Antihyperlipidemics

Question 1

Statins

Answer 1

Competitive HMG-CoA reductase inhibitors
Mechanism: 👇🏽intracellular cholesterol = upregulation of LDL receptor
Action: 👆🏽clearing of LDL from blood so 👇🏽LDL and 👇🏽TAGs
*Category X (CI in pregnancy)

Question 2

Rosuvastatin

Answer 2

Most potent statin in lowering LDL

Question 3

Fluvastatin

Answer 3

Least potent statin

Question 4

Atorvastatin

Answer 4

Second most potent statin in lowering LDL

Question 5

Niacin

Answer 5

Inhibits adenylyl cyclase in adipocytes
MOA: inactivation of hormone-sensitive lipase
Effect: 👆🏽HDL, 👇🏽VLDL, 👇🏽LDL, 👇🏽Lp(a), 👇🏽plasma FFAs
Use: pt’s w/ combined hyperlipidemia and low HDL levels, effective in combo w/ satins

Question 6

Niacin SEs

Answer 6

Common SE: intense cutaneous flush (can administer aspirin prior to niacin to decrease flush), pruritis, rash, dry skin, acanthosis nigricans, nausea, abd pn
Severe SE: hepatotoxicity and hyperglycemia, elevated uric acid levels may precipitate gout
Rare SE: atrial arrhythmia, toxic amblyopia, toxic maculopathy

Question 7

Gemfibrozil / Fenofibrate

Answer 7

Peroxisome proliferator-activated receptor-α agonists (PPAR-α)
MOA: activation of PPAR-α induces lipoprotein lipase (promoting catabolism of VLDL)
Effect: 👇🏽TGs and 👆🏽HDL
SE: myositis (especially when combined with STATINS)
*Category C

Question 8

Cholestyramine / Colestipol / Colesevelam

Answer 8

Bile acid binding resins
MOA: bind to bile acids in intestinal lumen to prevent reabsorption by making an insoluble complex
Effect: upregulation of LDL receptors in liver so 👇🏽plasma LDL and 👆🏽HDL levels
Use: DOC for pregnant women and children
SE: GI sx’s d/t fat malabsorption (less with Colesevelam), may increase TG
CI: pt with hypertrygliceridemia

Question 9

Ezetimibe

Answer 9

Inhibits intestinal transport protein NPC1L1
MOA: impairs absorption of dietary and biliary cholesterol in the intestine which upregulates LDL receptors
Effect: 👇🏽LDL
Use: in combo with Statin to lower LDL levels
SE: rare cases liver damage
CI: bile acid sequestrants inhibit absorption of Ezetimibe

Question 10

EPA / DHA

Answer 10

MOA: reduce TG synthesis and increase FA oxidation in the liver
Effect: 👆🏽HDL

Question 11

Lovaza

Answer 11

Contains EPA and DHA
Use: adjunct to 👇🏽 TG levels
SE: may 👆🏽LDL when TG levels are high