Lipid Lowering Drugs

Question 1

Which lipoprotein type contributes to atherosclerosis?

Answer 1

LDL (the most)

probably VLDL also

Question 2

Which lipoprotein type protects against atherosclerosis

Answer 2

HDL

Question 3

First line treatment for hypercholesterolemia

Answer 3

lifestyle measures

Question 4

which drug class for hypercholesterolemia results in the greatest decrease in LDL

Answer 4

monoclonal antibodies (but not widely used)

**HMG-CoA reductase inhibitors (statins)

Question 5

How do HMG-CoA reductase inhibitors work?

Answer 5

inhibit the enzyme HMG-CoA reductase = increased LDL receptors and increased LDL uptake
–> decreased free LDL

Question 6

Adverse effects of HMG-CoA reductase inhibitors

Answer 6

myopathies (can lead to rhabdomyolysis)
hepatotoxicity

Question 7

mechanism of action of bile acid sequestrants

Answer 7

remain in GI tract and bind up bile acids –> decreased absorption/increased excretion

Question 8

adverse effects of bile acid sequestrants

Answer 8

GI side effects (i.e. constipation)

Question 9

mechanism of action of fibrates

Answer 9

inhibit hepatic production of triglycerides - VLDL
(i.e. NOT LDL which holds cholesterol)

Question 10

adverse effects of fibrates?

Answer 10

GI disturbances
gallstones
myopathy
hepatotoxicity

Question 11

mechanism of action of ezetimibe

Answer 11

decreased dietary & biliary cholesterol absorption/reabsorption

Question 12

adverse effects of ezetimibe

Answer 12

myopathy/rhabdomyolysis
hepatitis
pancreatitis
thrombocytopenia

Question 13

mechanism of action of monoclonal antibody (PCSK) inhibitors

Answer 13

inhibit PCSK9
PCSK9 usually binds LDL receptors in liver

free LDL receptors = increased LDL uptake & less free LDL

Question 14

adverse effects of monoclonal antibody (PCSK9) inhibitors

Answer 14

hypersensitivity
immunogenicity

Question 15

mechanism of action of ACL inhbitors

Answer 15

inhibit ACL activity –> increased LDL receptor & increased uptake of LDL

Question 16

adverse effects of ACL inhibitors

Answer 16

increased uric acid (gout risk)
tendon rupture

Question 17

When & how should patients take their HMG-CoA Reductase inhibitor medication

Answer 17

at night, PO

Question 18

list some HMG-CoA Reductase inhibitors

Answer 18

“statins”

atorvastatin
lovastatin
simvastatin
rosuvastatin

Question 19

s/s of myopathy that can lead to rhabdo with statin administration

Answer 19

muscle aches
tenderness
weakness

Question 20

What is the risk if patient doesn’t call provider w/ myopathies?

Answer 20

progression to myositis with increased CK & K+
can lead to renal injury

Question 21

What labs do we monitor upon initial therapy with HMG-CoA reductase inhibitors?

Answer 21

CK

at start of therapy and again if symptomatic

Question 22

Name some bile acid sequestrants

Answer 22

colesevelam
cholestyramine
colestipol

Question 23

Name some fibric acid derivatives

Answer 23

gemfibrozil
fenofibrate
bezafibrate