Lipid lowering agents

Question 1

HMG-CoA reductase inhibitors (statins)

Answer 1

Lowers LDL significantly
Raises HDL
Lowers TGs

Inhibits HMG-CoA to mevalonate (cholesterol precursor)
Decreases mortality in CAD

Increase LDL-R density!

AE: Hepatotoxicity (check LFTs); myopathy (esp. with fibrates or niacin)

Question 2

Bile acid resins (cholestyramine, colestipol, colesevelam)

Answer 2

Lowers LDL significantly
Slightly raises HDL and TGs

Prevents intestinal resorption of BA; liver must make more cholesterol, mobilizing it from the periphery

AE: GI upset, decrease absorption of drugs and fat-soluble vitamins

Question 3

Ezetimibe

Answer 3

Decreases LDL
Increases HDL
Decrease TG

Prevent cholesterol abs. at brush border

AE: rarely increases LFTs and diarrhea

Question 4

Fibrates (gemfibrozil, bezafibrate, fenofibrate)

Answer 4

decrease LDL
increases HDL
Significantly lowers TG

Up-regulate LPL to increase TG clearance; Activates PPAR-alpha to induce HDL synthesis

AE: myopathy (increased risk with statins); cholesterol gallstones

Question 5

Niacin

Answer 5

decrease LDL
increase HDL
decrease TG

Inhibits lipolysis (HSL) in adipose tissue; reduces hepatic VLDL synthesis

AE: red, flushed face (reduces with time or NSAIDs)
Hyperglycemia, hyperuricemia

Question 6

PCSK9 inhibitors

Answer 6

Significantly decreases LDL
raises HDL
decreases TG

Inactivate LDL-R degradation, increases LDL removed from blood stream

AE: myalgias, delirium, dementia,