in pts with complete biliary obstruction
- must take other medications and vitamins either 1 hour before or 4 hours after this medication ( can impact drug/vitamin absoprtion)
ONLY ONE SAFE FOR PREGNANGY AND LACTATION
Cholesterol Absorption Inhibitors (Ezetimibe/Zetia) MOA
- directly blocks absorption of cholesterol across intestinal border
- leads to a decreased delivery of cholesterol to the liver, decreased hepatic cholesterol stores, and increased clearance of cholesterol from the bloodstream
- can safely be used with -statins
Ezetimibe/Zetia ADRs
- fatigue
- diarrhea (greasy/tarry stools)
- arthralgias/joint pain
- increased serum transaminases
Ezetimibe/Zetia cautions/contraindications
- avoid in liver dz
- avoid in pregnancy/lactation
PCSK9 (Evolocumab/Repatha) MOA
- subq injection $$$
- human monoclonal antibody that binds to PCSK9 and inhibits the binding of PCSK9 to LDL receptors = increase LDL receptors on cell surface, decreasing LDL in bloodstream
- 50 to 70% LDL reducation as monotherapy (can be used with statins)
Indication: for genetic disorder called familial homozygous hypercholesteremia causing their lipids to skyrocket
PCSK9 ADRs
- pain at injection site
- anaphyslaxis/hypersensitivity rxns
PCSK9/Repatha cautions/ contraindications
- avoid in pregnancy/lactation
Four Major Statin Benefit Groups
- Group 1: nave clinical ASCVD - use high intensity statin if = 75y/o - use moderate intensity statin is > 75 y/o
- Group 2: No ASCVD but have LDL-C levels >/= 190 - high intensity statin unless contraindication/unable to tolerate
Group 3: No ASCVD - age 40-75 w/ diabetes and LDL levels of 70-189 - moderate intensity statin if 10yr ASCVD risk is <7.5%; high intensity statin if 10yr ASCVD risk is > 7.5%
Group 4: NO ASCVD or DM; age 40-75 w/ LDL-C 70-189 and 10yr ASCVD risk >/= 7.5%- moderate intensity statin
