Therapeutic Considerations

Question 1

What are the drugs of choice for lowering LDL?

Answer 1

-statins

Question 2

Which status are the most potent? Least potent?

Answer 2

• most potent = atrovastatin and rosuvastatin

- least potent = fluvastatin

Question 3

Which statins are metabolized by P450 3A4?

Answer 3

-lovastatin, simvastatin, and atorvastatin

Question 4

What do the inhibitors of P450 3A4 increase the risk of?

Answer 4

-myopathy

Question 5

Which statins are metabolized by a cytochrome P450 mediated pathway? (not P450 34A)

Answer 5

-fluvastatin and pitvastatin

Question 6

Which statins are not metabolized by cytochrome P450s? When should these drugs be considered?

Answer 6

• prvastatin and rosuvastatin

- they should be chosen for patients who are currently taking drugs that are metabolized by cytochrome P450s

Question 7

Which drugs can be used with statins to further lower LDL levels?

Answer 7

-bile acid sequestrants or cholesterol absorption inhibitors

Question 8

Which drug can be used with statins for treatment of high LDL and low HDL? What is a risk?

Answer 8

• niacin

- risk of myopathy when taken together

Question 9

Which drug decreases statin clearance and raises plasma concentration of statins? What is the risk?

Answer 9

• gemfibrozil

- risk of rhabdomyolysis

Question 10

What are the therapeutic effect of the inhibitors of bile acid absorption?

Answer 10

• lower LDL levels dose-dependently, increase HDL modestly

- also raise triglycerides (undesirable effect)

Question 11

What are the second-line agents for lipid reduction?

Answer 11

-inhibitors of bile acid absorption

Question 12

When are inhibitors of bile acid absorption used of statins?

Answer 12

-hyperlipidemia in young patients and in patients for whom statins alone do not provide sufficient LDL reduction

Question 13

What side effects limit patient adherence to treatment with inhibitors of bile acid absorption?

Answer 13

-significant bloating and dyspepsia

Question 14

Which class of drugs decreases the absorption of fat soluble drugs? What are the side effects?

Answer 14

• inhibitors of bile acid absorption

- bleeding may result due to vitamin K deficiency; bind certain drugs such as digoxin and warfarin

Question 15

Which side effect of ezetimibe partially offsets of the benefits of reduced cholesterol absorption? What should this drug be combined with to prevent this side effect?

Answer 15

• the inhibition of cholesterol causes a compensatory increase in hepatic cholesterol synthesis
• by combining a statin with ezetimibe, the compensatory increase in hepatic cholesterol synthesis is prevented

Question 16

Where is ezetimibe absorbed?

Answer 16

-it is absorbed by enterocytes and circulates enterohepatically

Question 17

Which drugs cause an increase in ezetimibe levels?

Answer 17

-cyclosporine and fibrates

Question 18

Ezetimibe can increase the plasma concentration of which drug?

Answer 18

-cyclosporine

Question 19

Which class of drugs are the drugs of choice for hypertriglyceridemia?

Answer 19

-fibrates

Question 20

What is an important risk of combining fib rates with statins?

Answer 20

-increased risk of myopathy

Question 21

Does fenofibrate or gemfibrozil have fewer GI and myopathy adverse effects?

Answer 21

-fenofibrate

Question 22

Fibrates increase the levels of which other drug?

Answer 22

-warfarin

Question 23

Which side effect of niacin limits its use? How can it be prevented?

Answer 23

-flushing occurs during the first few weeks of use and can be prevented by pretreatment with aspirin

Question 24

What are two major side effects of niacin, other than flushing?

Answer 24

• hyperuricemia my precipitate gout

- it is associated with impaired insulin sensitivity

Question 25

What is the prescription strength omega-3 fatty acid?

Answer 25

-Lovaza